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Drugs Fut 2002, 27(3): 211
ISSN 0377-8282
Copyright 2002 Prous Science
CCC: 0377-8282
DOI: 10.1358/dof.2002.027.03.661047		 
 
Aprepitant and L-758298
Sorbera, L.A., Castaner, J., Bayes, M., Silvestre, J.		 
 
Despite recent progress in the development of better tolerated and more effective treatments for controlling chemotherapy-induced nausea and vomiting, emesis continues to be problematic for many patients receiving chemotherapy. A new class of antiemetics that are nonpeptide antagonists to the tachykinin neurokinin NK1 receptor (the substance P receptor) have emerged as potential candidates for antiemetic therapy as well as other widespread therapeutic applications. One such compound, aprepitant and its prodrug (L-758298), have demonstrated an excellent preclinical and clinical ability to antagonize the emetic effects of a number of stimuli, including chemotherapy agents such as cisplatin. The agent has also shown promise in preclinical and clinical studies of depression and anxiety.


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