Therapy Detail

Therapy Name Derazantinib
Synonym
Therapy Description

Derazantinib (ARQ 087) is an ATP-competitive multi-kinase inhibitor with activity against Fgfr 1/2, FGFR fusions, Arg, Lck, and Kit, which prevents cell proliferation and angiogenesis (PMID: 27627808).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Derazantinib ARQ 087 FGFR1 Inhibitor 21 FGFR2 Inhibitor 15 KIT Inhibitor 50 Derazantinib (ARQ 087) is an ATP-competitive multi-kinase inhibitor with activity against Fgfr 1/2, FGFR fusions, Arg, Lck, and Kit, which prevents cell proliferation and angiogenesis (PMID: 27627808).
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
FGFR2 over exp Advanced Solid Tumor sensitive Derazantinib Preclinical - Cell line xenograft Actionable In a preclinical study, Derazantinib (ARQ 087) inhibited growth of transformed cells overexpressing Fgfr2 in culture and in cell line xenograft models (PMID: 27627808). 27627808
FGFR3-TACC3 urinary bladder cancer sensitive Derazantinib Preclinical - Cell culture Actionable In a preclinical study, Derazantinib (ARQ 087) inhibited growth of bladder cancer cell lines harboring FGFR3-TACC3 fusion in culture (PMID: 27627808). 27627808
FGFR2 fusion intrahepatic cholangiocarcinoma sensitive Derazantinib Phase I Actionable In a Phase I trial, Derazantinib (ARQ 087) treatment resulted in partial response in 2 and stable disease in 1 of the 5 intrahepatic cholangiocarcinoma patients harboring FGFR2 fusions, and progressive disease in 5 patients without FGFR aberrations (PMID: 28972963; NCT01752920). detail... 28972963
FGFR1 over exp Advanced Solid Tumor sensitive Derazantinib Preclinical - Cell culture Actionable In a preclinical study, Derazantinib (ARQ 087) inhibited growth of transformed cells overexpressing Fgfr1 in culture (PMID: 27627808). 27627808
KIT over exp Advanced Solid Tumor sensitive Derazantinib Preclinical - Cell culture Actionable In a preclinical study, Derazantinib (ARQ 087) inhibited growth of transformed cells overexpressing Kit in culture (PMID: 27627808). 27627808
FGFR1 amp adrenocortical carcinoma sensitive Derazantinib Phase I Actionable In a Phase I trial, ARQ 087 treatment resulted in stable disease with a tumor reduction of 20% in an adrenocortical carcinoma patient harboring FGFR1 amplification, who remained on study for 3.5 years (PMID: 28972963; NCT01752920). 28972963
FGFR3 K652E urinary bladder cancer sensitive Derazantinib Preclinical - Cell culture Actionable In a preclinical study, Derazantinib (ARQ 087) inhibited growth of bladder cancer cells harboring FGFR3 K652E in culture (PMID: 27627808). 27627808
FGFR2 amp FGFR2-COL14A1 colon cancer sensitive Derazantinib Preclinical - Cell line xenograft Actionable In a preclinical study, Derazantinib (ARQ 087) inhibited Fgfr signaling and growth of colon cancer cells harboring FGFR2 amplification and FGFR2-COL14A1 fusion in culture and in cell line xenograft models (PMID: 27627808). 27627808
FGFR2 N549K endometrial cancer sensitive Derazantinib Preclinical - Cell culture Actionable In a preclinical study, Derazantinib (ARQ 087) inhibited growth of endometrial cancer cell lines harboring FGFR2 N549K in culture (PMID: 27627808). 27627808
FGFR2 amp breast cancer sensitive Derazantinib Preclinical - Cell culture Actionable In a preclinical study, Derazantinib (ARQ 087) inhibited growth of breast cancer cells harboring FGFR2 amplification in culture (PMID: 27627808). 27627808
FGFR2 S252W endometrial cancer sensitive Derazantinib Preclinical - Cell culture Actionable In a preclinical study, Derazantinib (ARQ 087) inhibited growth of endometrial cancer cells harboring FGFR2 S252W in culture (PMID: 27627808). 27627808
FGFR3-BAIAP2L1 Advanced Solid Tumor sensitive Derazantinib Preclinical - Cell culture Actionable In a preclinical study, Derazantinib (ARQ 087) inhibited growth of transformed cells expressing FGFR3-BAIAP2L1 in culture (PMID: 27627808). 27627808
FGFR2 amp FGFR2 fusion stomach cancer sensitive Derazantinib Preclinical - Cell line xenograft Actionable In a preclinical study, Derazantinib (ARQ 087) inhibited Fgfr signaling and growth of gastric cancer cells harboring FGFR2 amplification and PDHX-FGFR2 fusion in culture, resulted in tumor regression in cell line xenograft models (PMID: 27627808). 27627808
Unknown unknown Advanced Solid Tumor not applicable Derazantinib Phase I Actionable In a Phase I trial, Derazantinib (ARQ 087) treatment resulted in partial response in 4.5% (3/67) and stable disease in 38.8% (26/67) of patients with advanced solid tumors (PMID: 28972963; NCT01752920). 28972963
FGFR3-BAIAP2L1 urinary bladder cancer sensitive Derazantinib Preclinical - Cell culture Actionable In a preclinical study, Derazantinib (ARQ 087) inhibited growth of bladder cancer cells harboring FGFR3-BAIAP2L1 fusion in culture (PMID: 27627808). 27627808
FGFR2-CASP7 Advanced Solid Tumor sensitive Derazantinib Preclinical - Cell culture Actionable In a preclinical study, Derazantinib (ARQ 087) inhibited growth of transformed cells expressing FGFR2-CASP7 in culture (PMID: 27627808). 27627808
SRC amp non-small cell lung carcinoma sensitive Derazantinib Phase I Actionable In a Phase I trial, ARQ 087 treatment resulted in 25% tumor reduction and stable disease for 36 weeks in a squamous non-small cell lung carcinoma patient harboring SRC amplification (PMID: 28972963; NCT01752920). 28972963 detail...
FGFR2 amp stomach cancer sensitive Derazantinib Preclinical - Cell culture Actionable In a preclinical study, Derazantinib (ARQ 087) inhibited Fgfr signaling and growth of gastric cancer cells harboring FGFR2 amplification in culture (PMID: 27627808). 27627808
FGFR1 fusion hematologic cancer sensitive Derazantinib Preclinical - Cell culture Actionable In a preclinical study, Derazantinib (ARQ 087) inhibited growth of hematologic cancer cells harboring FGFROP2-FGFR1 fusion in culture (PMID: 27627808). 27627808
FGFR2 - CIT Advanced Solid Tumor sensitive Derazantinib Preclinical - Cell culture Actionable In a preclinical study, Derazantinib (ARQ 087) inhibited growth of transformed cells expressing FGFR2-CIT in culture (PMID: 27627808). 27627808
Clinical Trial Phase Therapies Title Recruitment Status
NCT03230318 Phase III Derazantinib ARQ 087 in Subjects With FGFR2 Gene Fusion Positive Inoperable or Advanced Intrahepatic Cholangiocarcinoma Recruiting
NCT01752920 Phase I Derazantinib Phase 1 Dose Escalation Study of ARQ 087 in Adult Subjects With Advanced Solid Tumors Completed