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Lapatinib

  • 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 Lapatinib does in the body

Lapatinib tablets are indicated in combination with: capecitabine for the treatment of patients with advanced or metastatic breast cancer whose tumors overexpress human epidermal growth factor receptor 2 (HER2) and who have received prior therapy, including an anthracycline, a taxane, and trastuzumab.

From the FDA-approved label: Lapatinib is a 4-anilinoquinazoline kinase inhibitor of the intracellular tyrosine kinase domains of both Epidermal Growth Factor Receptor (EGFR [ErbB1]) and of Human Epidermal Receptor Type 2 (HER2 [ErbB2]) receptors (estimated Ki app values of 3nM and 13nM, respectively) with a dissociation half-life of greater than or equal to 300 minutes. Lapatinib inhibits ErbB-driven tumor cell growth in vitro and in various animal models. An additive effect was demonstrated in an in vitro study when lapatinib and 5-FU (the active metabolite of capecitabine) were used in combination in the 4-tumor cell lines tested.

Why people take it. Lapatinib tablets are indicated in combination with: capecitabine for the treatment of patients with advanced or metastatic breast cancer whose tumors overexpress human epidermal growth factor receptor 2 (HER2) and who have received prior therapy, including an anthracycline, a taxane, and trastuzumab.

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 · G873GX646R · read 2026-08-29

  • Its recorded molecular formula is C29H26ClFN4O4S, weighing 943.5 g/mol.

    US prescribing information · 302a4346-a68d-af3e-e063-6294a90a4a6f · read 2026-08-30

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 192 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.

Disease-Free Survival (DFS) at the Primary Analysis

The study did not show it

Who was studied
NCT00490139
How many people
8381
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

Number of Participants (Par.) With Any Recurrence of the Initial Disease, Second Primary Cancer, Contralateral Breast Cancer, or Death (Disease-free Survival [DFS])

The study did not show it

Who was studied
NCT00374322
How many people
3166
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

To compare the pCR rates of neoadjuvant treatment in all 3 Settings

The study did not show it

Who was studied
NCT00567554
How many people
2600
Study design
Phase 3
Compared against
Not recorded for this study
Kind of result
A number that stands in for health
What was found
Result not recorded on this page
Repeated elsewhere
Unreplicated

What this does not prove. A study that did not show an effect does not show that no effect exists anywhere.

The limits of this study, and where it came from

Main limit. No limitation is recorded for this study.

How far it carries. This study is recorded from the curated record, not from the registry match.

Form and route. Oral

Interval reported. Not recorded in this summary

Written into the record, not signed off as a reviewed claim.

  • openFDA Drugs@FDA · a recorded source, not a stored snapshot
  • openFDA NDC Directory · a recorded source, not a stored snapshot
  • openFDA SPL label · a recorded source, not a stored snapshot
  • PubChem PUG-REST · a recorded source, not a stored snapshot

Number of Participants With Progression Free Survival (PFS) in the Human Epidermal Growth Factor Receptor 2 (HER2)-Positive Advanced or Metastatic Breast Cancer as Assessed by the Investigator

The study did not show it

Who was studied
NCT00073528
How many people
1286
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

Safety

The study did not show it

Who was studied
NCT00450203
How many people
1103
Study design
Phase 2/Phase 3
Compared against
Not recorded for this study
Kind of result
A number that stands in for health
What was found
Result not recorded on this page
Repeated elsewhere
Unreplicated

What this does not prove. A study that did not show an effect does not show that no effect exists anywhere.

The limits of this study, and where it came from

Main limit. No limitation is recorded for this study.

How far it carries. This study is recorded from the curated record, not from the registry match.

Form and route. Oral

Interval reported. Not recorded in this summary

Written into the record, not signed off as a reviewed claim.

  • openFDA Drugs@FDA · a recorded source, not a stored snapshot
  • openFDA NDC Directory · a recorded source, not a stored snapshot
  • openFDA SPL label · a recorded source, not a stored snapshot
  • PubChem PUG-REST · a recorded source, not a stored snapshot

Percentage of Participants With PD or Death as Assessed by an Independent Review Committee (IRC)

The study did not show it

Who was studied
NCT00829166
How many people
991
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.

  • Lapatinib tablets are indicated in combination with: capecitabine for the treatment of patients with advanced or metastatic breast cancer whose tumors overexpress human epidermal growth factor receptor 2 (HER2) and who have received prior therapy, including an anthracycline, a taxane, and trastuzumab.

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 lapatinib in pediatric patients have not been established.”

    US prescribing information · 302a4346-a68d-af3e-e063-6294a90a4a6f · read 2026-08-30

  • On older people, the label states: “Of the total number of metastatic breast cancer patients in clinical studies of lapatinib in combination with capecitabine (N = 198), 17% were 65 years of age and older, and 1% were 75 years of age and older.”

    US prescribing information · 302a4346-a68d-af3e-e063-6294a90a4a6f · read 2026-08-30

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

    US prescribing information · 302a4346-a68d-af3e-e063-6294a90a4a6f · read 2026-08-30

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

    US prescribing information · 302a4346-a68d-af3e-e063-6294a90a4a6f · read 2026-08-30

  • On people with reduced liver function, the label states: “The pharmacokinetics of lapatinib were examined in subjects with preexisting moderate (n = 8) or severe (n = 4) hepatic impairment (Child-Pugh Class B/C, respectively) and in 8 healthy control subjects.”

    US prescribing information · 302a4346-a68d-af3e-e063-6294a90a4a6f · read 2026-08-30

  • On people with reduced kidney function, the label states: “Lapatinib pharmacokinetics have not been specifically studied in patients with renal impairment or in patients undergoing hemodialysis.”

    US prescribing information · 302a4346-a68d-af3e-e063-6294a90a4a6f · 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, S6.

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

  • 15 products list this as an active ingredient in the United States drug directory. 15 of them contain it and nothing else.

    FDA National Drug Code directory · 68554-0072 · read 2026-08-29

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

    FDA National Drug Code directory · 68554-0072 · 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 · 68554-0072 · read 2026-08-29

  • 4 published labels name it as an active ingredient. 4 of them describe this substance alone, which is where its own label text on this page comes from.

    US prescribing information · 302a4346-a68d-af3e-e063-6294a90a4a6f · read 2026-08-29

  • Those labels are classed as human prescription drug.

    US prescribing information · 302a4346-a68d-af3e-e063-6294a90a4a6f · read 2026-08-29

  • Lapatinib is oral at 3 DOSAGE FORMS AND STRENGTHS Tablets: 250 mg - Each yellow, oval, film-coated tablet, debossed with “L250” on one side and “TV” on the other side contains 398 mg lapatinib ditosylate equivalent to 250 mg of lapatinib., recorded as fda label in effect 2025-03-12 in the United States.

    US prescribing information · 302a4346-a68d-af3e-e063-6294a90a4a6f · 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 Lapatinib 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 Lapatinib 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)
G873GX646R
CAS registry number
388082-78-8
PubChem compound
11557040
ChEMBL
CHEMBL554
ChEBI
49603
RxNorm concept
481474
EMA substance identifier
300000034642
DrugBank
DB01259

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, S6.

  • 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

  • 3 approved applications cover products containing this substance. The earliest was NDA022059, approved 20070313 to NOVARTIS.

    Drugs@FDA application register · NDA022059 · read 2026-08-29

  • Marketing status on the register: prescription.

    Drugs@FDA application register · NDA022059 · read 2026-08-29

  • The earliest marketing start date recorded for a listed product is 20070313.

    FDA National Drug Code directory · 68554-0072 · 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 (10)

On the Lapatinib label: indicated for what?

"TYKERB ® is indicated in combination with: capecitabine for the treatment of patients with advanced or metastatic breast cancer whose tumors overexpress human epidermal growth factor receptor 2 (HER2) and who have received prior therapy, including an anthracycline, a taxane, and trastuzumab. Limitations of Use :…": indications and usage on Lapatinib's label. DailyMed label · eee37f88-ec6a-4c30-b8aa-e2c71f93088c · 2026-01-27

235 registered trials of Lapatinib — at which phases?

Registered studies posting no result
126 of 235

235 registered studies of Lapatinib: 136 phase2, 71 phase1, 34 phase3, 5 early phase1, 4 na, 4 na or unstated, 1 phase4. CLINICALTRIALS_SNAPSHOT · 2026-09-01

1 with a PubMed record

Show the evidence
  • phase2
    136
  • phase1
    71
  • phase3
    34
  • early phase1
    5
  • na
    4
  • na or unstated
    4
7 more recorded rows
  • phase4
    1
  • completed
    160
  • terminated
    48
  • unknown
    16
  • withdrawn
    7
  • active not recruiting
    3
  • recruiting
    1

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

42 of Lapatinib's trials stopped: safety, futility/efficacy, accrual/recruitment, funding/business, sponsor decision unspecified, other?

safety (3), futility/efficacy (2), accrual/recruitment (21), funding/business (1), sponsor decision unspecified (1) and other (14): Lapatinib's stop wording, clustered. CLINICALTRIALS_SNAPSHOT · 2026-09-01

"slow accrual"; 42 of 235 registered studies

Show the evidence

Trial

  • NCT00225758
    terminated; "slow accrual"
  • NCT00239200
    terminated; "notification from sponsor"
  • NCT00272987
    terminated; "Enrollment was closed after the open label stage due to poor recruitment rate (randomized stage never opened)."
  • NCT00317434
    terminated; "Due to unacceptable non-dose limiting toxicities, excessive treatment delays and limited clinical responses."
  • NCT00437073
    terminated; "Lapatinib-topotecan arm enrollment closed early per protocol amendment 2. Then enrollment into remaining arm terminated due to operational issues."
  • NCT00447122
    terminated; "slow enrollment and lack of funding"
14 further recorded trials
  • NCT00479856
    terminated; "Study was terminated due to difficulty in identifying eligible subjects"
  • NCT00490061
    terminated; "Poor accrual."
  • NCT00499681
    terminated; "slow accrual"
  • NCT00508274
    terminated; "Primary analysis was completed in 2015 and data collection post 1-Jul-2019 was not reportable due to local regulations in China."
  • NCT00513253
    withdrawn; "It was determined not to be needed based on the clinical development plan of Tykerb."
  • NCT00709618
    terminated; "Evolving standard of care practices in this disease setting was limiting enrolment and leading to a delay in delivering this study information to the public."
  • NCT00754702
    terminated; "Poor accrual"
  • NCT00756470
    terminated; "Slow accrual."
  • NCT00759642
    terminated; "IRB decision"
  • NCT00804310
    terminated; "Lack of funding"
  • NCT00857714
    terminated; "Terminated due to low accrual"
  • NCT00881621
    terminated; "slow enrollment"
  • NCT00888810
    terminated; "lack of efficacy (intermediate analysis)"
  • NCT00953576
    terminated; "The study terminated early due to concerns about drug toxicity."

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

Human studies of Lapatinib used lapatinib (GW572016) 1500 mg — over how long?

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

5 recorded entries; human; also "lapatinib (GW572016) 1500 mg", "lapatinib (GW572016) 1000 mg", "Lapatinib 1000mg/d"

Show the evidence

human

  • NCT00347919
    lapatinib (GW572016) 1500 mg
  • NCT00347919
    lapatinib (GW572016) 1000 mg
  • NCT00447122
    Lapatinib 1000mg/d
  • NCT00447122
    Lapatinib 1500mg/d
  • NCT02029001
    Lapatinib (1500 mg QD)

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

Lapatinib's half-life is 6 to 7 days — which schedules were studied?

6 to 7 days, the half-life Lapatinib's label states: "Daily dosing of TYKERB results in achievement of steady state within 6 to 7 days, indicating an effective half-life of 24 hours." DailyMed label · eee37f88-ec6a-4c30-b8aa-e2c71f93088c · 2026-01-27

tmax 4 hours.

Show the evidence
  • half life pharmacokinetics
    6 to 7 days; Daily dosing of TYKERB results in achievement of steady state within 6 to 7 days, indicating an effective half-life of 24 hours.
  • tmax pharmacokinetics
    4 hours; Peak plasma concentrations (C max ) of lapatinib are achieved approximately 4 hours after administration.
  • metabolism pharmacokinetics
    Metabolism : Lapatinib undergoes extensive metabolism, primarily by CYP3A4 and CYP3A5, with minor contributions from CYP2C19 and CYP2C8 to a variety of oxidated metabolites, none of which accounts for more than 14% of the dose recovered in the feces or 10% of lapatinib concentration in plasma.

recorded 2026-01-27 · last checked 2026-09-04

Which 71 trials of Lapatinib posted no result?

Posted no result
71 of 71 completed trials
Registrations
NCT00044343, NCT00085020, NCT00148902, NCT00114283, NCT00111787 and NCT00462956, and 65 more
Completion dates
oldest 2003-10; newest 2023-03-14
Show the evidence

Trial

  • NCT00044343
    2003-10
  • NCT00085020
    2005-02
  • NCT00148902
    2006-01-21
  • NCT00114283
    2006-10
  • NCT00111787
    2006-11-01
  • NCT00462956
    2006-12-20
14 further recorded trials
  • NCT00258050
    2007-02-08
  • NCT00259987
    2007-05
  • NCT00158782
    2007-08-21
  • NCT00099060
    2007-11
  • NCT00359190
    2008-01-09
  • NCT00498953
    2009-03
  • NCT00528281
    2009-05-27
  • NCT00650910
    2009-07-10
  • NCT00388076
    2009-07-21
  • NCT00316407
    2009-11
  • NCT00849329
    2009-11-24
  • NCT00078572
    2010-02
  • NCT00105950
    2010-05
  • NCT00424164
    2010-05-28

At the median, Lapatinib's trials enrolled 35 people — anything larger?

Median enrolment
35
Largest enrolment
8381
Registered trials counted
235

What do 4955 spontaneous reports say about Lapatinib — 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.

Lapatinib appears in spontaneous reports to regulators. Across the 10 most-reported reaction terms, 4955 reaction mentions were counted: diarrhoea 1414; nausea 547; vomiting 518; palmar-plantar erythrodysaesthesia syndrome 513. FAERS via Open Targets · CHEMBL1201179 · 2026-06-24

Show the evidence
  • diarrhoea
    1414
  • nausea
    547
  • vomiting
    518
  • palmar-plantar erythrodysaesthesia syndrome
    513
  • rash
    379
  • disease progression
    357
4 more recorded rows
  • pyrexia
    355
  • neutropenia
    347
  • dehydration
    324
  • malignant neoplasm progression
    201

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

Which 10 reactions does Lapatinib's label not list?

dehydration, diarrhoea and disease progression and 7 more reported for Lapatinib, absent from its label. FAERS via Open Targets · CHEMBL1201179 · 2026-06-24

2 label terms; 10 reported and unlisted; eee37f88-ec6a-4c30-b8aa-e2c71f93088c

Show the evidence
  • dehydration
    count not stated
  • diarrhoea
    count not stated
  • disease progression
    count not stated
  • malignant neoplasm progression
    count not stated
  • nausea
    count not stated
  • neutropenia
    count not stated
4 more recorded rows
  • palmar-plantar erythrodysaesthesia syndrome
    count not stated
  • pyrexia
    count not stated
  • rash
    count not stated
  • vomiting
    count not stated

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

Lapatinib and CYP3A4, CYP2C8 and P-GLYCOPROTEIN: shared by which compounds?

CYP3A4, CYP2C8 and P-GLYCOPROTEIN appear in Lapatinib's recorded interaction sentences, 8 in all. DailyMed label · eee37f88-ec6a-4c30-b8aa-e2c71f93088c · 2026-01-27

CYP1A2, CYP2C19, CYP2C8, CYP2C8, CYP2C9, CYP2D6; 11 shared nodes; drug_interactions

Show the evidence

Interaction statement

  • drug_interactions
    TYKERB is likely to increase exposure to concomitantly administered drugs which are substrates of CYP3A4, CYP2C8, or P-glycoprotein (ABCB1).
  • drug_interactions
    ( 7.1 ) Avoid strong CYP3A4 inhibitors.
  • drug_interactions
    If unavoidable, consider dose reduction of TYKERB in patients coadministered a strong CYP3A4 inhibitor.
  • drug_interactions
    ( 2.2 , 7.2 ) Avoid strong CYP3A4 inducers.
  • drug_interactions
    If unavoidable, consider gradual dose increase of TYKERB in patients coadministered a strong CYP3A4 inducer.
  • drug_interactions
    ( 2.2 , 7.2 ) 7.1 Effects of Lapatinib on Drug-Metabolizing Enzymes and Drug Transport Systems Lapatinib inhibits CYP3A4, CYP2C8, and P-glycoprotein (P-gp, ABCB1) in vitro at clinically relevant concentrations and is a weak inhibitor of CYP3A4 in vivo.
2 more recorded rows
  • Interaction statement drug_interactions
    Caution should be exercised and dose reduction of the concomitant substrate drug should be considered when dosing TYKERB concurrently with medications with narrow therapeutic windows that are substrates of CYP3A4, CYP2C8, or P-gp.
  • Interaction statement drug_interactions
    Lapatinib did not significantly inhibit the following enzymes in human liver microsomes: CYP1A2, CYP2C9, CYP2C19, and CYP2D6 or UGT enzymes in vitro, however, the clinical significance is unknown.
  • CYP1A2
    FINGOLIMOD LAURYL SULFATE, FOSAPREPITANT DIMEGLUMINE, TAFAMIDIS MEGLUMINE, Arimoclomol, Rasagiline, Sofpironium, Golodirsen, Tinidazole
  • CYP2C19
    FINGOLIMOD LAURYL SULFATE, FOSAPREPITANT DIMEGLUMINE, TAFAMIDIS MEGLUMINE, Arimoclomol, Rasagiline, Golodirsen, Naldemedine, Etravirine

CYP2C8

  • FINGOLIMOD LAURYL SULFATE, TAFAMIDIS MEGLUMINE, Arimoclomol, Golodirsen, Naldemedine, Methylnaltrexone, Tivozanib, Metaxalone
  • FINGOLIMOD LAURYL SULFATE, TAFAMIDIS MEGLUMINE, Arimoclomol, Golodirsen, Naldemedine, Methylnaltrexone, Tivozanib, Metaxalone
  • 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
  • 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 2026-01-27 · last checked 2026-09-04

Where it is registered
Identifiers, relations and other names

The exact record

ChEMBL id
CHEMBL1201179
PubChem CID
11557040
CAS number
388082-78-8
RxCUI
481474
InChIKey
BCFGMOOMADDAQU-UHFFFAOYSA-N
Also called
LAPATINIB DITOSYLATE, Lapatinib tosilate, Tycerb, FMM, GSK 572016, GSK572016, GW-2016, GW2016, GW-572016, GW572016, GW-572016X, LAPATANIB
Development code
GW-572016F, GW572016F
Salt form
Lapatinib ditoluenesulfonate monohydrate, Lapatinib ditosylate anhydrous, Lapatinib ditosylate monohydrate, Lapatinib tosilate hydrate
Trade name
Tykerb, Tyverb, Lapatinib / Tykerb
Sources (6)

Sources

ChEMBL 37 — CC BY-SA 3.0 Unported · 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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