Drugs / Tucatinib
last change Aug 2026 re-read 2 minutes ago

Tucatinib

also known as ONT-380 · ARRY-380 · Irbinitinib · MK-7119 · Tukysa

Small molecule targets ERBB2 via inhibition

Developed for
HER2 positive breast carcinoma · breast cancer · metastatic malignant neoplasm in the brain · female breast carcinoma · gastroesophageal junction adenocarcinoma · non-small cell lung carcinoma · esophageal adenocarcinoma · gastric adenocarcinoma
+26 more · invasive breast carcinoma · neoplastic meningitis · non-Hodgkin lymphoma · plasma cell myeloma · rectum adenocarcinoma · biliary tract neoplasm · breast carcinoma by gene expression profile · breast neoplasm · cancer · cancer of unknown primary site · cervical cancer · cholangiocarcinoma · colon adenocarcinoma · colorectal adenocarcinoma · colorectal cancer · colorectal carcinoma · colorectal neoplasm · gallbladder carcinoma · gastric cancer · gastroesophageal adenocarcinoma · Her2-receptor negative breast cancer · malignant colon neoplasm · malignant leptomeningeal tumor · metastatic malignant neoplasm · synchronous bilateral breast carcinoma · urothelial neoplasm
Investigated by
Seagen Inc. · Pfizer · Pfizer · National Cancer Institute (NCI) · AstraZeneca · Criterium, Inc.
+61 more · Genentech, Inc. · Novartis · UNICANCER · Academic and Community Cancer Research United · Bristol-Myers Squibb · Cascadian Therapeutics Inc. · Daiichi Sankyo · Dana-Farber Cancer Institute · Eli Lilly and Company · Institut Curie · Johns Hopkins University · Memorial Sloan Kettering Cancer Center · Merck Sharp & Dohme LLC · QuantumLeap Healthcare Collaborative · Translational Breast Cancer Research Consortium · ARCAGY/ GINECO GROUP · Alliance for Clinical Trials in Oncology · American Society of Clinical Oncology · Array BioPharma · Baptist Health South Florida · Bayer · Biocon Biologics Inc. · Boehringer Ingelheim · Breast Cancer Trials, Australia and New Zealand · Canadian Cancer Trials Group · Carey Anders, M.D. · Eurofins · Foundation Medicine · Georgetown University · Gruppo Oncologico del Nord-Ovest · Hoffmann-La Roche · Indiana University · Jazz Pharmaceuticals · Jonathan Riess · Jonsson Comprehensive Cancer Center · M.D. Anderson Cancer Center · MedSIR · Merck Institute for Therapeutic Research · Parexel · Peking University International Hospital · Providence Health & Services · RemeGen Co., Ltd. · Reva Basho · SCRI Development Innovations, LLC · Seattle Genetics (now a wholly owned subsidiary of Pfizer) · Second Affiliated Hospital, School of Medicine, Zhejiang University · Servier · Silverback Therapeutics · Spanish Breast Cancer Research Group · Sun Yat-sen University · Sunnybrook Health Sciences Centre · Taiho Oncology, Inc. · The Netherlands Cancer Institute · University of Alabama at Birmingham · University of California, San Francisco · University of Chicago · University of Colorado, Denver · University of Michigan · University of Texas · University of Washington · Zhejiang University

Regulatory milestones approvals, filings & regulatory actions · 3 recorded

MilestoneJurisdictionBrandIndicationDateSentence it was read from
Label expansion US (FDA) TUKYSA 2023-01-19 fda.gov
Approved EU (EMA) Tukysa 2021-02-11 europa.eu
Approved US (FDA) TUKYSA 2020-04-17 fda.gov

Trials 61 · a red edge is where a trial was stopped

PhaseRegistry idDatesIndicationSponsorStatusOutcome
Phase 116 trials
Phase 1 NCT05553522 Jan 2024 → Dec 2025 HER2 positive breast carcinoma, metastatic malignant neoplasm in the brain Baptist Health South Florida Terminated No outcome recorded
Phase 1 NCT06067776 Jan 2024 → Jan 2025 overdue non-small cell lung carcinoma Jonathan Riess Not yet recruiting No outcome recorded
Phase 1 NCT06162559 Dec 2023 → Aug 2026 overdue breast cancer The Netherlands Cancer Institute Recruiting No outcome recorded
Phase 1 NCT05868226 Feb 2023 → Dec 2028 expected HER2 positive breast carcinoma, hormone receptor-positive breast cancer, metastatic malignant neoplasm, triple-negative breast carcinoma QuantumLeap Healthcare Collaborative Recruiting No outcome recorded
Phase 1 NCT05382364 Jun 2022 → Dec 2026 expected HER2 positive breast carcinoma, colorectal cancer, gastroesophageal adenocarcinoma Pfizer Active not recruiting No outcome recorded
Phase 1 NCT03846583 Jun → Sep 2020 breast cancer Dana-Farber Cancer Institute Withdrawn No outcome recorded
Phase 1 NCT03914755 May → Aug 2019 Seagen Inc. Completed No outcome recorded
Phase 1 NCT03826602 Feb → Mar 2019 Seagen Inc. Completed No outcome recorded
Phase 1 NCT03777761 Dec 2018 → Mar 2019 Seagen Inc. Completed No outcome recorded
Phase 1 NCT03722823 Oct 2018 → May 2019 Seagen Inc. Completed No outcome recorded
Phase 1/29 trials
Phase 1/2 NCT07494448 Jul 2026 → Dec 2027 expected HER2 positive breast carcinoma MedSIR Not yet recruiting No outcome recorded
Phase 1/2 NCT06686394 Feb 2025 → Apr 2030 expected breast cancer Merck Sharp & Dohme LLC Recruiting No outcome recorded
Phase 1/2 NCT05230810 Aug 2022 → Mar 2026 overdue HER2 positive breast carcinoma Criterium, Inc. Active not recruiting No outcome recorded
Phase 1/2 NCT04512261 Jun 2022 → Jun 2024 HER2 positive breast carcinoma, metastatic malignant neoplasm in the brain Reva Basho Withdrawn No outcome recorded
Phase 1/2 NCT05319873 Apr 2022 → Apr 2027 expected HER2 positive breast carcinoma, invasive breast carcinoma Jonsson Comprehensive Cancer Center Active not recruiting No outcome recorded
Phase 1/2 NCT05091528 Feb → Jul 2022 HER2 positive breast carcinoma, non-small cell lung carcinoma Silverback Therapeutics Terminated No outcome recorded
Phase 1/2 NCT04896320 Dec 2021 → Jun 2023 female breast carcinoma Providence Health & Services Withdrawn No outcome recorded
Phase 1/2 NCT04538742 Dec 2020 → Jan 2025 overdue breast cancer AstraZeneca Active not recruiting No outcome recorded
Phase 1/2 NCT03054363 Nov 2017 → Jan 2023 breast cancer University of Colorado, Denver Completed No outcome recorded
Phase 229 trials
Phase 2 NCT07193394 Jan 2026 → Dec 2028 expected Her2-receptor negative breast cancer Institut Curie Recruiting No outcome recorded
Phase 2 NCT06439693 Aug 2024 → Mar 2030 expected HER2 positive breast carcinoma, estrogen-receptor positive breast cancer, female breast carcinoma Dana-Farber Cancer Institute Recruiting No outcome recorded
Phase 2 NCT06157892 May 2024 → Jul 2029 expected HER2 positive breast carcinoma, gastric cancer, gastroesophageal junction adenocarcinoma, triple-negative breast carcinoma Pfizer Active not recruiting No outcome recorded
Phase 2 NCT05458674 Jan 2024 → Jun 2027 expected breast carcinoma by gene expression profile Criterium, Inc. Active not recruiting No outcome recorded
Phase 2 NCT05955170 Dec 2023 → Dec 2027 expected HER2 positive breast carcinoma Institut Curie Recruiting No outcome recorded
Phase 2 NCT05800275 Dec 2023 → Dec 2026 expected HER2 positive breast carcinoma, malignant leptomeningeal tumor, neoplastic meningitis UNICANCER Recruiting No outcome recorded
Phase 2 NCT06016387 Nov 2023 → Dec 2026 expected HER2 positive breast carcinoma Sunnybrook Health Sciences Centre Recruiting No outcome recorded
Phase 2 NCT05356897 Oct 2023 → Sep 2024 colon adenocarcinoma, rectum adenocarcinoma Academic and Community Cancer Research United Withdrawn No outcome recorded
Phase 2 NCT05748834 Jul 2023 → Nov 2027 expected breast cancer SCRI Development Innovations, LLC Recruiting No outcome recorded
Phase 2 NCT05062889 May 2023 → Oct 2027 malignant colon neoplasm Gruppo Oncologico del Nord-Ovest Suspended No outcome recorded
Phase 2/31 trial
Phase 2/3 NCT04499924 Mar 2021 → Apr 2024 esophageal adenocarcinoma, gastric adenocarcinoma, gastroesophageal junction adenocarcinoma Seagen Inc. Completed No outcome recorded
Phase 34 trials
Phase 3 NCT05253651 Oct 2022 → Dec 2027 expected colorectal neoplasm Pfizer Recruiting No outcome recorded
Phase 3 NCT05132582 Mar 2022 → Sep 2025 overdue HER2 positive breast carcinoma Pfizer Active not recruiting No outcome recorded
Phase 3 NCT04457596 Mar 2021 → Jan 2028 expected HER2 positive breast carcinoma, invasive breast carcinoma, synchronous bilateral breast carcinoma Alliance for Clinical Trials in Oncology Active not recruiting No outcome recorded
Phase 3 NCT03975647 Oct 2019 → Jun 2023 overdue HER2 positive breast carcinoma Pfizer Active not recruiting No outcome recorded
Phase not stated2 trials
NCT04220203 HER2 positive breast carcinoma Pfizer Approved for marketing No outcome recorded
NCT03424473 Seagen Inc. No longer available No outcome recorded
Also used as a comparator or background therapy in 6 trials
PhaseRegistry idDatesIndicationSponsorStatusOutcome
Phase 01 trial
Phase 0 NCT07318389 Background Jun 2026 → Nov 2027 expected colorectal cancer M.D. Anderson Cancer Center Not yet recruiting No outcome recorded
Phase 12 trials
Phase 1 NCT06239467 Background Feb 2024 → Dec 2026 expected breast cancer OnKure, Inc. Active not recruiting No outcome recorded
Phase 1 NCT01921335 Comparator Aug 2013 → Mar 2018 HER2 positive breast carcinoma, metastatic malignant neoplasm in the brain Dana-Farber Cancer Institute Completed No outcome recorded
Phase 22 trials
Phase 2 NCT05227131 Background May 2022 → Oct 2024 HER2 positive breast carcinoma MedSIR Withdrawn No outcome recorded
Phase 2 NCT05190445 Background Nov 2021 → Feb 2023 overdue carcinoma Pieris Pharmaceuticals GmbH Active not recruiting No outcome recorded
Phase 2/31 trial
Phase 2/3 NCT07413939 Comparator May 2026 → May 2029 expected HER2 positive breast carcinoma Hoffmann-La Roche Recruiting No outcome recorded

Press releases naming this drug 2 releases

DateIssuerRelease
2025-12-10 Pfizer TUKYSA Added to First-Line Maintenance Therapy Extends Median Progression-Free Survival by Over 8 Months in Patients with HER2+ Metastatic Breast Cancer pfizer.com
2025-10-14 Pfizer TUKYSA Combination Significantly Improves Progression-Free Survival as First-Line Maintenance in HER2+ Metastatic Breast Cancer in HER2CLIMB-05 Trial pfizer.com

Evidence & citations 10 cited values

Every value below carries the sentence it was read from. 70 sources stand behind the page.

FieldValueCited text
Known as Tucatinib “ONT-380 (tucatinib) is a potent selective inhibitor of HER2 with intracranial activity in preclinical models.” PMID 32461105 May 2020
65

Tucatinib: 300mg po Q12H” NCT04760431

“Drug: TucatinibNCT02892123

“Drug: TucatinibNCT05583110

NCT04220203

NCT05955170

NCT05553522

NCT05382364

NCT03501979

NCT06067776

NCT02693535

NCT03043313

NCT03975647

NCT05062889

NCT03424473

NCT05868226

NCT06016387

NCT05230810

NCT04430738

NCT05673928

NCT04721977

NCT04789096

NCT03054363

NCT05748834

NCT05227131

NCT03846583

NCT05892068

NCT03914755

NCT04538742

NCT03297606

NCT07494448

NCT05319873

NCT05091528

NCT05132582

NCT01042379

NCT04579380

NCT03826602

NCT07413939

NCT02614794

NCT05253651

NCT03722823

NCT04512261

NCT06239467

NCT06157892

NCT07193394

NCT05800275

NCT05190445

NCT03723395

NCT01983501

NCT04539938

NCT04896320

NCT04457596

NCT03777761

NCT05458674

NCT03758339

NCT02025192

NCT05672524

NCT05041842

NCT06162559

NCT06439693

NCT04632992

NCT06686394

NCT05323955

NCT05356897

NCT07318389

NCT04499924

Known as ARRY-380 ClinicalTrials.gov intervention name — accepted as the source's own label NCT00650572
Known as Irbinitinib ChEMBL registry synonym — accepted as the source's own label CHEMBL3989868
Known as MK-7119 ChEMBL registry synonym — accepted as the source's own label CHEMBL3989868
Known as ONT-380 “A Phase 1, Open Label, Safety, Tolerability, and Pharmacokinetic Study of Tucatinib (ONT-380) in Healthy Japanese and Caucasian Subjects” NCT03914755
4

ONT-380 (tucatinib) is a potent selective inhibitor of HER2 with intracranial activity in preclinical models.” PMID 32461105 May 2020

“Tucatinib (ONT-380) is a potent, highly selective, oral HER2 small molecule tyrosine kinase inhibitor (TKI)” NCT04789096

“Tucatinib (ONT-380) will be administered orally, twice per day on days 1-21 of each cycle.” NCT01983501

“Tucatinib (ONT-380)” NCT07193394

Known as Tukysa ChEMBL registry synonym — accepted as the source's own label CHEMBL3989868
Action Inhibit “HER2 inhibitor” NCT00650572
Modality Small molecule “Tucatinib is a potent and selective oral HER2 tyrosine kinase inhibitor” PMID 29804905 May 2018
Route Oral oralNCT00650572
Target ERBB2 “Tucatinib is an oral, potent, human epidermal growth factor receptor 2 (HER2)-specific tyrosine kinase inhibitor (TKI) being developed as a novel treatment for...” PMID 29955792 Sep 2018