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

NCT03758339 | Completed Phase 1 FDA Drug

• 1 other identifier: ONT-380-008
• Study Type: interventional
• Target: 8
• Locations: 1 country
• Sites: 1

Brief Summary

This study will look at how a drug (tucatinib) leaves the body and what happens to tucatinib while it is still in the body. Healthy participants will get one dose of tucatinib by mouth. Patients will be monitored for 8-14 days after they take the dose of tucatinib.

Conditions

Healthy

Outcome Measures

Primary Outcomes (18)

• Area under the concentration-time curve (AUC) from time 0 to infinity (AUC[0-inf])

  PK outcome parameter for tucatinib, ONT-993, and total radioactivity derived from the whole blood and plasma concentration-time profiles

  Up to 14 days

• AUC from time 0 to last quantifiable concentration

  PK outcome parameter for tucatinib, ONT-993, and total radioactivity derived from the whole blood and plasma concentration-time profiles

  Up to 14 days

• Maximum observed concentration

  PK outcome parameter for tucatinib, ONT-993, and total radioactivity derived from the whole blood and plasma concentration-time profiles

  Up to 14 days

• Time of maximum observed concentration

  PK outcome parameter for tucatinib, ONT-993, and total radioactivity derived from the whole blood and plasma concentration-time profiles

  Up to 14 days

• Apparent terminal elimination half-life

  PK outcome parameter for tucatinib, ONT-993, and total radioactivity derived from the whole blood and plasma concentration-time profiles

  Up to 14 days

• Apparent total clearance

  PK outcome parameter for tucatinib derived from the whole blood and plasma concentration-time profiles

  Up to 14 days

• Apparent volume of distribution

  PK outcome parameter for tucatinib derived from the whole blood and plasma concentration-time profiles

  Up to 14 days

• AUC[0-inf] plasma tucatinib/total radioactivity ratio

  AUC\[0-inf\] of plasma tucatinib relative to AUC\[0-inf\] of plasma total radioactivity

  Up to 14 days

• AUC[0-inf] blood/plasma ratio

  AUC\[0-inf\] of whole blood total radioactivity to AUC\[0-inf\] of plasma total radioactivity

  Up to 14 days

• Amount excreted in urine (Aeu)

  PK outcome endpoint of tucatinib, ONT-993, and total radioactivity derived from urine collections

  Up to 14 days

• Cumulative Aeu

  PK outcome endpoint of tucatinib, ONT-993, and total radioactivity derived from urine collections

  Up to 14 days

• Percentage excreted in urine (Feu)

  PK outcome endpoint of tucatinib and total radioactivity derived from urine collections

  Up to 14 days

• Cumulative Feu

  PK outcome endpoint of tucatinib and total radioactivity derived from urine collections

  Up 14 days

• Renal clearance

  PK outcome endpoint of tucatinib derived from urine collections

  Up to 14 days

• Amount excreted in feces [Aef]

  PK outcome endpoint of total radioactivity derived from feces collection

  Up to 14 days

• Cumulative Aef

  PK outcome endpoint of total radioactivity derived from feces collection

  Up to 14 days

• Percentage excreted in feces [Fef]

  PK outcome endpoint of total radioactivity derived from feces collection

  Up to 14 days

• Cumulative Fef

  PK outcome endpoint of total radioactivity derived from feces collection

  Up to 14 days

Secondary Outcomes (3)

• Relative abundance of tucatinib and its metabolites eliminated in urine and feces

  Up to 14 days

• Relative abundance of tucatinib and its metabolites in plasma

  Up to 14 days

• Incidence of adverse events (AEs)

  Up to 14 days

Study Arms (1)

Tucatinib

EXPERIMENTAL

Drug: tucatinib

Interventions

tucatinib DRUG

Single dose of 300 mg of \[¹⁴C\]-tucatinib containing approximately 150 μCi of \[¹⁴C\] radioactivity

Tucatinib

Eligibility Criteria

• Age: 18 Years - 65 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• In good health, determined by no clinically significant findings from medical history, physical examination, 12-lead ECG, vital signs measurements, or lab evaluations
• Body mass index (BMI) between 18 and 32 kg/m²
• Weight between 50 and 100 kg
• Females must be of non-childbearing potential
• Males must agree to use contraception

You may not qualify if:

• History of any metabolic, allergic, dermatological, hepatic, renal, hematological, pulmonary, cardiovascular, gastrointestinal, neurological, respiratory, endocrine, or psychiatric disorder
• Any condition affecting drug absorption
• History of hypersensitivity or allergy to any drug compound, food, or other substance
• History of alcoholism or drug/chemical abuse within 2 years
• Use of prescription products within 28 days prior to check in
• Use of tobacco- or nicotine-containing products within 3 months prior to check in

Sponsors & Collaborators

• Cascadian Therapeutics Inc.: lead

Study Sites (1)

Covance Clinical Research Unit

Madison, Wisconsin, 53704, United States

Location

MeSH Terms

Interventions

tucatinib

Study Officials

• Alex Vo, PhD

  Cascadian Therapeutics Inc.

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NA
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: November 13, 2018
• First Posted: November 29, 2018
• Study Start: December 30, 2017
• Primary Completion: January 30, 2018
• Study Completion: January 30, 2018
• Last Updated: November 29, 2018

Record last verified: 2018-11

Data Sharing

• IPD Sharing: Will not share

Locations

US (1)