| Title | Novel neurokinin-1 antagonists as antiemetics for the treatment of chemotherapy-induced emesis. | | Author(s) | Reddy GK, Gralla RJ, Hesketh PJ | | Institution | CIG Media Group, LP, Dallas, TX. | | Source | Support Cancer Ther 2006 Apr 1; 3(3):140-2. | | Abstract | Despite significant advances in supportive care in oncology, many patients with cancer still experience chemotherapy- induced nausea and vomiting (CINV). Historically, there were only 3 neurotransmitter receptors (dopamine D2, cannabinoid- 1, and 5-hydroxytryptamine-3) that were the known targets for antiemetic therapy. Major advances in the management of chemotherapy-induced emesis were seen with the introduction of 5-hydroxytryptamine-3 receptor antagonists, which include palonosetron, ondansetron, tropisetron, dolasetron, and granisetron. However, recently, selective inhibitors of substance P have shown promising activity in the management of CINV in patients with cancer. Substance P mediates a number of biologic effects by binding to a specific neuroreceptor, neurokinin-1 (NK-1). Among the NK-1 receptor antagonists, aprepitant has been approved for the treatment of CINV. Currently, several other NK-1 receptor antagonists, including casopitant, vestipitant, netupitant, and SCH619734, are undergoing clinical evaluation for the prevention of CINV in patients with a variety of malignancies. The clinical potential of these novel NK-1 receptor antagonists and their respective ongoing clinical trials for the management of chemotherapy-induced emesis are discussed briefly herein. | | Language | eng | | Pub Type(s) | Journal Article
| | PubMed ID | 18632487 |
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