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

A Phase 1 Clinical Study to Investigate the Safety and Pharmacokinetics of Tucatinib (MK-7119) in China Participants With HER2+ Advanced Breast Cancer, Gastric or Gastroesophageal Junction Adenocarcinoma and Colorectal Cancer

The primary purpose of this study is to characterize the safety and tolerability of tucatinib (MK-7119) in Chinese participants with human epidermal growth factor receptor 2 positive (HER2+) advanced breast cancer, gastric or gastroesophageal junction adenocarcinoma (GEC), and colorectal cancer.

Study Overview

• Status: Active, not recruiting
• Conditions: Breast Neoplasms; Colorectal Cancer; Metastatic HER2+ Advanced Breast Cancer; Gastric or Gastroesophageal Junction Adenocarcinoma (GEC)
• Intervention / Treatment: Drug: Tucatinib

• Study Type: Interventional
• Enrollment (Actual): 25
• Phase: Phase 1

Contacts and Locations

Study Locations

• China
  • Shanghai, China, 201321
    • Fudan University Shanghai Cancer Center
  • Tianjin, China, 300060
    • Tianjin Medical University Cancer Institute and Hospital
  • Heilongjiang
    • Harbin, Heilongjiang, China, 150081
      • Harbin medical university cancer hospital
  • Hunan
    • Changsha, Hunan, China, 421000
      • Hunan Cancer Hospital
  • Jilin
    • Changchun, Jilin, China, 130012
      • Jilin Cancer Hospital

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years and older (Adult, Older Adult)
• Accepts Healthy Volunteers: No

Description

Inclusion Criteria:

• Histologically or cytologically confirmed HER2+ advanced breast cancer, gastric or GEC, and colorectal cancer
• Have progressed at least one previous therapeutic regimen and either no longer are candidates for standard therapy, have no standard therapy available, or choose not to pursue standard therapy
• Have a performance status of 0 or 1 on the Eastern Cooperative Oncology Group (ECOG) Performance within 7 days prior to allocation
• Has life expectancy >6 months in the opinion of the investigator
• Have measurable disease per Response Evaluation Criteria in Solid Tumours (RECIST) 1.1 as assessed by the local site investigator/radiologist
• Must test negative for hepatitis B surface antigen (HBsAg)
• If there is a history of hepatitis C virus (HCV) infection, has undetectable HCV viral load at screening
• For males, agree to be abstinent from heterosexual intercourse, or agree to use acceptable contraception, for the duration of study and 1 week after
• For females, is not pregnant or breastfeeding AND one of the following applies:
• Is not a woman of childbearing potential (WOCBP)
• Is a WOCBP and uses highly effective contraception and is not pregnant

Exclusion Criteria:

• History of prior cancer within <3 year, except for adequately treated basal cell or squamous cell carcinoma of the skin, cervical cancer in situ, or other in situ carcinomas which needs discussion between the investigator and the Sponsor
• Participants with leptomeningeal disease are excluded
• Has symptomatic central nervous system (CNS) metastases
• Has active human immunodeficiency virus (HIV), hepatitis B virus, or HCV infection
• Has had chemotherapy, immunotherapy, radioimmunotherapy, definitive radiation, or biological cancer therapy or treatment with an investigational product within 4 weeks (2 weeks for palliative radiation) before the first dose of study intervention
• Has an active infection requiring therapy
• Has refractory nausea/vomiting, chronic gastrointestinal disease, or significant bowel resection
• Has a history or current evidence of any condition, therapy, or laboratory abnormality that might confound the results of the study
• Has a QTc prolongation
• Has uncontrolled illness including but not limited to ongoing symptomatic congestive heart failure (New York Heart Association [NYHA] Class III or IV heart failure), unstable angina pectoris, cardiac arrhythmia, and psychiatric illness that would limit compliance with study requirements
• Has had major surgery within 4 weeks prior to first dose of study intervention
• Is currently participating in another clinical trial
• Has psychiatric or substance abuse disorder

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: N/A
• Interventional Model: Single Group Assignment
• Masking: None (Open Label)

Number of Arms

1

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Tucatinib Treatment; Chinese participants with HER2+ advanced breast cancer, gastric or gastroesophageal junction adenocarcinoma, or colorectal cancer receive tucatinib 300 mg by mouth twice daily during 21-day cycles. Treatment continues until there is evidence of unacceptable toxicity or documented progression.	Drug: Tucatinib; Tucatinib 150 mg and 50 mg tablets taken by mouth at a dose of 300 mg twice daily.; Other Names: MK-7119

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Percentage of participants with ≥1 adverse event (AE)	An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of study intervention, whether or not considered related to the study intervention.	Up to approximately 2.5 years
Percentage of participants discontinuing from study therapy due to AE	An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of study intervention, whether or not considered related to the study intervention.	Up to approximately 2.5 years

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Maximum plasma concentration (Cmax) of first dose of tucatinib	The Cmax of tucatinib will be determined after the first dose.	Cycle 1, Day 1: predose and 0.5, 1, 2, 3, 4, 6, 8, 10, and 12 hours postdose
Time of maximum plasma concentration (Tmax) of first dose of tucatinib	The Tmax of tucatinib will be determined after the first dose.	Cycle 1, Day 1: predose and 0.5, 1, 2, 3, 4, 6, 8, 10, and 12 hours postdose
Area under the plasma concentration time curve from dosing to 12 hours postdose (AUC0-12) of first dose of tucatinib	The AUC0-12 of tucatinib will be determined after the first dose.	Cycle 1, Day 1: predose and 0.5, 1, 2, 3, 4, 6, 8, 10, and 12 hours postdose
Apparent plasma half-life (t½) of first dose of tucatinib	The t½ of tucatinib will be determined after the first dose.	Cycle 1, Day 1: predose and 0.5, 1, 2, 3, 4, 6, 8, 10, and 12 hours postdose
Apparent clearance (CL/F) of first dose of tucatinib	The CL/F of tucatinib will be determined after the first dose.	Cycle 1, Day 1: predose and 0.5, 1, 2, 3, 4, 6, 8, 10, and 12 hours postdose
Volume of distribution (Vz/F) of first dose of tucatinib	The Vz/F of tucatinib will be determined after the first dose.	Cycle 1, Day 1: predose and 0.5, 1, 2, 3, 4, 6, 8, 10, and 12 hours postdose
Trough concentration (Ctrough) of tucatinib at steady state	The Ctrough of tucatinib will be determined at steady state.	Cycle 1, Days 8 and 15: predose and 0.5, 1, 2, 3, 4, 6, 8, 10, and 12 hours postdose
Accumulation ratio of tucatinib at steady state	The accumulation ratio of tucatinib will be determined at steady state.	Cycle 2, Day 1: predose and 0.5, 1, 2, 3, 4, 6, 8, 10, and 12 hours postdose
Cmax at steady state (Cmaxss) of tucatinib	The Cmaxss of tucatinib will be determined at steady state.	Cycle 2, Day 1: predose and 0.5, 1, 2, 3, 4, 6, 8, 10, and 12 hours postdose
Tmax at steady state (Tmaxss) of tucatinib	The Tmaxss of tucatinib will be determined at steady state.	Cycle 2, Day 1: predose and 0.5, 1, 2, 3, 4, 6, 8, 10, and 12 hours postdose
AUC0-12 at steady state (AUC0-12ss) of tucatinib	The AUC0-12ss of tucatinib will be determined at steady state.	Cycle 2, Day 1: predose and 0.5, 1, 2, 3, 4, 6, 8, 10, and 12 hours postdose
t½ of tucatinib at steady state	The t½ of tucatinib will be determined at steady state.	Cycle 2, Day 1: predose and 0.5, 1, 2, 3, 4, 6, 8, 10, and 12 hours postdose
CL/F at steady state (CL/Fss) of tucatinib	The CL/Fss of tucatinib will be determined at steady state.	Cycle 2, Day 1: predose and 0.5, 1, 2, 3, 4, 6, 8, 10, and 12 hours postdose
Vz/F at steady state (Vz/Fss) of tucatinib	The Vz/Fss of tucatinib will be determined at steady state.	Cycle 2, Day 1: predose and 0.5, 1, 2, 3, 4, 6, 8, 10, and 12 hours postdose
Objective Response Rate (ORR) per Response Evaluation Criteria In Solid Tumors Version 1.1 (RECIST 1.1)	ORR is defined as the percentage of participants who have a Complete Response (CR: disappearance of all target lesions) or a Partial Response (PR: at least a 30% decrease in the sum of diameters of target lesions) per RECIST 1.1. The percentage of participants who experience a CR or PR based on RECIST 1.1 will be presented.	Up to approximately 19 months
Duration of Response (DOR) Per Response Evaluation Criteria In Solid Tumors Version 1.1 (RECIST 1.1)	For participants who demonstrate a confirmed complete response (CR: Disappearance of all target lesions) or confirmed Partial Response (PR: At least a 30% decrease in the sum of diameters of target lesions) per RECIST 1.1, DOR is defined as the time from first documented evidence of CR or PR until disease progression or death.	Up to approximately 19 months

Collaborators and Investigators

• Sponsor: Pfizer
• Investigators: Study Director: Pfizer CT.gov Call Center, Pfizer

Publications and helpful links

Helpful Links

• To obtain contact information for a study center near you, click here.

Study record dates

Study Major Dates

• Study Start (Actual): June 29, 2022
• Primary Completion (Estimated): December 31, 2026
• Study Completion (Estimated): December 31, 2026

Study Registration Dates

• First Submitted: May 16, 2022
• First Submitted That Met QC Criteria: May 16, 2022
• First Posted (Actual): May 19, 2022

Study Record Updates

• Last Update Posted (Actual): March 12, 2026
• Last Update Submitted That Met QC Criteria: March 11, 2026
• Last Verified: March 1, 2026

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Neoplasms by Site; Neoplasms; Intestinal Diseases; Gastrointestinal Neoplasms; Digestive System Neoplasms; Digestive System Diseases; Gastrointestinal Diseases; Intestinal Neoplasms; Rectal Diseases; Colonic Diseases; Skin Diseases; Breast Diseases; Skin and Connective Tissue Diseases; Colorectal Neoplasms; Breast Neoplasms; Antineoplastic Agents; Molecular Mechanisms of Pharmacological Action; Enzyme Inhibitors; Protein Kinase Inhibitors; tucatinib
• Other Study ID Numbers: MK-7119-002 (Merck); 7119-002 (Other Identifier: Alias Study Number); C4251016 (Other Identifier: Alias Study Number)

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: NO
• IPD Plan Description: http://engagezone.msd.com/doc/ProcedureAccessClinicalTrialData.pdf

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: Yes
• Studies a U.S. FDA-regulated device product: No
• product manufactured in and exported from the U.S.: Yes