Drug intelligence / Profile preview

pomalidomide + ketoconazole + fluvoxamine

Development stage
Phase 1
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral
01

Overview

This is a **combination of three small-molecule drugs**: pomalidomide (an immunomodulatory agent), ketoconazole (a strong CYP3A4/P-gp inhibitor and antifungal), and fluvoxamine (a strong CYP1A2 inhibitor and selective serotonin reuptake inhibitor). This combination does not correspond to any approved commercial product. It has been studied for pharmacokinetic drug-drug interaction effects. Coadministration of ketoconazole and fluvoxamine with pomalidomide substantially increases pomalidomide exposure by **inhibiting its major metabolic pathways (CYP1A2 and CYP3A4/P-gp)**. This markedly elevates the plasma concentration and area under the curve (AUC) of pomalidomide, greatly enhancing the risk of exposure-related toxicities. Pomalidomide is developed primarily for **relapsed/refractory multiple myeloma**, with ketoconazole and fluvoxamine used here as **pharmacokinetic modulators** rather than for their approved indications[1][2][5][6][7][8].

02

Targets

CRBN (Cereblon)SERT (Sodium-dependent serotonin transporter)

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