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ixazomib + ketoconazole

Development stage
Preclinical
Lead developer
Takeda
Modality
Small Molecules
Administration
Oral
01

Overview

This entry refers to the **combination of ixazomib (a proteasome inhibitor) and ketoconazole (a strong CYP3A inhibitor)**. Ixazomib is an orally available small molecule proteasome inhibitor indicated (in combination with lenalidomide and dexamethasone) for the treatment of patients with multiple myeloma who have received at least one prior therapy. Ketoconazole is an antifungal agent also used experimentally as a strong inhibitor of the cytochrome P450 3A enzyme (CYP3A), which can affect the metabolism of many drugs. Clinical studies specifically examining this combination show that ketoconazole, as a strong CYP3A inhibitor, **does not have a clinically meaningful effect on the pharmacokinetics of ixazomib**, indicating that CYP3A’s role in ixazomib clearance is relatively minor. The combination is not marketed as a fixed product and is not an approved therapeutic regimen. This combination is studied chiefly to assess drug–drug interactions—particularly the effect of CYP3A inhibition on ixazomib exposure in humans[1][3].

Other names
ixazomib citrate
02

Targets

CYP3A7 (Cytochrome P450 3A7)PSMB2 (Proteasome subunit beta type-2)PSMB5 (Proteasome subunit beta Type-5)

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