AMPLIMED PRESENTS DATA ON IMEXON IN ADVANCED SOLID TUMORS

AmpliMed reported final results from the Phase I trial of its lead drug candidate, Amplimexon (imexon for injection), in patients with advanced solid tumors. The results were presented the International Conference on Molecular Targets and Cancer Therapeutics.

Data from the Phase I study show that Amplimexon is well-tolerated and provides objective evidence of antitumor activity. The multicenter study involved 49 patients with a variety of solid tumors including melanoma, pancreatic, ovarian, colon, uterine, lung and prostate cancers. Patients were administered a range of doses from 20 to 1,000 mg/m2 of Amplimexon as a 30-minute infusion daily for five days every two weeks. The maximum tolerated dose (MTD) of this schedule of administration was determined to be 875 mg/m2/day. Pharmacokinetic studies revealed peak blood levels of imexon at the MTD that were well in excess of those shown to have antitumor effects in preclinical testing. Pharmacodynamic studies showed a correlation between a decrease in the plasma levels of cystine, a thiol-containing compound, and blood levels of imexon, providing additional support for the theory that imexon exerts its effects in part by binding thiols in cells and causing increased intracellular antioxidant levels.

Imexon is a cyanoaziridine compound that showed evidence of activity in limited studies in lung cancer, melanoma and breast cancer that were documented in publications in the 1980s. The potential of imexon as a cancer drug was never fully explored, until 1994 when AmpliMed initiated a program to decipher Amplimexon's mechanism of action. This led to the start in 2003 of a Phase I clinical study of the drug as a standalone therapy in late-stage cancer patients. Further preclinical research revealed that the combined use of Amplimexon and certain other chemotherapeutics resulted in a significant increase in efficacy compared with either drug alone. These findings are now being translated into a series of Phase I/II clinical studies of combination therapy in patients with various types of cancer.