Drug

Tucatinib

Approved · EMA

ClassReceptor protein-tyrosine kinase erbB-2 inhibitorEmerging researchLate-stage developmentRising momentum

Also known as Tukysa.

RxNorm2361285 ChEMBLCHEMBL3989868 ATCL01EH03UNII234248D0HH

Research papers

Active clinical trials

ERBB2

Primary target

Regulatory events

Latest activity

beta

Recent clinical, regulatory, research and industry developments relating to this drug.

Neoadjuvant Trastuzumab, Pertuzumab and Tucatinib Without Chemotherapy in HER2-positive Breast Cancer: the TRAIN-4 Study

Clinical trial2026-08-01Primary completion · ClinicalTrials.gov

A Phase 1b/2 Open-Label Study of Disitamab Vedotin in Combination With Other Anticancer Therapies in Solid Tumors

Clinical trial2026-07-22Results expected Q3 2029 · ClinicalTrials.gov

A Phase II Study of Tucatinib and Ado-trastuzumab Emtansine (T-DM1) in Patients With HER2-positive Metastatic Solid Tumors and Metastases to Brain (TUCATEMEB)

Clinical trial2026-07-16Results expected Q1 2027 · ClinicalTrials.gov

A Phase II Study of the Safety, Tolerability and Antitumor Activity of Tucatinib in Combination With Eribulin and Trastuzumab in Patients With Pretreated Unresectable Locally Advanced or Metastatic HER2+ Breast Cancer

Clinical trial2026-07-10Results expected Q2 2027 · ClinicalTrials.gov

A Two-part, Seamless, Multicenter, Randomized, Open-label, Adaptive Phase II/III Study of the Blood-brain Barrier Penetrant RO7771950 Versus Tucatinib, Both in Combination With Trastuzumab and Capecitabine, in Patients With Pretreated Unresectable Locally Advanced or Metastatic HER2-Positive Breast Cancer, With or Without Central Nervous System Metastases

Clinical trial2026-07-09Results expected Q2 2029 · ClinicalTrials.gov

PIKture-01: First-in-Human Study of the PI3KαH1047R Mutant-Selective Inhibitor OKI-219 as Monotherapy in Participants With Advanced Solid Tumors and as Part of Combination Therapy in Participants With Advanced Breast Cancer

Clinical trial2026-07-06Status changed to Active, not recruiting · ClinicalTrials.gov

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

Clinical trial2026-06-23Results expected Q4 2026 · ClinicalTrials.gov

Tucatinib and trastuzumab in HER2-mutated metastatic breast cancer: a phase 2 basket trial.

Research2025-01-17Nature medicine

MOUNTAINEER-03 phase III study design: first-line mFOLFOX6 + tucatinib + trastuzumab for HER2+ metastatic colorectal cancer.

Research2024-12-26Future oncology (London, England)

Tucatinib and Trastuzumab for Previously Treated Human Epidermal Growth Factor Receptor 2-Positive Metastatic Biliary Tract Cancer (SGNTUC-019): A Phase II Basket Study.

Research2023-09-26Journal of clinical oncology : official journal of the American Society of Clinical Oncology

Approval: Tukysa (EMA)

Regulatory2021-02-11EMA

Intracranial Efficacy and Survival With Tucatinib Plus Trastuzumab and Capecitabine for Previously Treated HER2-Positive Breast Cancer With Brain Metastases in the HER2CLIMB Trial.

Research2020-05-29Journal of clinical oncology : official journal of the American Society of Clinical Oncology

Profile

Identifiers & mechanism

Canonical identifiers, marketed brand names and mechanism, resolved across RxNorm, ChEMBL and ATC.

Canonical name

Tucatinib

Aliases & brands

Tukysa

RxNorm CUI

2361285

ChEMBL ID

CHEMBL3989868

ATC codes

L01EH03

UNII

234248D0HH

Primary mechanism

Receptor protein-tyrosine kinase erbB-2 inhibitor

Regulatory jurisdictions

ema

Pharmacology & targets

1 target

Known molecular targets and mechanisms supported by curated pharmacology databases.

Receptor tyrosine-protein kinase erbB-2

ERBB2 · P04626

INHIBITORReceptor protein-tyrosine kinase erbB-2 inhibitor

Regulatory timeline

1 event

The complete regulatory record, grouped by authority — approvals, safety advisories and label changes. Each authority shows its most recent events; expand one to read its full history.

Earliest approval

2021-02-11

Latest approval

2021-02-11

Authorities

EMA

Total events

emaEuropean Medicines Agency· 1 event

2021-02-11Approval

Approval: Tukysa (EMA)

Indication: Tukysa is indicated in combination with trastuzumab and capecitabine for the treatment of adult patients with HER2?positive locally advanced or metastatic breast cancer who have… Show full indication

Tukysa is indicated in combination with trastuzumab and capecitabine for the treatment of adult patients with HER2?positive locally advanced or metastatic breast cancer who have received at least 2 prior anti-HER2 treatment regimens.

Evidence ↗

Contains information from the European Medicines Agency (European Medicines Agency), © EMA, reused under CC BY 4.0.

Clinical trials

56 trials

The current development programme across all trial phases — status mix, phase distribution and the late-stage studies shaping the evidence base.

Development programme

CLINICALTRIALS.GOV · LIVE REGISTRY

registered trials across all phases

LATEST COMPLETION 2025

Active studies

Recruiting

Late-stage (III+)

Completed

Discontinued

PHASE DISTRIBUTIONn = 56

Early Phase 11Phase 115Phase 1 / 28Phase 226Phase 2 / 32Phase 34

Late-stage studies

Phase III+ trials still open or recently active — where late-stage evidence is being generated.

The CompassHER2 Trials (COMprehensive Use of Pathologic Response ASSessment to Optimize Therapy in HER2-Positive Breast Cancer): CompassHER2 Residual Disease (RD), A Double-Blinded, Phase III Randomized Trial of T-DM1 and Placebo Compared With T-DM1 and Tucatinib

Active, not recruitingPH IIIKey trialAlliance for Clinical Trials in Oncologyn=1,0562035

RecruitingPH II/IIIHoffmann-La Rochen=6502032

An Open-label Randomized Phase 3 Study of Tucatinib in Combination With Trastuzumab and mFOLFOX6 Versus mFOLFOX6 Given With or Without Either Cetuximab or Bevacizumab as First-line Treatment for Subjects With HER2+ Metastatic Colorectal Cancer

RecruitingPH IIISeagen, a wholly owned subsidiary of Pfizern=4002030

Randomized, Double-blind, Phase 3 Study of Tucatinib or Placebo in Combination With Ado-trastuzumab Emtansine (T-DM1) for Subjects With Unresectable Locally-advanced or Metastatic HER2+ Breast Cancer (HER2CLIMB-02)

Active, not recruitingPH IIISeagen, a wholly owned subsidiary of Pfizern=4662029

A Randomized, Double-blind, Phase 3 Study of Tucatinib or Placebo in Combination With Trastuzumab and Pertuzumab as Maintenance Therapy for Metastatic HER2+ Breast Cancer (HER2CLIMB-05)

Active, not recruitingPH IIISeagen, a wholly owned subsidiary of Pfizern=6542027

Recent completions

Trials that read out recently, adding to the completed evidence base.

A Single Arm, Open Label Phase 2 Study of Tucatinib in Combination With Trastuzumab Deruxtecan in Subjects With Previously Treated Unresectable Locally-Advanced or Metastatic HER2+ Breast Cancer

CompletedPH IISeagen, a wholly owned subsidiary of Pfizern=702025

Phase I Trial of ZW25 in Patients With Locally Advanced (Unresectable) and/or Metastatic HER2-expressing Cancers

CompletedPH IJazz Pharmaceuticalsn=2792024

A Randomized, Double-blind, Placebo-controlled, Active Comparator Phase 2/3 Study of Tucatinib in Combination With Trastuzumab, Ramucirumab, and Paclitaxel in Subjects With Previously Treated, Locally-advanced Unresectable or Metastatic HER2+ Gastric or Gastroesophageal Junction Adenocarcinoma (GEC)

CompletedPH II/IIISeagen Inc.n=172024

MyTACTIC: An Open-Label Phase II Study Evaluating Targeted Therapies in Patients Who Have Advanced Solid Tumors With Genomic Alterations or Protein Expression Patterns Predictive of Response

CompletedPH IIGenentech, Inc.n=2522024

MOUNTAINEER: A Phase II, Open Label Study of Tucatinib Combined With Trastuzumab in Patients With HER2+ Metastatic Colorectal Cancer

CompletedPH IISeagen Inc.n=1172023

Phase 2 Randomized, Double-Blinded, Controlled Study of Tucatinib vs Placebo in Combination With Capecitabine and Trastuzumab in Patients With Pretreated Unresectable Locally Advanced or Metastatic HER2+ Breast Carcinoma

CompletedPH IISeagen Inc.n=6122022

Research activity

5 papers

Key research shaping understanding of this drug, combining the latest publications with the most influential evidence.

Publications over time

20202025

Most influential

Tucatinib, Trastuzumab, and Capecitabine for HER2-Positive Metastatic Breast Cancer.

The New England journal of medicine · 2020 · 948 cites

Intracranial Efficacy and Survival With Tucatinib Plus Trastuzumab and Capecitabine for Previously Treated HER2-Positive Breast Cancer With Brain Metastases in the HER2CLIMB Trial.

Journal of clinical oncology : official journal of the American Society of Clinical Oncology · 2020 · 421 cites

Tucatinib and Trastuzumab for Previously Treated Human Epidermal Growth Factor Receptor 2-Positive Metastatic Biliary Tract Cancer (SGNTUC-019): A Phase II Basket Study.

Journal of clinical oncology : official journal of the American Society of Clinical Oncology · 2023 · 77 cites

Tucatinib and trastuzumab in HER2-mutated metastatic breast cancer: a phase 2 basket trial.

Nature medicine · 2025 · 14 cites

MOUNTAINEER-03 phase III study design: first-line mFOLFOX6 + tucatinib + trastuzumab for HER2+ metastatic colorectal cancer.

Future oncology (London, England) · 2025 · 8 cites

Related diseases

3 conditions

Regulator-approved indications and conditions co-mentioned with this drug across the research literature. Number shows shared papers.

Active research areas

Breast Neoplasms3 Brain Neoplasms2 Neoplasm Metastasis2

Related drugs

3 matches

Drugs sharing diseases, protein targets and literature with this one. Ranked by graph evidence (shared targets + diseases weighted above co-mentions).

Capecitabine

Studied across 5 of the same disease areas as Tucatinib in the shared literature.

5 shared diseases2 shared papers

Fluorouracil

Studied across 5 of the same disease areas as Tucatinib in the shared literature.

5 shared diseases1 shared paper

Leucovorin

Studied across 3 of the same disease areas as Tucatinib in the shared literature.

3 shared diseases1 shared paper

References & data sources

RxNorm (U.S. National Library of Medicine) — drug identity
ChEMBL (EMBL-EBI) & UniProt — pharmacology and targets
Europe PMC — research literature
ClinicalTrials.gov — clinical trials
Regulatory event sources are credited in the Regulatory Timeline above.