Delving into the Latest Updates on Gabapentin Enacarbil with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Gabapentin enacarbil (JAN/USAN/INN), Gabapentin-XP

+ [8]

Target

CACNA2D1 x CACNA2D2

Mechanism

CACNA2D1 blockers(Voltage-gated calcium channel alpha2/delta subunit 1 blockers), CACNA2D2 blockers(Voltage-gated calcium channel alpha2/delta subunit 2 blockers)

Therapeutic Areas

Nervous System Diseases

Active Indication

Neuralgia, PostherpeticRestless Legs Syndrome

Inactive Indication

Alcohol Use DisorderDiabetic NeuropathiesDiabetic peripheral neuropathy

Originator Organization

XenoPort, Inc.

Active Organization

Azurity Pharmaceuticals, Inc.

Astellas Pharma, Inc.

Inactive Organization

XenoPort, Inc.Arbor Pharmaceuticals, Inc.

Drug Highest PhaseApproved

First Approval Date

US (06 Apr 2011),

Restless Legs Syndrome

RegulationOrphan Drug (US)

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Structure

Molecular FormulaC16H27NO6

InChIKeyTZDUHAJSIBHXDL-UHFFFAOYSA-N

CAS Registry478296-72-9

Nighttime agitation in persons with Alzheimer's disease causes patient suffering, distresses caregivers, and often results in prescriptions for harmful antipsychotics. Effective treatments are lacking because of limited knowledge of the etiology of nighttime agitation. The investigators propose a clinical trial to better elucidate whether a sleep disorder, restless legs syndrome, may be a mechanism for nighttime agitation, and if treatment with gabapentin enacarbil (Horizant®) reduces nighttime agitation, improves sleep, reduces restless legs syndrome behaviors, and reduces antipsychotic medications.

Start Date01 Jul 2017

Sponsor / Collaborator

The University of Texas at Austin

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100 Clinical Results associated with Gabapentin Enacarbil

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100 Translational Medicine associated with Gabapentin Enacarbil

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100 Patents (Medical) associated with Gabapentin Enacarbil

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118

Literatures (Medical) associated with Gabapentin Enacarbil

01 Jul 2024·Journal of Addiction Medicine

Reductions in World Health Organization Risk Drinking Level Are Associated With Reductions in Alcohol Use Disorder Diagnosis and Criteria: Evidence From an Alcohol Pharmacotherapy Trial

Article

Author: Richards, Dylan K ; Aldridge, Arnie ; Kranzler, Henry R ; Witkiewitz, Katie ; Tuchman, Felicia R ; Aubin, Henri-Jean ; Mann, Karl ; Hallgren, Kevin A ; O'Malley, Stephanie S ; Anton, Raymond F

ObjectivesThis study aimed to evaluate the validity of World Health Organization (WHO) risk drinking level reductions as meaningful endpoints for clinical practice and research. This study examined whether such reductions were associated with a lower likelihood of a current alcohol use disorder (AUD) diagnosis and fewer AUD criteria.MethodsWe conducted a secondary data analysis to address these objectives using data from a multisite randomized controlled trial of gabapentin enacarbil extended release in treating moderate to severe AUD among adults (N = 346). Participants received gabapentin enacarbil extended release or placebo for 6 months. The timeline follow-back was used to assess WHO risk drinking level reductions, and the Mini-International Neuropsychiatric Interview was used to assess Diagnostic and Statistical Manual of Mental Disorders (Fifth Edition) AUD diagnosis and criteria at baseline (past year) and end of treatment (past month).ResultsMost participants (80.1%) achieved at least a 1-level reduction in the WHO risk drinking levels from baseline to end of treatment, and nearly half of participants (49.8%) achieved at least a 2-level reduction. At least a 1-level reduction or at least a 2-level reduction in WHO risk drinking level predicted lower odds of an active AUD diagnosis (1-level: odds ratio, 0.74 [95% confidence interval (CI), 0.66–0.84]; 2-level: odds ratio, 0.71 [95% CI, 0.64–0.79]) and fewer AUD criteria (1-level: B, −1.66 [95% CI, −2.35 to −0.98]; 2-level: B, −1.76 [95% CI, −2.31 to −1.21]) at end of treatment.ConclusionsWorld Health Organization risk drinking level reductions correlate with Diagnostic and Statistical Manual of Mental Disorders (Fifth Edition) AUD diagnosis and criteria, providing further evidence for their use as endpoints in alcohol intervention trials, which has potential implications for broadening the base of AUD treatment.

16 Mar 2024·Alcohol and Alcoholism

Reductions in World Health Organization risk drinking level are associated with improvements in sleep problems among individuals with alcohol use disorder

Article

Author: Hoffman, Michaela ; Hallgren, Kevin A ; Tuchman, Felicia R ; Anton, Raymond F ; Aldridge, Arnie ; Garcia, Christian C ; Aubin, Henri-Jean ; Kranzler, Henry R ; Richards, Dylan K ; Mann, Karl ; O’Malley, Stephanie S ; Witkiewitz, Katie

AbstractAimsAmong individuals with alcohol use disorder (AUD), sleep disturbances are pervasive and contribute to the etiology and maintenance of AUD. However, despite increased attention toward the relationship between alcohol use and sleep, limited empirical research has systematically examined whether reductions in drinking during treatment for AUD are associated with improvements in sleep problems.MethodsWe used data from a multisite, randomized, controlled trial that compared 6 months of treatment with gabapentin enacarbil extended-release with placebo for adults with moderate-to-severe AUD (N = 346). The Timeline Follow-back was used to assess WHO risk drinking level reductions and the Pittsburgh Sleep Quality Index was used to assess sleep quality over the prior month at baseline and the end of treatment.ResultsSleep problem scores in the active medication and placebo groups improved equally. Fewer sleep problems were noted among individuals who achieved at least a 1-level reduction (B = −0.99, 95% confidence interval (CI) [−1.77, −0.20], P = .014) or at least a 2-level reduction (B = −0.80, 95% CI [−1.47, −0.14], P = .018) in WHO risk drinking levels at the end of treatment. Reductions in drinking, with abstainers excluded from the analysis, also predicted fewer sleep problems at the end of treatment (1-level: B = −1.01, 95% CI [−1.83, −0.20], P = .015; 2-level: B = −0.90, 95% CI [−1.59, −0.22], P = .010).ConclusionsDrinking reductions, including those short of abstinence, are associated with improvements in sleep problems during treatment for AUD. Additional assessment of the causal relationships between harm-reduction approaches to AUD and improvements in sleep is warranted.

03 Mar 2024·Expert Opinion on Drug Metabolism & Toxicology

A comprehensive update on the ADMET considerations for α2δ calcium channel ligand medications for treating restless legs syndrome

Review

Author: Versace, Salvatore ; Nilo, Annacarmen ; Pellitteri, Gaia ; Valente, Mariarosaria ; Merlino, Giovanni ; Gigli, Gian Luigi

INTRODUCTIONRestless legs syndrome/Willis-Ekbom disease (RLS/WED) is a sleep-related sensory-motor disorder associated with poor sleep quality and impaired daily functioning. In patients affected by chronic RLS/WED, a pharmacological therapy is recommended. International guidelines suggest to start the treatment with a α2δ calcium channel ligand in most cases, unless contraindicated.AREAS COVEREDThe present review is based on an extensive Internet and PubMed search from 1986 to 2024. Our purpose is to describe the absorption, distribution, metabolism, and toxicology (ADMET) of the α2δ ligands, with common consideration for the therapeutic class, specificities of different compounds, efficacy, and safety in relation to other treatment options.EXPERT OPINIONα2δ ligands are quite similar in their ADMET profiles, sharing most of the pharmacokinetics and potential adverse effects. However, we highlight the linear kinetic of gabapentin enacarbil and pregabalin, differently from gabapentin. α2δ ligands are safe and effective for the treatment of RLS/WED. Additional benefits can be obtained in comorbid insomnia, chronic pain syndromes, history of impulse control disorder, and comorbid anxiety. The use of α2δ ligands is associated with poor risk of augmentation. We still need new long-term safe and effective treatments, which could be developed along with our knowledge of RLS/WED pathophysiology.

100 Deals associated with Gabapentin Enacarbil

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External Link

KEGG	Wiki	ATC	Drug Bank
D09539	Gabapentin Enacarbil	N03AX12	DB08872

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Neuralgia, Postherpetic	US	Azurity Pharmaceuticals, Inc.	06 Jun 2012
Restless Legs Syndrome	US	Azurity Pharmaceuticals, Inc.	06 Apr 2011

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Diabetic Neuropathies	Preclinical	JP	Astellas Pharma, Inc.	01 Jul 2007
Alcohol Use Disorder	Discovery	US	Arbor Pharmaceuticals, Inc.	01 Jun 2015
Diabetic peripheral neuropathy	Discovery	US	XenoPort, Inc.	01 Mar 2008
Neuralgia	Discovery	US	XenoPort, Inc.	01 Mar 2008
Neuralgia, Postherpetic	Discovery	CA	XenoPort, Inc.	01 Feb 2008
Restless Legs Syndrome	Discovery	-	XenoPort, Inc.	01 Mar 2006

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02840240 (CTgov)	Not Applicable	Pain \| Anesthesia	107	Gabapentin enacarbil (Gabapentin Enacarbil)	ehukhktynq(xttsbcvrmm) = hjotacmfsl ppnmngtiwb (aygcoimqsa, kfqpkrehzz - nyraohasos) View more	-	09 Jan 2024
				Placebo (Placebo)	ehukhktynq(xttsbcvrmm) = xvysihqfus ppnmngtiwb (aygcoimqsa, ftxmbabtqs - npejftnoyd) View more
NCT03053427 (CTgov)	Phase 4	Restless Legs Syndrome	375	Placebo (Placebo)	mqshyswvar(bsingkvikf) = xmjlopdexz gvtdjfwdtv (rnqadxouhr, hcxonpffsb - ilkzwhsgjd) View more	-	10 Jul 2019
				Gabapentin enacarbil (Gabapentin Enacarbil)	mqshyswvar(bsingkvikf) = mlfpozyxxi gvtdjfwdtv (rnqadxouhr, pcvzfdnqxv - fourdxkrwu) View more
NCT02252536 (Pubmed) Manual	Phase 2	Alcohol Use Disorder	346	gabapentin enacarbil	feuieyljam(ooafedkjyh) = soljseigem dvymxwubbj (uvzgtpkbrp )	Negative	01 Jan 2019
				Placebo	feuieyljam(ooafedkjyh) = wsgztkwqyx dvymxwubbj (uvzgtpkbrp )
NCT02252536 (CTgov)	Phase 2	Alcohol Use Disorder	346	Placebo (Sugar Pill)	zyhpjfhwfw(engvahfwwc) = rpsfvspozs fprohismsq (xzcgdnakuj, tmtzvrtrut - yrzgnqubzd) View more	-	21 Sep 2018
				gabapentin enacarbil (Gabapentin Enacarbil)	zyhpjfhwfw(engvahfwwc) = haafvzxxko fprohismsq (xzcgdnakuj, emgqkbvtuh - iamjkmhhcx) View more
NCT01668667 (CONCORD, CTgov)	Phase 4	Restless Legs Syndrome	501	GSK1838262 600 mg (GSK1838262 600 mg)	dkbaaoeasv(oklyxaerql) = vojqtfiesl uidapryuez (uleggygfqd, drweixsskn - qndromrmbe) View more	-	17 Nov 2014
				GSK1838262 450 mg (GSK1838262 450 mg)	dkbaaoeasv(oklyxaerql) = oqmlwoczel uidapryuez (uleggygfqd, hoxktsuxqw - gbperzpmhg) View more
NCT01332305 (Pubmed \| Clin Neuropharmacol) Manual	Phase 2	Restless Legs Syndrome	217	gabapentin enacarbil	pygmgchotg(kedbfhpcjw) = mfoulmrvwj eqwqbvumcw (bydbwbktde )	Positive	01 Jul 2012
				Placebo	pygmgchotg(kedbfhpcjw) = lesadhefko eqwqbvumcw (bydbwbktde )
NCT00742209 (111381, CTgov)	Phase 2	Migraine Disorders	526	Placebo	zsprfshuqo(fjrqdmotii) = scaegsgehn lyleaqrncu (sgukzvjubu, muihrqqile - rhcbpywxfl) View more	-	05 Dec 2011
NCT00365352 (Pubmed \| J Clin Sleep Med)	Phase 3	Restless Legs Syndrome	325	Gabapentin enacarbil 1200 mg	qoelbxaqqs(piwhxwmmim) = jzinxpaxpa hwtkidjwea (ddbsqrzyoz )	-	15 Jun 2011
				Gabapentin enacarbil 600 mg	qoelbxaqqs(piwhxwmmim) = prgpptyhxd hwtkidjwea (ddbsqrzyoz )
NCT00365352 (CTgov)	Phase 3	Restless Legs Syndrome	325	PLACEBO	jaimvureav(zmghiqunex) = jqislanoli lvdorxioru (rywuasedpj, qqmblehnno - jqcemfuhly) View more	-	11 May 2011