Scientists in the United States (US) say they have developed
a non-hormonal contraceptive pill for males.
The researchers from the University of Minnesota presented
the results of their trial on Wednesday at the spring meeting of the American
Chemical Society (ACS).
There are currently two effective birth control options for
men — condoms and vasectomy.
According to a statement issued on the pill, Gunda Georg,
head of the medicinal chemistry department at the university, said testing of
the pill — YCT529 — which was found to be “99 percent effective in mice”, will
be used in human clinical trials to begin in the third or fourth quarter of
2022.
“Because it can be difficult to predict if a compound that
looks good in animal studies will also pan out in human trials, we’re currently
exploring other compounds as well,” Georg said.
A statement by the ACS also noted that the pill, which
limits chances of impregnating females, loses effect when no longer taken.
“To develop their non-hormonal male contraceptive, the
researchers targeted a protein called the retinoic acid receptor alpha (RAR-α).
This protein is one of a family of three nuclear receptors that bind retinoic
acid, a form of vitamin A that plays important roles in cell growth,
differentiation (including sperm formation) and embryonic development,” the
statement reads.
“Knocking out the RAR-α gene in male mice makes them
sterile, without any obvious side effects. Other scientists have developed an
oral compound that inhibits all three members of the RAR family (RAR-α, -β and
-γ) and causes reversible sterility in male mice, but Georg’s team and their
reproductive biology collaborators wanted to find a drug that was specific for
RAR-α and therefore less likely to cause side effects.
“So the researchers closely examined crystal structures of
RAR-α, -β and -γ bound to retinoic acid, identifying structural differences in
the ways the three receptors bind to their common ligand.
“With this information, they designed and synthesized
approximately 100 compounds and evaluated their ability to selectively inhibit
RAR-α in cells. They identified a compound, which was named YCT529, that
inhibited RAR-α almost 500 times more potently than it did RAR-β and -γ.
“When given orally to male mice for 4 weeks, YCT529
dramatically reduced sperm counts and was 99% effective in preventing
pregnancy, without any observable side effects. The mice could father pups
again 4-6 weeks after they stopped receiving the compound.”
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