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Tucatinib

  • 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 Tucatinib does in the body

TUKYSA is a kinase inhibitor indicated: • in combination with trastuzumab and capecitabine for treatment of adult patients with advanced unresectable or metastatic HER2-positive breast cancer, including patients with brain metastases, who have received one or more prior anti-HER2-based regimens in the metastatic setting.

From the FDA-approved label: Tucatinib is a tyrosine kinase inhibitor of HER2. In vitro, tucatinib inhibits phosphorylation of HER2 and HER3, resulting in inhibition of downstream MAPK and AKT signaling and cell proliferation, and showed anti-tumor activity in HER2 expressing tumor cells. In vivo, tucatinib inhibited the growth of HER2 expressing tumors. The combination of tucatinib and trastuzumab showed increased anti-tumor activity in vitro and in vivo compared to either drug alone.

Why people take it. TUKYSA is a kinase inhibitor indicated: • in combination with trastuzumab and capecitabine for treatment of adult patients with advanced unresectable or metastatic HER2-positive breast cancer, including patients with brain metastases, who have received one or more prior anti-HER2-based regimens in the metastatic setting.

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 · 234248D0HH · read 2026-08-29

  • Its recorded molecular formula is C26H24N8O2, weighing 480.52 g/mol.

    US prescribing information · f27eb1b9-b7fc-424e-988f-84dd7bb195a3 · 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 169 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.

Determine whether adding experimental agents to standard neoadjuvant medications increases the probability of pathologic complete response (pCR) over standard neoadjuvant chemotherapy for each biomarker signature established at trial entry.

The study did not show it

Who was studied
NCT01042379
How many people
5000
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

Objective Response Rate defined as % of participants in a cohort with complete or partial response or with stable disease according to standard response criteria

The study did not show it

Who was studied
NCT02693535
How many people
4200
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

Modified invasive disease-free survival (iDFS)

The study did not show it

Who was studied
NCT04457596
How many people
1056
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

Objective response rate defined as the number of patients with complete response or partial response

The study did not show it

Who was studied
NCT03297606
How many people
720
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 (PFS) by investigator assessment per Response Evaluation Criteria in Solid Tumors (RECIST) v1.1

The study did not show it

Who was studied
NCT05132582
How many people
654
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 (PFS) as Determined by Blinded Independent Central Review (BICR)

The study did not show it

Who was studied
NCT07413939
How many people
650
Study design
Phase 2/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.

  • TUKYSA is a kinase inhibitor indicated: • in combination with trastuzumab and capecitabine for treatment of adult patients with advanced unresectable or metastatic HER2-positive breast cancer, including patients with brain metastases, who have received one or more prior anti-HER2-based regimens in the metastatic setting.

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 TUKYSA in pediatric patients have not been established.”

    US prescribing information · f27eb1b9-b7fc-424e-988f-84dd7bb195a3 · read 2026-08-30

  • On older people, the label states: “In HER2CLIMB, 82 patients who received TUKYSA were ≥ 65 years, of whom 8 patients were ≥ 75 years.”

    US prescribing information · f27eb1b9-b7fc-424e-988f-84dd7bb195a3 · read 2026-08-30

  • On people who are pregnant, the label states: “Risk Summary TUKYSA is used in combination with trastuzumab and capecitabine.”

    US prescribing information · f27eb1b9-b7fc-424e-988f-84dd7bb195a3 · read 2026-08-30

  • On people with reduced liver function, the label states: “Tucatinib exposure is increased in patients with severe hepatic impairment (Child-Pugh C).”

    US prescribing information · f27eb1b9-b7fc-424e-988f-84dd7bb195a3 · read 2026-08-30

  • On people with reduced kidney function, the label states: “The use of TUKYSA in combination with capecitabine and trastuzumab is not recommended in patients with severe renal impairment (creatinine clearance [CLcr]: < 30 mL/min estimated by Cockcroft-Gault Equation), because capecitabine is contraindicated in patients with severe renal impairment.”

    US prescribing information · f27eb1b9-b7fc-424e-988f-84dd7bb195a3 · 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, 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

  • 8 products list this as an active ingredient in the United States drug directory. 8 of them contain it and nothing else.

    FDA National Drug Code directory · 43265-7480 · read 2026-08-29

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

    FDA National Drug Code directory · 43265-7480 · read 2026-08-29

  • The regulator's established pharmacologic class for it is cytochrome p450 2c8 inhibitors [moa], cytochrome p450 3a inhibitors [moa] and kinase inhibitor [epc].

    FDA National Drug Code directory · 43265-7480 · 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 · f27eb1b9-b7fc-424e-988f-84dd7bb195a3 · read 2026-08-29

  • Those labels are classed as human prescription drug.

    US prescribing information · f27eb1b9-b7fc-424e-988f-84dd7bb195a3 · read 2026-08-29

  • TUKYSA is oral at 3 DOSAGE FORMS AND STRENGTHS Tablets: • 50 mg: round, yellow, film-coated, debossed with “TUC” on one side and “50” on the other side. • 150 mg: oval-shaped, yellow, film-coated, debossed with “TUC” on one side and “150…, recorded as fda label in effect 2024-11-04 in the United States.

    US prescribing information · f27eb1b9-b7fc-424e-988f-84dd7bb195a3 · 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 Tucatinib 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 Tucatinib 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)
234248D0HH
RxNorm concept
2361290

Checks this page had to pass

  • Passed

    Identity resolved

    no open identity hold

  • Passed

    No unresolved merge across substance families

    no quarantine open

  • Passed

    Every public sentence names a source

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

  • Not passed

    Trial roles classified for highlighted evidence

    No registered study is classified as testing this substance.

  • Passed

    No internal keys in reader text

    enforced by the copy-contract test over the rendered page

  • Passed

    Safety mode resolved

    Suppression classes recorded: S1, S3, S4.

  • Passed

    Canonical metadata present

    slug and display name present

What is missing or unclearRead from sources, not yet reviewed

How this medicine reached us

Kept near the foot of the page. A historical event moves up only when it changes something about this substance today.

What the approval register records

  • 1 approved application covers products containing this substance. The earliest was NDA213411, approved 20200417 to SEAGEN.

    Drugs@FDA application register · NDA213411 · read 2026-08-29

  • Marketing status on the register: prescription.

    Drugs@FDA application register · NDA213411 · read 2026-08-29

  • The earliest marketing start date recorded for a listed product is 20200417.

    FDA National Drug Code directory · 43265-7480 · 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 Tucatinib label: indicated for what?

"TUKYSA is a kinase inhibitor indicated: • in combination with trastuzumab and capecitabine for treatment of adult patients with advanced unresectable or metastatic HER2-positive breast cancer, including patients with brain metastases, who have received one or more prior anti-HER2-based regimens in the metastatic…": indications and usage on Tucatinib's label. DailyMed label · f27eb1b9-b7fc-424e-988f-84dd7bb195a3 · 2024-11-04

61 registered trials of Tucatinib — at which phases?

Registered studies posting no result
50 of 61

61 registered studies of Tucatinib: 36 phase2, 23 phase1, 6 phase3, 4 na or unstated, 1 early phase1, 1 phase4. CLINICALTRIALS_SNAPSHOT · 2026-09-01

19 with a PubMed record

Show the evidence
  • phase2
    36
  • phase1
    23
  • phase3
    6
  • na or unstated
    4
  • early phase1
    1
  • phase4
    1
9 more recorded rows
  • active not recruiting
    16
  • completed
    16
  • recruiting
    13
  • withdrawn
    5
  • not yet recruiting
    4
  • terminated
    4
  • approved for marketing
    1
  • no longer available
    1
  • suspended
    1

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

10 of Tucatinib's trials stopped: safety, accrual/recruitment, funding/business, other?

safety (1), accrual/recruitment (4), funding/business (1) and other (4): Tucatinib's stop wording, clustered. CLINICALTRIALS_SNAPSHOT · 2026-09-01

"Study accrual ended early due to the FDA approval of tucatinib in metastatic HER2+ breast cancer"; 10 of 61 registered studies

Show the evidence

Trial

  • NCT03501979
    terminated; "Study accrual ended early due to the FDA approval of tucatinib in metastatic HER2+ breast cancer"
  • NCT03846583
    withdrawn; "Study halted prematurely, prior to enrollment of first participant."
  • NCT04512261
    withdrawn; "Study withdrawn due to change in treatment landscape for HER2+ metastatic breast cancer."
  • NCT04789096
    terminated; "Stopped on the recommendation of the BCT Independent Data and Monitoring Committee"
  • NCT04896320
    withdrawn; "Study will be closed due to zero enrollment."
  • NCT05062889
    suspended; "due to earlier termination of the agreement between the Sponsor and Central Laboratory for screening test. Enrollment will reopen as soon as a new laboratory is identified."
4 further recorded trials
  • NCT05091528
    terminated; "Sponsor decision based on strategic re-alignment"
  • NCT05227131
    withdrawn; "Funder decided to not continue the study"
  • NCT05356897
    withdrawn; "no sites were regulatory ready and the SC took the study to a different group."
  • NCT05583110
    terminated; "The study was closed early due to safety concerns and an unfavorable benefit-risk balance. Unexpected high neutropenia rates required a costly sub-study, which was not feasible, forcing the sponsor to terminate the trial prematurely."

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

Human studies of Tucatinib used Tucatinib 150 MG — over how long?

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

1 recorded entry; human; also "Tucatinib 150 MG"

Show the evidence
  • human NCT06016387
    Tucatinib 150 MG

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

Tucatinib's half-life is 11.9 hours — which schedules were studied?

11.9 hours, the half-life Tucatinib's label states: "Elimination At steady-state, tucatinib effective half-life was approximately 11.9 hours and geometric mean (CV%) apparent clearance was 53 (43) L/h in patients with mBC." DailyMed label · f27eb1b9-b7fc-424e-988f-84dd7bb195a3 · 2024-11-04

tmax 2 hours.

Show the evidence
  • half life pharmacokinetics
    11.9 hours; Elimination At steady-state, tucatinib effective half-life was approximately 11.9 hours and geometric mean (CV%) apparent clearance was 53 (43) L/h in patients with mBC.
  • tmax pharmacokinetics
    2 hours; Table 9: Tucatinib C max and AUC Tumor Type AUC ss (ng*h/mL) C max,ss (ng/mL) C trough,ss (ng/mL) mBC 5620 (43) 747 (45) 288 (59) mCRC 3370 (49) 405 (45) 197 (63) Absorption The median time to peak plasma concentration of tucatinib was approximately 2 hours (range 1 to 4 hours).
  • metabolism pharmacokinetics
    Metabolism Tucatinib is metabolized primarily by CYP2C8 and to a lesser extent via CYP3A.

recorded 2024-11-04 · last checked 2026-09-04

Which running trial of Tucatinib could settle lifespan?

NCT05041842 measures Progression-Free Survival, reading out 2026-04-30.

10 open trials; n 53; "Treatment With Tucatinib in Patients With an Isolated Brain Progression of a Metastatic Breast Cancer"

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Trial

  • NCT05041842
    "Treatment With Tucatinib in Patients With an Isolated Brain Progression of a Metastatic Breast Cancer"; n 53; "Progression-Free Survival"; 2026-04-30
  • NCT05800275
    "Capecitabine, Tucatinib, and Intrathecal Trastuzumab for Breast Cancer Patients With Leptomeningeal Disease"; n 30; "overall survival rate at 12 months"; 2027-06
  • NCT05132582
    "A Study of Tucatinib or Placebo With Trastuzumab and Pertuzumab for Metastatic HER2+ Breast Cancer"; n 654; "Progression-free survival (PFS) by investigator assessment per Response Evaluation Criteria in Solid Tumors (RECIST) v1.1"; 2027-09-28
  • NCT05323955
    "Secondary BRain Metastases Prevention After Isolated Intracranial Progression on Trastuzumab/Pertuzumab or T-DM1 in Patients With aDvanced Human Epidermal Growth Factor Receptor 2+ brEast Cancer With the Addition of Tucatinib"; n 48; "Progression Free Survival (PFS)"; 2027-11
  • NCT06016387
    "Tucatinib, Trastuzumab and Capecitabine With Brain and/or Spinal Radiotherapy (XRT) in Patients With HER2+, HER2 Mutated and/or HER2-amplified Metastatic Breast Cancer and Leptomeningeal Disease: A Multi-centre Phase II, Single Arm Feasibility Study"; n 30; "Survival status from the start of XRT"; 2028-10-05
  • NCT03975647
    "A Study of Tucatinib vs. Placebo in Combination With Ado-trastuzumab Emtansine (T-DM1) for Patients With Advanced or Metastatic HER2+ Breast Cancer"; n 466; "Progression-Free Survival (PFS) as Per Response Evaluation Criteria in Solid Tumors (RECIST) Version (v)1.1 Based on Investigator Assessment"; 2029-03-10
4 further recorded trials
  • NCT05253651
    "A Study of Tucatinib With Trastuzumab and mFOLFOX6 Versus Standard of Care Treatment in First-line HER2+ Metastatic Colorectal Cancer"; n 400; "Progression-free survival (PFS) per Response Evaluation Criteria in Solid Tumors Version 1.1 (RECIST v1.1) by Blinded Independent Central Review (BICR)"; 2030-07-03
  • NCT07413939
    "RO7771950 Versus Tucatinib in Combination With Trastuzumab and Capecitabine in People With Locally Advanced or Metastatic Breast Cancer That is Human Epidermal Growth Factor Receptor 2 (HER2)-Positive"; n 650; "Progression-free Survival (PFS) as Determined by Blinded Independent Central Review (BICR)"; 2032-09-29
  • NCT06439693
    "The SAPPHO Study: Sequential Therapy With Curative Intent in de Novo HER2+ Metastatic Breast Cancer"; n 72; "Disease Free Survival at 4 Years (DFS4)"; 2033-03-30
  • NCT04457596
    "T-DM1 and Tucatinib Compared With T-DM1 Alone in Preventing Relapses in People With High Risk HER2-Positive Breast Cancer, the CompassHER2 RD Trial"; n 1056; "Modified invasive disease-free survival (iDFS)"; 2035-05-31

Which 8 trials of Tucatinib posted no result?

Posted no result
8 of 8 completed trials
Registrations
NCT03758339, NCT03723395, NCT03777761, NCT03826602, NCT03722823 and NCT03914755, and 2 more
Completion dates
oldest 2018-01-30; newest 2020-09-03
Show the evidence

Trial

  • NCT03758339
    2018-01-30
  • NCT03723395
    2018-12-28
  • NCT03777761
    2019-03-11
  • NCT03826602
    2019-03-15
  • NCT03722823
    2019-05-07
  • NCT03914755
    2019-08-04
2 further recorded trials
  • NCT02025192
    2020-03-16
  • NCT01983501
    2020-09-03

At the median, Tucatinib's trials enrolled 48 people — anything larger?

Median enrolment
48
Largest enrolment
1056
Registered trials counted
59

What do 1543 spontaneous reports say about Tucatinib — 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.

Tucatinib appears in spontaneous reports to regulators. Across the 10 most-reported reaction terms, 1543 reaction mentions were counted: diarrhoea 449; fatigue 247; nausea 233; product dose omission issue 124. FAERS via Open Targets · CHEMBL3989868 · 2026-06-24

Show the evidence
  • diarrhoea
    449
  • fatigue
    247
  • nausea
    233
  • product dose omission issue
    124
  • vomiting
    120
  • decreased appetite
    97
4 more recorded rows
  • disease progression
    74
  • palmar-plantar erythrodysaesthesia syndrome
    68
  • unevaluable event
    66
  • asthenia
    65

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

Which 10 reactions does Tucatinib's label not list?

asthenia, decreased appetite and diarrhoea and 7 more reported for Tucatinib, absent from its label. FAERS via Open Targets · CHEMBL3989868 · 2026-06-24

2 label terms; 10 reported and unlisted; f27eb1b9-b7fc-424e-988f-84dd7bb195a3

Show the evidence
  • asthenia
    count not stated
  • decreased appetite
    count not stated
  • diarrhoea
    count not stated
  • disease progression
    count not stated
  • fatigue
    count not stated
  • nausea
    count not stated
4 more recorded rows
  • palmar-plantar erythrodysaesthesia syndrome
    count not stated
  • product dose omission issue
    count not stated
  • unevaluable event
    count not stated
  • vomiting
    count not stated

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

Tucatinib and CYP2C8, CYP3A and P-GP: shared by which compounds?

CYP2C8, CYP3A and P-GP appear in Tucatinib's recorded interaction sentences, 8 in all. DailyMed label · f27eb1b9-b7fc-424e-988f-84dd7bb195a3 · 2024-11-04

CYP2C8, CYP2C8, CYP3A, CYP3A, P-gp; 5 shared nodes; drug_interactions

Show the evidence

Interaction statement

  • drug_interactions
    • Strong CYP3A Inducers or Moderate CYP2C8 Inducers : Avoid concomitant use.
  • drug_interactions
    ( 7.1 ) • Strong CYP2C8 Inhibitors : Avoid concomitant use; reduce TUKYSA dose if concomitant use cannot be avoided.
  • drug_interactions
    ( 2.4 , 7.1 ) • CYP3A Substrates : Avoid concomitant use with CYP3A substrates, where minimal concentration changes may lead to serious or life-threatening toxicities.
  • drug_interactions
    ( 7.2 ) • P-gp Substrates : Consider reducing the dose of P-gp substrates, where minimal concentration changes may lead to serious or life-threatening toxicities.
  • drug_interactions
    Table 7: Drug Interactions that Affect TUKYSA Strong CYP3A Inducers or Moderate CYP2C8 Inducers Clinical Impact Concomitant use of TUKYSA with a strong CYP3A or moderate CYP2C8 inducer decreased tucatinib plasma concentrations [see Clinical Pharmacology (12.3) ] , which may reduce TUKYSA activity.
  • drug_interactions
    Management Avoid concomitant use of TUKYSA with a strong CYP3A inducer or a moderate CYP2C8 inducer.
2 more recorded rows
  • Interaction statement drug_interactions
    Strong or Moderate CYP2C8 Inhibitors Clinical Impact Concomitant use of TUKYSA with a strong CYP2C8 inhibitor increased tucatinib plasma concentrations [see Clinical Pharmacology (12.3) ] , which may increase the risk of TUKYSA toxicity.
  • Interaction statement drug_interactions
    Management Avoid concomitant use of TUKYSA with a strong CYP2C8 inhibitor.

CYP2C8

  • FINGOLIMOD LAURYL SULFATE, TAFAMIDIS MEGLUMINE, Arimoclomol, Golodirsen, Naldemedine, Methylnaltrexone, Lapatinib, Tivozanib
  • FINGOLIMOD LAURYL SULFATE, TAFAMIDIS MEGLUMINE, Arimoclomol, Golodirsen, Naldemedine, Methylnaltrexone, Lapatinib, Tivozanib

CYP3A

  • FINGOLIMOD LAURYL SULFATE, Darunavir Propylene Glycolate, Vincristine, Naldemedine, Pemetrexed, Eravacycline, Rasburicase, Repotrectinib
  • FINGOLIMOD LAURYL SULFATE, Darunavir Propylene Glycolate, Vincristine, Naldemedine, Pemetrexed, Eravacycline, Rasburicase, Repotrectinib
  • P-gp
    FINGOLIMOD LAURYL SULFATE, ERYTHROMYCIN LACTOBIONATE, Darunavir Propylene Glycolate, FOSAPREPITANT DIMEGLUMINE, TAFAMIDIS MEGLUMINE, Arimoclomol, Ceftobiprole Medocaril, Vincristine

recorded 2024-11-04 · last checked 2026-09-04

Where it is registered
Identifiers, relations and other names

The exact record

ChEMBL id
CHEMBL3989868
PubChem CID
51039094
CAS number
937263-43-9
RxCUI
2361285
InChIKey
SDEAXTCZPQIFQM-UHFFFAOYSA-N
Also called
Irbinitinib, Ont-380, TUCATINIB [MI], TUCATINIB [ORANGE BOOK], TUCATINIB [USAN], Tucatinib [WHO-DD], tucatinib [INN]
Development code
ARRY-380, MK-7119
Trade name
Tukysa
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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