Zanzalintinib (XL092) is an orally active, ATP-competitive inhibitor of multiple receptor tyrosine kinases (RTKs) including MET, VEGFR2, AXL and MER, with IC50s in cell-based assays of 15 nM, 1.6 nM, 3.4 nM, 7.2 nM respectively. Zanzalintinib exhibits anti-tumor activity. Zanzalintinib has the potential for kinase-dependent diseases and conditions research[1][2].
Zanzalintinib (10 mg/kg/day; oral; for 14 days) causes substantial tumor growth inhibition in xenograft studies. Zanzalintinib shows 82% and 96% inhibition on p-MET and p-VEGFR2, respectively[1].
Zanzalintinib (compound 8; 3 mg/kg; iv) has a T1/2 of 5.4 hours, a CL of 43 mL/hr kg. Zanzalintinib (3 mg/kg; po) has a T1/2 of 7.1 hours and a Cmax of 11.4 μM for rats[2].
| Animal Model: | Rat[1] |
| Dosage: | 3 mg/kg (Pharmacokinetic Analysis) |
| Administration: | IV |
| Result: | Had a T1/2 of 5.4 hours, a CL of 43 mL/hrkg. |
Axl; Mer; VEGFR2: 1.6 nM (IC50); AXL: 3.4 nM (IC50); MER: 7.2 nM (IC50)
[1] J. Hsu, et al. XL092, a multi-targeted inhibitor of MET, VEGFR2, AXL and MER with an optimized pharmacokinetic profile. European Journal of Cancer, Volume 138, Supplement 2, October 2020, Page S16.
[2] Lynne Canne Bannen, et al. Compounds for the treatment of kinase-dependent disorders. WO2019148044A1.
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