Aprepitant属于SPA类化合物,能阻断神经激肽1(NK1)受体。
Aprepitant is a potent and selective neurokinin-1 receptor antagonist.
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Tattersall FD, et al. Neuropharmacology, 2000, 39(4), 652-663.
分子式 C23H21F7N4O3 |
分子量 534.43 |
CAS号 170729-80-3 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO ≥100 mg/mL |
Water <1 mg/mL |
Ethanol 15 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT01963793 | Pruritus | Drug: Aprepitant|Drug: Placebo | LEO Pharma | Phase 2 | 2013-10-01 | 2014-10-06 |
NCT02154360 | HIV Infection | Drug: Aprepitant | University of Pennsylvania | Phase 1 | 2014-05-01 | 2016-06-01 |
NCT01402024 | Chemotherapy Induced Nausea and Vomiting | Drug: Aprepitant|Drug: Placebo | All India Institute of Medical Sciences, New Delhi|Dr. Reddy's Laboratories Limited | Phase 3 | 2011-08-01 | 2015-01-16 |
NCT01074255 | Chemotherapy-induced Nausea and Vomiting | Drug: EMEND | Merck Sharp & Dohme Corp. | 2007-04-01 | 2015-04-02 | |
NCT01661335 | Nausea|Vomiting|Childhood Cancer | Drug: Ondansetron, dexamethasone, aprepitant|Drug: Ondansetron, Dexamethasone, placebo | University of Oklahoma | Phase 3 | 2012-06-01 | 2014-12-02 |
NCT02161991 | Carcinoma, Non-small Cell Lung | Drug: Aprepitant|Drug: placebo | Hunan Province Tumor Hospital | Phase 3 | 2014-06-01 | 2016-02-14 |
NCT01527994 | Opioid Dependence | Drug: Aprepitant|Drug: Placebo pill | New York University|National Institute on Drug Abuse (NIDA) | Phase 1 | 2012-01-01 | 2015-04-13 |
NCT01012336 | Chemotherapy-Induced Nausea and Vomiting|Ovarian Cancer | Drug: Aprepitant/Ramosetron/Dexamethasone | Samsung Medical Center|Merck Sharp & Dohme Corp. | Phase 2 | 2010-05-01 | 2012-10-08 |
NCT01149369 | Gastroparesis | Drug: Aprepitant|Drug: Placebo | National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) | Phase 3 | 2013-04-01 | 2016-03-18 |
NCT01249001 | Nausea|Vomiting|Chemotherapy | Drug: Oral Aprepitant|Drug: Aprepitant | The Hospital for Sick Children | Phase 2 | 2010-10-01 | 2017-02-22 |
NCT01683552 | ITCH | Drug: Aprepitant|Drug: Prednisone|Drug: Fexofenadine | Campus Bio-Medico University | Phase 2 | 2010-09-01 | 2012-09-11 |
NCT01334086 | Acute Myeloid Leukemia | Drug: Aprepitant | University Health Network, Toronto|Merck Sharp & Dohme Corp. | Phase 2 | 2011-09-01 | 2015-06-19 |
NCT02532634 | Cancer|Tumors | Drug: ramosetron, aprepitant, dexamethasone|Drug: palonosetron, aprepitant, dexamethasone | Kangdong Sacred Heart Hospital|The Catholic University of Korea|Astellas Pharma Korea, Inc. | Phase 4 | 2015-08-01 | 2016-08-30 |
NCT00999544 | Narcotic Abuse | Drug: Aprepitant|Drug: Placebo|Drug: Oxycodone | University of Kentucky|National Institute on Drug Abuse (NIDA)|Merck Sharp & Dohme Corp. | 2009-10-01 | 2013-07-19 | |
NCT00819039 | Postoperative Nausea and Vomiting | Drug: Aprepitant|Drug: Ondansetron | Merck Sharp & Dohme Corp. | Phase 1 | 2009-01-01 | 2015-06-08 |
NCT01897337 | Postoperative Nausea and Vomiting | Drug: Aprepitant|Drug: placebo | Yonsei University | Phase 4 | 2012-06-01 | 2013-07-08 |
NCT00717054 | Nausea|Vomiting | Drug: Aprepitant|Drug: Scopolamine | Drexel University|Merck Sharp & Dohme Corp. | 2008-02-01 | 2014-05-01 | |
NCT02097823 | Chemotherapy Induced Nausea and Vomiting | Drug: Olanzapine|Drug: Aprepitant | Indiana University | Phase 2 | 2014-02-01 | 2014-03-24 |
NCT02347878 | Leukemia|Lymphoma | Drug: Aprepitant | Sun Yat-sen University | Phase 4 | 2015-04-01 | 2015-01-26 |
NCT00970905 | Nausea|Vomiting | Drug: aprepitant|Drug: Ondansetron | University of Vermont|Mayo Clinic|Wake Forest University Health Sciences|Norris Cotton Cancer Center|University of Massachusetts, Worcester | Phase 2 | 2009-10-01 | 2015-12-27 |
NCT02646020 | Non-small Cell Lung Cancer | Drug: Aprepitant and placebo|Drug: desloratadine and placebo | Sun Yat-sen University | Phase 2 | 2015-12-01 | 2016-01-02 |
NCT02939287 | Nausea|Vomiting | Drug: Aprepitant|Drug: Olanzapine | Rush University Medical Center | Phase 3 | 2016-11-01 | 2016-10-18 |
NCT00314743 | Nausea|Vomiting | Drug: Ondansetron|Drug: Dexamethasone|Drug: Aprepitant | Washington University School of Medicine | Early Phase 1 | 2005-10-01 | 2013-05-22 |
NCT01874119 | Chemotherapy-induced Nausea and Vomiting | Drug: Fosaprepitant | St. Louis University|Merck Sharp & Dohme Corp. | Phase 2 | 2013-09-01 | 2016-10-12 |
NCT00888329 | Postoperative Nausea and Vomiting | Drug: Aprepitant|Drug: Placebo | Mayo Clinic | Phase 4 | 2007-07-01 | 2012-03-05 |
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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