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 6 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
- 6 sitesUnited States
- Study dates
- 21 Jul 2026to Oct 2028
- Phase
- Phase 1
- Are there results?
- Not yet: the study is under way
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
6 sites in 1 country. Contact the study team or a site near you to ask about taking part.
6 sites in 1 country
United States6 sites, 6 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
University of Pittsburgh Medical Center
Pittsburgh, Pennsylvania, 15213
- 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 start21 Jul 2026
- 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
- Oct 2026
- First submitted
- 31 Mar 2026
- Last updated
- 2 Nov 2026
- Results posted
- No
- Data monitoring committee
- No
- FDA-regulated drug
- Yes
- FDA-regulated device
- No
Study at a glance
From the registry record, last updated by the sponsor on 2 Nov 2026. Recruitment status is as the sponsor reported it: confirm with the study team.
- 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
- ClinicalTrials.gov ID
- NCT07524322
- Acronym / sponsor ID
- RGT-490-101
- Conditions
- Breast Cancer, Ovarian Cancer, Endometrial Cancer, PIK3CA Mutation, HER2- Negative Breast Cancer, Advanced Breast Cancer
- Phase
- Phase 1
- Study type
- Interventional
- Recruitment status
- Recruiting
- Enrolment
- 63 participants (estimated)
- Lead sponsor
- Regor Pharmaceuticals Inc.Industry (pharma, biotech, devices)
- Study start
- 21 Jul 2026 (actual)
- Primary completion
- Apr 2028 (estimated)
- Study completion
- Oct 2028 (estimated)
- First posted
- 13 Apr 2026 (actual)
- Results
- Not posted in the source record
Clinical summary
The research question as the sponsor registered it. This describes what the study plans to test, not what it found.
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.
Study design
- Primary purpose
- Treatment
- Allocation
- Non-randomised
- Intervention model
- Sequential
- Masking
- None (open label)
- Number of arms
- 2
| Arm | Type | Receives |
|---|---|---|
| Phase 1 Dose Escalation (Advanced Solid Tumors with PIK3CA mutation) | Experimental | Drug: RGT-490RGT-490 given alone as monotherapy |
| Phase 1b Dose Expansion (HR+/HER2- locally advanced or metastatic breast cancer) | Experimental | Drug: RGT-490RGT-490 given alone as monotherapy |
Who may qualify
- Ages
- 18 years and older
- Sex
- All
- Healthy volunteers
- Not accepted
- Age groups
- Adult, Older adult
Key inclusion criteria (5 listed)
- 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
Key exclusion criteria (6 listed)
- 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
Eligibility is decided by the study team after screening; this overview does not establish that a patient qualifies. Full inclusion and exclusion criteria.
Interventions
| Intervention | Type | Arms |
|---|---|---|
| RGT-490Oral tablets | Drug | Phase 1 Dose Escalation (Advanced Solid Tumors with PIK3CA mutation), Phase 1b Dose Expansion (HR+/HER2- locally advanced or metastatic breast cancer) |
Primary outcome
Incidence of dose limiting toxicities (DLTs)
Time frame: 4 weeks (1 cycle)
Number of subjects who experience at least 1 Dose Limiting Toxicity (DLT)
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)
9 secondary outcomes
Characterize the Cmax (PK) of RGT-490 monotherapy in Dose Escalation
Time frame: First 3 treatment cycles (each cycle is 28 days)
Characterize the Tmax (PK) of RGT-490 monotherapy in Dose Escalation
Time frame: First 3 treatment cycles (each cycle is 28 days)
Characterize the AUC (PK) of RGT-490 monotherapy in Dose Escalation
Time frame: First 3 treatment cycles (each cycle is 28 days)
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
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
Changes in longitudinal glucose metabolism (All Phases)
Time frame: 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
Time frame: Approximately every 8 weeks until progressive disease, approximately 12 months
Evaluate additional measures of efficacy of RGT-490
Time frame: Approximately every 8 weeks until progressive disease, approximately 36 months
Evaluate additional measures of efficacy of RGT-490
Time frame: Approximately every 8 weeks until progressive disease, approximately 36 months
Results and safety
This study is still under way. Results are not available in the source record yet.
Research links
- Official record on ClinicalTrials.govLast updated by the sponsor 2 Nov 2026.
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Referral and contact
AzTrials does not enrol participants or take referrals. Contact the study team or a site listed below; they decide who can take part.
6 sites in 1 country: see every site and its status.
Questions about this trial
What is this clinical trial studying?
A Phase 1 study testing RGT-490 in people with Breast Cancer and Ovarian Cancer, run by Regor Pharmaceuticals Inc. at 6 sites in United States.
The full registered description is in the About this study section and the official record.
Who may be eligible to take part?
The sponsor lists 5 inclusion and 6 exclusion criteria. Eligibility is decided by the study team after screening, so read the full criteria and contact a listed site.
Is this clinical trial currently recruiting?
The record says: looking for participants now, as of the sponsor's last update on 2 Nov 2026. Status can change between updates, so confirm with the study contact before making plans.
Where is the study taking place?
The record lists 6 sites in United States. Whether a site is taking part right now should be confirmed with that site. See every site.
What are the possible benefits and risks?
They depend on the study and the treatment, and no study can promise a benefit. The study team explains the known risks during informed consent, before anyone joins; the record itself does not list them.
What does this phase mean?
Phase 1 studies test a treatment in a small group of people for the first time or in a new way, mainly to check safety and find the right dose.
Not every study follows the same path, and some studies (observational studies, device studies) have no phase.
Are results available for this study?
This study is still under way. Results are not available in the source record yet.
How can a doctor refer a patient or contact the research team?
Contact Sarah Wheeler (857-331-3898, Sarah.Wheeler@regor.com), or a site near the patient. AzTrials does not enrol participants or take referrals.
What does the primary outcome measure?
Incidence of dose limiting toxicities (DLTs) (time frame: 4 weeks (1 cycle)). The study lists 2 primary outcomes in all. It is what the study was designed to measure, not a finding.
Where can I read the original study information?
Does a listing mean the treatment is approved or proven to work?
No. A listing means the study is registered. It does not show that the treatment is safe, works, or is approved by a regulator.
How often is this information updated?
AzTrials copies changed records from ClinicalTrials.gov every night and reloads the whole registry every week. The sponsor last updated this record on 2 Nov 2026.