Delving into the Latest Updates on Laropiprant/Nicotinic Acid with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Cordaptive, ER niacin/laropiprant, ERN/LRPT

+ [13]

Target

HCAR3 x NIACR1 x PGD2 receptor

Action

agonists, antagonists

Mechanism

HCAR3 agonists(HM74 nicotinic acid GPCR agonists), NIACR1 agonists(Hydroxycarboxylic acid receptor 2 agonists), PGD2 receptor antagonists(Prostaglandin D2 receptor antagonists)

Therapeutic Areas

Endocrinology and Metabolic DiseaseNervous System DiseasesCardiovascular Diseases+ [2]

Active Indication-

Inactive Indication

Angina PectorisAtherosclerosisCardiovascular Diseases+ [14]

Originator Organization

Merck Sharp & Dohme Corp.

Active Organization-

Inactive Organization

Merck Sharp & Dohme Corp.Merck Sharp & Dohme (Ireland) Ltd.Merck Sharp & Dohme SA

+ [4]

License Organization-

Drug Highest PhaseWithdrawn

First Approval Date

European Union (03 Jul 2008),

DyslipidemiasPrimary hypercholesterolemia

Regulation-

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Structure/Sequence

Molecular FormulaC21H19ClFNO4S

InChIKeyNXFFJDQHYLNEJK-CYBMUJFWSA-N

CAS Registry571170-77-9

View All Structures (2)

The aim this study is to investigate the effects of time-restricted eating (TRE) on body composition, muscle function and markers of metabolic health of adults over 60 years old. This study will compare different variations of TRE - with and without an additional protein.
This study involves attending two study days at the University of Surrey for baseline and end-of-intervention measurement of body composition using a gold-standard dual energy x-ray absorptiometry (DEXA) scan; muscle function using hand grip strength and 30-second sit-to-stand tests; weight. A blood sample will be taken at each study visit to measure markers of lipid and glucose control, and insulin sensitivity.
Participants will be randomly allocated to one of four study groups:
* control group: maintain habitual dietary patterns
* TRE group: fast for 16 hours overnight, eat between 12-8pm
* TRE + Protein (AM): fast for 16 hours overnight, eat between 12-8pm; take a 30g plant-based protein supplement in the morning
* TRE + Protein (PM): fast for 16 hours overnight, eat between 12-8pm; take a 30g plant-based protein supplement in the afternoon Participants will be asked to follow the intervention according to their allocated group for 8 weeks.

Start Date01 Dec 2025

Sponsor / Collaborator

University of Surrey

NCT01683656

/ TerminatedPhase 4IIT

ER Niacin/Laropiprant Impact on Cardiovascular Markers and Atheroprogression in HIV-infected Individuals on cART

HIV-infected patients are at increased risk for cardiovascular disease. Large investigations support an inverse correlation between HDL-C levels and coronary heart disease. Therefore a treatment lowering HDL-C such as niacin could reduce the risk of atheroprogression not only through its benefit in terms of lipid profile, but also by reducing atherosclerotic inflammation.
The study aims at showing that a therapy targeting HDL-C increase in HIV-infected patients on suppressive cART has the potential for reducing subclinical atherosclerotic inflammation associated with HIV itself in HIV-individuals on cART.
NILACH is a randomised, multicenter, double blind, placebo controlled, 48 weeks trial to test the effect of the newly marketed niacin/laropiprant on carotid intima-media thickness (IMT) in 90 subjects.
* Regimen 1: ER niacin/laropiprant 1g/20 mg for the first 4 weeks and 2g/40mg from week 5 to the end of the study (the titration aims to reduce adverse reactions)
* Regimen 2: ER niacin/laropiprant placebo p.m.
The primary end point is the change in mean common carotid intima-media thickness from baseline and 48 weeks, compared between the niacin/laropiprant group and the placebo group.
The proposed in vivo experiments should provide insights on the potential benefits of niacin treatment of cardiovascular disease in HIV patients. In addition, we will be able to further clarify the role of systemic inflammatory mediators in the development of early atherosclerosis of HIV-infected patients on antiretroviral therapy. Detection and treatment of non-infectious co-morbidities such as cardiovascular diseases have become essential for HIV-infected individuals exposed to lifelong antiretroviral therapy and go beyond mere management of opportunistic infections or virologic suppression.

Start Date01 Aug 2012

Sponsor / Collaborator

Les Hôpitaux Universitaires de Genève

[+3]

NCT01583647

/ TerminatedPhase 1

A Single Dose Study to Evaluate the Safety, Tolerability and Pharmacokinetics of ER Niacin/Laropiprant in Adolescents With Heterozygous Familial Hypercholesterolemia

The purpose of this study is to determine the pharmacokinetics of laropiprant following administration of a single dose of 1 (Panel A) and 2 (Panel B) combination tablets of MK-0524A in adolescents with heterozygous familial hypercholesterolemia.

Start Date01 Jun 2012

Sponsor / Collaborator

Merck Sharp & Dohme Corp.

100 Clinical Results associated with Laropiprant/Nicotinic Acid

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100 Translational Medicine associated with Laropiprant/Nicotinic Acid

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100 Patents (Medical) associated with Laropiprant/Nicotinic Acid

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363

Literatures (Medical) associated with Laropiprant/Nicotinic Acid

01 Mar 2026·ENVIRONMENTAL POLLUTION

Chlorpyrifos-induced autism and depression-like behaviors are ameliorated by trehalose: Integrating network pharmacology and toxicology analyses and animal experiments

Article

Author: Tao, Junyan ; Tu, Ying ; Song, Shushu ; Zhou, Jiaojiao ; Wei, Qinghao ; Chen, Yun ; Zhou, Shun ; Zhou, Hao ; You, Mingdan

The risk of autism spectrum disorder (ASD) is elevated by exposure to the organophosphate pesticide chlorpyrifos (CPF) during pregnancy and lactation. As a neurodevelopmental disorder, ASD often co-occurs with depression, exacerbating the social isolation experienced by affected individuals. Trehalose (Tre), a naturally occurring non-reducing sugar, has neuroprotective properties. Nevertheless, the mechanisms by which it exerts protective effects against CPF-induced ASD and depression-like behaviors remain unclear. The objective of study was to investigate the mechanisms underlying Tre combating CPF-induced ASD and depression through network pharmacology and toxicology analyses. In animal studies, Tre was administered to offspring mice exposed to CPF during pregnancy and lactation. Behavioral assessments revealed that Tre alleviated CPF-induced repetitive and stereotypic behaviors, social deficits, and depression-like behaviors in offspring mice. Findings from network pharmacology and toxicology analyses and animal experiments supported the notion that mammalian target of rapamycin-related autophagy and TLR4-related necroptosis signaling may contribute to the protective effects of Tre against CPF-induced hippocampal damage. This research offers valuable information regarding the potential protective effects of Tre against neurodevelopmental disorders linked to environmental chemicals.

01 Feb 2026·NUTRITION METABOLISM AND CARDIOVASCULAR DISEASES

The effect of intermittent fasting on sleep in adults with overweight or obesity: a network meta-analysis of randomized controlled trials

Article

Author: Song, Guang ; Zhang, Huishu ; Zhou, Ke

AIMS:

Overweight and obesity have become significant public health concerns. Three types of intermittent fasting (IF)-alternate-day fasting (ADF), time-restricted eating (TRE), and the 5:2 diet-have shown potential for weight loss. However, the effects of IF on sleep remain unclear.

DATA SYNTHESIS:

Multiple databases were searched in January 2025. Randomized controlled trials (RCTs) in adults with overweight and obese that compared the effects of IF, continuous energy restriction (CER), and usual diet (UD) on sleep-related outcomes were eligible. The primary outcome was the global Pittsburgh Sleep Quality Index (PSQI) and secondary outcomes included PSQI components, the Epworth sleepiness scale, and other subjective and objective sleep parameters. A Bayesian network meta-analysis was performed. Sixteen trials were included. There were no significant differences in PSQI components among ADF, CER, TRE, the 5:2 diet, and the UD. ADF had a higher sleep latency score than CER and the UD (MD = 1.04, 95 % CI: 0.15-1.93; MD = 1.39, 95 % CI: 0.37-2.60, respectively). TRE had a longer time in bed than UD (MD = 26.04, 95 % CI: 3.36-48.73), and a longer sleep onset latency than CER (MD = 9.54, 95 % CI: 3.43-15.68). No differences were found for most other sleep parameters.

CONCLUSIONS:

ADF and TRE were shown to have slight effects on some sleep parameters. However, due to limitations, such as small sample sizes and varying protocols of the included studies, the results should be interpreted cautiously. Well-designed and comprehensive studies are warranted.

01 Feb 2026·JOURNAL OF ORAL REHABILITATION

Effects of Tongue Resistance and Strengthening Exercises on Tongue Strength and Oropharyngeal Swallowing in Frail Older Adults With Mild Cognitive Impairment: A Double‐Blind Randomised Controlled Trial

Article

Author: Sung, Chien‐Mei ; Kao, Shu‐Hua ; Chou, Kuei‐Ru ; Chen, Ruey ; Pien, Li‐Chung ; Chu, Hsin ; Chiang, Kai‐Jo ; Banda, Kondwani Joseph ; Chang, Li‐Fang

ABSTRACT:

Background:

Reduced tongue function in older adults leads to inefficient bolus transit. Tongue resistance exercises (TRE) involve isometric or isotonic tongue movements performed against an external load to improve tongue strength. Whereas, tongue strengthening exercises (TSE) involve repetitive, high‐intensity tongue movements enhancing tongue pressure and swallowing coordination, contributing to safer and more efficient swallowing. However, evidence on the effectiveness of combined TRE and TSE in frail older adults with mild cognitive impairment (MCI) remains unknown.

Objective:

Explore effects of combined TRE and TSE on tongue function, swallowing pressure, clinical swallowing function, and quality of life in frail older adults with MCI.

Methods:

A prospective, double‐blind, three‐arm randomised controlled trial registered with ClinicalTrials.gov : NCT06490705. Participants were randomly assigned to (i) TRE + TSE ( n = 29), (ii) TRE alone ( n = 30), and (iii) cheek‐bulging exercises (control group, n = 30) for 12 weeks with a follow‐up 12‐week booster program. The primary outcome was tongue function (IOPI), including anterior (ATS) and posterior (PTS) tongue strength, and anterior (ATE) and posterior (PTE) tongue endurance. The secondary outcomes were swallowing pressure (IOPI), including saliva (SSP) and effortful (ESP) swallowing pressure, clinical swallowing function including difficulty of oral phase (DOP) and number of saliva swallows ‐ NRSS (repetitive saliva swallowing test, RSST), and swallowing quality of life (SWAL‐QOL). Generalised estimating equation model was used for data analysis.

Results:

Frail older adults with MCI ( n = 89, mean age: 75.3 ± 6.9 years; 82% women) were recruited. Combined TRE + TSE significantly improved ATS [β = 9.5, 95% CI = 3.8–15.1], PTE [β = 9.7, 95% CI = 2.8–16.6], SSP [β = 8.9, 95% CI = 5.0–12.9], effortful swallow pressure (ESP) [β = 12.1, 95% CI = 6.8–17.4], NRSS [β = 4.0, 95% CI = 2.7–5.3] and SWAL‐QOL [β = 29.3, 95% CI = 22.4–36.2] with sustained effects on NRSS and SWAL‐QOL at 12‐week follow‐up compared to cheek‐bulging exercises. TRE alone improved ATS, SSP, ESP, NRSS, and SWAL‐QOL immediate post‐test, with sustained effects on SSP, ESP, and SWAL‐QOL at follow‐up compared to cheek‐bulging exercises. Booster training maintained these improvements over time.

Conclusion:

A combined tongue training offers more comprehensive benefits than TRE alone, with booster training maintaining short‐term effects.

1

News (Medical) associated with Laropiprant/Nicotinic Acid

01 May 2008

·www.pharmatimes.com

FDA sends warning letter to Merck & Co over vaccines plant

Merck & Co’s week of woe has continued with the news that US regulators have told the firm to correct what are described as “numerous manufacturing deficiencies” at its main vaccines plant. The US Food and Drug Administration has issued a warning letter to Merck having conducted an inspection of the firm’s West Point, Pennsylvania facility between November 26, 2007 and January 17 this year. The agency’s investigators say they documented “significant deviations from current good manufacturing practice” at the plant in the manufacture of vaccine products, bulk drug substances and drug components. The products manufactured at the West Point site include Merck & Co’s cervical cancer vaccine Gardasil and ProQuad, its combination jab against measles, mumps, rubella and chicken pox. Also produced at the facility are the Haemophilus influenzae type B vaccine PedvaxHIB and ComVax for haemophilius b and hepatitis B and 1.2 million doses of these two jabs were voluntarily recalled in December because Merck said it could not assure sterility of those specific vaccine lots. The warning letter, which is posted on the FDA’s website in a heavily edited form, has been issued because Merck's response to the FDA’s initial inspection report was "inadequate to address the serious deviations noted”. Most of the myriad complaints appear to deal with procedural errors but the agency stresses it "does not believe that the issues identified will affect the safety of the vaccines" made at the facility. Merck says that it is committed to working with the FDA to address these issues, adding that it does not distribute contaminated products and is confident in their “quality, effectiveness and safety”. The letter comes in a week when Merck’s stock has taken a bashing after the FDA rejected applications firstly for a proposed fixed combination of Singulair (montelukast) and S-P’s Claritin (loratadine) as a treatment for allergic rhinitis and secondly for its new cholesterol compound MK-0524A (extended-release niacin/laropiprant).

Vaccine

100 Deals associated with Laropiprant/Nicotinic Acid

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External Link

KEGG	Wiki	ATC	Drug Bank
-	Laropiprant/Nicotinic Acid	C10AD52	DB11629

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Dyslipidemias	European Union	Merck Sharp & Dohme (Ireland) Ltd.	03 Jul 2008
Dyslipidemias	Iceland	Merck Sharp & Dohme (Ireland) Ltd.	03 Jul 2008
Dyslipidemias	Liechtenstein	Merck Sharp & Dohme (Ireland) Ltd.	03 Jul 2008
Dyslipidemias	Norway	Merck Sharp & Dohme (Ireland) Ltd.	03 Jul 2008
Primary hypercholesterolemia	European Union	Merck Sharp & Dohme (Ireland) Ltd.	03 Jul 2008
Primary hypercholesterolemia	Iceland	Merck Sharp & Dohme (Ireland) Ltd.	03 Jul 2008
Primary hypercholesterolemia	Liechtenstein	Merck Sharp & Dohme (Ireland) Ltd.	03 Jul 2008
Primary hypercholesterolemia	Norway	Merck Sharp & Dohme (Ireland) Ltd.	03 Jul 2008

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Cardiovascular Diseases	Phase 3	-	Merck Sharp & Dohme Corp.	01 Sep 2011
Flushing	Phase 3	-	Merck Sharp & Dohme Corp.	01 Apr 2007
Angina Pectoris	Phase 3	United Kingdom	Merck Sharp & Dohme Corp.	01 Jan 2007
Coronary Disease	Phase 3	United Kingdom	Merck Sharp & Dohme Corp.	01 Jan 2007
Coronary Restenosis	Phase 3	United Kingdom	Merck Sharp & Dohme Corp.	01 Jan 2007
Diabetes Mellitus	Phase 3	United Kingdom	Merck Sharp & Dohme Corp.	01 Jan 2007
Peripheral Arterial Disease	Phase 3	United Kingdom	Merck Sharp & Dohme Corp.	01 Jan 2007
Heterozygous familial hypercholesterolemia	Phase 3	-	Merck Sharp & Dohme Corp.	01 Sep 2006
Hypercholesterolemia, Familial	Phase 3	-	Merck Sharp & Dohme Corp.	01 Sep 2006
Hypercholesterolemia	Phase 3	-	Merck Sharp & Dohme Corp.	01 Jul 2006

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT00461630 (HPS2-THRIVE, Pubmed \| Clin Ther)	Phase 3	-	25,673	Niacin-laropiprant	ldgduspfoi(cdigovdbcv): HR = 1.38 (95% CI, 1.17 - 1.63) View more	-	01 Sep 2019
				Placebo
NCT00796887 (ISC2018)	Phase 2	Stroke	27	Extended-release niacin 500 mg	ixexbnlfrm(kyxaxblenx) = csuibaxdor pkokvhiruo (cukdpljrop )	Negative	22 Jan 2018
				Placebo	ixexbnlfrm(kyxaxblenx) = lxvmiopquq pkokvhiruo (cukdpljrop )
NCT01294683 (0524B-118, CTgov)	Phase 3	Primary hypercholesterolemia	977	MK-0524B (Sequence 1: MK-0524B 2g/40g)	efhjuvguxl = nzbywhdslo megbdahpfk (hvozvxhvdv, pbnwfgoaka - zrmodptcpa) View more	-	13 Dec 2016
				Simvastatin+MK-0524A (Sequence 2: MK-0524A 2g + Simvastatin 40 mg)	efhjuvguxl = hzfokvalgq megbdahpfk (hvozvxhvdv, tbzlzofhgr - xfdwpdrtsq) View more
NCT00461630 (HPS2-THRIVE, Pubmed \| Circ Cardiovasc Qual Outcomes)	Phase 3	Diabetes Mellitus \| Coronary Disease \| Peripheral Arterial Disease	25,673	Extended-release niacin with laropiprant	uvhqfgoxxx(ejoiujsbqs) = UK £101 [SE £37]; US $145 [SE $53] uialpubowh (hnmkpjaklv ) View more	-	01 Jul 2016
NCT00461630 (HPS2-THRIVE, Pubmed \| N Engl J Med)	Phase 3	-	25,673	Extended-release niacin-laropiprant	oyhomhnqjq(vuhlffcxyr) = pacnnrmmvy vutnryevmj (xzntaqzulc ) View more	Negative	17 Jul 2014
				Placebo	dilpbdnmlr(lnnrjrgyyo) = oeswrritlz lpfiodxmja (itchihuqok )
NCT01118598 (Pubmed \| Diabetes Obes Metab)	Phase 4	Polycystic Ovary Syndrome	25	Niacin/laropiprant	ntubswehvb(zclwpalddb) = liuirsbjrr kaybxqcqni (iobqydsopz ) View more	-	01 Jun 2014
				Placebo	ntubswehvb(zclwpalddb) = ortjcfdswu kaybxqcqni (iobqydsopz ) View more
NCT01239992 (CTgov)	Phase 4	Hyperlipoproteinemias \| Metabolic Syndrome	12	Niacin/ Laropiprant	epkwxrtaod(ffgczpdexh) = itfdswrlrp rpvpezmldq (pwsxjqkquk, 5) View more	-	10 Apr 2014
NCT01414166 (0524A-108, CTgov)	Phase 3	Cardiovascular Diseases \| Dyslipidemias \| Coronary Disease	244	Extended-release niacin+laropiprant (ERN/LPRT)	htmzqppukx(eqfigkcont) = kpvnptlcqt wayxucltzt (wzeuscdyak, yllcutddct - kdtsqxubnh) View more	-	14 Mar 2014
				placebo (Placebo)	htmzqppukx(eqfigkcont) = mxieuqlrcd wayxucltzt (wzeuscdyak, tbaowszfio - yslogxnose) View more
NCT01274559 (0524A-133, CTgov)	Phase 3	Primary hypercholesterolemia	1,173	Extended-release niacin/laropiprant (ERN/LRPT) (Extended-release Niacin/Laropiprant)	cmzqvnyonm(dnryozfacw) = zvzuvdmlyo skkpunapln (rusyckpdpp, gpkumwlfor - ekjmbnestr) View more	-	14 Mar 2014
				Placebo (Placebo)	cmzqvnyonm(dnryozfacw) = svgdaphjin skkpunapln (rusyckpdpp, xedwieskcd - arwfbwbccp) View more
NCT00461630 (HPS2-THRIVE, CTgov)	Phase 3	Angina Pectoris \| Diabetes Mellitus \| Coronary Restenosis ... View more	25,673	simvastatin+ezetimibe/simvastatin+ER niacin/laropiprant (ER Niacin/Laropiprant)	nhavguaglg = jtqohuwfyi iejjrmdhfv (dxxhzjmfbf, ggyyrpmlhw - oceoenbddh) View more	-	28 Jan 2014
				simvastatin+ezetimibe/simvastatin (Placebo)	nhavguaglg = kdnchapjpp iejjrmdhfv (dxxhzjmfbf, ibulxnswsi - hcpihwmssa) View more