Pune:CSIR-National Chemical Laboratory (CSIR-NCL), Pune and University of Hyderabad have discovered novel hydrate polymorphs of Entresto, a product is used to treat certain types of heart failure
CSIR-NCL as part of a Mission Mode program funded by the Council of Scientific and Industrial Research (CSIR), had initiated research on novel crystalline hydrate forms and polymorphs of Entresto in 2018. Ashwini Kumar Nangia, then Director of CSIR-NCL, and Dr Rajesh G. Gonnade, chief scientist from the Physical and Materials Chemistry Division, led the project.
The comprehensive study has appeared in the Royal Society of Chemistry journal CrystEngComm, which deals with crystal engineering and drug polymorphs. The research team has successfully characterized and identified six different crystalline forms of Entresto, with varying amounts of water content and containing the active pharmaceutical ingredients (APIs) valsartan and sacubitril in their anionic state with bonded sodium cations.
The different hydrated forms of Entresto have 2.0-3.2% water and exhibit additional stability to temperature and moisture, which is vital for their long-term storage, shelf-life, and drug bioavailability. This paper is a first of its kind wherein investigators have shown that large supramolecular drug complexes pose unique challenges in the characterization of polymorphs and hydrate structures by powder X-ray diffraction, thermal measurements, and spectroscopic techniques. The next task for the team will be to understand the molecular packing arrangement and hydrogen bonding with water by determining its crystal structures.
Entresto is the world’s top-selling drug launched for the treatment of chronic heart failure in advanced critical patients, approved by the US FDA in 2015.

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