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

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.

Inclusion Criteria:

• 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 Criteria:

• 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).