GSK3052230 + pemetrexed + cisplatin

GSK3052230 + pemetrexed + cisplatin is an experimental combination regimen for treating cancers, notably malignant pleural mesothelioma and non-small cell lung cancer. GSK3052230 (also called FP-1039) is a recombinant fusion protein that acts as a ligand trap for fibroblast growth factors (FGFs); it is designed to sequester members of the FGF family, particularly FGF2, thereby inhibiting FGF receptor signaling implicated in tumor growth and angiogenesis. Pemetrexed is a multi-targeted antifolate chemotherapy that disrupts folate-dependent enzymatic processes essential for DNA replication and cell proliferation, while cisplatin is a platinum-based chemotherapeutic that forms DNA cross-links leading to apoptosis in rapidly dividing cancer cells. The combination is administered intravenously and has shown improved survival in clinical trials when pemetrexed and cisplatin are compared to cisplatin alone in pleural mesothelioma. GSK3052230 is under development as an adjunct to this backbone to further inhibit FGF-driven cancer proliferation.

Other names

pemetrexed + cisplatin (for this combination)