Drug intelligence / Profile preview

fluconazole + famitinib

Development stage
Phase 1
Lead developer
Jiangsu HengRui Medicine Co., Ltd.
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination of two small molecule drugs: **Fluconazole** is a triazole antifungal agent that inhibits fungal cytochrome P450 enzyme 14α-demethylase, thereby blocking the conversion of lanosterol to ergosterol, an essential component of the fungal cell membrane. It is primarily used to treat systemic and superficial fungal infections, including candidiasis and cryptococcal meningitis[1][4]. **Famitinib** is an orally active tyrosine kinase inhibitor targeting multiple receptor tyrosine kinases such as vascular endothelial growth factor receptors 2/3, platelet-derived growth factor receptor, stem cell factor receptor (c-Kit), FMS-like tyrosine kinases Flt1 and Flt3. It has antitumor activity by inhibiting tumor angiogenesis and proliferation. Developed for advanced solid tumors including colorectal cancer, non-small cell lung cancer, gastrointestinal stromal tumors, cervical cancer, endometrial cancer, nasopharyngeal carcinoma and others[6][8][10]. The combination has been studied in drug-drug interaction trials in healthy subjects[2].

Brand names
艾比特Aibite
Other names
TriflucanDifluconazoleFluconazolumFamitinib maleate
02

Targets

VEGFR-1 (Vascular endothelial growth factor receptor 1)FLT3 (Fms related receptor tyrosine kinase 3)CYP51A1 (Sterol 14α-demethylase)CYP2C19 (Cytochrome P450 2C19)PDGFR (PDGFR family)RET (Rearranged during transfection receptor tyrosine kinase)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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