A Clinical Trial to Investigate the Clinical Drug-Drug Interaction of Divarasib With Probe Substrates of P-Glycoprotein and Breast Cancer Resistance Protein in Healthy Participants

A Phase I, Open-Label, Two-Period, One-Sequence, Crossover Study in Healthy Subjects to Evaluate the Clinical Drug-Drug Interaction of Divarasib With Probe Substrates of P-Glycoprotein (Digoxin) and Breast Cancer Resistance Protein (Rosuvastatin)

Status

Completed

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT06677957

Enrollment

Registered

2024-11-07

Start date

2024-11-06

Completion date

2024-12-30

Last updated

2025-01-03

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Healthy Participants

Brief summary

This is a Phase 1, open-label, two-period, one-sequence, crossover drug-drug interaction study to assess the P-gp and BCRP inhibition potential of divarasib using digoxin and rosuvastatin as probe substrates, respectively, in healthy participants.

Interventions

DRUGDigoxin

Digoxin will be administered together with Rosuvastatin as a drug cocktail as specified for the respective period

DRUGDivarasib

Divarasib will be administered in combination with Digoxin and Rosuvastatin as specified for the respective period

DRUGRosuvastatin

Rosuvastatin will be administered together with Digoxin as a drug cocktail as specified for the respective period

Study design

Allocation

RANDOMIZED

Intervention model

CROSSOVER

Primary purpose

BASIC_SCIENCE

Masking

NONE

Eligibility

Sex/Gender

ALL

Age

18 Years to 60 Years

Healthy volunteers

Yes

Inclusion criteria

* Males or females of non-childbearing potential * Within body mass index (BMI) range of 18.0 to 32.0 kg/m2, inclusive

Exclusion criteria

* Significant history or clinical manifestation of any metabolic, allergic, dermatological, hepatic, renal, hematological, pulmonary, cardiovascular, gastrointestinal (GI), neurological, or psychiatric disorder * History of significant hypersensitivity, intolerance, or allergy to any drug compound, food, or other substance, unless approved by the investigator * Poor peripheral venous access

Design outcomes

Primary

Measure	Time frame
Maximum Observed Plasma Concentration (Cmax) of Digoxin and Rosuvastatin	Day 1 of Period 1 and Day 5 of Period 2
Area Under the Plasma Concentration-Time Curve from Hour 0 to the Last Measurable Concentration (AUC0-t) of Digoxin and Rosuvastatin	Day 1 of Period 1 and Day 5 of Period 2
Area Under the Plasma Concentration-Time Curve (AUC0-inf) of Digoxin and Rosuvastatin	Day 1 of Period 1 and Day 5 of Period 2
Time to Cmax (Tmax) of Digoxin and Rosuvastatin	Day 1 of Period 1 and Day 5 of Period 2

Secondary

Measure	Time frame
Percentage of Participants with Adverse Events (AEs)	From Day 1 until end of study participation (approximately 2 months)

Countries

United States

Outcome results

None listed

Source: ClinicalTrials.gov · Data processed: Feb 4, 2026