Aprepitant (BioDeep_00000014108)

human metabolite blood metabolite

代谢物信息卡片

3-(((2R,3S)-3-(p-Fluorophenyl)-2-(((alphar)-alpha-methyl-3,5-bis(trifluoromethyl)benzyl)oxy)morpholino)methyl)-Delta(2)-1,2,4-triazolin-5-one

化学式: C23H21F7N4O3 (534.15018)
中文名称: 阿瑞吡坦
谱图信息: 最多检出来源 Homo sapiens(blood) 31.91%

分子结构信息

SMILES: CC(C1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F)OC2C(N(CCO2)CC3=NNC(=O)N3)C4=CC=C(C=C4)F
InChI: InChI=1S/C23H21F7N4O3/c1-12(14-8-15(22(25,26)27)10-16(9-14)23(28,29)30)37-20-19(13-2-4-17(24)5-3-13)34(6-7-36-20)11-18-31-21(35)33-32-18/h2-5,8-10,12,19-20H,6-7,11H2,1H3,(H2,31,32,33,35)/t12-,19+,20-/m1/s1

描述信息

Aprepitant, an antiemetic, is a substance P/neurokinin 1 (NK1) receptor antagonist which, in combination with other antiemetic agents, is indicated for the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy. Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors. Aprepitant has little or no affinity for serotonin (5-HT3), dopamine, and corticosteroid receptors, the targets of existing therapies for chemotherapy-induced nausea and vomiting (CI NV).
A - Alimentary tract and metabolism > A04 - Antiemetics and antinauseants > A04A - Antiemetics and antinauseants
D018377 - Neurotransmitter Agents > D064729 - Neurokinin-1 Receptor Antagonists
D018373 - Peripheral Nervous System Agents > D001337 - Autonomic Agents
C78272 - Agent Affecting Nervous System > C267 - Antiemetic Agent
D005765 - Gastrointestinal Agents > D000932 - Antiemetics
D002491 - Central Nervous System Agents
Aprepitant (MK-0869) is a selective and high-affinity neurokinin 1 receptor antagonist with a Kd of 86 pM.

同义名列表

16 个代谢物同义名

3-(((2R,3S)-3-(p-Fluorophenyl)-2-(((alphar)-alpha-methyl-3,5-bis(trifluoromethyl)benzyl)oxy)morpholino)methyl)-Delta(2)-1,2,4-triazolin-5-one; 3-(((2R,3S)-3-(p-Fluorophenyl)-2-(((alphar)-a-methyl-3,5-bis(trifluoromethyl)benzyl)oxy)morpholino)methyl)-delta(2)-1,2,4-triazolin-5-one; 3-{[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholin-4-yl]methyl}-4,5-dihydro-1H-1,2,4-triazol-5-one; 3-[[(2R,3R)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholin-4-yl]methyl]-1,4-dihydro-1,2,4-triazol-5-one; 3-(((2R,3S)-3-(p-Fluorophenyl)-2-(((alphar)-α-methyl-3,5-bis(trifluoromethyl)benzyl)oxy)morpholino)methyl)-δ(2)-1,2,4-triazolin-5-one; 3-(((2R,3S)-3-(p-Fluorophenyl)-2-(((alphar)-a-methyl-3,5-bis(trifluoromethyl)benzyl)oxy)morpholino)methyl)-δ(2)-1,2,4-triazolin-5-one; (2R)-(1R)-3,5-Bis(trifluoromethylphenyl)ethoxy)-(3S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazole)methyl-morpholine; (1-(3,5-Bis(trifluoromethyl)phenyl)ethoxy)-3-(fluoro)phenyl-4-(3-oxo-1,2,4-triazol-5-yl)methylmorpholine; Aprepitantum; Aprepitant; Cinvanti; MK-0517; MK-869; Emend; MK-0869; L-754030

数据库引用编号

18 个数据库交叉引用编号

ChEBI: CHEBI:499361
KEGG: C21555
KEGGdrug: D02968
PubChem: 135761774
PubChem: 135413536
PubChem: 6918365
HMDB: HMDB0014811
DrugBank: DB00673
ChEMBL: CHEMBL1471
Wikipedia: Aprepitant
MeSH: Aprepitant
chemspider: 5293568
CAS: 321125-94-4
CAS: 170729-80-3
PMhub: MS000028725
PubChem: 336445193
PDB-CCD: GBQ
medchemexpress: HY-10052

分类词条

Phenylmorpholines

代谢反应

0 个相关的代谢反应过程信息。

Reactome(0)

BioCyc(0)

WikiPathways(0)

Plant Reactome(0)

INOH(0)

PlantCyc(0)

COVID-19 Disease Map(0)

PathBank(0)

PharmGKB(0)

1 个相关的物种来源信息

9606 - Homo sapiens: -

在这里通过桑基图来展示出与当前的这个代谢物在我们的BioDeep知识库中具有相关联信息的其他代谢物。在这里进行关联的信息来源主要有：

PubMed: 来源于PubMed文献库中的文献信息，我们通过自然语言数据挖掘得到的在同一篇文献中被同时提及的相关代谢物列表，这个列表按照代谢物同时出现的文献数量降序排序，取前10个代谢物作为相关研究中关联性很高的代谢物集合展示在桑基图中。
NCBI Taxonomy: 通过文献数据挖掘，得到的代谢物物种来源信息关联。这个关联信息同样按照出现的次数降序排序，取前10个代谢物作为高关联度的代谢物集合展示在桑吉图上。
Chemical Taxonomy: 在物质分类上处于同一个分类集合中的其他代谢物
Chemical Reaction: 在化学反应过程中，存在为当前代谢物相关联的生化反应过程中的反应底物或者反应产物的关联代谢物信息。

点击图上的相关代谢物的名称，可以跳转到相关代谢物的信息页面。

文献列表

Zhuo Zhang, Guizhou Hao, Xuemei Sun, Feibo Wang, Dengbo Zhang, Dedong Hu. PVP/aprepitant microcapsules produced by supercritical antisolvent process. Scientific reports. 2024 05; 14(1):10679. doi: 10.1038/s41598-024-60323-z. [PMID: 38724534]
Reham H Mohyeldin, Walaa Yehia Abdelzaher, Ehab E Sharata, Hamza M A Mohamed, Mohamed Y M Ahmed, Josef Zekry Attia, Medhat Atta, Rabeh Khairy Saleh, Elshimaa A Ghallab, Heba Marey, Mahmoud A Elrehany, Remon Roshdy Rofaeil. Aprepitant boasted a protective effect against olanzapine-induced metabolic syndrome and its subsequent hepatic, renal, and ovarian dysfunction; Role of IGF1/p-AKT/FOXO1 and NFκB/IL-1β/TNF-α signaling pathways in female Wistar albino rats. Biochemical pharmacology. 2024 Jan; 221(?):116020. doi: 10.1016/j.bcp.2024.116020. [PMID: 38237301]
Yan Li, Hong Yin, Chensi Wu, Jia He, Chunyan Wang, Bo Ren, Heping Wang, Dandan Geng, Yirong Zhang, Ligang Zhao. Preparation and in vivo evaluation of an intravenous emulsion loaded with an aprepitant-phospholipid complex. Drug delivery. 2023 Dec; 30(1):2183834. doi: 10.1080/10717544.2023.2183834. [PMID: 36843571]
Alan Hegron, Chloe J Peach, Raquel Tonello, Philipp Seemann, Shavonne Teng, Rocco Latorre, Harald Huebner, Dorothee Weikert, Jeanette Rientjes, Nicholas A Veldhuis, Daniel P Poole, Dane D Jensen, Alex R B Thomsen, Brian L Schmidt, Wendy L Imlach, Peter Gmeiner, Nigel W Bunnett. Therapeutic antagonism of the neurokinin 1 receptor in endosomes provides sustained pain relief. Proceedings of the National Academy of Sciences of the United States of America. 2023 05; 120(22):e2220979120. doi: 10.1073/pnas.2220979120. [PMID: 37216510]
Aharon Oren, Maria Chuvochina. Naming genera after geographical locations. Proposal to emend Appendix 9 of the International Code of Nomenclature of Prokaryotes. International journal of systematic and evolutionary microbiology. 2023 May; 73(5):. doi: 10.1099/ijsem.0.005873. [PMID: 37163413]
Jinwen Liu, Shuyan Li, Wuliji Ao, Yongji Li, Yingge Xiao, Meirong Bai. Fabrication of an aprepitant nanosuspension using hydroxypropyl chitosan to increase the bioavailability. Biochemical and biophysical research communications. 2022 Nov; 631(?):72-77. doi: 10.1016/j.bbrc.2022.09.031. [PMID: 36179498]
Mervat Z Mohamed, Mohamed F Abed El Baky, Merhan E Ali, Heba M Hafez. Aprepitant exerts anti-fibrotic effect via inhibition of TGF-β/Smad3 pathway in bleomycin-induced pulmonary fibrosis in rats. Environmental toxicology and pharmacology. 2022 Oct; 95(?):103940. doi: 10.1016/j.etap.2022.103940. [PMID: 35931359]
Rongrong Shen, Horst Aspöck, Ulrike Aspöck, John Plant, Yuting Dai, Xingyue Liu. Unraveling the evolutionary history of the snakefly family Inocelliidae (Insecta: Raphidioptera) through integrative phylogenetics. Cladistics : the international journal of the Willi Hennig Society. 2022 10; 38(5):515-537. doi: 10.1111/cla.12503. [PMID: 35349190]
Benxun Pan, Dongsheng Liu, Lingyun Yang, Kurt Wüthrich. GPCR large-amplitude dynamics by 19F-NMR of aprepitant bound to the neurokinin 1 receptor. Proceedings of the National Academy of Sciences of the United States of America. 2022 04; 119(15):e2122682119. doi: 10.1073/pnas.2122682119. [PMID: 35377814]
Hideyuki Hibino, Naomi Sakiyama, Yoshinori Makino, Reiko Makihara-Ando, Hidehito Horinouchi, Yutaka Fujiwara, Shintaro Kanda, Yasushi Goto, Tatsuya Yoshida, Yusuke Okuma, Yuki Shinno, Shuji Murakami, Hironobu Hashimoto, Takeshi Akiyoshi, Ayuko Imaoka, Yuichiro Ohe, Masakazu Yamaguchi, Hisakazu Ohtani. Evaluation of hepatic CYP3A enzyme activity using endogenous markers in lung cancer patients treated with cisplatin, dexamethasone, and aprepitant. European journal of clinical pharmacology. 2022 Apr; 78(4):613-621. doi: 10.1007/s00228-022-03275-5. [PMID: 35039908]
Sergei Spitsin, Vasiliki Pappa, Annemarie Kinder, Dwight L Evans, Jay Rappaport, Steven D Douglas. Effect of aprepitant on kynurenine to tryptophan ratio in cART treated and cART naïve adults living with HIV. Medicine. 2021 Jun; 100(23):e25313. doi: 10.1097/md.0000000000025313. [PMID: 34114978]
Takafumi Naito, Yusuke Suzuki, Kaito Shibata, Junichi Kawakami. Simple Liquid Chromatography-Tandem Mass Spectrometry Method for Quantitation of Total and Free Aprepitant and Its Active N-Dealkylated Metabolites in Human Plasma. Therapeutic drug monitoring. 2021 06; 43(3):422-428. doi: 10.1097/ftd.0000000000000815. [PMID: 32960546]
A Laura Nijstad, Matthijs M Tibben, Abadi Gebretensae, Hilde Rosing, Evelien de Vos-Kerkhof, C Michel Zwaan, Alwin D R Huitema, Jos H Beijnen. Development and validation of a combined liquid chromatography tandem-mass spectrometry assay for the quantification of aprepitant and dexamethasone in human plasma to support pharmacokinetic studies in pediatric patients. Journal of chromatography. B, Analytical technologies in the biomedical and life sciences. 2021 May; 1171(?):122639. doi: 10.1016/j.jchromb.2021.122639. [PMID: 33756449]
Nazlı Erdoğar, Tuba Reçber, Alper Bektas İskit, Erem Bilensoy, Sedef Kır, Emirhan Nemutlu. Determination and validation of aprepitant in rat plasma using LC-MS/MS. Bioanalysis. 2021 03; 13(5):363-372. doi: 10.4155/bio-2020-0293. [PMID: 33682445]
Padmanabhan Mannangatti, Durairaj Ragu Varman, Sammanda Ramamoorthy, Lankupalle D Jayanthi. Neurokinin-1 Antagonism Distinguishes the Role of Norepinephrine Transporter from Dopamine Transporter in Mediating Amphetamine Behaviors. Pharmacology. 2021; 106(11-12):597-605. doi: 10.1159/000518033. [PMID: 34515205]
Kristina Rodionova, Karl F Hilgers, Eva-Maria Paulus, Gisa Tiegs, Christian Ott, Roland Schmieder, Mario Schiffer, Kerstin Amann, Roland Veelken, Tilmann Ditting. Neurogenic tachykinin mechanisms in experimental nephritis of rats. Pflugers Archiv : European journal of physiology. 2020 12; 472(12):1705-1717. doi: 10.1007/s00424-020-02469-z. [PMID: 33070237]
Harun Un, Rustem Anil Ugan, Duygu Kose, Yasin Bayir, Elif Cadirci, Jale Selli, Zekai Halici. A novel effect of Aprepitant: Protection for cisplatin-induced nephrotoxicity and hepatotoxicity. European journal of pharmacology. 2020 Aug; 880(?):173168. doi: 10.1016/j.ejphar.2020.173168. [PMID: 32423870]
Julien Wils, Céline Duparc, Anne-Françoise Cailleux, Antoine-Guy Lopez, Caroline Guiheneuf, Isabelle Boutelet, Hadrien-Gaël Boyer, Christophe Dubessy, Saloua Cherifi, Bruno Cauliez, Françoise Gobet, Guillaume Defortescu, Jean-François Ménard, Estelle Louiset, Hervé Lefebvre. The neuropeptide substance P regulates aldosterone secretion in human adrenals. Nature communications. 2020 05; 11(1):2673. doi: 10.1038/s41467-020-16470-8. [PMID: 32471973]
Joanna J Chmielinska, Jay H Kramer, I-Tong Mak, Christopher F Spurney, William B Weglicki. Substance P receptor blocker, aprepitant, inhibited cutaneous and other neurogenic inflammation side effects of the EGFR1-TKI, erlotinib. Molecular and cellular biochemistry. 2020 Feb; 465(1-2):175-185. doi: 10.1007/s11010-019-03677-7. [PMID: 31853800]
Xinyu Zhang, Ying Wei, Zhijun Cao, Ying Xu, Cong Lu, Meiqi Zhao, Jingxin Gou, Tian Yin, Yu Zhang, Haibing He, Yanjiao Wang, Xing Tang. Aprepitant Intravenous Emulsion Based on Ion Pairing/Phospholipid Complex for Improving Physical and Chemical Stability During Thermal Sterilization. AAPS PharmSciTech. 2020 Jan; 21(3):75. doi: 10.1208/s12249-019-1605-7. [PMID: 31965388]
Meng-Jie Yang, Hong-Rong Xu, Hui Li, Wei-Li Chen, Fei Yuan, Xue-Ning Li. Comparison of Pharmacokinetics of Aprepitant in Healthy Chinese and Caucasian Subjects. Drug design, development and therapy. 2020; 14(?):1219-1226. doi: 10.2147/dddt.s243924. [PMID: 32273684]
Hongzhang Wu, Xurui Cheng, Feiyan Huang, Gang Shao, Yueming Meng, Lingfei Wang, Tao Wang, Xiaoyuan Jia, Tianxin Yang, Xi Wang, Caiyun Fu. Aprepitant Sensitizes Acute Myeloid Leukemia Cells to the Cytotoxic Effects of Cytosine Arabinoside in vitro and in vivo. Drug design, development and therapy. 2020; 14(?):2413-2422. doi: 10.2147/dddt.s244648. [PMID: 32606608]
Paulina D Ramírez-García, Jeffri S Retamal, Priyank Shenoy, Wendy Imlach, Matthew Sykes, Nghia Truong, Luis Constandil, Teresa Pelissier, Cameron J Nowell, Song Y Khor, Louis M Layani, Chris Lumb, Daniel P Poole, TinaMarie Lieu, Gregory D Stewart, Quynh N Mai, Dane D Jensen, Rocco Latorre, Nicole N Scheff, Brian L Schmidt, John F Quinn, Michael R Whittaker, Nicholas A Veldhuis, Thomas P Davis, Nigel W Bunnett. A pH-responsive nanoparticle targets the neurokinin 1 receptor in endosomes to prevent chronic pain. Nature nanotechnology. 2019 12; 14(12):1150-1159. doi: 10.1038/s41565-019-0568-x. [PMID: 31686009]
Priya Patel, Paul C Nathan, Scott E Walker, Sue Zupanec, Jocelyne Volpe, L Lee Dupuis. Relative bioavailability of an extemporaneously prepared aprepitant oral suspension in healthy adults. Journal of oncology pharmacy practice : official publication of the International Society of Oncology Pharmacy Practitioners. 2019 Dec; 25(8):1907-1915. doi: 10.1177/1078155219828806. [PMID: 31694495]
Mahmoud A Tantawy, Soheir Alweshahy, Dalia A Elshabasy, Nadia F Youssef. Simultaneous Determination of Co-administrated Deflazacort, Aprepitant and Granisetron in Dosage Forms and Spiked Human Plasma by RP-HPLC/PAD. Journal of chromatographic science. 2019 Oct; 57(9):790-798. doi: 10.1093/chromsci/bmz062. [PMID: 31504281]
Chara Litou, Nikunjkumar Patel, David B Turner, Edmund Kostewicz, Martin Kuentz, Karl J Box, Jennifer Dressman. Combining biorelevant in vitro and in silico tools to simulate and better understand the in vivo performance of a nano-sized formulation of aprepitant in the fasted and fed states. European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences. 2019 Oct; 138(?):105031. doi: 10.1016/j.ejps.2019.105031. [PMID: 31386891]
F Tansu Salman, Cara DiCristina, Anne Chain, Amna Sadaf Afzal. Pharmacokinetics and pharmacodynamics of aprepitant for the prevention of postoperative nausea and vomiting in pediatric subjects. Journal of pediatric surgery. 2019 Jul; 54(7):1384-1390. doi: 10.1016/j.jpedsurg.2018.09.006. [PMID: 30381138]
Erlend Skaga, Ida Ø Skaga, Zanina Grieg, Cecilie J Sandberg, Iver A Langmoen, Einar O Vik-Mo. The efficacy of a coordinated pharmacological blockade in glioblastoma stem cells with nine repurposed drugs using the CUSP9 strategy. Journal of cancer research and clinical oncology. 2019 Jun; 145(6):1495-1507. doi: 10.1007/s00432-019-02920-4. [PMID: 31028540]
Jie Xiong, Guifang Zhao, Shengli Yang, Jing Chen. Efficacy, Tolerability and Pharmacokinetic Impact of Aprepitant in Sarcoma Patients Receiving Ifosfamide and Doxorubicin Chemotherapy: A Randomized Controlled Trial. Advances in therapy. 2019 02; 36(2):355-364. doi: 10.1007/s12325-018-0862-2. [PMID: 30607545]
Bo-Ke Liu, Xing-Wei Jin, Hao-Zhong Lu, Xiang Zhang, Zhong-Hua Zhao, Yuan Shao. The Effects of Neurokinin-1 Receptor Antagonist in an Experimental Autoimmune Cystitis Model Resembling Bladder Pain Syndrome/Interstitial Cystitis. Inflammation. 2019 Feb; 42(1):246-254. doi: 10.1007/s10753-018-0888-2. [PMID: 30196377]
Naohisa Yoshida, Tetsuya Taguchi, Masayoshi Nakanishi, Ken Inoue, Tetsuya Okayama, Takeshi Ishikawa, Eigo Otsuji, Koichi Takayama, Haruo Kuroboshi, Motohiro Kanazawa, Yoshito Itoh. Efficacy of the combination use of aprepitant and palonosetron for improving nausea in various moderately emetogenic chemotherapy regimens. BMC pharmacology & toxicology. 2019 Jan; 20(1):6. doi: 10.1186/s40360-018-0278-2. [PMID: 30642399]
Kun Sheng, Xi Lu, Jianming Yue, Wei Gu, Chao Gu, Haibin Zhang, Wenda Wu. Role of neurotransmitters 5-hydroxytryptamine and substance P in anorexia induction following oral exposure to the trichothecene T-2 toxin. Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association. 2019 Jan; 123(?):1-8. doi: 10.1016/j.fct.2018.10.041. [PMID: 30336258]
Shu-Yue Zheng, Wen Shen, Yan-Mei Peng, Hui-Juan Cui, Hua Duan, Yu-Qin Qiu, Qiang Li, Jing-Yi Zhang, Chen-Yao Sun, Xu Zhang. Treatment of severe rash caused by crizotinib with both traditional Chinese medicine and Western medicine: Two case reports and literature review. Medicine. 2018 Nov; 97(48):e13088. doi: 10.1097/md.0000000000013088. [PMID: 30508887]
Tatevik Ohanyan, Nicole Schoepke, Stefan Eirefelt, Gert Hoey, Witte Koopmann, Tomasz Hawro, Marcus Maurer, Martin Metz. Role of Substance P and Its Receptor Neurokinin 1 in Chronic Prurigo: A Randomized, Proof-of-Concept, Controlled Trial with Topical Aprepitant. Acta dermato-venereologica. 2018 Jan; 98(1):26-31. doi: 10.2340/00015555-2780. [PMID: 28853492]
Tom Ottoboni, Mary Rose Keller, Matt Cravets, Neil Clendeninn, Barry Quart. Bioequivalence of HTX-019 (aprepitant IV) and fosaprepitant in healthy subjects: a Phase I, open-label, randomized, two-way crossover evaluation. Drug design, development and therapy. 2018; 12(?):429-435. doi: 10.2147/dddt.s155875. [PMID: 29535504]
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. Aprepitant Has Mixed Effects on Nausea and Reduces Other Symptoms in Patients With Gastroparesis and Related Disorders. Gastroenterology. 2018 01; 154(1):65-76.e11. doi: 10.1053/j.gastro.2017.08.033. [PMID: 29111115]
Carl Roos, David Dahlgren, Staffan Berg, Jan Westergren, Bertil Abrahamsson, Christer Tannergren, Erik Sjögren, Hans Lennernäs. In Vivo Mechanisms of Intestinal Drug Absorption from Aprepitant Nanoformulations. Molecular pharmaceutics. 2017 12; 14(12):4233-4242. doi: 10.1021/acs.molpharmaceut.7b00294. [PMID: 28737398]
Mihoko Morita, Shinji Kishi, Miyuki Ookura, Yasufumi Matsuda, Katsunori Tai, Takahiro Yamauchi, Takanori Ueda. Efficacy of aprepitant for CHOP chemotherapy-induced nausea, vomiting, and anorexia. Current problems in cancer. 2017 Nov; 41(6):419-425. doi: 10.1016/j.currproblcancer.2017.09.001. [PMID: 29061362]
Sergei Spitsin, Pablo Tebas, Jeffrey S Barrett, Vasiliki Pappa, Deborah Kim, Deanne Taylor, Dwight L Evans, Steven D Douglas. Antiinflammatory effects of aprepitant coadministration with cART regimen containing ritonavir in HIV-infected adults. JCI insight. 2017 10; 2(19):. doi: 10.1172/jci.insight.95893. [PMID: 28978797]
N Fountoulakis, J Dunn, S Thomas, J Karalliedde. Successful management of refractory diabetic gastroparesis with long-term Aprepitant treatment. Diabetic medicine : a journal of the British Diabetic Association. 2017 10; 34(10):1483-1486. doi: 10.1111/dme.13413. [PMID: 28636760]
Poe-Hirr Hsyu, Daniela Soriano Pignataro, Kyle Matschke. Effect of aprepitant, a moderate CYP3A4 inhibitor, on bosutinib exposure in healthy subjects. European journal of clinical pharmacology. 2017 Jan; 73(1):49-56. doi: 10.1007/s00228-016-2108-z. [PMID: 27718000]
Alice He, Jihad M Alhariri, Ronald J Sweren, Madan M Kwatra, Shawn G Kwatra. Aprepitant for the Treatment of Chronic Refractory Pruritus. BioMed research international. 2017; 2017(?):4790810. doi: 10.1155/2017/4790810. [PMID: 29057261]
Jeffrey S Barrett, Sergei Spitsin, Ganesh Moorthy, Kyle Barrett, Kate Baker, Andrew Lackner, Florin Tulic, Angela Winters, Dwight L Evans, Steven D Douglas. Pharmacologic rationale for the NK1R antagonist, aprepitant as adjunctive therapy in HIV. Journal of translational medicine. 2016 05; 14(1):148. doi: 10.1186/s12967-016-0904-y. [PMID: 27230663]
Qi Shi, Wen Li, Hongjia Li, Qiqi Le, Shanshan Liu, Shaoqi Zong, Leizhen Zheng, Fenggang Hou. Prevention of cisplatin-based chemotherapy-induced delayed nausea and vomiting using triple antiemetic regimens: a mixed treatment comparison. Oncotarget. 2016 Apr; 7(17):24402-14. doi: 10.18632/oncotarget.8255. [PMID: 27015550]
Hiroshi Kitamura, Atsushi Takahashi, Hiroshi Hotta, Ryuichi Kato, Yasuharu Kunishima, Fumiyasu Takei, Hiroki Horita, Naoya Masumori. Palonosetron with aprepitant plus dexamethasone to prevent chemotherapy-induced nausea and vomiting during gemcitabine/cisplatin in urothelial cancer patients. International journal of urology : official journal of the Japanese Urological Association. 2015 Oct; 22(10):911-4. doi: 10.1111/iju.12842. [PMID: 26087891]
Andrew P Degnan, George O Tora, Ying Han, Ramkumar Rajamani, Robert Bertekap, Rudolph Krause, Carl D Davis, Joanna Hu, Daniel Morgan, Sarah J Taylor, Kelly Krause, Yu-Wen Li, Gail Mattson, Melissa A Cunningham, Matthew T Taber, Nicholas J Lodge, Joanne J Bronson, Kevin W Gillman, John E Macor. Biaryls as potent, tunable dual neurokinin 1 receptor antagonists and serotonin transporter inhibitors. Bioorganic & medicinal chemistry letters. 2015 Aug; 25(15):3039-43. doi: 10.1016/j.bmcl.2015.04.098. [PMID: 26048800]
Kosuke Nishizawa, Hideaki Shimada, Masaaki Ito, Yoko Oshima, Satoshi Yajima, Yoshinori Kikuchi, Yasukiyo Sumino, Hironori Kaneko, Kenji Nishizawa, Masahiko Obayashi. The correlation between plasma aprepitant concentration and antiemetic effect in Japanese gastric or esophageal cancer patients. International journal of clinical oncology. 2015 Jun; 20(3):538-42. doi: 10.1007/s10147-014-0747-6. [PMID: 25196862]
Pablo Tebas, Sergei Spitsin, Jeffrey S Barrett, Florin Tuluc, Okan Elci, James J Korelitz, Wayne Wagner, Angela Winters, Deborah Kim, Renae Catalano, Dwight L Evans, Steven D Douglas. Reduction of soluble CD163, substance P, programmed death 1 and inflammatory markers: phase 1B trial of aprepitant in HIV-1-infected adults. AIDS (London, England). 2015 May; 29(8):931-9. doi: 10.1097/qad.0000000000000638. [PMID: 25915168]
I Tong Mak, Jay H Kramer, Joanna J Chmielinska, Christopher F Spurney, William B Weglicki. EGFR-TKI, erlotinib, causes hypomagnesemia, oxidative stress, and cardiac dysfunction: attenuation by NK-1 receptor blockade. Journal of cardiovascular pharmacology. 2015 Jan; 65(1):54-61. doi: 10.1097/fjc.0000000000000163. [PMID: 25343568]
John Sarantopoulos, Alain C Mita, James L Wade, John C Morris, Olivier Rixe, Monica M Mita, Jean-François Dedieu, Claudine Wack, Laurent Kassalow, A Craig Lockhart. Phase I study of cabazitaxel plus cisplatin in patients with advanced solid tumors: study to evaluate the impact of cytochrome P450 3A inhibitors (aprepitant, ketoconazole) or inducers (rifampin) on the pharmacokinetics of cabazitaxel. Cancer chemotherapy and pharmacology. 2014 Dec; 74(6):1113-24. doi: 10.1007/s00280-014-2572-z. [PMID: 25307552]
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Sergei Spitsin, Florin Tuluc, John Meshki, Jian Ping Lai, Richard Tustin Iii, Steven D Douglas. Analog of somatostatin vapreotide exhibits biological effects in vitro via interaction with neurokinin-1 receptor. Neuroimmunomodulation. 2013; 20(5):247-55. doi: 10.1159/000350468. [PMID: 23921645]
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Thomas C Marbury, Phung L Ngo, Craig R Shadle, Bo Jin, Deborah Panebianco, Luzelena Caro, Jack Valentine, Gail Murphy. Pharmacokinetics of oral dexamethasone and midazolam when administered with single-dose intravenous 150 mg fosaprepitant in healthy adult subjects. Journal of clinical pharmacology. 2011 Dec; 51(12):1712-20. doi: 10.1177/0091270010387792. [PMID: 21209230]
Toshiaki Takahashi, Yukiko Nakamura, Asuka Tsuya, Haruyasu Murakami, Masahiro Endo, Nobuyuki Yamamoto. Pharmacokinetics of aprepitant and dexamethasone after administration of chemotherapeutic agents and effects of plasma substance P concentration on chemotherapy-induced nausea and vomiting in Japanese cancer patients. Cancer chemotherapy and pharmacology. 2011 Sep; 68(3):653-9. doi: 10.1007/s00280-010-1519-2. [PMID: 21125277]
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Pablo Tebas, Florin Tuluc, Jeffrey S Barrett, Wayne Wagner, Deborah Kim, Huaquing Zhao, René Gonin, James Korelitz, Steven D Douglas. A randomized, placebo controlled, double masked phase IB study evaluating the safety and antiviral activity of aprepitant, a neurokinin-1 receptor antagonist in HIV-1 infected adults. PloS one. 2011; 6(9):e24180. doi: 10.1371/journal.pone.0024180. [PMID: 21931661]
Gerlinde Egerer, Kathrin Eisenlohr, Martina Gronkowski, Juergen Burhenne, Klaus-Dieter Riedel, Gerd Mikus. The NK₁ receptor antagonist aprepitant does not alter the pharmacokinetics of high-dose melphalan chemotherapy in patients with multiple myeloma. British journal of clinical pharmacology. 2010 Dec; 70(6):903-7. doi: 10.1111/j.1365-2125.2010.03792.x. [PMID: 21175446]
Mark J Millan, Anne Dekeyne, Alain Gobert, Clotilde Mannoury la Cour, Mauricette Brocco, Jean-Michel Rivet, Benjamin Di Cara, Françoise Lejeune, Thomas I Cremers, Gunnar Flik, Trynke R de Jong, Berend Olivier, Guillaume de Nanteuil. S41744, a dual neurokinin (NK)1 receptor antagonist and serotonin (5-HT) reuptake inhibitor with potential antidepressant properties: a comparison to aprepitant (MK869) and paroxetine. European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology. 2010 Sep; 20(9):599-621. doi: 10.1016/j.euroneuro.2010.04.003. [PMID: 20483567]
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C M Chavez-Eng, M L Constanzer, B K Matuszewski. Simultaneous determination of Aprepitant and two metabolites in human plasma by high-performance liquid chromatography with tandem mass spectrometric detection. Journal of pharmaceutical and biomedical analysis. 2004 Sep; 35(5):1213-29. doi: 10.1016/j.jpba.2004.03.020. [PMID: 15336366]
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Craig R Shadle, Yih Lee, Anup K Majumdar, Kevin J Petty, Cynthia Gargano, Thomas E Bradstreet, Judith K Evans, Robert A Blum. Evaluation of potential inductive effects of aprepitant on cytochrome P450 3A4 and 2C9 activity. Journal of clinical pharmacology. 2004 Mar; 44(3):215-23. doi: 10.1177/0091270003262950. [PMID: 14973304]
Su-Er W Huskey, Brian J Dean, George A Doss, Zhen Wang, Cornelis E C A Hop, Reza Anari, Paul E Finke, Albert J Robichaud, Minghua Zhang, Bonnie Wang, John R Strauss, Paul K Cunningham, William P Feeney, Ronald B Franklin, Thomas A Baillie, Shuet-Hing L Chiu. The metabolic disposition of aprepitant, a substance P receptor antagonist, in rats and dogs. Drug metabolism and disposition: the biological fate of chemicals. 2004 Feb; 32(2):246-58. doi: 10.1124/dmd.32.2.246. [PMID: 14744948]
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Martin Feuring, Yih Lee, Laura H Orlowski, Nicole Michiels, Marina De Smet, Anup K Majumdar, Kevin J Petty, Michael R Goldberg, M Gail Murphy, Keith M Gottesdiener, Michael Hesney, L Ellen Brackett, Martin Wehling. Lack of effect of aprepitant on digoxin pharmacokinetics in healthy subjects. Journal of clinical pharmacology. 2003 Aug; 43(8):912-7. doi: 10.1177/0091270003256113. [PMID: 12953348]
Jacqueline B McCrea, Anup K Majumdar, Michael R Goldberg, Marian Iwamoto, Cynthia Gargano, Deborah L Panebianco, Michael Hesney, Christopher R Lines, Kevin J Petty, Paul J Deutsch, M Gail Murphy, Keith M Gottesdiener, D Ronald Goldwater, Robert A Blum. Effects of the neurokinin1 receptor antagonist aprepitant on the pharmacokinetics of dexamethasone and methylprednisolone. Clinical pharmacology and therapeutics. 2003 Jul; 74(1):17-24. doi: 10.1016/s0009-9236(03)00066-3. [PMID: 12844131]
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