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Aprepitant

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https://www.readbyqxmd.com/read/29130344/neurokinin-1-receptor-antagonists-in-the-prevention-of-chemotherapy-induced-nausea-and-vomiting-focus-on-fosaprepitant
#1
Bernardo L Rapoport, Karin Jordan, Cindy Weinstein
Chemotherapy-induced nausea and vomiting (CINV) remains a challenge in cancer care. Improved understanding of CINV pathophysiology has triggered the development of new antiemetic therapeutic options, such as selective neurokinin-1 (NK1) receptor antagonists (RAs), which effectively prevent CINV when added to a standard antiemetic regimen (serotonin-3 RA and dexamethasone). Aprepitant and its water-soluble prodrug, fosaprepitant dimeglumine, are the most widely used NK1 RAs, with extensive clinical use worldwide...
November 13, 2017: Future Oncology
https://www.readbyqxmd.com/read/29111115/aprepitant-has-mixed-effects-on-nausea-and-reduces-other-symptoms-in-patients-with-gastroparesis-and-related-disorders
#2
Pankaj J Pasricha, Katherine P Yates, Irene Sarosiek, Richard W McCallum, Thomas L Abell, Kenneth L Koch, Linda Anh B Nguyen, William J Snape, William L Hasler, John O Clarke, Sameer Dhalla, Ellen M Stein, Linda A Lee, Laura A Miriel, Mark L Van Natta, Madhusudan Grover, Gianrico Farrugia, James Tonascia, Frank A Hamilton, Henry P Parkman
BACKGROUND & AIMS: There are few effective treatments for nausea and other symptoms in patients with gastroparesis and related syndromes. We performed a randomized trial of the ability of the neurokinin-1 receptor antagonist aprepitant to reduce symptoms in patients with chronic nausea and vomiting due to gastroparesis or gastroparesis-like syndrome. METHODS: We conducted a 4-week multicenter, double-masked trial of 126 patients with at leastmoderate symptoms of chronic nausea and vomiting of presumed gastric origin for at least 6 months...
October 27, 2017: Gastroenterology
https://www.readbyqxmd.com/read/29092012/a-randomized-phase-3-study-evaluating-the-efficacy-of-single-dose-nepa-a-fixed-antiemetic-combination-of-netupitant-and-palonosetron-versus-an-aprepitant-regimen-for-prevention-of-chemotherapy-induced-nausea-and-vomiting-cinv-in-patients-receiving-highly-emetogenic
#3
L Zhang, S Lu, J Feng, A Dechaphunkul, J Chang, D Wang, S Chessari, C Lanzarotti, K Jordan, M Aapro
Background: Co-administration of multiple antiemetics that inhibit several molecular pathways involved in emesis is required to optimize CINV control in patients receiving highly emetogenic chemotherapy (HEC). NEPA, a fixed combination of a highly selective NK1 receptor antagonist (RA), netupitant (300 mg), and the pharmacologically distinct 5-HT3RA, palonosetron (PALO 0.50 mg), has shown superior CINV prevention compared to PALO in cisplatin and anthracycline/cyclophosphamide-based settings...
October 28, 2017: Annals of Oncology: Official Journal of the European Society for Medical Oncology
https://www.readbyqxmd.com/read/29090385/phase-ii-open-label-pilot-trial-of-aprepitant-and-palonosetron-for-the-prevention-of-chemotherapy-induced-nausea-and-vomiting-cinv-in-patients-receiving-moderately-emetogenic-folfox-chemotherapy-for-the-treatment-of-colorectal-cancer
#4
Joseph S Bubalo, Jon D Herrington, Marc Takemoto, Patricia Willman, Michael S Edwards, Casey Williams, Alan Fisher, Alison Palumbo, Eric Chen, Charles Blanke, Charles D Lopez
PURPOSE: Chemotherapy-induced nausea and vomiting (CINV) causes significant morbidity among colorectal cancer patients, receiving fluorouracil, oxaliplatin, and leucovorin (FOLFOX) chemotherapy even with standard antiemetic prophylaxis. The purpose of this study is to determine if the addition of aprepitant to standard antiemetic therapy improves CINV in these patients. METHODS: Patients receiving FOLFOX for colorectal cancer were given antiemetic prophylaxis with aprepitant 125 mg orally on day 1 and 80 mg on days 2 and 3...
October 31, 2017: Supportive Care in Cancer: Official Journal of the Multinational Association of Supportive Care in Cancer
https://www.readbyqxmd.com/read/29075004/from-receptor-binding-kinetics-to-signal-transduction-a-missing-link-in-predicting-in-vivo-drug-action
#5
Indira Nederpelt, Maria Kuzikov, Wilbert E A de Witte, Patrick Schnider, Bruno Tuijt, Sheraz Gul, Adriaan P IJzerman, Elizabeth C M de Lange, Laura H Heitman
An important question in drug discovery is how to overcome the significant challenge of high drug attrition rates due to lack of efficacy and safety. A missing link in the understanding of determinants for drug efficacy is the relation between drug-target binding kinetics and signal transduction, particularly in the physiological context of (multiple) endogenous ligands. We hypothesized that the kinetic binding parameters of both drug and endogenous ligand play a crucial role in determining cellular responses, using the NK1 receptor as a model system...
October 26, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29061362/efficacy-of-aprepitant-for-chop-chemotherapy-induced-nausea-vomiting-and-anorexia
#6
Mihoko Morita, Shinji Kishi, Miyuki Ookura, Yasufumi Matsuda, Katsunori Tai, Takahiro Yamauchi, Takanori Ueda
The objective of this study was to evaluate whether aprepitant in addition to 5-HT3 receptor antagonist is useful for preventing chemotherapy-induced nausea and vomiting (CINV) and anorexia in patients receiving CHOP therapy, and to evaluate the relationship between in vivo kinetics of plasma substance P and these adverse events. Patients with malignant lymphoma who received CHOP chemotherapy or THP (THP-ADR)-COP therapy were investigated for CINV and anorexia for 5 days after the start of chemotherapy. With the first course of chemotherapy, all patients received only granisetron on day1 as an antiemetic...
September 23, 2017: Current Problems in Cancer
https://www.readbyqxmd.com/read/29057261/aprepitant-for-the-treatment-of-chronic-refractory-pruritus
#7
REVIEW
Alice He, Jihad M Alhariri, Ronald J Sweren, Madan M Kwatra, Shawn G Kwatra
Chronic pruritus is a difficult condition to treat and is associated with several comorbidities, including insomnia, depression, and decreased quality of life. Treatment for chronic itch includes corticosteroids, antihistamines, and systemic therapies such as naltrexone, gabapentin, UV light therapy, and immunomodulatory treatments, including azathioprine, methotrexate, and cellcept. However, some patients still remain refractory to conventional therapy. Aprepitant is a neurokinin-1 receptor antagonist approved for the prevention of chemotherapy-induced and postoperative nausea and vomiting (CINV, PONV)...
2017: BioMed Research International
https://www.readbyqxmd.com/read/29056150/substance-p-and-the-neurokinin-1-receptor-the-new-crf
#8
Jesse R Schank, Markus Heilig
Substance P (SP) is an 11-amino acid neuropeptide of the tachykinin family that preferentially activates the neurokinin-1 receptor (NK1R). First isolated 85 years ago and sequenced 40 years later, SP has been extensively studied. Early studies identified a role for SP and the NK1R in contraction of intestinal smooth muscle, central pain processing, and neurogenic inflammation. An FDA-approved NK1R antagonist, aprepitant, is used clinically for the treatment of chemotherapy-induced nausea, as the NK1R influences the activity of the brain stem emesis centers...
2017: International Review of Neurobiology
https://www.readbyqxmd.com/read/29043811/investigation-of-the-intra-and-interlaboratory-reproducibility-of-a-small-scale-standardized-supersaturation-and-precipitation-method
#9
Jakob Plum, Cecilie M Madsen, Alexandra Teleki, Jan Bevernage, Claudia da Costa Mathews, Eva M Karlsson, Sara Carlert, Rene Holm, Thomas Müller, Wayne Matthews, Alice Sayers, Krista Ojala, Konstantin Tsinsman, Ram Lingamaneni, Christel As Bergström, Thomas Rades, Anette Müllertz
The high number of poorly water-soluble compounds in drug development has increased the need for enabling formulations to improve oral bioavailability. One frequently applied approach is to induce supersaturation at the absorptive site, e.g., the small intestine, increasing the amount of dissolved compound available for absorption. However, due to the stochastic nature of nucleation, supersaturating drug delivery systems may lead to inter- and intrapersonal variability. The ability to define a feasible range with respect to the supersaturation level is a crucial factor for a successful formulation...
November 7, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29039073/a-double-blind-randomized-phase-ii-dose-finding-study-of-olanzapine-10%C3%A2-mg-or-5%C3%A2-mg-for-the-prophylaxis-of-emesis-induced-by-highly-emetogenic-cisplatin-based-chemotherapy
#10
Takako Yanai, Satoru Iwasa, Hironobu Hashimoto, Fumiyoshi Ohyanagi, Tomomi Takiguchi, Koji Takeda, Masahiko Nakao, Hiroshi Sakai, Toshiaki Nakayama, Koichi Minato, Takahiro Arai, Kenichi Suzuki, Yasuhiro Shimada, Kengo Nagashima, Hiroyuki Terakado, Noboru Yamamoto
PURPOSE: The aim of this phase II study was to evaluate the efficacy and safety of two doses (10 and 5 mg) of olanzapine in combination with standard antiemetic treatment (aprepitant, palonosetron, and dexamethasone) for patients receiving highly emetogenic chemotherapy (HEC). METHODS: A multi-institutional, double-blind, randomized phase II, dose-finding study of olanzapine was performed in patients with a malignant solid tumor who were receiving HEC with cisplatin (≥ 50 mg/m(2))...
October 16, 2017: International Journal of Clinical Oncology
https://www.readbyqxmd.com/read/29031010/evaluation-of-aprepitant-for-acute-chemotherapy-induced-nausea-and-vomiting-in-children-and-adolescents-with-acute-lymphoblastic-leukemia-receiving-high-dose-methotrexate
#11
Femi Felix-Ukwu, Kate Reichert, M Brooke Bernhardt, Eric S Schafer, Amanda Berger
BACKGROUND: Chemotherapy-induced nausea and vomiting (CINV) negatively impacts patients' quality of life. The emetogenicity of high-dose methotrexate in children and adolescents with cancer is incompletely characterized. At our institution, a number of patients with acute lymphoblastic leukemia (ALL) have received aprepitant with courses of high-dose methotrexate after poor CINV control with prior courses. PROCEDURE: We conducted a retrospective cohort analysis on patients with ALL who received methotrexate 5 g/m(2) /dose with and without concomitant aprepitant at Texas...
October 14, 2017: Pediatric Blood & Cancer
https://www.readbyqxmd.com/read/29022160/a-catalyst-from-burkholderia-cenocepacia-for-efficient-anti-prelog-s-bioreduction-of-3-5-bis-trifluoromethyl-acetophenone
#12
Songzhu Yu, Hongxia Li, Yan Lu, Guojun Zheng
(R)-3, 5-Bis(trifluoromethyl)phenyl ethanol is a key chiral intermediate for the synthesis of aprepitant. Through a genome mining approach, an NADPH-dependent short-chain dehydrogenases derived from Burkholderia cenocepacia (Bc-SDR) was discovered with excellent anti-Prelog's stereoselectivity of reducing 3, 5-bis(trifluoromethyl) acetophenone. The enzyme with 247 amino acids was successfully expressed in Escherichia coli and the molecular weight was about 26 kDa. Optimization of reaction conditions showed that the optimum temperature and pH of the enzyme was 25 °C and pH 7...
October 12, 2017: Applied Biochemistry and Biotechnology
https://www.readbyqxmd.com/read/28987539/statistical-investigation-of-the-full-concentration-range-of-fasted-and-fed-simulated-intestinal-fluid-on-the-equilibrium-solubility-of-oral-drugs
#13
Jeremy Perrier, Zhou Zhou, Claire Dunn, Ibrahim Khadra, Clive G Wilson, Gavin Halbert
Upon oral administration the solubility of a drug in intestinal fluid is a key property influencing bioavailability. It is also recognised that simple aqueous solubility does not reflect intestinal solubility and to optimise in vitro investigations simulated intestinal media systems have been developed. Simulated intestinal media which can mimic either the fasted or fed state consists of multiple components each of which either singly or in combination may influence drug solubility, a property that can be investigated by a statistical design of experiment technique...
October 5, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28986196/effect-of-composition-of-simulated-intestinal-media-on-the-solubility-of-poorly-soluble-compounds-investigated-by-design-of-experiments
#14
Cecilie Maria Madsen, Kung-I Feng, Andrew Leithead, Nicole Canfield, Søren Astrup Jørgensen, Anette Müllertz, Thomas Rades
The composition of the human intestinal fluids varies both intra- and inter-individually. This will influence the solubility of orally administered drug compounds, and hence, the absorption and efficacy of compounds displaying solubility limited absorption. The purpose of this study was to assess the influence of simulated intestinal fluid (SIF) composition on the solubility of poorly soluble compounds. Using a Design of Experiments (DoE) approach, a set of 24 SIF was defined within the known compositions of human fasted state intestinal fluid...
October 3, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28980185/development-of-a-new-aprepitant-liquisolid-formulation-with-the-aid-of-artificial-neural-networks-and-genetic-programming
#15
Panagiotis Barmpalexis, Agni Grypioti, Georgios K Eleftheriadis, Dimitris G Fatouros
In the present study, liquisolid formulations were developed for improving dissolution profile of aprepitant (APT) in a solid dosage form. Experimental studies were complemented with artificial neural networks and genetic programming. Specifically, the type and concentration of liquid vehicle was evaluated through saturation-solubility studies, while the effect of the amount of viscosity increasing agent (HPMC), the type of wetting (Soluplus® vs. PVP) and solubilizing (Poloxamer®407 vs. Kolliphor®ELP) agents, and the ratio of solid coating (microcrystalline cellulose) to carrier (colloidal silicon dioxide) were evaluated based on in vitro drug release studies...
October 4, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28978797/antiinflammatory-effects-of-aprepitant-coadministration-with-cart-regimen-containing-ritonavir-in-hiv-infected-adults
#16
Sergei Spitsin, Pablo Tebas, Jeffrey S Barrett, Vasiliki Pappa, Deborah Kim, Deanne Taylor, Dwight L Evans, Steven D Douglas
BACKGROUND: HIV-infected individuals, even well controlled with combined antiretroviral therapy (cART), have systemic inflammation and comorbidities. Substance P (SP) is an undecapeptide, which mediates neurotransmission and inflammation through its cognate neurokinin 1 receptor (NK1R). Plasma SP levels are elevated in HIV-infected individuals. The FDA-approved antiemetic aprepitant, an NK1R antagonist, has anti-HIV effects and antiinflammatory actions. We evaluated the safety, pharmacokinetics, and antiinflammatory properties of aprepitant in HIV-positive individuals receiving cART...
October 5, 2017: JCI Insight
https://www.readbyqxmd.com/read/28952201/a-phase-ii-randomised-study-to-evaluate-the-efficacy-of-aprepitant-plus-palonosetron-for-preventing-delayed-phase-cinv-associated-with-tc-therapy-in-gynaecological-cancer
#17
Yayoi Sugimori, Tsuyoshi Ota, Takafumi Ujihira, Tomonori Ishiguro, Daiki Ogishima
AIM: Chemotherapy-induced nausea and vomiting (CINV) is one of the most frequently encountered side effects of cancer treatment. Severe CINV can lead patients to refuse chemotherapy, which ultimately affects cancer outcomes. The development of fairly new antiemetic agents, 5-hydroxytryptamine-3 receptor antagonists, palonosetron and neurokinin-1 receptor antagonists and aprepitant has reduced the risk and incidence of CINV. In this study, we assessed the efficacy of aprepitant plus palonosetron against palonosetron for CINV in patients receiving moderately emetic cancer chemotherapy (paclitaxel and carboplatin combination [TC] therapy)...
September 2017: Journal of Obstetrics and Gynaecology Research
https://www.readbyqxmd.com/read/28919769/evaluating-the-antiemetic-administration-consistency-to-prevent-chemotherapy-induced-nausea-and-vomiting-with-the-standard-guidelines-a-prospective-observational-study
#18
Afsaneh Vazin, Davood Eslami, Ebrahim Sahebi
Nausea and vomiting (NV) are the most prevalent adverse effects of chemotherapy (CT). This study was conducted to evaluate adherence of the health care team to standard guidelines for antiemetics usage to prevent acute chemotherapy-induced nausea and vomiting (CINV) in a large CT center. A prospective study was performed during an 11-month period on patients receiving CT. A form was designed to collect patients' demographic information and their chemotherapeutic and antiemetic regimen data. The Likert scale was used to measure the effectiveness of the antiemetics in patients...
2017: Therapeutics and Clinical Risk Management
https://www.readbyqxmd.com/read/28919712/recent-developments-in-the-clinical-pharmacology-of-rolapitant-subanalyses-in-specific-populations
#19
REVIEW
Bernardo Leon Rapoport, Matti Aapro, Martin R Chasen, Karin Jordan, Rudolph M Navari, Ian Schnadig, Lee Schwartzberg
Knowledge of the involvement of the neurokinin substance P in emesis has led to the development of the neurokinin-1 receptor antagonists (NK-1 RAs) for control of chemotherapy-induced nausea and vomiting (CINV), in combination with serotonin type 3 receptor antagonists and corticosteroids. The NK-1 RA rolapitant, recently approved in oral formulation, has nanomolar affinity for the NK-1 receptor, as do the other commercially available NK-1 RAs, aprepitant and netupitant. Rolapitant is rapidly absorbed and has a long half-life in comparison to aprepitant and netupitant...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28867732/comparison-between-antiemetic-effects-of-palonosetron-and-granisetron-on-chemotherapy-induced-nausea-and-vomiting-in-japanese-patients-treated-with-r-chop
#20
Mayako Uchida, Yasuo Mori, Tsutomu Nakamura, Koji Kato, Kenjiro Kamezaki, Katsuto Takenaka, Motoaki Shiratsuchi, Kaori Kadoyama, Toshihiro Miyamoto, Koichi Akashi
In the present study, the antiemetic effect of palonosetron, not combined with dexamethasone and aprepitant, on chemotherapy-induced nausea and vomiting was evaluated in patients with malignant lymphoma receiving first-line rituximab, cyclophosphamide, doxorubicin, vincristine, and prednisone (R-CHOP) therapy, and was compared to that of granisetron. A total of 74 patients with non-Hodgkin lymphoma were included in this study (April 2007 to December 2015). Palonosetron (0.75 mg) or granisetron (3 mg) was intravenously administered before R-CHOP therapy...
2017: Biological & Pharmaceutical Bulletin
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