Drug Type Small molecule drug |
Synonyms RLY 2608, RLY-2608, RLY-PI3K1047 |
Action inhibitors |
Mechanism PIK3CA E542K inhibitors, PIK3CA E545K inhibitors, PIK3CA H1047X inhibitors(PIK3CA H1047X inhibitors) |
Therapeutic Areas |
Active Indication |
Inactive Indication- |
Originator Organization |
Inactive Organization- |
License Organization- |
Drug Highest PhasePhase 3 |
First Approval Date- |
RegulationBreakthrough Therapy (United States) |
Molecular FormulaC29H14ClF5N6O2 |
InChIKeyVYWRYBZVVSPTQN-SANMLTNESA-N |
CAS Registry2733573-94-7 |
| Indication | Highest Phase | Country/Location | Organization | Date |
|---|---|---|---|---|
| Advanced breast cancer | Phase 3 | United States | 26 Aug 2025 | |
| Advanced breast cancer | Phase 3 | Argentina | 26 Aug 2025 | |
| Advanced breast cancer | Phase 3 | Australia | 26 Aug 2025 | |
| Advanced breast cancer | Phase 3 | Austria | 26 Aug 2025 | |
| Advanced breast cancer | Phase 3 | Belgium | 26 Aug 2025 | |
| Advanced breast cancer | Phase 3 | Brazil | 26 Aug 2025 | |
| Advanced breast cancer | Phase 3 | Bulgaria | 26 Aug 2025 | |
| Advanced breast cancer | Phase 3 | Canada | 26 Aug 2025 | |
| Advanced breast cancer | Phase 3 | Czechia | 26 Aug 2025 | |
| Advanced breast cancer | Phase 3 | Denmark | 26 Aug 2025 |
Phase 3 | 540 | qwzsscyqrm(jgtbtanaif) = pcvwxdrsbp edjgxzsyhx (dtdkehbmtj, 24.9 - NR) | Positive | 29 May 2026 | |||
Phase 1/2 | PIK3CA mutation/HR-positive/HER2-negative Breast Cancer HER2 Negative | HR Positive | 60 | mhrbznrovj(qezmhvobpu) = uhvtblxsnh hmffqukcqa (mtvwdtwddx, 7.3 - 13.0) View more | Positive | 16 Mar 2026 | ||
(kinase mutations) | mhrbznrovj(qezmhvobpu) = sdbdhffshh hmffqukcqa (mtvwdtwddx ) | ||||||
Phase 3 | 540 | xihvwvpbea(vklrndcftx) = RLY-2608 + fulvestrant: 1.1% (pneumonitis), capivasertib + fulvestrant: 1.2% (gastrointestinal bleeding) vufdlijplx (gihrjpffdp ) View more | Positive | 12 Dec 2025 | |||
Phase 1 | 118 | bbudbflxqq(oanmgyytub) = 34.7%; 0.8% Gr 3 dhpdvjbpqn (itrxnmnwgq ) View more | Positive | 30 May 2025 | |||
Phase 1 | 118 | gvegzggads(khdpcqjeik) = 600mg BID cwzzcxtgse (hyiwrsouxe ) | Positive | 09 Sep 2024 | |||
(kinase mutations) | |||||||
Phase 1 | PIK3CA mutation/HR-positive/HER2-negative Breast Cancer | Solid tumor PIK3CA Mutation | HR Positive | HER2 Negative | 42 | (unresectable or metastatic solid tumors with a PI3Kα mutation) | cjtxmfnyhj(gbearwmwox) = Among patients receiving doses at target exposures (mono: 400mg BID; combo: 600mg BID & 800mg BID; n=17), AEs were mostly low-grade events that were manageable and reversible:No Grade 3 hyperglycemia, diarrhea, or rash, which are the AEs most commonly associated with treatment discontinuation for existing investigational and approved therapies. gekawgukzs (fvdaqaslaz ) View more | Positive | 18 Apr 2023 | |
(PI3Kα-mutant, HR+, HER2– locally advanced or metastatic breast cancer) |





