Blood Publication Shows MLN4924 Preclinical Activity In Lymphoma

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BlankBlood Publication Shows MLN4924 Preclinical Activity In Lymphoma

05 Sep 2010

Millennium: The Takeda Oncology Company announced the publication of an article

in the journal Blood describing the novel mechanism of action of MLN4924 through

targeted pathway modulation in diffuse large B-cell lymphoma (DLBCL). MLN4924 is

a small molecule inhibitor of the NEDD8-Activating Enzyme (NAE), a key component

of the protein homeostasis pathway. It is the first small molecule inhibitor

specifically targeting this class of enzyme to be studied clinically, and is

currently being examined in Phase I clinical trials.

NAE is an enzyme that modulates the level of proteins critical for the

regulation of cancer cell growth and survival pathways. One such pathway that is

controlled by NAE is the NF-?B signaling pathway, known to be important in the

survival of some types of DLBCL. The publication in Blood demonstrates that

MLN4924 has antitumor activity in preclinical DLBCL models through the

inhibition of the NF-?B pathway. In addition, the publication showed that

MLN4924 has antitumor activity in non-NF-?B dependent DLBCLs through other

mechanisms including DNA re-replication.

" The research highlighted in this paper shows a strong rationale for the

clinical development of MLN4924 in lymphoma, particularly NF-?B dependent

lymphomas, and in additional cancers with NF-?B implications, " said G.

, Senior Scientist at Millennium and lead author of the publication.

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