Tucatinib

Generic Name: Tucatinib

Brand Names: Tukysa

Drug Type: Small Molecule

Chemical Formula: C_₂₆H_₂₄N_₈O_₂

CAS Number: 937263-43-9

Unique Ingredient Identifier: 234248D0HH

Background: Tucatinib is a kinase inhibitor drug used with trastuzumab and capecitabine in the treatment of unresectable or metastatic HER-2 positive breast cancer. It was developed by Seattle Genetics and approved by the FDA on April 17, 2020. Tucatinib is a promising new treatment for patients with metastatic breast cancer who have not responded adequately to other chemotherapy regimens.

Indication: 本品与曲妥珠单抗和卡培他滨联用治疗人类表皮生长因子受体2(HER2)阳性且已出现转移(如脑转移)或无法进行乳房切除术的乳腺癌成人患者，患者应接受过一种或多种抗HER2乳腺癌药物治疗。

Associated Conditions: Breast Cancer, Unresectable Breast Cancer, Wild-type RAS Metastatic Colorectal Cancer, Unresectable RAS Wild Type Colorectal Cancer

Clinical Trials

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

Phase 1

Completed

Conditions: Healthy

Interventions: Drug: Tucatinib

First Posted Date: 2019-04-16

Last Posted Date: 2019-09-06

Lead Sponsor: Seagen Inc.

Target Recruit Count: 36

Registration Number: NCT03914755

Locations: 🇺🇸
PAREXEL International, Early Phase Clinical Unit - Los Angeles, Glendale, California, United States

Tucatinib + Abemaciclib + Herceptin for HER2+ MBC

Phase 1

Withdrawn

Conditions: Breast Cancer

Interventions: Drug: Tucatinib
Drug: Abemaciclib
Drug: Trastuzumab
Drug: Aromatase Inhibitor

First Posted Date: 2019-02-19

Last Posted Date: 2020-10-23

Lead Sponsor: Dana-Farber Cancer Institute

Registration Number: NCT03846583

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

Phase 1

Completed

Conditions: Drug-drug Interaction

Interventions: Drug: Tucatinib
Drug: Metformin
Drug: Iohexol

First Posted Date: 2019-02-01

Last Posted Date: 2019-03-27

Lead Sponsor: Seagen Inc.

Target Recruit Count: 18

Registration Number: NCT03826602

Locations: 🇺🇸
Pharmaceutical Research Associates, Salt Lake City, Utah, United States

Effects of Tucatinib on Cardiac Repolarization in Healthy Participants

Phase 1

Completed

Conditions: Healthy

Interventions: Drug: tucatinib
Drug: placebo
Drug: moxifloxacin

First Posted Date: 2018-12-17

Last Posted Date: 2019-04-12

Lead Sponsor: Seagen Inc.

Target Recruit Count: 55

Registration Number: NCT03777761

Locations: 🇺🇸
Covance Clinical Research Unit - Dallas, Dallas, Texas, United States

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

Phase 1

Completed

Conditions: Healthy

Interventions: Drug: tucatinib

First Posted Date: 2018-11-29

Last Posted Date: 2018-11-29

Lead Sponsor: Cascadian Therapeutics Inc.

Target Recruit Count: 8

Registration Number: NCT03758339

Locations: 🇺🇸
Covance Clinical Research Unit, Madison, Wisconsin, United States

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

Phase 1

Completed

Conditions: Drug-drug Interaction

Interventions: Drug: tucatinib
Drug: repaglinide
Drug: itraconazole
Drug: rifampin
Drug: gemfibrozil
Drug: digoxin
Drug: tolbutamide
Drug: midazolam

First Posted Date: 2018-10-29

Last Posted Date: 2019-12-18

Lead Sponsor: Seagen Inc.

Target Recruit Count: 116

Registration Number: NCT03723395

Locations: 🇺🇸
Covance Clinical Research Unit, Dallas, Texas, United States

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

Phase 1

Completed

Conditions: Hepatic Impairment

Interventions: Drug: Tucatinib

First Posted Date: 2018-10-29

Last Posted Date: 2019-05-20

Lead Sponsor: Seagen Inc.

Target Recruit Count: 37

Registration Number: NCT03722823

Locations: 🇺🇸
Orange County Research Center, Tustin, California, United States
🇺🇸
Orlando Clinical Research Center, Orlando, Florida, United States
🇺🇸
Texas Liver Institute, San Antonio, Texas, United States

and more 1 locations

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

Phase 2

Active, not recruiting

Conditions: Metastatic Breast Cancer
Leptomeningeal Disease

Interventions: Drug: Tucatinib
Drug: Trastuzumab
Drug: Capecitabine

First Posted Date: 2018-04-18

Last Posted Date: 2024-01-11

Lead Sponsor: University of Alabama at Birmingham

Target Recruit Count: 17

Registration Number: NCT03501979

Locations: 🇺🇸
University of Michigan-, Ann Arbor, Michigan, United States
🇺🇸
UCSF-Mission Bay, San Francisco, California, United States
🇺🇸
University of Chicago, Chicago, Illinois, United States

and more 6 locations

Expanded Access Use of Tucatinib for HER2+ Metastatic Breast Cancer

First Posted Date: 2018-02-07

Last Posted Date: 2020-02-25

Lead Sponsor: Seagen Inc.

Registration Number: NCT03424473

Canadian Profiling and Targeted Agent Utilization Trial (CAPTUR)

Phase 2

Recruiting

Conditions: Lymphoma, Non-Hodgkin
Multiple Myeloma
Advanced Solid Tumors

Interventions: Drug: Erlotinib
Drug: Dasatinib
Drug: Axitinib
Drug: Bosutinib
Drug: Crizotinib
Drug: Nivolumab plus Ipilimumab
Drug: Olaparib
Drug: Palbociclib
Drug: Sunitinib
Drug: Temsirolimus
Drug: Trastuzumab plus Pertuzumab
Drug: Vemurafenib plus Cobimetinib
Drug: Vismodegib
Drug: Tucatinib

First Posted Date: 2017-09-29

Last Posted Date: 2025-03-11

Lead Sponsor: Canadian Cancer Trials Group

Target Recruit Count: 720

Registration Number: NCT03297606

Locations: 🇨🇦
London Health Sciences Centre Research Inc., London, Ontario, Canada
🇨🇦
Cross Cancer Institute, Edmonton, Alberta, Canada
🇨🇦
BCCA - Kelowna, Kelowna, British Columbia, Canada

and more 7 locations

Drug Development Updates

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