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Xenical

Roche Holding AG

Drug Names(s): Orlistat, tetrahydrolipstatin, Alli (OTC name)

Description: Xenical (Orlistat) is the first prescription treatment for obesity that does not act as an appetite suppressant. It works by interfering with the action of gastrointestinal (GI) lipase in the GI tract. As a result of this mechanism of action, 30% of ingested dietary fat is not absorbed, reducing total energy intake.

Xenical is a reversible inhibitor of lipases. It exerts its therapeutic activity in the lumen of the stomach and small intestine by forming a covalent bond with the active serine residue site of gastric and pancreatic lipases. The inactivated enzymes are thus unavailable to hydrolyze dietary fat in the form of triglycerides into absorbable free fatty acids and monoglycerides. As undigested triglycerides are not absorbed, the resulting caloric deficit may have a positive effect on weight control.

Deal Structure: In July 2004, Roche announced that it has out-licensed US non-prescription rights to orlistat to GlaxoSmithKline for an upfront payment of 120 million Swiss Francs plus milestone payments and royalties.

In February 2007, GlaxoSmithKline acquired from Roche exclusive rights to orlistat for over-the-counter (OTC) use in markets outside the US, excluding Japan. Financial terms of the agreement remains undisclosed although as part of the licensing agreement, Roche will receive an upfront payment from GSK.

In January 2009, Taisho Pharmaceutical Co. reached an agreement with Glaxo Group Limited, a subsidiary of GlaxoSmithKline, to grant Taisho the rights for the development and marketing of orlistat in Japan.

Partners: GlaxoSmithKline plc Taisho Pharmaceutical Co., Ltd.


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