Drug intelligence / Profile preview

enzalutamide + sorafenib

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

Overview

Enzalutamide + sorafenib is a combination of two small molecule drugs investigated primarily for advanced cancers, including hepatocellular carcinoma (HCC) and castration-resistant prostate cancer (CRPC). Enzalutamide is an androgen receptor antagonist that blocks multiple steps in the androgen receptor signaling pathway, thereby inhibiting tumor growth driven by androgens. Sorafenib is an oral multikinase inhibitor that targets cell surface tyrosine kinase receptors and downstream kinases involved in tumor proliferation and angiogenesis, notably inhibiting the RAF/MEK/ERK pathway as well as VEGFR and PDGFR signaling. The combination has been studied for potential synergistic effects; preclinical models suggest enhanced inhibition of both AR and ERK pathways, but clinical studies have shown limited additional benefit over monotherapy in HCC. Both drugs are approved individually for other indications but not as a combination[1][2][3][4][8].

Brand names
Nexavar
02

Targets

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

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