Almorexant
Encyclopedia
Almorexant is a competitive receptor antagonist
of the OX1 and OX2 orexin
receptors, which was being developed
by the pharmaceutical companies Actelion
and GSK
for the treatment of insomnia
. Development of the drug was abandoned in January 2011.
and z drugs which dominated the multi-billion dollar insomnia medication market.
In 2008, pharmaceutical giant GlaxoSmithKline
bought the development and marketing rights for almorexant from Actelion for an initial payment of $147 million. The deal was worth a potential $3.2billion if the drug were to successfully complete clinical development and obtain FDA approval. GSK and Actelion continued to develop the drug together, and completed a Phase III clinical trial
in November 2009.
However in January 2011 Actelion and GSK announced they were abandoning the development of almorexant because of its side effect profile.
mobilization.
Receptor antagonist
A receptor antagonist is a type of receptor ligand or drug that does not provoke a biological response itself upon binding to a receptor, but blocks or dampens agonist-mediated responses...
of the OX1 and OX2 orexin
Orexin
Orexins, also called hypocretins, are the common names given to a pair of excitatory neuropeptide hormones that were simultaneously discovered by two groups of researchers in rat brains....
receptors, which was being developed
Drug development
Drug development is a blanket term used to define the process of bringing a new drug to the market once a lead compound has been identified through the process of drug discovery...
by the pharmaceutical companies Actelion
Actelion
Actelion was founded in December 1997 and is headquartered in Allschwil near Basel . Its CEO and co-founder is cardiologist Jean-Paul Clozel. Actelion scientists were among the first to work in the field of endothelian receptor antagonists...
and GSK
GlaxoSmithKline
GlaxoSmithKline plc is a global pharmaceutical, biologics, vaccines and consumer healthcare company headquartered in London, United Kingdom...
for the treatment of insomnia
Insomnia
Insomnia is most often defined by an individual's report of sleeping difficulties. While the term is sometimes used in sleep literature to describe a disorder demonstrated by polysomnographic evidence of disturbed sleep, insomnia is often defined as a positive response to either of two questions:...
. Development of the drug was abandoned in January 2011.
Development
Originally developed by Actelion, from 2007 almorexant was being reported as a potential blockbuster drug, as its novel mechanism of action (orexin receptor antagonism) was thought to produce better quality sleep and fewer side effects than the traditional benzodiazepineBenzodiazepine
A benzodiazepine is a psychoactive drug whose core chemical structure is the fusion of a benzene ring and a diazepine ring...
and z drugs which dominated the multi-billion dollar insomnia medication market.
In 2008, pharmaceutical giant GlaxoSmithKline
GlaxoSmithKline
GlaxoSmithKline plc is a global pharmaceutical, biologics, vaccines and consumer healthcare company headquartered in London, United Kingdom...
bought the development and marketing rights for almorexant from Actelion for an initial payment of $147 million. The deal was worth a potential $3.2billion if the drug were to successfully complete clinical development and obtain FDA approval. GSK and Actelion continued to develop the drug together, and completed a Phase III clinical trial
Clinical trial
Clinical trials are a set of procedures in medical research and drug development that are conducted to allow safety and efficacy data to be collected for health interventions...
in November 2009.
However in January 2011 Actelion and GSK announced they were abandoning the development of almorexant because of its side effect profile.
Mechanism of action
Almorexant is a competitive, dual OX1 and OX2 receptor antagonist and selectively inhibits the functional consequences of OX1 and OX2 receptor activation, such as intracellular Ca2+Calcium
Calcium is the chemical element with the symbol Ca and atomic number 20. It has an atomic mass of 40.078 amu. Calcium is a soft gray alkaline earth metal, and is the fifth-most-abundant element by mass in the Earth's crust...
mobilization.