Drug intelligence / Profile preview

everolimus + sorafenib

Development stage
Unknown
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral
01

Overview

Everolimus + sorafenib is a combination of two small molecule targeted therapies used primarily in oncology research and clinical trials. Everolimus is an inhibitor of the mammalian target of rapamycin (mTOR), binding to FKBP-12 and blocking mTOR activity, which leads to cell cycle arrest, reduced proliferation, angiogenesis inhibition, and increased apoptosis[6]. Sorafenib is a multikinase inhibitor that targets serine/threonine kinases (including Raf-1 and B-Raf) as well as several receptor tyrosine kinases such as VEGFR-1/2/3, PDGFR-β, KIT, FLT3, and RET. This dual action blocks tumor cell proliferation via the RAF/MEK/ERK pathway and inhibits angiogenesis by targeting VEGF and PDGF signaling[8]. The combination has been studied in various cancers including hepatocellular carcinoma (HCC), thyroid cancer (differentiated thyroid cancer [DTC] and medullary thyroid cancer [MTC]), pancreatic cancer, adrenocortical carcinoma (ACC), osteosarcoma, among others. Preclinical studies suggest additive or synergistic effects on tumor growth inhibition; however, clinical benefit over monotherapy varies by indication[1][2][3][4][5].

Brand names
Nexavar
Other names
everolimus + sorafenibRAD001 + sorafenib
02

Targets

FKBP1ABRAF (B-Raf proto-oncogene, serine/threonine kinase)KIT (c-KIT proto-oncogene receptor tyrosine kinase)VEGFR2 (Vascular endothelial growth factor receptor 2)Mechanistic target of rapamycin complex 1PDGFRB (Platelet-derived growth factor receptor beta)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR3 (Vascular endothelial growth factor receptor 3)RAF1 (c-Raf-1 (Y340D/Y341D))RET (Rearranged during transfection receptor tyrosine kinase)FLT3 (Fms related receptor tyrosine kinase 3)

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