Breast CancerPhase 1NCT07524322
Study of RGT-490 in Patients With PIK3CA-Mutated Advanced Solid Tumors
A Phase 1 study testing RGT-490 in people with Breast Cancer and Ovarian Cancer, run by Regor Pharmaceuticals Inc. at 5 sites in United States.
Trial 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… Read more about this study
- Who is it for?
- Ages 18 years and older
- Conditions the study is for
- Breast Cancer, Ovarian Cancer, Endometrial Cancer
- What is being tested?
- RGT-490
- Type of treatment
- Pill or oral medicine
- Could I receive a placebo?
- No, everyone receives an active treatment
- How many people
- 63 participants
- Where
- 5 sitesUnited States
- Study dates
- Jun 2026to Oct 2028
- Phase
- Phase 1
Key requirements
Who can take part, as listed by the sponsor. Only the study team can confirm whether you are eligible, so take this list to your doctor.
- Ages 18 years and older
- All sexes
- No healthy volunteers
- Adult, Older adult
Who may be able to join
- 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
Who cannot join
- 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).
Trial locations and contacts
5 sites in 1 country. Contact the study team or a site near you to ask about taking part.
5 sites in 1 country
United States5 sites, 5 recruiting
- Recruiting
NEXT Virginia
Fairfax, Virginia, 22031
- Recruiting
The University of Texas MD Anderson Cancer Center
Houston, Texas, 77030
- Recruiting
NEXT Houston
Houston, Texas, 77054
- Recruiting
START Los Angeles
Los Angeles, California, 90025
- Recruiting
NEXT San Antonio
San Antonio, Texas, 78229
About this study
Official 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
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
- Being tested
- RGT-490
- Medical subject headings
- Breast Neoplasms, Ovarian Neoplasms, Endometrial Neoplasms, Uterine Cervical Neoplasms
What participants receive
What participants receive. In a randomised study each person is assigned to one group by chance.
RGT-490Drug
Oral tablets
| Study group | Role | What they receive |
|---|---|---|
| Phase 1 Dose Escalation (Advanced Solid Tumors with PIK3CA mutation) | Experimental | RGT-490 given alone as monotherapy Receives: Drug: RGT-490 |
| Phase 1b Dose Expansion (HR+/HER2- locally advanced or metastatic breast cancer) | Experimental | RGT-490 given alone as monotherapy Receives: Drug: RGT-490 |
What is being measured
The primary outcome is the main question the study is designed to answer.
Incidence of dose limiting toxicities (DLTs)
Number of subjects who experience at least 1 Dose Limiting Toxicity (DLT)
Measured: 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)
Measured: 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
Maximum observed plasma concentration (Cmax) of RGT-490
Measured: First 3 treatment cycles (each cycle is 28 days)
Characterize the Tmax (PK) of RGT-490 monotherapy in Dose Escalation
Maximum observed plasma concentration (Tmax) of RGT-490
Measured: First 3 treatment cycles (each cycle is 28 days)
Characterize the AUC (PK) of RGT-490 monotherapy in Dose Escalation
Calculated area under the plasma concentration curve (AUC) of RGT-490
Measured: First 3 treatment cycles (each cycle is 28 days)
Measure PD effects of RGT-490 monotherapy in Dose Escalation and Phase 1b
Change from baseline in ctDNA levels; Change from baseline in PD markers in paired biopsies
Measured: First 7 cycles (each cycle is 28 days) and at study discontinuation
Changes in fasting blood glucose
Measured by fasting blood glucose
Measured: 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
Changes in longitudinal glucose metabolism (All Phases)
Measured by HbA1c
Measured: Approximately every cycle (4-week cycles) until study discontinuation, approximately 24 months
Assess preliminary efficacy of RGT-490 monotherapy in dose escalation and Phase 1b
Objective response rate (ORR) based on RECIST v1.1
Measured: Approximately every 8 weeks until progressive disease, approximately 12 months
Evaluate additional measures of efficacy of RGT-490
Duration of response (DoR) according to RECIST v1.1
Measured: Approximately every 8 weeks until progressive disease, approximately 36 months
Evaluate additional measures of efficacy of RGT-490
Progression free survival (PFS) according to RECIST v1.1
Measured: Approximately every 8 weeks until progressive disease, approximately 36 months
Timeline
From the start of the study to its completion; the mark is today. Estimated dates are the sponsor’s plan.
- First posted13 Apr 2026
- Study startJun 2026 (estimated)
- Primary completionApr 2028 (estimated)
- Study completionOct 2028 (estimated)
Resources
- Official record on ClinicalTrials.govThe registry entry this page is built from, with its full change history.
- Other trials for Breast CancerStudies of the same condition, open and under way.
- What the trial phases meanHow a treatment moves from first tests in people to approval.
More details
For doctors and researchers: how the study is designed, who runs it, and its registry IDs.
Study design
- Study type
- Interventional
- Phase
- Phase 1
- Primary purpose
- Treatment
- Allocation
- Non-randomised
- Intervention model
- Sequential
- Masking
- None (open label)
- Enrolment
- 63 participants (estimated)
Sponsor and investigators
- Lead sponsor
- Regor Pharmaceuticals Inc.
- Sponsor type
- Industry (pharma, biotech, devices)
- Responsible party
- Sponsor
IDs, dates and publications
- ClinicalTrials.gov ID
- NCT07524322
- Sponsor's protocol ID
- RGT-490-101
- Status last verified
- Jul 2026
- First submitted
- 31 Mar 2026
- Last updated
- 22 Jul 2026
- Results posted
- No
- Data monitoring committee
- No
- FDA-regulated drug
- Yes
- FDA-regulated device
- No