Drug intelligence / Profile preview

volasertib + itraconazole

Development stage
Unknown
Lead developer
Oncoheroes Biosciences
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

A fixed-sequence, open-label combination of **volasertib**, a potent and selective small-molecule inhibitor of polo-like kinase 1 (PLK1), with **itraconazole**, a systemic antifungal agent that is a strong inhibitor of cytochrome P450 3A4 (CYP3A4) and P-glycoprotein (P-gp). This combination has been clinically investigated to elucidate potential drug-drug interactions, specifically whether itraconazole alters the pharmacokinetics or safety of volasertib in patients with solid tumors. PLK1 inhibition by volasertib disrupts mitotic progression and cell division, exerting antineoplastic effects, while itraconazole's antifungal role is complemented by pharmacokinetic modulation through CYP3A4 and P-gp inhibition.

02

Targets

ABCB1 (P-glycoprotein)PLK1 (Polo like kinase 1)PLK3CYP3A4 (Cytochrome P450 3A4)PLK2 (Polo-like kinase 2)

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