-Celmatix Inc., the leading women’s health biotechnology company focused on ovarian biology, today announced the identification of promising early leads in its latest drug program, aimed at developing the world’s first oral FSH receptor (FSHR) agonist drug. The innovative investigational product has the potential to revolutionize fertility treatments. The announcement coincides with the annual meeting of the European Society of Human Reproduction and Embryology (ESHRE), currently underway in Copenhagen, Denmark.

“Our goal is to eliminate the need for injections during ovarian stimulation ahead of egg freezing and IVF procedures,” said Dr. Piraye Yurttas Beim , Founder and CEO of Celmatix. “We also want to reduce the need for women to undergo IVF procedures in the first place, by both providing a more effective strategy for restoring ovulatory function in women with ovarian conditions like polycystic ovary syndrome (PCOS) and addressing the significant burden that male infertility places on couples by also advancing our program to help men increase their sperm count and viability.”

Infertility rates are rising rapidly: according to the CDC, nearly 1 in 5 married women (ages 18-49) in the United States experience infertility and 1 in 4 women in this group have difficulty carrying a pregnancy to term. Despite this, very little innovation has occurred in bringing novel fertility drugs to market.

“Hormone injections for treating infertility date back to studies first performed literally 100 years ago, at a time when the average life expectancy for a woman in the US was just 48,” explains Dr. Beim, “Now that women are living into their 80s, they naturally want to start and expand their families much later in their lives. That means that more women are proactively seeking egg freezing but also are increasingly relying on fertility treatments, including IVF, to get pregnant.”

Women undergo, on average, 60 injections across two treatment cycles to generate enough viable eggs to achieve a pregnancy. Injectable fertility drugs generate an estimated $5 billion dollars of sales for the pharmaceutical industry globally.

Dr. Beim continues, “We have heard for over a decade from both women and their doctors about the high burden of hormone injections, which are required for these procedures. Interestingly, the same hormone injections could be used to improve sperm quality in men and avoid IVF altogether for many couples with infertility; however, men have rejected the idea of undergoing months of painful injections. The burden of infertility treatment, therefore, disproportionately and unfairly falls on women. We also know that many women undergo IVF because current methods of improving ovulation for conditions like PCOS have low success rates. We knew that a simple pill that could eliminate injections from fertility treatments and provide alternatives to IVF would be a game changer.”

The Celmatix drug program benefits from recent advances in AI/computational methods for drug design and decades of publications in the field on the prior challenges of developing oral FSHR agonists. FSHR is a member of the G protein-coupled receptor (GPCR) family of proteins, which are among the most common class of targets for small, orally available therapeutic drugs. One challenge to developing oral drugs targeting FSHR has been that it is closely related to the receptor for thyroid hormone. Therefore, a successful oral FSHR drug must stimulate the FSH receptor without stimulating the thyroid hormone receptor (TSHR). Early Celmatix data suggests that their unique, rationally designed compounds overcome this significant hurdle to drug development for this target.

Celmatix Chief Scientific Officer, Dr. Stephen Palmer, notes, “We are very pleased to see that several of our novel compounds demonstrate the desired potency and selectivity required for a successful oral FSH drug. Furthermore, several of these early leads also demonstrate solubility and metabolic stability that are a 20-fold improvement compared to previously reported FSHR small molecule ligands. As we move these promising hits into lead optimization, we are hopeful to be on track to initiating clinical studies by 2025.”

Celmatix has previously announced pioneering drug development collaborations with industry leaders, its lead AMHR2 agonist program, aimed at optimizing ovarian health and making menopause a choice, and its novel melatonin agonist program for PCOS.