fruquintinib   Click here for help

GtoPdb Ligand ID: 9428

Synonyms: Elunate® | HMPL-013 | HMPL013
Approved drug
fruquintinib is an approved drug (China (2018))
Compound class: Synthetic organic
Comment: Fruquintinib (HMPL-013) is a potent and selective inhibitor of VEGFR 1, 2, 3 tyrosine kinases, being developed for potential antineoplastic efficacy [1]; preclinical data is reported in this reference.
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 4
Hydrogen bond donors 1
Rotatable bonds 6
Topological polar surface area 95.71
Molecular weight 393.13
XLogP 2.46
No. Lipinski's rules broken 0
SMILES / InChI / InChIKey
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Canonical SMILES CNC(=O)c1c(C)oc2c1ccc(c2)Oc1ncnc2c1cc(OC)c(c2)OC
Isomeric SMILES CNC(=O)c1c(C)oc2c1ccc(c2)Oc1ncnc2c1cc(OC)c(c2)OC
InChI InChI=1S/C21H19N3O5/c1-11-19(20(25)22-2)13-6-5-12(7-16(13)28-11)29-21-14-8-17(26-3)18(27-4)9-15(14)23-10-24-21/h5-10H,1-4H3,(H,22,25)
InChI Key BALLNEJQLSTPIO-UHFFFAOYSA-N
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Summary of Clinical Use Click here for help
HMPL-013 (as fruquintinib) is in Phase 3 clinical trial as monotherapy in patients with advanced non-small cell lung cancer (NSCLC; see NCT02691299) and Phase 2 for the same indication but in combination with the approved EGFR inhibitor gefitinib (see NCT02976116). In 2018 China's drug regulatory agency (NMPA) approved the use of fruquintinib to treat metastatic colorectal cancer that has been prevoiusly treated with at least 2 prior chemotherapy regimens, including those treated with anti-VEGF or anti-EGFR (WT) drugs.
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT02691299 A Phase III Clinical Trial of Fruquintinib in Patients With Advanced Non-small Cell Lung Cancer Phase 3 Interventional Hutchison Medipharma Limited
NCT02976116 A Phase II Study of Fruquintinib in Combination With Gefitinib in Patients With Advanced Non-small Cell Lung Cancer Phase 2 Interventional Hutchison Medipharma Limited
NCT02314819 A Phase III Trial Evaluating Fruquintinib Efficacy and Safety in 3+ Line Colorectal Cancer Patients (FRESCO) Phase 3 Interventional Hutchison Medipharma Limited
NCT04322539 A Study of Efficacy and Safety of Fruquintinib (HMPL-013) in Patients With Metastatic Colorectal Cancer Phase 3 Interventional Hutchison Medipharma Limited Results from this study will inform the progress of fruquintinib's development outside of China.