picoplatin

Picoplatin is a new-generation platinum-based antineoplastic agent developed to overcome resistance to earlier platinum drugs such as cisplatin. It is a sterically hindered platinum(II) complex containing a 2-methylpyridine ligand, which enhances its ability to evade deactivation by thiol-containing molecules in cancer cells. Picoplatin exerts its cytotoxic effect by binding to DNA and forming both interstrand and intrastrand cross-links, thereby inhibiting DNA replication and transcription and inducing apoptosis. It has been investigated for the treatment of various solid tumors including small cell lung cancer (SCLC), non-small cell lung cancer (NSCLC), ovarian cancer, colorectal cancer, and hormone-refractory prostate cancer. Despite promising activity in early-phase trials for several tumor types, picoplatin failed to meet primary endpoints in Phase III trials for advanced SCLC[1][2][4][5][6].

Other names

(SP-4-3)-Amminedichloro(2-methylpyridine)platiniumPicoplatin [INN]Platinum, amminedichloro(2-methylpyridine)-, (SP-4–3)