Results 1 to 10 of about 461 (138)

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

Pharmacology Research and 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
exaly   +6 more sources

Clinical Evaluation of Drug–Drug Interactions With Aficamten [PDF]

Clinical and Translational Science
Aficamten is a next‐in‐class small molecule cardiac myosin inhibitor that was recently approved by the United States Food and Drug Administration (FDA) for the treatment of symptomatic obstructive hypertrophic cardiomyopathy (oHCM).
Neha Maharao, Donghong Xu, Punag Divanji, Tyrell J. Simkins, Jianlin Li, Camelia Dumitrescu, Priyanka Solanki, Adrienne Griffith, Stephen B. Heitner, Stuart Kupfer, Polina German, Justin D. Lutz   +11 more
doaj   +5 more sources

Comprehensive Review: Mavacamten and Aficamten in Hypertrophic Cardiomyopathy [PDF]

Biomedicines
Hypertrophic cardiomyopathy (HCM) is the most common monogenic heart disease, with an estimated prevalence of 1:600 in the general population, and is associated with significant morbidity.
Helin Savsin, Tomasz Tokarek
doaj   +5 more sources

Toward a Quantitative Understanding of Aficamten Clinical Pharmacology: Population Pharmacokinetic Modeling [PDF]

CPT: Pharmacometrics & Systems Pharmacology
Aficamten is a next‐in‐class, cardiac myosin inhibitor in development as a potential chronic oral treatment for patients with hypertrophic cardiomyopathy (HCM).
Donghong Xu, Hanbin Li, Stephen B. Heitner, Daniel L. Jacoby, Stuart Kupfer, Polina German, Justin Lutz   +6 more
doaj   +5 more sources

Safety, tolerability, pharmacokinetics, and pharmacodynamics of single and multiple doses of aficamten in healthy Chinese participants: a randomized, double-blind, placebo-controlled, phase 1 study [PDF]

Frontiers in Pharmacology, 2023
Objectives: Aficamten is a selective, small-molecule allosteric inhibitor of cardiac sarcomere being developed as a chronic oral treatment for patients with symptomatic obstructive hypertrophic cardiomyopathy.
He Yu, Wang Hongyun
exaly   +4 more sources

Towards a Quantitative Understanding of Aficamten Clinical Pharmacology: Pharmacokinetic‐Cardiodynamic Modeling to Support Safety and Efficacy [PDF]

CPT: Pharmacometrics & Systems Pharmacology
In the phase 3 study SEQUOIA‐HCM (NCT05186818), aficamten, a next‐in‐class cardiac myosin inhibitor, was safe and efficacious in participants with obstructive hypertrophic cardiomyopathy (oHCM). Using pharmacokinetics/pharmacodynamics (PKPD) modeling, we
Justin D. Lutz, Russ Wada, Daniel L. Jacoby, Stephen B. Heitner, Stuart Kupfer, Polina German   +5 more
doaj   +3 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

Myosin Modulator Aficamten Inhibits Force by Altering Myosin’s Biochemical Activity Without Changing Thick Filament Structure [PDF]

JACC: Basic to Translational Science
Summary: We investigated the effects of aficamten on cardiac muscle structure, biochemical activity, and contractile function. Aficamten does not structurally sequester myosin heads along the thick filament.
Saffie Mohran, PhD, Kristina B. Kooiker, PhD, Ateeqa Naim, BS, Matvey Pilagov, BS, Anthony Asencio, BS, Kyrah L. Turner, BS, Weikang Ma, PhD, Galina Flint, MD., Siyao Jiang, BS, Jing Zhao, BS, Timothy S. McMillen, PhD, Christian Mandrycky, PhD, Max Mahoney-Schaefer, BS, Thomas C. Irving, PhD, Bertrand C.W. Tanner, PhD, Neil M. Kad, PhD, Michael Regnier, PhD, Farid Moussavi-Harami, MD   +17 more
doaj   +2 more sources

Targeting the Sarcomere: Myosin Inhibitors as the Revolutionary Game Changer in Hypertrophic Cardiomyopathy [PDF]

Reviews in Cardiovascular Medicine
Hypertrophic cardiomyopathy (HCM) represents the most common inherited cardiac disease and a leading cause of heart failure, arrhythmias, and sudden cardiac death in young individuals.
Farbod Sedaghat-Hamedani, Elham Kayvanpour, Benjamin Meder   +2 more
doaj   +2 more sources

Effect of Cardiac Myosin Inhibitors on Echocardiographic Features of Cardiac Structure and Function in Hypertrophic Cardiomyopathy: A Systematic Review and Meta-Analysis [PDF]

Reviews in Cardiovascular Medicine
Background: Recent advancements have introduced novel cardiac myosin inhibitors (CMIs) that have demonstrated significant efficacy in treating hypertrophic cardiomyopathy (HCM).
Yang Lu, Yuanyuan Zhu, Zhuang Tian
doaj   +2 more sources