Aprepitant and L-758298 -: Antiemetic -: Antidepressant -: Tachykinin Nk1 antagonist

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.