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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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| 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 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 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 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 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 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 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 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 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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