Therapy Detail
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| Therapy Name | BMS-777607 + Buparlisib |
| Synonyms | |
| Therapy Description | |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| BMS-777607 | ASLAN002|BMS777607|BMS 777607 | AXL Inhibitor 30 MET Inhibitor 59 RON Inhibitor 11 TYRO3 Inhibitor 7 | BMS-777607 (ASLAN002) is a small molecule that inhibits MET, MST1R (RON), TYRO3, and AXL, resulting in decreased downstream pathway activation, potentially resulting in decreased tumor cell growth and metastasis (PMID: 19260711, PMID: 20515943, PMID: 24233399, PMID: 26555154). | |
| Buparlisib | BKM-120|BKM120 | PI3K Inhibitor (Pan) 43 | Buparlisib (BKM120) specifically inhibits class I PI3K in the PI3K/AKT kinase (or protein kinase B) signaling pathway in an ATP-competitive manner, and may result in apoptotic activity and inhibition of cell proliferation (PMID: 22188813). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| MST1R pos PIK3CA H1047R | estrogen-receptor positive breast cancer | predicted - sensitive | BMS-777607 + Buparlisib | Preclinical - Pdx | Actionable | In a preclinical study, the combination of BKM120 and BMS-777607 (ASLAN002) inhibited tumor growth in patient-derived xenograft (PDX) models of estrogen-receptor positive breast cancer harboring PIK3CA H1047R and expressing the short isoform of MST1R (RON) (PMID: 26289070). | 26289070 |
| MST1R pos PIK3CA wild-type | estrogen-receptor positive breast cancer | predicted - sensitive | BMS-777607 + Buparlisib | Preclinical - Pdx | Actionable | In a preclinical study, the combination of BKM120 and BMS-777607 (ASLAN002) inhibited tumor growth in patient-derived xenograft (PDX) models of estrogen-receptor positive breast cancer with wild-type PIK3CA and expressing the short isoform of MST1R (RON) (PMID: 26289070). | 26289070 |
| MST1R act mut | breast cancer | predicted - sensitive | BMS-777607 + Buparlisib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, the combination of BKM120 and BMS-777607 (ASLAN002) inhibited tumor growth in breast cancer cell line xenograft models expressing a constitutively active short isoform of MST1R (RON), with increased efficacy over either agent alone (PMID: 26289070). | 26289070 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|
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