Therapy Detail

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Therapy Name Derazantinib
Synonyms
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 23 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).

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
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
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
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
FGFR2 - CCAR2 intrahepatic cholangiocarcinoma predicted - sensitive Derazantinib Case Reports/Case Series Actionable In a Phase Ib/II trial, a patient with intrahepatic cholangiocarcinoma harboring FGFR2-CCAR2 demonstrated stable disease when treated with Derazantinib (ARQ 087) (PMID: 30420614; NCT01752920). 30420614
FGFR2 - TACC1 intrahepatic cholangiocarcinoma predicted - resistant Derazantinib Case Reports/Case Series Actionable In a Phase Ib/II trial, a patient with intrahepatic cholangiocarcinoma harboring FGFR2-TACC1 demonstrated progressive disease when treated with Derazantinib (ARQ 087) (PMID: 30420614; NCT01752920). 30420614
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
FGFR2 - TACC2 intrahepatic cholangiocarcinoma predicted - sensitive Derazantinib Case Reports/Case Series Actionable In a Phase Ib/II trial, a patient with intrahepatic cholangiocarcinoma harboring FGFR2-TACC2 demonstrated sensitivity to treatment with Derazantinib (ARQ 087) (PMID: 30420614; NCT01752920). 30420614
FGFR2 - AHCYL1 intrahepatic cholangiocarcinoma predicted - sensitive Derazantinib Case Reports/Case Series Actionable In a Phase Ib/II trial, a patient with intrahepatic cholangiocarcinoma harboring FGFR2-AHCYL1 demonstrated stable disease when treated with Derazantinib (ARQ 087) (PMID: 30420614; NCT01752920). 30420614
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 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
FGFR2 fusion FGFR2 amp 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
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 - CCDC6 intrahepatic cholangiocarcinoma predicted - sensitive Derazantinib Case Reports/Case Series Actionable In a Phase Ib/II trial, a patient with intrahepatic cholangiocarcinoma harboring FGFR2-CCDC6 demonstrated stable disease when treated with Derazantinib (ARQ 087) (PMID: 30420614; NCT01752920). 30420614
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
FGFR2 - SH3GLB1 intrahepatic cholangiocarcinoma predicted - sensitive Derazantinib Case Reports/Case Series Actionable In a Phase Ib/II trial, a patient with intrahepatic cholangiocarcinoma harboring FGFR2-SH3GLB1 demonstrated a partial response when treated with Derazantinib (ARQ 087) (PMID: 30420614; NCT01752920). 30420614
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 - COL14A1 FGFR2 amp 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
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 - CIT intrahepatic cholangiocarcinoma predicted - resistant Derazantinib Case Reports/Case Series Actionable In a Phase Ib/II trial, a patient with intrahepatic cholangiocarcinoma harboring FGFR2-CIT demonstrated progressive disease when treated with Derazantinib (ARQ 087) (PMID: 30420614; NCT01752920). 30420614
SRC amp lung non-small cell carcinoma sensitive Derazantinib Case Reports/Case Series Actionable In a Phase I trial, Derazantinib (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 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
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
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
FGFR2 - BFSP2 intrahepatic cholangiocarcinoma predicted - sensitive Derazantinib Case Reports/Case Series Actionable In a Phase Ib/II trial, a patient with intrahepatic cholangiocarcinoma harboring FGFR2-BFSP2 demonstrated stable disease when treated with Derazantinib (ARQ 087) (PMID: 30420614; NCT01752920). 30420614
FGFR2 - BICC1 intrahepatic cholangiocarcinoma predicted - sensitive Derazantinib Case Reports/Case Series Actionable In a Phase Ib/II trial, treatment with Derazantinib (ARQ 087) in four patients with intrahepatic cholangiocarcinoma harboring FGFR2-BICC1 resulted in one partial response, stable disease in two, and progressive disease in one (PMID: 30420614; NCT01752920). 30420614
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
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
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 fusion intrahepatic cholangiocarcinoma sensitive Derazantinib Phase I Actionable In a Phase Ib/II trial, Derazantinib (ARQ 087) treatment resulted in an overall response rate of 20.7% (6/29), a disease control rate of 82.8% (24/29), and a median progression-free survival of 5.7 months in patients with intrahepatic cholangiocarcinoma harboring FGFR2 fusions (PMID: 30420614; NCT01752920). 30420614
FGFR2 - KIAA1217 intrahepatic cholangiocarcinoma predicted - sensitive Derazantinib Case Reports/Case Series Actionable In a Phase Ib/II trial, treatment with Derazantinib (ARQ 087) in two patients with intrahepatic cholangiocarcinoma harboring FGFR2-KIAA1217 resulted in one with a partial response and one with stable disease (PMID: 30420614; NCT01752920). 30420614

Filtering

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  • Use quotes to match a longer phrase which contains spaces "mtor c1483f"

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  • Click on any column header arrows to sort by that column
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Clinical Trial Phase Therapies Title Recruitment Status
NCT04045613 Phase Ib/II Derazantinib Atezolizumab + Derazantinib Derazantinib and Atezolizumab in Patients With Urothelial Cancer (FIDES-02) Recruiting
NCT01752920 Phase I Derazantinib Phase 1 Dose Escalation Study of ARQ 087 in Adult Subjects With Advanced Solid Tumors Completed
NCT03230318 Phase III Derazantinib ARQ 087 in Subjects With FGFR2 Gene Fusion Positive Inoperable or Advanced Intrahepatic Cholangiocarcinoma Recruiting


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