Howard B. Haimes, Ph.D., President
Jozef Oleksyszyn, Ph.D., V.P. of Research
Alan R. Jacobson, Ph.D., Director of Medicinial Chemistry

Product Line or Service — The goal of Akoslogic is to develop and commercialize novel and proprietary therapeutics based on two classes of small molecule enzyme inhibitors, phosphates and ketoamides directed against serine and cysteine proteases.  Its first molecular target, DPP IV, has not been commercialized.  The company’s lead compound, AKOS-1000, has been validated in peer reviewed, published independent preclinical studies of acute transplant rejection.   Potent, irreversible inhibitors of this enzyme, will be assessed for their clinical utility (human studies) against acute transplant rejection and rheumatoid arthritis.  It isexpected that AKOS-1000 will be given Orphan Drug Status by the FDA for acute transplant rejection which will benefit the Company by expedited review and possible grants to the Company.

Technology/Proprietary Rights — The company has an exclusive option to license 15 Composition of Matter Patents for phosphonate and ketoamide enzyme inhibitors, which will form the basis for the Company’s development of therapeutic agents.

Market Opportunities — Although constrained by limited organ supply, the market for immunosuppressive drugs is expected to grow at 10.3% annually over the next 5 years to 2.4 billion dollars (US).  Demand for organ transplantation has doubled since 1988.  The market for transplantation drugs was estimated as 1.5 billion dollars (US) in 1996.  Although Novartis will continue to grow its business in absolute terms, it will lose market share from 75% in 1996 to an estimated 62% in 2001.  Roche is expected to achieve a 20% market share through CellCept and Zenapax by 2001. Akoslogic expects to be able to introduce AKOS-1000 into the market rapidly for acute transplant rejection, with sales approaching 10% market share by 2003. Akoslogic expects AKOS-1000 to achieve at least a 2.5% market share for rheumatoid arthritis by year 5, with a minimum royalty stream of $5 million and $20 million in licensing payments.

Competition — Recent efforts have focused on targeting known mediators of the inflammatory cascade.  Small molecule compounds have focused on inhibition of cytokines and cyclooxygenases.  Monoclonal antibodies have been developed against  cytokine targets TNF (tumor necrosis factor ) and IL-1 (interleukin 1).  The largest player is Novartis and its U.S. marketing partner SangStat, whose Sandimmune (cyclosporine) sales are estimated to reach over $1 billion in revenue, nearly a 75% share of the market. Sandimmune is going off-patent in 1999.