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Chemical Compound Review

Aprepitant     5-[[(2S,3S)-2-[(1R)-1-[3,5...

Synonyms: Emend, AC1OCFCG, CHEMBL1471, S1189_Selleck, CHEMBL135613, ...
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Disease relevance of Aprepitant

  • Confirming and extending previous findings, the triple combination of a 5HT(3) antagonist, MK-869, and dexamethasone provided the best control of acute emesis [1].
  • Efficacy and tolerability of aprepitant for the prevention of chemotherapy-induced nausea and vomiting in patients with breast cancer after moderately emetogenic chemotherapy [2].
  • Aprepitant pharmacokinetic parameters in ESRD patients were clinically similar when haemodialysis was initiated at 4 hours or 48 hours after aprepitant administration [3].
  • Other adverse events experienced by aprepitant recipients include anorexia, constipation, diarrhoea, nausea (after day 5 of the study) and hiccups [4].
  • In one trial, there was a higher incidence of serious infection or febrile neutropenia in the aprepitant plus standard therapy arm than the standard therapy plus placebo arm; this was attributed to a pharmacokinetic interaction between aprepitant and dexamethasone [4].

Psychiatry related information on Aprepitant

  • RESULTS: In the first cycle, 64% of patients in the aprepitant group and 49% in the standard therapy group had a complete response [5].

High impact information on Aprepitant


Chemical compound and disease context of Aprepitant


Biological context of Aprepitant


Anatomical context of Aprepitant


Associations of Aprepitant with other chemical compounds


Gene context of Aprepitant

  • Collectively, these results indicated that aprepitant is both a substrate and a moderate inhibitor of CYP3A4 [18].
  • Aprepitant has been noted to produce modest decreases in plasma S(-)-warfarin concentrations, suggesting potential induction of CYP2C9 [24].
  • The contribution of human cytochrome P450 (P450) isoforms to the metabolism of aprepitant in humans was investigated using recombinant P450s and inhibition studies [18].
  • Furthermore, these behavioral effects were blocked by the selective NK1 receptor antagonist, MK-869 [25].
  • Lack of effect of aprepitant on hydrodolasetron pharmacokinetics in CYP2D6 extensive and poor metabolizers [26].

Analytical, diagnostic and therapeutic context of Aprepitant


  1. Prevention of cisplatin-induced emesis by the oral neurokinin-1 antagonist, MK-869, in combination with granisetron and dexamethasone or with dexamethasone alone. Campos, D., Pereira, J.R., Reinhardt, R.R., Carracedo, C., Poli, S., Vogel, C., Martinez-Cedillo, J., Erazo, A., Wittreich, J., Eriksson, L.O., Carides, A.D., Gertz, B.J. J. Clin. Oncol. (2001) [Pubmed]
  2. Efficacy and tolerability of aprepitant for the prevention of chemotherapy-induced nausea and vomiting in patients with breast cancer after moderately emetogenic chemotherapy. Warr, D.G., Hesketh, P.J., Gralla, R.J., Muss, H.B., Herrstedt, J., Eisenberg, P.D., Raftopoulos, H., Grunberg, S.M., Gabriel, M., Rodgers, A., Bohidar, N., Klinger, G., Hustad, C.M., Horgan, K.J., Skobieranda, F. J. Clin. Oncol. (2005) [Pubmed]
  3. Effect of impaired renal function and haemodialysis on the pharmacokinetics of aprepitant. Bergman, A.J., Marbury, T., Fosbinder, T., Swan, S., Hickey, L., Bradstreet, T.E., Busillo, J., Petty, K.J., Aiyer, K.J., Constanzer, M., Huskey, S.E., Majumdar, A. Clinical pharmacokinetics. (2005) [Pubmed]
  4. Aprepitant: a review of its use in the prevention of chemotherapy-induced nausea and vomiting. Dando, T.M., Perry, C.M. Drugs (2004) [Pubmed]
  5. Addition of the oral NK1 antagonist aprepitant to standard antiemetics provides protection against nausea and vomiting during multiple cycles of cisplatin-based chemotherapy. de Wit, R., Herrstedt, J., Rapoport, B., Carides, A.D., Carides, G., Elmer, M., Schmidt, C., Evans, J.K., Horgan, K.J. J. Clin. Oncol. (2003) [Pubmed]
  6. The oral neurokinin-1 antagonist aprepitant for the prevention of chemotherapy-induced nausea and vomiting: a multinational, randomized, double-blind, placebo-controlled trial in patients receiving high-dose cisplatin--the Aprepitant Protocol 052 Study Group. Hesketh, P.J., Grunberg, S.M., Gralla, R.J., Warr, D.G., Roila, F., de Wit, R., Chawla, S.P., Carides, A.D., Ianus, J., Elmer, M.E., Evans, J.K., Beck, K., Reines, S., Horgan, K.J. J. Clin. Oncol. (2003) [Pubmed]
  7. Lack of efficacy of the substance p (neurokinin1 receptor) antagonist aprepitant in the treatment of major depressive disorder. Keller, M., Montgomery, S., Ball, W., Morrison, M., Snavely, D., Liu, G., Hargreaves, R., Hietala, J., Lines, C., Beebe, K., Reines, S. Biol. Psychiatry (2006) [Pubmed]
  8. Human positron emission tomography studies of brain neurokinin 1 receptor occupancy by aprepitant. Bergström, M., Hargreaves, R.J., Burns, H.D., Goldberg, M.R., Sciberras, D., Reines, S.A., Petty, K.J., Ogren, M., Antoni, G., Långström, B., Eskola, O., Scheinin, M., Solin, O., Majumdar, A.K., Constanzer, M.L., Battisti, W.P., Bradstreet, T.E., Gargano, C., Hietala, J. Biol. Psychiatry (2004) [Pubmed]
  9. Characterization and quantitation of aprepitant drug substance polymorphs by attenuated total reflectance fourier transform infrared spectroscopy. Helmy, R., Zhou, G.X., Chen, Y.W., Crocker, L., Wang, T., Wenslow, R.M., Vailaya, A. Anal. Chem. (2003) [Pubmed]
  10. Contributions of Histamine, Prostanoids, and Neurokinins to Edema Elicited by Edema Toxin from Bacillus anthracis. Tessier, J., Green, C., Padgett, D., Zhao, W., Schwartz, L., Hughes, M., Hewlett, E. Infect. Immun. (2007) [Pubmed]
  11. The novel NK1 receptor antagonist MK-0869 (L-754,030) and its water soluble phosphoryl prodrug, L-758,298, inhibit acute and delayed cisplatin-induced emesis in ferrets. Tattersall, F.D., Rycroft, W., Cumberbatch, M., Mason, G., Tye, S., Williamson, D.J., Hale, J.J., Mills, S.G., Finke, P.E., MacCoss, M., Sadowski, S., Ber, E., Cascieri, M., Hill, R.G., MacIntyre, D.E., Hargreaves, R.J. Neuropharmacology (2000) [Pubmed]
  12. Effects of oral pregabalin and aprepitant on pain and central sensitization in the electrical hyperalgesia model in human volunteers. Chizh, B.A., Göhring, M., Tröster, A., Quartey, G.K., Schmelz, M., Koppert, W. British journal of anaesthesia (2007) [Pubmed]
  13. Effects of the neurokinin1 receptor antagonist aprepitant on the pharmacokinetics of dexamethasone and methylprednisolone. McCrea, J.B., Majumdar, A.K., Goldberg, M.R., Iwamoto, M., Gargano, C., Panebianco, D.L., Hesney, M., Lines, C.R., Petty, K.J., Deutsch, P.J., Murphy, M.G., Gottesdiener, K.M., Goldwater, D.R., Blum, R.A. Clin. Pharmacol. Ther. (2003) [Pubmed]
  14. Pharmacokinetics of aprepitant after single and multiple oral doses in healthy volunteers. Majumdar, A.K., Howard, L., Goldberg, M.R., Hickey, L., Constanzer, M., Rothenberg, P.L., Crumley, T.M., Panebianco, D., Bradstreet, T.E., Bergman, A.J., Waldman, S.A., Greenberg, H.E., Butler, K., Knops, A., De Lepeleire, I., Michiels, N., Petty, K.J. Journal of clinical pharmacology. (2006) [Pubmed]
  15. The metabolic disposition of aprepitant, a substance P receptor antagonist, in rats and dogs. Huskey, S.E., Dean, B.J., Doss, G.A., Wang, Z., Hop, C.E., Anari, R., Finke, P.E., Robichaud, A.J., Zhang, M., Wang, B., Strauss, J.R., Cunningham, P.K., Feeney, W.P., Franklin, R.B., Baillie, T.A., Chiu, S.H. Drug Metab. Dispos. (2004) [Pubmed]
  16. Aprepitant: a novel antiemetic for chemotherapy-induced nausea and vomiting. Massaro, A.M., Lenz, K.L. The Annals of pharmacotherapy. (2005) [Pubmed]
  17. Lack of effect of aprepitant on the pharmacokinetics of docetaxel in cancer patients. Nygren, P., Hande, K., Petty, K.J., Fedgchin, M., van Dyck, K., Majumdar, A., Panebianco, D., de Smet, M., Ahmed, T., Murphy, M.G., Gottesdiener, K.M., Cocquyt, V., van Belle, S. Cancer Chemother. Pharmacol. (2005) [Pubmed]
  18. Cytochrome P450 3A4 is the major enzyme involved in the metabolism of the substance P receptor antagonist aprepitant. Sanchez, R.I., Wang, R.W., Newton, D.J., Bakhtiar, R., Lu, P., Chiu, S.H., Evans, D.C., Huskey, S.E. Drug Metab. Dispos. (2004) [Pubmed]
  19. Role of neurokinin-1 receptor antagonists in chemotherapy-induced emesis: summary of clinical trials. Navari, R.M. Cancer Invest. (2004) [Pubmed]
  20. The role of biopharmaceutics in the development of a clinical nanoparticle formulation of MK-0869: a Beagle dog model predicts improved bioavailability and diminished food effect on absorption in human. Wu, Y., Loper, A., Landis, E., Hettrick, L., Novak, L., Lynn, K., Chen, C., Thompson, K., Higgins, R., Batra, U., Shelukar, S., Kwei, G., Storey, D. International journal of pharmaceutics. (2004) [Pubmed]
  21. Demonstration of the efficacy and safety of a novel substance P (NK1) receptor antagonist in major depression. Kramer, M.S., Winokur, A., Kelsey, J., Preskorn, S.H., Rothschild, A.J., Snavely, D., Ghosh, K., Ball, W.A., Reines, S.A., Munjack, D., Apter, J.T., Cunningham, L., Kling, M., Bari, M., Getson, A., Lee, Y. Neuropsychopharmacology (2004) [Pubmed]
  22. Aprepitant inhibits cyclophosphamide bioactivation and thiotepa metabolism. de Jonge, M.E., Huitema, A.D., Holtkamp, M.J., van Dam, S.M., Beijnen, J.H., Rodenhuis, S. Cancer Chemother. Pharmacol. (2005) [Pubmed]
  23. Aprepitant when added to a standard antiemetic regimen consisting of ondansetron and dexamethasone does not affect vinorelbine pharmacokinetics in cancer patients. Loos, W.J., de Wit, R., Freedman, S.J., Van Dyck, K., Gambale, J.J., Li, S., Murphy, G.M., van Noort, C., de Bruijn, P., Verweij, J. Cancer Chemother. Pharmacol. (2007) [Pubmed]
  24. Evaluation of potential inductive effects of aprepitant on cytochrome P450 3A4 and 2C9 activity. Shadle, C.R., Lee, Y., Majumdar, A.K., Petty, K.J., Gargano, C., Bradstreet, T.E., Evans, J.K., Blum, R.A. Journal of clinical pharmacology. (2004) [Pubmed]
  25. Centrally administered hemokinin-1 (HK-1), a neurokinin NK1 receptor agonist, produces substance P-like behavioral effects in mice and gerbils. Duffy, R.A., Hedrick, J.A., Randolph, G., Morgan, C.A., Cohen-Williams, M.E., Vassileva, G., Lachowicz, J.E., Laverty, M., Maguire, M., Shan, L.S., Gustafson, E., Varty, G.B. Neuropharmacology (2003) [Pubmed]
  26. Lack of effect of aprepitant on hydrodolasetron pharmacokinetics in CYP2D6 extensive and poor metabolizers. Li, S.X., Pequignot, E., Panebianco, D., Lupinacci, P., Majumdar, A., Rosen, L., Ahmed, T., Royalty, J.E., Rushmore, T.H., Murphy, M.G., Petty, K.J. Journal of clinical pharmacology. (2006) [Pubmed]
  27. Health outcomes and cost-effectiveness of aprepitant in outpatients receiving antiemetic prophylaxis for highly emetogenic chemotherapy in Germany. Lordick, F., Ehlken, B., Ihbe-Heffinger, A., Berger, K., Krobot, K.J., Pellissier, J., Davies, G., Deuson, R. Eur. J. Cancer (2007) [Pubmed]
  28. Differential involvement of neurotransmitters through the time course of cisplatin-induced emesis as revealed by therapy with specific receptor antagonists. Hesketh, P.J., Van Belle, S., Aapro, M., Tattersall, F.D., Naylor, R.J., Hargreaves, R., Carides, A.D., Evans, J.K., Horgan, K.J. Eur. J. Cancer (2003) [Pubmed]
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