Tamsulosin (Harnal, Flomax, OMNIC)

Breakthrough Drug that Drastically Changed the Treatment of Prostatic Hyperplasia


Tamsulosin hydrochloride (Harnal) is a drug for dysuria associated with prostatic hyperplasia that was developed by Yamanouchi Pharmaceutical Co., Ltd. It works by blocking adrenergic α1-adrenoceptors. Dysuria covers a variety of urogenital issues, including prostatic hyperplasia, polyuria, and urinary incontinence. Among these conditions, tamsulosin is effective at reducing dysuria caused by hypertrophy of the prostatic gland. Tamsulosin is prescribed as a once-daily dose and has transformed prostate hyperplasia therapy. Indeed, tamsulosin is both a first-in-class and best-in-class drug that has dominated market share. The research and development (R&D) process for tamsulosin was distinctive in two ways. First, R&D into tamsulosin did not originally begin with the intent of creating a drug to treat dysuria. In fact, a new application of an already-known compound originally developed as an antihypertensive drug was discovered as a result of unauthorized research. Second, continued R&D into tamsulosin led to progress in the scientific understanding of the mechanism of action in the prostate, which was clarified by an academia–industry collaboration.


  1. Asano, M., & Takenaka, T. (2010). Drugs for the treatment of urinary disorders associated with prostate hypertrophy-harnal. Laboratory Medicine, 28(18), 3035–3040.Google Scholar
  2. Barnes, E. M., Langer, S. Z., & Weiner, N. (1974). Release of norepinephrine and dopamine-β-hydroxylase by nerve stimulation. I. Role of neuronal and extraneuronal uptake and of alpha presynaptic receptors. Journal of Pharmacology and Experimental Therapeutics, 190(3), 431–450.Google Scholar
  3. Caine, M., Raz, S., & Zeigler, M. (1975). Adrenergic and cholinergic receptors in the human prostate, prostatic capsule and bladder neck. British Journal of Urology, 47(2), 193–202.CrossRefGoogle Scholar
  4. Edvardsen, P., & Setekleiv, J. (1968). Distribution of adrenergic receptors in the urinary bladder of cats, rabbits and guinea-pigs. Acta Pharmacologica et Toxicologica, 26(5), 437–445.CrossRefGoogle Scholar
  5. Heisei Chozai Yakkyoku. (2013). Use of major α1-blockers and 5α-reductase inhibitors in benign prostatic hypertrophy. Accessed March 14, 2016.
  6. Hoffman, B. B., Lefkowitz, R. J. (1990) Goodman and Gilman’s the pharmacological basis of therapeutics (8th ed., p. 221). Pergamon Press.Google Scholar
  7. Honda, K., Miyata-Osawa, A., & Takenaka, T. (1985). alpha 1-Adrenoceptor subtype mediating contraction of the smooth muscle in the lower urinary tract and prostate of rabbits. Naunyn-Schmiedeberg’s Archives of Pharmacology, 330(1), 16–21.CrossRefGoogle Scholar
  8. Honda, K., & Nakagawa, C. (1986). Alpha-1 adrenoceptor antagonist effects of the optical isomers of ym-12617 in rabbit lower urinary-tract and prostate. Journal of Pharmacology and Experimental Therapeutics, 239(2), 512–516.Google Scholar
  9. Honda, Kazuo. (2006). Tamsulosin hydrochloride inventory. Chemistry and Education, 54(3), 134–137.Google Scholar
  10. Kawabe, K., Ueno, A., Takimoto, Y., Aso, Y., & Kato, H. (1990a). Use of an α1-blocker, YM617, in the treatment of benign prostatic hypertrophy. Journal of Urology, 144(4), 908–911.CrossRefGoogle Scholar
  11. Kawabe, K., Seishi, U., Naitsu, T., Kato, A., & Kitagawa, R. (1990b). Optimal dose setting test of YM617 for urination disorder associated with prostatic hypertrophy. Urology Surgery., 3, 1247–1259.Google Scholar
  12. Kawai, K., Ueno, S., Nakamoto, T., Kato, J., Kitagawa, R., Imamura, K., Oshima, H., et al. (1991). Clinical evaluation of YM617 for dysuria associated with benign prostatic hyperplasia (in Japanese). Urological Surgery, 4, 231–242.Google Scholar
  13. Kunisawa, Y., Kawabe, K., Niijima, T., Honda, K., & Takenaka, T. (1985). A pharmacological study of alpha adrenergic receptor subtypes in smooth muscle of human urinary bladder base and prostatic urethra. The Journal of Urology, 134(2), 396–398.CrossRefGoogle Scholar
  14. Langer, Salomón Z. (1974). Presynaptic regulation of catecholamine release. Biochemical Pharmacology, 23(13), 1793–1800.CrossRefGoogle Scholar
  15. Minneman, Kenneth P. (1988). Alpha 1-adrenergic receptor subtypes, inositol phosphates, and sources of cell Ca2+. Pharmacological Reviews, 40(2), 87–119.Google Scholar
  16. Nishiura, M., Mizumoto, T. (2008). Modified-release fast-disintegrating tablet (Harnal D) containing fine, modified-release particles. Drug Delivery System, 23(1), 77–80.Google Scholar
  17. Sarma, A. V., Jacobson, D. J., McGree, M. E., Roberts, R. O., Lieber, M. M., & Jacobsen, S. J. (2005). A population based study of incidence and treatment of benign prostatic hyperplasia among residents of Olmsted County, Minnesota: 1987 to 1997. The Journal of Urology, 173(6), 2048–2053.CrossRefGoogle Scholar
  18. Sako, K. (2006). Current status and issues in drug discovery: Pharmaceutical products. In Symposium of Banyu Life Science Foundation, Public Interest Incorporated Foundation. Accessed March 14, 2016.Google Scholar
  19. Shintani, Fujio, Hayashi, Masahiro, & Hanano, Manabu. (1978). Transition of plasma concentration of prazosin hydrochloride and its efficacy and subjective symptoms (in Japanese). Clinical and Research, 55, 4037–4044.Google Scholar
  20. Sudo, K., Inagaki, O., Asano, M. (1990). The Japanese Journal of Pharmacology, 52, 131.Google Scholar
  21. Suto, Katsumi, & Takenaka, Toichi. (1993). How to proceed to medical care for the elderly-concerning the α-receptor subtype for benign prostatic hypertrophy. New Drug and Treatment, 43(4), 15.Google Scholar
  22. Taguchi, K., Saitoh, M., Sato, S., Asano, M., & Michel, M. C. (1997). Effects of tamsulosin metabolites at alpha-1 adrenoceptor subtypes. Journal of Pharmacology and Experimental Therapeutics, 280(1), 1–5.Google Scholar
  23. Takenaka, T. (2010). Legends in urology. The Canadian Journal of Urology, 17(5), 5345.Google Scholar
  24. Takenaka, T. (2015). Drug discovery and medical history of tamsulosin (Harnal) (in Japanese). Journal of Clinical and Experimental Medicine, 252(4), 323–325.Google Scholar
  25. Takenaka, Toichi. (2011). From drug discovery to management. Pharmacia\, 47(4), 291–293.Google Scholar
  26. Takenaka, T., Fujikura, S., Honda, K., Asano, M., & Niigata, K. (1995). R&D of a novel α1-receptor blocker, tamsulosin hydrochloride. Pharmaceutical Journal, 115(10), 773–789.Google Scholar
  27. Tsukazaki, A. (2014). Drugs by samurai: Part II, aiming at drug discovery from Japan Part II, Tamsulosin hydrochloride (in Japanese). Medical Asahi, 74–77.Google Scholar
  28. Yamada, S., Suzumi, M., Tanaka, C., Mori, R., Kimura, R., Inagaki, O., et al. (1994). Comparative-study on alpha(1)-adrenoceptor antagonist binding in human prostate and aorta. Clinical and Experimental Pharmacology and Physiology, 21(5), 405–411.CrossRefGoogle Scholar
  29. Yamanouchi Pharmaceutical. (1975). Yamanouchi 50 years. Yamanouchi Pharmaceutical.Google Scholar
  30. Yoshida, S., Hideo, T., Hidaka, Y., Okada, K., Akino, Y., Isomatsu, K., Fukuyama, T., et al. (1991) Efficacy and safety in the long-term administration of YM617 for patients with lower urinary tract transit disorder. Urology of Urology, 37(4), 421–429.Google Scholar

Copyright information

© Springer Nature Singapore Pte Ltd. 2019

Authors and Affiliations

  1. 1.CEAFJP/EHESSParisFrance
  2. 2.Faculty of EconomicsHitotsubashi UniversityTokyoJapan
  3. 3.Medical Affairs, Medical Science Liaison, MSD K.K.TokyoJapan
  4. 4.Faculty of Business AdministrationTohoku Gakuin UniversityMiyagiJapan

Personalised recommendations