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+ [13]

Originator Organization

Merck Sharp & Dohme Corp.

Active Organization-

Inactive Organization

Merck Sharp & Dohme Corp.Merck Sharp & Dohme Ireland Ltd.Merck GmbH

+ [1]

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)

A randomized, multicenter, open-label, two-arm, parallel, phase III study to evaluate the efficacy and safety of nicotinic acid administered in combination with simvastatin for 6 months in comparison to simvastatin therapy alone in inhibiting the progression of atherosclerosis in patients with carotid arteries stenosis and dyslipidemia.

Start Date02 Mar 2015

Sponsor / Collaborator-

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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386

Literatures (Medical) associated with Laropiprant/Nicotinic Acid

31 Dec 2025·Journal of the International Society of Sports Nutrition

Efficacy of time restricted eating and resistance training on body composition and mood profiles among young adults with overweight/obesity: a randomized controlled trial

Article

Author: Ye, Weibing ; Cui, Tingting ; Liu, Yubo ; Sun, Yichao ; Korivi, Mallikarjuna

BACKGROUND/OBJECTIVE:

Dietary restriction or exercise regimens can promote weight loss or physical fitness among patients with obesity. However, intervention-associated adverse effects may impede patients' motivation to participate in dietary/exercise interventions. We examined the effects of time restricted eating (TRE) with or without resistance training (RT) on body composition, mood profile, and sleep quality in young college adults with overweight or obesity.

METHODS:

Fifty-four young college students with overweight/obesity were randomized into control (CON), TRE, RT, and TRE plus RT (TRE+RT) trials. The TRE trials restricted to an eating window of 10-hour/day for 8-week. The RT trials performed supervised resistance exercise, while the control trial maintained a regular lifestyle. Changes in body composition variables, blood pressure, mood status, and sleep quality were measured before and after the intervention.

RESULTS:

TRE intervention alone or in combination with RT significantly (p < 0.01) decreased body weight (>2 kg) and BMI (~1 kg/m²) in adults with overweight/obesity. Both RT alone and combined with TRE substantially decreased fat mass by 1.1 ± 0.5 and 3.2 ± 0.4 kg, respectively. The decreased fat mass was greater in the combination trial than in the RT trial, whereas TRE alone had no effect. In contrast, fat-free mass was significantly (p < 0.01) decreased with TRE (-2.3 ± 06 kg), increased with RT (1.6 ± 0.3 kg), and was stably maintained with combination interventions. The reduced waist and hip circumferences in the TRE (p < 0.01) were similar to those in the TRE+RT trials, however, RT alone had no effect. Time and group interaction showed a large effect size (partial eta squared) for all body composition variables. In addition, RT with or without TRE notably decreased diastolic blood pressure (RT: -5.5 ± 1.9 mmHg, TRE+RT: -4.1 ± 1.5 mmHg, p < 0.05). Mild anxiety levels at baseline in RT (4.8 ± 2.6) and TRE+RT (4.1 ± 3) trials were found to be normal at postintervention in TRE+RT (3.6 ± 1.7) but not in RT (5.6 ± 3.5). No depression or stress was recorded among the participants during the intervention. The reported poor sleep quality among participants at baseline was significantly improved with RT (4.8 ± 2.9; p < 0.05), and tended to improve with TRE+RT interventions (4.5 ± 1.9).

CONCLUSIONS:

10-hour TRE is beneficial for weight/fat loss without affecting mood status. However, TRE combined with RT might be more effective for weight/fat loss, maintaining muscle mass, and good quality of sleep among young adults with overweight or obesity.

31 Dec 2025·Journal of the International Society of Sports Nutrition

Hypercaloric 16:8 time-restricted eating during 8 weeks of resistance exercise in well-trained men and women

Article

Author: Campidell, Thomas ; Galpin, Andrew J. ; Hamane, Cody ; Tinsley, Grant M. ; Pacheco, Chelscie ; Costa, Pablo ; Blake, Daniel T. ; Coburn, Jared W. ; Henselmans, Menno

BACKGROUND:

The effectiveness and practicality of time-restricted eating (TRE) when trying to maximize muscle mass and strength is unclear. Thus, we examined the effects of a hypercaloric 16:8 TRE approach during supervised progressive resistance exercise.

METHODS:

Seventeen healthy and well-trained men (n = 10) and women (n = 7) were randomly assigned to TRE or control (FED). Both groups consumed a 10% hypercaloric high-protein (2.2 g/kg/d) diet and performed supervised resistance exercise 4× per wk for 8 wk. TRE consumed all calories within an 8 h window starting at least 1 h post-exercise, while FED consumed the same number of calories throughout the day.

RESULTS:

Eating windows were significantly different (TRE: 7.9 ± 0.1 h vs. FED: 13.2 ± 0.6 h). Calorie, carbohydrate, fat, and protein intake did not differ statistically between groups. Total exercise volume was significantly lower in TRE than FED (6,960 ± 287 vs. 7,334 ± 289 repetitions), as were subjective daily energy ratings (week 4 = -1.41; p = 0.04, week 8 = -1.04; p = 0.06). Both groups increased maximal upper and lower body strength (1RM) and muscular endurance (ME); however, gains in squat 1RM were 4.0 ± 1.9 kg lower in TRE (p = 0.05). Both groups increased fat-free mass similarly (TRE: 2.67 kg; FED: 1.82 kg, p = 0.04), but FED added 1.4 ± 0.6 kg more fat mass (p = 0.04). Subjective mood and sleep ratings did not change in either group.

CONCLUSIONS:

16:8 TRE is viable during periods of muscle size, strength, and endurance development in well-trained young men and women when engaging in progressive resistance exercise and eating in a caloric surplus with adequate protein. However, the differences in total training volume, squat 1RM, fat mass accumulation, and energy are notable and practically relevant. These findings should be considered within the broader context of an individual's goals, lifestyle, preferences, and exercise demands.

01 Nov 2025·EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES

Synthesis and in vitro evaluation of polyethylene glycol-treprostinil conjugates for sustained local delivery in pulmonary arterial hypertension

Article

Author: Perros, Frédéric ; Vanbever, Rita ; Frédérick, Raphaël ; Ucakar, Bernard ; Leone, Giuditta

Treprostinil (TRE) is a prostacyclin analogue approved for the treatment of pulmonary arterial hypertension (PAH). Despite its effectiveness, TRE has a short half-life, necessitating frequent or continuous administration to maintain therapeutic levels while minimizing adverse effects. To improve pharmacokinetics and pulmonary targeting of TRE, we designed a series of polyethylene glycol (PEG) ester conjugates for inhalation. The increase in molecular size achieved through polymer conjugation prevents the passive diffusion of TRE across the alveolar-capillary barrier, a common drawback of small, lipophilic drugs delivered to the lungs. The ester bond between TRE and PEG enables a gradual release of the active compound within the alveolar space. TRE was chemically modified with seven different alkyne-bearing linkers and subsequently conjugated to PEG-azide 6 kDa via click chemistry. These linkers were strategically designed to modulate the chemical environment around the cleavable ester bond, allowing for the systematic evaluation of the steric and electronic effects on the stability of the PEG-TRE conjugates. Drug release studies in bronchoalveolar lavage from healthy rats demonstrated that sterically hindered and electronically stabilized linkers significantly slowed the release of TRE. Moreover, conjugate stability was dependent on the enzymes availability, with a higher conjugate-enzyme ratio leading to slower release, suggesting enzyme saturation as a potential mechanism for controlled drug release. Overall, these findings demonstrate a tunable strategy for releasing drugs from polymer-drug conjugates in biological media.

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
Hyperlipoproteinemia Type II	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	ngvrstpryx(dhsiugyztx): 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	yjvkfwmuqr(whweyreusu) = qroovzyjcm ctqroirzls (jtwwhokcga )	Negative	22 Jan 2018
				Placebo	yjvkfwmuqr(whweyreusu) = srhmgxihlt ctqroirzls (jtwwhokcga )
NCT00461630 (HPS2-THRIVE, Pubmed \| Circ Cardiovasc Qual Outcomes)	Phase 3	Diabetes Mellitus \| Coronary Disease \| Peripheral Arterial Disease	25,673	Extended-release niacin with laropiprant	qivbegtewp(oivdpzibim) = UK £101 [SE £37]; US $145 [SE $53] ovbxkofwil (bkkvhtlfve ) View more	-	01 Jul 2016
NCT00461630 (HPS2-THRIVE, Pubmed \| N Engl J Med)	Phase 3	-	25,673	Extended-release niacin-laropiprant	gkspofrvhi(ohthfdkjkx) = cqtdoxscpq ewjwlnphci (sxqbkfxrlb ) View more	Negative	17 Jul 2014
				Placebo	jfpmdyanaf(ywgmwziflu) = ozgmlcvcxd cgjlclyutl (qjczdhmznj )
NCT01118598 (Pubmed \| Diabetes Obes Metab)	Phase 4	Polycystic Ovary Syndrome	25	Niacin/laropiprant	vrawqmialx(fzcoraegxw) = juvbwwqbby tauyoqrgvw (pvdvmterzm ) View more	-	01 Jun 2014
				Placebo	vrawqmialx(fzcoraegxw) = swcynwyqto tauyoqrgvw (pvdvmterzm ) View more
NCT01239992 (CTgov)	Phase 4	Hyperlipoproteinemias \| Metabolic Syndrome	12	Niacin/ Laropiprant	npenxhchkv(ogyycttcyn) = ombtjuoajs gqivmsvihh (ycxkmlljfm, 5) View more	-	10 Apr 2014
NCT01414166 (0524A-108, CTgov)	Phase 3	Cardiovascular Diseases \| Dyslipidemias \| Coronary Disease	244	Extended-release niacin+laropiprant (ERN/LPRT)	rfeuxswwey(vstoxedqxv) = zhahsnoxax gioerrsamw (tjxziefcdx, moszvvhmey - nquwzywinl) View more	-	14 Mar 2014
				placebo (Placebo)	rfeuxswwey(vstoxedqxv) = jyufkxkhev gioerrsamw (tjxziefcdx, tfetoyhtfp - enfmjikygv) View more
NCT01274559 (0524A-133, CTgov)	Phase 3	Primary hypercholesterolemia	1,173	Extended-release niacin/laropiprant (ERN/LRPT) (Extended-release Niacin/Laropiprant)	qautksolgt(xwefypxipi) = gbvzgotrnp iymgbvrjhg (whaphxgbys, bhhshccbwe - nenvwodhdv) View more	-	14 Mar 2014
				Placebo (Placebo)	qautksolgt(xwefypxipi) = cpwhyrheyf iymgbvrjhg (whaphxgbys, xvzipytjnx - pwxnpdmwtw) 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)	sxpngbejnj = ziwydyfkgu ratfqvzkgp (phzouyruoc, xhcxuxhkyt - jvhdhvxdbw) View more	-	28 Jan 2014
				simvastatin+ezetimibe/simvastatin (Placebo)	sxpngbejnj = vpptntkppp ratfqvzkgp (phzouyruoc, toyvwyxtci - wahlqqbarp) View more
NCT01012219 (Pubmed \| Platelets)	Phase 1	Dyslipidemias \| Primary hypercholesterolemia \| Hyperlipidemia, Familial Combined	36	Laropiprant	bhcurugalh(qypulmqbdg) = mctefzpqmi hvsafjeffz (qsedgsiydt ) View more	-	01 Jan 2014
				Placebo	bhcurugalh(qypulmqbdg) = jugbgdqejd hvsafjeffz (qsedgsiydt ) View more