Drug intelligence / Profile preview

sitravatinib + itraconazole

Development stage
Phase 1
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral
01

Overview

This is a **combination of sitravatinib and itraconazole**, two small molecule drugs with distinct mechanisms of action. Sitravatinib is a multi-targeted tyrosine kinase inhibitor under investigation primarily for cancer indications, such as advanced or metastatic carcinoma, due to its inhibition of various receptor tyrosine kinases implicated in tumorigenesis and resistance to immunotherapy. Itraconazole is a triazole antifungal agent that inhibits fungal ergosterol synthesis, blocking cytochrome P448 14α-demethylase, resulting in impaired cell membrane formation and cell death. There is no evidence that sitravatinib + itraconazole is an approved or clinically investigated drug combination; instead, there is a significant potential for drug-drug interactions because itraconazole is a potent inhibitor of CYP3A4, the main enzyme responsible for metabolizing sitravatinib. Its main significance is as a possible object of drug-drug interaction studies or for understanding likely pharmacokinetic boosting or safety risks when co-administered, particularly in oncology patients.

02

Targets

CSF1R (Macrophage colony-stimulating factor receptor)CYP51A1 (Sterol 14α-demethylase)FLT3 (Fms related receptor tyrosine kinase 3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)NPC1 (Niemann-Pick C1 protein binding inhibition)TEK (Tie2)VDAC1 (Hexokinase 2–voltage-dependent anion channel 1 complex)VEGFR2 (Vascular endothelial growth factor receptor 2)

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