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 - 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
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
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 - 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
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 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 - 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
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
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 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
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 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 - 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 - 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
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 - 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 - 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
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
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 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 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 - 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
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
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
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 - 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
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 - 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 - 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

Filtering

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  • Separate multiple filter terms with a spaces, order doesn't matter (a b c and c b a are equivalent )
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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
  • Hold down the Shift key and click multiple columns to sort by more than one column, be sure to set ascending or descending order for a given column, before moving on to the next column.

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


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