The Untapped Potential Of Antiobesity Drugs

Christian Fat Loss

Best Weight Loss Programs That Work

Get Instant Access

The large potential market and the shortage of safe, efficacious compounds is driving many researchers to undertake the difficult task of creating new anti-obesity drugs. Overall the track record of the pharmaceutical industry has been poor in this area, but the recent explosion in our understanding of the biology of obesity has changed the drug discovery landscape. The identification of a multitude of new targets for obesity therapeutics, and a deeper understanding of existing targets, has increased our potential for finding the "right" focus for increasing efficacy. And while there is a higher sensitivity for safety in anti-obesity therapeutics then that for cancer

therapeutics, there is also a greater understanding of the health and financial consequences of this unmet medical need. While the potential of anti-obesity drugs currently remains largely untapped, the industry should be optimistic about the finding solutions to these dual issues In the future.


  1. K.M. Flegal, M.D. Carroll, C.L. Ogden and C.L. Johnson, JAMA, 288,1723, (2002).
  2. D.B. Allison, K.R. Fontaine, J.E. Manson and T.B. Vanltallie, JAMA, 282,1530, (1999).
  3. A.H. Mokdad, E.S. Ford, B.A. Bowan, W.H. Dietz, F. Vinicor, V.S. Bales and J.S. Marks, JAMA, 289, 76, (2003).
  4. D. Thompson and A.M. Wolf, Obesity Rev., 2, 189 (2001).
  5. C. Farrigan and K. Pang, Nature Rev., 1, 257, (2002).
  6. A M. Mclntyre, J.R.Soc.Health, 118, 76, (1998).
  7. A. Halpern and M.C. Mancini, Obesity Rev., 4, 25, (2003).
  8. J.F. Fernandez-Lopez, X. Remesar, M. Foz and M. Alemany, Drugs, 62, 915 (2002).
  9. N. Finer, Best Prac. & Res. Clin. Endo. And. Meta., 16, 717 (2002).
  10. G. Glazer, Arch. Intern. Med., 161.1814, (2001).
  11. H. Bays and C. Dujovne, Expert.Opin.lnvestig.Drugs, H, 1189, (2002).
  12. D.P. Hurst, D.L. Lynch, J. Barnett-Norris, S.M. Hyatt, H.H. Seltzman, M. Zhong, J. Nie, D. Lewis and P.H. Reggio, Mol.Pharmacol., 62,1274, (2002).
  13. M. Arnone, J. Maruani, F. Chaperon, M.H. Thiebot, M. Poncelet, P. Soubrie and G. Le Fur, Psychopharm. 132,104 (1997).
  14. R. Gomez, M. Navarro, B. Ferrer, J.M. Trigo, A. Bilbao, I. Del Arco, A. Cippitelli, F. Nava, D. Piomelli and F. Rodriguez de Fonseca, J.Neurosci., 22, 9612, (2002).
  15. M.E. Francisco, H.H. Seltzmann, A.F. Gilliam, R.A.Mitchell, S.L. Rider, R.G. Pertwee, L.A. Stevenson and B.F. Thomas, J.Med.Chem., 45, 2708, (2002).
  16. R. Katoch-Rouse, O.A. Pavlova, T. Vaulder, A.F. Hoffman, A.G. Mukhin and A.G. Horti, J.Med.Chem., 46, 642 (2003).
  17. A.R. Stoit, J.H. Lange, A.P. Hartog, E. Ronken, K. Tipker, H.H. Stuivenberg, J.A. Dijksman, H.C. Wals and C.G. Kruse, Chem Pharm. Bull., 50,1109, (2002).
  18. J. Shim, W.J. Welsh, E. Cartier, J.L. Edwards and A.C. Howlett, J.Med.Chem. 45, 1447, (2002).
  19. M. Habeck, DTT, 7, 280, (2002).
  20. J. Häkkinen, R.M. Horak and V. Maharaj, U.S. Patent US 6,488,967 B1 (2002).
  21. I.D. Rubin, M.A. Cawthorne and J.S. Brindra, Eur. Patent Application EP 1 166 792 A2 (2001).
  22. J.P. Fandl and N. Stahl, Eur. Patent EP 1 056 856 B1 (2002).
  23. T. Gura, Science, 299, 849, (2003).
  24. V.E.F. Crowley, G.S.H. Yeo and S. O'Rahilly, Nature Rev., 1, 276, (2002).
  25. D.J. MacNeil, A.D. Howard, X. Guan, T.M. Fong, R.P. Nargund, M.A. Bednarek, M.T. Goulet, D.H. Weinberg, A.M. Strack, D.J. Marsh, et al., Eur.J.Pharmacol., 450, 93, (2002).
  26. I.K. Sebhat, W.J. Martin, Z. Ye, K. Barakat, R.T. Moseley, D.B. Johnston, R. Bakshi, B. Palucki, D.H. Weinberg, T. MacNeil et al., J.Med.Chem., 45,4589, (2002).
  27. F. Mutulis, I. Mutule, and J. E. S. Wikberg, Bioorg. Med. Chem. Letters, 12,1039, (2002).
  28. P.Renhowe, et al., PCT Int. Appl. (2002), 145 pp. WO 02/18327 A2
  29. M.P. Maguire, M. Dai, and T.J. Vos, WO 02/062766 A2
  30. K. Pan, M.K. Scott, D.H. Lee, L.J. Fitzpatrick, J.J. Cooke, R.A. Rivero, D.I. Rosenthal, A.H. Vaidya, B. Zhao, A.B. Reitz, Bioorg. Med. Chem. H, 185, (2003).
  31. W.J. Martin, E. MacGowan, D.E. Cashen, L.T. Gantert, J.E. Drisko, G.J. Horn, R. Nargund, I. Sebhat, A.D. Howard, L.H. Van der Ploeg and D.E. Maclntyre, Eur.J.Pharmacol., 454, 71, (2002).
  32. E. Parker, M. Van Heek and A. Stamford, Eur.J.Pharmacol., 440, 173, (2002).
  33. B.L. Largent, A. J. Robichaud and K. J. Miller, Ann. Reports Med. Chem., 37,1, (2002).
  34. R.L. Batterham, M.A. Cowley, C.J. Small, H. Herzog, M.A. Cohen, C.L. Dakin, A.M. Wren, A.E. Brynes, M.J. Low, M.A. Ghatei, R.D. Cone and S.R. Bloom, Nature, 418, 650 (2002).
  35. M.H. Block, S. Boyer, W. Brailsford, D.R. Brittain, D. Carroll, S. Chapman, D.S. Clarke, C.S. Donald, K.M. Foote, L. Godfrey, etal., J.Med.Chem., 45, 3509, (2002).
  36. N. Sato, T. Takahashi, T. Shibata, Y. Haga, A. Sakuraba, M. Hirose, M. Sato, K. Nonoshita, Y. Koike, H. Kitazawa, etal., J.Med.Chem., 46, 666, (2003).
  37. A.J. Daniels, M. K. Grizzle, R. P. Wiard, J. E. Matthews and D. Heyer, Regul. Peptides, 106, 47, (2002).
  38. T.O. Johnson, J. Ermolieff and M. R. Jirousek, Nature Rev., 1,696, (2002).
  39. M. Elchebly, P. Payette, E. Michaliszyn, W. Cromlish, S. Collins, A.L. Loy, D. Normandin, A. Cheng, J. Himms-Hagen, C.C. Chan, etal., Science, 283,1544 (1999).
  40. J.H. Ahn, S.Y. Cho, J.D. Ha, S.Y. Chu, S.H. Jung, Y.S. Jung, J.Y. Baek, I.K. Choi, E.Y. Shin, S.K. Kang etal.,, Bioorg. Med. Chem. Letters, 12,1941, (2002).
  41. C. Liljebris, J. Martinsson, L. Tedenborg, M. Williams, E. Barker, J.E. Duffy, A. Nygren and S. James, Bioorg. Med. Chem., 10, 3197, (2002).
  42. G. Hum, J. Lee and S. D. Taylor, Med. Chem. Letters, 12, 3471 (2002).
  43. H.S. Andersen, O.H. Olsen, L.F. Iversen, A.L. Soresen, S.B. Mortensen, M.S. Christensen, S. Branner, T.K. Hansen, J.F. Lau, L. Jeppesen, et al., J.Med.Chem., 45, 4443, (2002).
  44. C. Forray, Current Opinion in Pharm., 3,85, (2003).
  45. Y. Chen, C. Hu, C.K. Hsu, Q. Zhang, C. Bi, M. Asnicar, H.M. Hsiung, N. Fox, L.J. Slieker, D.D. Yang, M.L. Heiman and Y. Shi, Endocrinology, 143,2469, (2002).
  46. D.J. Marsh, D.T. Weingarth, D.E. Novi, H.Y. Chen, M.E. Trumbauer, A.S. Chen, X.-M. Guan, M.M. Jiang, Y. Feng, R.E. Camacho et al., Proc.Natl.Acad.Sci. U.S.A., 99, 3240, (2002).
  47. S. Takekawa, A. Asami, Y. Ishihara, J. Terauchi, K. Kato, Y. Shimomura, M. Mori, H. Murakoshi, K. Kato, N. Suzuki, O. Nishimura and M. Fujino, Eur.J. Pharmacol., 438, 129, (2002).
  48. B. Borowsky, M.M. Durkin, K. Ogozalek, M.R. Marzabadi, J. DeLeon, B. Lagu, R. Heurich, H. Lichtblau, Z. Shaposhnik, I. Daniewska, et al., Nature Med., 8, 825, (2002).
  49. M. Krotkiewski, Eur.J.Pharmacol., 440, 85, (2002).
  50. J.R.S Arch, Eur.J.Pharmacol., 440, 99, (2002).
  51. D.W. Lee, M. C. Leinung, M. Rozhavskaya-Arena and P. Grasso, Eur.J.Pharmacol., 440. 129, (2002).
  52. P.J. Larsen, N. Vrang, M. Tang-Christensen, P.B. Jensen, A. Hay-Schmidt, J. Romer, L. Bjerre-Knudsen and P. Kristensen, Eur.J.Pharmacol., 440,159, (2002).
  53. D. Richard, Q. Lin and E. Timofeeva, Eur.J.Pharmacol., 440,189, (2002).
  54. D. Smart, A.C. Haynes, G. Williams and J.R.S. Arch, Eur.J.Pharmacol., 440,199, (2002).
  55. T.Tsao, H.F. Lodish and J. Fruebis, Eur.J.Pharmacol., 440, 213, (2002).
  56. G. Muccioli, M. Tschop, M. Papotti, R. Deghenghi, M. Heiman and E. Ghigo, Eur.J.Pharmacol., 440, 235, (2002).
  57. A.L. Gundlach, Eur.J.Pharmacol., 440, 255, (2002).
  58. J.J. Meiet, B. Gallwitz, W. E. Schmidt and M.A. Nauck, Eur.J.Pharmacol., 440, 269, (2002).
  59. K. Yamada, E. Wada, Y. Santo-Yamada and K. Wada, Eur.J.Pharmacol., 440, 281, (2002).
  60. B. Rolin, M.O. Larsen, C.F. Gotfredsen, C.F. Deacon, R.D. Carr, M. Wilken and L.B. Knudsen, Am.J.PhysioI.Endocrinol. Metab., 283- E745, (2002).
  61. H. Agerso, L.B. Jensen, B. Elbrond, P. Rolan and M. Zdravkovic, Diabetologia, 45, 195, (2002).
  62. D.M. Wilson, A.P. Termin, L. Mao, M.M. Ramirez-Weinhouse, V. Molteni and P.D.J. Grootenhuis, J.Med.Chem., 45,2123, (2002).
  63. K. Saar, A.M. Mazarati, R. Mahlapuu, G. Hallnemo, U. Soomets, K. Kilk, S. Hellberg, M. Pooga, B.R. Tolf, T.S. Shi et al., Proc.Natl.Acad.Sci.U.S.A., 99, 7136, (2002).
  64. K.N. Hewitt, M.D. Lee, C.T. Dourish and P.G. Clifton, Pharmacol, Biochem Behav, 71. 691, (2002).

Was this article helpful?

0 0
Quick Weight Loss Action

Quick Weight Loss Action

Why Indulge In Self-Pity When You Can Do Something About Your Weight Now. Say Goodbye to Your Weight Problems That Have Only Make Your Life Nothing But Miserable. Have you often felt short-changed because of your weight or physical appearance?

Get My Free Ebook

Post a comment