Novel Sterically Hindered Platinum Complex: In Vivo Activity, Toxicology, and Pharmacokinetics in Mice'

A novel sterically hindered platinum complex, AMD473 [cis-amminedichboro(2-methylpyridine) platinum(II)J, designed primarily to be less susceptible to inactivation by thiobs, has shownin vitro activity against several ovarian carcinoma cell lines. Notably, AMD473 has shown activity in vitro in human carcinoma cells that have acquired cisplatin resistance due to reduced drug transport (41M/4lMcisR) or enhanced DNA repair/increased tolerance of platinum-DNA