NK3

Bayer reported further positive Phase III study results for elinzanetant in treating severe vasomotor symptoms (VMS) associated with menopause, but the wait continues for detailed data to see how the NK-1,3 receptor antagonist stacks up against Astellas' marketed drug Veozah (fezolinetant).In January, Bayer announced that elinzanetant met the primary endpoints of the OASIS 1 and 2 trials in women with VMS associated with menopause, with the oral drug demonstrating statistically significant reductions in the frequency and severity of moderate-to-severe VMS from baseline to week four and 12 compared to placebo.Meanwhile, the results disclosed Tuesday come from the OASIS 3 study, with elinzanetant again demonstrating a statistically significant reduction in the frequency of moderate-to-severe VMS from baseline to week 12 compared to placebo. Bayer added that the long-term safety profile observed over 52 weeks in the trial was “overall consistent” with previously conducted studies.Results from all three OASIS studies are expected to be presented at upcoming medical meetings, with elinzanetant’s safety profile seen as key to competing with Astellas’ NK3 receptor antagonist. Veozah’s label in the US includes a warning for elevated hepatic transaminase and requires blood tests for liver damage or infection prior to treatment and every three months for the first nine months of use.Bayer said it will submit the data from the OASIS programme to health authorities seeking approval of elinzanetant for the treatment of moderate-to-severe VMS associated with menopause.More to come.

Pictured: Bayer's office in Berlin, Germany/iStock, Elenasfotos Bayer reported another Phase III win for its menopause drug candidate Tuesday, linking the molecule to improved outcomes in a long-term study and setting the stage for approval filings. The clinical trial evaluated the safety and efficacy of elinzanetant, a dual neurokinin-1,3 (NK-1,3) receptor antagonist, in the treatment of hot flashes associated with menopause over 52 weeks. Bayer reported a pair of 12-week Phase III studies met their coprimary endpoints in January 2024, but still needed a hit on the third trial to show the long-term effects of the molecule. Bayer’s topline readout revealed that the trial met its primary endpoint, which tracked the mean change in the frequency of moderate to severe hot flashes after 12 weeks of oral daily dosing with elinzanetant or placebo. The company also said the safety pro across 52 weeks of dosing was consistent with the results of previously published studies including its Phase 2b dose-finding trial. The company plans to include data from all three clinical trials in applications for approval. If Bayer wins approval, it will face competition from Astellas’ rival NK3 receptor antagonist Veozah (fezolinetant). The FDA approved Veozah for the treatment of vasomotor symptoms, the medical term for hot flashes, due to menopause in May 2023. Bayer is keeping back data from all three trials to present at upcoming scientific congresses, making it impossible to assess how elinzanetant compares to Veozah. Astellas reported 3.6 billion yen ($24 million) of Veozah sales over the first nine months of its financial year and has run ads during the Super Bowl and the Oscars to promote the product. Elinzanetant may have an advantage over Veozah because it targets NK1 and NK3, rather than just the latter receptor. Some studies have suggested NK1 antagonists may improve sleep. Bayer’s long-term trial looked at changes in sleep disturbances, which are frequently associated with hot flashes, but the company has yet to release the data. The details of the readout will shape the prospects of an important molecule for Bayer. The company has 10 programs in Phase III development but CEO Bill Anderson has warned the “late-stage pipeline is thin relative to the patent losses we have in the next years,” telling the Financial Times that the problems stem from historical under-investment. Having stopped a Phase III trial of the investigational factor XIa inhibitor asundexian in November 2023, Bayer is looking to elinzanetant and late-phase prostate cancer and chronic kidney disease prospects to drive growth and offset the upcoming loss of patent protection for Xarelto (rivaroxaban). Nick Paul Taylor is a freelance pharmaceutical and biotech writer based in London. He can be reached on LinkedIn.

TOKYO, March 3, 2024 /PRNewswire/ -- Astellas Pharma Inc. (TSE: 4503, President and CEO: Naoki Okamura, "Astellas") today announced dosing of the first patient in the STARLIGHT™ 2 Phase 3 pivotal study for fezolinetant, an investigational oral, nonhormonal compound being studied for the treatment of vasomotor symptoms (VMS) associated with menopause in Japanese women. In Japan, two Phase 3 clinical studies are underway. STARLIGHT 2 is evaluating the efficacy and safety of fezolinetant once-daily through 12 weeks. STARLIGHT 3 is evaluating the safety and tolerability of fezolinetant once-daily through 52 weeks. Marci English, Vice President, Head of BioPharma Development, Astellas "VMS associated with menopause affects millions of women in Japan. We are excited the STARLIGHT Phase 3 clinical studies are underway, bringing us one step closer to making this novel, nonhormonal treatment option available in Japan for women experiencing VMS associated with menopause." Dosing for the STARLIGHT Phase 3 clinical studies was determined based on available global data, including the STARLIGHT Phase 2b study (NCT05034042) that enrolled 147 patients and completed in 2022. Primary results of STARLIGHT Phase 2b were presented at the Annual Meeting of the Japan Society for Menopause and Women's Health on Dec. 3, 2023. About STARLIGHT 2 STARLIGHT 2 (NCT06206408) is a 12-week randomized, double-blind, placebo-controlled, parallel-group, multicenter clinical study to evaluate the superiority of fezolinetant versus placebo and assess the safety of fezolinetant in Japanese women experiencing VMS associated with menopause. Approximately 390 participants will be randomized to this study with 130 participants per treatment arm (fezolinetant low dose, fezolinetant high dose or placebo). The primary endpoint is mean change in the frequency of VMS from baseline to week 8, with total treatment duration of 12 weeks. About STARLIGHT 3 STARLIGHT 3 (NCT06206421) is a 52-week randomized, double-blind, placebo-controlled, parallel-group, multicenter clinical study to assess the safety and tolerability of fezolinetant in Japanese women experiencing VMS associated with menopause. Approximately 260 participants will be randomized to this study with 130 participants per treatment arm (fezolinetant or placebo). The primary endpoint is frequency and severity of adverse events through 52 weeks. About VMS VMS, also known as hot flashes and/or night sweats, are common symptoms of menopause that can have a disruptive impact on women's daily activities and overall quality of life.1,2 Worldwide, more than half of women 40 to 64 years of age experience VMS.3,4 In Japan, about 25% to 37% of women experience these symptoms during or after the menopausal transition.5,6 About Fezolinetant Fezolinetant is an investigational oral, nonhormonal medicine in clinical development in Japan for the treatment of VMS associated with menopause. VMS are also known as hot flashes or night sweats. Fezolinetant works by blocking neurokinin B (NKB) binding on the kisspeptin/neurokinin/dynorphin (KNDy) neuron, helping restore the balance in the brain's temperature control center (the hypothalamus) to reduce the number and intensity of hot flashes and night sweats.7,8,9 There is no guarantee the agent will receive regulatory approval in Japan or become commercially available for the uses being investigated. About Astellas Astellas Pharma Inc. is a pharmaceutical company conducting business in more than 70 countries around the world. We are promoting the Focus Area Approach that is designed to identify opportunities for the continuous creation of new drugs to address diseases with high unmet medical needs by focusing on Biology and Modality. Furthermore, we are also looking beyond our foundational Rx focus to create Rx+® healthcare solutions that combine our expertise and knowledge with cutting-edge technology in different fields of external partners. Through these efforts, Astellas stands on the forefront of healthcare change to turn innovative science into VALUE for patients. For more information, please visit our website at . Cautionary Notes In this press release, statements made with respect to current plans, estimates, strategies and beliefs and other statements that are not historical facts are forward-looking statements about the future performance of Astellas. These statements are based on management's current assumptions and beliefs in light of the information currently available to it and involve known and unknown risks and uncertainties. A number of factors could cause actual results to differ materially from those discussed in the forward-looking statements. Such factors include, but are not limited to: (i) changes in general economic conditions and in laws and regulations, relating to pharmaceutical markets, (ii) currency exchange rate fluctuations, (iii) delays in new product launches, (iv) the inability of Astellas to market existing and new products effectively, (v) the inability of Astellas to continue to effectively research and develop products accepted by customers in highly competitive markets, and (vi) infringements of Astellas' intellectual property rights by third parties. Information about pharmaceutical products (including products currently in development) which is included in this press release is not intended to constitute an advertisement or medical advice. References 1 Utian WH. Psychosocial and socioeconomic burden of vasomotor symptoms in menopause: a comprehensive review. Health Qual Life Outcomes. 2005;3:47. 2 Jones RE, Lopez KH, eds. Human Reproductive Biology. 4th ed. Waltham, MA: Elsevier, 2014:120. 3 Makara-Studzinska MT, Krys-Noszczyk KM, Jakiel G. Epidemiology of the symptoms of menopause - an intercontinental review. Przegl Menopauzalny [Menopause Rev]. 2014;13:203-211. 4 Gold EB, Colvin A, Avis N, et al. Longitudinal analysis of the association between vasomotor symptoms and race/ethnicity across the menopausal transition: study of women's health across the nation. Am J Public Health. 2006;96:1226-1235. 5 Tomida M, Otsuka R, Tange C, et al. Vasomotor symptoms, sleep problems, and depressive symptoms in community-dwelling Japanese women. J Obstet Gynaecol Res. 2021 Oct;47(10):3677-3690. doi: 10.1111/jog.14937. Epub 2021 Jul 18. PMID: 34278662; PMCID: PMC9291044. 6 NHK World-Japan. Survey on Menopause and Work 2021: Summary of Results. 7 Depypere H, Timmerman D, Donders G, et al. Treatment of menopausal vasomotor symptoms with fezolinetant, a neurokinin 3 receptor antagonist: a phase 2a trial. J Clin Endocrinol Metab. 2019;104:5893-5905. 8 Fraser GL, Lederman S, Waldbaum A, et al. A phase 2b, randomized, placebo-controlled, double-blind, dose-ranging study of the neurokinin 3 receptor antagonist fezolinetant for vasomotor symptoms associated with menopause. Menopause. 2020;27:382-392. 9 Fraser GL, Hoveyda HR, Clarke IJ, et al. The NK3 receptor antagonist ESN364 interrupts pulsatile LH secretion and moderate levels of ovarian hormones throughout the menstrual cycle. Endocrinology. 2015;156:4214-4225. SOURCE ASTELLAS PHARMA INC.