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Also known as RLY-2608
Zovegalisib · 3 trials · 16 indications
| Arm | Type | Description |
|---|---|---|
| Zovegalisib + fulvestrant | EXPERIMENTAL | Zovegalisib + fulvestrant combination for participants with HR+/HER2- advanced breast cancer |
| capivasertib + fulvestrant | ACTIVE_COMPARATOR | capivasertib + fulvestrant combination for participants with HR+/HER2- advanced breast cancer |
| Part 1, Group 1 | EXPERIMENTAL | RLY-2608 for patients ≥12 years old with PROS or malformations with PIK3CA mutation. Multiple doses of RLY-2608 for oral administration. |
| Part 1, Group 2 | EXPERIMENTAL | RLY-2608 for participants 6 to \<12 years old with PROS or malformations with PIK3CA mutation. RLY-2608 will be studied in pediatric participants in a dose escalation design. |
| Part 1, Group 3 | EXPERIMENTAL | Part 1, Group 3: RLY-2608 for participants 2 to \<6 years old with PROS or malformations with PIK3CA mutation. RLY-2608 will be studied in pediatric participants in a dose escalation design. |
| Part 2, Group 1 | EXPERIMENTAL | Dose expansion single-arm cohorts for various subpopulations of participants ≥12 years old with PROS or malformations with PIK3CA mutation. Oral dose of RLY-2608 as determined during Part 1. |
| Part 2, Group 2 | EXPERIMENTAL | Dose expansion cohorts for participants 6 to \<12 years old with PROS or malformations with PIK3CA mutation. Oral dose of RLY-2608 as determined during Part 1. |
| Part 2, Group 3 | EXPERIMENTAL | Dose expansion cohorts for participants 2 to \<6 years old with PROS or malformations with PIK3CA mutation. Oral dose of RLY-2608 as determined during Part 1. |
| Part 3, Arm 1 | EXPERIMENTAL | Adult (\>18 yo) and pediatric (6 to \<18 yo) participants with PROS and malformations with PIK3CA mutation will be randomized to receive RLY-2608 at oral dose determined during Part 1/2. |
| Part 3, Arm 2 | PLACEBO_COMPARATOR | Adult (\>18 yo) and pediatric (6 to \<18 yo) participants with PROS and malformations with PIK3CA mutation will be randomized to receive placebo. |
| RLY-2608 for patients with unresectable or metastatic solid tumors | EXPERIMENTAL | Multiple doses of RLY-2608 for oral administration. |
| RLY-2608 + fulvestrant combination for HR+ HER2- locally advanced or metastatic breast cancer | EXPERIMENTAL | Oral dose of RLY-2608 in addition to fulvestrant as determined during Part 1 Dose Escalation. |
| RLY-2608+fulvestrant+palbo125mg for HR+HER2- locally advanced metastatic breast cancer | EXPERIMENTAL | Oral dose of RLY-2608 in addition to fulvestrant and palbociclib 125mg as determined during Part 1 Dose Escalation. |
| RLY-2608+fulvestrant+ribo400mg for HR+HER2- locally advanced metastatic breast cancer | EXPERIMENTAL | Oral dose of RLY-2608 in addition to fulvestrant and ribociclib 400mg as determined during Part 1 Dose Escalation. |
| RLY-2608+fulvestrant+ribo600mg for HR+HER2- locally advanced metastatic breast cancer | EXPERIMENTAL | Oral dose of RLY-2608 in addition to fulvestrant and ribociclib 600mg as determined during Part 1 Dose Escalation. |
| RLY-2608+fulvestrant+PF-07220060 100 mg for HR+ HER2- locally advanced or metastatic breast cancer | EXPERIMENTAL | Oral dose of RLY-2608 in addition to fulvestrant and PF-07220060 100 mg as determined during Part 1 Dose Escalation |
| RLY-2608+fulvestrant+PF-07220060 300 mg for HR+ HER2- locally advanced or metastatic breast cancer | EXPERIMENTAL | Oral dose of RLY-2608 in addition to fulvestrant and PF-07220060 300 mg as determined during Part 1 Dose Escalation |
| Name | Type | Description |
|---|---|---|
| Zovegalisib | DRUG | 400 mg orally BID administered daily on a 28-day treatment cycle |
| Capivasertib | DRUG | 400mg orally BID administered on an intermittent weekly dosing schedule. Patients will dose on Days 1 through 4 each week of a 28-day treatment cycle |
| Fulvestrant | DRUG | 500 mg intramuscularly administered on Cycle 1 Day 1, Day 15, and Day 1 of each subsequent cycle (28-day treatment cycle) |
| RLY-2608 | DRUG | RLY-2608 is a mutant-selective, oral PI3Kα inhibitor. |
| Placebo | DRUG | RLY-2608 matched-placebo |
| Palbociclib 125mg | DRUG | 125mg palbociclib is taken orally once daily for 28-day cycles that include 21 days of treatment followed by 7 days off treatment. |
| Ribociclib 400mg | DRUG | 400mg ribociclib is taken orally once daily for 28-day cycles that include 21 days of treatment followed by 7 days off treatment. |
| Ribociclib 600mg | DRUG | 600mg ribociclib is taken orally once daily for 28-day cycles that include 21 days of treatment followed by 7 days off treatment. |
| PF-07220060 100mg | DRUG | PF-07220060 100 mg is taken orally twice daily at the same time with RLY-2608 during each 28-day cycle. |
| PF-07220060 300 mg | DRUG | PF-07220060 300 mg is taken orally twice daily at the same time with RLY-2608 during each 28-day cycle. |
Inclusion Criteria: * Patient has ECOG performance status of 0-1 * One or more known primary oncogenic PIK3CA mutation(s) * Adult females, pre- and/or post-menopausal, and adult males. Pre-menopausal (and peri-menopausal) women can be enrolled if amenable to treatment with a gonadotropin-releasing ...
Zovegalisib is an investigational small molecule being developed for PIK3CA-mutant cancers and PIK3CA-Related Overgrowth Spectrum (PROS). Its lead programs include locally advanced or metastatic PIK3CA-mutant HR+/HER2- breast cancer and PROS with malformations driven by PIK3CA mutation, including lymphatic and vascular malformations.
Zovegalisib targets PIK3CA, the gene encoding the PI3K alpha isoform. It is described as a mutant-selective PI3K alpha inhibitor, part of the -lisib PI3K inhibitor class, meaning it is designed to act on the mutant form of the target. It is a small molecule given orally.
Zovegalisib is being developed by Relay Therapeutics, Inc., which trades under the ticker RLAY. The company is running the clinical program for the drug across breast cancer and PIK3CA-Related Overgrowth Spectrum indications.
Zovegalisib is in Phase 3 development. It is investigational and has not been approved by the FDA. The FDA has granted it Breakthrough Therapy designation. The Phase 3 program is evaluating the drug in PIK3CA-mutant HR+/HER2- breast cancer, while earlier-stage studies cover additional indications.
Zovegalisib is being studied in three recruiting trials. NCT06982521 is a Phase 3 study in PIK3CA-mutant HR+/HER2- breast cancer. NCT06789913 is the Phase 2 ReInspire study in PIK3CA-Related Overgrowth Spectrum. NCT05216432 is the first-in-human Phase 1 study in advanced solid tumors and breast cancer.
Yes, Zovegalisib is the same drug as RLY-2608. RLY-2608 is the earlier code name used for the compound in trial titles and publications, while Zovegalisib is the current name. Both refer to the mutant-selective PI3K alpha inhibitor developed by Relay Therapeutics.