Therapeutic program targets a novel mechanism of melatonin receptor action outside of the CNS
Celmatix Inc. today announced its latest drug program that targets melatonin receptors outside of the central nervous system (CNS). The company hopes the therapeutic drug will address a critical gap in the market for effective first-line treatments for a range of women’s health indications, starting with polycystic ovary syndrome (PCOS) and with the potential to expand into the treatment of endometriosis and menopausal symptoms.
Despite the condition’s prevalence, no drug has been developed specifically to treat PCOS. The existing standard of care for PCOS focuses on symptom management, including birth control pills to regularize periods, metformin to address insulin resistance, statins to control high cholesterol, ovarian stimulation for ovulatory dysfunction, and cosmetic procedures to remove unwanted hair.
This program emerged from a decade-long multi-omics initiative at Celmatix to understand the molecular and genetic mechanisms underlying ovarian health and conditions like PCOS.
Melatonin functions in the central nervous system (CNS), where it regulates the circadian rhythm. Increasing evidence has revealed an additional mechanism for melatonin signaling outside of the CNS, in peripheral tissues (including the ovary). A number of preclinical studies have validated the mechanism of melatonin receptor signaling outside of the CNS, and independent studies and clinical trials have demonstrated that melatonin supplements can improve endocrine, metabolic, and reproductive traits in women with PCOS and other women’s health conditions, including menopausal symptoms.
However, the therapeutic effect from melatonin supplements is small before women develop significant side effects, including drowsiness due to the CNS-activity. Melatonin supplements also have low bioavailability and half-life in the body. Selective melatonin receptor agonists have been developed, however, these compounds were developed as sleep aids and therefore they are potently active in the CNS.
The Celmatix therapeutic program is focused on developing a novel melatonin receptor agonist compound with peripherally-preferred pharmacokinetics to increase therapeutic action at the target tissues, including the ovary, and minimize unwanted side effects like drowsiness.
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