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Selpercatinib

  • Prescription medicine
  • Prescription only
  • Identity checked
  • Sources last checked 2026-09-04

This page shows what was measured, who it was measured in, and what that does not settle.

What Selpercatinib does in the body

RETEVMO ® is a kinase inhibitor indicated for the treatment of: Adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) with a rearranged during transfection (RET) gene fusion, as detected by an FDA-approved test ( 1.1 )

From the FDA-approved label: Selpercatinib is a kinase inhibitor. 8 nM. In other enzyme assays, selpercatinib also inhibited FGFR 1, 2, and 3 at higher concentrations that were still clinically achievable. In cellular assays, selpercatinib inhibited RET at approximately 60-fold lower concentrations than FGFR1 and 2 and approximately 8-fold lower concentration than VEGFR3.

Why people take it. RETEVMO ® is a kinase inhibitor indicated for the treatment of: Adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) with a rearranged during transfection (RET) gene fusion, as detected by an FDA-approved test ( 1.1 )

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
Professional supervision is normally required. A regulator classifies this substance in a way that restricts how it is supplied.

What the registries record it as

  • The substance registry classes this as chemical.

    FDA substance registry · CEGM9YBNGD · read 2026-08-29

Where each sentence above came from

The use the label states, quoted from it. No plain-language version of this sentence has been written.

The use the label states, quoted from it. It is written for a clinician, not for a reader without medical training.

No statement of the main limit is recorded.

The four opening statements run to 140 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 peopleRead 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.

16 weeks clinical response

The study did not show it

Who was studied
NCT04817956
How many people
3000
Study design
Phase 2
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

Percentage of patients that are treated based on their molecular tumor profile

The study did not show it

Who was studied
NCT02925234
How many people
1550
Study design
Phase 2
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

Proportion of Pediatric Patients Whose Advanced Tumors Have Pathway Alterations That Can be Targeted by Select Anti-cancer Drugs

The study did not show it

Who was studied
NCT03155620
How many people
1377
Study design
Phase 2
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

Phase 1: Maximum Tolerated Dose (MTD)

The study did not show it

Who was studied
NCT03157128
How many people
857
Study design
Phase 1/Phase 2
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

Objective Response Rate(ORR)

The study did not show it

Who was studied
NCT06195228
How many people
800
Study design
Phase 4
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

OVERALL RESPONSE RATE (ORR)

The study did not show it

Who was studied
NCT04591431
How many people
400
Study design
Phase 2
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 peopleRead 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.

  1. Living longer, or avoiding a major event Evidence recorded. Death, a heart attack, a stroke, a hospital stay.4 registered measures of this kind. No reviewed result.
  2. What a body can do day to day No evidence recorded. Walking, dressing, breathing, recovering.No registered study measures this.
  3. Measured performance No evidence recorded. How much was lifted, how far was run, how fast.No registered study measures this.
  4. Symptoms and quality of life No evidence recorded. Pain, tiredness, mood, sleep, as the person rated it.No registered study measures this.
  5. A number that stands in for health Evidence recorded. Cholesterol, blood sugar, bone density. A stand-in, not the thing itself.3 registered measures of this kind.
  6. A step measured inside a person Evidence recorded. Something measured in human tissue or human cells.A human record sits on the stored organism ladder.
  7. Animals Evidence 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.
  8. Cells in a dish Evidence recorded. Cells or chemistry on a bench, far from a whole body.Stored mechanism abstracts describe steps measured in cells or tissue.
  9. A guess from software No 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 takeRead 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.

  • pharmacokinetics maximum concentration of dabigatran
  • pk maximum observed concentration of repaglinide
  • pharmacokinetics maximum concentration of rosuvastatin

Meaningful

Things that change how a life goes, not only a number.

  • event free survival
  • investigator assessed progression free survival
  • real world progression free survival
  • progression free survival

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 (14)
  • that are treated based on their molecular tumor profile
  • objective tumor response
  • stable disease
  • treatment related grade 3 and serious adverse events
  • phase 1 maximum tolerated dose
  • phase 1 recommended phase 2 dose
  • phase 1 number of dose limiting toxicities
  • objective response rate
  • overall response rate
  • tumor response
  • pk apparent volume of distribution
  • pk of auc0 inf extrapolated of repaglinide
  • radiographic response
  • pathologic response

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 takeRead 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.

  1. Before anything is noticed. RNAWiki does not store this separately, and never works it out from another figure on this page.

  2. Before a test result moves. RNAWiki does not store this separately, and never works it out from another figure on this page.

  3. Before performance moves. RNAWiki does not store this separately, and never works it out from another figure on this page.

  4. How long the result was watched. No finished study window is recorded for a study that tested this substance.

  5. How long people took it. How long people actually took it is not stored. The study window is not the same thing.

  6. 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.

  7. How fast the body clears it. 32 hours hours

    Read from the label, which states: “Elimination The apparent clearance (CL/F) of selpercatinib is 6 L/h in patients and the half-life is 32 hours following oral administration of RETEVMO in healthy subjects.”

  8. How long effects linger. RNAWiki does not store this separately, and never works it out from another figure on this page.

  9. 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 unclearRead 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.

  • RETEVMO ® is a kinase inhibitor indicated for the treatment of: Adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) with a rearranged during transfection (RET) gene fusion, as detected by an FDA-approved test ( 1.1 ) Adult and pediatric patients 2 years of age and older with advanced or metastatic medullary thyroid cancer (MTC) with a RET mutation, as detected by an FDA-approved…

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 RETEVMO have not been established in these indications in patients aged less than 2 years.”

    US prescribing information · 7fa848ba-a59c-4144-9f52-64d090f4d828 · read 2026-08-30

  • On older people, the label states: “Of 857 patients who received RETEVMO, 35% (298 patients) were ≥65 years of age and 10% (85 patients) were ≥75 years of age.”

    US prescribing information · 7fa848ba-a59c-4144-9f52-64d090f4d828 · read 2026-08-30

  • On people who are pregnant, the label states: “Risk Summary Based on findings from animal studies, and its mechanism of action [see Clinical Pharmacology ( 12.1 )] , RETEVMO can cause fetal harm when administered to a pregnant woman.”

    US prescribing information · 7fa848ba-a59c-4144-9f52-64d090f4d828 · read 2026-08-30

  • On people who are breastfeeding, the label states: “Risk Summary There are no data on the presence of selpercatinib or its metabolites in human milk or on their effects on the breastfed child or on milk production.”

    US prescribing information · 7fa848ba-a59c-4144-9f52-64d090f4d828 · read 2026-08-30

  • On people with reduced liver function, the label states: “Reduce the dose when administering RETEVMO to patients with severe [total bilirubin > 3 to 10 × upper limit of normal (ULN) and any AST] hepatic impairment [see Dosage and Administration ( 2.7 )] .”

    US prescribing information · 7fa848ba-a59c-4144-9f52-64d090f4d828 · read 2026-08-30

  • On people with reduced kidney function, the label states: “No dosage modification is recommended for patients with mild to severe renal impairment [estimated Glomerular Filtration Rate (eGFR) ≥15 to 89 mL/min, estimated by Modification of Diet in Renal Disease (MDRD) equation].”

    US prescribing information · 7fa848ba-a59c-4144-9f52-64d090f4d828 · 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 takeRead 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 takeRead 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

Professional supervision is normally required. A regulator classifies this substance in a way that restricts how it is supplied.

Quoted from a source

Where this came from

Copied from a source RNAWiki stored, with the source named.

Suppression classes recorded: S1, S3, S4.

No source is stored against this line.

What is in the pack

Sold as capsule, tablet, tablet, coated, 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 takeNothing 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.

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 unclearRead 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

  • 16 products list this as an active ingredient in the United States drug directory. 16 of them contain it and nothing else.

    FDA National Drug Code directory · 54893-0503 · read 2026-08-29

  • They are sold as capsule, powder and tablet, coated, taken oral.

    FDA National Drug Code directory · 54893-0503 · read 2026-08-29

  • The regulator's established pharmacologic class for it is breast cancer resistance protein inhibitors [moa], cytochrome p450 2c8 inhibitors [moa] and cytochrome p450 3a inhibitors [moa].

    FDA National Drug Code directory · 54893-0503 · read 2026-08-29

  • 1 published label names it as an active ingredient. 1 of them describe this substance alone, which is where its own label text on this page comes from.

    US prescribing information · 7fa848ba-a59c-4144-9f52-64d090f4d828 · read 2026-08-29

  • Those labels are classed as human prescription drug.

    US prescribing information · 7fa848ba-a59c-4144-9f52-64d090f4d828 · read 2026-08-29

  • RETEVMO is oral at 3 DOSAGE FORMS AND STRENGTHS Capsules: 40 mg: gray opaque capsule imprinted with “Lilly”, “3977” and “40 mg” in black ink. 80 mg: blue opaque capsule imprinted with “Lilly”, “2980” and “80 mg” in black ink., recorded as fda label in effect 2026-07-14 in the United States.

    US prescribing information · 7fa848ba-a59c-4144-9f52-64d090f4d828 · 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 takeRead 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.

Self-experiment planning is not offered for a prescription or clinician-supervised medicine. The questions below are for a clinician or pharmacist.

Questions worth asking

  • Which of the trials of Selpercatinib 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 unclearRead from sources, not yet reviewed

What nobody knows yet

Open questions, each with why it is open and what would close it.

How much did people take in the studies?

The sources RNAWiki checked hold nothing for this field.

Why it matters. A result belongs to an amount. Without the amount the result floats free.

What would answer it

A stored source that records 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 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 Selpercatinib 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 peopleRead 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.

Where else this substance is registered

FDA substance identifier (UNII)
CEGM9YBNGD
RxNorm concept
2370164

Checks this page had to pass

  • Passed

    Identity resolved

    no open identity hold

  • Passed

    No unresolved merge across substance families

    no quarantine open

  • Passed

    Every public sentence names a source

    The opening statement carries the origin: Quoted from a stored source.

  • Not passed

    Trial roles classified for highlighted evidence

    No registered study is classified as testing this substance.

  • Passed

    No internal keys in reader text

    enforced by the copy-contract test over the rendered page

  • Passed

    Safety mode resolved

    Suppression classes recorded: S1, S3, S4.

  • Passed

    Canonical metadata present

    slug and display name present

What is missing or unclearRead from sources, not yet reviewed

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

  • 2 approved applications cover products containing this substance. The earliest was NDA213246, approved 20200508 to ELI LILLY AND CO.

    Drugs@FDA application register · NDA213246 · read 2026-08-29

  • Marketing status on the register: prescription.

    Drugs@FDA application register · NDA213246 · read 2026-08-29

  • The earliest marketing start date recorded for a listed product is 20200508.

    FDA National Drug Code directory · 54893-0503 · read 2026-08-29

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Recorded evidence blocks (10)

What did Selpercatinib's largest trial (1550 people) and its longest (11 years) measure?


1550 people in Selpercatinib's largest registered study, 11 years in its longest registered window, measuring Pharmacokinetics (PK): Maximum Concentration (Cmax) of Dabigatran. ClinicalTrials.gov · 2026-09-01

17 phase1, 12 phase2, 4 na or unstated, 3 phase3, 1 early phase1, 1 phase4; NCT02925234; 2027-12; no ageing endpoint recorded. Last human test completed 2026, NCT07543887.

Interpretation These counts include studies where Selpercatinib 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
  • phase1
    17
  • phase2
    12
  • na or unstated
    4
  • phase3
    3
  • early phase1
    1
  • phase4
    1
1 more recorded row
  • Last recorded human test NCT07543887
    2026-04-04

recorded 2026-09-01 · last checked 2026-09-04

From mouse to human: where has Selpercatinib shown biomarker?


mouse: mechanism-only and human: biomarker (36): the rungs where Selpercatinib has a recorded finding. Europe PMC and ClinicalTrials.gov · organism ladder · 2026-09-01

Interpretation Pharmacokinetics (PK): Maximum Concentration (Cmax) of Dabigatran — the recorded outcome words.

Yeast C. elegans Drosophila Mouse mechanism-onlyRat Dog Non-human primate Human biomarker
Show the evidence
  • mouse
    mechanism-only
  • human NCT04782076
    biomarker; Pharmacokinetics (PK): Maximum Concentration (Cmax) of Dabigatran; 36

recorded 2026-09-01 · last checked 2026-09-04

Why did Selpercatinib's trial NCT05364645 stop?


1 recorded trial of Selpercatinib stopped. ClinicalTrials.gov · 2026-09-01

"lack of accrual"; 1 of 36 registered studies

Show the evidence
  • Trial NCT05364645
    withdrawn; "lack of accrual"

recorded 2026-09-01 · last checked 2026-09-04

Selpercatinib's half-life is 32 hours — which schedules were studied?


32 hours, the half-life Selpercatinib's label states. openfda-label · 7fa848ba-a59c-4144-9f52-64d090f4d828 · 2026-08-30

bioavailability 73% %.

Show the evidence
  • half life
    32 hours hours; Elimination The apparent clearance (CL/F) of selpercatinib is 6 L/h in patients and the half-life is 32 hours following oral administration of RETEVMO in healthy subjects.
  • tmax
    Mean steady-state selpercatinib [coefficient of variation (CV%)] C max was 2,980 (53%) ng/mL and AUC 0-24h was 51,600 (58%) ng*h/mL. Absorption The median t max of selpercatinib is 2 hours.
  • bioavailability
    73% %; The mean absolute bioavailability of RETEVMO capsules is 73% (60% to 82%) in healthy subjects.
  • metabolism
    Metabolism Selpercatinib is metabolized predominantly by CYP3A4.

recorded 2026-08-30 · last checked 2026-09-04

Which of event free survival, investigator assessed progression free survival and objective response rate did Selpercatinib's trials measure?


event free survival, investigator assessed progression free survival and objective response rate lead 21 outcome terms across Selpercatinib's trials. ClinicalTrials.gov · 2026-09-01

treatment related grade 3 and serious adverse events, phase 1 maximum tolerated dose, phase 1 recommended phase 2 dose, phase 1 number of dose limiting toxicities, objective response rate and overall response rate follow.

Show the evidence
  • that are treated based on their molecular tumor profile
    1
  • objective tumor response
    1
  • stable disease
    1
  • treatment related grade 3 and serious adverse events
    1
  • phase 1 maximum tolerated dose
    1
  • phase 1 recommended phase 2 dose
    1
14 more recorded rows
  • phase 1 number of dose limiting toxicities
    1
  • objective response rate
    1
  • overall response rate
    1
  • tumor response
    1
  • pharmacokinetics maximum concentration of dabigatran
    1
  • event free survival
    1
  • pk apparent volume of distribution
    1
  • investigator assessed progression free survival
    1
  • pk of auc0 inf extrapolated of repaglinide
    1
  • pk maximum observed concentration of repaglinide
    1
  • pharmacokinetics maximum concentration of rosuvastatin
    1
  • real world progression free survival
    1
  • radiographic response
    1
  • pathologic response
    1

recorded 2026-09-01 · last checked 2026-09-04

Which of Selpercatinib's 17 ongoing trials reports first?


17 registered trials of Selpercatinib are open; earliest completion 2025-05-06. ClinicalTrials.gov · 2026-09-01

Percentage of patients that are treated based on their molecular tumor profile; Proportion of Pediatric Patients Whose Advanced Tumors Have Pathway Alterations That Can be Targeted by Select Anti-cancer Drugs; latest 2030-06

Show the evidence

Trial

  • NCT02925234
    "The Drug Rediscovery Protocol (DRUP Trial)"; n 1550; "Percentage of patients that are treated based on their molecular tumor profile"; 2027-12
  • NCT03155620
    "Targeted Therapy Directed by Genetic Testing in Treating Pediatric Patients With Relapsed or Refractory Advanced Solid Tumors, Non-Hodgkin Lymphomas, or Histiocytic Disorders (The Pediatric MATCH Screening Trial)"; n 1377; "Proportion of Pediatric Patients Whose Advanced Tumors Have Pathway Alterations That Can be Targeted by Select Anti-cancer Drugs"; 2027-01-06
  • NCT03157128
    "A Study of Selpercatinib (LOXO-292) in Participants With Advanced Solid Tumors, RET Fusion-Positive Solid Tumors, and Medullary Thyroid Cancer (LIBRETTO-001)"; n 857; "Phase 1: Maximum Tolerated Dose (MTD)"; 2027-02
  • NCT03899792
    "A Study of Oral LOXO-292 (Selpercatinib) in Pediatric Participants With Advanced Solid or Primary Central Nervous System (CNS) Tumors"; n 36; "Phase 1: Number of Participants With Dose Limiting Toxicities (DLTs)"; 2029-05
  • NCT03944772
    "Phase 2 Platform Study in Patients With Advanced Non-Small Lung Cancer Who Progressed on First-Line Osimertinib Therapy (ORCHARD)"; n 247; "Objective response rate (ORR)"; 2025-05-06
  • NCT04194944
    "A Study of Selpercatinib (LY3527723) in Participants With Advanced or Metastatic RET Fusion-Positive Non-Small Cell Lung Cancer"; n 261; "Progression Free Survival (PFS) by Blinded Independent Central Review (BICR) (With Pembrolizumab)"; 2030-06
11 further recorded trials
  • NCT04211337
    "A Study of Selpercatinib (LY3527723) in Participants With RET-Mutant Medullary Thyroid Cancer"; n 291; "Progression Free Survival (PFS) by Blinded Independent Central Review (BICR)"; 2027-11
  • NCT04268550
    "Targeted Treatment for RET Fusion-Positive Advanced Non-Small Cell Lung Cancer (A LUNG-MAP Treatment Trial)"; n 124; "Response rate by blinded independent centralized review (BICR)"; 2026-12-01
  • NCT04280081
    "A Study of Selpercatinib (LY3527723) in Participants With Advanced Solid Tumors Including RET Fusion-positive Solid Tumors, Medullary Thyroid Cancer and Other Tumors With RET Activation"; n 77; "Primary Analysis Set: Overall Response Rate (ORR): Percentage of Participants With Complete Response (CR) or Partial Response (PR) as Assessed by Independent Review Committee (IRC)"; 2028-11
  • NCT04320888
    "Selpercatinib for the Treatment of Advanced Solid Tumors, Lymphomas, or Histiocytic Disorders With Activating RET Gene Alterations, a Pediatric MATCH Treatment Trial"; n 1; "Objective Response Rate (Complete Response + Partial Response) in Pediatric Patients Treated With Selpercatinib (LOXO-292)"; 2027-06-30
  • NCT04759911
    "Selpercatinib Before Surgery for the Treatment of RET-Altered Thyroid Cancer"; n 30; "Objective response rate (ORR)"; 2027-11-30
  • NCT04819100
    "A Study of Selpercatinib After Surgery or Radiation in Participants With Non-Small Cell Lung Cancer (NSCLC)"; n 152; "Event-Free Survival (EFS)"; 2028-05
  • NCT05668962
    "Restor. I-131 Upt. + Selpercatinib in RET F-P RAI-R TC"; n 30; "Objective Response Rate"; 2026-01-01
  • NCT06532149
    "ERectile Dysfunctions, gOnadotoxicity and Sexual Health Assessment in Men With Lung Cancer"; n 80; "Incidence of treatment-related sexual dysfuction in male patients with ANSCLC"; 2026-09-30
  • NCT07010393
    "Genotype-Driven Neoadjuvant Therapy for Locally Advanced Thyroid Cancer: A Real-World Cohort Study"; n 335; "Real-World Progression-Free Survival (rwPFS)"; 2028-12-31
  • NCT07146893
    "Feasibility Study for Repurposing RET Inhibitors"; n 7; "Mean (± SD) changes in body weight after 12 weeks"; 2028-02-23
  • NCT07419932
    "Response to Neoadjuvant Treatment in Locally Advanced Thyroid Cancer"; n 120; "Radiographic Response"; 2029-06-30

recorded 2026-09-01 · last checked 2026-09-04

Which running trial of Selpercatinib could settle lifespan?


NCT04211337 measures Progression Free Survival (PFS) by Blinded Independent Central Review (BICR), reading out 2027-11.

4 open trials; n 291; "A Study of Selpercatinib (LY3527723) in Participants With RET-Mutant Medullary Thyroid Cancer"

Show the evidence

Trial

  • NCT04211337
    "A Study of Selpercatinib (LY3527723) in Participants With RET-Mutant Medullary Thyroid Cancer"; n 291; "Progression Free Survival (PFS) by Blinded Independent Central Review (BICR)"; 2027-11
  • NCT04819100
    "A Study of Selpercatinib After Surgery or Radiation in Participants With Non-Small Cell Lung Cancer (NSCLC)"; n 152; "Event-Free Survival (EFS)"; 2028-05
  • NCT07010393
    "Genotype-Driven Neoadjuvant Therapy for Locally Advanced Thyroid Cancer: A Real-World Cohort Study"; n 335; "Real-World Progression-Free Survival (rwPFS)"; 2028-12-31
  • NCT04194944
    "A Study of Selpercatinib (LY3527723) in Participants With Advanced or Metastatic RET Fusion-Positive Non-Small Cell Lung Cancer"; n 261; "Progression Free Survival (PFS) by Blinded Independent Central Review (BICR) (With Pembrolizumab)"; 2030-06

At the median, Selpercatinib's trials enrolled 36 people — anything larger?


Median enrolment
36
Largest enrolment
1550
Registered trials counted
35

Selpercatinib and MATE1, P-GP and BCRP: shared by which compounds?


MATE1, P-GP and BCRP appear in Selpercatinib's recorded interaction sentences, 7 in all. openfda-label+europepmc · 2026-08-30

Interpretation pharmacokinetics

Show the evidence
  • CYP1A2 pharmacokinetics
    In Vitro Studies CYP Enzymes: Selpercatinib does not inhibit or induce CYP1A2, CYP2B6, CYP2C9, CYP2C19, or CYP2D6 at clinically relevant concentrations.
  • CYP2B6 pharmacokinetics
    In Vitro Studies CYP Enzymes: Selpercatinib does not inhibit or induce CYP1A2, CYP2B6, CYP2C9, CYP2C19, or CYP2D6 at clinically relevant concentrations.
  • CYP2C19 pharmacokinetics
    In Vitro Studies CYP Enzymes: Selpercatinib does not inhibit or induce CYP1A2, CYP2B6, CYP2C9, CYP2C19, or CYP2D6 at clinically relevant concentrations.
  • CYP2C8 pharmacokinetics
    CYP2C8 Substrates : Coadministration of RETEVMO with repaglinide (sensitive CYP2C8 substrate) increased the repaglinide AUC 0-INF 2.9-fold and C max 1.9-fold.
  • CYP2C9 pharmacokinetics
    In Vitro Studies CYP Enzymes: Selpercatinib does not inhibit or induce CYP1A2, CYP2B6, CYP2C9, CYP2C19, or CYP2D6 at clinically relevant concentrations.
  • CYP2D6 pharmacokinetics
    In Vitro Studies CYP Enzymes: Selpercatinib does not inhibit or induce CYP1A2, CYP2B6, CYP2C9, CYP2C19, or CYP2D6 at clinically relevant concentrations.
1 more recorded row
  • CYP3A4 pharmacokinetics
    Metabolism Selpercatinib is metabolized predominantly by CYP3A4.

recorded 2026-08-30 · last checked 2026-09-04

What is recorded about Selpercatinib and mTOR?


"Our results suggest the involvement of AKT-mTOR pathway activation in selpercatinib resistance in thyroid cancer and that inhibition of the AKT-mTOR pathway may have therapeutic potential to overcome selpercatinib resistance." — where Selpercatinib and mTOR appear together. Europe PMC · pathway abstract search · 2025-07-07

mTOR; PMID 40688508

Show the evidence
  • mTOR PMID 40688508
    "Our results suggest the involvement of AKT-mTOR pathway activation in selpercatinib resistance in thyroid cancer and that inhibition of the AKT-mTOR pathway may have therapeutic potential to overcome selpercatinib resistance."

recorded 2025-07-07 · last checked 2026-09-04

Where it is registered
Identifiers, relations and other names

The exact record

PubChem CID
155804485
CAS number
2152628-33-4
RxCUI
2370164
InChIKey
XIIOFHFUYBLOLW-ZRZAMGCNSA-N
Trade name
Retevmo, Retsevmo
Development code
LOXO-292, LY-3527723, LY3527723
Also called
RET INHIBITOR LOXO-292, SELPERCATINIB [JAN], SELPERCATINIB [MI], SELPERCATINIB [ORANGE BOOK], SELPERCATINIB [USAN], Selpercatinib [WHO-DD], selpercatinib [INN]
Sources (7)

Sources

  • ClinicalTrials.gov ClinicalTrials.gov API v2 snapshot 2026-09-01T09:00:05 ·
  • this record's own fields 2,3,5 ·
  • Europe PMC pathway abstract search ·
  • Europe PMC and ClinicalTrials.gov organism ladder ·
  • openfda-label 7fa848ba-a59c-4144-9f52-64d090f4d828 ·
  • openfda-label+europepmc K1:CEGM9YBNGD ·
1 more source

ClinicalTrials.gov — US Government work · Europe PMC — metadata only, under the recorded legal gate · 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

How these records are assembled · Which registers were checked

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