Drug intelligence / Profile preview

axitinib + everolimus

Development stage
Phase 1
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Axitinib + everolimus is a combination of two oral small molecule drugs used in oncology, primarily investigated for the treatment of advanced or metastatic solid tumors, including renal cell carcinoma. Axitinib is a potent and selective inhibitor of vascular endothelial growth factor receptor 1 (VEGFR1), vascular endothelial growth factor receptor 2 (VEGFR2), and vascular endothelial growth factor receptor 3 (VEGFR3) tyrosine kinases, thereby blocking angiogenesis and tumor growth[3][6]. Everolimus is an inhibitor of the mammalian target of rapamycin (mTOR), binding to FKBP-12 to inhibit mTOR activity; this results in reduced cell proliferation, angiogenesis, and glucose uptake[5]. The combination targets both tumor vasculature via VEGFR inhibition (axitinib) and cellular proliferation pathways via mTOR inhibition (everolimus). Clinical studies have explored this combination in patients with advanced cancers such as metastatic renal cell carcinoma; however, toxicity has limited its use[1].

Other names
axitinib + everolimus
02

Targets

FKBP1APDGFRB (Platelet-derived growth factor receptor beta)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)mTOR (Mammalian target of rapamycin kinase)

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