Table 7.

Potential drug–drug interaction risks with the NK₁-receptor antagonists aprepitant, netupitant, and rolapitant

	Aprepitant	Netupitant	Rolapitant
CYP enzymes	3A4, 1A2, 2C9	3A4	2D6
Mechanism	Inhibitor of 3A4 and substrate for 3A4 and inducer of 3A4 and 2C9	Inhibitor of 3A4 and substrate for 3A4	Inhibitor of 2D6 and of BCRP
No DI risk	IV vinorelbine, docetaxel, cyclophosphamide, ondansetron, granisetron, palonosetron, digoxin	Palonosetron, digoxin, docetaxel, etoposide, cyclophosphamide, digoxin	Dexamethasone, ranitidine, ondansetron, metoclopramide, doxorubicin, epirubicin, irinotecan, topotecan, docetaxel, 5-FU, etoposide, methotrexate, ketoconazole, midazolam
PDI risks	Dexamethasone, methylprednisolone, warfarin, oral contraceptives, midazolam, tolbutamid, ifosfamide, ritonavir clarithromycin, itraconazole, phenytoin rifampicin, phenobarbital, carbamazepine, oxycodone	Dexamethasone, methylprednisolone, oral contraceptives, clarithromycin, erythromycin, itraconazole, ritonavir, rifampicin, carbamazepine, phenytoin, phenobarbital, SSRI, SNRI	Antidepressants, thioridazine, pimozide

BCRP breast cancer resistance protein, CYP cytochrome 450, DI drug–drug interaction, IV intravenously, PDI potential drug–drug interaction, SNRI selective noradrenaline reuptake inhibitor, SSRI selective serotonin reuptake inhibitor

Bold indicates the primary metabolizing CYP enzyme for each antiemetic agent