PF-04136309

PF-04136309 is an orally available small molecule antagonist of the chemokine receptor CCR2. It specifically binds to CCR2 and blocks the interaction with its ligand, CCL2 (also known as monocyte chemoattractant protein 1 or MCP1), thereby inhibiting CCR2 activation and downstream signal transduction. This mechanism can suppress inflammatory processes, angiogenesis, tumor cell migration, and proliferation by preventing the recruitment of monocytes and macrophages to sites of inflammation or tumors. Developed primarily by Pfizer, PF-04136309 was investigated for its immunomodulating and antineoplastic activities in diseases such as pancreatic cancer, hepatic fibrosis, and pain[1][4][5][7]. Clinical trials included combination therapy with FOLFIRINOX chemotherapy in pancreatic cancer patients[7][8]. The drug received orphan drug status for pancreatic cancer but development has since been discontinued for all indications[4].

Other names

N-(2-((3S)-3-((trans-4-hydroxy-4-(5-(pyrimidin-2-yl)pyridin-2yl)cyclohexyl)amino)pyrrolidin1yl)-2oxoethyl)-3(trifluoromethyl)benzamideBenzamide, n-(2((3s)-3((trans4hydroxy4(5(2-pyrimidinyl) 2-pyridinyl)cyclohexyl)amino)-1-pyrrolidinyl)-2oxoethyl)-3(trifluoromethyl)