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+ [12]

Originator Organization

Merck Sharp & Dohme Corp.

Active Organization-

Inactive Organization

Merck Sharp & Dohme (Ireland) Ltd.

Merck Sharp & Dohme Corp.Merck Sharp & Dohme LLC

+ [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)

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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387

Literatures (Medical) associated with Laropiprant/Nicotinic Acid

01 Apr 2026·Contemporary Clinical Trials

Trial design: Evaluating the safety, feasibility, and acceptability of time-restricted eating in pregnant women with obesity

Article

Author: Fought-Boudaia, Anisa ; Burton, Tristesse ; Tardif, Adrienne ; Patel, Bhumi ; Li, Yanqiao ; DiPiazza, Brittany ; Pezley, Lacey ; Buhimschi, Irina ; Koenig, Mary Dawn ; Steffen, Alana ; Varady, Krista ; Tussing-Humphreys, Lisa

BACKGROUND:

In the United States (U.S.), approximately 15% of women of reproductive age have a body mass index (BMI) of at least 35.0 kg/m², which is associated with increased risks of adverse maternal and fetal health outcomes. However, interventions targeting gestational weight gain have not improved perinatal health outcomes among this population, suggesting the need for innovation. Time-restricted eating (TRE) is an accessible eating pattern in which individuals consume food within a limited time frame each day. We hypothesize that TRE has the potential to optimize gestational weight gain and improve maternal cardiometabolic health and perinatal health outcomes among women with prenatal obesity.

METHODS:

We describe a randomized controlled pilot study of TRE among pregnant women with a pre-pregnancy BMI between 35 and 60 kg/m². The study aims to enroll 60 participants. The study commences at 14 to ≤20 weeks gestational age and continues through labor and delivery. The TRE intervention includes an 8-h eating window (10 a.m. - 6 p.m. or 11 a.m. - 7 p.m.) during the 2nd trimester and a 10-h eating window (9 a.m. - 7 p.m. or 10 a.m. - 8 p.m.) during the 3rd trimester, for each day of the participants' enrollment in the study.

RESULTS:

The study will: 1) examine the safety, feasibility, and acceptability of TRE during pregnancy, 2) explore the impact of TRE on maternal body weight and cardiometabolic markers, and 3) explore the impact of TRE on perinatal health outcomes.

CONCLUSION:

The primary outcomes of this study are focused on examining the safety, feasibility, and acceptability of TRE in pregnant women with class II and III obesity.

01 Apr 2026·INTERNATIONAL JOURNAL OF PHARMACEUTICS

Hydroxypropyl-β-cyclodextrin as a multifunctional excipient for enhancing stability and aerosol performance of spray-dried protein formulations

Article

Author: Bera, Hriday ; Deng, Xiaoxi ; Wei, Liping ; Yang, Mingshi ; Abbasi, Yasir Faraz ; Zhu, Qingyi ; Yang, Yuchen ; Cun, Dongmei

Protein-based drugs are precise therapeutic options for various refractory lung diseases, significantly improving patient prognosis and quality of life. In this study, a comparative spray-drying approach was employed to prepare inhalable dry-powder formulations of bovine serum albumin (BSA), a surface-active model protein, using established pharmaceutical excipients, including 2-hydroxypropyl-β-cyclodextrin (HP-β-CD), trehalose (Tre), leucine (Leu), and a Tre-Leu combination. The relative performance of HP-β-CD was systematically benchmarked against Tre, Leu, and dual-excipient systems under identical formulation and processing conditions, with respect to protein protection and aerodynamic properties. After 3 months of storage under accelerated stability condition (40 ± 2 °C and 20 ± 5% relative humidity), the protein monomer content in the HP-β-CD-based formulations was marginally lower than that observed in the Tre- and dual-excipient-containing dry powders but still demonstrated effective protein protection. Moreover, the aerosol performance of HP-β-CD formulations surpassed that of other excipients, indicating its superior potential for pulmonary delivery of protein molecules. Overall, this comparative study highlights the potential of HP-β-CD as an alternative excipient for protein-based aerosol dry-powder formulations.

01 Apr 2026·Liver International

Lymphocyte–Monocyte Ratio Predicts the Survival in Patients With HCC Treated With Durvalumab Plus Tremelimumab

Article

Author: Ishikawa, Toru ; Hatanaka, Takeshi ; Morishita, Asahiro ; Ueda, Yoshihide ; Nouso, Kazuhiro ; Tada, Fujimasa ; Yata, Yutaka ; Aoki, Tomoko ; Tanaka, Hironori ; Komatsu, Shohei ; Ohama, Hideko ; Nagano, Takuya ; Nishikawa, Hiroki ; Matsui, Kosuke ; Koshiyama, Yuichi ; Nakamura, Shinichiro ; Ochi, Hironori ; Imai, Michitaka ; Naganuma, Atsushi ; Fukumoto, Takumi ; Tajiri, Kazuto ; Hiasa, Yoichi ; Okamura, Jumpei ; Matono, Tomomitsu ; Enomoto, Hirayuki ; Kawata, Kazuhito ; Kuroda, Hidekatsu ; Okubo, Tomomi ; Kaibori, Masaki ; Arai, Taeang ; Hiraoka, Atsushi ; Kim, Soo Ki ; Noritake, Hidenao ; Tani, Joji ; Kakizaki, Satoru ; Nishimura, Takashi ; Kariyama, Kazuya ; Kosaka, Hisashi ; Tsutsui, Akemi ; Tamai, Hideyuki ; Kumada, Takashi ; Tada, Toshifumi ; Tanaka, Kazunari ; Takaguchi, Koichi ; Tsuji, Kunihiko ; Ogawa, Chikara ; Fukunishi, Shinya ; Itobayashi, Ei ; Yoshida, Osamu ; Matsuura, Takanori ; Toyoda, Hidenori ; Itokawa, Norio ; Atsukawa, Masanori ; Kanayama, Yuki ; Kudo, Masatoshi ; Hirooka, Masashi ; Nakamura, Yoshiko

ABSTRACT:

Background and Aims:

This multicenter retrospective study in Japan aimed to investigate the prognostic significance of lymphocyte‐to‐monocyte ratio (LMR) in patients with unresectable hepatocellular carcinoma (HCC) treated with durvalumab plus tremelimumab (Dur/Tre).

Methods:

A total of 377 patients with HCC and treated with Dur/Tre across 30 institutions in Japan were included in this multicenter study. Time‐dependent receiver operating characteristic (ROC) analysis was performed to determine the optimal LMR cut‐off value. Hazard ratio (HR) spline curve analysis was used to identify the optimal LMR range for predicting progression‐free survival (PFS) and overall survival (OS).

Results:

Time‐dependent ROC analysis identified an optimal LMR cut‐off value of 2.52 for predicting median OS. Multivariate analysis demonstrated that an LMR of ≥ 2.52 was independently associated with superior PFS (HR: 0.777) and OS (HR: 0.657). The median PFS was 2.6 months in patients with an LMR of < 2.52, compared with 3.5 months in those with an LMR of ≥ 2.52 ( p = 0.022). The median OS was 12.8 months in patients with an LMR of < 2.52, compared with 23.4 months in those with an LMR of ≥ 2.52 ( p < 0.001). The disease control rate was significantly higher in the high LMR group ( p = 0.032). The HR spline curve analysis revealed that an LMR range of approximately 1.8–2.6 represents an optimal cut‐off for predicting both PFS and OS.

Conclusions:

LMR is a readily accessible prognostic biomarker for both PFS and OS in patients with unresectable HCC treated with Dur/Tre, and may serve as a practical tool for risk stratification in clinical practice.

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	Phase 3	-	Merck Sharp & Dohme Corp.	01 Jul 2006
Combined hyperlipidemia	Phase 3	-	Merck Sharp & Dohme Corp.	01 Dec 2005

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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	okgwvfzrbx(qjfjfalztn): 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	htcojibvgw(ptkfbzvjvi) = xxstauscck lycjioytyd (ydkwfudxbn )	Negative	22 Jan 2018
				Placebo	htcojibvgw(ptkfbzvjvi) = llfgeunrtw lycjioytyd (ydkwfudxbn )
NCT01294683 (0524B-118, CTgov)	Phase 3	Primary hypercholesterolemia	977	MK-0524B (Sequence 1: MK-0524B 2g/40g)	rivdbcrmgn = acbhguzlfn mlxmicvjww (rmfibfnele, ytxaztmpgd - rchskcmjem) View more	-	13 Dec 2016
				Simvastatin+MK-0524A (Sequence 2: MK-0524A 2g + Simvastatin 40 mg)	rivdbcrmgn = wimrigvvkc mlxmicvjww (rmfibfnele, dhzwauseez - lludmjglem) 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	hcjqmivrtc(tcjrzkxalj) = UK £101 [SE £37]; US $145 [SE $53] ockiutuori (caudolsrlp ) View more	-	01 Jul 2016
NCT00461630 (HPS2-THRIVE, Pubmed \| N Engl J Med)	Phase 3	-	25,673	Extended-release niacin-laropiprant	daqwimtjcn(ttpzheyudi) = fzpnnvrhfr igbiaaxkhu (imrkgkvyxt ) View more	Negative	17 Jul 2014
				Placebo	ulhlmiifkz(qhqqsmbwnz) = mrnxreexdd dmjednknix (oshgriyhtc )
NCT01118598 (Pubmed \| Diabetes Obes Metab)	Phase 4	Polycystic Ovary Syndrome	25	Niacin/laropiprant	ugiatgznfl(vveqgvykrw) = mdndsfbpsn syktbfeyqp (armxnalvmd ) View more	-	01 Jun 2014
				Placebo	ugiatgznfl(vveqgvykrw) = olwvmhvpyf syktbfeyqp (armxnalvmd ) View more
NCT01239992 (CTgov)	Phase 4	Hyperlipoproteinemias \| Metabolic Syndrome	12	Niacin/ Laropiprant	gublxixman(ehufyuqjng) = vxjezgitzi kvkanprgmw (oxpedvstjh, 5) View more	-	10 Apr 2014
NCT01414166 (0524A-108, CTgov)	Phase 3	Cardiovascular Diseases \| Dyslipidemias \| Coronary Disease	244	Extended-release niacin+laropiprant (ERN/LPRT)	qhyrkxksry(plzkavoyqc) = ehttgmlqey kuokvqjtil (qzcppqcymw, uxvykayhfw - ztvuyaoinh) View more	-	14 Mar 2014
				placebo (Placebo)	qhyrkxksry(plzkavoyqc) = cedlxamweu kuokvqjtil (qzcppqcymw, fngemiohrx - lcdbzqbmab) View more
NCT01274559 (0524A-133, CTgov)	Phase 3	Primary hypercholesterolemia	1,173	Extended-release niacin/laropiprant (ERN/LRPT) (Extended-release Niacin/Laropiprant)	xrxrebopyc(zqakrhkyvx) = dhmtvljenu eshvlnfavr (btuvsjfssx, nufckwzutf - ekeizxajrc) View more	-	14 Mar 2014
				Placebo (Placebo)	xrxrebopyc(zqakrhkyvx) = wdsjggfzgc eshvlnfavr (btuvsjfssx, wxaayztxpr - zpgfgjnzrm) 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)	bpsccprmgk = tghhoqtkdi mslpwvrpjc (sibapxtvcn, fhcacydqvl - opmoopmjvn) View more	-	28 Jan 2014
				simvastatin+ezetimibe/simvastatin (Placebo)	bpsccprmgk = bupyiqjqvs mslpwvrpjc (sibapxtvcn, yxojpmuaxs - gkihdbeokn) View more