Therapy Detail
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| Therapy Name | Buparlisib + Fexagratinib |
| Synonyms | |
| Therapy Description | |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| Buparlisib | BKM-120|BKM120 | PI3K Inhibitor (Pan) 42 | 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). | |
| Fexagratinib | AZD-4547|AZD4547|AZD 4547|ABSK091|KB-74810|ABSK 091|ABSK-091|KB74810|KB 74810 | FGFR1 Inhibitor 28 FGFR2 Inhibitor 23 FGFR3 Inhibitor 19 | Fexagratinib selectively binds and inhibits FGFR1, 2, and 3, which may result in the inhibition of FGFR-mediated signal transduction pathways and inhibition of tumor cell proliferation (PMID: 22369928, PMID: 30115694, PMID: 32463741), and has demonstrated inhibitory effects on NTRK signaling (PMID: 34790577). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| FGFR1 amp | transitional cell carcinoma | sensitive | Buparlisib + Fexagratinib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of AZD4547 and Buparlisib (BKM120) worked synergistically to induce apoptosis and inhibit growth of a urothelial cell carcinoma cell line with FGFR1 amplification in culture, with increased efficacy over either agent alone (PMID: 28108151). | 28108151 |
| FGFR1 amp | lung small cell carcinoma | sensitive | Buparlisib + Fexagratinib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of AZD4547 and Buparlisib (BKM120) induced apoptosis in a small cell lung cancer cell line with amplification of FGFR1 in culture (PMID: 28108151). | 28108151 |
| FGFR1 amp | lung squamous cell carcinoma | sensitive | Buparlisib + Fexagratinib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of AZD4547 and Buparlisib (BKM120) induced apoptosis in a squamous cell lung cancer cell line with amplification of FGFR1 in culture (PMID: 28108151). | 28108151 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
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