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NCT Number: NCT07524322

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

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.

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Key information

Conditions

Breast Cancer Adnexal Diseases Advanced Breast Cancer Breast Diseases Breast Neoplasms Cervical Cancer Endocrine Gland Neoplasms Endocrine System Diseases Endometrial Cancer Endometrial Neoplasms Female Urogenital Diseases Female Urogenital Diseases and Pregnancy Complications Genital Diseases Genital Diseases, Female Genital Neoplasms, Female Gonadal Disorders HER2- Negative Breast Cancer Hormone Receptor Positive Tumor Neoplasms Neoplasms by Site Ovarian Cancer Ovarian Diseases Ovarian Neoplasms PIK3CA Mutation Skin Diseases Skin and Connective Tissue Diseases Unresectable Solid Tumor Urogenital Diseases Urogenital Neoplasms Uterine Cervical Diseases Uterine Cervical Neoplasms Uterine Diseases Uterine Neoplasms

Age range

18 year and older

Sex eligibility

All sexes

Study type

Interventional

Phase

Phase 1

Primary location

START Los Angeles, Los Angeles, California, United States

Loading trial locations.

Who can participate

Healthy volunteers accepted: No

Only the study team can determine whether someone qualifies for participation.

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).

Treatment and study plan

RGT-490

Drug

Oral tablets

Primary outcomes

  1. Incidence of dose limiting toxicities (DLTs)

    Time frame: 4 weeks (1 cycle)

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

  2. Incidence and grade of Adverse Events (AEs) and Serious Adverse Events (SAEs)

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

    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)

Secondary outcomes

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

    Time frame: First 3 treatment cycles (each cycle is 28 days)

    Maximum observed plasma concentration (Cmax) of RGT-490

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

    Time frame: First 3 treatment cycles (each cycle is 28 days)

    Maximum observed plasma concentration (Tmax) of RGT-490

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

    Time frame: First 3 treatment cycles (each cycle is 28 days)

    Calculated area under the plasma concentration curve (AUC) of RGT-490

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

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

    Change from baseline in ctDNA levels; Change from baseline in PD markers in paired biopsies

  5. Changes in fasting blood glucose

    Time frame: 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

    Measured by fasting blood glucose

  6. Changes in longitudinal glucose metabolism (All Phases)

    Time frame: Approximately every cycle (4-week cycles) until study discontinuation, approximately 24 months

    Measured by HbA1c

  7. Assess preliminary efficacy of RGT-490 monotherapy in dose escalation and Phase 1b

    Time frame: Approximately every 8 weeks until progressive disease, approximately 12 months

    Objective response rate (ORR) based on RECIST v1.1

  8. Evaluate additional measures of efficacy of RGT-490

    Time frame: Approximately every 8 weeks until progressive disease, approximately 36 months

    Duration of response (DoR) according to RECIST v1.1

  9. Evaluate additional measures of efficacy of RGT-490

    Time frame: Approximately every 8 weeks until progressive disease, approximately 36 months

    Progression free survival (PFS) according to RECIST v1.1

Study contacts

Contact information is provided by the study sponsor or research team.

Regor Pharmaceuticals Central Office

CONTACT

[email protected]

617-315-9070

Sarah Wheeler

CONTACT

[email protected]

857-331-3898

Sponsors and collaborators

Lead sponsor

Regor Pharmaceuticals Inc.

Industry

Registry information

Official study title

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

Important dates

Study start
2026
Primary completion
2028
Study completion
2028
First posted
Apr 13, 2026
Registry last updated
Jul 22, 2026

OpenTrials presents study information sourced from ClinicalTrials.gov. The official registry record should be consulted for the latest information.

View the official ClinicalTrials.gov record (opens in a new tab)

This listing is for discovery and informational purposes only. It is not medical advice, does not guarantee that a study is recruiting, and does not determine eligibility. Contact the study team and a qualified healthcare professional when considering participation.

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