Drug intelligence / Profile preview

pazopanib + gemcitabine

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

Overview

Pazopanib + gemcitabine is a combination therapy used primarily in the treatment of advanced solid tumors, including soft tissue sarcoma. Pazopanib is an oral small molecule tyrosine kinase inhibitor that targets vascular endothelial growth factor receptor 1 (VEGFR-1), vascular endothelial growth factor receptor 2 (VEGFR-2), and vascular endothelial growth factor receptor 3 (VEGFR-3), platelet-derived growth factor receptor alpha (PDGFR-α) and platelet-derived growth factor receptor beta (PDGFR-β), and c-kit, thereby inhibiting angiogenesis essential for tumor growth[6][1]. Gemcitabine is an intravenous nucleoside analog that interferes with DNA synthesis by incorporating into DNA as its active metabolite dFdCTP, leading to masked chain termination and apoptosis of malignant cells[5]. The combination has shown improved progression-free survival compared to pazopanib alone in pretreated soft tissue sarcoma patients[2][3]. The regimen is generally tolerable with adverse events consistent with those expected from each agent individually; common side effects include fatigue, neutropenia, nausea, and decreased appetite[1].

Brand names
GemzarVotrient
Other names
gemcitabine hydrochloridepazopanib hydrochloride
02

Targets

VEGFR2 (Vascular endothelial growth factor receptor 2)RNR (Ribonucleotide reductase)PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)KIT (c-KIT proto-oncogene receptor tyrosine kinase)DNAVEGFR3 (Vascular endothelial growth factor receptor 3)VEGFR-1 (Vascular endothelial growth factor receptor 1)

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