Drug intelligence / Profile preview

isavuconazole + lopinavir + ritonavir

Development stage
Unknown
Lead developer
Astellas Pharma
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a **combination of three small-molecule pharmaceuticals**: - **Isavuconazole**: a triazole antifungal approved for the treatment of invasive aspergillosis and mucormycosis. It inhibits fungal cell membrane synthesis by blocking cytochrome P450-dependent lanosterol 14-α-demethylase, disrupting ergosterol biosynthesis[2][4]. - **Lopinavir**: an antiretroviral protease inhibitor used as part of combination therapy for HIV-1 infection, almost always co-formulated with ritonavir for pharmacokinetic boosting. - **Ritonavir**: originally developed as a protease inhibitor for HIV, now primarily used to inhibit CYP3A-mediated metabolism and boost the systemic concentration of other protease inhibitors (notably lopinavir), as well as being a substrate and inhibitor for P-gp, OATP1B1, and OATP1B3[1][3]. **Clinical studies have investigated the pharmacokinetic interactions among these agents, finding that isavuconazole increases exposure of itself when coadministered with lopinavir/ritonavir, but decreases the exposure of lopinavir and ritonavir, which may reduce antiviral efficacy and increase gastrointestinal adverse events[1][3][5].** This combination does not have a unique brand or proprietary name and is used only in research or as coadministered agents, not as a formulated product.

02

Targets

OATP1B1 (Organic anion transporting polypeptide 1B1)CYP51A1 (Sterol 14α-demethylase)ABCB1 (P-glycoprotein)CYP3A4 (Cytochrome P450 3A4)SLCO1B3 (Organic anion transporting polypeptide 1B3)PR (Progesterone receptor)

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