Extended-release niacin/laropiprant: reducing niacin-induced flushing to better realize the benefit of niacin in improving cardiovascular risk factors.
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.
Paolini
John F
JF
Merck & Company, Incorporated, 126 East Lincoln Avenue, Rahway, NJ 07065, USA. john_paolini@merck.com
Bays
Harold E
HE
Ballantyne
Christie M
CM
Davidson
Michael
M
Pasternak
Richard
R
Maccubbin
Darbie
D
Norquist
Josephine M
JM
Lai
Eseng
E
Waters
M Gerard
MG
Kuznetsova
Olga
O
Sisk
Christine McCrary
CM
Mitchel
Yale B
YB
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*
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