Mechanisms and latest clinical studies of new NK1 receptor antagonists for chemotherapy-induced nausea and vomiting: Rolapitant and NEPA (netupitant/palonosetron)

2015 ◽  
Vol 41 (10) ◽  
pp. 904-913 ◽  
Author(s):  
Camilo Rojas ◽  
Barbara S. Slusher
Keyword(s):  
Clinical Studies ◽  
Nausea And Vomiting ◽  
Nk1 Receptor ◽  
Receptor Antagonists ◽  
Nk1 Receptor Antagonists

scholarly journals Investigating racial disparities in use of NK1 receptor antagonists to prevent chemotherapy-induced nausea and vomiting among women with breast cancer

2016 ◽  
Vol 156 (2) ◽  
pp. 351-359 ◽  
Author(s):  
Devon K. Check ◽  
Katherine E. Reeder-Hayes ◽  
Ethan M. Basch ◽  
Leah L. Zullig ◽  
Morris Weinberger ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Racial Disparities ◽  
Nausea And Vomiting ◽  
Nk1 Receptor ◽  
Receptor Antagonists ◽  
Nk1 Receptor Antagonists

NK1 receptor antagonists for the prevention of chemotherapy-induced nausea and vomiting: An updated meta-analysis.

2013 ◽  
Vol 31 (15_suppl) ◽  
pp. e20506-e20506
Author(s):  
Lucas Vieira dos Santos ◽  
Andre Tesainer Brunetto ◽  
Andre Deeke Sasse ◽  
Fabiano Hahn Souza ◽  
Joao Paulo Lima
Keyword(s):  
Infection Rate ◽  
Safety Issue ◽  
Rescue Therapy ◽  
Meta Analysis ◽  
Severe Infection ◽  
Complete Response ◽  
Nausea And Vomiting ◽  
Nk1 Receptor ◽  
Receptor Antagonists ◽  
Nk1 Receptor Antagonists

e20506 Background: We have previously shown (dos Santos JNCI 2012) that NK1 receptor antagonists (NK1RA), such as aprepitant and casopitant, improve chemotherapy-induced nausea and vomiting (CINV) at the cost of increasing severe infection risk. Herein, we update our results. Methods: We searched MEDLINE, EMBASE, CENTRAL and meeting proceedings to identify randomized controlled trials (RCTs) comparing standard antiemetic therapy (dexamethasone + 5-HT3R inhibitors) versus NK1RA plus standard therapy for CINV prevention. Complete response (CR) was defined as absence of emesis and rescue therapy. The endpoints were CR post-chemotherapy in the overall phase (first 120 hours), CR in the acute phase (first 24 hours), and the delayed phase (24–120 hours), nausea, and toxicity. Subgroup analyses evaluated the type of NK1RA, the emetogenic potential of the chemotherapy, and prolonged use of 5-HT3R inhibitor. Odds ratios (ORs) and 95% confidence intervals (CIs) were calculated using a random-effects model. Results: A total of 20 trials (9,935 patients) were included. NK1RA increased CR rate and nausea in all phases and subgroups. The CR in overall phase improved from 56% to 72% (OR = 0.52, 95% CI = 0.46 to 0.59, P < .00001, NNT=6). The side effects of NK1RA followed our previous report: the severe infection rate increased from 2.4% to 5.6% in the NK1RA group (four trials, 1656 patients; OR = 2.87; 95% CI = 1.58 to 5.19, P = .0005, NNH=31). Conclusions: NK1RA consistently improve CINV control in the acute, delayed, and overall phases, either for moderately or highly emetogenic chemotherapy regimens. Their use might be associated with increased infection rate, and a patient-level meta-analysis is warranted to clarify this safety issue.

Current Trends and Future Directions in the Management of Delayed Nausea and Vomiting

2013 ◽  
Vol 09 (02) ◽  
pp. 84
Author(s):  
Bernardo L Rapoport ◽  
Georgia S Demetriou ◽  
◽  
Keyword(s):  
Single Dose ◽  
Receptor Occupancy ◽  
Nausea And Vomiting ◽  
Nk1 Receptor ◽  
Binding Studies ◽  
Receptor Antagonists ◽  
Novel Approach ◽  
Delayed Nausea ◽  
Neurokinin 1 ◽  
Nk1 Receptor Antagonists

The prophylaxis of chemotherapy-induced nausea and vomiting benefited greatly from the introduction of neurokinin-1 (NK1) receptor antagonists (RAs). Current emesis guidelines recommend that NK1 receptor antagonists be combined with 5-HT3 receptor antagonists and dexamethasone for highly emetic chemotherapy and moderately emetic chemotherapy. The first such medication, aprepitant, was approved in the US in 2003. Fosaprepitant, an intravenous prodrug of aprepitant, is also available as a single dose on day 1 in combination with other antiemetics. Fosaprepitant is rapidly converted to the active aprepitant and exhibits a similar half-life to orally administered aprepitant. In addition, receptor-binding studies have shown aprepitant striatal NK1 receptor occupancy of 90 % for over 48 hours after exposure. These characteristics may allow aprepitant, fosaprepitant and the newer NK1 RAs to be administered in a single dose on day 1. Olanzapine may prove to be a novel approach in the treatment of CINV, particularly in the management of nausea.

Discovery of orally bioavailable NK1 receptor antagonists

2003 ◽  
Vol 13 (3) ◽  
pp. 437-442 ◽  
Author(s):  
C. Genicot ◽  
B. Christophe ◽  
P. Collart ◽  
M. Gillard ◽  
L. Goossens ◽  
...  
Keyword(s):  
Nk1 Receptor ◽  
Receptor Antagonists ◽  
Orally Bioavailable ◽  
Nk1 Receptor Antagonists

Oral anti-hyperalgesic and anti-inflammatory activity of NK1 receptor antagonists in models of inflammatory hyperalgesia of the guinea-pig

Pain ◽  
2000 ◽  
Vol 87 (3) ◽  
pp. 253-263 ◽  
Author(s):  
Elizabeth A. Campbell ◽  
Clive Gentry ◽  
Sadhana Patel ◽  
Bruce Kidd ◽  
Simon Cruwys ◽  
...  
Keyword(s):  
Guinea Pig ◽  
Inflammatory Activity ◽  
Nk1 Receptor ◽  
Receptor Antagonists ◽  
Inflammatory Hyperalgesia ◽  
Anti Inflammatory ◽  
Nk1 Receptor Antagonists

Bioactive conformations of peptides and mimetics as milestones in drug design: Investigation of NK1 receptor antagonists

1995 ◽  
Vol 2 (3-4) ◽  
pp. 125-134 ◽  
Author(s):  
Solo Goldstein ◽  
Michel Neuwels ◽  
Florence Moureau ◽  
Didier Berckmans ◽  
Marie-Agn�s Lassoie ◽  
...  
Keyword(s):  
Drug Design ◽  
Nk1 Receptor ◽  
Receptor Antagonists ◽  
Nk1 Receptor Antagonists

The site of the anti-emetic action of tachykinin NK1 receptor antagonists may exist in the medullary area adjacent to the semicompact part of the nucleus ambiguus

1999 ◽  
Vol 818 (2) ◽  
pp. 439-449 ◽  
Author(s):  
Hiroyuki Fukuda ◽  
Emi Nakamura ◽  
Tomoshige Koga ◽  
Naohiro Furukawa ◽  
Yasuteru Shiroshita
Keyword(s):  
Nucleus Ambiguus ◽  
Nk1 Receptor ◽  
Receptor Antagonists ◽  
Nk1 Receptor Antagonists
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