Drug intelligence / Profile preview

capivasertib + itraconazole

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral
01

Overview

Capivasertib + itraconazole is an unbranded investigational combination of capivasertib, an orally available small molecule pan-AKT (serine/threonine protein kinase B) inhibitor, and itraconazole, an oral triazole antifungal agent and strong cytochrome P450 3A4 (CYP3A4) inhibitor. Capivasertib inhibits AKT isoforms (AKT1/2/3), blocking downstream PI3K/AKT signaling and reducing tumor cell growth; it is approved as monotherapy or in combination with fulvestrant for HR+, HER2- breast cancer with PIK3CA/AKT1/PTEN alterations. Itraconazole is used clinically to treat fungal infections, but in this context acts as a CYP3A4 inhibitor to investigate drug-drug interactions, affecting capivasertib’s metabolism and pharmacokinetics. This combination is studied for pharmacokinetic interactions and safety, primarily in healthy volunteers, to inform clinical use of capivasertib in patients requiring CYP3A4 inhibitors[1][2][3][5].

Other names
capivasertibAZD5363AZD-5363AZD 5363itraconazoleSporanox
02

Targets

CYP3A4 (Cytochrome P450 3A4)AKT2 (Rac-beta serine/threonine-protein kinase)AKT1 (Proto-oncogene serine/threonine-protein kinase Akt1)

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