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Cimetidine was first marketed in the United Kingdom in 1976, and in the . in August 1977; therefore, it took 12 years from initiation of the H 2 receptor antagonist program to commercialization. By 1979, Tagamet was being sold in more than 100 countries and became the top-selling prescription product in the ., Canada, and several other countries. In November 1997, the American Chemical Society and the Royal Society of Chemistry in the . jointly recognized the work as a milestone in drug discovery by designating it an International Historic Chemical Landmark during a ceremony at SmithKline Beecham's New Frontiers Science Park research facilities in Harlow, England. [50]

Flutamide acts as a selective, competitive , silent antagonist of the androgen receptor (AR). [1] Its active metabolite , 2-hydroxyflutamide , has between 10- to 25-fold higher affinity for the AR than does flutamide, and hence is a more powerful antiandrogen in comparison. [1] [21] [46] [47] However, at high concentrations, unlike flutamide, 2-hydroxyflutamide is able to weakly activate the AR. [1] [48] Flutamide has far lower affinity for the AR than do steroidal antiandrogens like spironolactone and cyproterone acetate, and it is a relatively weak antiandrogen in terms of potency by weight, but the large dosages at which flutamide is used appear to compensate for this. [49] In accordance with its selectivity for the AR, flutamide possesses no progestogenic , (direct) estrogenic , glucocorticoid , or antigonadotropic activity. [25] [50] Similarly to nilutamide, bicalutamide, and enzalutamide , flutamide crosses the blood-brain-barrier and exerts central antiandrogen actions. [51]

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