Arbaclofen placarbil

Arbaclofen Placarbil (also known as AP) is a prodrug of R-baclofen. It is designed to improve the pharmacokinetic profile of baclofen by utilizing a transport pathway to deliver more consistent and prolonged exposure.

Pharmacology

Arbaclofen Placarbil is a prodrug of R-baclofen, meaning it is metabolized in the body to produce R-baclofen. R-baclofen is the active compound that exerts the therapeutic effects. It acts as a selective agonist for the GABAB receptors, which are found in the central nervous system. This action results in decreased neuronal excitability, which can help to manage symptoms in a variety of neurological conditions.

Clinical Uses

Arbaclofen Placarbil has been investigated for use in several conditions, including spasticity related to multiple sclerosis, alcohol dependence, and gastroesophageal reflux disease (GERD). However, its most notable application is in the treatment of fragile X syndrome, a genetic disorder that causes a range of developmental problems and cognitive impairment.

Development and Approval

Arbaclofen Placarbil was developed by XenoPort, a biopharmaceutical company based in Santa Clara, California. The drug was granted Orphan Drug Designation by the Food and Drug Administration (FDA) for the treatment of fragile X syndrome. However, in 2013, XenoPort announced that it would not continue the development of Arbaclofen Placarbil due to negative results in phase III clinical trials.

See Also

• Baclofen
• Fragile X syndrome
• GABA
• Orphan drug