Drug intelligence / Profile preview

bicalutamide + sunitinib

Development stage
Unknown
Lead developer
University at Buffalo
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination drug consisting of bicalutamide and sunitinib used in cancer treatment, specifically studied for advanced renal cell carcinoma (RCC) resistant to receptor tyrosine kinase inhibitors (RTKIs). Bicalutamide is a nonsteroidal antiandrogen that blocks androgen receptors, inhibiting the growth stimulation by androgens in prostate and possibly other cancers. Sunitinib is a small-molecule multi-targeted receptor tyrosine kinase inhibitor that targets PDGF receptors, VEGF receptors, KIT, RET, CSF-1R, and FLT3 to inhibit tumor angiogenesis and proliferation. The combination aims to provide antineoplastic effects by combining hormonal therapy with targeted RTK inhibition. Bicalutamide is administered orally at 50 mg daily; sunitinib dosing follows a schedule of two weeks on treatment followed by one week off. The combination has been evaluated in Phase I/II clinical trials for safety and efficacy in patients with advanced RCC who progressed after prior RTKI therapy.

Other names
(RS)-N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl sulfonyl]-2-hydroxy-2-methylpropanamideCASODEX + Sutent
02

Targets

CSF1R (Macrophage colony-stimulating factor receptor)PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)ABCB1 (P-glycoprotein)AR (Adrenergic receptors)VEGFR3 (Vascular endothelial growth factor receptor 3)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)ABCG2 (Breast cancer resistance protein)RET (Rearranged during transfection receptor tyrosine kinase)FLT3 (Fms related receptor tyrosine kinase 3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)

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