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Therapy Name | AZ8010 |
Synonyms | |
Therapy Description |
AZ12908010 (AZ8010) 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: 22869148). |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
AZ8010 | AZ12908010 | FGFR1 Inhibitor 28 FGFR2 Inhibitor 24 FGFR3 Inhibitor 21 | AZ12908010 (AZ8010) 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: 22869148). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
FGFR3 K650E FGFR3 over exp HRAS K117E | myeloid neoplasm | sensitive | AZ8010 | Preclinical | Actionable | In a preclinical study, AZ8010 inhibited Fgfr3 signaling and decreased proliferation of myeloma cells with HRAS K117E and overexpression of FGFR3 K650E in culture (PMID: 22869148). | 22869148 |
FGFR2 over exp | breast cancer | sensitive | AZ8010 | Preclinical | Actionable | In a preclinical study, AZ8010 inhibited downstream Erk phosphorylation and proliferation of breast cancer cells over expressing FGFR2 in culture (PMID: 22869148). | 22869148 |
FGFR3 dec exp FGFR3 wild-type HRAS G12V | transitional cell carcinoma | decreased response | AZ8010 | Preclinical | Actionable | In a preclinical study, urothelial cancer cells with low expression of wild-type FGFR3 that harbored HRAS G12V demonstrated resistance to AZ8010 in culture (PMID: 22869148). | 22869148 |
FGFR3 Y373C FGFR3 over exp | multiple myeloma | sensitive | AZ8010 | Preclinical | Actionable | In a preclinical study, AZ8010 inhibited Fgfr3 signaling, induced cell-cycle arrest, and decreased proliferation of multiple myeloma cells over expressing FGFR3 Y373C in culture (PMID: 22869148). | 22869148 |
FGFR3 G384D FGFR3 over exp | multiple myeloma | decreased response | AZ8010 | Preclinical | Actionable | In a preclinical study, multiple myeloma cells over expressing FGFR3 G384D had reduced sensitivity to AZ8010 in culture, compared to cells with ligand-independent activation of FGFR3 (PMID: 22869148). | 22869148 |
FGFR3 over exp | transitional cell carcinoma | sensitive | AZ8010 | Preclinical | Actionable | In a preclinical study, AZ8010 inhibited proliferation of urothelial cancer cells with over expression of FGFR3 in culture (PMID: 22869148). | 22869148 |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
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