title: Extended-release niacin/laropiprant: reducing niacin-induced flushing to better realize the benefit of niacin in improving cardiovascular risk factors.
abstract: Treatment with niacin effectively improves multiple lipid parameters and cardiovascular outcomes. Widespread use of niacin, however, is limited by flushing, which is mediated primarily by prostaglandin D2 (PGD2). Laropiprant is a selective PGD2 receptor 1 (DP1) antagonist that reduces objective measures of niacin-induced flushing symptoms upon initiation of therapy and with more chronic use. Results from early dosing and formulation studies have culminated in the development of a combination extended-release (ER) niacin/laropiprant tablet aimed at providing the beneficial lipid-modifying effects of niacin, while reducing niacin-induced flushing. The improvement in the tolerability of niacin with ER niacin/laropiprant allows niacin dosing to initiate directly at 1 g and rapidly advance to a 2-g target dose. ER niacin/laropiprant generally is tolerated well and represents a new treatment option for dyslipidemia that offers the potential for more patients to receive the lipid-modifying and cardiovascular benefits of niacin.
authors.affiliation: Merck & Company, Incorporated, 126 East Lincoln Avenue, Rahway, NJ 07065, USA. john_paolini@merck.com
authors.forename: John F
authors.initials: JF
authors.lastname: Paolini
authors.forename: Harold E
authors.initials: HE
authors.lastname: Bays
authors.forename: Christie M
authors.initials: CM
authors.lastname: Ballantyne
authors.forename: Michael
authors.initials: M
authors.lastname: Davidson
authors.forename: Richard
authors.initials: R
authors.lastname: Pasternak
authors.forename: Darbie
authors.initials: D
authors.lastname: Maccubbin
authors.forename: Josephine M
authors.initials: JM
authors.lastname: Norquist
authors.forename: Eseng
authors.initials: E
authors.lastname: Lai
authors.forename: M Gerard
authors.initials: MG
authors.lastname: Waters
authors.forename: Olga
authors.initials: O
authors.lastname: Kuznetsova
authors.forename: Christine McCrary
authors.initials: CM
authors.lastname: Sisk
authors.forename: Yale B
authors.initials: YB
authors.lastname: Mitchel
mesh_terms: D000818:Animals; D003692:Delayed-Action Preparations; D004338:Drug Combinations; D050171:Dyslipidemias / Q000097:blood / Q000188:drug therapy*; D005483:Flushing / Q000139:chemically induced / Q000517:prevention & control*; D006801:Humans; D000960:Hypolipidemic Agents / Q000008:administration & dosage* / Q000009:adverse effects; D007211:Indoles / Q000008:administration & dosage*; D008055:Lipids / Q000097:blood; D009525:Niacin / Q000008:administration & dosage* / Q000009:adverse effects; D011971:Receptors, Immunologic / Q000037:antagonists & inhibitors*; D011982:Receptors, Prostaglandin / Q000037:antagonists & inhibitors*
chemical_list: D003692:Delayed-Action Preparations; D004338:Drug Combinations; D000960:Hypolipidemic Agents; D007211:Indoles; D008055:Lipids; C518174:MK-0524; D011971:Receptors, Immunologic; D011982:Receptors, Prostaglandin; D009525:Niacin; C036293:prostaglandin D2 receptor