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Table representation of search results timeline featuring number of search results per year.

Year Number of Results
2006 3
2007 14
2008 12
2009 24
2010 21
2011 16
2012 14
2013 22
2014 22
2015 18
2016 8
2017 5
2018 4
2019 3
2020 2
2022 2
2023 1
2024 0

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167 results

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Page 1
Inverse agonist and pharmacochaperone properties of MK-0524 on the prostanoid DP1 receptor.
Labrecque P, Roy SJ, Fréchette L, Iorio-Morin C, Gallant MA, Parent JL. Labrecque P, et al. PLoS One. 2013 Jun 10;8(6):e65767. doi: 10.1371/journal.pone.0065767. Print 2013. PLoS One. 2013. PMID: 23762421 Free PMC article.
Basal ERK1/2 activation by DP1 was not modulated by MK-0524. Interestingly, treatment of HEK293 cells expressing Flag-tagged DP1 with MK-0524 promoted DP1 cell surface expression time-dependently to reach a maximum increase of 50% compared to control a …
Basal ERK1/2 activation by DP1 was not modulated by MK-0524. Interestingly, treatment of HEK293 cells expressing Flag-tagged D …
Extended-release niacin (nicotinic acid)/laropiprant.
Perry CM. Perry CM. Drugs. 2009 Aug 20;69(12):1665-79. doi: 10.2165/11203730-000000000-00000. Drugs. 2009. PMID: 19678716 Review.

Niacin (vitamin B3) is a lipid-modifying drug and laropiprant is an anti-flushing agent, which reduces flushing induced by niacin. ...The incidence and intensity of flushing (an efficacy endpoint) were significantly (p < 0.05) reduced with ER niacin/laropiprant c

…
Niacin (vitamin B3) is a lipid-modifying drug and laropiprant is an anti-flushing agent, which reduces flushing induced by niacin. .. …
[Pharmacovigilance update].
Diezi L, Renard D, Rothuizen LE, Livio F. Diezi L, et al. Rev Med Suisse. 2014 Jan 15;10(412-413):119-22. Rev Med Suisse. 2014. PMID: 24558915 Review. French.
Fingolimod: rare cases of progressive multifocal leucoencephalopathy. Tolvaptan: potential for hepatotoxicity. Nicotinic acid/laropiprant: suspension of marketing authorization as benefits no longer outweigh risks....
Fingolimod: rare cases of progressive multifocal leucoencephalopathy. Tolvaptan: potential for hepatotoxicity. Nicotinic acid/laropiprant …
Metabolism of MK-0524, a prostaglandin D2 receptor 1 antagonist, in microsomes and hepatocytes from preclinical species and humans.
Dean BJ, Chang S, Silva Elipe MV, Xia YQ, Braun M, Soli E, Zhao Y, Franklin RB, Karanam B. Dean BJ, et al. Drug Metab Dispos. 2007 Feb;35(2):283-92. doi: 10.1124/dmd.106.011551. Epub 2006 Nov 28. Drug Metab Dispos. 2007. PMID: 17132765
The major in vitro and in vivo metabolite of MK-0524 is the acyl glucuronic acid conjugate of the parent compound, M2. ...MK-0524 also was subject to phase I oxidative metabolism; however, the rate was significantly lower than that of glucuronidation. …
The major in vitro and in vivo metabolite of MK-0524 is the acyl glucuronic acid conjugate of the parent compound, M2. ...M …
The pharmacokinetics and disposition of MK-0524, a Prosglandin D2 Receptor 1 antagonist, in rats, dogs and monkeys.
Chang SW, Reddy V, Pereira T, Dean BJ, Xia YQ, Seto C, Franklin RB, Karanam BV. Chang SW, et al. Xenobiotica. 2007 May;37(5):514-33. doi: 10.1080/00498250601175565. Xenobiotica. 2007. PMID: 17523054
MK-0524 is a potent, selective and orally active Prosglandin D(2) Receptor 1 (DP(1)) antagonist currently under clinical development for the treatment of niacin-induced flushing. Experiments to study the pharmacokinetics, metabolism and excretion of MK-052 …
MK-0524 is a potent, selective and orally active Prosglandin D(2) Receptor 1 (DP(1)) antagonist currently under clinical devel …
Review of extended-release niacin/laropiprant fixed combination in the treatment of mixed dyslipidemia and primary hypercholesterolemia.
Parhofer KG. Parhofer KG. Vasc Health Risk Manag. 2009;5:901-8. doi: 10.2147/vhrm.s4502. Epub 2009 Nov 16. Vasc Health Risk Manag. 2009. PMID: 20016845 Free PMC article. Review.
Although the addition of laropiprant will reduce the frequency of flushing, it will not completely eliminate this side effect. Laropiprant does not change the effect of niacin on lipids or other side effects of niacin (ie, gastro-intestinal problems, glucose elevati …
Although the addition of laropiprant will reduce the frequency of flushing, it will not completely eliminate this side effect. Lar …
Using human recombinant UDP-glucuronosyltransferase isoforms and a relative activity factor approach to model total body clearance of laropiprant (MK-0524) in humans.
Gibson CR, Lu P, Maciolek C, Wudarski C, Barter Z, Rowland-Yeo K, Stroh M, Lai E, Nicoll-Griffith DA. Gibson CR, et al. Xenobiotica. 2013 Dec;43(12):1027-36. doi: 10.3109/00498254.2013.791761. Epub 2013 May 3. Xenobiotica. 2013. PMID: 23641955 Clinical Trial.
A major pathway of elimination of the prostaglandin D2 receptor 1 antagonist laropiprant in humans is by uridine diphosphate-glucuronosyltransferase (UGT)-mediated biotransformation. In this study, liver and kidney relative activity factors were developed for UGT1A1, 1A9 a …
A major pathway of elimination of the prostaglandin D2 receptor 1 antagonist laropiprant in humans is by uridine diphosphate-glucuron …
The effects of laropiprant on the antiplatelet activity of co-administered clopidogrel and aspirin.
De Kam PJ, Luo WL, Wenning L, Ratcliffe L, Sisk CM, Royalty J, Radziszewski W, Wagner JA, Lai E. De Kam PJ, et al. Platelets. 2014;25(7):480-7. doi: 10.3109/09537104.2013.836747. Epub 2013 Nov 8. Platelets. 2014. PMID: 24206527 Clinical Trial.
Laropiprant is an antagonist of the prostaglandin PGD2 receptor DP1. Laropiprant has a weak affinity for the thromboxane A2 receptor TP. ...
Laropiprant is an antagonist of the prostaglandin PGD2 receptor DP1. Laropiprant has a weak affinity for the thromboxane A2 re …
Drug-drug noninteractions.
Greenblatt DJ. Greenblatt DJ. Cardiovasc Ther. 2009 Winter;27(4):226-9. doi: 10.1111/j.1755-5922.2009.00111.x. Cardiovasc Ther. 2009. PMID: 19903185 Free article.
Efficacy of Laropiprant in Minimizing Brain Injury Following Experimental Intracerebral Hemorrhage.
Ahmad AS, Mendes M, Hernandez D, Doré S. Ahmad AS, et al. Sci Rep. 2017 Aug 25;7(1):9489. doi: 10.1038/s41598-017-09994-5. Sci Rep. 2017. PMID: 28842638 Free PMC article.
To test the therapeutic potential of laropiprant, WT mice subjected to ICH were treated with laropiprant at 1 hour after the ICH. ...Finally, the roles of laropiprant on gliosis and iron accumulation were also investigated. ...
To test the therapeutic potential of laropiprant, WT mice subjected to ICH were treated with laropiprant at 1 hour after the I …
167 results