NK3

TOKYO, Oct. 10, 2024 /PRNewswire/ -- Astellas Pharma Inc. (TSE: 4503, President and CEO: Naoki Okamura, "Astellas") announced that VEOZA™ (fezolinetant)*, its first-in-class treatment for moderate to severe vasomotor symptoms (VMS) associated with menopause, will be featured in four oral and two poster presentations during the International Menopause Society (IMS) 19th World Congress on Menopause in Melbourne, Australia, October 19-22. VMS, also known as hot flashes and/or night sweats, are common symptoms of menopause.1,2 Marci English, Vice President, Head of BioPharma Development, Astellas "Astellas is committed to advancing innovative science, and the data at the World Congress on Menopause further our understanding of how VMS impacts individuals and women's preferences for treatment. In addition, we are excited to share trial design for our recently initiated HIGHLIGHT study assessing fezolinetant for the treatment of moderate to severe VMS in patients with breast cancer taking adjuvant endocrine therapy." Emad Siddiqui, M.D., Vice President, Head of Specialty Therapeutic Area for Medical Affairs, Astellas "We are dedicated to continuing to expand the knowledge about fezolinetant beyond the pivotal trials. Our presentations at the World Congress on Menopause encompass a broad range of clinical and health-related quality of life analyses that further highlight the safety and efficacy of fezolinetant, as well as its positive impact on patient-reported outcomes including sleep and productivity at work." Fezolinetant data will be featured in four oral and two poster presentations: Two oral presentations from the SKYLIGHT 1 and 2 studies focus on patient-reported sleep outcomes and impact on work productivity with fezolinetant (Menopause New Treatments 1 and 2; Monday, Oct. 21, 3:50-5:20 p.m.; A. Cano and R. Nappi, respectively). Two oral presentations from the DAYLIGHT study highlight response and quality of life in women treated with fezolinetant who are unsuitable for hormone therapy (Menopause New Treatments 1; Monday, Oct. 21, 3:50-5:20 p.m.; A. Hirschberg and M. Shapiro, respectively). Poster highlights analyses of clinical and nonclinical data demonstrating no association between fezolinetant treatment and incidence of malignant neoplasm (P073; Sunday, Oct. 20, 7:40-9 p.m.; M. Shapiro). Poster reviews study design for the recently initiated HIGHLIGHT 1 phase 3 clinical study designed to evaluate the efficacy and safety of fezolinetant for the treatment of moderate to severe VMS in women with stage 0 to 3 hormone receptor-positive breast cancer receiving adjuvant endocrine therapy (P055; Sunday, Oct. 20, 7:40-9 p.m.; P. Briggs). Two additional oral presentations highlight Australian women's preferences for treatment of VMS associated with menopause and results of a literature review designed to identify and characterize concepts relevant to individuals' experiences of VMS with a goal of informing the development of a culturally sensitive self-assessment tool for VMS. *VEOZA: Approved as "VEOZAH ™" in U.S. About the BRIGHT SKY™ Phase 3 Program The BRIGHT SKY pivotal trials, SKYLIGHT 1™ (NCT04003155) and SKYLIGHT 2™ (NCT04003142), enrolled over 1,000 menopausal women with moderate to severe VMS. The trials are double-blinded, placebo-controlled for the first 12 weeks followed by a 40-week treatment extension period. Women were enrolled at over 180 sites within the U.S., Canada and Europe. SKYLIGHT 4™ (NCT04003389) is a 52-week double-blinded, placebo-controlled study designed to investigate the long-term safety of fezolinetant. For SKYLIGHT 4, over 1,800 menopausal women with VMS were enrolled at over 180 sites within the U.S., Canada and Europe. About DAYLIGHT DAYLIGHT (NCT05033886) is a Phase 3b, randomized, double-blind, placebo-controlled, 24-week study to assess the efficacy and safety of fezolinetant in menopausal women aged 40-65 suffering from moderate to severe VMS and considered unsuitable for hormone therapy. A total of 453 women were enrolled at 69 sites in Canada, Europe and Turkey. About HIGHLIGHT 1™ HIGHLIGHT 1 (NCT06440967) is a randomized, placebo-controlled, double-blind, Phase 3 clinical study to assess the efficacy and safety of fezolinetant for the treatment of moderate to severe VMS in women with stage 0 to 3 hormone receptor-positive breast cancer who are receiving adjuvant endocrine therapy. Approximately 540 participants are planned to be randomized 1:1 to fezolinetant or placebo at up to 100 sites in Europe and Canada. The four coprimary endpoints are change in the frequency and severity of moderate to severe VMS from baseline to weeks 4 and 12. Patients will be treated for 52 weeks with a final evaluation at 55 weeks. About VEOZA™ (fezolinetant) VEOZA (fezolinetant) is a nonhormonal neurokinin 3 (NK3) receptor antagonist indicated in Australia for the treatment of moderate to severe vasomotor symptoms (hot flashes and night sweats) associated with menopause. VEOZA works by blocking neurokinin B (NKB) binding on the kisspeptin/neurokinin/dynorphin (KNDy) neuron to modulate neuronal activity in the brain's temperature control center (the hypothalamus) to reduce the number and intensity of hot flashes and night sweats.3,4,5 Important Safety Information The full Australian Product Information and Australian Public Assessment Report (AusPAR) for fezolinetant is available from the Australian Government Therapeutic Goods Administration. 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 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. 4 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. 5 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. WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

On October 9, Bayer officially announced that its New Drug Marketing Application (NDA) has been accepted by the US Food and Drug Administration (FDA). The application is for Elinzanetant (Elinetant), a dual NK-1/NK-3 receptor antagonist, indicated for moderate to severe vasomotor symptoms (VMS) associated with menopause, commonly known as menopausal hot flashes. The application is based on the positive results of three Phase III clinical studies, OASIS 1, OASIS 2, and OASIS 3. These studies were designed to comprehensively evaluate the efficacy and safety of Elinzanetant in the treatment of menopausal associated VMS. The results of the study showed that Elinzanetant (120mg orally once daily) was excellent in reducing the frequency and severity of moderate-to severe VMS and demonstrated a good safety profile. In the Elinzanetant treatment group, headache and fatigue were the most common adverse events. In addition, the OASIS 1 and OASIS 2 studies observed sustained improvements across three key secondary endpoints, including a significant reduction in VMS frequency at week 1, improvements in sleep disturbances, and improvements in menopause-related quality of life. Elinzanetant is an innovative dual NK-1 and NK-3 receptor antagonist whose unique mechanism of action lies in the regulation of a group of estrogen-sensitive neurons within the hypothalamus in the brain (KNDy neurons). During menopause, KNDy neurons become hypertrophic due to decreased estrogen levels and lead to overactivation of the thermoregulatory pathway, which in turn disrupts the body temperature control mechanism and triggers VMS. Hot flashes, one of the most common symptoms of menopause, have a significant negative impact on women's quality of life. It is predicted that by 2030, 1.2 billion women worldwide will be affected by menopausal hot flashes. In addition to the OASIS project, Bayer is actively advancing the NIRVANA (NCT06112756) study, which aims to further evaluate Elinzanetant in the treatment of menopausal related sleep disorders.

Astellas’ headquarters for the Americas iStock, JHVEPhoto One patient developed elevated liver blood tests after receiving Astellas Pharma’s non-hormonal small molecule blocker, leading the regulator to add a warning to the drug’s label. The FDA on Thursday added a warning to the label of Astellas Pharma ’s hot flash therapy Veozah (fezolinetant), alerting patients and prescribers to a newly documented risk of “rare but serious” liver injury. The new warning was prompted by a postmarketing review of a patient who was taking Veozah and subsequently saw spikes in liver blood test values. The patient also showed signs of liver injury after being treated for around 40 days, according to the regulator. Per Veozah’s updated label , prescribers should test their patients’ blood liver markers more frequently, including monthly screens for the first two months after initiating Veozah, followed by additional tests after three, six and nine months. Doctors and prescribers should also conduct hepatic testing before starting patients on Veozah. In case of signs that could indicate liver problems, patients should stop taking Veozah “immediately” and contact their healthcare professional, according to the FDA. Common symptoms of liver harm include fatigue, jaundice, nausea and vomiting, as well as unusual itching and light-colored stools. Despite being a hit to Veozah’s safety profile, Thursday’s label seems unlikely to substantially hurt Astellas. Jeffries analysts in a note to investors said that the new warning “strengthened Veozah’s label” and that while the additional testing requirements will put more burden on patients, they “may not have much impact on demand overall.” Administered orally, Veozah is a non-hormonal small molecule blocker of the NK3 receptor which plays a part in the signaling cascade that results in the release of specific hormones involved in the menstrual cycle. Veozah specifically acts on neurons in the brain’s thermoregulatory centers, allowing it to reduce the frequency and intensity of hot flashes and night sweats. The FDA approved Veozah in May 2023 for women in menopause. In December 2023, Astellas unveiled more Phase IIIb data for Veozah, touting statistically significant improvements in moderate to severe vasomotor symptoms in patients at 24 weeks compared with placebo. Veozah also reduced sleep disturbance in these patients. At the time, the pharma noted that these findings will help it with reimbursement negotiations in Europe. Bayer is also advancing a non-hormonal competitor to Veozah. Elinzanetant is a small molecule dual inhibitor of the NK1 and NK3 receptors, which the pharma is also positioning as a treatment for moderate to severe vasomotor symptoms in menopause. Bayer won rights to elinzanetant when it bought KaNDy Therapeutics in August 2020 for $425 million upfront . In May 2024, Bayer reported data from its pivotal Phase III OASIS 1 and OASIS 2 studies, demonstrating that elinzanetant significantly lowered the frequency of hot flashes, reduced sleep disturbances and improved menopause-related quality of life.