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MLN944

Celtic Pharmaceutical Holdings L.P.

Drug Names(s): XR5944

Description: MLN944 is an oral agent that acts, at least in part, by inhibiting topoisomerase I and topoisomerase II. Several chemotherapeutics target topoisomerases, including irinotecan, topotecan, doxorubicin, and etoposide. Drugs of the fluoroquinolone antibiotic class also inhibit topoisomerases. On a spectrum from selective to dual activity, MLN944 lies toward the latter.

The drug has demonstrated a favorable preclinical profile in terms of its ability to evade the unfavorable actions of certain multidrug resistance proteins and biological phenomena such as upregulated P-glycoprotein or MDR-associated protein and downregulated topoisomerase II. Preclinical data are most encouraging for development in ovarian cancer, small cell lung cancer, colorectal cancer, and cutaneous melanoma.

Deal Structure: In September 2005, Celtic Pharmaceutical completed its takeover of Xenova Group plc and took full ownership of its drug candidate portfolio.

In December 2001, Xenova and Millennium partnered to develop MLN944, MLN576, and related anti-cancer drugs.

Millennium is developing MLN944 in collaboration with Xenova Group plc, the originators of the compound. Xenova retains responsibility for performing development activities associated with the program to the end of Phase II clinical trials. For development beyond that point, Millennium will assume responsibility in North America and Xenova will retain responsibility for the rest of the world. The compound is currently in preclinical development.

In April 2008, Takeda Pharmaceutical and Millennium Pharmaceuticals announced that they entered into a definitive agreement pursuant to which Takeda will acquire Millennium for approximately $8.8 billion through a cash tender offer of $25.00 per share. The acquisition closed in May 2008.

Partners: Takeda Pharmaceutical Company Ltd


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