pazopanib + temozolomide

pazopanib + temozolomide is a combination therapy investigated for the treatment of advanced pancreatic neuroendocrine tumors (PNETs). Pazopanib is an oral, multitargeted tyrosine kinase inhibitor (TKI) that targets vascular endothelial growth factor receptors (VEGFR-1, -2, and -3), platelet-derived growth factor receptors (PDGFR-α and -β), and the stem cell factor receptor (c-Kit), thereby inhibiting angiogenesis and tumor cell proliferation. Temozolomide is an oral alkylating agent and a derivative of dacarbazine that undergoes rapid chemical conversion at physiological pH to the active compound MTIC, which methylates DNA (primarily at the O6 and N7 positions of guanine), leading to DNA mismatch repair-mediated cell death. This combination was the subject of a Phase I/II clinical trial (NCT01465659) led by Northwestern University to determine the safety, maximum tolerated dose, and efficacy in patients with unresectable or metastatic PNETs.

Other names

pazopanib hydrochloride + temozolomide