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Afatinib

  • 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 Afatinib does in the body

Metastatic squamous NSCLC progressing after platinum-based chemotherapy

From the FDA-approved label: Afatinib covalently binds to the kinase domains of EGFR (ErbB1), HER2 (ErbB2), and HER4 (ErbB4) and irreversibly inhibits tyrosine kinase autophosphorylation, resulting in downregulation of ErbB signaling. Certain mutations in EGFR, including non-resistant mutations in its kinase domain, can result in increased autophosphorylation of the receptor, leading to receptor activation, sometimes in the absence of ligand binding, and can support cell proliferation in NSCLC.

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 · 41UD74L59M · read 2026-08-29

  • Its recorded molecular formula is C32H33ClFN5O11, weighing 718.1 g/mol.

    US prescribing information · fd638e5e-8032-e7ca-0179-95e96ab5d387 · read 2026-08-30

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 88 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.

Objective response rate (ORR)

The study did not show it

Who was studied
NCT02465060
How many people
6452
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

Progression Free Survival (Part B)

The study did not show it

Who was studied
NCT01085136
How many people
1154
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 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

Progression-free Survival, Based on Central Independent Review as Determined by Response Evaluation Criteria in Solid Tumours 1.1

The study did not show it

Who was studied
NCT01523587
How many people
795
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 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

Characterize the safety of MRTX849 in patients having advanced solid tumor malignancies with KRAS G12C mutation

The study did not show it

Who was studied
NCT03785249
How many people
731
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

Disease Free Survival (DFS)

The study did not show it

Who was studied
NCT01345669
How many people
617
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 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 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.

  • GILOTRIF is a kinase inhibitor indicated for: First-line treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose tumors have non-resistant epidermal growth factor receptor (EGFR) mutations as detected by an FDA-approved test ( 1.1 ) Limitations of Use: Safety and efficacy of GILOTRIF were not established in patients whose tumors have resistant EGFR mutations ( 1.1 ) Treatment of patients with…

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: “Safety and effectiveness of GILOTRIF in pediatric patients have not been established.”

    US prescribing information · fd638e5e-8032-e7ca-0179-95e96ab5d387 · read 2026-08-30

  • On older people, the label states: “LUX-Lung 3 did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects.”

    US prescribing information · fd638e5e-8032-e7ca-0179-95e96ab5d387 · 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) ] , GILOTRIF can cause fetal harm when administered to a pregnant woman.”

    US prescribing information · fd638e5e-8032-e7ca-0179-95e96ab5d387 · read 2026-08-30

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

    US prescribing information · fd638e5e-8032-e7ca-0179-95e96ab5d387 · read 2026-08-30

  • On people with reduced liver function, the label states: “GILOTRIF has not been studied in patients with severe (Child Pugh C) hepatic impairment.”

    US prescribing information · fd638e5e-8032-e7ca-0179-95e96ab5d387 · read 2026-08-30

  • On people with reduced kidney function, the label states: “Patients with severe renal impairment have a higher exposure to afatinib than patients with normal renal function.”

    US prescribing information · fd638e5e-8032-e7ca-0179-95e96ab5d387 · 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

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 tablet, tablet, film 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

  • 3 products list this as an active ingredient in the United States drug directory. 3 of them contain it and nothing else.

    FDA National Drug Code directory · 0597-0141 · read 2026-08-29

  • They are sold as tablet, film coated, taken oral.

    FDA National Drug Code directory · 0597-0141 · read 2026-08-29

  • The regulator's established pharmacologic class for it is kinase inhibitor [epc] and protein kinase inhibitors [moa].

    FDA National Drug Code directory · 0597-0141 · 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 · fd638e5e-8032-e7ca-0179-95e96ab5d387 · read 2026-08-29

  • Those labels are classed as human prescription drug.

    US prescribing information · fd638e5e-8032-e7ca-0179-95e96ab5d387 · read 2026-08-29

  • Gilotrif is oral at 3 DOSAGE FORMS AND STRENGTHS GILOTRIF is available as: 40 mg tablets: light blue, film-coated, round, biconvex, bevel-edged tablets debossed with "T40" on one side and the Boehringer Ingelheim company symbol on the othe…, recorded as fda label in effect 2025-11-13 in the United States.

    US prescribing information · fd638e5e-8032-e7ca-0179-95e96ab5d387 · 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 Afatinib 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.

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 Afatinib 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)
41UD74L59M
RxNorm concept
1430446

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

  • 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.

    Drugs@FDA application register · ANDA210703 · read 2026-08-29

  • Marketing status on the register: none (tentative approval).

    Drugs@FDA application register · ANDA210703 · read 2026-08-29

  • The earliest marketing start date recorded for a listed product is 20130712.

    FDA National Drug Code directory · 0597-0141 · 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 (11)

On the Afatinib label: indicated for what?


"GILOTRIF is a kinase inhibitor indicated for: First-line treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose tumors have non-resistant epidermal growth factor receptor (EGFR) mutations as detected by an FDA-approved test ( 1.1 ) Limitations of Use : Safety and efficacy of GILOTRIF were not…": indications and usage on Afatinib's label. DailyMed label · fd638e5e-8032-e7ca-0179-95e96ab5d387 · 2025-11-13

141 registered trials of Afatinib — at which phases?


Registered studies posting no result
93 of 141

141 registered studies of Afatinib: 80 phase2, 34 phase1, 17 na or unstated, 12 phase3, 6 phase4, 2 na, 1 early phase1. CLINICALTRIALS_SNAPSHOT · 2026-09-01

192 with a PubMed record

Show the evidence
  • phase2
    80
  • phase1
    34
  • na or unstated
    17
  • phase3
    12
  • phase4
    6
  • na
    2
11 more recorded rows
  • early phase1
    1
  • completed
    67
  • unknown
    26
  • terminated
    17
  • active not recruiting
    10
  • recruiting
    10
  • withdrawn
    6
  • approved for marketing
    2
  • enrolling by invitation
    1
  • no longer available
    1
  • suspended
    1

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

20 of Afatinib's trials stopped: safety, futility/efficacy, accrual/recruitment, other?


safety (1), futility/efficacy (1), accrual/recruitment (12) and other (6): Afatinib's stop wording, clustered. CLINICALTRIALS_SNAPSHOT · 2026-09-01

"The recruitment was discontinued because of failure to meet expected enrolment goals"; 20 of 141 registered studies

Show the evidence

Trial

  • NCT01531764
    terminated; "The recruitment was discontinued because of failure to meet expected enrolment goals"
  • NCT01732640
    terminated; "Slow accrual and high levels of toxicity lead to early termination."
  • NCT01824823
    terminated; "Slow accrual"
  • NCT02115048
    terminated; "Study was completed as per amended protocol. Protocol was amended to close enrollment earlier than initially planned (study continued as per plan)."
  • NCT02122172
    terminated; "Unable to meet accrual goal after several years"
  • NCT02274012
    withdrawn; "Former PI left institution and had plans to continue at another institution."
14 further recorded trials
  • NCT02470065
    suspended; "Study never started"
  • NCT02488694
    terminated; "unsufficient recruitment"
  • NCT02541903
    terminated; "poor overall accrual"
  • NCT02595840
    terminated; "Futility"
  • NCT02768337
    terminated; "Slow recruitment"
  • NCT02876081
    withdrawn; "medical decision"
  • NCT03054038
    terminated; "Low accrual"
  • NCT03481842
    withdrawn; "Change in study design and sponsor"
  • NCT03652233
    withdrawn; "Low accrual"
  • NCT03711422
    terminated; "Decision to close the trial made due to low recruitment."
  • NCT03878524
    terminated; "Low accrual"
  • NCT05588609
    terminated; "Merus terminated the study early due to changes in organizational priorities."
  • NCT06804850
    withdrawn; "The study was withdrawn prior to participant enrollment due to administrative and protocol optimization considerations."
  • NCT06897735
    terminated; "adjustment of the study design taking into account the receipt of primary data"

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

Human studies of Afatinib used afatinib 20mg — over how long?


studies of Afatinib used the recorded amount. ClinicalTrials.gov · 2026-09-01

5 recorded entries; human; also "afatinib 20mg", "afatinib 40mg", "Afatinib 40 MG"

Show the evidence

human

  • NCT01214616
    afatinib 20mg
  • NCT01214616
    afatinib 40mg
  • NCT04410653
    Afatinib 40 MG
  • NCT06753747
    Afatinib(30mg)
  • NCT06753747
    Afatinib(40mg)

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

Afatinib's half-life is 37 hours — which schedules were studied?


37 hours, the half-life Afatinib's label states: "Elimination The elimination half-life of afatinib is 37 hours after repeat dosing in cancer patients." DailyMed label · fd638e5e-8032-e7ca-0179-95e96ab5d387 · 2025-11-13

tmax 2 to 5 hours; bioavailability 92 %.

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  • half life pharmacokinetics
    37 hours; Elimination The elimination half-life of afatinib is 37 hours after repeat dosing in cancer patients.
  • tmax pharmacokinetics
    2 to 5 hours; Absorption Following oral administration of GILOTRIF tablets, time to peak afatinib plasma concentrations (T max ) is 2 to 5 hours.
  • bioavailability pharmacokinetics
    92 %; The geometric mean relative bioavailability of 20 mg GILOTRIF tablets was 92% as compared to an oral solution.
  • metabolism pharmacokinetics
    Metabolism Covalent adducts to proteins are the major circulating metabolites of afatinib and enzymatic metabolism of afatinib is minimal.

recorded 2025-11-13 · last checked 2026-09-04

Which running trial of Afatinib could settle lifespan?


NCT06759857 measures Progression-Free Survival (PFS), reading out 2025-05-01.

3 open trials; n 350; "FHND9041 Versus Afatinib for Non-small Cell Lung Cancer"

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Trial

  • NCT06759857
    "FHND9041 Versus Afatinib for Non-small Cell Lung Cancer"; n 350; "Progression-Free Survival (PFS)"; 2025-05-01
  • NCT05215548
    "Primary Tumor Resection With EGFR TKI for Stage IV NSCLC"; n 100; "2 year progression free survival rate"; 2027-10
  • NCT02491099
    "A Phase II Evaluation of Afatinib in Patients With Persistent or Recurrent HER2-positive Uterine Serous Carcinoma"; n 50; "Progression free survival"; 2028-12

Which 24 trials of Afatinib posted no result?


Posted no result
24 of 24 completed trials
Registrations
NCT01594177, NCT02625168, NCT01538381, NCT02747953, NCT01542437 and NCT01783587, and 18 more
Completion dates
oldest 2014-03; newest 2024-07-31
Show the evidence

Trial

  • NCT01594177
    2014-03
  • NCT02625168
    2014-12
  • NCT01538381
    2015-08
  • NCT02747953
    2016-11
  • NCT01542437
    2017-06
  • NCT01783587
    2018-06-01
14 further recorded trials
  • NCT02142036
    2018-08
  • NCT01415011
    2018-11-30
  • NCT04640870
    2020-05
  • NCT02629523
    2020-05-11
  • NCT02716311
    2021-04-07
  • NCT01427478
    2021-05
  • NCT01156545
    2021-06-09
  • NCT02423525
    2021-08
  • NCT01415674
    2021-12
  • NCT03695510
    2022-04-14
  • NCT02451553
    2022-04-16
  • NCT04201756
    2022-08-30
  • NCT03727724
    2022-09-06
  • NCT02501603
    2022-12-20

At the median, Afatinib's trials enrolled 40 people — anything larger?


Median enrolment
40
Largest enrolment
6452
Registered trials counted
138

What do 4172 spontaneous reports say about Afatinib — 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.

Afatinib appears in spontaneous reports to regulators. Across the 10 most-reported reaction terms, 4172 reaction mentions were counted: diarrhoea 1223; malignant neoplasm progression 1057; rash 474; stomatitis 267. FAERS via Open Targets · CHEMBL1173655 · 2026-06-24

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  • diarrhoea
    1223
  • malignant neoplasm progression
    1057
  • rash
    474
  • stomatitis
    267
  • paronychia
    245
  • decreased appetite
    237
4 more recorded rows
  • vomiting
    231
  • dehydration
    193
  • metastases to central nervous system
    147
  • disease progression
    98

recorded 2026-06-24 · last checked 2026-09-04

Which 10 reactions does Afatinib's label not list?


decreased appetite, dehydration and diarrhoea and 7 more reported for Afatinib, absent from its label. FAERS via Open Targets · CHEMBL1173655 · 2026-06-24

2 label terms; 10 reported and unlisted; fd638e5e-8032-e7ca-0179-95e96ab5d387

Show the evidence
  • decreased appetite
    count not stated
  • dehydration
    count not stated
  • diarrhoea
    count not stated
  • disease progression
    count not stated
  • malignant neoplasm progression
    count not stated
  • metastases to central nervous system
    count not stated
4 more recorded rows
  • paronychia
    count not stated
  • rash
    count not stated
  • stomatitis
    count not stated
  • vomiting
    count not stated

recorded 2026-06-24 · last checked 2026-09-04

Afatinib and P-GP, P-GLYCOPROTEIN and CYP3A4: shared by which compounds?


P-GP, P-GLYCOPROTEIN and CYP3A4 appear in Afatinib's recorded interaction sentences, 8 in all. DailyMed label · fd638e5e-8032-e7ca-0179-95e96ab5d387 · 2025-11-13

CYP3A4, P-gp, P-gp; 3 shared nodes; drug_interactions, pharmacokinetics

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Interaction statement

  • drug_interactions
    P-glycoprotein (P-gp) Inhibitors : Co-administration of P-gp inhibitors can increase afatinib exposure.
  • drug_interactions
    ( 2.5 , 7 ) P-gp Inducers : Co-administration of chronic P-gp inducers orally can decrease afatinib exposure.
  • drug_interactions
    ( 2.5 , 7 ) Effect of P-glycoprotein (P-gp) Inhibitors and Inducers Concomitant taking of P-gp inhibitors (including but not limited to ritonavir, cyclosporine A, ketoconazole, itraconazole, erythromycin, verapamil, quinidine, tacrolimus, nelfinavir, saquinavir, and amiodarone) with GILOTRIF can increase exposure to afatinib [see Clinical Pharmacology (12.3) ].
  • drug_interactions
    Concomitant taking of P-gp inducers (including but not limited to rifampicin, carbamazepine, phenytoin, phenobarbital, and St.
  • pharmacokinetics
    Approximately 2% of the afatinib dose was metabolized by FMO3; the CYP3A4-dependent N-demethylation was not detected.
  • pharmacokinetics
    Drug Interactions Studies Clincial Studies Effect of P-gp Inhibitors and Inducers on Afatinib: The effect of ritonavir dosing time relative to a single oral dose of GILOTRIF was evaluated in healthy subjects taking 40 mg of GILOTRIF alone as compared to those after ritonavir (200 mg twice daily for 3 days) co-administration at 6 hours after GILOTRIF administration.
2 more recorded rows
  • Interaction statement pharmacokinetics
    Pre-treatment with a potent inducer of P-gp, rifampicin (600 mg once daily for 7 days) decreased the plasma exposure to afatinib by 34% (AUC 0-INF ) and 22% (C max ) [see Drug Interactions (7) ] .
  • Interaction statement pharmacokinetics
    In Vitro Studies Effect of Afatinib on P-gp: Based on in vitro data, afatinib is an inhibitor of P-gp.
  • CYP3A4
    FINGOLIMOD LAURYL SULFATE, ERYTHROMYCIN LACTOBIONATE, FOSAPREPITANT DIMEGLUMINE, TAFAMIDIS MEGLUMINE, Arimoclomol, Beclometasone, Rasagiline, Sofpironium

P-gp

  • FINGOLIMOD LAURYL SULFATE, ERYTHROMYCIN LACTOBIONATE, Darunavir Propylene Glycolate, FOSAPREPITANT DIMEGLUMINE, TAFAMIDIS MEGLUMINE, Arimoclomol, Ceftobiprole Medocaril, Vincristine
  • FINGOLIMOD LAURYL SULFATE, ERYTHROMYCIN LACTOBIONATE, Darunavir Propylene Glycolate, FOSAPREPITANT DIMEGLUMINE, TAFAMIDIS MEGLUMINE, Arimoclomol, Ceftobiprole Medocaril, Vincristine

recorded 2025-11-13 · last checked 2026-09-04

Where it is registered
Identifiers, relations and other names

The exact record

ChEMBL id
CHEMBL1173655
PubChem CID
10184653
CAS number
850140-72-6
RxCUI
1430438
InChIKey
ULXXDDBFHOBEHA-CWDCEQMOSA-N
Also called
AFATINIB DIMALEATE, AFATINIB FREE BASE, Bibw 2992, BIBW2992, BIBW2992AFATINIBTOVOKS1011, BIBW2992-MA2, GILOTRIF, GIOTRIF, NSC-750691, TOMTOVOK, TOVOK, (2E)-N-(4-(3-CHLORO-4-FLUOROANILINO)-7-(((3S)-OXOLAN-3-YL)OXY)QUINOXAZOLIN-6-YL)-4-(DIMETHYLAMINO)BUT-2-ENAMIDE
Salt form
Afatinib maleate
Development code
BIBW-2992 MA2, BIBW-2992MA2
Sources (6)

Sources

ChEMBL 37 — CC BY-SA 3.0 Unported · ChEMBL ATC CC BY-SA · ClinicalTrials.gov — US Government work · Open Targets 26.06 — CC0 · 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

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: 6 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

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