mipicoledine

Mipicoledine (also known as DM‑CHOC‑PEN or 4-demethyl‑4-cholesteryloxycarbonylpenclomedine) is a small molecule, polychlorinated pyridine cholesteryl carbonate derivative of penclomedine with potential antitumor activity. It acts primarily as a non-classical alkylating agent, binding to and alkylating DNA at the N7 position of guanine, leading to DNA crosslinking, inhibition of DNA replication, cell cycle arrest, and apoptosis. The drug’s lipophilic cholesteryl moiety enables it to cross the blood-brain barrier and be administered intravenously for central nervous system (CNS) tumors—unlike other alkylators that require intracranial delivery. Mipicoledine has demonstrated preclinical efficacy in models of glioma, breast cancer brain metastases, melanoma, and sarcoma. Clinical trials have reached Phase II for advanced cancers involving the CNS. The primary dose-limiting toxicity observed is hepatic (elevated bilirubin), with no significant neurotoxicity reported[1][2][5][6][7].

Other names

mipicoledine