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Orexigen Therapeutics, Inc.

Drug Names(s): bupropion and naltrexone, Mysimba (EU), NB32

Description: Contrave is a proprietary formulation of naltrexone, used to treat narcotic and alcohol dependency, and bupropion, a dopamine and norepinephrine reuptake inhibitor. Bupropion and naltrexone are thought to act on the regulatory cells of the hypothalamus to reduce food intake and increase energy expenditure.

Proopiomelanocortin (POMC) neurons in hypothalamus express receptors for the hormone leptin (involved in adjusting food intake and energy expenditure to maintain constant levels of fat) and play a central role in the control of energy homeostasis and body weight regulation. Fat cells release leptin, which enter the brain to provide information about the body's energy stores. Stimulation of leptin receptors in POMC neurons leads to the release of alpha-MSH which, in turn, stimulate MC4 receptors to decrease food intake and increase metabolic rate. Neuropeptide Y (NPY)/agouti-related protein (AgRP) neurons release AgRP, which acts in an opposite manner.

Blockade of dopamine and norepinephrine re-uptake by bupropion increases levels of these neurotransmitters, which is thought to cause release of alpha-MSH, but reduced secretion of AgRP, thereby reducing appetitite and increasing metabolism. Naltrexone prevents natural autoinhibition of POMC neurons by beta-endorphin (acting on the mu-opioid receptor), allowing alpha-MSH release to continue.

Deal Structure: Revenue splits for this drug are BioMedTracker estimates.

Contrave was originally developed by Orexigen.

Orexigen and GSK
On June 11, 2009, Orexigen announced the licensing of certain intellectual property (IP) from GlaxoSmithKline (GSK) that expands the Company's IP position underlying Contrave. In exchange for undisclosed upfront and future milestone payments, Orexigen secured non-exclusive rights to certain formulation patents related to bupropion, one of the constituents of Contrave.

Orexigen and Patheon
In March 2010, Orexigen and Patheon announced a long-term agreement for commercial manufacturing of Contrave as well as development of future formulations of Orexigen products. The financial terms of the deal were not disclosed.

Orexigen and Takeda
In September 2010, Orexigen and Takeda announced that they have entered into an exclusive partnership to develop and commercialize Contrave in the United States, Canada and...See full deal structure in Biomedtracker

Partners: Kwang Dong Pharmaceutical Co., LTD Laboratorios Farmacéuticos Rovi, S.A. Valeant Pharmaceuticals International, Inc.

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