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XL281

Exelixis, Inc.

Drug Names(s): BMS-908662

Description: XL281 is adesigned to specifically inhibit RAF kinases, which lie immediately downstream of RAS and are components of the RAS/RAF/MEK/ERK kinase signaling pathway. Genetic lesions that activate this pathway are common in human tumors, with activating mutations in K-RAS occurring in 30 percent of tumors and activating mutations in B-RAF occurring in approximately 60 percent of melanomas. The RAS/RAF/MEK/ERK pathway also plays a role in the transmission of growth-promoting signals downstream of receptor tyrosine kinases. This suggests that deregulation of this pathway plays a role in the progression of many human tumors, and that inhibition of the pathway may provide clinical benefit in the treatment of cancer.

Deal Structure: GlaxoSmithKline and Exelixis
GlaxoSmithKline and Exelixis have a partnership focused on the collaboration in 12 programs (XL784, XL647, XL999, XL880, XL184, XL820, XL844, XL281, XL418, XL228 and two earlier stage oncology programs). GlaxoSmithKline has the right to select from these programs up to two compounds at proof-of-concept (completion of Phase IIa clinical trial) or three compounds if GlaxoSmithKline extends the collaboration.

In June 2008, Exelixis announced that the company and GlaxoSmithKline will bring their collaboration to a conclusion on October 27, 2008.

In October 2008, Exelixis announced that GlaxoSmithKline decided not to exercise its option to license XL184, XL281, XL228, XL820, and XL844.

Bristol-Myers Squibb and Exelixis
In December 2008, Bristol-Myers Squibb and Exelixis announced a global collaboration covering two novel molecules for cancer with their associated development programs: Exelixis' XL184 and XL281.

Under the...See full deal structure in Biomedtracker


XL281 News


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