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001-es BibID:	BIBFORM077899
035-os BibID:	(PMID)29278207 (WoS)000432247500002 (Scopus)85048878557
Első szerző:	Nánási Péter Pál ifj. (sejtbiológus)
Cím:	Omecamtiv Mecarbil : a Myosin Motor Activator Agent with Promising Clinical Performance and New in vitro Results / Péter Nánási Jr., István Komáromi, Marta Gaburjakova, János Almássy
Dátum:	2018
ISSN:	0929-8673
Megjegyzések:	Abstract: Background: Clinical treatment of heart failure is still suffering from limited efficacy and unfavorable side effects. The recently developed group of agents, the myosin motor activators, act directly on cardiac myosin resulting in an increased force generation and prolongation of contraction. The lead molecule, omecamtiv mecarbil is now in human 3 stage. In addition tothe promising clinical data published so far, there are new in vitro results indicating that the effect of omecamtiv mecarbil on contractility is rate-dependent. Furthermore, omecamtiv mecarbilwas shown to activate cardiac ryanodine receptors, an effect that may carry proarrhythmic risk. Methods: These new results, together with the controversial effects of the drug on cardiac oxygen consumption, are critically discussed in this review in light of the current literature on omecamtiv mecarbil. Results: In therapeutically relevant concentrations the beneficial inotropic effect of the agent isnot likely affected by these new results - in accordance with the good clinical data. At supratherapeutic concentrations, however, activation of cardiac ryanodine receptors may increasearrhythmia propensity, and the stronger effect on diastolic than systolic cell shortening, observed at higher pacing frequencies, may decrease or offset the inotropic effect of omecamtivmecarbil. Conclusion: Further studies with definitely supratherapeutical concentrations of omecamtivmecarbil should be designed to map the actual risk of these potentially harmful side-effects.
Tárgyszavak:	Orvostudományok Elméleti orvostudományok idegen nyelvű folyóiratközlemény külföldi lapban folyóiratcikk Heart failure inotropic agents myosin activators Omecamtiv mecarbil Ryanodine receptor Cytosolic Ca 2+
Megjelenés:	Current Medicinal Chemistry. - 25 : 15 (2018), p. 1720-1728. -
További szerzők:	Komáromi István (1957-) (vegyész, molekuláris biológus, biokémikus) Gaburjakova, Marta Almássy János (1981-) (élettanász, biológus, angol-magyar szakfordító)
Pályázati támogatás:	NKFIH PD112199 NKFIH Janos Bolyai Research Scholarship of the Hungarian Academy of Sciences MTA Szodoray Scholarship of the University of Debrecen Egyéb
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