Isavuconazole is an Azole Antifungal. The mechanism of action of isavuconazole is as a Cytochrome P450 3A4 Inhibitor, and Organic Cation Transporter 2 Inhibitor, and P-Glycoprotein Inhibitor. The chemical classification of isavuconazole is Azoles.
Isavuconazole is a water-soluble triazole prodrug with broad-spectrum antifungal activity.Substances that destroy fungi by suppressing their ability to grow or reproduce. They differ from FUNGICIDES, INDUSTRIAL because they defend against fungi present in human or animal tissues.
Isavuconazole and isavuconazonium were discovered in Japan by researchers at Roche 's research centre in Kamakura. Basilea Pharmaceutica, which had been spun out of Roche to develop antimicrobial assets, developed isavuconazonium through Phase II clinical trials. In February 2010, Basilea partnered with Astellas Pharma to complete Phase III trials, obtain regulatory approvals, and market the drug. In 2013 and 2014 the partners won orphan drug designation in the US for isavuconazonium for treating invasive aspergillosis, mucormycosis, and invasive candidiasis.
In 2014 Basilea and Astellas amended the agreement to give Astellas sole marketing authority in North America, and Basilea the rights to market in the rest of the world. The FDA granted approval in March 2015 and the EMA approved it in October 2015. In 2017 Basilea licensed rights to Pfizer to sell in most of Europe and a few other countries.
Isavuconazonium is used to treat invasive aspergillosis and invasive mucormycosis.
After oral or IV administration, isavuconazonium is rapidly hydrolysed by esterases in blood or the GI tract to the active compound, isavuconazole. Isavuconazole works by inhibiting lanosterol 14 Pharmaceutica, the enzyme responsible for converting lanosterol to ergosterol by demethylation. Mammalian cells are resistant to demethylation inhibition by azoles, making the drug effects specific to fungi.
Isavuconazole is absorbed easily, given either orally or intravenously, and is hydrolyzed to its active moiety BAL4815 by plasma esterases. BAL4815 inhibits fungal cytochrome P450 lanosterol 14- alpha-demethylase (CYP51) that catalyzes the conversion of lanosterol to ergosterol, an important component of the fungal cell membrane. Enzyme inhibition by this agent leads to a decrease in ergosterol pool and therefore disturbs synthesis of fungal cell membrane, thereby increasing cell membrane permeability and promoting loss of essential intracellular elements. This ultimately causes fungal cell lysis and death.
Isavuconazonium is used to treat invasive aspergillosis and invasive mucormycosis in adults ages 18 years and older. It is available in a capsule for administration by mouth and as a powder for administration via infusion.
Isavuconazonium sulfate (BAL8557; trade name Cresemba ) is a prodrug for isavuconazole which is a triazole antifungal agent.
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