Harnie Gold
Member
Scientist in the US, working on male contraceptive pill (medication to prevent a man impregnanting a woman) have reported to have developed an oral non-hormonal contraceptive for man.
The result of the trial was presented by researchers from the University of Minnesota on Wednesday March 23, 2022, at the spring meeting of the American Chemical Society (ACS), the research, for male contraceptive pill was carried out on mice and it effectively prevented pregnancy without obvious side-effects.
Gunda Georg, head of the medicinal chemistry department at the university in a statement said the testing of the pill — YCT529 — was found to be “99 percent effective in mice” and the human clinical trials, will 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.
While women can prevent pregnancy in different ways which includes pills or intrauterine devices, men are only limited to single-use condoms or through vasectomies and whereas the use of condom is less expensive and very affordable for most men, vasectomy is not and it is mostly considered irreversible although there is an expensive surgical procedure that can reverse it yet, success is not guaranteed.
DrNoman, a graduate student in the Gunda Georg laboratory at the University of Minnesota, said "We wanted to develop a non-hormonal male contraceptive to avoid these side effects".
To develop a non-hormonal drug, Noman, who works in the lab of Professor Gunda Georg, targeted a protein called "retinoic acid receptor (RAR) alpha."
"If we know what the keyhole looks like, then we can make a better key -- that's where the computational model comes in," said Noman.
The funding for the research, was from the National Institutes of Health and the Male Contraceptive Initiative, the institute is also working with a company called YourChoice Therapeutics to start human trials by the third or fourth quarter of 2022, said Georg.
"I'm optimistic this will move forward quickly," she said, envisaging a possible timeline to market in five years or under.
"There is no guarantee that it will work...but I would really be surprised if we didn't see an effect in humans as well," she added.
The statement below:
“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.
“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.”