Approval Probability
TA Base Rate
Adjusted LOA
ML Risk
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 oral medicine being studied for cancers and overgrowth disorders driven by PIK3CA mutations. Its main programs are locally advanced or metastatic PIK3CA-mutant HR+/HER2- breast cancer and PIK3CA-Related Overgrowth Spectrum (PROS), which includes vascular and lymphatic malformations such as CLOVES syndrome and Klippel Trenaunay syndrome.
Zovegalisib targets mutant PIK3CA, the gene encoding the PI3K alpha isoform, and belongs to the -lisib class of PI3K inhibitors. It is designed to be mutant-selective, meaning it preferentially inhibits the mutated form of PI3K alpha found in tumors and malformations rather than the normal, wild-type protein.
Zovegalisib is being developed by Relay Therapeutics, Inc., which trades on the Nasdaq under the ticker RLAY. Relay is running the clinical program for the drug across both oncology and PIK3CA-Related Overgrowth Spectrum indications.
Zovegalisib is in Phase 3 development. The Phase 3 trial NCT06982521 is recruiting, and the drug also has an active Phase 2 study, NCT06789913, in PIK3CA-Related Overgrowth Spectrum, plus the ongoing first-in-human Phase 1 study NCT05216432. Zovegalisib has received Breakthrough Therapy designation from the FDA.
Zovegalisib is being studied in three recruiting trials. NCT06982521 is a Phase 3 study of Zovegalisib plus fulvestrant versus capivasertib plus fulvestrant in PIK3CA-mutant HR+/HER2- breast cancer. NCT06789913 is a Phase 2 study in PIK3CA-Related Overgrowth Spectrum, and NCT05216432 is the Phase 1 first-in-human solid tumor and breast cancer study.
Yes. Zovegalisib is the international nonproprietary name for RLY-2608, the code name Relay Therapeutics used during early development. Both names refer to the same mutant-selective PI3K alpha inhibitor, so trial records and publications listing RLY-2608 describe the same drug as Zovegalisib.