![]() | |
Clinical data | |
---|---|
Other names | ACT-078573 |
Routes of administration | By mouth |
Drug class | Orexin antagonist |
ATC code |
|
Pharmacokinetic data | |
Metabolism | Hepatic |
Elimination half-life | 13–19 hours [1] [2] |
Identifiers | |
| |
CAS Number |
|
PubChem CID | |
IUPHAR/BPS | |
ChemSpider | |
UNII | |
KEGG | |
ChEMBL | |
CompTox Dashboard ( EPA) | |
Chemical and physical data | |
Formula | C29H31F3N2O3 |
Molar mass | 512.573 g·mol−1 |
3D model ( JSmol) | |
| |
| |
![]() ![]() |
Almorexant ( INN), also known by its development code ACT-078573, is an orexin antagonist, acting as a competitive antagonist of the OX1 and OX2 orexin receptors, which was being developed by the pharmaceutical companies Actelion and GSK for the treatment of insomnia. [3] Development of the drug was abandoned in January 2011 due to concerns over the hepatic safety of almorexant after transient increases in liver enzymes were observed in trials. [4] [5]
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+ mobilization. It dissociates very slowly from the orexin receptors and this may prolong its duration of action. [6]
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 benzodiazepines and Z-drugs which dominated the multibillion-dollar insomnia medication market. [7]
In 2008, GlaxoSmithKline bought the development and marketing rights for almorexant from Actelion for an initial payment of $147 million. [8] The deal would have been worth an estimated $3.2 billion if the drug had successfully completed clinical development and obtained FDA approval. [9] GSK and Actelion continued to develop the drug together, and completed a Phase III clinical trial in November 2009. [10]
However, in January 2011 Actelion and GSK announced they were abandoning the development of almorexant because of its side effect profile. [4] [11]
In 2014 researchers from Actelion published work indicating that almorexant had mild abuse potential but significantly less abuse potential than zolpidem. [12]
![]() | |
Clinical data | |
---|---|
Other names | ACT-078573 |
Routes of administration | By mouth |
Drug class | Orexin antagonist |
ATC code |
|
Pharmacokinetic data | |
Metabolism | Hepatic |
Elimination half-life | 13–19 hours [1] [2] |
Identifiers | |
| |
CAS Number |
|
PubChem CID | |
IUPHAR/BPS | |
ChemSpider | |
UNII | |
KEGG | |
ChEMBL | |
CompTox Dashboard ( EPA) | |
Chemical and physical data | |
Formula | C29H31F3N2O3 |
Molar mass | 512.573 g·mol−1 |
3D model ( JSmol) | |
| |
| |
![]() ![]() |
Almorexant ( INN), also known by its development code ACT-078573, is an orexin antagonist, acting as a competitive antagonist of the OX1 and OX2 orexin receptors, which was being developed by the pharmaceutical companies Actelion and GSK for the treatment of insomnia. [3] Development of the drug was abandoned in January 2011 due to concerns over the hepatic safety of almorexant after transient increases in liver enzymes were observed in trials. [4] [5]
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+ mobilization. It dissociates very slowly from the orexin receptors and this may prolong its duration of action. [6]
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 benzodiazepines and Z-drugs which dominated the multibillion-dollar insomnia medication market. [7]
In 2008, GlaxoSmithKline bought the development and marketing rights for almorexant from Actelion for an initial payment of $147 million. [8] The deal would have been worth an estimated $3.2 billion if the drug had successfully completed clinical development and obtained FDA approval. [9] GSK and Actelion continued to develop the drug together, and completed a Phase III clinical trial in November 2009. [10]
However, in January 2011 Actelion and GSK announced they were abandoning the development of almorexant because of its side effect profile. [4] [11]
In 2014 researchers from Actelion published work indicating that almorexant had mild abuse potential but significantly less abuse potential than zolpidem. [12]