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Avutometinib

  • 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 Avutometinib does in the body

KRAS -mutated recurrent low-grade serous ovarian cancer (LGSOC) who have received prior systemic therapy

From the FDA-approved label: Avutometinib Avutometinib is a MEK1 inhibitor. Avutometinib induces the formation of inactive RAF/MEK complexes and prevents phosphorylation of MEK1/2 by RAF. RAF and MEK proteins are regulators of the RAS/RAF/MEK/ERK (MAPK) pathway. Avutometinib inhibited MEK1/2 and ERK1/2 phosphorylation and proliferation of tumor cell lines harboring KRAS mutations. Treatment of cancer cells with avutometinib increased the level of phosphorylated focal adhesion kinase (FAK). Defactinib Defactinib is an inhibitor of FAK and proline-rich tyrosine kinase-2 (Pyk2), the two members of the FAK family of nonreceptor tyrosine kinases.

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 · D0D4252V97 · read 2026-08-29

Where each sentence above came from

The recorded explanation is written in label language rather than for a beginner. 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 123 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.

Biomarker

A biomarker is a number from a test that stands in for something about health.

A picture of it, and where the picture fails

A biomarker is like a fuel gauge.

Where that stops being true. A gauge is wired to the tank. Many biomarkers are only loosely tied to health.

What people get wrong. A better number is read as a better life. Several medicines improved a number and helped nobody.

A measurable indicator used as a substitute for a clinical outcome of interest.

Placebo

A placebo is a dummy treatment given so the real one can be compared with it.

A picture of it, and where the picture fails

A placebo is like a blank control in an experiment.

Where that stops being true. A blank does nothing. People given a placebo often do get better.

What people get wrong. A placebo effect is read as imaginary. The improvement is measured and real.

An inactive intervention matched in appearance to the test intervention, used to control for non-specific effects.

Comparator

A comparator is whatever the treatment was measured against.

A picture of it, and where the picture fails

It is like the other runner in a race.

Where that stops being true. A race has one winner. A study can show both arms improved.

What people get wrong. Results are read without asking what the other group got. Beating nothing is not beating a treatment.

The control condition against which the experimental intervention is assessed.

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.

Progression Free Survival (PFS) per blinded independent central review (BICR)

The study did not show it

Who was studied
NCT06072781
How many people
270
Study design
Phase 3
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 SPL label · a recorded source, not a stored snapshot
  • PubChem PUG-REST · a recorded source, not a stored snapshot
  • FDA label (openFDA SPL) · a recorded source, not a stored snapshot

Part A: Determine optimal regimen of avutometinib (VS-6766) monotherapy or in combination with defactinib

The study did not show it

Who was studied
NCT04625270
How many people
225
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 SPL label · a recorded source, not a stored snapshot
  • PubChem PUG-REST · a recorded source, not a stored snapshot
  • FDA label (openFDA SPL) · a recorded source, not a stored snapshot

Phase 1b - To evaluate the safety and tolerability of investigational agent in patients with malignant brain tumours

The study did not show it

Who was studied
NCT06630260
How many people
182
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 SPL label · a recorded source, not a stored snapshot
  • PubChem PUG-REST · a recorded source, not a stored snapshot
  • FDA label (openFDA SPL) · a recorded source, not a stored snapshot

Part A: To determine RP2D for avutometinib in combination with sotorasib and the Alt-RP2D for avutometinib in combination with sotorasib and defactinib

The study did not show it

Who was studied
NCT05074810
How many people
153
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 SPL label · a recorded source, not a stored snapshot
  • PubChem PUG-REST · a recorded source, not a stored snapshot
  • FDA label (openFDA SPL) · a recorded source, not a stored snapshot

To determine the optimal regimen, either avutometinib (VS-6766) monotherapy or avutometinib (VS-6766) in combination with defactinib, in KRAS-G12V NSCLC

The study did not show it

Who was studied
NCT04620330
How many people
90
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 SPL label · a recorded source, not a stored snapshot
  • PubChem PUG-REST · a recorded source, not a stored snapshot
  • FDA label (openFDA SPL) · a recorded source, not a stored snapshot

Phase 1 Maximum tolerated dose (MTD)

The study did not show it

Who was studied
NCT05608252
How many people
63
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 SPL label · a recorded source, not a stored snapshot
  • PubChem PUG-REST · a recorded source, not a stored snapshot
  • FDA label (openFDA SPL) · 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 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.

  • AVMAPKI FAKZYNJA CO-PACK is indicated for the treatment of adult patients with KRAS -mutated recurrent low-grade serous ovarian cancer (LGSOC) who have received prior systemic therapy. This indication is approved under accelerated approval based on tumor response rate and duration of response [see Clinical Studies (14) ].

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 AVMAPKI FAKZYNJA CO-PACK in pediatric patients has not been established.”

    US prescribing information · 65889527-1406-45df-8a85-e2690dcf427d · read 2026-08-30

  • On older people, the label states: “Clinical studies of AVMAPKI FAKZYNJA CO-PACK did not include sufficient numbers of patients aged 65 and over to determine whether they respond differently from younger patients.”

    US prescribing information · 65889527-1406-45df-8a85-e2690dcf427d · read 2026-08-30

  • On people who are pregnant, the label states: “Risk Summary Based on the mechanisms of action, AVMAPKI FAKZYNJA CO-PACK can cause fetal harm when administered to a pregnant woman [see Clinical Pharmacology (12.1) ] .”

    US prescribing information · 65889527-1406-45df-8a85-e2690dcf427d · read 2026-08-30

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

    US prescribing information · 65889527-1406-45df-8a85-e2690dcf427d · 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 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 (11)
It was studied for a different goal
The studies measured something else entirely. Nothing in this record points to this reason.
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

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 capsule, tablet, 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

Not recorded.

Nothing recorded

Where this came from

RNAWiki holds nothing here and says so rather than guessing.

No register entry is recorded.

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 unclearNothing found in the sources checked

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.

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.

RNAWiki could not confidently classify this substance, so no self-experiment plan is offered.

Questions worth asking

  • Which of the trials of Avutometinib 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 Avutometinib 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)
D0D4252V97
CAS registry number
946128-88-7
PubChem compound
16719221
ChEMBL
CHEMBL3545081
WHO international nonproprietary name list entry
11815
EMA substance identifier
300000027351
DrugBank
DB15254

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: Written into the record, not signed off.

  • 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

  • Not passed

    Safety mode resolved

    No register row and no identity class settled the question.

  • 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

  • 1 approved application covers products containing this substance. The earliest was NDA219616, approved 20250508 to VERASTEM INC.

    Drugs@FDA application register · NDA219616 · read 2026-08-29

  • Marketing status on the register: prescription.

    Drugs@FDA application register · NDA219616 · read 2026-08-29

What is missing or unclearRead from sources, not yet reviewed

What to learn next

Ordered by what would most change how you read this page, starting with what is easiest to misunderstand.

This order is fixed in code and does not count clicks or time on the page.

What is not here

9 questions this page could not answer

These sections were prepared and left out because there was nothing to put in them. They are listed rather than hidden, so the gaps in this record are visible.

  • What was measured, goal by goal — found nothing in the sources checked.
  • How close this is to real life — found nothing in the sources checked.
  • The path through the body — found nothing in the sources checked.
  • Felt, measured, or meaningful — found nothing in the sources checked.
  • How long anything takes — found nothing in the sources checked.
  • What it may clash with — found nothing in the sources checked.
  • Other ways to the same goal — found nothing in the sources checked.
  • Claims that go past the evidence — found nothing in the sources checked.
  • What changed on this page — found nothing in the sources checked.

The record as stored

The full record, for auditing

Everything above is built from what is below. This layer keeps the technical vocabulary, record identifiers and every stored row, so a reader who wants to check the page can.

Recorded evidence blocks (7)

On the Avutometinib label: indicated for what?


"AVMAPKI FAKZYNJA CO-PACK is indicated for the treatment of adult patients with KRAS -mutated recurrent low-grade serous ovarian cancer (LGSOC) who have received prior systemic therapy. This indication is approved under accelerated approval based on tumor response rate and duration of response [see Clinical Studies…": indications and usage on Avutometinib's label. DailyMed label · 65889527-1406-45df-8a85-e2690dcf427d · 2026-08-30

23 registered trials of Avutometinib — at which phases?


Registered studies posting no result
22 of 23

23 registered studies of Avutometinib: 14 phase2, 11 phase1, 1 early phase1, 1 phase3. CLINICALTRIALS_SNAPSHOT · 2026-09-01

3 with a PubMed record

Show the evidence
  • phase2
    14
  • phase1
    11
  • early phase1
    1
  • phase3
    1
  • recruiting
    12
  • active not recruiting
    5
2 more recorded rows
  • completed
    5
  • terminated
    1

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

Why did Avutometinib's trial NCT04720417 stop?


1 recorded trial of Avutometinib stopped. CLINICALTRIALS_SNAPSHOT · 2026-09-01

"Trial enrollment was stopped early by study sponsors (before the anticipated accrual of 18 patients) due to no patients having significant reduction in disease."; 1 of 23 registered studies

Show the evidence
  • Trial NCT04720417
    terminated; "Trial enrollment was stopped early by study sponsors (before the anticipated accrual of 18 patients) due to no patients having significant reduction in disease."

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

Which running trial of Avutometinib could settle lifespan?


NCT06487221 measures Progression-free survival (PFS) Rate, reading out 2029-05-30.

4 open trials; n 27; "Avutometinib and Defactinib in Diffuse Gastric Cancer"

Show the evidence

Trial

  • NCT06487221
    "Avutometinib and Defactinib in Diffuse Gastric Cancer"; n 27; "Progression-free survival (PFS) Rate"; 2029-05-30
  • NCT06495125
    "Defactinib, Avutometinib and Nivolumab for the Treatment of Anti-PD1 Refractory LKB1-Mutant Advanced Non-Small Cell Lung Cancer"; n 50; "Progression free survival (PFS)"; 2029-09-17
  • NCT07126158
    "Stereotactic Body Radiotherapy Plus FAK and RAF/MEK Inhibition in Advanced Pancreatic Adenocarcinoma"; n 36; "Progression-free survival (PFS) - Experimental Arm Only"; 2030-04-30
  • NCT06072781
    "A Study of Avutometinib (VS-6766) + Defactinib (VS-6063) in Recurrent Low-Grade Serous Ovarian Cancer"; n 270; "Progression Free Survival (PFS) per blinded independent central review (BICR)"; 2031-02-09

Which 4 trials of Avutometinib posted no result?


Posted no result
4 of 4 completed trials
Registrations
NCT00773526, NCT05187169, NCT04620330 and NCT03681483
Completion dates
oldest 2011-09; newest 2024-07-08
Show the evidence

Trial

  • NCT00773526
    2011-09
  • NCT05187169
    2022-04-12
  • NCT04620330
    2023-12-12
  • NCT03681483
    2024-07-08

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


Median enrolment
36
Largest enrolment
270
Registered trials counted
23

Avutometinib and BCRP and CYP1A2: shared by which compounds?


BCRP and CYP1A2 appear in Avutometinib's recorded interaction sentences, 8 in all. DailyMed label · 65889527-1406-45df-8a85-e2690dcf427d · 2026-08-30

CYP1A2, CYP1A2, CYP2B6, CYP2B6, CYP2C19, CYP2C8; 30 shared nodes; pharmacokinetics

Show the evidence

Interaction statement

  • pharmacokinetics
    Transporter Systems: Avutometinib is a substrate of P-gp and BCRP, but not a substrate of MATE1, MATE2-K, OAT1, OAT3, OATP1B1, OATP1B3, OCT1 and OCT2.
  • pharmacokinetics
    Defactinib is a BCRP and P-gp substrate, but not a substrate of MATE1, MATE2-K, OAT1, OAT3, OATP1B1, OATP1B3, OCT1, and OCT2.
  • pharmacokinetics
    Defactinib is an inhibitor of P-gp, BCRP, OATP1B1, OATP1B3, and MATE2-K, but not an inhibitor of MATE1, OAT1, OAT3, OCT1, and OCT2.
  • pharmacokinetics
    Avutometinib is not an inhibitor of P-gp, BCRP, MATE1, MATE2-K, OAT1, OAT3, OATP1B1, OATP1B3, OCT1 and OCT2.
  • pharmacokinetics
    In Vitro Studies CYP450 Enzymes: Avutometinib is a CYP3A4 substrate, but not a substrate of CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, and CYP2D6.
  • pharmacokinetics
    Defactinib is a CYP3A4 and CYP2C9 substrate, but not a substrate of CYP1A2, CYP2B6, CYP2C8, CYP2C19, and CYP2D6.
2 more recorded rows
  • Interaction statement pharmacokinetics
    Avutometinib is not an inducer of CYP3A4, CYP2B6, and CYP1A2.
  • Interaction statement pharmacokinetics
    Defactinib is an inducer of CYP2B6, and CYP1A2, but not CYP3A4.

CYP1A2

  • FINGOLIMOD LAURYL SULFATE, FOSAPREPITANT DIMEGLUMINE, TAFAMIDIS MEGLUMINE, Arimoclomol, Rasagiline, Sofpironium, Golodirsen, Tinidazole
  • FINGOLIMOD LAURYL SULFATE, FOSAPREPITANT DIMEGLUMINE, TAFAMIDIS MEGLUMINE, Arimoclomol, Rasagiline, Sofpironium, Golodirsen, Tinidazole

CYP2B6

  • FINGOLIMOD LAURYL SULFATE, TAFAMIDIS MEGLUMINE, Arimoclomol, Sofpironium, Bupropion, Golodirsen, Tinidazole, Naldemedine
  • FINGOLIMOD LAURYL SULFATE, TAFAMIDIS MEGLUMINE, Arimoclomol, Sofpironium, Bupropion, Golodirsen, Tinidazole, Naldemedine
  • CYP2C19
    FINGOLIMOD LAURYL SULFATE, FOSAPREPITANT DIMEGLUMINE, TAFAMIDIS MEGLUMINE, Arimoclomol, Rasagiline, Golodirsen, Naldemedine, Etravirine
  • CYP2C8
    FINGOLIMOD LAURYL SULFATE, TAFAMIDIS MEGLUMINE, Arimoclomol, Golodirsen, Naldemedine, Methylnaltrexone, Lapatinib, Tivozanib
  • CYP2C9
    FINGOLIMOD LAURYL SULFATE, FOSAPREPITANT DIMEGLUMINE, TAFAMIDIS MEGLUMINE, Arimoclomol, Rasagiline, Golodirsen, Tinidazole, Naldemedine
  • CYP2D6
    FINGOLIMOD LAURYL SULFATE, Darunavir Propylene Glycolate, FOSAPREPITANT DIMEGLUMINE, TAFAMIDIS MEGLUMINE, Arimoclomol, Rasagiline, Sofpironium, Fluoxetine

CYP3A4

  • FINGOLIMOD LAURYL SULFATE, ERYTHROMYCIN LACTOBIONATE, FOSAPREPITANT DIMEGLUMINE, TAFAMIDIS MEGLUMINE, Arimoclomol, Beclometasone, Rasagiline, Sofpironium
  • FINGOLIMOD LAURYL SULFATE, ERYTHROMYCIN LACTOBIONATE, FOSAPREPITANT DIMEGLUMINE, TAFAMIDIS MEGLUMINE, Arimoclomol, Beclometasone, Rasagiline, Sofpironium

BCRP

  • TAFAMIDIS MEGLUMINE, Arimoclomol, Ceftobiprole Medocaril, Deoxycholic acid, Golodirsen, Naldemedine, Eravacycline, Omadacycline
  • TAFAMIDIS MEGLUMINE, Arimoclomol, Ceftobiprole Medocaril, Deoxycholic acid, Golodirsen, Naldemedine, Eravacycline, Omadacycline

MATE1

  • TAFAMIDIS MEGLUMINE, Arimoclomol, Ceftobiprole Medocaril, Sofpironium, Golodirsen, Eravacycline, Prucalopride, Chenodeoxycholic acid
  • TAFAMIDIS MEGLUMINE, Arimoclomol, Ceftobiprole Medocaril, Sofpironium, Golodirsen, Eravacycline, Prucalopride, Chenodeoxycholic acid

MATE2-K

  • TAFAMIDIS MEGLUMINE, Arimoclomol, Sofpironium, Golodirsen, Eravacycline, Prucalopride, Chenodeoxycholic acid, Methylnaltrexone
  • TAFAMIDIS MEGLUMINE, Arimoclomol, Sofpironium, Golodirsen, Eravacycline, Prucalopride, Chenodeoxycholic acid, Methylnaltrexone

OAT1

  • TAFAMIDIS MEGLUMINE, Arimoclomol, Ceftobiprole Medocaril, Deoxycholic acid, Golodirsen, Naldemedine, Eravacycline, Prucalopride
  • TAFAMIDIS MEGLUMINE, Arimoclomol, Ceftobiprole Medocaril, Deoxycholic acid, Golodirsen, Naldemedine, Eravacycline, Prucalopride

OAT3

  • TAFAMIDIS MEGLUMINE, Arimoclomol, Ceftobiprole Medocaril, Deoxycholic acid, Golodirsen, Naldemedine, Pemetrexed, Eravacycline
  • TAFAMIDIS MEGLUMINE, Arimoclomol, Ceftobiprole Medocaril, Deoxycholic acid, Golodirsen, Naldemedine, Pemetrexed, Eravacycline

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

Where it is registered
Identifiers, relations and other names

The exact record

ChEMBL id
CHEMBL3264002
PubChem CID
16719221
CAS number
946128-88-7
InChIKey
LMMJFBMMJUMSJS-UHFFFAOYSA-N
Development code
CH-5126766, CH5126766, CKI-27, R-7304, Ro-5126766, VS-6766, CH5126766-002, RO5126766, RO5126766-002
Also called
Rg-7304, AVUTOMETINIB POTASSIUM, AVUTOMETINIB POTASSIUM [USAN]
Salt form
RO-5126766 POTASSIUM, RO5126766 POTASSIUM, VS-6766 POTASSIUM
Trade name
Avmapki Fakzynja Co-Pack (Copackaged), AVMAPKI
Sources (2)

Sources

ClinicalTrials.gov — US Government work · openFDA / DailyMed — US Government work

How these records are assembled · Which registers were checked

Index-quality checks
  • identity passed: no open identity hold
  • required summary fields resolved: 4 required field(s) not terminal: Why people use it, Best-supported result, Biggest unanswered question, Human evidence
  • public claims reviewed: 0 reviewed claim(s); drafts are never rendered
  • source coverage passed: 2 source rows
  • no critical contamination: no quarantine open
  • canonical metadata passed: slug and display name present
  • no raw internal fields: enforced by the copy-contract test over the rendered page

This is a record of evidence. It is not medical advice, and it does not say this substance suits you. Nothing here says any substance on RNAWiki is appropriate for a child.