Clinical studies of SP1049C, a polymer based anthracycline effective against drug resistant tumors. Results of phase II trial and pivotal phase Ⅲ program in upper gastrointestinal cancer indications

摘要

SP1049C is a micellar composition doxorubicin that provides is with an MDR targeted synergistic apoptotic signal toward ABC transporter (P-gp and some others) positive cancers. This is achieved through the polymer induced formation of P-gp rafts that are further transported to mitochondria of the MRD cells, which results in the depolarization of the mitochondrial membrane followed by very strong and selective uncoupling of respiration and almost complete ATP depletion in the target cells.