Aprepitant

This page contains recent news articles, when available, and an overview of Aprepitant but does not offer medical advice. You should contact your physician with regard to any health issues or concerns.

Overview:

Aprepitant (when available)

Pharmacology and use:
Aprepitant, an antiemetic, is a substance P/neurokinin 1 (NK1) receptor antagonist which, in combination with other antiemetic agents, is indicated for the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy. Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors. Aprepitant has little or no affinity for serotonin (5-HT₃), dopamine, and corticosteroid receptors, the targets of existing therapies for chemotherapy-induced nausea and vomiting (CI NV). For the prevention of nausea and vomiting associated with highly emetogenic cancer chemotherapy, including high-dose cisplatin (in combination with other antiemetic agents).

Mechanism Of Action:
Aprepitant has been shown in animal models to inhibit emesis induced by cytotoxic chemotherapeutic agents, such as cisplatin, via central actions. Animal and human Positron Emission Tomography (PET) studies with Aprepitant have shown that it crosses the blood brain barrier and occupies brain NK1 receptors. Animal and human studies show that Aprepitant augments the antiemetic activity of the 5-HT₃-receptor antagonist ondansetron and the corticosteroid ethasone and inhibits both the acute and delayed phases of cisplatin induced emesis.

News Articles on Aprepitant

Elan Corp: First Japanese OK Of Pdt Using Its NanoCrystal  -  ‎Dec 13, 2009‎
Japanese Ministry of Health, Labour and Welfare has approved EMEND or aprepitant for the treatment of cancer chemotherapy-induced nausea and vomiting. ... Wall Street Journal

ADR Report: ADRs Close Up With Oil, Solar Companies Higher  -  ‎Dec 14, 2009‎
...(ELN), said Monday that the Japanese Ministry of Health, Labour and Welfare has approved EMEND, or aprepitant, for the treatment of cancer ... Wall Street Journal

Schering-Plough and Merck & Co., Inc.; Analysis of Agreement Containing ...  -  ‎Nov 10, 2009‎
Merck introduced the first NK1 receptor antagonist, Emend(R) (aprepitant), in 2003, and remains the only firm in the United States with an approved drug in ... Trading Markets (press release)

日 '서바릭스' '�?누비아' 등 신약 대거 승�?�  -  ‎Oct 20, 2009‎
...치료제 '글랙티브'(Glactiv, sitagliptin phosphate hydrate)와 선�?�? 뉴로퀴닌1(NK1) 수용체 길항형 제토제 '�?�멘드'(Emend, aprepitant)가 �?�시�? 승�?��??다. ... 디지틀보사

Brand Names/Synonyms:
Aprepitant is also known by the following brand names and/or synonymsAprepitant; Aprepitant [Usan]; Emend; MK 0869; MK 869

Drug Category:
Aprepitant is categorized under the following by the FDA: Antiemetics; ATC:A04AD12

Dosage Forms:
CAPSULE

Absorption:
The mean absolute oral bioavailability of aprepitant is approximately 60 to 65%.

Interactions:
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Chemical IUPAC Name:
5-[[2-[1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-morpholin-4-yl]methyl]-1,2-dihydro-1,2,4-triazol-3-one

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