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Santen Pharmaceutical Co., Ltd.

Drug Names(s): DE-109, rapamycin, Sirolimus

Description: Sirolimus is a macrocyclic lactone produced by Streptomyces hygroscopicus found in the soil of Easter Island. Structurally, sirolimus resembles tacrolimus and binds to the same intracellular binding protein or immunophilin known as FKBP-12. However, sirolimus has a novel mechanism of action. Whereas tacrolimus and cyclosporine block lymphokine (e.g., IL2) gene transcription , sirolimus acts later to blocks IL2-dependent T lymphocyte proliferation and the stimulation caused by cross-linkage of CD28, possibly by blocking activation of a kinase referred to as mammalian target of rapamycin or mTOR, a serine-threonine kinase that is important for cell cycle progression. Therefore, sirolimus is believed to act in synergy with cyclosporine (or tacrolimus) in suppressing the immune system.

Deal Structure: In May 2008, Santen acquired rights from MacuSight for the Japanese and Asian development and commercialization for all ophthalmic indications of sirolimus (DE-109).

Santen acquired global development, manufacturing and marketing rights ofsirolimus from MacuSight in June 2010.

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