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NK3R antagonist improves vasomotor symptoms
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Women assigned to an oral neurokinin-3 receptor, or NK3R, antagonist experienced reductions in menopausal hot flush severity and frequency within 3 days of initiating treatment and during the 4-week dosing period, whereas vasomotor symptoms did not improve in women assigned to placebo, according to findings published in Menopause.
“We already knew this compound could be a game changer for menopausal women and get rid of three-quarters of their hot flushes in 4 weeks,” Waljit S. Dhillo, PhD, professor in the department of investigative medicine at Imperial College London, said in a press release. “But this new analysis confirms the beneficial effect is obtained very quickly — within just 3 days.”
Dhillo and colleagues evaluated 37 women aged 40 to 62 years reporting at least seven hot flushes over 24 hours assigned to MLE4901 (Millendo Therapeutics), an oral NK3R antagonist, or placebo for 4 weeks, and then the reverse, in random order, after a 2-week washout period.
In the post hoc analysis, hot flush frequency diminished by 72% by day 3 of treatment with MLE4901 compared with baseline (P < .0001; 51-percentage-point decrease vs. placebo). Hot flush severity decreased by 38% compared with baseline by day 3 of treatment (P < .0001; 31-percentage-point decrease vs. placebo). By day 3 of treatment compared with baseline, hot flush bother (39%; P < .0001; 34-percentage-point decrease vs. placebo) and interference (61%; P = .0006; 37-percentage-point decrease vs. placebo) also decreased. Improvement in hot flush symptoms was not observed with placebo.
Researchers also observed improvements in the psychosocial and physical domains of the Menopause-Specific Quality of Life Questionnaire with treatment compared with placebo.
“The novel data that we report in this manuscript, which details the time course of the effect of an NK3R antagonist to relieve menopausal symptoms and the impact on sleep, fit entirely with the pre-existing literature and are timely as there is significant interest in the NK3R antagonist class as a future therapeutic for vasomotor symptoms,” the researchers wrote. “Larger-scale studies assessing efficacy, safety and optimal dosing strategy are already underway. If these studies are also positive and provide good long-term safety data, then this novel approach of using NK3R antagonism to treat menopausal flushing will be practice changing.”
“As [neurokinin B] has many targets of action within the brain, the potential for this drug class to really improve many of the symptoms of the menopause, such as hot flushes, difficulty sleeping, weight gain and poor concentration, is huge,” Julia K. Prague, MBBS, an MRC clinical research fellow at Imperial College London, said in the release. “To see the lives of our participants change so dramatically and so quickly was so exciting, and suggests great promise for the future of this new type of treatment.” – by Amber Cox
Disclosures: Dhillo reports he was funded by the National Institute for Health Research, is an inventor on a patent application registered to Imperial Innovations and was previously an investigator for a separate study of MLE4901 in polycystic ovary syndrome, for which a consultancy fee was paid. Please see the study for all other authors’ relevant financial disclosures.
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