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fanregratinib + itraconazole
- Development stage
- Unknown
- Lead developer
- HUTCHMED
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
HMPL-453 + itraconazole is a drug combination used in clinical pharmacology studies to evaluate the pharmacokinetic impact of CYP3A and P-glycoprotein (P-gp) inhibition on HMPL-453 (fanregratinib). HMPL-453 is an investigational, highly selective, and potent small molecule inhibitor of fibroblast growth factor receptors (FGFR) 1, 2, and 3, developed by HUTCHMED. It is being investigated for the treatment of advanced solid tumors, including intrahepatic cholangiocarcinoma and gastric cancer. Itraconazole, a known potent inhibitor of the CYP3A4 enzyme and P-gp transporter, is co-administered in these trials to determine if HMPL-453 is a substrate for these pathways and to guide dosing recommendations in the presence of metabolic inhibitors.
- Other names
- HMPL-453 tartrate + itraconazole
02
Targets
CYP51A1 (Sterol 14α-demethylase)CYP3A4 (Cytochrome P450 3A4)ABCB1 (P-glycoprotein)FGFR3 (Fibroblast growth factor receptor 3)FGFR2 (Keratinocyte growth factor receptor)FGFR1 (Fibroblast growth factor receptor 1)
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