Detail of > 170729-80-3
- CAS Number:
- 170729-80-3
- Name:
Aprepitant
- Formula:
- C23H21F7N4O3
- Molecular Structure:

- Synonyms:
- 3H-1,2,4-Triazol-3-one,5-[[2-[1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2-dihydro-,[2R-[2a(R*),3a]]-;Emend;L 754030;MK 0869;MK 869;ONO7436;
- Molecular Weight:
- 534.43
- Density:
- 1.51 g/cm3
- Appearance:
- off-white to light yellow cyrstalline solid
- Deleted CAS:
- 221350-96-5
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- 170729-80-3Aprepitant
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Reference
- Aprepitant as salvage therapy in patients with chemotherapy-induced nausea and emesis refractory to prophylaxis with 5-HT3 antagonists and dexamethasone
- All Rights Reserved. Aprepitant as salvage therapy in patients with chemotherapy-induced nausea and emesis refractory to prophylaxis with 5-HT3 antagonists and dexamethasone. Oechsle, Karin; Mueller, Martin R.; Hartmann, Joerg T.; Kanz, Lothar; Bokemeyer, Carsten (Medizinsche Klinik und Poliklinik II, Abteilung fuer Haematologie / Onkologie / Immunologie / Rheumatologie / Pulmonologie, Universitaetsklinik Tuebingen, Tuebingen, Germany). Onkologie, 29(12), 557-561 (German) 2006 S. Karger GmbH. CODEN: ONKOD2. ISSN: 0378-584X. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Despite prophylaxis with 5-HT3 antagonists and dexamethasone, nausea/emesis are common chemotherapy-induced toxicities. The aim of this trial was to evaluate the efficacy of adding the NK1 antagonist aprepitant in patients refractory to std. prophylaxis. Patients with significant nausea/vomiting despite prophylaxis with 5-HT3 antagonists and dexamethasone were eligible. Aprepitant was added to the same antiemetic regimen used during previous cycles. 34 Patients received 92 cycles of chemotherapy with aprepitant which was applied orally at 125 mg on day 1 and 80 mg on days 2 and 3. All patients were refractory to std. 50-02-2 and 170729-80-3 are cas registry numbers of chemicals which are used as reagents here. antiemetic prophylaxis during cisplatin-based (n = 12) or other chemotherapy (n = 22). With the addn. of aprepitant, all patients reported subjective improvement. The no. of patients with nausea for >4 days decreased from 24 (71%) to 4 (12%) (p < 0.001), and the no. of those with emesis for >2 days decreased from 26 (77%) to 0 (0%) (p < 0.001). In 12 patients receiving aprepitant for >2 cycles (3-8) the efficacy was maintained. No toxicity possibly related to aprepitant was obsd. Aprepitant demonstrated significant activity in patients with nausea/vomiting refractory to prophylaxis with 5-HT3 antagonists and dexamethasone. .
- Role of Neurokinin-1 Receptor Antagonists in Chemotherapy-Induced Emesis: Summary of Clinical Trials
- Role of Neurokinin-1 Receptor Antagonists in Chemotherapy-Induced Emesis: Summary of Clinical Trials. Navari, Rudolph M. (Walther Cancer Research Center, University of Notre Dame, Notre Dame, IN 46556, USA). Cancer Investigation, 22(4), 569-576 (English) 2004 Marcel Dekker, Inc. CODEN: CINVD7. ISSN: 0735-7907. DOCUMENT TYPE: Journal; General Review CA Section: 1 (Pharmacology) A review. Chemotherapy-induced nausea and vomiting (CINV) is assocd. with a significant deterioration in quality of life, and although the use of 5-hydroxytryptamine3 (5-HT3) receptor antagonists plus dexamethasone has significantly improved the control of acute CINV, delayed nausea and vomiting remain a significant clin.In this article, certain chemicals are used. Some of their cas registry numbers are 50-02-2 and 170729-80-3 problem. Aprepitant is the first agent available in the new drug class of neurokinin-1 receptor antagonists. When added to a std. regimen of a 5-HT3 receptor antagonist and dexamethasone in patients receiving highly emetogenic chemotherapy, it improves the complete response rate of acute CINV. Aprepitant also improves the complete response of delayed CINV when used in combination with dexamethasone compared to dexamethasone alone. The use of aprepitant in patients receiving moderately emetogenic chemotherapy will await the review and anal. of recently completed phase III trials. The control of nausea is improved in some studies with the use of aprepitant when it is combined with a 5HT3 receptor antagonist and dexamethasone, but nausea control remains suboptimal. The current data suggest that the mechanism of action of the NK-1s appears to be different from the 5-HT3 receptor antagonists. Future studies may explore the use of aprepitant and other NK-1s in moderately and highly emetogenic chemotherapy, as well in the clin. settings of multiple-day chemotherapy and bone marrow transplantation. .
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