Therapy Detail

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Therapy Name RLY-2608
Synonyms
Therapy Description

RLY-2608 selectively inhibits PIK3CA with higher selectivity and potency against mutant forms of PIK3CA (including PIK3CA E542K, PIK3CA E545K, and PIK3CA H1047R), leading to decreased downstream signaling, and potentially resulting in reduced tumor cell viability and tumor growth (Mol Cancer Ther 2021;20(12 Suppl):Abstract nr P251).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
RLY-2608 RLY 2608|RLY2608 PIK3CA inhibitor 23 RLY-2608 selectively inhibits PIK3CA with higher selectivity and potency against mutant forms of PIK3CA (including PIK3CA E542K, PIK3CA E545K, and PIK3CA H1047R), leading to decreased downstream signaling, and potentially resulting in reduced tumor cell viability and tumor growth (Mol Cancer Ther 2021;20(12 Suppl):Abstract nr P251).

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  • Use quotes to match on a longer phrase with spaces (i.e. "mtor c1483f")

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
PIK3CA E726K PIK3CA H1047R breast cancer resistant RLY-2608 Preclinical - Cell culture Actionable In a preclinical study, a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA E726K was resistant to RLY-2608 treatment in culture (PMID: 37916958). 37916958
PIK3CA H1047R breast cancer sensitive RLY-2608 Preclinical - Cell line xenograft Actionable In a preclinical study, RLY-2608 inhibited viability of hormone receptor-positive breast cancer cells harboring PIK3CA H1047R in culture, and inhibited tumor growth in a cell line xenograft model (PMID: 37916956). 37916956
PIK3CA I817F PIK3CA H1047R breast cancer sensitive RLY-2608 Preclinical - Cell culture Actionable In a preclinical study, RLY-2608 treatment decreased viability of a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA I817F in culture (PMID: 37916958). 37916958
PIK3CA Q859K PIK3CA H1047R breast cancer sensitive RLY-2608 Preclinical - Cell culture Actionable In a preclinical study, RLY-2608 inhibited downstream signaling and viability in a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA Q859K in culture (PMID: 37916958). 37916958
PIK3CA W780R PIK3CA H1047R breast cancer sensitive RLY-2608 Preclinical - Cell culture Actionable In a preclinical study, RLY-2608 inhibited downstream signaling and viability in a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA W780R in culture (PMID: 37916958). 37916958
PIK3CA act mut Advanced Solid Tumor predicted - sensitive RLY-2608 Preclinical - Cell line xenograft Actionable In a preclinical study, RLY-2608 treatment led to inhibition of cell viability in a panel of cancer cell lines harboring PIK3CA hotspot mutations, and led to tumor regression or stasis in cell line xenograft models (Mol Cancer Ther 2021;20(12 Suppl):Abstract nr P251). detail...
PIK3CA E542K estrogen-receptor positive breast cancer predicted - sensitive RLY-2608 Case Reports/Case Series Actionable In a clinical case study, treatment with RLY-2608 resulted in a partial response with disappearance of the soft tissue target lesion, which was ongoing at day 141, in a patient with ESR1/PGR-positive, ERBB2 (HER2)-negative breast cancer harboring PIK3CA E542K (PMID: 37916956; NCT05216432). 37916956
PIK3CA E545K breast cancer sensitive RLY-2608 Preclinical - Cell line xenograft Actionable In a preclinical study, RLY-2608 inhibited proliferation of hormone receptor-positive breast cancer cells harboring PIK3CA E545K in culture, and led to tumor regression in a cell line xenograft model (PMID: 37916956). 37916956
PIK3CA Q859H PIK3CA H1047R breast cancer sensitive RLY-2608 Preclinical - Cell culture Actionable In a preclinical study, RLY-2608 inhibited downstream signaling and viability in a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA Q859H in culture (PMID: 37916958). 37916958
PIK3CA E453K PIK3CA H1047R estrogen-receptor positive breast cancer predicted - sensitive RLY-2608 Case Reports/Case Series Actionable In a clinical case study, treatment with RLY-2608 resulted in a partial response with a reduction in liver, lung, and soft tissue target lesions in a patient with ESR1/PGR-positive, ERBB2 (HER2)-low breast cancer harboring PIK3CA H1047R and PIK3CA E453K (PMID: 37916956; NCT05216432). 37916956

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Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries
NCT05216432 Phase I RLY-2608 Fulvestrant + RLY-2608 First-in-Human Study of Mutant-selective PI3Kalpha Inhibitor, RLY-2608, as a Single Agent in Advanced Solid Tumor Patients and in Combination With Fulvestrant in Patients With Advanced Breast Cancer Recruiting USA | ITA | FRA | ESP 0


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