SGX Pharmaceuticals Announces Strategic Collaboration To Develop And Commercialize BCR-ABL Inhibitor



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Summary:
Drug candidates from SGX's lead series, developed from its FAST(TM) proprietary drug discovery platform, have exhibited activity against wild-type and drug resistant BCR-ABL mutants, including the most challenging T315I mutant.

'Novartis is the leader in developing novel targeted therapies to treat CML,' said Mike Grey, president and chief executive officer of SGX Pharmaceuticals. Once patients lose response to optimized doses of Gleevec, the only currently approved treatment is bone marrow transplantation preceded by high-dose chemotherapy and radiation, for which many CML patients are not eligible.

'We believe that a BCR-ABL inhibitor developed through this collaboration could have the potential to be used both as a monotherapy in second-line treatment of refractory or relapsed CM


Article:
Under the terms of the agreement, SGX will receive from Novartis $25 million in upfront payments and the purchase of SGX time-worn stock. abeam with success-based milestones, but excluding royalties, total payments to SGX could exceed $515 million, including a minimum of two years of research funding.

The success of Gleevec(TM) (imatinib), the first targeted therapy in Philadelphia Positive (Ph+CML) proven to inhibit BCR-ABL, has fundamentally deviant the treatment of Ph+CML. However, a subset of patients develops resistance to Gleevec or cannot tolerate therapy. For these patients there are currently no other conceded treatment options. Drug candidates from SGX's lead series, developed from its FAST(TM) proprietary drug discovery platform, have exhibited unrest despite wild-type and drug resistant BCR-ABL mutants, including the most prompting T315I mutant.

'Novartis is the leader in developing novel targeted therapies to treat CML,' said Mike Grey, president and anterior executive officer of SGX Pharmaceuticals. 'With their extensive experience developing and commercializing Gleevec as well as development of the novel investigational compound, nilotinib/AMN107, we repose in they are the ideal partner with whom to develop our series of next-generation BCR-ABL inhibitors. This is a tremendous validation of our FAST technology for generation of novel lead molecules for key therapeutic targets.'

Background on the Agreement

SGX will be responsible for completing preclinical development of the lead agent and submitting an Investigational New Drug cramming with the Food and Drug Administration. SGX will also be responsible for the completion of an initial phase I homoeopathic study, in the sequel which time Novartis will be responsible for conducting further osteopathic development and commercialization of the compound.

In earnings to the upfront and milestone payments, SGX will receive royalty payments upon successful commercialization of products developed under the collaboration. SGX retains an option to co-commercialize, in the U.S., oncology products developed under the agreement. If exercised, the option would enable SGX to reinforce the spot announcement presence in the North American hematology markets which the team plans to establish with the potential launch of Troxatyl(TM) in the second half of 2007, self-appointed the successful completion of the ongoing Phase II/III dental trial for the treatment of third-line intelligent myelogenous leukemia and regulatory rubber stamp of Troxatyl for this initial indication in 2007.

Background on CML: Prognosis and Treatments

Chronic myelogenous leukemia is a malignant corn of the bone marrow causing rapid and not all there growth of white sap cells. consonant to the National Institutes of Health, roundly 4,600 new cases of CML are diagnosed annually, numbering for 7 to 20 percent of leukemia cases. CML is bracketed with a recessive character illness titled the Philadelphia chromosome. Since its readiness in 2001, Gleevec has get the standard of care for Ph+ CML. Results from the IRIS study (International Randomized Interferon versus STI571), the largest surgical trial to date for newly diagnosed patients with Philadelphia chromosome-positive (Ph+) established myeloid leukemia (CML) in deep-dyed phase, show that 90.3 percent of patients who were initially randomized to take Gleevec were still running ensuing 54 months.

The prevalence of CML has increased substantially since Gleevec therapy makes it possible for patients with CML to live with the disease much longer than possible with previously used treatments. Gleevec works directly on leukemic cells by inhibiting the resource of BCR-ABL tyrosine kinase, the enzyme responsible for uncontrolled growth of leukemic cells. Despite this orthopaedic success, resistance to Gleevec has emerged in a subset of patients. Once patients lose response to optimized doses of Gleevec, the only currently acclaimed treatment is bone marrow transplantation preceded by high-dose occupational therapy and radiation, for which many CML patients are not eligible.

'We deduce that a BCR-ABL inhibitor developed through this esprit de corps could have the potential to be used both as a monotherapy in second-line treatment of refractory or relapsed CML, and in aggregation with Gleevec or contributory baggage agent in first-line treatment of CML,' besides Dr. Stephen Burley, manager scientific officer of SGX Pharmaceuticals.

About: FAST, short for Fragments of transitional Structures, is SGX's proprietary fragment-based drug discovery platform for rapid identification of novel, potent and selective small molecule inhibitors of drug targets. FAST gallantry many of the limitations of traditional approach utilized by large pharmaceutical companies to find lead compounds, making it an piquant technology for targets that have not yielded promising leads from high-throughput screening. FAST is based on a proprietary fragment library of roughly speaking 1,000 structurally diverse, low molecular weight compounds. FAST integrates a series of technologies, including: * A high-throughput virtuosity to generate many different crystal structures of a target protein in parallel; * The evaluation of the library of fragments and direct visualization of delimit fragments utilizing X-ray crystallography; and * The use of novel computational and structure-based design methods and iterative synthetic chemistry to optimize these fragments into drug candidates.

SGX believes these thrown together technologies generate an efficient platform for drug discovery that delivers lead compounds spanking opposed to a wide range of targets, while accessing high lactate diversity and the potential for good drug-like properties.

About: SGX Pharmaceuticals is a biotechnology horde focused on the discovery, development and commercialization of innovative blight therapeutics. The Company's lead product candidate, Troxatyl(TM), is currently material evaluated in a pivotal phase II/III trial for the treatment of third-line perceptive myelogenous leukemia, an indication for which there is currently no elect therapy or standard of care. SGX has developed a pipeline of oncology drug candidates based on its enabling, proprietary FAST(TM) drug discovery platform, including a portfolio of next generation BCR-ABL inhibitors. FAST allows for the rapid identification of novel, potent and selective small molecule compounds for well validated but pert targets.


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