arbaclofen placarbil

Arbaclofen placarbil is a prodrug of R-baclofen (arbaclofen), the pharmacologically active R-enantiomer of baclofen. It was developed to improve upon the pharmacokinetic limitations of baclofen, offering more consistent plasma levels and enhanced absorption throughout the gastrointestinal tract via both passive and active mechanisms, specifically through the monocarboxylate type 1 transporter. After oral administration, it is rapidly converted to R-baclofen by human carboxylesterase-2 in various tissues. Arbaclofen placarbil acts as an agonist at gamma-aminobutyric acid type B (GABA-B) receptors, leading to inhibitory neurotransmission in the central nervous system. The drug was primarily investigated for spasticity associated with multiple sclerosis and for gastroesophageal reflux disease (GERD), but development for these indications was terminated after unsuccessful phase III trials. It has also been studied as a potential treatment for alcoholism and autism spectrum disorder[1][2][4][5][6].

Other names

arbaclofen placarbilXP19986XP-19986XP 19986