Scientific Reports · 2023 · 23 citations · 25 references
MedicineCardiologyPharmacologyMolecular PharmacologyPharmacodynamicsProtein-protein InteractionsCardiac MedicationsCardiac PharmacotherapyCardiomyopathy PharmacotherapyCardiovascular PharmacodynamicsHeart FailureInherited CardiomyopathiesActin InteractionsCardiac Systolic FunctionHeart Failure SymptomsHypertrophic Cardiomyopathy Drug TherapyMybpc3 MutationsMyocardial Contractility ModulationMyosin Inhibitor TherapyMyosin Inhibitors
Hypertrophic cardiomyopathy (HCM) is the most prevalent inherited cardiac disease in humans and cats and lacks efficacious pharmacologic interventions in the preclinical phase of disease. LV outflow tract obstruction (LVOTO) is commonly observed in HCM-affected patients and is a primary driver of heart failure symptoms and reduced quality of life. Novel small-molecule cardiac myosin inhibitors target actin-myosin interactions to alleviate overactive protein interactions. A prospective, randomized, controlled cross-over study was performed to evaluate pharmacodynamic effects of two doses (0.3 and 1 mg/kg) of a next-in-class cardiac myosin inhibitor, aficamten (CK-3773274, CK-274), on cardiac function in cats with the A31P MYBPC3 mutation and oHCM. Dose-dependent reductions in LV systolic function, LVOT pressure gradient, and isovolumetric relaxation times compared to baseline were observed. Promising beneficial effects of reduced systolic function warrant further studies of this next-in-class therapeutic to evaluate the benefit of long-term administration in this patient population.
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Iacopo Olivotto, Artur Oręziak, Roberto Barriales‐Villa et al. · The Lancet · 2020 · 1.2K citations · Full text
A small-molecule inhibitor of sarcomere contractility suppresses hypertrophic cardiomyopathy in mice
Eric M. Green, Hiroko Wakimoto, Robert L. Anderson et al. · Science · 2016 · 709 citations · Full text
Medicine, Cardiology, Pharmacology +15
Virginia Luis Fuentes, Jonathan A. Abbott, Valérie Chetboul et al. · Journal of Veterinary Internal Medicine · 2020 · 412 citations · Full text