Compound GPHR-529 Pill: Advanced Pregnancy Prevention for Males

After successful tests in mice, the researchers hope to begin human trials in the year end. The medication could bring balance for contraceptive pill for both.

A team of research scientists said that they have developed a male oral contraceptive pill that didn’t cause observable side effects, with the drug expected to enter human trials by the end of 2022. It was found 99% effective in mice keeping them sterile for four to six weeks with seemingly no side effects.

The findings will be presented at the American Chemical Society’s Spring Meeting, and will mark a key step in expanding options for men. The initial compound was known as GPHR-529.

‘The large-scale IIb test of the gel is expected to be completed by the beginning of 2023, although additional tests will be required for FDA approval.’

Md Abdullah Al Noman, a graduate student at the University of Minnesota, told AFP that since the female contraceptive pill was first approved in the 1960s, researchers have been interested in a male equivalent.

"Multiple studies showed that men are interested in sharing the responsibility of birth control with their partners," he said — but until now, there have been only two effective options: condoms or vasectomies.

The female pill uses hormones to disrupt the menstrual cycle, and historical attempts at a male equivalent development targeting the male sex hormone testosterone. However, the problem with this approach is that it can cause side effects such as weight gain, depression and increased cholesterol levels.

To develop the non-hormonal drug, Noman, who works in Prof. Gunda Georg’s laboratory, targeted a protein called the "retinoic acid receptor (RAR) alpha."

Inside the body, vitamin A is converted into various forms, including retinoic acid, which plays an important role in cell growth, sperm formation and embryonic development. Retinoic acid must interact with RAR-alpha to perform these functions. But GPHR-529 prevents the interactions of this retinoic acid.

For their work, Noman and Georg developed a compound that inhibits the activity of RAR-alpha.

“Since men do not have to suffer the consequences of pregnancy, the threshold for side effects from birth control pills is rather low,” Noman said. “That’s why we’re trying to develop non-hormonal birth control pills to avoid hormonal side effects.”

So far, the compound "GPHR-529" seems to work as intended. Other research in animals has similarly shown that inhibiting RAR-α should be safe and effective at inducing temporary male sterility.

“This all looks promising so far. But clinical trials are the definitive test for the safety of any drug candidate,” Noman noted.

The team has licensed GPHR-529 to YourChoice Therapeutics for further development, and they hope to begin early phase clinical trials with the public later this year. If GPHR-529 does not pan out, the committee would still working additionally to improve their current perception and identify other hopeful candidates.

Elsewhere, the male conception gel NES/T, which lowers sperm and natural testosterone levels, but replenishes its own testosterone to reduce side effects. The large-scale IIb test of the gel is expected to be completed by the beginning of 2023, although additional tests will be required for FDA approval.

Source-Medindia