The year 2024 was quietly eventful for our company. We received funding from Capital-K, a venture capital fund in Mountain View, CA. in April, 2024. Since then, we accelerated our efforts on three fronts:

1. The optimization of MF5 our estrogen receptor beta (ERβ) selective agonist drug for the treatment of menopausal symptoms and the prevention of breast cancer.
2. The optimization of BZL2 our glycolysis inhibitor/ PARP1 activator drug for the treatment of solid tumors and more specifically triple negative breast cancer.
3. The optimization of MD1 our first in class nuclear receptor reprogramming drug for the treatment of menopausal metabolic syndrome and the prevention of Type 2 Diabetes in menopausal women.

Iaterion is determined to advance novel therapies to the sadly neglected field of Women’s medicine. The proportion of diseases affected specifically or mostly by women is 56%. Despite that, the share of assets in the current healthcare pipeline focused on female conditions is only 5%. Although there are more efforts from within the healthcare and advocate communities to increase the funding and accelerate innovation in the field of Women’s Health, the industry is slow to include the entire field in their strategic outlook.
Our initial focus is on aging women’s issues, related to the biologically unique feature of female human mammalians undergoing menopause and unlike any animal in nature living a third of their life in menopause.

MF5

MF5 is our lead product for the treatment of menopausal symptoms such hot flashes, nighttime awakening and mood changes. Unlike current menopause hormone therapies (MHT) MF5 will not increase the risk of breast and uterine cancer. MF5 has the potential of serving millions of women suffering from menopausal symptoms world-wide.
In the past year we were able to optimize the chemistry of the drug. We significantly improved the drug potency (we need a far lower dose) and the drug selectivity toward the ERβ. This improvement will result in lower dose necessary to reach greater activity and reduce any safety concerns. We were also able to show the potent compounds are bioavailable with oral administration.
The next steps are to select the final single compound that demonstrates greatest efficacy, safety and bioavailability in animal studies. Following that step we will engage with the FDA on the future development plan for MF5 throughout the clinical development stage.

BZL2

We previously published that compounds identified in BZL101 selectively inhibit glycolysis in cancer cells and not in normal cells, resulting in selectively killing cancer cells with no damage to normal cells. We also showed that this process is initiated by activation of poly (ADP-ribose) polymerase 1 (PARP1) a nuclear enzyme involved in sensing DNA damage and DNA repair.
We initiated studies for the optimization of the compounds. The first steps were to involve AI aided computational modeling of the relationship of the compounds and PARP1. These studies demonstrate a close binding affinity and activation of the protein. The next steps involve AI generated medicinal chemistry of analogs, the synthesis and biological testing of the activity. We also initiated in depth structural studies of the mechanisms of BZL2 initiating the cancer selective killing effect.
Discussion with the FDA will take place following the final candidate drug selection following animal studies.

MD1

MD1 is based on the unique discovery Iaterion made in the field of nuclear receptors (the main hormone receptors such as estrogen, progesterone, testosterone, thyroid and glucocorticoids). The canonical model in biology is that protein nuclear receptors are regulated by a single compound (ligand) binding at a unique binding site in the ligand binding domain. The unique, almost singular, structure of this domain allows interaction with only specific chemical structures. We discovered a unique set of compounds that bind to the estrogen receptor alpha (ERα) that on their own result in no regulating activity, but when combined with the natural hormone, estrogen, they significantly modify estrogens activity. We termed these Co-ligand compounds nuclear receptor reprogramming (NRRP) drugs. This discovery changes the canonical model, where now at least two compounds can co-bind to the receptor and result in modification of the biological outcomes. This discovery may result in a new field in molecular toxicology, potentially explaining why, beyond differences in genetics and metabolism, people experience dramatic differences when exposed to drugs.
We are in the process of optimizing these compounds to result in greater potency, selectivity and desired programming activity. These drugs can be utilized for multiple diseases where estrogen is used to increase specificity and improve long-term safety.

2025 in view

This year is marked by multiple changes and uncertainties related to the entire world. Despite the uncertainty we are very optimistic about Iaterion’s prospect of succeeding in both the development process as well as in securing future funds for continued development.

We look forward to reporting to you sooner rather than later the development of all the programs and the financial success of the company.

Forward Looking Statements

This release contains certain forward-looking statements relating to the business of Iaterion, Inc. that can be identified by the use of forward-looking terminology such as “believes,” “expects,” or similar expressions. Such forward-looking statements involve known and unknown risks and uncertainties, including uncertainties relating to product development, efficacy and safety, regulatory actions or delays, the ability to obtain or maintain patent or other proprietary intellectual property protection, market acceptance, physician acceptance, third party reimbursement, future capital requirements, competition in general and other factors that may cause actual results to be materially different from those described herein as anticipated, believed, estimated or expected. Iaterion, Inc. is under no obligation (and expressly disclaims any such obligation) to update or alter its forward-looking statements whether as a result of new information, future events or otherwise.