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Long-acting contraceptive agents: design of the WHO Chemical Synthesis Programme.

The great demand for improved long-acting injectable steroid contraceptives, particularly in developing countries, and the relative lack of interest from the pharmaceutical industry to develop such products stimulated WHO to launch a synthetic and screening programme to find improved, safe and acceptable injectable preparations. More than 210 esters of norethisterone (17 alpha-ethynyl-17 beta-hydroxyestr-4-en-3-one) and levonorgestrel (D-(-)-13 beta-ethyl-17 alpha-ethynyl-17 beta-hydroxygon-4-en-3-one) have been prepared in university-based research laboratories situated mainly in developing countries, and then screened by NICHHD in animal models. The following three compounds, levonorgestrel butanoate, cyclopropylcarboxylate and cyclobutylcarboxylate, proved to be particularly long-acting when administered as microcrystalline suspensions. The overall strategy of this research and development programme is described.[1]

References

  1. Long-acting contraceptive agents: design of the WHO Chemical Synthesis Programme. Crabbé, P., Archer, S., Benagiano, G., Diczfalusy, E., Djerassi, C., Fried, J., Higuchi, T. Steroids (1983) [Pubmed]
 
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