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.
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.
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.