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Annals of Oncology

Annals of Oncology

IF: 56.7
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Aprepitant: drug–drug interactions in perspective

Published:1 December 2010 DOI: 10.1093/annonc/mdq149 PMID: 20488873
M.S. Aapro , C.M. Walko

Abstract

The implications of chemotherapeutic drug–drug interactions can be serious and thus need to be addressed. This review concerns the potential interactions of the antiemetic aprepitant, a neurokinin-1 receptor antagonist indicated for use (in Europe) in highly emetogenic chemotherapy and moderately emetogenic chemotherapy (MEC) in combination with a 5-hydroxytryptamine-3 (5-HT3) receptor antagonist and corticosteroids and (in the United States) in combination with other antiemetic agents, for the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy including high-dose cisplatin. When considering use of aprepitant for prevention of chemotherapy-induced nausea and vomiting, its potential drug–drug interaction profile as a moderate inhibitor of cytochrome P-450 isoenzyme 3A4 (CYP3A4) has been a source of concern for some physicians and other health care professionals. We explore in this paper how real those concerns are. Our conclusion is that either no interaction or no clinically relevant interaction exists with chemotherapeutic agents (intravenous cyclophosphamide, docetaxel, intravenous vinorelbine) or 5-HT3 antagonists (granisetron, ondansetron, palonosetron). For relevant interactions, appropriate measures, such as corticosteroid dose modifications and extended International Normalized Ratio monitoring of patients on warfarin therapy, can be taken to effectively manage them. Therefore, the concern of negative interactions remains largely theoretical but needs to be verified with new agents extensively metabolized through the 3A4 pathway.

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Related products
Procduct Name CAS Molecular Formula Supplier Price
Docetaxel 114977-28-5 C43H53NO14 1002 suppliers $27.00-$1750.00
Cisplatin 15663-27-1 Cl2H6N2Pt 921 suppliers $17.00-$7570.00
Aprepitant 170729-80-3 C23H21F7N4O3 668 suppliers $5.00-$3204.00
Cyclophosphamide 50-18-0 C7H15Cl2N2O2P 427 suppliers $35.00-$1005.43
Ondansetron 99614-02-5 C18H19N3O 343 suppliers $10.00-$1509.88
Granisetron 109889-09-0 C18H24N4O 252 suppliers $48.00-$1100.00
Vinorelbine 71486-22-1 C45H54N4O8 248 suppliers $39.00-$2913.80
Warfarin 81-81-2 C19H16O4 227 suppliers $19.00-$2055.90
Palonosetron 135729-61-2 C19H24N2O 78 suppliers $42.00-$1212.75
cytochrome P-450 2A7 10 suppliers Inquiry

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