What is it about?

New oral salts and cocrystals of isavuconazole are being investigated as an alternative to the prodrug form. It is likely that the prodrug in aqueous media is transformed into isavuconazole hydrate. If you use pure isavuconazole, this does not happen. Molecular causes are explained in the paper.

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Why is it important?

The existing prodrug of isavuconazole (ISV) has a number of disadvantages. Firstly, the hydrolysis enzyme, butyrylcholinesterase, is active only at neutral pH values, and in addition, we should not forget about people who have a hereditary pseudocholinesterase deficiency. Second, along with the ISV molecule and the inactive second compound, an acetaldehyde molecule is released. Thus, for 1 mol of isavuconazole in the human body, there is 1 mol of acetaldehyde, which causes great concern when taken by people with congenital alcohol intolerance. About a third of East Asians suffer from this syndrome to varying degrees of severity. In addition, a 2020 study by Indian scientists showed that this prodrug breaks down into several long-lived intermediates with unknown properties and safety performance. Our alternative solid forms of izuvuconazole avoid these drawbacks while increasing dissolution rates and dissolution rates similar to the prodrug


Treatment of systemic fungal infections for people with hereditary pseudocholinesterase deficiency and/or congenital alcohol intolerance without additional side effects

Nikita Vasilev
Institute of Solution Chemistry of RAS

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This page is a summary of: Exploring the solid form landscape of the antifungal drug isavuconazole: crystal structure analysis, phase transformation behavior and dissolution performance, CrystEngComm, January 2021, Royal Society of Chemistry,
DOI: 10.1039/d1ce01353j.
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