Results 11 to 20 of about 51,089 (251)

Pharmacokinetics, disposition, and biotransformation of the cardiac myosin inhibitor aficamten in humans [PDF]

Pharmacology Research & Perspectives
Aficamten, a cardiac myosin inhibitor, is being developed for the treatment of patients with symptomatic hypertrophic cardiomyopathy (HCM). The purpose of this study was to determine the absorption, metabolism, and excretion of aficamten.
Donghong Xu, Punag Divanji, Adrienne Griffith, Rajaa Sukhun, Kathleen Cheplo, Jianlin Li, Polina German   +6 more
doaj   +4 more sources

Aficamten is a small-molecule cardiac myosin inhibitor designed to treat hypertrophic cardiomyopathy. [PDF]

Nat Cardiovasc Res
AbstractHypertrophic cardiomyopathy (HCM) is an inherited disease of the sarcomere resulting in excessive cardiac contractility. The first-in-class cardiac myosin inhibitor, mavacamten, improves symptoms in obstructive HCM. Here we present aficamten, a selective small-molecule inhibitor of cardiac myosin that diminishes ATPase activity by strongly ...
Hartman JJ, Hwee DT, Robert-Paganin J, Chuang C, Chin ER, Edell S, Lee KH, Madhvani R, Paliwal P, Pernier J, Sarkar SS, Schaletzky J, Schauer K, Taheri KD, Wang J, Wehri E, Wu Y, Houdusse A, Morgan BP, Malik FI.   +19 more
europepmc   +6 more sources

Cardiac Myosin Inhibitors in the Treatment of Hypertrophic Cardiomyopathy: Clinical Trials and Future Challenges [PDF]

Biomolecules
Hypertrophic cardiomyopathy (HCM) is a prevalent and often underdiagnosed genetic cardiac disorder characterized by left ventricular hypertrophy and, in many cases, dynamic left ventricular outflow tract obstruction (LVOTO).
Arnold Kukowka, Marek Droździk
doaj   +3 more sources

Novel cardiac myosin inhibitor for hypertrophic cardiomyopathy. [PDF]

J Gen Physiol
New RLC-1 small-molecule inhibits actomyosin interactions, reduces contractile force, and speeds up myosin cross-bridge kinetics.
Szczesna-Cordary D.
europepmc   +3 more sources

Mavacamten Cardiac Myosin Inhibitor: Clinical Applications and Future Perspectives. [PDF]

Cureus
Mavacamten is a first-in-class, selective allosteric inhibitor of cardiac myosin adenosine triphosphatase (ATPase) that has emerged as a novel therapeutic option for patients with symptomatic hypertrophic obstructive cardiomyopathy (HOCM) who remain refractory to conventional therapy, such as beta-blockers and calcium channel blockers.
Ramadan MM, Al-Najjar RA, Abady RS, Obaid HA, Mostafa YA, Al-Obeid MT, Elmahal M.   +6 more
europepmc   +3 more sources

Mechanisms of a novel regulatory light chain-dependent cardiac myosin inhibitor. [PDF]

J Gen Physiol
Hypertrophic cardiomyopathy (HCM) is a genetic disease of the heart characterized by thickening of the left ventricle (LV), hypercontractility, and impaired relaxation. HCM is caused primarily by heritable mutations in sarcomeric proteins, such as β myosin heavy chain.
Kooiker K, Gan QF, Yu M, Sa N, Mohran S, Cheng Y, Flint G, Neys S, Gao C, Nissen D, McMillen T, Asencio A, Ma W, Irving TC, Moussavi-Harami F, Regnier M.   +15 more
europepmc   +3 more sources

Cardiac myosin-specific autoimmune T cells contribute to immune-checkpoint-inhibitor-associated myocarditis

Cell Reports, 2022
Immune checkpoint inhibitors (ICIs) are an effective therapy for various cancers; however, they can induce immune-related adverse events (irAEs) as a side effect. Myocarditis is an uncommon, but fatal, irAE caused after ICI treatments. Currently, the mechanism of ICI-associated myocarditis is unclear. Here, we show the development of myocarditis in A/J
Taejoon Won, Hannah M. Kalinoski, Megan K. Wood, David M. Hughes, Camille M. Jaime, Paul Delgado, Monica V. Talor, Ninaad Lasrado, Jay Reddy, Daniela Čiháková   +9 more
openaire   +4 more sources

Novel Cardiac Myosin Inhibitor Therapy for Hypertrophic Cardiomyopathy in Adults: A Contemporary Review. [PDF]

Am J Cardiovasc Drugs
Hypertrophic cardiomyopathy (HCM) affects as many as 1 in 200 people in the adult population globally. Patients may present with exertional dyspnea, presyncope or syncope, atrial and ventricular arrhythmias, heart failure, and even sudden cardiac death.
Kalinski JK, Xu B, Boyd R, Tasseff N, Rutkowski K, Ospina S, Smedira N, Thamilarasan M, Popovic ZB, Desai MY.   +9 more
europepmc   +3 more sources

Cardiac myosin inhibitor, CK-586, minimally reduces systolic function and ameliorates obstruction in feline hypertrophic cardiomyopathy [PDF]

Scientific Reports
Hypertrophic cardiomyopathy (HCM) remains the most common cardiomyopathy in humans and cats with few preclinical pharmacologic interventional studies. Small-molecule sarcomere inhibitors are promising novel therapeutics for the management of obstructive ...
Victor N. Rivas, Amanda E. Crofton, Carina E. Jauregui, Jalena R. Wouters, Betty S. Yang, Luke A. Wittenburg, Joanna L. Kaplan, Darren T. Hwee, Anne N. Murphy, Bradley P. Morgan, Fady I. Malik, Samantha P. Harris, Joshua A. Stern   +12 more
doaj   +2 more sources

Cardiac Myosin Inhibitors in Hypertrophic Cardiomyopathy: From Sarcomere to Clinic. [PDF]

Int J Mol Sci
Hypertrophic cardiomyopathy (HCM) is a primary myocardial disease characterized by unexplained left ventricular hypertrophy, often resulting from pathogenic variants of sarcomeric protein genes. Conventional treatments, such as the use of beta blockers or calcium channel blockers, focus on symptomatic control but do not address the underlying ...
Nakamura K, Okumura T, Kato S, Onoue K, Kubo T, Kouzu H, Yano T, Inomata T.   +7 more
europepmc   +3 more sources