MKC-1 is an orally-active, small molecule, cell cycle inhibitor with in vitro and in vivo efficacy against a broad range of human solid tumor cell lines, including multi-drug resistant cell lines. MKC-1 acts through multiple mechanisms of action (MOA), arresting cellular mitosis and inducing cell death (apoptosis) by binding to tubulin and to members of the importin β family, which are proteins involved in nuclear transport, spindle formation, and mitotic progression. MKC-1 also inhibits activation of the oncogenic kinase Akt and the mTOR pathway through a mechanism that is a subject of intensive investigation by EntreMed scientists.

MKC-1 has demonstrated broad antitumor effects in multiple preclinical models, including paclitaxel-resistant models, and was evaluated in several Phase 1 and 2 clinical studies involving nearly 270 patients prior to the licensing of the drug from Roche. These studies resulted in extensive pharmacokinetic and safety data.

MKC-1 is currently in multiple phase 1 and phase 2 clinical studies in cancer.Please visit the Clinical section of our website for a complete listing of clinical studies with MKC-1.