Optimizing the Therapeutic Potential of Sacubitril/Valsartan: The Promise of Co-Crystal Engineering

Authors: Sharma R*

DOI: 10.23880/oajc-16000215

Volume 9, Issue 1

Abstract

Heart failure (HF) is a complex clinical syndrome with high morbidity and mortality, posing a significant global healthcare burden. Guideline-directed medical therapy remains the standard for managing HF with reduced ejection fraction (HFrEF), incorporating four key drug classes, including angiotensin receptor–neprilysin inhibitors (ARNIs). Sacubitril/valsartan (Entresto, development code LCZ696) was approved as the first successful angiotensin receptor neprilysin inhibitor (ARNI) in the market in 2015 and has demonstrated efficacy in treating HF. The sacubitril/valsartan combination was developed by Novartis and marketed by JB Chemicals as Azmarda (Innovator Sacubitril/Valsartan) in India. The co-crystal technology utilized in the innovator’s Sacubitril/Valsartan formulation, enhances its solubility, stability, and bioavailability, thereby optimizing therapeutic effectiveness. Co-crystal technology offers advantages over generic formulations by improving drug dissolution, permeability, and pharmacokinetics. A recent study comparing different sacubitril/valsartan brands highlights the superior dissolution characteristics and stability of co-crystal formulations, such as Azmarda, which utilize a patented polymorphic technology. As HF treatment continues to evolve, integration of innovative co-crystal technology in drug formulations represents a promising approach to enhancing drug performance and improving patient outcomes.

Keywords: Heart Failure; Co-Crystal Technology; Sacubitril/Valsartan; Bioavailability; Angiotensin Receptor-Neprilysin Inhibitors

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