MILLENNIUM BEGINS PHASE I TRIAL OF IKK2 INHIBITOR

Millennium Pharmaceuticals has initiated a Phase I study of MLN0415, an oral, highly selective, small-molecule inhibitor of IKK2, which targets a major inflammatory pathway. The randomized, double-blind, placebo-controlled study will enroll up to 72 healthy volunteers and assess safety, tolerability, pharmacokinetic and pharmacodynamic effects. MLN0415 has a unique mechanism of action that has the potential to address multiple inflammatory disorders including rheumatoid arthritis and multiple sclerosis.

In preclinical studies, MLN0415 was shown to decrease NF-kB activation and down-regulate the expression of a number of inflammatory proteins. Because inflammatory proteins play a critical role in inflammation and drive the inflammatory response to disease, controlling these proteins may prevent or slow disease progression.

Millennium and sanofi-aventis have an alliance focused on developing and commercializing small-molecule drugs for the treatment of inflammatory diseases such as rheumatoid arthritis and multiple sclerosis. MLN0415 is one of several small molecules that are part of this collaboration, of which three are in clinical trials.