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Xenobiotica
the fate of foreign compounds in biological systems
Volume 40, 2010 - Issue 10
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Clinical Pharmacokinetics and Metabolism

Metabolism and excretion of [14C]taranabant, a cannabinoid-1 inverse agonist, in humans

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Pages 691-700 | Received 18 Jun 2010, Accepted 17 Jul 2010, Published online: 19 Aug 2010

References

  • Addy C, Cote J, Li S, Agrawal N, Majumdar A, Li H, Yuan J, Dunbar S, Lasseter K, Stoch A, Gottesdiener K, Wagner J. (2007). Taranabant plasma concentrations increased when co-administered with ketoconazole and diltiazem. Obes Program Abstract Suppl 15:A147–A148.
  • Addy C, Li S, Agrawal N, Stone J, Majumdar A, Zhong L, Li H, Yuan J, Maes A, Rothenberg P, Cote J, Rosko K, Cummings C, Warrington S, Boyce M, Gottesdiener K, Stoch A, Wagner J. (2008a). Safety, tolerability, pharmacokinetics, and pharmacodynamic properties of taranabant, a novel selective cannabinoid-1 receptor inverse agonist, for the treatment of obesity: results from a double-blind, placebo-controlled, single oral dose study in healthy volunteers. J Clin Pharmacol 48:418–427.
  • Addy C, Rothenberg P, Li S, Majumdar A, Agrawal N, Li H, Zhong L, Yuan J, Maes A, Dunbar S, Cote J, Rosko K, van Dyck K, De Lepeleire I, de Hoon J, van Hecken A, Depré M, Knops A, Gottesdiener K, Stoch A, Wagner J (2008b) Multiple-dose pharmacokinetics, pharmacodynamics, and safety of taranabant, a novel selective cannabinoid-1 receptor inverse agonist, in healthy male volunteers. J Clin Pharmacol 48:734–744.
  • Addy C, Wright H, Van Laere K, Gantz I, Erondu N, Musser BJ, Lu K, Yuan J, Sanabria-Bohórquez SM, Stoch A, Stevens C, Fong TM, De Lepeleire I, Cilissen C, Cote J, Rosko K, Gendrano IN 3rd, Nguyen AM, Gumbiner B, Rothenberg P, de Hoon J, Bormans G, Depré M, Eng WS, Ravussin E, Klein S, Blundell J, Herman GA, Burns HD, Hargreaves RJ, Wagner J, Gottesdiener K, Amatruda JM, Heymsfield SB. (2008c). The acyclic CB-1R inverse agonist taranabant mediates weight loss by increasing energy expenditure and decreasing caloric intake. Cell Metab 7:68–78.
  • Blundell JE, Jebb SA, Stiubbs RJ, Wilding JR, Lawton CL, Browning L, Whybrow S, Halford JCG. (2006). Effect of rimonabant on energy intake, motivation to eat and body weight with or without hypocaloric diet: the REBA study. Obes Rev 7(Suppl 2):104.
  • Breivogel CS, Childers SR. (1998). The functional neuroanatomy of brain cannabinoid receptors. Neurobiol Dis 5:417–431.
  • Di Marzo V, Goparaju SK, Wang L, Liu J, Bátkai S, Járai Z, Fezza F, Miura GI, Palmiter RD, Sugiura T, Kunos G. (2001). Leptin-regulated endocannabinoids are involved in maintaining food intake. Nature 410:822–825.
  • Fong TM, Guan XM, Marsh DJ, Shen CP, Stribling DS, Rosko KM, Lao J, Yu H, Feng Y, Xiao JC, Van der Ploeg LH, Goulet MT, Hagmann WK, Lin LS, Lanza TJ Jr, Jewell JP, Liu P, Shah SK, Qi H, Tong X, Wang J, Xu SS, Francis B, Strack AM, MacIntyre DE, Shearman LP. (2007). Antiobesity efficacy of a novel cannabinoid-1 receptor inverse agonist, N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-[[5-(trifluoromethyl)pyridin-2-yl]oxy]propanamide (MK-0364), in rodents. J Pharmacol Exp Ther 321:1013–1022.
  • Freedland CS, Poston JS, Porrino LJ. (2000). Effects of SR141716A, a central cannabinoid receptor antagonist, on food-maintained responding. Pharmacol Biochem Behav 67:265–270.
  • Hagmann WK. (2008). The discovery of taranabant, a selective cannabinoid-1 receptor inverse agonist for the treatment of obesity. Arch Pharm (Weinheim) 341:405–411.
  • Lin LS, Lanza TJ Jr, Jewell JP, Liu P, Shah SK, Qi H, Tong X, Wang J, Xu SS, Fong TM, Shen CP, Lao J, Xiao JC, Shearman LP, Stribling DS, Rosko K, Strack A, Marsh DJ, Feng Y, Kumar S, Samuel K, Yin W, Van der Ploeg LH, Goulet MT, Hagmann WK. (2006). Discovery of N-[(1S,2S)-3-(4-Chlorophenyl)-2- (3-cyanophenyl)-1-methylpropyl]-2-methyl-2- {[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide (MK-0364), a novel, acyclic cannabinoid-1 receptor inverse agonist for the treatment of obesity. J Med Chem 49:7584–7587.
  • Reddy VBG, Doss G, Karanam BV, Samuel K, Lanza T, Lin L, Yu N, Zhang A, Raab C, Stearns R, Kumar S. (2010). l. In vitro and in vivo metabolism of a cannibinoid-1 receptor inverse agonist, taranabant, in rats and monkeys. Xenobiotica (In Press).
  • Schwartz MW, Porte D Jr. (2005). Diabetes, obesity, and the brain. Science 307:375–379.

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