Drug intelligence / Profile preview

gemcitabine + sunitinib

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

Overview

Gemcitabine + sunitinib is a combination therapy consisting of gemcitabine, a nucleoside analog, and sunitinib, a multi-targeted receptor tyrosine kinase inhibitor. Gemcitabine works by inhibiting DNA synthesis and promoting apoptosis in malignant cells undergoing DNA synthesis. It is phosphorylated to active metabolites that compete with deoxycytidine triphosphate for incorporation into DNA, leading to chain termination and cell death. It also inhibits Ribonucleoside-diphosphate reductase large subunit and subunit M2, and UMP-CMP kinase. Sunitinib inhibits multiple receptor tyrosine kinases including VEGFR-1,-2,-3, PDGFR-α,-β, KIT, RET, CSF-1R, and FLT3, affecting both tumor angiogenesis and direct tumor cell growth. The combination has shown additive effects in inhibiting cell proliferation and inducing apoptosis in preclinical studies.

Brand names
SutentGemzar
Other names
sunitinib malategemcitabine hydrochloride
02

Targets

RNR (Ribonucleotide reductase)PDGFRA (Platelet-derived growth factor receptor alpha)KIT (c-KIT proto-oncogene receptor tyrosine kinase)CSF1R (Macrophage colony-stimulating factor receptor)DNARET (Rearranged during transfection receptor tyrosine kinase)FLT3 (Fms related receptor tyrosine kinase 3)

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