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Antiemetic Studies on the NK1 Receptor Antagonist Aprepitant

John P. Stoutenburg and Harry Raftopoulos

-acting morpholine acetal human NK-1 receptor antagonist . J Med Chem 1998 ; 41 : 4607 – 4614 . 24 Blum RA Majumdar A McCrea J : Effects of aprepitant on the pharmacokinetics of ondansetron and granisetron in healthy subjects . Clin Ther 2003 ; 25

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BPI20-019: Pooled Analysis of Phase 3 Studies Comparing a Single-Dose Fixed Combination of Netupitant / Palonosetron (NEPA) vs a 3-Day Aprepitant-Based Regimen (APR) for Prevention of Chemotherapy-Induced Nausea and Vomiting (CINV) in Patients Receiving Highly Emetogenic Chemotherapy (HEC)

Rudolph M. Navari, Erminio Bonizzoni, Rita Wickham, and Rebecca Clark-Snow

. In the clinical development program of NEPA, 3 HEC (cisplatin-based) registration studies included an NK 1 RA (aprepitant; APR) + 5-HT 3 RA + DEX arm. This post-hoc analysis evaluated the efficacy of NEPA versus APR across the cisplatin trials

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Use of Acupuncture in the Control of Chemotherapy-Induced Nausea and Vomiting

Ting Bao

. J Clin Oncol 2005 ; 23 : 1289 – 1294 . 17 Hesketh PJ Grunberg SM Gralla RJ . The oral neurokinin-1 antagonist aprepitant for the prevention of chemotherapy-induced nausea and vomiting: a multinational, randomized, double-blind, placebo

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Prevention of Emesis from Multiple-Day and High-Dose Chemotherapy Regimens

Rudolph M. Navari

-induced emesis by a selective neurokin-1-receptor antagonist . L-754,030 Antiemetic Trials Group . N Engl J Med 1999 ; 340 : 190 – 195 . 60. Chawla SP Grunberg SM Gralla RJ . Establishing the dose of the oral NK1 antagonist aprepitant for

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Ten-Year Trends in Antiemetic Prescribing in Patients Receiving Highly Emetogenic Chemotherapy

Ciara C. O'Sullivan, Holly K. Van Houten, Lindsey R. Sangaralingham, Alexis D. Leal, Shivani Shinde, Hongfang Liu, David Ettinger, Charles L. Loprinzi, and Kathryn J. Ruddy

. The combination of palonosetron and glucocorticoids has resulted in superior control of delayed emesis compared with glucocorticoids combined with first-generation 5-HT3RAs. 6 , 7 The subsequent approval of the NK1RAs (initially oral aprepitant [2003

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Cannabinoids in the Treatment of Chemotherapy-Induced Nausea and Vomiting

Barbara Todaro

after chemotherapy treatment. Acute CINV is managed through prevention using a 2 or 3 drug combination. Delayed CINV is prevented with effective treatment of acute CINV and the addition of aprepitant to the antiemetic regimen. Palonosetron, a new

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Are All 5-HT3 Receptor Antagonists the Same?

Robert McNulty

The 5-hydroxytryptamine type 3 (5-HT3) receptor antagonists have become the cornerstone for preventing and treating chemotherapy-induced nausea and vomiting. Four 5-HT3 antagonists are commercially available in the United States, and numerous reports have been published comparing 2 or more agents. The studies ranged from randomized, double-blinded to open-label or retrospective trials; included chemotherapy-naïve and –non-naïve patients; and covered a range of doses and routes of administration with and without concomitant steroids, for preventing and treating nausea and vomiting after highly and moderately high emetogenic chemotherapy. With few exceptions, the studies uniformly show an equivalent efficacy rate and side effect profile among the various agents at equivalent doses. This article reviews the pharmacology of the class for insight into minor differences among the agents that could possibly influence drug selection for certain patients, and considers data on the absorption, half-life, metabolism, and receptor activity. Clinical trials support the claim of various guidelines that the 5-HT3 receptor antagonists are therapeutically similar in safety and efficacy, particularly because the current best practice for preventing nausea and vomiting after highly and moderately high emetogenic chemotherapy is a combination of a 5-HT3 antagonist, steroids, and aprepitant.

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Antiemesis

David S. Ettinger, Debra K. Armstrong, Sally Barbour, Michael J. Berger, Philip J. Bierman, Bob Bradbury, Georgianna Ellis, Steve Kirkegaard, Dwight D. Kloth, Mark G. Kris, Dean Lim, Laura Boehnke Michaud, Lida Nabati, Kim Noonan, Hope S. Rugo, Darby Siler, Steven M. Sorscher, Sundae Stelts, Lisa Stucky-Marshall, Barbara Todaro, and Susan G. Urba

Intravenous palonosetron seems to be effective for preventing both delayed and acute emesis. NK-1 Receptor Antagonist Aprepitant selectively blocks the binding of substance P at the NK-1 receptor in the central nervous system. Thus, aprepitant provides

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Antiemesis

David S. Ettinger, Debra K. Armstrong, Sally Barbour, Michael J. Berger, Philip J. Bierman, Bob Bradbury, Georgianna Ellis, Steve Kirkegaard, Dwight D. Kloth, Mark G. Kris, Dean Lim, Michael Anne Markiewicz, Lida Nabati, Carli Nesheiwat, Hope S. Rugo, Steven M. Sorscher, Lisa Stucky-Marshal, Barbara Todaro, and Susan Urba

trials [Abstract] . J Clin Oncol 2004 ; 22 : Abstract 6037 . 73 Chawla SP Grunberg SM Gralla RJ . Establishing the dose of the oral NK1 antagonist aprepitant for the prevention of chemotherapy-induced nausea and vomiting . Cancer 2003

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Antiemetic Guidelines: Not Just for the HEC of It

Kelsey A. Klute

-model–guided approach to adding aprepitant with or without olanzapine to dexamethasone and a serotonin type-3 receptor antagonist in patients receiving AC for early-stage breast cancer, the risk-model–guided approach was more effective than physician antiemetic choice