Aprepitant - CAS 170729-80-3
Catalog number: 170729-80-3
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
Molecular Weight:
Neurokinin Receptor
Aprepitant is a specific NK-1R antagonist, used as an antiemetic agent.
white solid powder
Emend, L-754030; MK-0869; ONO-7436.
Canonical SMILES:
1.Preparation and Characterization of Nanosuspension of Aprepitant by H96 Process.
Kalvakuntla S1, Deshpande M2, Attari Z1, Kunnatur B K1. Adv Pharm Bull. 2016 Mar;6(1):83-90. doi: 10.15171/apb.2016.013. Epub 2016 Mar 17.
PURPOSE: Nanosuspension in drug delivery is known to improve solubility, dissolution and eventually bioavailability of the drugs. The purpose of the study was to compare particle size of nanosuspensions prepared by the first generation approach and H96 approach and to evaluate the effectiveness of H96 approach.
2.Infusion site adverse events in breast cancer patients receiving highly emetic chemotherapy with prophylactic anti-emetic treatment with aprepitant and fosaprepitant: A retrospective comparison.
Tsuda T1, Kyomori C2, Mizukami T1, Taniyama T1, Izawa N1, Horie Y1, Hirakawa M1, Ogura T1, Nakajima TE1, Tsugawa K3, Boku N1. Mol Clin Oncol. 2016 Apr;4(4):603-606. Epub 2016 Feb 5.
The incidences of infusion site adverse events in chemotherapy regimens, including anthracyclines with either fosaprepitant or aprepitant as the anti-emetic, were not highlighted in the randomized trial comparing aprepitant and fosaprepitant. The present retrospective analysis was performed in breast cancer patients receiving anthracycline-containing chemotherapy, a combination of epirubicin and cyclophosphamide with or without 5-fluorouracil as the adjuvant or neoadjuvant, at the outpatient infusion center of St. Marianna University Hospital (Kawasaki, Japan). Infusion site adverse events were retrospectively compared between the 3 months prior to and three months following switching from 3 day oral administration of aprepitant to intravenous infusion of fosaprepitant. A total of 62 patients were included in the aprepitant group and 38 in the fosaprepitant group. Of these patients, 26 (42%) in the aprepitant group and 36 patients (96%) in the fosaprepitant group experienced any grade of infusion site adverse events at least once (P<0.
3.A phase II, randomized study of aprepitant in the prevention of chemotherapy-induced nausea and vomiting associated with moderately emetogenic chemotherapies in colorectal cancer patients.
Aridome K1, Mori SI2, Baba K2, Yanagi M2, Hamanoue M3, Miyazono F4, Tokuda K5, Imamura H6, Ogura Y7, Kaneko K8, Kijima F9, Maemura K2, Ishigami S2, Natsugoe S2. Mol Clin Oncol. 2016 Mar;4(3):393-398. Epub 2015 Dec 31.
The present study aimed to study the efficacy of aprepitant in the prevention of chemotherapy-induced nausea and vomiting (CINV) in patients receiving moderately emetogenic chemotherapy (MEC) for colorectal cancer (CRC), and comprised a multicenter, phase II, open-label, randomized, parallel comparative study conducted as part of the Kagoshima aprepitant study for colon cancer in Japan. Patients with advanced or recurrent CRC were treated with standard MEC regimens (FOLFOX, XELOX or FOLFIRI) and received either standard chemotherapy [5-hydroxytryptamine-3 receptor antagonist (5-HT3RA) + dexamethasone] or aprepitant regimen chemotherapy (5-HT3 RA + reduced-dose dexamethasone + aprepitant). The primary endpoint of the present study was the proportion of patients who achieved a complete response (CR) during the overall, acute, and delayed phases of the first planned chemotherapy cycle. Secondary endpoints were complete protection, the proportions of patients without emetic episodes or nausea, patients with no more than moderate nausea during the overall, acute and delayed phases, and the time to treatment failure.
4.Combination of palonosetron, aprepitant, and dexamethasone as primary antiemetic prophylaxis for cisplatin-based chemotherapy.
Yang CK1, Wu CE1, Liaw CC2. Biomed J. 2016 Feb;39(1):60-6. doi: 10.1016/j.bj.2015.08.006. Epub 2016 Mar 29.
BACKGROUND: The purpose of this study was to evaluate the efficacy of combined treatment with the long-acting 5-hydroxytryptamine receptor-3 antagonist, palonosetron, the neurokinin-1 receptor antagonist, oral aprepitant, and dexamethasone as primary antiemetic prophylaxis for cancer patients receiving highly emetogenic cisplatin-based chemotherapy.
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CAS 170729-80-3 Aprepitant

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