 |
|
Success at last
Durant's compound became the lead, and after two years of hard work, an active antagonist called
burimamide was produced. Burimamide was not orally active and so a new analogue, metiamide, which was
orally active and ten times more potent, replaced it. The results of clinical trials with metiamide
begun in 1973 were impressive: ulcers were healed within three weeks. Unfortunately, metiamide gave rise
to a blood disorder called agranulocytosis as a side effect of treatment. This had been anticipated as a
possibility, so as an insurance policy, the team prepared a similar compound replacing the thiourea group
with a cyanoguanidine moiety. The new lead compound, cimetidine, passed every test with flying colors and in November 1976 was launched
as Tagamet® (derived from the anTAGonist and ciMETidine). Tagamet® was greeted with great enthusiasm by
doctors and patients alike. Ten years after its introduction, it had achieved sales of one billion dollars
and had become the world's number one prescription drug.
A new era of logical drug design |
Discovery of H2-receptor antagonists |
A new receptor
Success at last |
A better manufacturing process |
The people |
Landmark designation and acknowledgments
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