This page shows what was measured, who it was measured in, and what that does not settle.
What Linagliptin does in the body
Glycemic control
From the FDA-approved label: Linagliptin is an inhibitor of DPP-4, an enzyme that degrades the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). Thus, linagliptin increases the concentrations of active incretin hormones, stimulating the release of insulin in a glucose-dependent manner and decreasing the levels of glucagon in the circulation. Both incretin hormones are involved in the physiological regulation of glucose homeostasis. Incretin hormones are secreted at a low basal level throughout the day and levels rise immediately after meal intake.
What happened in people
RNAWiki has not yet published a reviewed conclusion for this use.
§ A fixed RNAWiki sentence
Where this came from
Wording RNAWiki always uses, not a finding about this substance.
No reviewed claim names a result for any goal on this record.
No source is stored against this line.
The limit that matters most
Not recorded.
Where it acts
Not recorded.
Kind of result
No result is published, so no kind of result applies yet
Supervision
RNAWiki has not recorded a supervision or regulatory status for this substance.
What the registries record it as
The substance registry classes this as chemical.
FDA substance registry · 3X29ZEJ4R2 · read 2026-08-29
Its recorded molecular formula is C25H28N8O2, weighing 472.54 g/mol.
US prescribing information · b1da67d4-51e0-41b7-9fe1-7f38c0d1baa1 · read 2026-08-30
Where each sentence above came from
No recorded sentence describes the change this makes in a way that stands on its own. The page opens with what it is taken for instead, and the recorded explanation follows below.
Shown as the opening line on this page.
No statement of the main limit is recorded.
The four opening statements run to 98 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.
Enzyme
An enzyme is a protein that speeds up one chemical change.
A picture of it, and where the picture fails
An enzyme is like a machine on a production line doing one cut.
Where that stops being true. A machine is switched on and off by a person. Enzymes are controlled by the cell.
What people get wrong. Enzymes are thought to be used up. They are not; they work again and again.
A catalytic protein that lowers the activation energy of a specific reaction.
Receptor
A receptor is a part of a cell that a signal fits into.
A picture of it, and where the picture fails
A receptor is like a lock waiting for one key.
Where that stops being true. A lock either opens or does not. A receptor can be half-triggered, or worn out.
What people get wrong. Fitting a receptor is read as causing a benefit. It causes a step, and nothing more.
A protein that binds a specific ligand and converts that binding into a cellular response.
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 moved18 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 change from baseline at week 12; hba1c change from baseline at week 24; hba1c change from baseline at week 52; hba1c change from baseline at week 104; hba1c at week 12; hba1c at week 26; weighted mean glucose change from baseline at day 28; hba1c change from baseline at week 18
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
18 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.
Time to the First Occurrence of Any of the Following Adjudication-confirmed Components of the Primary Composite Endpoint 3-point Major Adverse Cardiovascular (CV) Events (3-point MACE): CV Death, Non-fatal Myocardial Infarction (MI) or Non-fatal Stroke.
✗ The study did not show it
Who was studied
NCT01897532
How many people
6991
Study design
Phase 4
Compared against
Not recorded for this study
Kind of result
Living longer, or avoiding a major event
What was found
Result not recorded on this page
Repeated elsewhere
Unreplicated
What this does not prove. A study that did not show an effect does not show that no effect exists anywhere.
The limits of this study, and where it came from
Main limit. No limitation is recorded for this study.
How far it carries. This study is recorded from the curated record, not from the registry match.
Form and route. Oral
Interval reported. Not recorded in this summary
Written into the record, not signed off as a reviewed claim.
openFDA Drugs@FDA · a recorded source, not a stored snapshot
openFDA NDC Directory · a recorded source, not a stored snapshot
openFDA SPL label · a recorded source, not a stored snapshot
PubChem PUG-REST · a recorded source, not a stored snapshot
The First 3-point Major Adverse Cardiovascular Events (3P-MACE)
✗ The study did not show it
Who was studied
NCT01243424
How many people
6103
Study design
Phase 3
Compared against
Not recorded for this study
Kind of result
A number that stands in for health
What was found
Result not recorded on this page
Repeated elsewhere
Unreplicated
What this does not prove. A study that did not show an effect does not show that no effect exists anywhere.
The limits of this study, and where it came from
Main limit. No limitation is recorded for this study.
How far it carries. This study is recorded from the curated record, not from the registry match.
Form and route. Oral
Interval reported. Not recorded in this summary
Written into the record, not signed off as a reviewed claim.
openFDA Drugs@FDA · a recorded source, not a stored snapshot
openFDA NDC Directory · a recorded source, not a stored snapshot
openFDA SPL label · a recorded source, not a stored snapshot
PubChem PUG-REST · a recorded source, not a stored snapshot
Frequency of Patients With Adverse Events (AEs)
✗ The study did not show it
Who was studied
NCT00736099
How many people
2122
Study design
Phase 3
Compared against
Not recorded for this study
Kind of result
A number that stands in for health
What was found
Result not recorded on this page
Repeated elsewhere
Unreplicated
What this does not prove. A study that did not show an effect does not show that no effect exists anywhere.
The limits of this study, and where it came from
Main limit. No limitation is recorded for this study.
How far it carries. This study is recorded from the curated record, not from the registry match.
Form and route. Oral
Interval reported. Not recorded in this summary
Written into the record, not signed off as a reviewed claim.
openFDA Drugs@FDA · a recorded source, not a stored snapshot
openFDA NDC Directory · a recorded source, not a stored snapshot
openFDA SPL label · a recorded source, not a stored snapshot
PubChem PUG-REST · a recorded source, not a stored snapshot
HbA1c Change From Baseline at Week 52
✗ The study did not show it
Who was studied
NCT00622284
How many people
1560
Study design
Phase 3
Compared against
Not recorded for this study
Kind of result
A number that stands in for health
What was found
Result not recorded on this page
Repeated elsewhere
Unreplicated
What this does not prove. A study that did not show an effect does not show that no effect exists anywhere.
The limits of this study, and where it came from
Main limit. No limitation is recorded for this study.
How far it carries. This study is recorded from the curated record, not from the registry match.
Form and route. Oral
Interval reported. Not recorded in this summary
Written into the record, not signed off as a reviewed claim.
openFDA Drugs@FDA · a recorded source, not a stored snapshot
openFDA NDC Directory · a recorded source, not a stored snapshot
openFDA SPL label · a recorded source, not a stored snapshot
PubChem PUG-REST · a recorded source, not a stored snapshot
Change From Baseline in Glycosylated Hemoglobin (HbA1c) for Metformin Background Patients
✗ The study did not show it
Who was studied
NCT01422876
How many people
1405
Study design
Phase 3
Compared against
Not recorded for this study
Kind of result
A number that stands in for health
What was found
Result not recorded on this page
Repeated elsewhere
Unreplicated
What this does not prove. A study that did not show an effect does not show that no effect exists anywhere.
The limits of this study, and where it came from
Main limit. No limitation is recorded for this study.
How far it carries. This study is recorded from the curated record, not from the registry match.
Form and route. Oral
Interval reported. Not recorded in this summary
Written into the record, not signed off as a reviewed claim.
openFDA Drugs@FDA · a recorded source, not a stored snapshot
openFDA NDC Directory · a recorded source, not a stored snapshot
openFDA SPL label · a recorded source, not a stored snapshot
PubChem PUG-REST · a recorded source, not a stored snapshot
Change From Baseline in HbA1c After 24 Weeks
✗ The study did not show it
Who was studied
NCT00954447
How many people
1263
Study design
Phase 3
Compared against
Not recorded for this study
Kind of result
A number that stands in for health
What was found
Result not recorded on this page
Repeated elsewhere
Unreplicated
What this does not prove. A study that did not show an effect does not show that no effect exists anywhere.
The limits of this study, and where it came from
Main limit. No limitation is recorded for this study.
How far it carries. This study is recorded from the curated record, not from the registry match.
Form and route. Oral
Interval reported. Not recorded in this summary
Written into the record, not signed off as a reviewed claim.
openFDA Drugs@FDA · a recorded source, not a stored snapshot
openFDA NDC Directory · a recorded source, not a stored snapshot
openFDA SPL label · a recorded source, not a stored snapshot
PubChem PUG-REST · a recorded source, not a stored snapshot
What we know
RNAWiki holds 6 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 eventEvidence recorded. Death, a heart attack, a stroke, a hospital stay.1 registered measure of this kind. 1 written-up study measured this and did not show a benefit.
□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.24 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 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 change from baseline at week 12
hba1c change from baseline at week 24
hba1c change from baseline at week 52
hba1c change from baseline at week 104
hba1c at week 12
hba1c at week 26
weighted mean glucose change from baseline at day 28
hba1c change from baseline at week 18
hba1c at week 18
hba1c after 24 weeks
and 14 more.
Meaningful
Things that change how a life goes, not only a number.
first 3 major adverse cardiovascular events
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 (15)
glp 1 auec change from baseline at day 28
incidence of adverse events
postprandial increase in intact proinsulin levels
fasting intact proinsulin levels
fasting lipids
postprandial lipids
fasting erythrocyte flexibility
postprandial erythrocyte flexibility
flow mediated vasodilation under fasted condition on day 28
frequency of adverse events and serious adverse events
cmax of metformin
left ventricular diastolic function
panss
metformin cmax
gastric evacuation velocity
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. 100 hours hours
Read from the label, which states: “Plasma concentrations of linagliptin decline in at least a biphasic manner with a long terminal half-life (>100 hours), related to the saturable binding of linagliptin to DPP-4.”
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.
TRADJENTA is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. TRADJENTA is a dipeptidyl peptidase-4 (DPP-4) inhibitor indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus ( 1 ) Limitations of Use • Not recommended in patients with type 1 diabetes mellitus as it would not be effective ( 1 ) •…
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 TRADJENTA have not been established in pediatric patients.”
US prescribing information · b1da67d4-51e0-41b7-9fe1-7f38c0d1baa1 · read 2026-08-30
On older people, the label states: “In linagliptin studies, 1,085 linagliptin-treated patients were 65 years of age and older and 131 patients were 75 years of age and older.”
US prescribing information · b1da67d4-51e0-41b7-9fe1-7f38c0d1baa1 · read 2026-08-30
On people who are pregnant, the label states: “Risk Summary The limited data with TRADJENTA use in pregnant women are not sufficient to inform of drug-associated risk for major birth defects and miscarriage.”
US prescribing information · b1da67d4-51e0-41b7-9fe1-7f38c0d1baa1 · read 2026-08-30
On people who are breastfeeding, the label states: “Risk Summary There is no information regarding the presence of linagliptin in human milk, the effects on the breastfed infant, or the effects on milk production.”
US prescribing information · b1da67d4-51e0-41b7-9fe1-7f38c0d1baa1 · read 2026-08-30
On people with reduced liver function, the label states: “No dose adjustment is recommended for patients with hepatic impairment [see Clinical Pharmacology (12.3) ] .”
US prescribing information · b1da67d4-51e0-41b7-9fe1-7f38c0d1baa1 · read 2026-08-30
On people with reduced kidney function, the label states: “No dosage adjustment is recommended for patients with renal impairment [see Clinical Pharmacology (12.3) ].”
US prescribing information · b1da67d4-51e0-41b7-9fe1-7f38c0d1baa1 · read 2026-08-30
Where the result stopped carrying
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
✎ 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
Sold as tablet, tablet, extended release, tablet, film coated, tablet, film coated, extended release, given by the oral route.
✎ 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∅Nothing found in the sources checked
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.
∅Nothing found in the sources checked
No harm is recorded against this substance in the sources RNAWiki checked. Finding nothing is not the same as showing there is nothing.
The sources listed were searched and held nothing. That is not the same as nothing existing.
Reports sent to a regulator
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.
Linagliptin appears in spontaneous reports to regulators. Across the 10 most-reported reaction terms, 1780 reaction mentions were counted. One report can name several reactions.
diabetes mellitus inadequate control — 53 reaction mentions
pancreatic carcinoma — 52 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
✎ 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
Not recorded.
∅ Nothing recorded
Where this came from
RNAWiki holds nothing here and says so rather than guessing.
Nothing further is recorded about which forms are sold.
No source is stored against this line.
What is recorded as being sold
40 products list this as an active ingredient in the United States drug directory. 23 of them contain it and nothing else.
FDA National Drug Code directory · 72205-407 · read 2026-08-29
They are sold as powder, tablet, tablet, extended release, tablet, film coated and tablet, film coated, extended release, taken oral.
FDA National Drug Code directory · 72205-407 · 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 · 72205-407 · read 2026-08-29
8 published labels name it as an active ingredient. 3 of them describe this substance alone, which is where its own label text on this page comes from.
US prescribing information · 5cff87ef-97f9-4e3c-9e06-fd257f3cb3fb · read 2026-08-29
Those labels are classed as human prescription drug.
US prescribing information · 5cff87ef-97f9-4e3c-9e06-fd257f3cb3fb · read 2026-08-29
Tradjenta is oral at 3 DOSAGE FORMS AND STRENGTHS Tablets: 5 mg, light red, round, biconvex, bevel-edged, film-coated tablets with "D5" debossed on one side and the Boehringer Ingelheim symbol debossed on the other side., recorded as fda label in effect 2024-01-22 in the United States.
US prescribing information · b1da67d4-51e0-41b7-9fe1-7f38c0d1baa1 · read 2026-08-30
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 Linagliptin 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
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 Linagliptin 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.
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Check any of this yourself
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3 documents were read for this substance.
RNAWiki source record
3 of them state the same halfLife, and they agree.
RNAWiki source record
3 of them state the same bioavailability, and they agree.
RNAWiki source record
3 of them state the same tMax, and they agree.
RNAWiki source record
3 of them state the same proteinBinding, and they agree.
RNAWiki source record
Where else this substance is registered
FDA substance identifier (UNII)
3X29ZEJ4R2
RxNorm concept
1100702
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How this medicine reached us
Kept near the foot of the page. A historical event moves up only when it changes something about this substance today.
What the approval register records
25 approved applications cover products containing this substance. The earliest was NDA201280, approved 20110502 to BOEHRINGER INGELHEIM.
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5 questions this page could not answer
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Recorded evidence blocks (14)
Q1
What did Linagliptin's largest trial (781430 people) and its longest (8.3 years) measure?
781430 people in Linagliptin's largest registered study, 8.3 years in its longest registered window, measuring Relative hazard of composite outcome of Stroke, MI, and Mortality. ClinicalTrials.gov · 2026-09-01
39 phase3, 36 phase1, 34 phase4, 11 na or unstated, 7 na, 6 phase2; NCT02041234; 2022-06; no ageing endpoint recorded. Last human test completed 2026, NCT05313529.
Interpretation These counts include studies where Linagliptin 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
39
phase1
36
phase4
34
na or unstated
11
na
7
phase2
6
1 more recorded row
Last recorded human testNCT05313529
2026-07-01
recorded 2026-09-01 · last checked 2026-09-04
Q2
From mouse to human: where has Linagliptin shown lifespan?
Linagliptin's half-life is 100 hours — which schedules were studied?
100 hours, the half-life Linagliptin's label states. openfda-label · dfe327e8-f6ab-41e5-bdef-d520118cd83a · 2026-08-30
bioavailability 30% %.
Show the evidence
half life
100 hours hours; Plasma concentrations of linagliptin decline in at least a biphasic manner with a long terminal half-life (>100 hours), related to the saturable binding of linagliptin to DPP-4.
tmax
After oral administration of a single 5 mg dose to healthy subjects, peak plasma concentrations of linagliptin occurred at approximately 1.5 hours post dose (T max ); the mean plasma area under the curve (AUC) was 139 nmol*h/L and maximum concentration (C max ) was 8.9 nmol/L. Plasma concentrations of linagliptin decline in at least a biphasic manner with a long terminal half-life (>100 hours),…
bioavailability
30% %; Absorption The absolute bioavailability of linagliptin is approximately 30%.
metabolism
Renal clearance at steady-state was approximately 70 mL/min. Metabolism Following oral administration, the majority (about 90%) of linagliptin is excreted unchanged, indicating that metabolism represents a minor elimination pathway.
recorded 2026-08-30 · last checked 2026-09-04
Q6
Could one person measure Linagliptin's effect on hba1c change from baseline at week 12?
Hba1c change from baseline at week 12: measured in Linagliptin's trials.
hba1c change from baseline at week 12 is the recorded endpoint.
Show the evidence
biomarkers
hba1c change from baseline at week 12; 2026-09-01
hba1c change from baseline at week 24; 2026-09-01
hba1c change from baseline at week 52; 2026-09-01
hba1c change from baseline at week 104; 2026-09-01
hba1c at week 12; 2026-09-01
hba1c at week 26; 2026-09-01
14 more recorded rows
biomarkers
weighted mean glucose change from baseline at day 28; 2026-09-01
biomarkers
glp 1 auec change from baseline at day 28; 2026-09-01
biomarkers
hba1c change from baseline at week 18; 2026-09-01
biomarkers
hba1c at week 18; 2026-09-01
biomarkers
hba1c after 24 weeks; 2026-09-01
biomarkers
hba1c change from baseline to week 12; 2026-09-01
biomarkers
hba1c after 30 weeks of treatment; 2026-09-01
biomarkers
incidence of adverse events; 2026-09-01
biomarkers
first 3 major adverse cardiovascular events; 2026-09-01
biomarkers
glycosylated hemoglobin for metformin background; 2026-09-01
biomarkers
glycosylated hemoglobin for treatment naive; 2026-09-01
biomarkers
postprandial increase in intact proinsulin levels; 2026-09-01
0; NCT02768220; PHASE4; the smallest recorded human enrolment at or below 30; the registry states no direction of its result; WITHDRAWN
Q7
Which of achieving hba1c of 6 without diabetic medication, blood pressure and cmax of metformin did Linagliptin's trials measure?
achieving hba1c of 6 without diabetic medication, blood pressure and cmax of metformin lead 40 outcome terms across Linagliptin's trials. ClinicalTrials.gov · 2026-09-01
hba1c change from baseline at week 104, hba1c at week 12, hba1c at week 26, weighted mean glucose change from baseline at day 28, glp 1 auec change from baseline at day 28 and hba1c change from baseline at week 18 follow.
Show the evidence
hba1c change from baseline at week 12
1
hba1c change from baseline at week 24
1
hba1c change from baseline at week 52
1
hba1c change from baseline at week 104
1
hba1c at week 12
1
hba1c at week 26
1
14 more recorded rows
weighted mean glucose change from baseline at day 28
1
glp 1 auec change from baseline at day 28
1
hba1c change from baseline at week 18
1
hba1c at week 18
1
hba1c after 24 weeks
1
hba1c change from baseline to week 12
1
hba1c after 30 weeks of treatment
1
incidence of adverse events
1
first 3 major adverse cardiovascular events
1
glycosylated hemoglobin for metformin background
1
glycosylated hemoglobin for treatment naive
1
postprandial increase in intact proinsulin levels
1
postprandial proinsulin/insulin
1
fasting intact proinsulin levels
1
recorded 2026-09-01 · last checked 2026-09-04
Q8
Which of Linagliptin's 5 ongoing trials reports first?
"Comparative Effectiveness and Safety of Four Second Line Pharmacological Strategies in Type 2 Diabetes Study"; n 781430; "MACE"; 2027-09-30
NCT05886088
"Efficacy and Safety of LID104 in the Treatment of Type II Diabetes Mellitus"; n 597; "Glycated hemoglobin (HbA1c)"; 2027-01
NCT06095492
"Effect of Empagliflozin vs Linagliptin on Glycemic Outcomes,Renal Outcomes & Body Composition in Renal Transplant Recipients With Diabetes Mellitus"; n 200; "Estimated glomerular filtration rate (eGFR)"; 2025-12-01
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
NCT07786571
"Study on Improving Blood Glucose Homeostasis With Dorzagliatin Tablets in the Treatment of Type 2 Diabetes Mellitus Patients With Moderate to Severe Chronic Renal Insufficiency"; n 206; "Change in Time in Range (TIR, 3.9-10.0 mmol/L) from baseline to Week 14"; 2029-07-01
recorded 2026-09-01 · last checked 2026-09-04
Q9
Which 23 trials of Linagliptin posted no result?
Posted no result
23 of 23 completed trials
Registrations
NCT01835678, NCT02376075, NCT01617824, NCT02212782, NCT02180334 and NCT02401880, and 17 more
Completion dates
oldest 2014-04; newest 2022-06
Show the evidence
Trial
NCT01835678
2014-04
NCT02376075
2014-09
NCT01617824
2014-12
NCT02212782
2015-01
NCT02180334
2015-04
NCT02401880
2015-12
14 further recorded trials
NCT02015299
2016-03
NCT01903070
2016-04
NCT02106104
2016-04
NCT02857946
2016-04
NCT02092597
2016-09
NCT02974504
2018-03
NCT02442817
2018-03-02
NCT02792400
2018-07
NCT03011177
2018-09
NCT03470454
2018-11-30
NCT03970668
2019-04-30
NCT03667300
2019-05-14
NCT02851745
2019-07-02
NCT03936036
2021-02-18
Q10
At the median, Linagliptin's trials enrolled 85 people — anything larger?
Median enrolment
85
Largest enrolment
781430
Registered trials counted
131
Q11
What do 1780 spontaneous reports say about Linagliptin — 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.
Linagliptin appears in spontaneous reports to regulators. Across the 10 most-reported reaction terms, 1780 reaction mentions were counted: pancreatitis 345; pemphigoid 293; hypoglycaemia 242; dermatitis bullous 222. open-targets-adr · CHEMBL237500 · 2026-06-24
Show the evidence
pancreatitis
345
pemphigoid
293
hypoglycaemia
242
dermatitis bullous
222
blood glucose increased
207
diabetic ketoacidosis
154
4 more recorded rows
pancreatitis acute
109
glycosylated haemoglobin increased
103
diabetes mellitus inadequate control
53
pancreatic carcinoma
52
recorded 2026-06-24 · last checked 2026-09-04
Q12
Linagliptin and P-GP, CYP3A4 and CYP1A2: shared by which compounds?
P-GP, CYP3A4 and CYP1A2 appear in Linagliptin's recorded interaction sentences, 6 in all. openfda-label+europepmc · 2026-08-30
Interpretation pharmacokinetics
Show the evidence
CYP1A2pharmacokinetics
Drug Interaction Studies In vitro Assessment of Drug Interactions Linagliptin is a weak to moderate inhibitor of CYP isozyme CYP3A4, but does not inhibit other CYP isozymes and is not an inducer of CYP isozymes, including CYP1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 4A11.
CYP2C8pharmacokinetics
In vivo studies indicated evidence of a low propensity for causing drug interactions with substrates of CYP3A4, CYP2C9, CYP2C8, P-gp and organic cationic transporter (OCT).
CYP2C9pharmacokinetics
In vivo studies indicated evidence of a low propensity for causing drug interactions with substrates of CYP3A4, CYP2C9, CYP2C8, P-gp and organic cationic transporter (OCT).
CYP3A4
pharmacokinetics
Drug Interaction Studies In vitro Assessment of Drug Interactions Linagliptin is a weak to moderate inhibitor of CYP isozyme CYP3A4, but does not inhibit other CYP isozymes and is not an inducer of CYP isozymes, including CYP1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 4A11.
pharmacokinetics
In vivo Assessment of Drug Interactions Strong inducers of CYP3A4 or P-gp (e.g., rifampin) decrease exposure to linagliptin to subtherapeutic and likely ineffective concentrations [see Drug Interactions (7) ].
pharmacokinetics
In vivo studies indicated evidence of a low propensity for causing drug interactions with substrates of CYP3A4, CYP2C9, CYP2C8, P-gp and organic cationic transporter (OCT).
recorded 2026-08-30 · last checked 2026-09-04
Q13
Was Linagliptin studied with fasting and exercise?
fasting and exercise are named in Linagliptin's label sentences: "Similarly, both sitagliptin 100 mg/day (MD, -15.16 mg/dL [95% CrI, -18.82, -11.55]; high confidence) and linagliptin 5 mg/day (-13.88 mg/dL [-17.54, -10.04]; moderate confidence) were significantly superior to placebo in reducing fasting plasma glucose." openfda-label+europepmc · 2026-08-30
2 recorded statements; fasting, exercise
Show the evidence
fasting
Similarly, both sitagliptin 100 mg/day (MD, -15.16 mg/dL [95% CrI, -18.82, -11.55]; high confidence) and linagliptin 5 mg/day (-13.88 mg/dL [-17.54, -10.04]; moderate confidence) were significantly superior to placebo in reducing fasting plasma glucose.
exercise
The present meta-analysis evaluated the efficacy and safety of empagliflozin + linagliptin combination compared with either monotherapy [n=6 randomized controlled trials; 2857 adults with type 2 diabetes (T2DM) on diet + exercise ± metformin; 39.7% women; mean age: 54.6-59.9 years].
recorded 2026-08-30 · last checked 2026-09-04
Q14
What is recorded about Linagliptin and AMPK?
"Linagliptin demonstrates potent cardioprotective effects against cisplatin-induced toxicity, primarily through modulation of the SIRT1/AMPK/Nrf2 signaling pathway, thereby resulting in reduced oxidative stress and inflammation." — where Linagliptin and AMPK appear together. Europe PMC · pathway abstract search · 2026-08-11
"Linagliptin demonstrates potent cardioprotective effects against cisplatin-induced toxicity, primarily through modulation of the SIRT1/AMPK/Nrf2 signaling pathway, thereby resulting in reduced oxidative stress and inflammation."
sirtuin
PMID 42578690
"Linagliptin demonstrates potent cardioprotective effects against cisplatin-induced toxicity, primarily through modulation of the SIRT1/AMPK/Nrf2 signaling pathway, thereby resulting in reduced oxidative stress and inflammation."
PMID 39642562
"Therefore, the present study reveals the ability of linagliptin, through the activation of SIRT1/Nrf2 signaling, to suppress NLRP3 inflammasome-mediated pyroptosis and protect against rotenone-induced parkinsonism."
mTORPMID 37630980
"In tandem, linagliptin activated hippocampal autophagy by lowering SQSTM-1/p62 accumulation, upregulating Beclin 1, and stimulating AMPK/mTOR pathway."
AMPKPMID 37630980
"In tandem, linagliptin activated hippocampal autophagy by lowering SQSTM-1/p62 accumulation, upregulating Beclin 1, and stimulating AMPK/mTOR pathway."
autophagy
PMID 37630980
"In tandem, linagliptin activated hippocampal autophagy by lowering SQSTM-1/p62 accumulation, upregulating Beclin 1, and stimulating AMPK/mTOR pathway."
PMID 40581165
"This study evaluated the effects of linagliptin on HCC cell lines, focusing on mechanisms involving reactive oxygen species (ROS) production, nuclear factor erythroid 2-related factor 2 (NRF2) pathway activation, and autophagy."
AMPKPMID 40221059
"It has been found that linagliptin, a dipeptidyl peptidase-4 inhibitor, activates AMPK in different disease conditions."
autophagyPMID 35890148
"Herein, the present study investigated targeting inflammation, apoptosis, and autophagy by linagliptin for potential modulation of cadmium-induced testicular dysfunction in rats."
mTORPMID 35122774
"In parallel linagliptin reduced mTOR levels and upregulated expression levels of SHP and MKP-1 which is postulated to mediate AMPK-driven JAK2/STAT3 inhibition."
sirtuinPMID 35122774
"Based on these findings, linagliptin showed promising anti-inflammatory activity against acetic acid-induced colitis that is mainly attributed to the activation of the AMPK-SIRT1-PGC-1α pathway as well as suppression of the JAK2/STAT3 signaling pathway that might be partly mediated through AMPK activation."
mTOR
"Moreover, we confirmed that the Akt/mammalian target of rapamycin (mTOR) pathway was involved in BLM-induced EndMT in vivo, which was suppressed by linagliptin."
IGF-1PMID 33105604
"Thus, linagliptin improved hepatic steatosis induced by IR and IGF1R inhibition via a previously unknown mechanism that did not involve gluconeogenesis, lipogenesis, or inflammation, suggesting the non-canonical actions of DPP-4 inhibitors in the treatment of hepatic steatosis under insulin-resistant conditions."
1 more recorded row
NAD+PMID 30369549
"Moreover, heme oxygenase-1 (HO-1) and NAD (P) H quinine oxidoreductase 1 (NQO1), two downstream targets of NRF2, were further up-regulated after linagliptin treatment compared with injury group."
recorded 2026-08-11 · last checked 2026-09-04
Where it is registeredIdentifiers, relations and other names
ChEMBL ATC CC BY-SA · ClinicalTrials.gov — US Government work · Europe PMC — metadata only, under the recorded legal gate · Open Targets 26.06 — CC0 · derived from this page's own recorded fields; no external licence · mixed register set; per-register licences in docs/specs/corpus-20k-sources.md · openFDA / DailyMed — US Government work
✗ required summary fields resolved: 5 required field(s) not terminal: Why people use it, Best-supported result, Most important common problem, Biggest unanswered question, Human evidence
✓ public claims reviewed: 0 reviewed claim(s); drafts are never rendered
✓ source coverage passed: 11 source rows
✓ no critical contamination: no quarantine open
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