Page last updated: 2024-10-14

arbaclofen placarbil

Description

arbaclofen placarbil: an R-baclofen prodrug; may improve the treatment of patients with gastroesophageal reflux disease, spasticity; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID11281011
CHEMBL ID2107312
SCHEMBL ID351833
MeSH IDM0539122

Synonyms (30)

Synonym
arbaclofen placarbil (usan/inn)
847353-30-4
D08861
xp-19986
w89h91r7vx ,
arbaclofen placarbil [usan:inn]
(3r)-3-(4-chlorophenyl)-4-((((1s)-2-methyl-1-((2- methylpropanoyl)oxy)propoxy)carbonyl)amino)butanoic acid
arbaclofen placarbil
benzenepropanoic acid, 4-chloro-beta-(((((1s)-2-methyl-1-(2-methyl-1-oxopropoxy)propoxy)carbonyl)amino)methyl)-, (betar)-
unii-w89h91r7vx
xp19986
xp 19986
CHEMBL2107312
SCHEMBL351833
arbaclofen placarbil [mi]
arbaclofen placarbil [usan]
(3r)-3-(4-chlorophenyl)-4-[[[(1s)-2-methyl-1-[(2-methylpropanoyl)oxy]propoxy]carbonyl]amino]butanoic acid
benzenepropanoic acid, 4-chloro-.beta.-(((((1s)-2-methyl-1-(2-methyl-oxopropoxy)propoxy)carbonyl)amino)methyl)-, (.beta.r)-
arbaclofen placarbil [inn]
DTXSID40233754
benzenepropanoic acid, 4-chloro-b-[[[[(1s)-2-methyl-1-(2-methyl-1-oxopropoxy)propoxy]carbonyl ]amino]methyl]-, (br)-
DB08892
JXTAALBWJQJLGN-KSSFIOAISA-N
(3r)-4-{[(1s)-2-methyl-1-(2-methylpropanoyloxy)propoxy]carbonylamino}-3-(4-chlorophenyl)butanoic acid
Q15408425
(r)-3-(4-chlorophenyl)-4-((((s)-1-(isobutyryloxy)-2-methylpropoxy)carbonyl)amino)butanoic acid
HY-14735
(3r)-3-(4-chlorophenyl)-4-[[(1s)-2-methyl-1-(2-methylpropanoyloxy)propoxy]carbonylamino]butanoic acid
CS-0003528
AKOS040750560

Research Excerpts

Overview

Arbaclofen placarbil has been shown to reduce reflux episodes in patients with gastro-oesophageal reflux disease (GERD) It is designed to be absorbed throughout the intestine by both passive and active mechanisms via the monocarboxylate type 1 transporter.

ExcerptReference
"Arbaclofen placarbil is a pro-drug of the gamma-aminobutyric acid-B agonist R-baclofen that has been shown to reduce reflux episodes in patients with gastro-oesophageal reflux disease (GERD)."( Randomised clinical trial: arbaclofen placarbil in gastro-oesophageal reflux disease--insights into study design for transient lower sphincter relaxation inhibitors.
Cundy, KC; Huff, FJ; Vakil, NB, 2013
)
"Arbaclofen placarbil is a novel transported prodrug of the pharmacologically active R-isomer of baclofen designed to be absorbed throughout the intestine by both passive and active mechanisms via the monocarboxylate type 1 transporter."( Arbaclofen placarbil, a novel R-baclofen prodrug: improved absorption, distribution, metabolism, and elimination properties compared with R-baclofen.
Annamalai, T; Bao, Y; Bu, L; Cundy, KC; Dias, T; Gallop, MA; Gao, M; Koller, K; Lal, R; Ludwikow, M; Luo, W; Nguyen, S; Peng, G; Phan, T; Raillard, SP; Scheuerman, RA; Sukbuntherng, J; Tai, EH; Upadhyay, S; Warren, MS; Wu, QQ; Yan, H; Yao, F; Zamora, J, 2009
)

Bioavailability

ExcerptReference
" Sustained release formulations of arbaclofen placarbil demonstrated sustained R-baclofen exposure in dogs with bioavailability up to 68%."( Arbaclofen placarbil, a novel R-baclofen prodrug: improved absorption, distribution, metabolism, and elimination properties compared with R-baclofen.
Annamalai, T; Bao, Y; Bu, L; Cundy, KC; Dias, T; Gallop, MA; Gao, M; Koller, K; Lal, R; Ludwikow, M; Luo, W; Nguyen, S; Peng, G; Phan, T; Raillard, SP; Scheuerman, RA; Sukbuntherng, J; Tai, EH; Upadhyay, S; Warren, MS; Wu, QQ; Yan, H; Yao, F; Zamora, J, 2009
)

Dosage Studied

ExcerptReference
" Arbaclofen placarbil was efficiently absorbed and rapidly converted to R-baclofen after oral dosing in rats, dogs, and monkeys."( Arbaclofen placarbil, a novel R-baclofen prodrug: improved absorption, distribution, metabolism, and elimination properties compared with R-baclofen.
Annamalai, T; Bao, Y; Bu, L; Cundy, KC; Dias, T; Gallop, MA; Gao, M; Koller, K; Lal, R; Ludwikow, M; Luo, W; Nguyen, S; Peng, G; Phan, T; Raillard, SP; Scheuerman, RA; Sukbuntherng, J; Tai, EH; Upadhyay, S; Warren, MS; Wu, QQ; Yan, H; Yao, F; Zamora, J, 2009
)
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (15)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (6.67)29.6817
2010's14 (93.33)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials7 (46.67%)5.53%
Reviews5 (33.33%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other3 (20.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (8)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Randomized, Double Blind, Placebo-Controlled Efficacy and Safety Study of Arbaclofen Placarbil in Subjects With Spasticity Due to Multiple Sclerosis[NCT01359566]Phase 3228 participants (Actual)Interventional2011-05-31Completed
A Randomized, Double-blind, Placebo-controlled Study to Evaluate the Safety and Tolerability of XP19986 in Subjects With Acute Back Spasms[NCT00817986]Phase 2161 participants (Actual)Interventional2008-12-31Completed
A Randomized, Double-Blind, Placebo-Controlled, Dose-Escalation Study to Determine the Maximum Tolerated Dose of Arbaclofen Placarbil in Subjects With Alcohol Use Disorder[NCT02511886]Phase 218 participants (Actual)Interventional2015-09-30Completed
A Dose-Response Efficacy and Safety Study of Arbaclofen Placarbil (XP19986) as Adjunctive Therapy in Subjects With Gastroesophageal Reflux Disease (GERD) Who Are Incomplete Responders to a Proton Pump Inhibitor (PPI)[NCT00978016]Phase 2460 participants (Actual)Interventional2009-09-30Completed
A Multi-Center, Randomized, Double-Blind, Placebo-Controlled, Two Period Crossover, Single Dose-Finding Study to Assess the Efficacy and Safety of Controlled Release XP19986 in Patients With Gastroesophageal Reflux Disease[NCT00838396]Phase 258 participants (Actual)Interventional2005-10-31Completed
Multiple-Dose Efficacy and Safety Study of XP19986 in Subjects With Spasticity Due to Spinal Cord Injury[NCT00557973]Phase 237 participants (Actual)Interventional2007-12-31Completed
A Phase 1 Bioavailability Study of Arbaclofen Placarbil Modified Release Formulations in Healthy Volunteers[NCT03058237]Phase 140 participants (Actual)Interventional2017-01-24Completed
A Multi-Center Randomized, Parallel-Group, Double-Blind, Placebo-Controlled, Study of XP19986 in Subjects With Symptomatic Gastroesophageal Reflux Disease (GERD)[NCT00557401]Phase 2156 participants (Actual)Interventional2007-11-30Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]