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- Title
The myosin activator omecamtiv mecarbil: a promising new inotropic agent<sup>1</sup>.
- Authors
Nánási, Péter; Váczi, Krisztina; Papp, Zoltán
- Abstract
Heart failure became a leading cause of mortality in the past few decades with a progressively increasing prevalence. Its current therapy is restricted largely to the suppression of the sympathetic activity and the renin-angiotensin system in combination with diuretics. This restrictive strategy is due to the potential long-term adverse effects of inotropic agents despite their effective influence on cardiac function when employed for short durations. Positive inotropes include inhibitors of the Na+/K+ pump, β-receptor agonists, and phosphodiesterase inhibitors. Theoretically, Ca2+ sensitizers may also increase cardiac contractility without resulting in Ca2+ overload; nevertheless, their mechanism of action is frequently complicated by other pleiotropic effects. Recently, a new positive inotropic agent, the myosin activator omecamtiv mecarbil, has been developed. Omecamtiv mecarbil binds directly to β-myosin heavy chain and enhances cardiac contractility by increasing the number of the active force-generating cross-bridges, presumably without major off-target effects. This review focuses on recent in vivo and in vitro results obtained with omecamtiv mecarbil, and discusses its mechanism of action at a molecular level. Based on clinical data, omecamtiv mecarbil is a promising new tool in the treatment of systolic heart failure.
- Subjects
MYOSIN; HEART failure treatment; RENIN-angiotensin system; PHOSPHODIESTERASE inhibitors; DIGITALIS (Drug)
- Publication
Canadian Journal of Physiology & Pharmacology, 2016, Vol 94, Issue 10, p1033
- ISSN
0008-4212
- Publication type
Article
- DOI
10.1139/cjpp-2015-0573