This page shows what was measured, who it was measured in, and what that does not settle.
What Sitagliptin does in the body
Sitagliptin blocks that enzyme, so the hormones last longer and the pancreas responds more.
Your gut releases hormones after a meal that tell the pancreas to make insulin, and an enzyme in your bloodstream chops those hormones up within a couple of minutes. Because those hormones only act while blood sugar is high, the drug almost never pushes sugar too low.
Why people take it. Type 2 diabetes
What happened in people
A cardiovascular composite hazard ratio of 0.98 (0.88 to 1.09) in 14,671 patients over a median 3.0 years
✎ Source-linked record
Where this came from
A person wrote this into the record with the study named beside it. No reviewer has signed it off.
The recorded finding that sits closest to something a person would notice. Written into the record, not signed off, and it carries no population or interval.
That TECOS showed sitagliptin protects the heart — the design tested non-inferiority and the interval excludes any benefit above 12% relative
Where it acts
Endothelial cell surface and plasma, principally in the splanchnic circulation draining the gut
Kind of result
The kind of result is not recorded
Supervision
RNAWiki has not recorded a supervision or regulatory status for this substance.
What the registries record it as
Its recorded molecular formula is C16H15F6N5O•H3PO4, weighing 523.32.
US prescribing information · 62c4f58b-2b28-4825-aeb6-213ab9b7a026 · read 2026-08-30
Where each sentence above came from
A person wrote this explanation into the record, with the studies named in the path below.
The recorded use, written for a reader without medical training. Not signed off.
A limit recorded against this substance. Not signed off as a reviewed claim.
The four opening statements run to 87 words.
Words this page uses
Four words worth knowing first
Chosen from what this page shows, with each one explained before the word it depends on.
Stand-in result
A stand-in result is a number measured because the real result takes too long.
A picture of it, and where the picture fails
It is like judging a journey by the speedometer rather than by arriving.
Where that stops being true. Speed does predict arrival. Many stand-in results do not predict the real one.
What people get wrong. A stand-in result is often reported as the result itself.
A surrogate endpoint substituted for a clinical endpoint, valid only where the substitution has been shown to hold.
Randomisation
Randomisation means chance decides who gets which treatment.
A picture of it, and where the picture fails
It is like a coin toss deciding the groups.
Where that stops being true. A coin toss is fair once. Fairness here comes from doing it for everyone.
What people get wrong. It is thought to make groups identical. It makes them similar on average, including on things nobody measured.
Allocation of participants to arms by a chance process, so that unmeasured factors are balanced in expectation.
Confidence interval
A confidence interval is the range the true answer is likely to sit in.
A picture of it, and where the picture fails
It is like a weather forecast giving a range rather than one number.
Where that stops being true. A forecast range covers tomorrow. This one covers what the study could resolve.
What people get wrong. The middle number is read as the answer. A range crossing zero means no change is still possible.
An interval estimate that would contain the true parameter in a stated proportion of repeated studies.
Pathway
A pathway is a chain of steps inside a cell, each one setting off the next.
A picture of it, and where the picture fails
A pathway is like a row of dominoes.
Where that stops being true. Dominoes fall one way. Pathways loop back and can switch themselves off.
What people get wrong. Changing one step is read as changing the outcome. Other steps often absorb it.
An ordered series of molecular interactions producing a defined cellular change.
What happened in people◇Read from sources, not yet reviewed
What was measured, goal by goal
One row for each goal a registered study measured something for. One column for each kind of thing that could be measured.
Registered studies list 40 outcome measures that RNAWiki could read. A registered study says what someone planned to measure. It does not say what they found. 0 of the matched studies tested this substance, and 0 posted a result.
There is no single score. A strong test result and a weak life result are different facts.
Goals down the side, kinds of measurement across the top. Each cell says what kind of thing was registered, not what was found.
Goal
Life outcome
What a body can do
How a person feels
A test result
A step in the body
Harms
How long
Who was studied
Blood sugar
∅Nothing in the sources checkedNo registered study lists a life outcome for this goal.
∅Nothing in the sources checkedNo registered study lists a performance measure for this goal.
∅Nothing in the sources checkedNo registered study lists a symptom measure for this goal.
△Only a number moved14 registered test measure.
∅Nothing in the sources checkedNo registered study lists a body-step measure for this goal.
—Not recordedHarms were not a registered measure for this goal.
—Not recordedNo finished study window is recorded.
…Waiting for a reviewerWho was studied is listed further down the page.
Which registered measures put each goal on this table
Blood sugar
hba1c at week 24; hba1c at week 52; hba1c at week 12; hba1c at week 18; hba1c; effect of exenatide on postprandial glucose; change in hba1c from week 0 to week 16 endpoint; 24 hour weighted mean glucose
Sorted by fixed word lists, version v1. A name the rules do not recognise stays unsorted rather than moving to the nearest column.
What each mark on this table means
∅ Nothing in the sources checked
No registered study lists a life outcome for this goal.
△ Only a number moved
14 registered test measure.
— Not recorded
Harms were not a registered measure for this goal.
… Waiting for a reviewer
Who was studied is listed further down the page.
What happened in people◇Read from sources, not yet reviewed
What happened in people
Each card is one study: the exact question it asked, who was in it, and whether it showed what it set out to show.
Composite of cardiovascular death, non-fatal myocardial infarction, non-fatal stroke or hospitalisation for unstable angina
✓ The study showed what it set out to show
Who was studied
TECOS (NCT00790205)
How many people
14671
Study design
Randomised double-blind placebo-controlled cardiovascular safety trial, median 3.0 years
Compared against
A dummy treatment
Kind of result
Living longer, or avoiding a major event
What was found
HR 0.98 (95% CI 0.88-1.09); P < 0.001 for non-inferiority against a 1.3 margin. Not a superiority result.
Repeated elsewhere
Replicated
What this does not prove. Meeting one endpoint in one population does not carry to other goals or other people.
The limits of this study, and where it came from
Main limit. Acute pancreatitis gave p=0.07, a numerical imbalance that did not reach significance in a trial not powered for it.
How far it carries. This study is recorded from the curated record, not from the registry match.
Form and route. Oral tablet, and fixed combinations with metformin and with SGLT2 inhibitors
Interval reported. 95% CI 0
Written into the record, not signed off as a reviewed claim.
Composite of cardiovascular death, myocardial infarction or ischaemic stroke on saxagliptin
✓ The study showed what it set out to show
Who was studied
SAVOR-TIMI 53 (saxagliptin, NCT01107886)
How many people
16492
Study design
Randomised double-blind placebo-controlled trial, median 2.1 years
Compared against
A dummy treatment
Kind of result
Living longer, or avoiding a major event
What was found
HR 1.00 (95% CI 0.89-1.12); P = 0.99 for superiority, P < 0.001 for non-inferiority
Repeated elsewhere
Failed to Replicate
What this does not prove. Meeting one endpoint in one population does not carry to other goals or other people.
The limits of this study, and where it came from
Main limit. Hospitalisation for heart failure was 3.5% against 2.8%, HR 1.27 (1.07-1.51), p=0.007 — the class signal that TECOS then failed to reproduce for sitagliptin.
How far it carries. This study is recorded from the curated record, not from the registry match.
Form and route. Oral tablet, and fixed combinations with metformin and with SGLT2 inhibitors
Interval reported. 95% CI 0
Written into the record, not signed off as a reviewed claim.
RNAWiki holds 3 written-up human studies for this substance, each with the question it asked.
How we know it
Each card names the study, the number of people and what the study set out to measure.
What this does not prove
These summaries were written by a person and have not been signed off as reviewed claims.
Why it matters
A study that failed is as informative as one that worked, and both are here.
What we still do not know
No reviewed claim exists, so no exact population, effect size or interval is published yet.
What happened in people◇Read from sources, not yet reviewed
How close this is to real life
The top step is something a person would feel or care about. The bottom is a guess from software. Filled steps are where evidence exists for this substance.
□Living longer, or avoiding a major eventNo evidence recorded. Death, a heart attack, a stroke, a hospital stay.No registered study measures this.
□What a body can do day to dayNo evidence recorded. Walking, dressing, breathing, recovering.No registered study measures this.
□Measured performanceNo evidence recorded. How much was lifted, how far was run, how fast.No registered study measures this.
□Symptoms and quality of lifeNo evidence recorded. Pain, tiredness, mood, sleep, as the person rated it.No registered study measures this.
■A number that stands in for healthEvidence recorded. Cholesterol, blood sugar, bone density. A stand-in, not the thing itself.23 registered measures of this kind.
■A step measured inside a personEvidence recorded. Something measured in human tissue or human cells.A human record sits on the stored organism ladder.
■AnimalsEvidence recorded. Mice, rats, dogs. Useful for ideas, not proof about people.Stored records in Mouse. A result in animals says what to test next. It does not say what happens in people.
■Cells in a dishEvidence recorded. Cells or chemistry on a bench, far from a whole body.Stored mechanism abstracts describe steps measured in cells or tissue.
□A guess from softwareNo evidence recorded. Nobody measured it. RNAWiki never publishes one as a finding.RNAWiki stores no prediction for this record. Software can suggest a link. RNAWiki does not publish one as a finding.
Higher on these steps means closer to something a person would feel. It does not mean better done.
What it changes in the body◇Read from sources, not yet reviewed
The path through the body
From what a person takes to what changes. A solid line is a step measured in people. A dashed line is a step nobody has measured that way.
Where a source records it acting
Pancreas: By increasing and prolonging active incretin levels, sitagliptin increases insulin release and decreases glucagon levels; the label attributes these hormone effects to pancreatic beta and alpha cells
US prescribing information · cebc8388-c9db-4e27-8d6b-0d9bdc9d766d · read 2026-08-27
Start
Sitagliptin
What a person takes: Oral tablet, and fixed combinations with metformin and with SGLT2 inhibitors.
The measurement behind this step
Once daily, with or without food. Almost entirely renally cleared as unchanged drug, so exposure rises as kidney function falls and the label is written around estimated GFR. Its interaction profile is unusually clean because cytochrome metabolism is minimal.
Getting in
Absorbed almost completely and excreted almost unchanged
Nearly nine tenths of the tablet is absorbed, and the body barely alters it before the kidney gets rid of it.
╌╌Described, with no measurement named. No measurement is named for this step, so it is drawn as an unconfirmed link.
The measurement behind this step
Absolute oral bioavailability is about 87%, unaffected by food. Roughly 79% of a dose is excreted unchanged in urine, with minimal CYP3A4 and CYP2C8 metabolism, and renal elimination involves active tubular secretion by OAT3 and P-glycoprotein. The terminal half-life is about 12.4 hours, supporting once-daily dosing.
It meets its target on the surface of blood vessels, not inside a cell
The enzyme it blocks is anchored to the outside of cells lining blood vessels, with its business end facing the bloodstream. Nothing has to enter a cell.
╌╌Described, with no measurement named. No measurement is named for this step, so it is drawn as an unconfirmed link.
The measurement behind this step
DPP-4 is a type-II transmembrane serine exopeptidase, also known as CD26, expressed on endothelium, epithelium and lymphocytes, with a soluble circulating form as well. The physiologically decisive site is capillary endothelium in the splanchnic bed, where more than half of secreted GLP-1 is degraded before it reaches the systemic circulation.
A trifluorinated ring fills the pocket that normally grips the hormone
The drug slots into the enzyme's active site in the place where the end of the incretin hormone would sit, and holds there without being cut.
╌╌Described, with no measurement named. No measurement is named for this step, so it is drawn as an unconfirmed link.
The measurement behind this step
The 2,4,5-trifluorophenyl group occupies the S1 hydrophobic pocket, the primary amine of the beta-amino amide engages the S2 glutamate pair, and the trifluoromethyl-triazolopiperazine fills the adjacent lipophilic region. Inhibition is competitive and reversible, with more than 2,600-fold selectivity over DPP-8 and DPP-9 — the related peptidases whose inhibition was toxic in preclinical species.
Incretin hormones survive longer, and only act while glucose is high
Protected from destruction, the meal hormones circulate two to three times longer and keep telling the pancreas to release insulin — but only for as long as blood sugar stays up.
╌╌Described, with no measurement named. No measurement is named for this step, so it is drawn as an unconfirmed link.
The measurement behind this step
Intact GLP-1(7-36 amide) and GIP concentrations rise roughly two- to threefold. GLP-1 acts on beta-cell GLP-1 receptors to amplify glucose-stimulated insulin secretion through cyclic AMP and protein kinase A, and suppresses alpha-cell glucagon release. Both effects are glucose-dependent, which is why the drug produces almost no hypoglycaemia on its own.
HbA1c falls by a fraction of a point, and nothing else measurably changes
Blood sugar comes down modestly. In the trial that counted heart attacks, strokes and deaths across fifteen thousand people, there was no difference at all.
──Measured in people. Written by a person from the study named beside the step. Not signed off as a reviewed claim.
The measurement behind this step
In TECOS the on-treatment difference in glycated haemoglobin was -0.29 percentage points (95% CI -0.32 to -0.27) and the primary cardiovascular composite hazard ratio was 0.98 (0.88 to 1.09). In GRADE the drug had the highest rate of drifting above an HbA1c of 7.0% of the four arms, at 38.1 per 100 participant-years.
No suggested links are held for this record, so nothing is hidden from this path.
What we know
The record describes 5 steps from taking it to an effect in a person.
How we know it
Each step names the study behind it in the technical detail beside it.
What this does not prove
A change inside the body is a reason to look. It is not a result in a person.
Why it matters
A reader can see exactly where the chain stops being measured in people.
What we still do not know
No reviewed claim binds any of these steps to a named population.
What it would be like to take◇Read from sources, not yet reviewed
Felt, measured, or meaningful
Three different things that get called the same word. Registered studies measured all three, and mixing them is how a blood test becomes a health claim.
Felt
Things a person could notice without a test.
No registered study measured anything of this kind.
Measured
Things only a test, a scale or a device shows.
hba1c at week 24
hemoglobin a1c at week 24
hba1c at week 52
hba1c at week 12
hemoglobin a1c at week 18
hba1c at week 18
hba1c
hemoglobin a1c at week 12
effect of exenatide on postprandial glucose
change in hba1c from week 0 to week 16 endpoint
and 13 more.
Meaningful
Things that change how a life goes, not only a number.
No registered study measured anything of this kind.
A registered study says what someone planned to measure. It does not say what they found. A number moving is not the same as a life going better. The two are shown apart here.
Felt, but not shown to help. A person notices a change. No study showed it leads anywhere good.
Measured, but not felt. A number moves. The person notices nothing. Both can be true.
Measured, but not shown to matter. A number moves in the good direction. Nobody showed that lives went better.
Matters, but takes years. The result that counts may take longer than anyone would keep watching.
Names that fit none of the three (17)
a1c at week 24
safety
tolerability
who experienced one or more adverse events up to week 14
who experienced one or more ae up to week 54
who experienced one or more ae up to week 108
who experienced one or more ae up to week 160
who discontinued study treatment due to an ae up to week 12
who discontinued study treatment due to an ae up to week 52
who discontinued study treatment due to an ae up to week 106
who discontinued study treatment due to an ae up to week 158
gastric emptying rate
clinical adverse events
hypoglycemic events
map during placebo
glp 1 auec change from baseline at day 28
a1c at week 54
These are harms, study-process measures, or names the rules did not recognise. They are shown rather than dropped.
What it would be like to take◇Read from sources, not yet reviewed
How long anything takes
Nine different lengths of time that get confused with each other. None of them is worked out from another.
Before anything is noticed.RNAWiki does not store this separately, and never works it out from another figure on this page.
Before a test result moves.RNAWiki does not store this separately, and never works it out from another figure on this page.
Before performance moves.RNAWiki does not store this separately, and never works it out from another figure on this page.
How long the result was watched.No finished study window is recorded for a study that tested this substance.
How long people took it.How long people actually took it is not stored. The study window is not the same thing.
How long people were followed.Follow-up length is not stored separately. It is never read off the study window, which would be a different thing.
How fast the body clears it. 12.4 hours hours
Read from the label, which states: “Following a single oral 100-mg dose to healthy volunteers, mean plasma AUC of sitagliptin was 8.52 μM•hr, C max was 950 nM, and apparent terminal half-life (t 1/2 ) was 12.4 hours.”
How long effects linger.RNAWiki does not store this separately, and never works it out from another figure on this page.
Beyond the studies. Nothing is recorded about the long term.
The longest finished study sets the edge of what anyone measured.
A study window is not how long people took it, and neither is how long they were followed. Where RNAWiki holds only one of the three, it shows one.
What is missing or unclear◇Read from sources, not yet reviewed
Were people like you studied?
RNAWiki cannot tell whether a study fits you. It can show who was in it, and where the result stops carrying.
Who was studied
People similar to this profile were included.
Widely used as a second-line addition to metformin in type 2 diabetes, particularly where hypoglycaemia or weight gain is a concern. Generic sitagliptin entered the United States market in 2026.
Who is missing from the studies
Which groups were under-represented in the studies has not been recorded for this substance. Pregnancy, breastfeeding, children, older adults, and people with liver or kidney conditions are commonly excluded from trials; nothing here says whether they were.
What the label states about particular groups
On pediatric, the label states: “The safety and effectiveness of JANUVIA have not been established in pediatric patients.”
US prescribing information · 62c4f58b-2b28-4825-aeb6-213ab9b7a026 · read 2026-08-30
On older people, the label states: “Of the total number of subjects (N=3884) in pre-approval clinical safety and efficacy studies of JANUVIA, 725 patients were 65 years and over, while 61 patients were 75 years and over.”
US prescribing information · 62c4f58b-2b28-4825-aeb6-213ab9b7a026 · read 2026-08-30
On people who are pregnant, the label states: “Risk Summary The limited available data with JANUVIA in pregnant women are not sufficient to inform a drug-associated risk for major birth defects and miscarriage.”
US prescribing information · 62c4f58b-2b28-4825-aeb6-213ab9b7a026 · read 2026-08-30
On people who are breastfeeding, the label states: “Risk Summary There is no information regarding the presence of JANUVIA in human milk, the effects on the breastfed infant, or the effects on milk production.”
US prescribing information · 62c4f58b-2b28-4825-aeb6-213ab9b7a026 · read 2026-08-30
On people with reduced kidney function, the label states: “Sitagliptin is excreted by the kidney, and sitagliptin exposure is increased in patients with renal impairment.”
US prescribing information · 62c4f58b-2b28-4825-aeb6-213ab9b7a026 · read 2026-08-30
Where the result stopped carrying
GRADE: last of four add-ons on the primary metabolic endpoint, with the gap widening at higher baseline HbA1c
No cardiovascular benefit has ever been demonstrated for this drug, in the largest trial designed to look for one
SAVOR-TIMI 53 raised a heart failure signal for the class that led to labelling changes for two of its members
This is a scope explorer, not a diagnosis engine.
It shows who was studied so you can see whether people similar to you were included.
RNAWiki cannot tell whether a study fits you. It can show who was in it.
What it would be like to take◇Read from sources, not yet reviewed
Why it might seem to do nothing
A real effect and a noticed effect are different things. These are the recorded reasons the two come apart.
It was studied for a different goal
The studies measured something else entirely.
On this record: Some registered studies measured things that match no goal on this page.
It was studied in different people
The people in the studies were not much like the reader.
On this record: Which groups were under-represented in the studies has not been recorded for this substance. Pregnancy, breastfeeding, children, older adults, and people with liver or kidney conditions are commonly excluded from trials; nothing here says whether they were.
The evidence may simply be wrong
Small early studies often do not hold up.
On this record: RNAWiki has not yet published a reviewed conclusion for this use.
Other reasons RNAWiki checked and found nothing for (10)
A different form was studied
The studied form is not the form on the shelf. Nothing in this record points to this reason.
There was nothing to correct
Where a level is already normal, topping it up may change nothing. Nothing in this record points to this reason.
Something else had to happen too
In the studies it was paired with training, a diet or another treatment. Nothing in this record points to this reason.
The change is too small to feel
A real change can still sit below what a person notices. Nothing in this record points to this reason.
Day-to-day swing hides it
Sleep, food, stress and time of day move most numbers more than this would. Nothing in this record points to this reason.
Not enough time yet
The studies ran longer than the person has waited. Nothing in this record points to this reason.
It was not taken as studied
Missed days change the result, and studies count them. Nothing in this record points to this reason.
Something else changed at the same time
Two changes at once cannot be told apart afterwards. Nothing in this record points to this reason.
The product may not be what it says
Contents of a sold product are not always what the label states. Nothing in this record points to this reason.
No recorded reason
RNAWiki has nothing stored that would explain it. Nothing in this record points to this reason.
None of these is a reason to take more. Taking more is not a step this page ever suggests.
What it would be like to take◇Read from sources, not yet reviewed
What taking it involves
The recorded facts about getting hold of it and using it. Nothing here is a suggestion about what you should do.
How it is supplied
Prescription only
❝ Quoted from a source
Where this came from
Copied from a source RNAWiki stored, with the source named.
Read from the recorded approval status.
No source is stored against this line.
Form and route
Oral tablet, and fixed combinations with metformin and with SGLT2 inhibitors
✎ Source-linked record
Where this came from
A person wrote this into the record with the study named beside it. No reviewer has signed it off.
The form and route recorded on this substance.
No source is stored against this line.
Who oversees it
RNAWiki has not recorded a supervision or regulatory status for this substance.
❝ Quoted from a source
Where this came from
Copied from a source RNAWiki stored, with the source named.
No register row and no identity class settled the question.
No source is stored against this line.
What is in the pack
Once daily, with or without food. Almost entirely renally cleared as unchanged drug, so exposure rises as kidney function falls and the label is written around estimated GFR. Its interaction profile is unusually clean because cytochrome metabolism is minimal.
✎ Source-linked record
Where this came from
A person wrote this into the record with the study named beside it. No reviewer has signed it off.
Recorded notes on how this is sold and what that means for what is in the pack.
No source is stored against this line.
Where it is registered
Regulatory records are listed in the technical disclosure at the foot of this page.
# Counted from records
Where this came from
A count of rows RNAWiki holds. It describes our records, not your body.
Register entries are stored per jurisdiction and shown with their dates.
No source is stored against this line.
Why people stop
Not recorded.
∅ Nothing recorded
Where this came from
RNAWiki holds nothing here and says so rather than guessing.
No record of why people stopped taking it is stored for this substance.
No source is stored against this line.
What it would be like to take◇Read from sources, not yet reviewed
What can go wrong
Sorted by where each line came from. A regulator's label and a report somebody sent in are not the same kind of fact.
·Worth asking a clinician aboutWritten into the record from the studies named on this page
Very well tolerated: in TECOS there were no significant differences from placebo in any adverse event category examined, including heart failure hospitalisation. The class carries labelled warnings for acute pancreatitis, severe and disabling joint pain, and bullous pemphigoid. Hypoglycaemia is uncommon on its own but occurs when combined with a sulfonylurea or insulin. Dose depends on kidney function because clearance is renal.
Nobody counted how many people took this and were fine, so this cannot be turned into a rate.
These are reports people sent to a regulator. They do not show the medicine caused the reaction.
Nobody counted how many people took the medicine and reported nothing.
The same event can be reported more than once, and many reports are incomplete.
News coverage, lawsuits and new warnings change how often people report.
A count is not a rate and not a risk.
Sitagliptin appears in spontaneous reports to regulators. Across the 10 most-reported reaction terms, 4788 reaction mentions were counted. One report can name several reactions.
The recorded terms (10)
pancreatitis — 932 reaction mentions
blood glucose increased — 879 reaction mentions
hypoglycaemia — 857 reaction mentions
lactic acidosis — 416 reaction mentions
pancreatitis acute — 367 reaction mentions
diabetes mellitus inadequate control — 320 reaction mentions
open-targets-adr · recorded 2026-06-24 · a recorded source, not a stored snapshot
Over a long time. No completed tested study window is recorded, so long-term effects are not established by the registry record.
Groups the studies covered thinly. Which groups were under-represented in the studies has not been recorded for this substance. Pregnancy, breastfeeding, children, older adults, and people with liver or kidney conditions are commonly excluded from trials; nothing here says whether they were.
What is missing or unclear◇Read from sources, not yet reviewed
Does the exact form matter?
Evidence belongs to the exact thing that was tested. A different salt, a different mixture or a different preparation is a different question.
The form that was studied
Oral tablet, and fixed combinations with metformin and with SGLT2 inhibitors
✎ Source-linked record
Where this came from
A person wrote this into the record with the study named beside it. No reviewer has signed it off.
The form used in the studies cited on this page.
No source is stored against this line.
What is sold
Almost entirely renally cleared as unchanged drug, so exposure rises as kidney function falls and the label is written around estimated GFR. Its interaction profile is unusually clean because cytochrome metabolism is minimal.
✎ Source-linked record
Where this came from
A person wrote this into the record with the study named beside it. No reviewer has signed it off.
Recorded notes on which forms are sold and how they compare.
No source is stored against this line.
What is recorded as being sold
149 products list this as an active ingredient in the United States drug directory. 93 of them contain it and nothing else.
FDA National Drug Code directory · 84677-053 · read 2026-08-29
They are sold as poultice, powder, solution, tablet, tablet, film coated and tablet, film coated, extended release, taken oral.
FDA National Drug Code directory · 84677-053 · read 2026-08-29
The regulator's established pharmacologic class for it is dipeptidyl peptidase 4 inhibitor [epc] and dipeptidyl peptidase 4 inhibitors [moa].
FDA National Drug Code directory · 84677-053 · read 2026-08-29
35 published labels name it as an active ingredient. 18 of them describe this substance alone, which is where its own label text on this page comes from.
US prescribing information · 62c4f58b-2b28-4825-aeb6-213ab9b7a026 · read 2026-08-29
Those labels are classed as human prescription drug.
US prescribing information · 62c4f58b-2b28-4825-aeb6-213ab9b7a026 · read 2026-08-29
Sitagliptin Phosphate is tablets at Tablets: 100 mg, 50 mg, and 25 mg, recorded as prescription product; fda label in effect 2026-05-10 in the United States.
US prescribing information · cebc8388-c9db-4e27-8d6b-0d9bdc9d766d · read 2026-08-27
Recorded price in US: 3.46931–3.77084 USD per one unit as the pricing file counts it — a tablet, capsule, patch or single item, across 20 priced products whose strengths and pack forms differ, as of 2026-08-26, paid by retail pharmacies buying the product, as surveyed by the Centers for Medicare & Medicaid Services. It is not a list price, an insurance price, or what anyone pays at a counter..
Recorded source · 2026-08-26 · read 2026-08-28
Evidence carries across two names for one substance. It does not carry across a salt, a mirror form or a mixture.
What it would be like to take◇Read from sources, not yet reviewed
What you could measure
This one is decided with a clinician, so this section holds questions to ask rather than a plan to run.
RNAWiki could not confidently classify this substance, so no self-experiment plan is offered.
Questions worth asking
Which of the trials of Sitagliptin studied people like me?
What was measured, and for how long?
Was the result a laboratory value or a health outcome?
What would we watch for, and when would we stop?
Tracking can show whether something changed for you. It cannot show what caused it.
RNAWiki records evidence. It does not say whether this substance is right for you.
What is missing or unclear◇Read from sources, not yet reviewed
Claims that go past the evidence
Things said about this substance that sound reasonable, and the exact step that is missing between the evidence and the claim.
✗Goes past the evidence
That TECOS showed sitagliptin protects the heart — the design tested non-inferiority and the interval excludes any benefit above 12% relative
Why it sounds right. It follows from something real on this page: a body step, an animal result or a related finding.
The missing step. Nobody measured this in people for this use, or the study that did measure it did not show it.
What would change this
A study in people, for this exact use, measuring this exact thing, that a reviewer signs off.
RNAWiki has not yet published a reviewed conclusion for this use.
✗Goes past the evidence
That TECOS excluded pancreatitis and pancreatic cancer risk — events were too rare and follow-up too short for exclusion
Why it sounds right. It follows from something real on this page: a body step, an animal result or a related finding.
The missing step. Nobody measured this in people for this use, or the study that did measure it did not show it.
What would change this
A study in people, for this exact use, measuring this exact thing, that a reviewer signs off.
RNAWiki has not yet published a reviewed conclusion for this use.
✗Goes past the evidence
That the saxagliptin heart failure signal applies to sitagliptin — TECOS gave a hazard ratio of 1.00 in a larger, longer study
Why it sounds right. It follows from something real on this page: a body step, an animal result or a related finding.
The missing step. Nobody measured this in people for this use, or the study that did measure it did not show it.
What would change this
A study in people, for this exact use, measuring this exact thing, that a reviewer signs off.
RNAWiki has not yet published a reviewed conclusion for this use.
✗Goes past the evidence
That a smaller HbA1c reduction is unimportant because the drug is well tolerated — GRADE measured durability over five years and ranked it last of four
Why it sounds right. It follows from something real on this page: a body step, an animal result or a related finding.
The missing step. Nobody measured this in people for this use, or the study that did measure it did not show it.
What would change this
A study in people, for this exact use, measuring this exact thing, that a reviewer signs off.
RNAWiki has not yet published a reviewed conclusion for this use.
What is missing or unclear◇Read from sources, not yet reviewed
What nobody knows yet
Open questions, each with why it is open and what would close it.
Missing populations
Which groups were under-represented in the studies has not been recorded.
Why it matters. Recorded by the evidence model as a gap on this record.
What would answer it
A study that measures it, and a reviewer to sign it off.
Last checked 2026-09-04. Searched: The sources listed in the receipts at the foot of this page.
Missing long-term data
No completed tested study window is recorded.
Why it matters. Recorded by the evidence model as a gap on this record.
What would answer it
A study that measures it, and a reviewer to sign it off.
Last checked 2026-09-04. Searched: The sources listed in the receipts at the foot of this page.
No reviewed conclusion
RNAWiki has not yet published a reviewed conclusion for this use.
Why it matters. Recorded by the evidence model as a gap on this record.
What would answer it
A study that measures it, and a reviewer to sign it off.
Last checked 2026-09-04. Searched: The sources listed in the receipts at the foot of this page.
Missing interaction studies
No interaction was found in the registers checked. Not finding one is not the same as showing there is none.
Why it matters. Recorded by the evidence model as a gap on this record.
What would answer it
A study that measures it, and a reviewer to sign it off.
Last checked 2026-09-04. Searched: The sources listed in the receipts at the foot of this page.
Formulation uncertainty
Several salts, forms or products of Sitagliptin are recorded. Results from one form may not transfer to another.
Why it matters. Recorded by the evidence model as a gap on this record.
What would answer it
A study that measures it, and a reviewer to sign it off.
Last checked 2026-09-04. Searched: The sources listed in the receipts at the foot of this page.
Mechanism not reviewed
No reviewed mechanism story exists for this substance.
Why it matters. Recorded by the evidence model as a gap on this record.
What would answer it
A study that measures it, and a reviewer to sign it off.
Last checked 2026-09-04. Searched: The sources listed in the receipts at the foot of this page.
What happened in people◇Read from sources, not yet reviewed
Check any of this yourself
Every line above traced back to the study it came from. This is the technical layer, and the vocabulary changes here.
Every line above can be traced to the study named beside it. Follow the link and read it.
TECOS: cardiovascular safety demonstrated, with a hazard ratio of 0.98
In plain words
Nearly fifteen thousand people with type 2 diabetes and established heart disease took sitagliptin or placebo on top of usual care for three years. The number of cardiovascular events was the same in both groups.
What was measured
Composite of cardiovascular death, non-fatal myocardial infarction, non-fatal stroke or hospitalisation for unstable angina over a median 3.0 years
Effect estimate
No reviewed effect estimate exists for this record.
Limits
See the technical detail.
From the source
TECOS randomised 14,671 patients with type 2 diabetes and established cardiovascular disease to add sitagliptin or placebo to existing therapy, with open-label adjustment of other glucose-lowering drugs to reach individually appropriate targets in both arms. Over a median 3.0 years the difference in glycated haemoglobin was small (least-squares mean difference -0.29 percentage points, 95% CI -0.32 to -0.27). The primary composite of cardiovascular death, non-fatal myocardial infarction, non-fatal stroke or hospitalisation for unstable angina occurred in 839 patients on sitagliptin (11.4%, 4.06 per 100 person-years) and 851 on placebo (11.6%, 4.17 per 100 person-years): hazard ratio 0.98 (95% CI 0.88 to 1.09), meeting the prespecified non-inferiority margin of 1.3 at p<0.001. Hospitalisation for heart failure did not differ (hazard ratio 1.00, 0.83 to 1.20, p=0.98). Acute pancreatitis (p=0.07) and pancreatic cancer (p=0.32) did not differ significantly.
Written into the record, not signed off as a reviewed claim
A non-inferiority trial cannot show benefit, and TECOS is often cited as though it did
In plain words
TECOS was designed to prove the drug does not cause harm, using a statistical test that can only rule harm out. Its result is genuinely reassuring and is not evidence that the drug helps the heart.
What was measured
That TECOS showed sitagliptin protects the heart — the trial was powered and analysed to exclude harm, and its confidence interval excludes any benefit greater than 12% relative
Effect estimate
No reviewed effect estimate exists for this record.
Limits
See the technical detail.
From the source
TECOS used a relative risk of 1.3 as the marginal upper boundary for non-inferiority. The observed hazard ratio was 0.98 with a confidence interval from 0.88 to 1.09 — an interval centred on no effect and comfortably excluding the 1.3 harm boundary. That is a demonstration that sitagliptin does not increase major adverse cardiovascular events. It is not a demonstration of reduction, and the interval rules out any benefit larger than 12% relative. The trial was mandated by the regulatory framework created after the rosiglitazone controversy, whose purpose was safety exclusion. Contrast the design outcome with EMPA-REG OUTCOME, run under the same mandate, which crossed into superiority with p=0.04 and a 32% reduction in all-cause death.
Written into the record, not signed off as a reviewed claim
GRADE: last of four add-ons for keeping blood sugar at target
In plain words
Five thousand people already on metformin were randomised to one of four additional drugs and followed for five years. Sitagliptin was the least durable: more people on it drifted above target, and did so sooner.
What was measured
Cumulative incidence of confirmed HbA1c of 7.0% or higher over a mean 5.0 years, per 100 participant-years
Effect estimate
No reviewed effect estimate exists for this record.
Limits
This entry records a failure.
From the source
GRADE randomised 5,047 participants with type 2 diabetes of less than 10 years duration on metformin with HbA1c 6.8 to 8.5% to insulin glargine U-100, glimepiride, liraglutide or sitagliptin, and followed them a mean of 5.0 years. The cumulative incidence of the primary metabolic outcome — a confirmed HbA1c of 7.0% or higher — differed significantly across groups (p<0.001 for a global test). Rates per 100 participant-years were 26.5 for glargine, 26.1 for liraglutide, 30.4 for glimepiride and 38.1 for sitagliptin. The secondary outcome, confirmed HbA1c above 7.5%, paralleled it. Among participants with higher baseline HbA1c the advantage of the other three over sitagliptin appeared greater still. Severe hypoglycaemia was rare and most frequent on glimepiride (2.2%) against glargine (1.3%), liraglutide (1.0%) and sitagliptin (0.7%).
Written into the record, not signed off as a reviewed claim
The class heart failure signal belongs to saxagliptin, and TECOS did not reproduce it
In plain words
A trial of a related drug found more heart failure hospitalisations, which raised a question about the whole class. The sitagliptin trial specifically checked and found no difference at all.
What was measured
Hospitalisation for heart failure, saxagliptin versus placebo and sitagliptin versus placebo
Effect estimate
No reviewed effect estimate exists for this record.
Limits
See the technical detail.
From the source
SAVOR-TIMI 53 randomised 16,492 patients with type 2 diabetes to saxagliptin or placebo for a median 2.1 years. The primary composite of cardiovascular death, myocardial infarction or ischaemic stroke occurred in 7.3% against 7.2%: hazard ratio 1.00 (95% CI 0.89 to 1.12), p=0.99 for superiority and p<0.001 for non-inferiority. But hospitalisation for heart failure occurred in 3.5% against 2.8%: hazard ratio 1.27 (1.07 to 1.51), p=0.007. In TECOS the corresponding hazard ratio for sitagliptin was 1.00 (0.83 to 1.20), p=0.98, in a larger population followed longer. The two results together make the signal drug-specific rather than class-wide on the available evidence, which is what the sitagliptin label reflects.
Written into the record, not signed off as a reviewed claim
The pancreatitis and pancreatic cancer question was underpowered, not answered
In plain words
A long-running concern about this class is inflammation or cancer of the pancreas. TECOS found no significant difference, and the events were too rare for the trial to settle the question.
What was measured
That TECOS excluded a pancreatitis or pancreatic cancer risk — it detected no significant difference in events too rare, and follow-up too short, for exclusion
Effect estimate
No reviewed effect estimate exists for this record.
Limits
See the technical detail.
From the source
TECOS reported no significant between-group difference in acute pancreatitis (p=0.07) or pancreatic cancer (p=0.32) across 14,671 patients over a median 3.0 years. Both are low-frequency events, and a p-value of 0.07 for pancreatitis is a numerical imbalance that did not reach significance rather than a demonstration of equivalence — the trial was powered for a cardiovascular composite, not for these. A three-year median follow-up is also short relative to the latency usually assumed for a solid tumour. The accurate summary is that no signal was detected in a study with limited power to detect one.
Written into the record, not signed off as a reviewed claim
The glucose-dependence claim is real: 0.7% severe hypoglycaemia over five years
In plain words
Because the hormones this drug preserves only work when blood sugar is high, it hardly ever pushes sugar too low. In a five-year randomised comparison that was its clearest advantage.
What was measured
Proportion of participants with severe hypoglycaemia over a mean 5.0 years, by treatment arm
Effect estimate
No reviewed effect estimate exists for this record.
Limits
See the technical detail.
From the source
In GRADE, severe hypoglycaemia over a mean 5.0 years occurred in 0.7% of participants on sitagliptin, the lowest of the four arms, against 1.0% on liraglutide, 1.3% on insulin glargine and 2.2% on glimepiride — the difference from glimepiride being statistically significant. The mechanistic basis is that GLP-1 and GIP stimulate insulin secretion in a glucose-dependent manner and suppress glucagon only when glucose is elevated, so preserving them does not drive insulin release at normal glucose. This is the trade that defines the drug: the lowest hypoglycaemia rate of the four, and the weakest glycaemic durability of the four.
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What is not here
3 questions this page could not answer
These sections were prepared and left out because there was nothing to put in them. They are listed rather than hidden, so the gaps in this record are visible.
What it may clash with — found nothing in the sources checked.
Other ways to the same goal — found nothing in the sources checked.
What changed on this page — found nothing in the sources checked.
The record as stored
The full record, for auditing
Everything above is built from what is below. This layer keeps the technical vocabulary, record identifiers and every stored row, so a reader who wants to check the page can.
The older medicine-wide conclusion held in this record
Written for a clinical reader, and about the medicine as a whole rather than about one indication, population and set of trials. RNAWiki does not treat it as a programme conclusion and no reviewer has signed it off in that form. It is here word for word because it is what the record holds.
A well-tolerated glucose-lowering drug that produced a hazard ratio of 0.98 for major cardiovascular events across 14,671 patients with established cardiovascular disease — a demonstration of safety that is routinely and incorrectly read as a demonstration of benefit — and that ranked last of four add-ons for glycaemic durability in 5,047 participants followed a mean of five years.
Recorded evidence blocks (15)
Q1
What did Sitagliptin's largest trial (1499650 people) and its longest (11 years) measure?
1499650 people in Sitagliptin's largest registered study, 11 years in its longest registered window, measuring Area Under the Concentration-time Curve (AUC) From Time 0 to Infinity Following a Single Dose of Sitagliptin. ClinicalTrials.gov · 2026-09-01
126 phase3, 120 phase4, 70 phase2, 48 na, 48 phase1, 24 na or unstated, 2 early phase1; NCT00813228; 2019-11-26; no ageing endpoint recorded. Last human test completed 2026, NCT07567781.
Interpretation These counts include studies where Sitagliptin was a comparison treatment, a background treatment or an exposure in an observational study, and the longest window may be a planned end date. Trial roles have not yet been classified for this record.
Show the evidence
phase3
126
phase4
120
phase2
70
na
48
phase1
48
na or unstated
24
2 more recorded rows
early phase1
2
Last recorded human testNCT07567781
2026-07-21
recorded 2026-09-01 · last checked 2026-09-04
Q2
From mouse to human: where has Sitagliptin shown lifespan?
safety (2), accrual/recruitment (12), funding/business (6), sponsor decision unspecified (1) and other (11): Sitagliptin's stop wording, clustered. ClinicalTrials.gov · 2026-09-01
"inadequate recruitment"; 32 of 422 registered studies
Show the evidence
Trial
NCT00766441
terminated; "inadequate recruitment"
NCT00832624
terminated; "Business Reasons"
NCT00837759
terminated; "Changes to study personnel."
NCT00853944
terminated; "Sponsor withdrew funding du to lack of enrollment. Lack of enrollment was due to decrease in number of islet transplant procedures"
NCT00936663
terminated; "lack of funding"
NCT00939939
terminated; "Recruitment failure"
14 further recorded trials
NCT00947011
terminated; "PI left JHU"
NCT00958269
terminated; "Technical/operational issues"
NCT00967798
terminated; "Could not achieve target enrollment"
NCT01006018
terminated; "Unanticipated delays due to sterilization/stabilization testing of GLP-1."
NCT01257464
terminated; "Lack of recruitment"
NCT01260246
terminated; "Slow recruitment"
NCT01374568
terminated; "Study closed by sponsor. Funding ended."
NCT01477853
terminated; "The study was terminated early by the Sponsor for business reasons."
NCT01549964
terminated; "Due to concerns about potential liver safety (See Detailed Description)"
NCT01567540
terminated; "New treatments available, which prevents additional recruitment."
NCT01678820
terminated; "Merck terminated the study for business reasons in November 2013."
NCT01741103
withdrawn; "Study funding was for 1 year to a fellow who graduated in early stages of enrollment. While 6 patients were enrolled, many patients didn't finish the study and therefore little data was collected and no results will be entered."
NCT01834274
terminated; "Due to potential concerns about liver safety (See Detailed Description)"
NCT01970462
terminated; "Recruitment"
recorded 2026-09-01 · last checked 2026-09-04
Q4
Human studies of Sitagliptin used Comparator: MK0431 50 mg b.i.d. (b.i.d. = twice daily) — over how long?
Sitagliptin's half-life is 12.4 hours — which schedules were studied?
12.4 hours, the half-life Sitagliptin's label states. openfda-label · 58e23b30-451c-f451-e063-6394a90a35a7 · 2026-08-27
bioavailability approximately 87% %.
Show the evidence
half life
12.4 hours hours; Following a single oral 100-mg dose to healthy volunteers, mean plasma AUC of sitagliptin was 8.52 μM•hr, C max was 950 nM, and apparent terminal half-life (t 1/2 ) was 12.4 hours.
tmax
Absorption After oral administration of a 100 mg dose to healthy subjects, sitagliptin was rapidly absorbed with peak plasma concentrations (median T max ) occurring 1 to 4 hours postdose.
bioavailability
approximately 87% %; After oral administration of a 100 mg dose to healthy subjects, sitagliptin was rapidly absorbed with peak plasma concentrations (median T max ) occurring 1 to 4 hours postdose. The absolute bioavailability of sitagliptin is approximately 87%.
metabolism
Elimination Approximately 79% of sitagliptin is excreted unchanged in the urine with metabolism being a minor pathway of elimination.
recorded 2026-08-27 · last checked 2026-09-04
Q6
Could one person measure Sitagliptin's effect on hba1c at week 24?
Hba1c at week 24: measured in Sitagliptin's trials.
hba1c at week 24 is the recorded endpoint.
Show the evidence
biomarkers
hba1c at week 24; 2026-09-01
hemoglobin a1c at week 24; 2026-09-01
a1c at week 24; 2026-09-01
hba1c at week 52; 2026-09-01
hba1c at week 12; 2026-09-01
hemoglobin a1c at week 18; 2026-09-01
14 more recorded rows
biomarkers
hba1c at week 18; 2026-09-01
biomarkers
hba1c; 2026-09-01
biomarkers
safety; 2026-09-01
biomarkers
tolerability; 2026-09-01
biomarkers
hemoglobin a1c at week 12; 2026-09-01
biomarkers
effect of exenatide on postprandial glucose; 2026-09-01
biomarkers
who experienced one or more adverse events up to week 14; 2026-09-01
biomarkers
who experienced one or more ae up to week 54; 2026-09-01
biomarkers
who experienced one or more ae up to week 108; 2026-09-01
biomarkers
who experienced one or more ae up to week 160; 2026-09-01
biomarkers
who discontinued study treatment due to an ae up to week 12; 2026-09-01
biomarkers
who discontinued study treatment due to an ae up to week 52; 2026-09-01
biomarkers
who discontinued study treatment due to an ae up to week 106; 2026-09-01
biomarkers
who discontinued study treatment due to an ae up to week 158; 2026-09-01
Determination of the variability of HbA1c (by measurement of standard deviation of HbA1c) between the 2 diabetes treatment thresholds; Dipeptidyl peptidase 4 (DPP4); latest 2031-04-10
Show the evidence
Trial
NCT02879409
"HbA1c Variability in Type II Diabetes"; n 150; "Determination of the variability of HbA1c (by measurement of standard deviation of HbA1c) between the 2 diabetes treatment thresholds"; 2026-10-01
NCT04323189
"Effects of Sitagliptin in Individuals With Genetically Decreased DPP4"; n 20; "Dipeptidyl peptidase 4 (DPP4)"; 2026-02-28
NCT05195944
"Semaglutide vs Sitagliptin"; n 58; "Change in HbA1c level"; 2026-12
NCT05219409
"Effects of Sitagliptin in Relatives of T1D Patients"; n 70; "Rate of new diagnoses of Type 1 Diabetes Mellitus per year"; 2027-12
NCT05220917
"Comparative Effectiveness and Safety of Four Second Line Pharmacological Strategies in Type 2 Diabetes Study"; n 781430; "MACE"; 2027-09-30
NCT06246799
"Comparative Effectiveness of Two Initial Combination Therapies in Patients With Recent Onset Diabetes"; n 256; "number of subjects achieving HbA1c <6.5% at 6 months (Efficacy)"; 2029-06-30
13 further recorded trials
NCT06329882
"Doxycycline in Type II Diabetes"; n 60; "Change in glycemic profile"; 2026-04-20
NCT06587698
"Sitagliptin or BeiDouGen Capsule Improve the Pregnancy Outcome in Patients with PCOS"; n 300; "Clinical pregnancy rate"; 2029-07-01
NCT06851962
"Impact of Pharmacogenetic-Guided Treatment on Type 2 Diabetes."; n 504; "Comparison of HbA1c ≤7% goal at Week 24 between Pharmacogenetic-Guided and Standard Treatment in Type 2 Diabetes"; 2026-06-30
NCT07003542
"A Phase 2 and Pharmacodynamic Study of Sitagliptin in Patients With Progressive Grade 4 Gliomas"; n 48; "Difference in tumor CD8+ T cell count between the participants randomized to pre-surgical sitagliptin versus the participants randomized to no pre-surgical treatment."; 2028-06
NCT07108985
"Effect of Add-on SGLT2i, TZD, or Combination Therapy in Type 2 Diabetes Patients on DPP4 Inhibitors"; n 100; "change in HbA1c levels"; 2030-08-31
NCT07365592
"Neoadjuvant Chemotherapy, Anti-PD-1 Antibody and Sitagliptin for Locally Advanced pMMR CRC"; n 138; "Adverse events (AEs)"; 2029-12-31
NCT07374328
"Triple Hypoglycemic Regimens In Patients With Newly Diagnosed Type 2 Diabetes Mellitus"; n 240; "Diabetes remission rate"; 2026-08-31
NCT07390110
"Comparative Effectiveness of Oral Semaglutide vs Sitagliptin Among Individuals With Heart Failure With Preserved Ejection Fraction (STEP-HFpEF DM ORAL)"; n 25664; "Composite of worsening heart failure event (exacerbated symptoms of heart failure resulting in hospitalization, intravenous diuretic therapy in an urgent care setting) or all-cause mortality."; 2026-06-30
NCT07436663
"Comparative Study Between (SGLT-2i) and (DPP-4i) in the Prevention of DIC"; n 150; "Percentage of participants experiencing cardiotoxicity"; 2027-12-01
NCT07541781
"Sitagliptin in Recurrent/Progressive Grade 4 Glioma"; n 45; "Phase Ib: Dose-limiting toxicities as measured by CTCAE v5.0"; 2030-06-11
NCT07634380
"Sitagliptin With Pembro in RCC and Melanoma"; n 64; "Dose-Limiting Toxicities (DLTs)"; 2031-04-10
NCT07711171
"Efficacy and Safety of Canagliflozin in the Treatment of Type 2 Diabetes With Mild Cognitive Impairment"; n 60; "the changes in cerebral blood flow shown by fMRI"; 2026-10-30
NCT07717242
"Sun Yat-Sen Treatment Strategy for Enhancing Response in Muscle-invasive Bladder Cancer"; n 80; "Clinical Complete Response Rate"; 2029-01-31
recorded 2026-09-01 · last checked 2026-09-04
Q9
Which running trial of Sitagliptin could settle lifespan?
NCT07390110 measures Composite of worsening heart failure event (exacerbated symptoms of heart failure resulting in hospitalization, intravenous diuretic therapy in an urgent care setting) or all-cause mortality., reading out 2026-06-30.
1 open trial; n 25664; "Comparative Effectiveness of Oral Semaglutide vs Sitagliptin Among Individuals With Heart Failure With Preserved Ejection Fraction (STEP-HFpEF DM ORAL)"
Show the evidence
TrialNCT07390110
"Comparative Effectiveness of Oral Semaglutide vs Sitagliptin Among Individuals With Heart Failure With Preserved Ejection Fraction (STEP-HFpEF DM ORAL)"; n 25664; "Composite of worsening heart failure event (exacerbated symptoms of heart failure resulting in hospitalization, intravenous diuretic therapy in an urgent care setting) or all-cause mortality."; 2026-06-30
Q10
Which 122 trials of Sitagliptin posted no result?
Posted no result
122 of 122 completed trials
Registrations
NCT00696826, NCT00975052, NCT00481663, NCT00477581, NCT00961480 and NCT00642798, and 116 more
Completion dates
oldest 2004-05; newest 2024-04-30
Show the evidence
Trial
NCT00696826
2004-05
NCT00975052
2006-03
NCT00481663
2006-05-14
NCT00477581
2007-09
NCT00961480
2007-11
NCT00642798
2008-03
14 further recorded trials
NCT00760344
2008-03
NCT00971659
2008-11
NCT00842556
2009-05
NCT00425490
2009-07
NCT00871507
2009-07
NCT00968006
2010-01
NCT01054118
2010-02
NCT00978796
2010-03
NCT01104532
2010-03
NCT01095991
2010-05
NCT00901979
2010-06
NCT01035879
2010-08
NCT00747383
2010-09
NCT00976261
2010-09-05
Q11
At the median, Sitagliptin's trials enrolled 83 people — anything larger?
Median enrolment
83
Largest enrolment
1499650
Registered trials counted
422
Q12
What do 4788 spontaneous reports say about Sitagliptin — and not say?
These are reports people sent to a regulator. They do not show the medicine caused the reaction. Nobody counted how many people took the medicine and reported nothing. The same event can be reported more than once, and many reports are incomplete. News coverage, lawsuits and new warnings change how often people report. A count is not a rate and not a risk.
Sitagliptin appears in spontaneous reports to regulators. Across the 10 most-reported reaction terms, 4788 reaction mentions were counted: pancreatitis 932; blood glucose increased 879; hypoglycaemia 857; lactic acidosis 416. open-targets-adr · CHEMBL1201174 · 2026-06-24
Show the evidence
pancreatitis
932
blood glucose increased
879
hypoglycaemia
857
lactic acidosis
416
pancreatitis acute
367
diabetes mellitus inadequate control
320
4 more recorded rows
glycosylated haemoglobin increased
289
pancreatic carcinoma
264
hyperkalaemia
257
pemphigoid
207
recorded 2026-06-24 · last checked 2026-09-04
Q13
Sitagliptin and P-GP, CYP3A4 and CYP2C8: shared by which compounds?
P-GP, CYP3A4 and CYP2C8 appear in Sitagliptin's recorded interaction sentences, 3 in all. openfda-label+europepmc · 2026-08-30
Interpretation pharmacokinetics
Show the evidence
CYP2C8pharmacokinetics
In vitro studies indicated that the primary enzyme responsible for the limited metabolism of sitagliptin was CYP3A4, with contribution from CYP2C8.
CYP3A4
pharmacokinetics
In vitro studies indicated that the primary enzyme responsible for the limited metabolism of sitagliptin was CYP3A4, with contribution from CYP2C8.
pharmacokinetics
Drug Interaction Studies In Vitro Assessment of Drug Interactions Sitagliptin is not an inhibitor of CYP isozymes CYP3A4, 2C8, 2C9, 2D6, 1A2, 2C19 or 2B6, and is not an inducer of CYP3A4.
recorded 2026-08-30 · last checked 2026-09-04
Q14
Was Sitagliptin studied with fasting and exercise?
fasting and exercise are named in Sitagliptin's label sentences: "An open-label, randomized, single-dose, single-center, 2-sequence, 2-period, and cross-over phase 1 study was implemented to assess the pharmacokinetic bioequivalence of the test and reference formulations containing a single dose of sitagliptin 100 mg in 32 healthy volunteers under fasting…" openfda-label+europepmc · 2026-08-30
2 recorded statements; fasting, exercise
Show the evidence
fasting
An open-label, randomized, single-dose, single-center, 2-sequence, 2-period, and cross-over phase 1 study was implemented to assess the pharmacokinetic bioequivalence of the test and reference formulations containing a single dose of sitagliptin 100 mg in 32 healthy volunteers under fasting conditions.
exercise
As a pre-specified exploratory analysis, aimed at understanding the relevance of circulating lipid substrate availability in the effect of empagliflozin on cardiopulmonary function, we measured fasting plasma β-hydroxybutyrate (β(OH)B) and free fatty acids in 44 patients with T2D undergoing cardiopulmonary exercise tests (CPETs) before and after 6 months of randomised therapy with empagliflozin…
recorded 2026-08-30 · last checked 2026-09-04
Q15
What is recorded about Sitagliptin and autophagy?
"In vitro, sitagliptin (10-80 µM) and vildagliptin (5-40 µM) enhanced mitophagy and modulated autophagy pathway in neuronal cell lines." — where Sitagliptin and autophagy appear together. Europe PMC · pathway abstract search · 2026-03-16
"In vitro, sitagliptin (10-80 µM) and vildagliptin (5-40 µM) enhanced mitophagy and modulated autophagy pathway in neuronal cell lines."
"This study aims to evaluate the protective and autophagy induction properties of pterostilbene and sitagliptin on modulating the degree of atherosclerosis in rabbit models treated with an atherogenic diet."
AMPK
"Pterostilbene supplementation induced a significant reduction in tissue expression of PI3K and AKT, ( P <0.01), while sitagliptin induced significant increase in 5’ adenosine monophosphate-activated protein kinase (AMPK) levels, ( P <0.001)."
PMID 41752491
"Metformin, apart from the AMPK activation and its broad anti-inflammatory actions, has been indicated as a drug capable of influencing the synthesis of TRP metabolites, including the neuroprotective kynurenic acid (KYNA), whereas the effects of sitagliptin in this regard are not known."
PMID 40215713
"AMPK inhibitor treatment of rat BMSCs partially reversed these beneficial effects of sitagliptin on inflammation and osteogenesis."
mTORPMID 33453244
"Sitagliptin attenuated Cd-induced testicular injury via boosting the autophagy/apoptosis ratio through activation of AMPK/mTOR and Nrf2/HO-1 pathways."
autophagyPMID 33453244
"Sitagliptin attenuated Cd-induced testicular injury via boosting the autophagy/apoptosis ratio through activation of AMPK/mTOR and Nrf2/HO-1 pathways."
sirtuinPMID 37433152
"The objective of this study was to determine, whether sitagliptin, a DPP4 inhibitor, has effects on the expression of KAT7 and SIRT1 (genes encoding a histone acetyltransferase and a histone deacetylase, respectively) in MCF7 breast cancer cells, which play an essential role in modulating the epigenetic landscape of chromatin."
mTOR
PMID 37168300
"Sitagliptin medication slowed the development of atherosclerosis via increasing autophagy through suppression of the mTORC1 signaling pathway."
PMID 30123267
"This study indicates that sitagliptin significantly ameliorates the development of hepatic steatosis and insulin resistance in ob/ob mice by inhibiting inflammatory responses and activating autophagy via AMPK/mTOR signaling pathway."
sirtuin
PMID 30214535
"Furthermore, it was revealed that sitagliptin reactivated the HFD-suppressed SIRT1/AMPK axis pathway and upregulated its downstream target genes, modulating fatty acid metabolism."
PMID 31401381
"We hypothesized that sitagliptin could attenuate vascular inflammation via modulation of SIRT6 pathway."
recorded 2026-03-16 · last checked 2026-09-04
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