zanzalintinib   Click here for help

GtoPdb Ligand ID: 12093

Synonyms: CL-092 | compound 8 [WO2019148044A1] [1] | XL-092 | XL092
Compound class: Synthetic organic
Comment: We obtained the chemical structure for zanzalintinib from the WHO's proposed INN list 127 (21 July 2022). In this document it was described as a tyrosine kinase inhibitor and antineoplastic. The synonym list in PubChem's record for this compound suggests that zanzalintinib is the INN for Exelixis's clinical lead XL092 which is an analogue of cabozantinib [3]. XL092 is an ATP-competitive inhibitor of multiple RTKs including MET, VEGFR2, AXL and MER [2].
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 7
Hydrogen bond donors 3
Rotatable bonds 11
Topological polar surface area 118.65
Molecular weight 528.18
XLogP 4.34
No. Lipinski's rules broken 0
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Canonical SMILES CNC(=O)c1cc2c(ccnc2cc1OC)Oc1ccc(cc1)NC(=O)C1(CC1)C(=O)Nc1ccc(cc1)F
Isomeric SMILES Fc1ccc(cc1)NC(=O)C1(CC1)C(=O)Nc1ccc(cc1)Oc1ccnc2cc(c(cc12)C(=O)NC)OC
InChI InChI=1S/C29H25FN4O5/c1-31-26(35)22-15-21-23(16-25(22)38-2)32-14-11-24(21)39-20-9-7-19(8-10-20)34-28(37)29(12-13-29)27(36)33-18-5-3-17(30)4-6-18/h3-11,14-16H,12-13H2,1-2H3,(H,31,35)(H,33,36)(H,34,37)
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Summary of Clinical Use Click here for help
XL092 has advanced to clinical evaluations for efficacy in a range of solid tumours.
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT05425940 Study of XL092 + Atezolizumab vs Regorafenib in Subjects With Metastatic Colorectal Cancer Phase 3 Interventional Exelixis
NCT05176483 Study of XL092 in Combination With Immuno-Oncology Agents in Subjects With Solid Tumors Phase 1 Interventional Exelixis
NCT03845166 A Study of XL092 as Single-Agent and Combination Therapy in Subjects With Solid Tumors Phase 1 Interventional Exelixis