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RLY-2608 · 2 trials · 14 indications
| Arm | Type | Description |
|---|---|---|
| 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 |
|---|---|---|
| RLY-2608 | DRUG | RLY-2608 is a mutant-selective, oral PI3Kα inhibitor. |
| Placebo | DRUG | RLY-2608 matched-placebo |
| Fulvestrant | DRUG | 500 mg fulvestrant is administered intramuscularly on Cycle 1 Day 1, Day 15, and Day 1 of each subsequent cycle (where a cycle is 28 days). |
| 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. |
Key Inclusion Criteria: * The participant must have a clinical diagnosis of PROS or a malformation within the ISSVA classification. * One or more documented activating PIK3CA mutation(s) that are targeted by selective PI3Kα inhibitors in lesional tissue and/or cell-free DNA from the lesion or blood...
RLY-2608 is an investigational small molecule being studied for the treatment of cancers and conditions driven by PIK3CA mutations. It is being evaluated in advanced solid tumors, including HER2-negative and metastatic breast cancer, and in PIK3CA-Related Overgrowth Spectrum (PROS), a group of disorders involving overgrowth and vascular malformations.
RLY-2608 targets mutant PI3Kα, a form of the PI3K alpha enzyme that is mutated in certain cancers and overgrowth conditions. It is described as a mutant-selective PI3Kα inhibitor, meaning it is designed to act on the mutated version of the enzyme while potentially sparing normal PI3Kα activity.
RLY-2608 is being developed by Relay Therapeutics, Inc., a biopharmaceutical company traded on the stock exchange under the ticker symbol RLAY. The company is conducting clinical trials of RLY-2608 in both oncology and rare disease indications.
RLY-2608 is in Phase 1 and Phase 2 clinical development. A Phase 1 study is evaluating it as a single agent and in combination with other therapies in advanced solid tumors and breast cancer, while a Phase 2 study is assessing it in adults and children with PIK3CA-Related Overgrowth Spectrum. It is investigational and not yet approved.
RLY-2608 is being studied in two recruiting trials. NCT05216432 is a Phase 1 first-in-human study in advanced solid tumors and breast cancer, with an enrollment of 930 participants. NCT06789913 is a Phase 2 study in PIK3CA-Related Overgrowth Spectrum, enrolling 277 participants across multiple countries.
RLY-2608 is a PI3Kα inhibitor, specifically a mutant-selective one. It is designed to inhibit the alpha isoform of PI3K when it carries a mutation, which is relevant in certain cancers and overgrowth syndromes. It is not the same as pan-PI3K inhibitors that target multiple isoforms.