eribulin + ketoconazole

Eribulin is a synthetic analog of halichondrin B derived from the marine sponge Halichondria okadai. It is a non-taxane microtubule dynamics inhibitor that acts by inhibiting the growth phase of microtubules without affecting their shortening phase and sequesters tubulin into nonproductive aggregates. This leads to G2/M cell-cycle block, disruption of mitotic spindles, and ultimately apoptotic cell death after prolonged mitotic blockage. Eribulin is primarily indicated for metastatic breast cancer in patients who have previously received at least two chemotherapeutic regimens and for metastatic or unresectable liposarcoma[4][5][6][8]. Ketoconazole is a broad-spectrum antifungal agent used to treat seborrheic dermatitis and various fungal skin infections. It works mainly by inhibiting fungal cytochrome P450 enzymes involved in ergosterol synthesis[1][2]. Ketoconazole can also inhibit human CYP3A4 enzyme activity. The combination "eribulin + ketoconazole" refers to co-administration rather than a fixed-dose combination product; it may be relevant due to potential drug-drug interactions (e.g., ketoconazole as a strong CYP3A4 inhibitor could affect the pharmacokinetics of drugs metabolized by this pathway).

Brand names

NAT-eriBULin

Other names

eribulin mesylate