Therapy Detail

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Therapy Name Fexagratinib
Synonyms
Therapy Description

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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Drug Name Trade Name Synonyms Drug Classes Drug Description
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
FGFR2 A67V Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 A67V were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR1 M456V Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 M456V were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR3 rearrange myeloid neoplasm sensitive Fexagratinib Preclinical - Cell line xenograft Actionable In a preclinical study, AZD4547 inhibited survival of myeloma cells harboring FGFR3 translocation in culture and in cell line xenograft models (PMID: 27550940). 27550940
FGFR1 amp lung squamous cell carcinoma no benefit Fexagratinib Phase I Actionable In a Phase Ib trial, AZD4547 demonstrated limited efficacy in patients with squamous cell lung cancer with FGFR1 amplification, resulting in an overall response rate of 8% (1/15) and a median overall survival of 4.9 months (PMID: 28615371; NCT00979134). 28615371
FGFR1 D128V Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 D128V were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR3 S756P lung non-small cell carcinoma no benefit Fexagratinib Case Reports/Case Series Actionable In a Phase II trial (NLMT), AZD4547 treatment did not result in a confirmed response or durable clinical benefit in a patient with non-small cell lung cancer harboring FGFR3 S758P (corresponds to S756P in the canonical isoform (PMID: 32669708, NCT02664935). 32669708
FGFR2 A389T Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 A389T were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 V392A Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 V392A were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR1 amp lung cancer sensitive Fexagratinib Preclinical Actionable In a preclinical study, AZD4547 inhibited proliferation of lung cancer cell lines harboring FGFR1 amplification in culture and induced tumor regression in xenograft models (PMID: 23082000). 23082000
FGFR3 mutant urinary bladder cancer sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited survival of bladder cancer cells harboring FGFR3 mutation in culture (PMID: 27550940). 27550940
FGFR2 K660N Advanced Solid Tumor sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited growth of transformed cells expressing FGFR2 K660N in culture (PMID: 23786770). 23786770
FGFR1 E467K Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 E467K were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR3 act mut Advanced Solid Tumor predicted - sensitive Fexagratinib Phase II Actionable In a Phase II (MATCH) trial, AZD4547 treatment resulted in an overall response rate of 10.5% (2/19) in patients with advanced solid tumors harboring FGFR2 or 3 activating single nucleotide variants and a 6-month progression-free survival rate of 6%, with a partial response in 1 and stable disease in 2 of 7 patients with FGFR3 activating mutations (PMID: 32463741; NCT02465060). 32463741
FGFR1 P483L Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 P483L were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 R330W Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 R330W were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 Y769* breast cancer predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited growth of mouse mammary epithelial cells expressing FGFR2 Y674* (corresponding to Y769* in human) in culture (PMID: 35948633). 35948633
FGFR2 Y376C intrahepatic cholangiocarcinoma predicted - sensitive Fexagratinib Case Reports/Case Series Actionable In a Phase II (MATCH) trial, AZD4547 treatment resulted in an overall response rate of 10.5% (2/19) in patients with advanced solid tumors harboring FGFR2 or 3 activating single nucleotide variants and a 6-month progression-free survival rate of 6%, including a partial response with 69% reduction in target lesion size and progression-free survival of 9.8 months in a patient with intrahepatic cholangiocarcinoma harboring FGFR2 Y376C (PMID: 32463741; NCT02465060). 32463741
FGFR3 G384D FGFR3 over exp multiple myeloma decreased response Fexagratinib Preclinical Actionable In a preclinical study, multiple myeloma cells over expressing FGFR3 G384D had reduced sensitivity to AZD4547 in culture, compared to cells with ligand-independent activation of FGFR3 (PMID: 22869148). 22869148
FGFR3 S249C FGFR3 V555L Advanced Solid Tumor resistant Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, a cell line expressing FGFR3 S249C and V555L was resistant to AZD4547 in culture (PMID: 39082679). 39082679
FGFR2 S252W endometrial cancer decreased response Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, endometrial cells harboring Fgfr2 S252W were less sensitive to the anti-proliferative effects of AZD4547 than the Fgfr2 double mutant, K310R, N550K (PMID: 26294741). 26294741
FGFR2 M186T Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 M186T were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 G364E Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 G364E were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR1 amp Advanced Solid Tumor unknown Fexagratinib Phase II Actionable In a Phase II (MATCH) trial, AZD4547 treatment resulted in stable disease in 7 of 17 patients with advanced solid tumors harboring FGFR1 amplification, with 6 of the 17 patients experiencing progressive disease and 4 not evaluable for response, and a 6-month progression-free survival rate of 0% (PMID: 32463741; NCT02465060). 32463741
FGFR3 N540K Advanced Solid Tumor resistant Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells over expressing FGFR3 N540K were reistant to growth inhibition by AZD4547 in culture (PMID: 26992226). 26992226
FGFR1 R189C Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 R189C were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR1 S238N Advanced Solid Tumor predicted - resistant Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 S238N were resistant to treatment with AZD4547 in culture (PMID: 34272467). 34272467
FGFR2 C383R endometrial cancer sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, AZD4547 treatment induced cell death and reduced survival of an endometrial cancer cell line harboring FGFR2 C383R in culture (PMID: 30537101). 30537101
FGFR2 D101Y Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 D101Y were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 K660E Advanced Solid Tumor sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited growth of transformed cells expressing FGFR2 K660E in culture (PMID: 23786770). 23786770
FGFR1 positive uterus leiomyosarcoma decreased response Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, uterine leiomyosarcoma cells with moderate Fgfr1 expression level demonstrated decreased response to AZD4547 in culture (PMID: 27535980). 27535980
FGFR2 E768* breast cancer predicted - sensitive Fexagratinib Preclinical Actionable In a preclinical study, AZD4547 inhibited FGFR2 signaling and growth in mouse mammary epithelial cells expressing FGFR2 E673* (corresponding to E768* in human) in culture and inhibited tumor growth in an orthotopic model (PMID: 35948633). 35948633
FGFR1 T26I Advanced Solid Tumor predicted - resistant Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 T26I were resistant to treatment with AZD4547 in culture (PMID: 34272467). 34272467
FGFR2 V514L lung non-small cell carcinoma no benefit Fexagratinib Case Reports/Case Series Actionable In a Phase II trial (NLMT), AZD4547 treatment did not result in a confirmed response or durable clinical benefit in a patient with non-small cell lung cancer harboring FGFR2 V515L (corresponds to V514L in the canonical isoform (PMID: 32669708, NCT02664935). 32669708
FGFR2 E160K Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 E160K were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 H242Y Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 H242Y were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR1 A21T Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 A21T were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR3 fusion urinary bladder cancer sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited survival of bladder cancer cells harboring FGFR3 fusion in culture (PMID: 27550940). 27550940
FGFR2 W290C Advanced Solid Tumor sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited growth of transformed cells expressing FGFR2 W290C in culture (PMID: 23786770). 23786770
FGFR3 S249C FGFR3 V555M Advanced Solid Tumor resistant Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, a cell line expressing FGFR3 S249C and V555M was resistant to AZD4547 in culture (PMID: 39082679). 39082679
FGFR2 L776Rfs*6 breast cancer predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited growth of mouse mammary epithelial cells expressing FGFR2 L681Rfs*6 (corresponding to L776Rfs*6 in human) in culture (PMID: 35948633). 35948633
FGFR1 T319A Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 T319A were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR1 S588T Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 S588T were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 R399Q Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 R399Q were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR1 amp lung large cell carcinoma sensitive Fexagratinib Preclinical Actionable In a preclinical study, AZD4547 inhibited proliferation of a large cell lung cancer cell line harboring FGFR1 amplification in culture and induced tumor regression in xenograft models (PMID: 23082000). 23082000
FGFR3 L608V Advanced Solid Tumor decreased response Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells over expressing FGFR3 L608V demonstrated reduced sensitivity to AZD4547 in culture (PMID: 28034880). 28034880
FGFR2 R251Q Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 R251Q were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 G305R Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 G305R were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 A371V Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 A371V were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 Y375C breast cancer sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited viability of breast epithelial cells expressing FGFR2 Y375C in culture (PMID: 37980453). 37980453
FGFR2 G227E Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 G227E were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 R664W Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 R664W were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 over exp breast cancer sensitive Fexagratinib Preclinical Actionable In a preclinical study, AZD4547 inhibited downstream Erk phosphorylation and proliferation of breast cancer cells over expressing FGFR2 in culture (PMID: 22869148). 22869148
FGFR2 C382R breast cancer predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited growth of mouse mammary epithelial cells expressing FGFR2 C287R (corresponding to C382R in human) in culture (PMID: 35948633). 35948633
FGFR2 R203C Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 R203C were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR1 T141R Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 T141R were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR3 K650M Advanced Solid Tumor resistant Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR3 K650M were resistant to treatment with AZD4547 in culture (PMID: 34272467). 34272467
FGFR2 L560F Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 L560F were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR1 S436F Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 S436F were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 P253R Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 P253R were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 amp gastric adenocarcinoma no benefit Fexagratinib Phase II Actionable In a Phase II trial (SHINE), AZD4547 treatment did not improve progression-free survival compared to Taxol (paclitaxel) (1.8 vs 3.5 months, p=0.9581) in advanced gastric adenocarcinoma patients with FGFR2 amplification (PMID: 29177434; NCT01457846). 29177434
FGFR2 amp endometrial cancer sensitive Fexagratinib Preclinical - Cell line xenograft Actionable In a preclinical study, AZD4547 inhibited survival of FGFR2 amplified endometrial cancer cells in cell line xenograft models (PMID: 27550940). 27550940
FGFR2 K310R Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 K310R were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR1 wild-type lung cancer decreased response Fexagratinib Preclinical Actionable In a preclinical study, FGFR1 non-amplified lung cancer cell lines demonstrated reduced sensitivity to AZD4547 induced growth inhibition in culture and in xenograft models (PMID: 23082000). 23082000
FGFR3 over exp transitional cell carcinoma sensitive Fexagratinib Preclinical Actionable In a preclinical study, AZD4547 inhibited proliferation of urothelial cancer cells with over expression of FGFR3 in culture (PMID: 22869148). 22869148
FGFR2 amp colon cancer sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited survival of FGFR2 amplified colon cancer cells in culture (PMID: 27550940). 27550940
FGFR1 S125L Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 S125L were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 P582L Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 P582L were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 V564F Advanced Solid Tumor resistant Fexagratinib Preclinical - Cell line xenograft Actionable In a preclinical study, transformed cells over expressing FGFR2 V564F were resistant to AZD4547 in culture and in cell line xenograft models (PMID: 25169980). 25169980
FGFR1 positive leiomyosarcoma decreased response Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, leiomyosarcoma cells with moderate Fgfr1 expression level demonstrated decreased response to AZD4547 in culture (PMID: 27535980). 27535980
FGFR1 positive synovial sarcoma decreased response Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, synovial sarcoma cells with moderate Fgfr1 expression level demonstrated decreased response to AZD4547 in culture (PMID: 27535980). 27535980
FGFR1 amp synovial sarcoma sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited survival of FGFR1 amplified synovial sarcoma cells in culture (PMID: 27535980). 27535980
FGFR2 H544Q Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 H544Q were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 over exp endometrial cancer resistant Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, endometrial cells with Fgfr2 overexpression were resistant to the anti-proliferative effects of AZD4547 (PMID: 26294741). 26294741
FGFR2 K310R FGFR2 N550K endometrial cancer sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, AZD4547 treatment induced cell death and reduced survival of an endometrial cancer cell line harboring FGFR2 N550K and K310R in culture (PMID: 30537101). 30537101
FGFR2 K310R FGFR2 N550K endometrial cancer sensitive Fexagratinib Preclinical - Cell line xenograft Actionable In a preclinical study, AZD4547 inhibited proliferation of endometrial cancer cells harboring an FGFR2 K310R/N550K double mutation in culture and delayed tumor growth in xenograft models (PMID: 26294741). 26294741
FGFR2 C62Y Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 C62Y were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR1 K656M Advanced Solid Tumor predicted - resistant Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 K656M were resistant to treatment with AZD4547 in culture (PMID: 34272467). 34272467
FGFR2 K660N estrogen-receptor positive breast cancer sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, AZD4547 treatment decreased viability of ESR1-positive breast cancer cells expressing FGFR2 K660N in culture (PMID: 32723837). 32723837
FGFR1 rearrange leukemia sensitive Fexagratinib Preclinical - Cell line xenograft Actionable In a preclinical study, AZD4547 inhibited survival of leukemia cells harboring FGFR1 translocation in culture and in cell line xenograft models (PMID: 27550940). 27550940
FGFR1 amp breast cancer no benefit Fexagratinib Phase II Actionable In a Phase II clinical trial, treatment with AZD4547 resulted in a response rate of 12.5% (1/8) in patients with FGFR1-amplified breast cancer, and did not meet the predetermined criteria for efficacy (PMID: 27179038). 27179038
FGFR1 E592G Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 E592G were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 G613S Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 G613S were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR3 A391E Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR3 A391E were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 R203H Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 R203H were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 P253L Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 P253L were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR1 amp lung small cell carcinoma sensitive Fexagratinib Preclinical Actionable In a preclinical study, AZD4547 inhibited proliferation of a small cell lung cancer cell line harboring FGFR1 amplification in culture (PMID: 23082000). 23082000
FGFR3 K650E Advanced Solid Tumor decreased response Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells over expressing FGFR3 K650E demonstrated reduced sensitivity to growth inhibition by AZD4547 in culture (PMID: 26992226). 26992226
FGFR2 S252W Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 S252W were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 amp FGFR2 over exp stomach cancer sensitive Fexagratinib Preclinical - Pdx Actionable In a preclinical study, AZD4547 decreased Myc expression and inhibited tumor growth in patient-derived xenograft (PDX) models of gastric cancer with FGFR2 amplification and over expression (PMID: 27401245). 27401245
FGFR2 P781* breast cancer predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited growth of mouse mammary epithelial cells expressing FGFR2 P686* (corresponding to P781* in human) in culture (PMID: 35948633). 35948633
FGFR3 A391E bladder urothelial carcinoma predicted - sensitive Fexagratinib Case Reports/Case Series Actionable In a Phase II (MATCH) trial, AZD4547 treatment resulted in an overall response rate of 10.5% (2/19) in patients with advanced solid tumors harboring FGFR2 or 3 single nucleotide variants and a 6-month progression-free survival (PFS) rate of 6%, with stable disease in 2 of 7 patients with FGFR3 activating mutations, and a partial response in a patient with urinary bladder transitional cell carcinoma harboring FGFR3 A391E (reported as A393E) (PMID: 32463741; NCT02465060). 32463741
FGFR1 G703S Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 G703S were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 N82K Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 N82K were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 R210Q Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 R210Q were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 S791T Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 S791T were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR1 A121D Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 A121D were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 C382R Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 C382R were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR1 R475Q Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 R475Q were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR3 dec exp FGFR3 wild-type HRAS G12V transitional cell carcinoma resistant Fexagratinib Preclinical Actionable In a preclinical study, urothelial cancer cells with low expression of wild-type FGFR3 that harbored HRAS G12V demonstrated resistance to AZD4547 in culture (PMID: 22869148). 22869148
FGFR1 R809Q Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 R809Q were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 I422V Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 I422V were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 act mut Advanced Solid Tumor predicted - sensitive Fexagratinib Phase II Actionable In a Phase II (MATCH) trial, AZD4547 treatment resulted in an overall response rate of 10.5% (2/19) in patients with advanced solid tumors harboring FGFR2 or 3 activating single nucleotide variants and a 6-month progression-free survival rate of 6%, with a partial response in 1 and stable disease in 2 of 12 patients with FGFR2 activating mutations (PMID: 32463741; NCT02465060). 32463741
FGFR1 R250W Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 R250W were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 E596K Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 E596K were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 wild-type endometrial cancer resistant Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, endometrial cells with Fgfr2 wild-type were resistant to the anti-proliferative effects of AZD4547 (PMID: 26294741). 26294741
FGFR1 T340M Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 T340M were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR1 A268S Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 A268S were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR1 rearrange lung small cell carcinoma sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited survival of small cell lung cancer cells harboring FGFR1 translocation in culture (PMID: 27550940). 27550940
FGFR1 over exp uterus leiomyosarcoma sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited survival of FGFR1 over expressing uterus leiomyosarcoma cells in culture (PMID: 27535980). 27535980
FGFR3 P573S lung non-small cell carcinoma no benefit Fexagratinib Case Reports/Case Series Actionable In a Phase II trial (NLMT), AZD4547 treatment did not result in a confirmed response or durable clinical benefit in a patient with non-small cell lung cancer harboring FGFR3 P575S (corresponds to P573S in the canonical isoform (PMID: 32669708, NCT02664935). 32669708
FGFR1 D320N Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 D320N were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR1 amp lung non-small cell carcinoma sensitive Fexagratinib Preclinical - Pdx Actionable In a preclinical study, AZD4547 inhibited FGFR1 signaling and resulted in tumor regression in patient-derived xenograft models of non-small cell lung carcinoma harboring FGFR1 amplification, wild-type for EGFR, K-Ras and negative for EML4-ALK fusion (PMID: 23082000). 23082000
FGFR2 H416R Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 H416R were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR3 V555M Advanced Solid Tumor resistant Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells over expressing FGFR3 V555M were resistant to AZD4547 in culture (PMID: 28034880). 28034880
FGFR2 L33S Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 L33S were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 P303L Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 P303L were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR1 V561M lung non-small cell carcinoma resistant Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, non-small cell lung cancer cells expressing FGFR1 V561M demonstrated resistance to AZD4547 in culture (PMID: 30257990). 30257990
FGFR2 N549D Advanced Solid Tumor resistant Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 N549D were resistant to treatment with AZD4547 in culture (PMID: 34272467). 34272467
FGFR2 N550K estrogen-receptor positive breast cancer sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, AZD4547 treatment decreased viability of ESR1-positive breast cancer cells expressing FGFR2 N550K in culture (PMID: 32723837). 32723837
FGFR1 R445W Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 R445W were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 E718K Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 E718K were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 M640I Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 M640I were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 M538I estrogen-receptor positive breast cancer sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, AZD4547 treatment decreased viability of ESR1-positive breast cancer cells expressing FGFR2 M538I in culture (PMID: 32723837). 32723837
FGFR2 amp Advanced Solid Tumor unknown Fexagratinib Case Reports/Case Series Actionable In a Phase II (MATCH) trial, AZD4547 treatment resulted in stable disease in 2 of 3 of patients with advanced solid tumors harboring FGFR2 amplification, with a 6-month progression-free survival rate of 0% (PMID: 32463741; NCT02465060). 32463741
FGFR3 S249C renal pelvis transitional cell carcinoma predicted - sensitive Fexagratinib Case Reports/Case Series Actionable In a Phase II (MATCH) trial, AZD4547 treatment resulted in an overall response rate of 10.5% (2/19) in patients with advanced solid tumors harboring FGFR2 or 3 activating single nucleotide variants and a 6-month progression-free survival rate of 6%, including stable disease for greater than 6 months in a patient with transitional cell carcinoma of the renal pelvis harboring FGFR3 S249C (PMID: 32463741; NCT02465060). 32463741
FGFR2 N550K endometrial cancer predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, AZD4547 treatment induced cell death in an endometrial cancer cell line harboring FGFR2 N550K in culture (PMID: 30537101). 30537101
FGFR2 N550K endometrial cancer predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, endometrial cells harboring Fgfr2 N550K were less sensitive to the anti-proliferative effects of AZD4547 than the Fgfr2 double mutant, K310R, N550K (PMID: 26294741). 26294741
FGFR1 P150S Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 P150S were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 E475K Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 E475K were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 amp breast cancer sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited survival of FGFR2 amplified breast cancer cells in culture (PMID: 27550940). 27550940
FGFR2 K660N FGFR2 amp stomach cancer predicted - resistant Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, a gastric cancer cell line harboring an FGFR2 amplification was found to have developed resistance to AZD4547 after prolonged exposure in culture, and was subsequently found to have acquired FGFR2 K660N (PMID: 32973082). 32973082
FGFR1 V751A Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 V751A were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 Y328N Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 Y328N were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR1 D128N Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 D128N were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 Q212K Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 Q212K were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR3 S249C urinary system cancer sensitive Fexagratinib Preclinical - Cell line xenograft Actionable In a preclinical study, AZD4547 decreased Myc expression and inhibited growth of a urinary tract cancer cell line harboring FGFR3 S249C in culture and in xenograft models (PMID: 27401245). 27401245
FGFR2 A264T Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 A264T were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR1 D133N Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 D133N were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR1 pos FGFR2 pos hepatocellular carcinoma sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, hepatocellular carcinoma cell lines treated with AZD4547 demonstrated decreased phosphorylation of FGFR1 and FGFR2, reduced colony formation, and evidence of apoptotic activity in culture (PMID: 26351320). 26351320
FGFR1 N546K Advanced Solid Tumor predicted - resistant Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR1 N546K were resistant to treatment with AZD4547 in culture (PMID: 34272467). 34272467
FGFR2 E163K Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 E163K were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 amp stomach cancer sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, AZD4547 inhibited growth of a gastric cancer cell line harboring FGFR2 amplification in culture (PMID: 30045926). 30045926
FGFR2 amp stomach cancer sensitive Fexagratinib Preclinical Actionable In a preclinical study, AZD4547 inhibited FGFR signaling, and decreased proliferation and induced cell-cycle arrest in gastric cancer cells with amplification and over expression of FGFR2 in culture (PMID: 22869148). 22869148
FGFR2 amp stomach cancer sensitive Fexagratinib Phase II Actionable In a Phase II clinical trial, treatment with AZD4547 resulted in a 33% (3/9) response rate in patients with FGFR2-amplified gastroesophageal cancer, and high-level amplification was associated with clinical response (PMID: 27179038). 27179038
FGFR2 K659N Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 K659N were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR3 amp urinary system cancer sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, AZD4547 decreased Myc expression, induced cell cycle arrest, and inhibited growth of a urinary tract cancer cell line harboring FGFR3 amplification in culture (PMID: 27401245). 27401245
FGFR2 R6P Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 R6P were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467
FGFR2 N549K Advanced Solid Tumor resistant Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 N549K were resistant to treatment with AZD4547 in culture (PMID: 34272467). 34272467
FGFR2 Y375C Advanced Solid Tumor predicted - sensitive Fexagratinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing FGFR2 Y375C were sensitive to treatment with AZD4547 in culture, demonstrating reduced cell viability (PMID: 34272467). 34272467

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Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries
NCT02546661 Phase I Danvatirsen + Durvalumab Durvalumab + Selumetinib Fexagratinib Durvalumab + Olaparib Durvalumab Durvalumab + Fexagratinib Durvalumab + Vistusertib Adavosertib + Durvalumab Open-Label, Randomised, Multi-Drug, Biomarker-Directed, Phase 1b Study in Pts w/ Muscle Invasive Bladder Cancer (BISCAY) Active, not recruiting USA | GBR | FRA | ESP | CAN 0
NCT02154490 Phase II Docetaxel Nivolumab Palbociclib Durvalumab Ipilimumab + Nivolumab Fexagratinib Taselisib Durvalumab + Tremelimumab Erlotinib + Rilotumumab Talazoparib Erlotinib Lung-MAP: Biomarker-Targeted Second-Line Therapy in Treating Patients With Recurrent Stage IV Squamous Cell Lung Cancer Completed USA | CAN 0


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