derazantinib   Click here for help

GtoPdb Ligand ID: 9785

Synonyms: ARQ-087 | ARQ087
Compound class: Synthetic organic
Comment: Derazantinib (ARQ087) is an orally bioavailable, non-selective FGFR inhibitor being investigated for antineoplastic activity. Preclinical activity is reported by Hall et al. (2016) [1].
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 5
Hydrogen bond donors 2
Rotatable bonds 9
Topological polar surface area 59.07
Molecular weight 468.23
XLogP 4.73
No. Lipinski's rules broken 0
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Canonical SMILES COCCNCCc1cccc(c1)Nc1ncc2c(n1)c1ccccc1C(C2)c1ccccc1F
Isomeric SMILES COCCNCCc1cccc(c1)Nc1ncc2c(n1)c1ccccc1[C@@H](C2)c1ccccc1F
InChI InChI=1S/C29H29FN4O/c1-35-16-15-31-14-13-20-7-6-8-22(17-20)33-29-32-19-21-18-26(24-10-4-5-12-27(24)30)23-9-2-3-11-25(23)28(21)34-29/h2-12,17,19,26,31H,13-16,18H2,1H3,(H,32,33,34)/t26-/m1/s1
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Summary of Clinical Use Click here for help
Phase 1 clinical trial results in patients with advanced solid tumours are reported by Papadopoulos et al. (2017) [2]. The most appreciable objective responses were observed in patients with FGFR2 genetic alterations. The compound has progressed to Phase 3 trial (NCT03230318), specifically in patients with FGFR2 gene fusion positive tumours (inoperable or advanced intrahepatic cholangiocarcinoma).
Mechanism Of Action and Pharmacodynamic Effects Click here for help
Derazantinib promotes G1 cell cycle arrest and induction of apoptosis [1].
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT03230318 Derazantinib in Subjects With FGFR2 Gene Fusion-, Mutation- or Amplification- Positive Inoperable or Advanced Intrahepatic Cholangiocarcinoma Phase 2 Interventional Basilea Pharmaceutica