Millennium, The Takeda Oncology Company has initiated of a phase-1 trial series of MLN4924, the company's first-in-class, small molecule inhibitor of the Millennium-discovered target, the Nedd 8 Activating Enzyme (NAE).

MLN4924 advanced to the clinic with the first patient dosed in April 2008. The two phase-1 dose escalation studies aim to assess safety, tolerability, pharmacokinetic and pharmacodynamic effects in patients with advanced solid tumours or with haematological malignancies.

In addition, the company initiated a phase-1 rheumatologic trial of MLN8237, the first-in-class, specific Aurora A kinase inhibitor based on emerging pre-clinical data on the role of Aurora A in lymphomas and other rheumatologic tumours. Pre-clinical results also showed substantial activity in paediatric neuroblastoma and acute lymphocytic leukaemia (ALL).

Additional data related to the Aurora A kinase development programme are scheduled to be presented at the 20th EORTC-NCI-AACR Symposium in Geneva, Switzerland in October, 2008. Millennium plans to expand the program into Phase II trials in late 2008/early 2009.

MLN4924 targets NAE, a novel, Millennium-discovered target in the ubiquitin proteasome pathway (UPP). NAE controls a subset of proteins in the UPP that regulate cancer cell survival. MLN8237 is a second-generation small molecule backup of MLN8054, the company's first Aurora A kinase inhibitor. Both molecules were discovered and developed by scientists at Millennium for the treatment of cancer.

Millennium: The Takeda Oncology Company, and a leading biopharmaceutical company based in Cambridge, Massachusetts, markets Velcade, a novel cancer product, and has a robust clinical development pipeline of product candidates.