Tukysa

(Tucatinib)

ApprovedSmall molecule

Tucatinib is used to treat certain types of breast cancer, particularly HER2-positive breast cancer that has spread to other parts of the body. It is often used in combination with other cancer medications.[2] Tukysa is currently approved and in use across 22 indications[4].[1]

Tukysa is one of 415 small molecule programs targeting Colorectal Carcinoma. It is currently in Approved.

Indications

Total Trials

Active Trials

414

Competitors

FDA Applications

NDA/BLA/ANDA regulatory filings

Patents

Pipeline

Status by Indication[4][1]

Indication

Colorectal CarcinomaActive, not recruiting

MetastasisActive, not recruiting

Gastric AdenocarcinomaApproved

Intestinal CancerActive, not recruiting

Chronic Myelogenous LeukemiaApproved

Breast NeoplasmActive, not recruiting

HER2 Positive Breast CarcinomaActive, not recruiting

Liver DiseaseApproved

Breast CancerActive, not recruiting

HER2-Positive Breast CancerNot yet recruiting

Colorectal CarcinomaApproved

Active, not recruiting

MetastasisApproved

Active, not recruiting

Gastric AdenocarcinomaApproved

Approved

Intestinal CancerPhase 2

Active, not recruiting

Chronic Myelogenous LeukemiaApproved

Approved

Breast NeoplasmApproved

Active, not recruiting

HER2 Positive Breast CarcinomaApproved

Active, not recruiting

Liver DiseaseApproved

Approved

Breast CancerPhase 3

Active, not recruiting

HER2-Positive Breast CancerApproved

Not yet recruiting

Showing 10 of 22 indications

Competition

Competitive Landscape

706 competitors in Breast Cancer

#DrugCompanyPhaseTrials

Tukysa

Pfizer

Approved

27 2

Blenoxane

Bristol-Myers Squibb

Preclinical

1 3

Recombinant Human Endostatin

PPeking University Third Hospital

Preclinical

1 4

Neoadjuvant Treatment

SShanghai Zhongshan Hospital

Preclinical

1 5

Tianeptine

Pfizer

Preclinical

1 6

Ablavar

LLantheus Medical Imaging

Preclinical

2 7

Diuretic

RReprieve Cardiovascular, Inc

Preclinical

1 8

Bisphosphonate

Amgen

Preclinical

2 9

Naltrexone/bupropion

Novo Nordisk

Preclinical

1 10

Sertraline ODT

PPfizer's Upjohn has merged with Mylan to form Viatris Inc.

Preclinical

Ranked by pipeline maturity and clinical activity. Current drug highlighted in teal.

Timeline

Expected Milestones

Q4 2026

Phase 1Active, not recruiting

Cancer

NCT05382364

Phase 2Active, not recruiting

Intestinal Cancer

NCT04430738

Phase 2Active, not recruiting

Breast Cancer

NCT04721977

Phase 2Active, not recruiting

Uterine Neoplasms

NCT04579380

Q1 2027

Phase 2Recruiting

Trial

NCT03297606

Q2 2027

Phase 1/2Recruiting

Breast Cancer

NCT05319873

Clinical

Trials by Indication[1]

Breast Cancer27 trials

A Study of Tucatinib (ONT-380) Combined With Capecitabine and/or Trastuzumab in Patients With HER2+ Metastatic Breast Cancer

Completed· Pfizer logo

Pfizer·Phase 1·NCT02025192·60 enrolled

Ribociclib, Tucatinib, and Trastuzumab for the Treatment of HER2 Positive Breast Cancer

Recruiting·JJonsson Comprehensive Cancer Center·Phase 1/2·NCT05319873·18 enrolled

TOPAZ: Tucatinib in COmbination With Pembrolizumab And TrastuZumab in Patients With HER2-Positive Breast Cancer Brain Metastases

Withdrawn·RReva Basho·Phase 1/2·NCT04512261

Show 24 more trials

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

Recruiting·SSunnybrook Health Sciences Centre·Phase 2·NCT06016387·30 enrolled

Expanded Access Use of Tucatinib for HER2+ Metastatic Breast Cancer

No longer available· Pfizer logo

Pfizer··NCT03424473

A Study of Tucatinib vs. Placebo in Combination With Capecitabine & Trastuzumab in Patients With Advanced HER2+ Breast Cancer

Completed· Pfizer logo

Pfizer·Phase 2·NCT02614794·612 enrolled

I-SPY TRIAL: Neoadjuvant and Personalized Adaptive Novel Agents to Treat Breast Cancer

Recruiting·QQuantumLeap Healthcare Collaborative·Phase 2·NCT01042379·5,000 enrolled

Tucatinib in Combination With Oral Etoposide andTrastuzumab in Patients With Metastatic HER2+ Breast Cancer

Recruiting·IInstitut Curie·Phase 2·NCT05955170·66 enrolled

Tucatinib, Palbociclib and Letrozole in Metastatic Hormone Receptor Positive and HER2-positive Breast Cancer

Completed·UUniversity of Colorado, Denver·Phase 1/2·NCT03054363·42 enrolled

Tucatinib With Chemotherapy and Trastuzumab in Advanced Her-2-neu Overexpressing, Previously Treated Breast Cancer.

Withdrawn·PProvidence Health & Services·Phase 1/2·NCT04896320

Clinical Trial of Alpelisb and Tucatinib in Patients With PIK3CA-Mutant HER2+ Metastatic Breast Cancer.

Active, not recruiting·CCriterium, Inc.·Phase 1/2·NCT05230810·40 enrolled

A Phase 1b/2 Study of T-DXd Combinations in HER2-positive Metastatic Breast Cancer

Active, not recruiting· AstraZeneca logo

AstraZeneca·Phase 1/2·NCT04538742·245 enrolled

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

Active, not recruiting·AAlliance for Clinical Trials in Oncology·Phase 3·NCT04457596·1,056 enrolled

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

Recruiting·TThe Netherlands Cancer Institute·Phase 1·NCT06162559·30 enrolled

Real World-clinical Outcomes of Tucatinib, Trastuzumab, and Capecitabine Following Trastuzumab Deruxtecan (T-DXd) for the Treatment of HER2-positive Metastatic Breast Cancer.

Completed· Pfizer logo

Pfizer··NCT06961331·86 enrolled

Margetuximab Plus Tucatinib and Capecitabine in HER2-positive Metastatic Breast Cancer

Withdrawn·MMedSIR·Phase 2·NCT05227131

Treatment Protocol of Tucatinib With Capecitabine and Trastuzumab in Patients With Unresectable Previously Treated HER2+ Breast Cancer

Approved for marketing· Pfizer logo

Pfizer··NCT04220203

Study of Tucatinib and Doxil in Participants With Human Epidermal Growth Factor Receptor 2 Positive (HER2+) Metastatic Breast Cancer

Recruiting·SSCRI Development Innovations, LLC·Phase 2·NCT05748834·36 enrolled

Efficacy and Safety of the Combination of Trastuzumab Plus TUCAtinib Plus viNorelbine in Patients With HER2-positive Non-resectable Locally Advanced or Metastatic Breast Cancer

Terminated·SSpanish Breast Cancer Research Group·Phase 2·NCT05583110·13 enrolled

Treatment With Tucatinib in Patients With an Isolated Brain Progression of a Metastatic Breast Cancer

Active, not recruiting·UUNICANCER·Phase 2·NCT05041842·53 enrolled

A Study of Tucatinib Plus Trastuzumab Deruxtecan in HER2+ Breast Cancer

Completed· Pfizer logo

Pfizer·Phase 2·NCT04539938·70 enrolled

Tucatinib and Trastuzumab in HER3-mutant and HER2-not Amplified Metastatic Breast Cancer

Recruiting·IInstitut Curie·Phase 2·NCT07193394·20 enrolled

A Study of Tucatinib (ONT-380) Combined With Ado-trastuzumab Emtansine (T-DM1) in Patients With HER2+ Breast Cancer

Completed· Pfizer logo

Pfizer·Phase 1·NCT01983501·57 enrolled

Capecitabine, Tucatinib, and Intrathecal Trastuzumab for Breast Cancer Patients With Leptomeningeal Disease

Recruiting·UUNICANCER·Phase 2·NCT05800275·30 enrolled

A Phase II, Two-arm, Non-comparative, Multicentre Study of Tucatinib (ONT-380), Pembrolizumab and Trastuzumab in Patients With Pre-treated Advanced HER2-positive Breast Cancer

Terminated·BBreast Cancer Trials, Australia and New Zealand·Phase 2·NCT04789096·31 enrolled

A Phase 2 Open-label, Single Arm Study of MK-7119 in Combination With Trastuzumab and Capecitabine in Participants With Previously Treated Locally Advanced Unresectable or Metastatic HER2+ Breast Carcinoma

Active, not recruiting· Pfizer logo

Pfizer·Phase 2·NCT04721977·66 enrolled

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

Active, not recruiting·CCriterium, Inc.·Phase 2·NCT05458674·17 enrolled

HER2-positive Breast Cancer5 trials

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

Recruiting· Roche logo

Roche·Preclinical·NCT07413939·650 enrolled

PRE-Investigation of Serial Studies to Predict Your Therapeutic Response With Imaging And moLecular Analysis: A Phase I/II Platform Trial

Recruiting·QQuantumLeap Healthcare Collaborative·Preclinical·NCT05868226·280 enrolled

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 recruiting· Pfizer logo

Pfizer·Phase 3·NCT05132582·654 enrolled

Show 2 more trials

TUCATINIB CONTINUATION PROTOCOL: AN OPEN-LABEL STUDY FOR PARTICIPANTS FROM TUCATINIB CLINICAL STUDIES

Not yet recruiting· Pfizer logo

Pfizer·Approved·NCT07768358·175 enrolled

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 recruiting· Pfizer logo

Pfizer·Phase 3·NCT03975647·466 enrolled

Interaction2 trials

A Drug-Drug Interaction Study in Healthy Volunteers of the Effects of Tucatinib on Metformin

Completed· Pfizer logo

Pfizer·Phase 1·NCT03826602·18 enrolled

A Drug-Drug Interaction Study in Healthy Volunteers of the Effects of Tucatinib

Completed· Pfizer logo

Pfizer·Phase 1·NCT03723395·116 enrolled

Breast Neoplasms2 trials

HERTHENA-Breast-01: A Phase 1b/2, Multicenter, Open-label, Dose-Finding Study to Evaluate the Safety and Antitumor Activity of Patritumab Deruxtecan in Participants With HER2 Positive Unresectable Locally Advanced Breast Cancer or Metastatic Breast Cancer

Recruiting· Merck & Co. logo

Merck & Co.·Preclinical·NCT06686394·181 enrolled

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

Active, not recruiting· Pfizer logo

Pfizer·Phase 2·NCT06157892·54 enrolled

Abemaciclib1 trial

Tucatinib + Abemaciclib + Herceptin for HER2+ MBC

Withdrawn·—·Phase 1·NCT03846583

26 more indications

MPA1 trial

A Safety Study of Tucatinib in Healthy and Hepatically-Impaired Subjects

Completed· Pfizer logo

Pfizer·Phase 1·NCT03722823·37 enrolled

Metastatic Colorectal Cancer1 trial

Tucatinib Combined with Trastuzumab and TAS-102 for the Treatment of HER2 Positive Metastatic Colorectal Cancer in Molecularly Selected Patients, 3T Study

Withdrawn·—·Phase 2·NCT05356897

Colorectal Cancer1 trial

Tucatinib Plus Trastuzumab in Patients With HER2+ Colorectal Cancer

Completed· Pfizer logo

Pfizer·Phase 2·NCT03043313·117 enrolled

Cancer1 trial

Safety and Pharmacokinetics of Tucatinib (MK-7119) in Chinese Participants With Cancer (MK-7119-002)

Active, not recruiting· Pfizer logo

Pfizer·Phase 1·NCT05382364·25 enrolled

Intestinal Cancer1 trial

Tucatinib Plus Trastuzumab and Oxaliplatin-based Chemotherapy or Pembrolizumab-containing Combinations for HER2+ Gastrointestinal Cancers

Active, not recruiting· Pfizer logo

Pfizer·Phase 2·NCT04430738·40 enrolled

Trial1 trial

Canadian Profiling and Targeted Agent Utilization Trial (CAPTUR)

Recruiting·CCanadian Cancer Trials Group·Phase 2·NCT03297606·720 enrolled

Capecitabine1 trial

Tucatinib, Trastuzumab, and Capecitabine for the Treatment of HER2+ LMD

Terminated·UUniversity of Alabama at Birmingham·Phase 2·NCT03501979·17 enrolled

Surgery1 trial

A Study of Tucatinib Given Before Surgery to People With HER2+ Cancers That Have Spread to the Brain

Active, not recruiting·MMemorial Sloan Kettering Cancer Center·Phase 2·NCT05892068·9 enrolled

Advanced1 trial

Trial of ZW25 (Zanidatamab) in Patients With Advanced HER2-expressing Cancers

Completed· Jazz Pharmaceuticals logo

Jazz Pharmaceuticals·Phase 1·NCT02892123·279 enrolled

Esophageal Cancer1 trial

Tucatinib, Trastuzumab, Ramucirumab, and Paclitaxel Versus Paclitaxel and Ramucirumab in Previously Treated HER2+ Gastroesophageal Cancer

Completed· Pfizer logo

Pfizer·Phase 2/3·NCT04499924·17 enrolled

HER2 Positive1 trial

A Safety and Activity Study of SBT6050 in Combination With Other HER2-directed Therapies for HER2-positive Cancers

Terminated·SSilverback Therapeutics·Phase 1/2·NCT05091528·2 enrolled

Cardiac Repolarization1 trial

Effects of Tucatinib on Cardiac Repolarization in Healthy Participants

Completed· Pfizer logo

Pfizer·Phase 1·NCT03777761·55 enrolled

Advanced Solid Tumors1 trial

A Study Evaluating Targeted Therapies in Participants Who Have Advanced Solid Tumors With Genomic Alterations or Protein Expression Patterns Predictive of Response

Completed· Roche logo

Roche·Phase 2·NCT04632992·252 enrolled

Rectal Cancer1 trial

A Study of Tucatinib and Trastuzumab in People With Rectal Cancer

Recruiting·MMemorial Sloan Kettering Cancer Center·Phase 2·NCT05672524·37 enrolled

Absorption1 trial

A Study of the Absorption, Metabolism, and Excretion of Tucatinib in Healthy Participants

Completed·CCascadian Therapeutics Inc.·Phase 1·NCT03758339·8 enrolled

Osimertinib1 trial

Osimertinib, Cetuximab, and Tucatinib for the Treatment of EGFR-Mutant Stage IV or Recurrent Non-small Lung Cell Cancer

Not yet recruiting·JJonathan Riess·Phase 1·NCT06067776·36 enrolled

Colon Cancer1 trial

Exploiting Circulating Tumour DNA to Intensify the Postoperative Treatment Resected Colon Cancer Patients

Suspended·GGruppo Oncologico del Nord-Ovest·Phase 2·NCT05062889·477 enrolled

Resistance1 trial

ASCEND-CRC: Profiling and Targeting Dynamic Tumor Resistance in Patients With Metastatic Colorectal Cancer

Recruiting·MM.D. Anderson Cancer Center·Phase 1·NCT07318389·100 enrolled

Lymphoma, Non-Hodgkin1 trial

Targeted Agent and Profiling Utilization Registry (TAPUR) Study

Recruiting·AAmerican Society of Clinical Oncology·Phase 2·NCT02693535·4,200 enrolled

Uterine Neoplasms1 trial

A Phase 2 Basket Study of Tucatinib in Combination With Trastuzumab in Subjects With Previously Treated, Locally Advanced Unresectable or Metastatic Solid Tumors Driven by HER2 Alterations

Active, not recruiting· Pfizer logo

Pfizer·Phase 2·NCT04579380·217 enrolled

Breast Cancer Female1 trial

A Single-Arm, Phase II Study of Sequential Therapy With Curative Intent in de Novo HER2+ Metastatic Breast Cancer: The SAPPHO Study

Recruiting·DDana-Farber Cancer Institute·Phase 2·NCT06439693·72 enrolled

Colorectal Neoplasms1 trial

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

Recruiting· Pfizer logo

Pfizer·Phase 3·NCT05253651·400 enrolled

Metastatic Solid Tumor1 trial

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)

Recruiting·MM.D. Anderson Cancer Center·Phase 2·NCT05673928·30 enrolled

Advanced Cancer1 trial

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

Active, not recruiting·OOnKure, Inc.·Phase 1·NCT06239467·200 enrolled

Brain Metastases1 trial

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

Active, not recruiting·CCarey Anders, M.D.·Phase 2·NCT05323955·48 enrolled

Unspecified1 trial

A Safety, Tolerability, and Pharmacokinetic Study of Tucatinib in Healthy Japanese and Caucasian Subjects

Completed· Pfizer logo

Pfizer·Phase 1·NCT03914755·36 enrolled

Regulatory

FDA Approval Timeline[5]

Apr 17, 2020

TUKYSA

NDA NDA213411

Apr 17, 2020

TUKYSA

NDA NDA213411

Jan 19, 2023

TUKYSA

NDA NDA213411

Sources

References

[1]
ClinicalTrials.gov — 63 trial records for Tucatinib. U.S. National Library of Medicine, National Institutes of Health.
[2]
MedlinePlus Drug Information — Tukysa drug information. U.S. National Library of Medicine, National Institutes of Health.
[3]
ChEMBL — Tucatinib compound record. European Bioinformatics Institute (EMBL-EBI).
[4]
Open Targets Platform — Drug–disease associations for Tucatinib. EMBL-EBI & Wellcome Sanger Institute.
[5]
OpenFDA — FDA approval records (NDA NDA213411). U.S. Food & Drug Administration.
[6]
FDA Orange Book — Patent and exclusivity data for Tukysa. U.S. Food & Drug Administration.
[7]
PubMed — 2 publications indexed for Tucatinib. U.S. National Library of Medicine.
[8]
SEC EDGAR — Pfizer company filings. U.S. Securities and Exchange Commission.

Details

Drug Info

Quick Facts

Mechanism of Action: HER2 Kinase Inhibitor[3]
Modality: Small molecule[3]
Highest Phase: Approved[1]
Company: Pfizer

Patent Landscape[6]

Patent Cliff

May 9, 2027

Earliest patent expiration — generic entry possible after this date

Patent #Expires

9693989May 9, 2027

8648087Jan 14, 2031

9457093Oct 12, 2032

11504370Mar 25, 2033

12048698Apr 27, 2038

2 more patents

11207324Apr 27, 2038

11666572Apr 27, 2038

Key Publications[7]

Tucatinib Plus Trastuzumab for HER2+ mBC With Brain Metastases

N Engl J MedApr 12, 2023DOI: 10.1056/NEJMoa2303026

Tucatinib Plus Trastuzumab in HER2+ Colorectal Cancer: MOUNTAINEER

N Engl J MedFeb 2, 2023DOI: 10.1056/NEJMoa2214846

Tukysa

Status by Indication[4][1]

Competitive Landscape

Expected Milestones

Q4 2026

Q1 2027

Q2 2027

Trials by Indication[1]

Breast Cancer27 trials

HER2-positive Breast Cancer5 trials

Interaction2 trials

Breast Neoplasms2 trials

Abemaciclib1 trial

MPA1 trial

Metastatic Colorectal Cancer1 trial

Colorectal Cancer1 trial

Cancer1 trial

Intestinal Cancer1 trial

Trial1 trial

Capecitabine1 trial

Surgery1 trial

Advanced1 trial

Esophageal Cancer1 trial

HER2 Positive1 trial

Cardiac Repolarization1 trial

Advanced Solid Tumors1 trial

Rectal Cancer1 trial

Absorption1 trial

Osimertinib1 trial

Colon Cancer1 trial

Resistance1 trial

Lymphoma, Non-Hodgkin1 trial

Uterine Neoplasms1 trial

Breast Cancer Female1 trial

Colorectal Neoplasms1 trial

Metastatic Solid Tumor1 trial

Advanced Cancer1 trial

Brain Metastases1 trial

Unspecified1 trial

FDA Approval Timeline[5]

References

Drug Info

Quick Facts

Patent Landscape[6]

Key Publications[7]

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