RecruitingPhase 1NCT07524322

Study of RGT-490 in Patients With PIK3CA-Mutated Advanced Solid Tumors

A Phase 1/1b Open-Label, Multicenter, First-in-Human Study Evaluating Safety, Tolerability, Pharmacokinetics, and Antitumor Activity of RGT-490 as a Single Agent in Adult Subjects With Locally Advanced or Metastatic PIK3CA-Mutated Solid Tumors Including HR+/HER2- Breast Cancers

Sponsor

Regor Pharmaceuticals Inc.

Enrollment

63 participants

Start Date

Apr 1, 2026

Study Type

INTERVENTIONAL

Conditions

Breast Cancer Ovarian Cancer Endometrial Cancer PIK3CA Mutation

Summary

This is a phase 1/1b, open-label, multicenter study consisting of sequential parts designed to evaluate the safety, tolerability, and effects pharmacokinetic (PK) profile, and antitumor activity of RGT-490, an investigational oral therapy, in adults with locally advanced or metastatic solid tumors including breast cancer. Participants enrolled in the study have advanced disease that is not amendable to curative treatment and whose tumors harbor alterations in the PI3KCA gene.

Eligibility

Min Age: 18 Years

Inclusion Criteria5

Adults with metastatic or locally advanced, unresectable solid tumors that have progressed on or after at least one available therapy.
Presence of one or more documented activating PIK3CA mutation in tumor tissue and/or blood.
At least 1 measurable lesion or evaluable disease per RECIST v1.1.
An ECOG performance status of 0 or 1.
Adequate organ function

Exclusion Criteria6

Diabetes mellitus requiring anti-hyperglycemic medication.
Prior treatment with PI3Kα inhibitors
Symptomatic, untreated, or uncontrolled central nervous system metastases.
Receipt of any local or systemic anticancer therapy or investigational anticancer agent within a protocol-defined washout period prior to study treatment.
Unresolved clinically significant toxicities from prior anticancer therapy
History of a another malignancy within 2 years prior to screening (exception adequately treated cancers).