NCT07372625

A Study to Investigate the Effects of Multiple Doses of Rezatapopt on the Pharmacokinetics of Metformin, Rosuvastatin, Repaglinide, and Midazolam in Patients With Advanced Solid Tumors Harboring a TP53 Y220C Mutation.

A Phase 1, Open-label, 2-part, Drug-Drug Interaction Study to Evaluate the Effects of Multiple Oral Doses of Rezatapopt on the Pharmacokinetics of Metformin, Rosuvastatin, Repaglinide, and Midazolam in Patients With Advanced Solid Tumors Harboring a TP53 Y220C Mutation.

• Status: Recruiting
• Phase: Phase 1
• Study type: Interventional
• Enrollment: 14 (estimated)
• Sponsor: PMV Pharmaceuticals, Inc · Industry
• Sex: All
• Age: 18 Years
• Healthy volunteers: Not accepted

Summary

This study aims to evaluate the effects of rezatapopt on the pharmacokinetics of metformin, rosuvastatin, repaglinide, and midazolam in patients with advanced solid tumors harboring a TP53 Y220C mutation.

Detailed description

Rezatapopt (PC14586) is a first-in-class oral, small molecule p53 reactivator that is selective for the TP53 Y220C mutation. This Phase 1, open-label, drug-drug interaction study will investigate the effect of multiple oral doses of rezatapopt on the pharmacokinetics (PK) of metformin, rosuvastatin, repaglinide, and midazolam in patients with advanced solid tumors harboring a TP53 Y220C mutation. This study will consist of 2 parts, Part A and Part B. Part A is a 24-day drug-drug interaction (DDI) portion that follows a fixed- sequence design, including a screening period and 2 treatment periods. In Treatment Period 1 patients will receive metformin and rosuvastatin, followed by repaglinide and midazolam. Patients will not receive rezatapopt during Treatment Period 1. Following washout, in Treatment Period 2 which will begin on Day 6, patients will receive 2000 mg rezatapopt administered orally once daily along with metformin and rosuvastatin, and then repaglinide and midazolam in accordance with the fixed-sequence dosing schedule. Serial PK samples will be collected on designated days throughout Part A. Patients who complete Part A without suspected disease progression and unacceptable toxicity or another discontinuation criterion and who are deemed likely to continue benefiting from the study treatment, will be allowed to continue treatment with rezatapopt in Part B. In Part B, patients will receive 2000 mg rezatapopt orally daily in 21-day cycles, up to Cycle 33 (approximately 2 years of rezatapopt treatment, inclusive of Part A) or until another discontinuation criterion is met. A maximum of approximately 14 patients are planned to enroll in this study.

Conditions

• TP53 Y220C Mutation
• Advanced Solid Tumors

Interventions

Type	Name	Description
DRUG	metformin hydrochloride 500 mg tablet	500-mg immediate release tablet PO
DRUG	rosuvastatin 10 mg tablet	10-mg tablet PO
DRUG	repaglinide 0.5 mg tablet	0.5-mg tablet PO
DRUG	midazolam hydrochloride syrup	2 mg dose (5-mg/2.5 mL syrup) PO
DRUG	rezatapopt	2000 mg dose (4 x 500-mg tablets) PO

Timeline

• Start date: 2026-02-04
• Primary completion: 2027-03-01
• Completion: 2028-01-01
• First posted: 2026-01-28
• Last updated: 2026-03-12

Locations

5 sites across 1 country: United States

Regulatory

• FDA-regulated drug study