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

NCT07524322 | Recruiting Phase 1 FDA Drug

• 1 other identifier: RGT-490-101
• Study Type: interventional
• Target: 63
• Locations: 1 country
• Sites: 3

Brief 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.

Conditions

Breast Cancer; Ovarian Cancer; Endometrial Cancer; PIK3CA Mutation; HER2- Negative Breast Cancer; Advanced Breast Cancer; Unresectable Solid Tumor; Hormone Receptor Positive Tumor; Cervical Cancer

Outcome Measures

Primary Outcomes (2)

• Incidence of dose limiting toxicities (DLTs)

  Number of subjects who experience at least 1 Dose Limiting Toxicity (DLT)

  4 weeks (1 cycle)

• Incidence and grade of Adverse Events (AEs) and Serious Adverse Events (SAEs)

  Incidence and grade of Adverse Events (AEs) and Serious Adverse Events (SAEs) and AEs leading to dose modifications and dose limiting toxicities (DLTs) to determine the maximum tolerated dose (MTD)

  Every cycle (4-week cycles) until study discontinuation, approximately 12 months

Secondary Outcomes (9)

• Characterize the Cmax (PK) of RGT-490 monotherapy in Dose Escalation

  First 3 treatment cycles (each cycle is 28 days)

• Characterize the Tmax (PK) of RGT-490 monotherapy in Dose Escalation

  First 3 treatment cycles (each cycle is 28 days)

• Characterize the AUC (PK) of RGT-490 monotherapy in Dose Escalation

  First 3 treatment cycles (each cycle is 28 days)

• Measure PD effects of RGT-490 monotherapy in Dose Escalation and Phase 1b

  First 7 cycles (each cycle is 28 days) and at study discontinuation

• Changes in fasting blood glucose

  Approximately every week in Cycle 1 and Cycle 2 (4-week cycle), every 2 weeks in Cycles 3-6 (4-week cycle), and every cycle through end of treatment (4-week cycles), approximately 24 months

Study Arms (2)

Phase 1 Dose Escalation (Advanced Solid Tumors with PIK3CA mutation)

EXPERIMENTAL

RGT-490 given alone as monotherapy

Drug: RGT-490

Phase 1b Dose Expansion (HR+/HER2- locally advanced or metastatic breast cancer)

EXPERIMENTAL

RGT-490 given alone as monotherapy

Drug: RGT-490

Interventions

RGT-490 DRUG

Oral tablets

Phase 1 Dose Escalation (Advanced Solid Tumors with PIK3CA mutation); Phase 1b Dose Expansion (HR+/HER2- locally advanced or metastatic breast cancer)

Eligibility Criteria

• Age: 18 Years+
• Sex: all
• Healthy Volunteers: No
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• 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

You may not qualify if:

• 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).

Sponsors & Collaborators

• Regor Pharmaceuticals Inc.: lead

Study Sites (3)

NEXT Houston

Houston, Texas, 77054, United States

RECRUITING

NEXT San Antonio

San Antonio, Texas, 78229, United States

RECRUITING

NEXT Virginia

Fairfax, Virginia, 22031, United States

RECRUITING

MeSH Terms

Conditions

Breast Neoplasms; Ovarian Neoplasms; Endometrial Neoplasms; Uterine Cervical Neoplasms

Condition Hierarchy (Ancestors)

Neoplasms by Site; Neoplasms; Breast Diseases; Skin Diseases; Skin and Connective Tissue Diseases; Endocrine Gland Neoplasms; Ovarian Diseases; Adnexal Diseases; Genital Diseases, Female; Female Urogenital Diseases; Female Urogenital Diseases and Pregnancy Complications; Urogenital Diseases; Genital Neoplasms, Female; Urogenital Neoplasms; Genital Diseases; Endocrine System Diseases; Gonadal Disorders; Uterine Neoplasms; Uterine Diseases; Uterine Cervical Diseases

Central Study Contacts

Sarah Wheeler

CONTACT

857-331-3898; Sarah.Wheeler@regor.com

Regor Pharmaceuticals Central Office

CONTACT

617-315-9070; RGT-490-101@regor.com

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NON RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: SEQUENTIAL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: March 31, 2026
• First Posted: April 13, 2026
• Study Start: April 1, 2026
• Primary Completion (Estimated): April 1, 2028
• Study Completion (Estimated): October 1, 2028
• Last Updated: April 21, 2026

Record last verified: 2026-04

Locations

US (3)