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vorolanib + rifampicin
- Development stage
- Phase 1
- Lead developer
- Tyrogenex
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Vorolanib + rifampicin is a drug-drug interaction clinical trial regimen consisting of the co-administration of vorolanib and rifampicin. Vorolanib (formerly X-82 or CM082) is an orally active, small-molecule multi-targeted receptor tyrosine kinase inhibitor that potently inhibits VEGFR2, PDGFR, KIT, FLT3, and RET, thereby suppressing tumor angiogenesis and proliferation. Rifampicin is a semi-synthetic rifamycin antibiotic and a potent inducer of cytochrome P450 enzymes, particularly CYP3A4, via activation of the pregnane X receptor (PXR). In this combination, rifampicin is utilized as a pharmacokinetic tool rather than a therapeutic agent to evaluate the impact of strong CYP3A4 induction on the pharmacokinetics, safety, and exposure of vorolanib in healthy participants. This clinical evaluation is sponsored by Betta Pharmaceuticals.
- Other names
- rifampicin + vorolanibvorolanib and rifampicinvorolanib/rifampicin
02
Targets
PRKAA1 (AMP-activated protein kinase alpha catalytic subunit isoform alpha-1)FLT3 (Fms related receptor tyrosine kinase 3)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)PXR (Pregnane X receptor)
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