NCT06899061

Modular Clinical Pharmacology Study to Evaluate the Drug-drug Interaction Potential and Relative Bioavailability of Saruparib

A Modular Phase I, Open-label Study to Assess the Safety, Pharmacokinetics, and Drug Interaction Potential and Relative Bioavailability of Saruparib in Patients With Advanced Solid Malignancies

• Status: Active Not Recruiting
• Phase: Phase 1
• Study type: Interventional
• Enrollment: 41 (actual)
• Sponsor: AstraZeneca · Industry
• Sex: All
• Age: 18 Years
• Healthy volunteers: Not accepted

Summary

A Phase I modular study to assess the effect of oral saruparib on other treatments in patients with advanced solid malignancies.

Detailed description

Module 1 of the study is a Phase I, open-label study to assess the effects of saruparib on the PK of substrates digoxin (P-gp), furosemide (OAT1/3), metformin hydrochloride (OCT2/MATE1/2K), and rosuvastatin (OATP1B1/3) in participants with advanced solid malignancies. Module 2 of the study is a Phase I, open-label, 4-treatment period, multi-centre, relative bioavailability, PPI effect, randomised, crossover study of saruparib tablets manufactured using a direct compression (DC) process in participants with advanced solid malignancies. Module 1 of the study will include: * A Screening period of 28 days prior to Day 1. * Period 1: a single dose of a cocktail of substrates (digoxin, furosemide, metformin hydrochloride, and rosuvastatin) on Day 1. * A washout period of 1 to 3 days between Period 1 and Period 2. * Period 2: continuous dosing of saruparib from Day 1 to Day 9. On Day 5 saruparib will be administered in combination with the cocktail of substrates. * Period 3: a dose of saruparib per day for up to 3 cycles of 28 days each. * An End of Study visit up to 3 days after the last dose in Period 3. Module 2 of the study will include: * A Screening period of 28 days prior to Day 1. * Period 1 and Period 2: a single dose of roller compaction (RC) or DC saruparib. * Period 3: from Day 1 to 3, two doses of rabeprazole per day. On Day 4, a dose of rabeprazole followed by DC saruparib. * A washout period of at least 3 days between Period 1 and Period 3, and between Period 2 and Period 3. * Period 4: a single dose of RC saruparib for up to 3 cycles. * An End of Study visit up to 3 days after the last dose in Period 4.

Conditions

• Advanced Solid Malignancies

Interventions

Type	Name	Description
DRUG	Saruparib	Module 1: Period 2: participants will receive saruparib orally once daily from Day 1 to Day 9. On Day 5 saruparib will be administered orally in combination with the cocktail of substrates. Period 3: participants will receive saruparib orally once daily for up to 3 cycles of 28 days each. Module 2: Period 1 and Period 2: participants will receive a single oral dose of DC or RC saruparib. Period 3: participants will receive an oral dose of rabeprazole twice daily from Day 1 to 3, and a single oral dose of rabeprazole prior to DC saruparib on Day 4. Period 4: participants will receive an oral dose of RC saruparib daily for 3 cycles.
DRUG	Digoxin	Period 1: participants will receive a single oral dose of a cocktail of substrates (digoxin, furosemide, metformin hydrochloride, and rosuvastatin) on Day 1. Period 2: participants will receive a single oral dose of the cocktail of substrates in combination with saruparib on Day 5.
DRUG	Furosemide	Period 1: participants will receive a single oral dose of a cocktail of substrates (digoxin, furosemide, metformin hydrochloride, and rosuvastatin) on Day 1. Period 2: participants will receive a single oral dose of the cocktail of substrates in combination with saruparib on Day 5.
DRUG	Metformin Hydrochloride	Period 1: participants will receive a single oral dose of a cocktail of substrates (digoxin, furosemide, metformin hydrochloride, and rosuvastatin) on Day 1. Period 2: participants will receive a single oral dose of the cocktail of substrates in combination with saruparib on Day 5.
DRUG	Rosuvastatin	Period 1: participants will receive a single oral dose of a cocktail of substrates (digoxin, furosemide, metformin hydrochloride, and rosuvastatin) on Day 1. Period 2: participants will receive a single oral dose of the cocktail of substrates in combination with saruparib on Day 5.
DRUG	Rabeprazole	Period 3: Participants will receive two doses of rabeprazole per day from Day 1 to 3. On Day 4, participants will receive a dose of rabeprazole followed by DC saruparib.

Timeline

• Start date: 2025-03-25
• Primary completion: 2026-02-03
• Completion: 2026-04-30
• First posted: 2025-03-27
• Last updated: 2026-03-27

Locations

4 sites across 3 countries: Bulgaria, Moldova, Romania