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SuperGen CLIMBs on board with GSK
December 2009
by Lloyd Dunlap  |  Email the author
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DUBLIN, Calif.—Using epigenetics, the same process that results in cell differentiation in the zygote without any changes in the underlying DNA sequence, SuperGen and GlaxoSmithKline PLC (GSK) have embarked on a multi-year collaboration to discover and develop cancer therapeutics using CLIMB, SuperGen's proprietary drug discovery engine. Epigenetic processes are widely believed to play a central role in the development and progression of almost all cancers.  
 
Under the terms of the agreement, SuperGen will progress candidate compounds through early clinical proof-of-concept. GSK will then have the option to develop further and commercialize resulting products worldwide. SuperGen will receive $5 million upfront, inclusive of a $3 million common stock investment, priced at a premium to market. Total potential development and commercialization milestones payable to SuperGen could exceed $375 million, in addition to the potential for tiered double-digit royalties payable on net sales of any resulting products.
 
Dr. James S.J. Manuso, chairman, president and CEO of SuperGen, notes that two-thirds of the $375 million is front-loaded, with the final third payable when a product is commercialized. GSK will pay $80 million up to the time it exercises its option or declines to do so.
 
"GSK surveyed the market and found us," says SuperGen's Manuso, "and we are excited to be working with them. We believe this collaboration is a clear validation of our discovery platform, core expertise and capabilities.
 
CLIMB—a database holding 1,021 chemistries, combinations and permutations—is SuperGen's approach to small-molecule drug discovery. According to Manuso, the in silico process merges rapid screening of compound libraries with computational chemistry and systems biology techniques to rapidly and efficiently identify drug leads that bind to target proteins.  
 
"This is not a de novo program," Manuso adds. His company has been at the business of drug discovery and development of novel cancer therapeutics that work via epigenetic and cell signaling modulation for about 10 years. SuperGen develops products through biochemical and clinical proof-of-concept, then partners with companies such as GSK for further development and commercialization.  
 
In traditional small-molecule screening, he notes, as many as several million compounds may be tested in order to identify the few that interact selectively with a disease-related protein target.
 
"HTS is high-throughput," he notes, "but low-content."
 
CLIMB, on the other hand, has achieved results by screening as few as several hundred rationally selected compounds, all of which exhibit considerable activity. This reduces the time from target identification to clinical candidate by several years, he states, and vastly decreases the cost of drug development.  
 
After lead identification, SuperGen will use proprietary assays to winnow the number of leads down to "highly likely suspects," says Manuso, at which time GSK will enter the picture. He adds that partnering with a highly respected pharmaceutical giant such as GSK goes far to legitimize CLIMB and SuperGen's capabilities to investors and the broader scientific community. Plus, he adds, it provides SuperGen with enough resources to avoid doing suboptimal deals.  
 
Manuso points out that SuperGen's Dacogen, an injectable hypomethylating agent, is currently in use for treatment of myelodysplastic syndromes under license to Eisai for North American markets and Johnson & Johnson elsewhere in the world. SuperGen has two additional drugs in clinical trials: S-110, which is a pro-drug of Dacogen that is administered subcutaneously and can be deployed against solid tumors, and a small molecule drug that can be taken orally. Dacogen is currently in clinical trials involving 485 patients who suffer from elderly AML in a comparison study against Ara-C, the current standard of care.
 
Code: E120903

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