Taranabant Explained

Taranabant (codenamed MK-0364) is a cannabinoid receptor type 1 (CB1) inverse agonist that was investigated as a potential treatment for obesity due to its anorectic effects.[1] [2] It was discovered by Merck & Co.

In October 2008, Merck has stopped its phase III clinical trials with the drugs due to high level of central nervous system side effects, mainly depression and anxiety.[3] [4] [5] [6]

See also

Notes and References

  1. Armstrong HE, Galka A, Lin LS, Lanza TJ Jr, Jewell JP, Shah SK . etal . 2007 . Substituted acyclic sulfonamides as human cannabinoid-1 receptor inverse agonists . Bioorganic & Medicinal Chemistry Letters . 17 . 8. 2184–7 . 10.1016/j.bmcl.2007.01.087 . 17293109 .
  2. Fong TM, Guan XM, Marsh DJ, Shen CP, Stribling DS, Rosko KM . etal . Jun 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 . Journal of Pharmacology and Experimental Therapeutics . 321 . 3. 1013–22 . 10.1124/jpet.106.118737 . 17327489 . 20001781 .
  3. Web site: Press release by Merck . 4 October 2008.
  4. Aronne LJ, Tonstad S, Moreno M, Gantz I, Erondu N, Suryawanshi S, Molony C, Sieberts S, Nayee J, Meehan AG, Shapiro D, Heymsfield SB, Kaufman KD, Amatruda JM . A clinical trial assessing the safety and efficacy of taranabant, a CB1R inverse agonist, in obese and overweight patients: a high-dose study . International Journal of Obesity . 34 . 5 . 919–35 . May 2010 . 20157323 . 10.1038/ijo.2010.21 . 6769554 .
  5. Kipnes MS, Hollander P, Fujioka K, Gantz I, Seck T, Erondu N, Shentu Y, Lu K, Suryawanshi S, Chou M, Johnson-Levonas AO, Heymsfield SB, Shapiro D, Kaufman KD, Amatruda JM . A one-year study to assess the safety and efficacy of the CB1R inverse agonist taranabant in overweight and obese patients with type 2 diabetes . Diabetes, Obesity & Metabolism . 12 . 6 . 517–31 . June 2010 . 20518807 . 10.1111/j.1463-1326.2009.01188.x . 23886192 .
  6. Proietto J, Rissanen A, Harp JB, Erondu N, Yu Q, Suryawanshi S, Jones ME, Johnson-Levonas AO, Heymsfield SB, Kaufman KD, Amatruda JM . A clinical trial assessing the safety and efficacy of the CB1R inverse agonist taranabant in obese and overweight patients: low-dose study . International Journal of Obesity . 34 . 8 . 1243–54 . August 2010 . 20212496 . 10.1038/ijo.2010.38 . 23352608 .

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