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Drug intelligence / Profile preview
vorolanib + itraconazole
- Development stage
- Phase 1
- Lead developer
- Tyrogenex
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
The combination of vorolanib and itraconazole is evaluated in clinical pharmacology studies to characterize the drug-drug interaction (DDI) profile of vorolanib. Vorolanib (formerly X-82 or CM-082) is an orally active, small-molecule multi-kinase inhibitor that targets VEGFR2, KIT, PDGFR, FLT3, and RET, primarily exerting anti-tumor effects by inhibiting angiogenesis. It is approved in China in combination with everolimus for advanced renal cell carcinoma. Itraconazole is a triazole antifungal agent and a potent inhibitor of cytochrome P450 3A4 (CYP3A4) and P-glycoprotein. Because vorolanib is primarily metabolized by CYP3A4, co-administration with itraconazole in Phase 1 crossover trials serves as a pharmacokinetic probe to evaluate the impact of strong CYP3A4 inhibition on the systemic exposure, safety, and tolerability of vorolanib.
- Other names
- itraconazole + vorolanibvorolanib and itraconazolevorolanib plus itraconazole
02
Targets
PRKAA1 (AMP-activated protein kinase alpha catalytic subunit isoform alpha-1)FLT3 (Fms related receptor tyrosine kinase 3)CYP51A1 (Sterol 14α-demethylase)PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)RET (Rearranged during transfection receptor tyrosine kinase)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)
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