Aprepitant--a novel NK1-receptor antagonist. 2003

Lisa Patel, and Celeste Lindley
Division of Pharmacotherapy, School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.

Recently, a new class of agents, the substance P antagonists, has heralded a novel approach for the control of emesis. Aprepitant (Emend, Merck & Co., Inc.), the first of this class, was recently approved by the FDA for the prevention of both acute and delayed chemotherapy-induced nausea and vomiting (CINV). Of interest is the vast array of processes in which substance P is involved such as pain, anxiety, depression and inflammation and the potential wide applicability of substance P antagonists to a number of medical conditions outside of the nausea and vomiting realm. The following review provides an overview of aprepitant including pharmacokinetics, pharmacology and clinical evidence for its use in CINV. A brief discussion of other possible indications for aprepitant will also be presented.

UI MeSH Term Description Entries
D009025 Morpholines Tetrahydro-1,4-Oxazines,Tetrahydro 1,4 Oxazines
D009325 Nausea An unpleasant sensation in the stomach usually accompanied by the urge to vomit. Common causes are early pregnancy, sea and motion sickness, emotional stress, intense pain, food poisoning, and various enteroviruses.
D002986 Clinical Trials as Topic Works about pre-planned studies of the safety, efficacy, or optimum dosage schedule (if appropriate) of one or more diagnostic, therapeutic, or prophylactic drugs, devices, or techniques selected according to predetermined criteria of eligibility and observed for predefined evidence of favorable and unfavorable effects. This concept includes clinical trials conducted both in the U.S. and in other countries. Clinical Trial as Topic
D004347 Drug Interactions The action of a drug that may affect the activity, metabolism, or toxicity of another drug. Drug Interaction,Interaction, Drug,Interactions, Drug
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000077608 Aprepitant A morpholine neurokinin-1 (NK1) receptor antagonist that is used in the management of nausea and vomiting caused by DRUG THERAPY, and for the prevention of POSTOPERATIVE NAUSEA AND VOMITING. (1-(3,5-bis(Trifluoromethyl)phenyl)ethoxy)-3-(fluoro)phenyl-4-(3-oxo-1,2,4-triazol-5-yl)methylmorpholine,(2R)-(1R)-3,5-bis(Trifluoromethylphenyl)ethoxy)-(3S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazole)methyl-morpholine,Emend,L 754,030,L 754030,L-754,030,L-754030,MK 0517,MK 0869,MK 869,MK-0517,MK-0869,MK-869,MK0517,L754,030,L754030,MK0869,MK869
D000932 Antiemetics Drugs used to prevent NAUSEA or VOMITING. Anti-emetic,Antiemetic,Antiemetic Agent,Antiemetic Drug,Anti-Emetic Effect,Anti-Emetic Effects,Anti-emetics,Antiemetic Agents,Antiemetic Drugs,Antiemetic Effect,Antiemetic Effects,Agent, Antiemetic,Agents, Antiemetic,Anti Emetic Effect,Anti Emetic Effects,Anti emetic,Anti emetics,Drug, Antiemetic,Drugs, Antiemetic,Effect, Anti-Emetic,Effect, Antiemetic,Effects, Anti-Emetic,Effects, Antiemetic
D000970 Antineoplastic Agents Substances that inhibit or prevent the proliferation of NEOPLASMS. Anticancer Agent,Antineoplastic,Antineoplastic Agent,Antineoplastic Drug,Antitumor Agent,Antitumor Drug,Cancer Chemotherapy Agent,Cancer Chemotherapy Drug,Anticancer Agents,Antineoplastic Drugs,Antineoplastics,Antitumor Agents,Antitumor Drugs,Cancer Chemotherapy Agents,Cancer Chemotherapy Drugs,Chemotherapeutic Anticancer Agents,Chemotherapeutic Anticancer Drug,Agent, Anticancer,Agent, Antineoplastic,Agent, Antitumor,Agent, Cancer Chemotherapy,Agents, Anticancer,Agents, Antineoplastic,Agents, Antitumor,Agents, Cancer Chemotherapy,Agents, Chemotherapeutic Anticancer,Chemotherapy Agent, Cancer,Chemotherapy Agents, Cancer,Chemotherapy Drug, Cancer,Chemotherapy Drugs, Cancer,Drug, Antineoplastic,Drug, Antitumor,Drug, Cancer Chemotherapy,Drug, Chemotherapeutic Anticancer,Drugs, Antineoplastic,Drugs, Antitumor,Drugs, Cancer Chemotherapy
D014839 Vomiting The forcible expulsion of the contents of the STOMACH through the MOUTH. Emesis
D064729 Neurokinin-1 Receptor Antagonists Compounds that inhibit or block the activity of NEUROKININ-1 RECEPTORS. Neurokinin 1 Receptor Antagonist,Neurokinin-1 Receptor Antagonist,Neurokinin-1 Receptor Blocker,Neuroleukin-1 Receptor Blocker,Substance P Receptor Antagonist,Substance P Receptor Blocker,Tachykinin Receptor 1 Antagonist,Tachykinin Receptor 1 Blocker,Neurokinin-1 Receptor Blockers,Neuroleukin-1 Receptor Blockers,Substance P Receptor Antagonists,Substance P Receptor Blockers,Tachykinin Receptor 1 Antagonists,Tachykinin Receptor 1 Blockers,Antagonist, Neurokinin-1 Receptor,Antagonists, Neurokinin-1 Receptor,Blocker, Neurokinin-1 Receptor,Blocker, Neuroleukin-1 Receptor,Blockers, Neurokinin-1 Receptor,Blockers, Neuroleukin-1 Receptor,Neurokinin 1 Receptor Antagonists,Neurokinin 1 Receptor Blocker,Neurokinin 1 Receptor Blockers,Neuroleukin 1 Receptor Blocker,Neuroleukin 1 Receptor Blockers,Receptor Antagonist, Neurokinin-1,Receptor Antagonists, Neurokinin-1,Receptor Blocker, Neurokinin-1,Receptor Blocker, Neuroleukin-1,Receptor Blockers, Neurokinin-1,Receptor Blockers, Neuroleukin-1

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