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April 6, 2005 |
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- Plexxikon Inc. today announced an agreement under which Invitrogen Corporation will profile Plexxikon's proprietary kinase inhibitor libraries. These libraries represent high-value drug discovery assets based on eight different scaffolds, or chemotypes, with co-crystal structural information available and pharmaceutical properties profiled for many compounds. Under the agreement, Plexxikon's libraries will be screened in parallel against the most therapeutically relevant kinase targets among a panel of 100 enzymes available currently. Plexxikon anticipates a significant expansion of its preclinical portfolio of novel drug candidates for oncology, inflammation and metabolic disorders this year as a result of this further acceleration in its drug discovery process. Financial terms of the agreement were not disclosed.
"By strategically utilizing Invitrogen's SelectScreen™ Kinase Profiling service to profile the kinase inhibitor libraries generated via our proprietary Scaffold-Based Drug Discovery™ platform, we expect to rapidly identify the most promising starting points for development of novel inhibitors of multiple kinase targets spanning a broad array of therapeutic indications," said Gideon E. Bollag, vice president, discovery biology of Plexxikon. "Invitrogen's use of functional activity assays will provide us with the optimal read-out for determining selectivity and identification of the best drug candidates. Based on previous validation work, we anticipate producing optimized development candidates in less than six months, thereby further accelerating our timeline to IND filing."
Plexxikon already is developing a number of kinase inhibitors from these libraries, including PLX647, a dual Kit and Fms kinase inhibitor for the treatment of rheumatoid arthritis and other inflammatory diseases, and a B-Raf inhibitor for the treatment of cancer. An IND filing is targeted for PLX647 by year end 2005 and for the B-Raf inhibitor in 2006. Additionally, Plexxikon also has identified nanomolar lead compounds for numerous other therapeutic kinase targets. The company is seeking development partners for a number of these programs.
Plexxikon employs a proprietary Scaffold-Based Drug Discovery™ platform in the discovery of novel small molecules, and has developed a portfolio of clinical and preclinical stage programs for the treatment of oncology, inflammation, metabolic disorders, and other diseases. The company has applied the platform in a number of target families, including kinases, nuclear receptors, and phosphodiesterases. The platform has been highly productive in the identification and development of novel drug candidates, successfully delivering IND candidates with attractive pharmaceutical properties in approximately two years. Plexxikon's proprietary kinase inhibitor libraries are anticipated to further accelerate these pre-IND discovery and development timelines.
Plexxikon Profile
Plexxikon is a leader in the discovery and development of novel small molecule pharmaceuticals to treat human disease. Plexxikon's proprietary Scaffold-Based Drug Discovery™ platform is being applied to build therapeutic franchises in metabolic and cardiovascular disease, inflammation and oncology. This discovery process integrates a number of state-of-the-art technologies, including structural screening as one key component that provides a significant competitive advantage over other drug discovery approaches. To date, the company has discovered a portfolio of clinical and preclinical stage compounds in each of these franchises.
Currently, the company's most advanced program is a PPAR pan-agonist for the treatment of diabetes and related cardiovascular complications, with the lead candidate now in Phase 2 clinical testing in collaboration with Wyeth Pharmaceuticals. Other discovery programs include a dual kinase inhibitor for the treatment of rheumatoid arthritis and other inflammatory diseases and a renin inhibitor for hypertension in collaboration with Servier. Plexxikon is seeking pharmaceutical and biotechnology partners for select collaboration opportunities. For more information, please visit www.plexxikon.com.
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