GNRH1

Endometriosis can cause severe pain, heavy periods, fatigue, and fertility issues. Credit: LaylaBird via Getty Images. The UK’s National Institute for Health and Care (NICE) has approved Gedeon Richter’s Ryeqo (relugolix–estradiol–norethisterone), a once-daily oral treatment for endometriosis, for use on the National Health Service (NHS). The drug works by blocking gonadotrophin releasing hormone (GnRH) that contributes to endometriosis while simultaneously providing necessary hormone replacement. Unlike traditional GnRH agonists – such as Takeda’s Prostap (leuprorelin) and AstraZeneca’s Zoladex (goserelin) – which are limited to six months of use, Ryeqo can be taken until menopause. NICE estimates that around 1,000 women per year could benefit from the treatment, which has a list price of £72 per 28-day pack. Helen Knight, director of medicines evaluation at NICE, highlighted the benefits of a pill-based treatment: “Instead of travelling to clinics for injections, there is now a daily tablet that can be taken at home. The treatment can also be stopped and started more easily, which is particularly important for those planning to have children and for managing side effects.” Endometriosis, a condition where tissue similar to the womb lining grows outside the uterus, causes severe pain, heavy periods, fatigue and fertility issues. Current treatment options include pain relief, hormonal therapy, and surgery. Ryeqo is now an option for those who have previously undergone medical or surgical treatments but found alternatives like tranexamic acid, hormonal contraceptives, and intrauterine delivery systems ineffective or unsuitable. NICE’s final draft guidance emphasised the need for non-invasive, long-term treatment options for endometriosis symptoms, as there is no cure. Charities, including Endometriosis UK, welcomed the news, but noted that Ryeqo induces a state of “medical menopause” alongside hormone replacement therapy (HRT), meaning it may only be suitable for “a small proportion of the 1.5 million with the disease”. NICE reversed its previous negative stance on the drug after Gedeon Richter provided additional evidence on the drug’s effectiveness and cost-effectiveness. Ryeqo improved endometriosis-associated pain and was well tolerated compared to placebo in the Phase III SPIRIT 1 (NCT03204318) and SPIRIT 2 (NCT03204331) clinical studies, which enrolled over 1,200 women. Beyond the approval of new treatments, Endometriosis UK has called for greater investment in research to find the root cause of the disease, improve management strategies, and to develop a cure. At the Royal Society of Medicine’s Innovation in Women’s Health and Femtech meeting on 3 March 2025, McKinsey partner Anouk Petersen pointed out that despite affecting a similar proportion of the population as diabetes (about 10%), endometriosis receives eight to ten times less funding. A report from McKinsey & Company and the World Economic Forum underscored the economic impact of conditions like endometriosis, finding that while women live longer than men, they spend 25% more of their lives in debilitating health conditions. This has direct productivity consequences, with 60% of the gender health gap occurring during prime working years, contributing to 80% of the economic burden on gross domestic product (GDP). According to GlobalData’s Pharma Intelligence Center, Ryeqo is forecast to generate up to $775m in sales in 2030. GlobalData is the parent company of Pharmaceutical Technology.

DEERFIELD, Ill.--( BUSINESS WIRE )--TerSera Therapeutics LLC announced the presentation of new real-world analyses on the use of goserelin 3.6 mg and goserelin 10.8 mg in premenopausal women with breast cancer. These data were presented in a poster session at the 2024 San Antonio Breast Cancer Symposium, held December 10-13 in San Antonio, TX. 1 A copy of the poster is available here . This was a retrospective, observational, non-inferiority study using structured, de-identified, patient-level data and curated progress notes from U.S. electronic medical record (EMR) data from the ConcertAI Patient360™ Breast Cancer Dataset. The objective of this study was to compare real-world treatment outcomes among breast cancer patients treated with goserelin 3.6 mg and 10.8 mg. The primary outcome was the real-world event-free survival (rwEFS) rate at 12 months to assess the non-inferiority of the goserelin 10.8 mg dose given every 12 weeks vs. the 3.6 mg dose given every 4 weeks. The 12-month rwEFS rates for goserelin 3.6 mg and goserelin 10.8 mg, respectively, were 76.6% vs. 79.2% (treatment difference: 2.7% [95% CI: -1.8%, 7.0%]) which supports the non-inferiority of goserelin 10.8 mg to goserelin 3.6 mg at the prespecified -15% margin based on previously published oncology trials. In evaluating time to discontinuation, this study also found that more patients remained on goserelin 10.8 mg than 3.6 mg at years 1 and 2 post treatment initiation (51.2% vs. 39.6% and 32.4% vs. 23.1%, respectively), supporting previously published data in a separate real-world evidence analysis of breast cancer patients receiving goserelin 10.8 mg. 2 “Ovarian function suppression (OFS) with gonadotropin-releasing hormone agonists (GnRHas) is an essential component of therapy for a large proportion of pre- or perimenopausal women with hormone-sensitive breast cancer,” said Kelly E. McCann, M.D., Ph.D., assistant clinical professor of medicine at the UCLA Health David Geffen School of Medicine. “ZOLADEX 3.6 mg given every 4 weeks is the only FDA-approved GnRHa for women with breast cancer. Our data suggests that the 10.8 mg dose given every 12 weeks may also be an effective option.” U.S. INDICATIONS ZOLADEX 3.6 mg and ZOLADEX 10.8 mg are indicated for: Management of locally confined Stage T2b-T4 (Stage B2-C) carcinoma of the prostate in combination with flutamide. Treatment with ZOLADEX and flutamide should start 8 weeks prior to initiating radiation therapy and continue during radiation therapy. Palliative treatment of advanced carcinoma of the prostate. ZOLADEX 3.6 mg is also indicated for: Management of endometriosis, including pain relief and reduction of endometriotic lesions for the duration of therapy. Experience with ZOLADEX for the management of endometriosis has been limited to women 18 years of age and older treated for 6 months. Use as an endometrial-thinning agent prior to endometrial ablation for dysfunctional uterine bleeding. Palliative treatment of advanced breast cancer in pre- and perimenopausal women. IMPORTANT SAFETY INFORMATION Anaphylactic reactions to ZOLADEX have been reported in the medical literature. ZOLADEX is contraindicated in patients with a known hypersensitivity to GnRH, GnRH agonist analogues, or any of the components in ZOLADEX. ZOLADEX is contraindicated during pregnancy unless used for palliative treatment of advanced breast cancer. ZOLADEX can cause fetal harm when administered to a pregnant woman. If used during pregnancy, the patient should be apprised of the potential hazard to the fetus. There is an increased risk for pregnancy loss due to expected hormonal changes that occur with ZOLADEX treatment. ZOLADEX should not be given to women with undiagnosed abnormal vaginal bleeding. Pregnancy must be excluded for use in benign gynecological conditions. Women should be advised against becoming pregnant while taking ZOLADEX. Effective nonhormonal contraception must be used by all premenopausal women during ZOLADEX therapy and for 12 weeks following discontinuation of therapy. Transient worsening of tumor symptoms, or the occurrence of additional signs and symptoms of breast cancer, may occasionally develop during the first few weeks of treatment. Some patients may experience a temporary increase in bone pain. Monitor patients at risk for complications of tumor flare. Hyperglycemia and an increased risk of developing diabetes or worsening of glycemic control in patients with diabetes have been reported in men receiving GnRH agonists like ZOLADEX. Monitor blood glucose levels and glycosylated hemoglobin (HbA1c) periodically and manage according to current clinical practice. Increased risk of developing myocardial infarction, sudden cardiac death and stroke has been reported in association with use of GnRH agonists like ZOLADEX in men. Patients receiving a GnRH agonist should be monitored for symptoms and signs suggestive of development of cardiovascular disease and be managed according to current clinical practice. Hypercalcemia has been reported in some breast cancer patients with bone metastases after starting treatment with ZOLADEX. If hypercalcemia does occur, appropriate treatment measures should be initiated. Hypersensitivity, antibody formation and acute anaphylactic reactions have been reported with GnRH agonist analogues. ZOLADEX may cause an increase in cervical resistance. Therefore, caution is recommended when dilating the cervix for endometrial ablation. GnRH agonists may prolong the QT/QTc interval. Providers should consider whether the benefits of androgen deprivation therapy outweigh the potential risks in patients with congenital long QT syndrome, congestive heart failure, frequent electrolyte abnormalities, and in patients taking drugs known to prolong the QT interval. Electrolyte abnormalities should be corrected. Consider periodic monitoring of electrocardiograms and electrolytes. Injection site injury and vascular injury including pain, hematoma, hemorrhage and hemorrhagic shock, requiring blood transfusions and surgical intervention, have been reported with ZOLADEX. Extra care should be taken when administering ZOLADEX to patients with low BMI and/or to patients receiving full dose anticoagulation. Depression may occur or worsen in women receiving GnRH agonists. Treatment with ZOLADEX may be associated with a reduction in bone mineral density over the course of treatment. Data suggest a possibility of partial reversibility. In women, current available data suggest that recovery of bone loss occurs on cessation of therapy in the majority of patients. In women, the most frequently reported adverse reactions were related to hypoestrogenism. The adverse reaction profile was similar for women treated for breast cancer, dysfunctional uterine bleeding, and endometriosis. The most commonly reported adverse reactions with ZOLADEX in clinical trials for endometriosis were: hot flashes (96%), vaginitis (75%), headache (75%), decreased libido (61%), emotional lability (60%), depression (54%), sweating (45%), acne (42%), breast atrophy (33%), seborrhea (26%), and peripheral edema (21%). The most commonly reported adverse reactions with ZOLADEX in clinical trials for endometrial thinning were: vasodilation/hot flashes (57%), headache (32%), sweating (16%), and abdominal pain (11%). The most commonly reported adverse reactions with ZOLADEX in breast cancer clinical trials were hot flashes (70%), decreased libido (47.7%), tumor flare (23%), nausea (11%), edema (5%), and malaise/fatigue/lethargy (5%). Injection site reactions were reported in less than 1% of patients. For ZOLADEX 3.6 mg: Hot flashes (62%), sexual dysfunction (21%), decreased erections (18%), lower urinary tract symptoms (13%), lethargy (8%), pain (worsened in the first 30 days) (8%), edema (7%), upper respiratory infection (7%), rash (6%), and sweating (6%). For ZOLADEX 10.8 mg: Hot flashes (64%), pain (general) (14%), gynecomastia (8%), pelvic pain (6%), and bone pain (6%). In the locally advanced carcinoma of the prostate clinical trial, additional adverse event data were collected for the combination therapy with radiation group during both the hormonal treatment and hormonal treatment plus radiation phases of this study. Adverse experiences (incidence >5%) in both phases of this study were hot flashes (46%), diarrhea (40%), nausea (9%), and skin rash (8%). Treatment with ZOLADEX and flutamide did not add substantially to the toxicity of radiation treatment alone. Please see Full Prescribing Information for ZOLADEX 3.6 mg and ZOLADEX 10.8 mg . You are encouraged to report negative side effects of prescription drugs to the FDA. Visit fda.gov/safety/medwatch or call 1-800-FDA-1088. You can also contact TerSera Therapeutics at 1-844-334-4035 or medicalInformation@tersera.com . About HR-positive breast cancer Breast cancer is the second most commonly diagnosed cancer and one of the leading causes of cancer-related deaths worldwide. 3 In the United States, over 310,000 women will be diagnosed with breast cancer this year; 40,000 will be under the age of 50. 4 Approximately 75% of diagnosed cases in women under age 50 are considered to be hormone positive (HR+) breast cancer. Compared to older women, young women generally face more aggressive cancers and lower survival rates. 5-7 Recent studies have shown that breast cancer before age 40 differs biologically from the cancer faced by older women. 6,7 About ZOLADEX® (goserelin implant) ZOLADEX is an injectable luteinizing hormone-releasing hormone agonist (LHRHa) used to treat prostate cancer, breast cancer, and certain benign gynecological disorders. First approved in the U.S. in 1989, ZOLADEX is available as a 3.6 mg implant dosed every 28 days or as a 10.8 mg implant dosed every 12 weeks. Worldwide, ZOLADEX 3.6 mg is approved for use in breast cancer in 125 countries. ZOLADEX 10.8 mg is approved for use in breast cancer in over 60 countries. About TerSera Therapeutics TerSera Therapeutics is a biopharmaceutical company with a focus in oncology and non-opioid pain management. Founded in 2016, TerSera is building new cornerstones of care through its portfolio of unique therapeutics, amplifying their ability to deliver meaningful outcomes for patients. TerSera has been recognized as a 2024 Top Workplace. For additional information, please visit TerSera.com and follow us on LinkedIn . References McCann KE, Osman N, Cannon, J, et al. Real-world outcomes comparing 3-monthly with monthly goserelin implant in premenopausal women with breast cancer. Poster presented at: San Antonio Breast Cancer Symposium (SABCS); December 10-13, 2024; San Antonio, TX. Abstract #SESS-672; Poster ID: P1-08-09. McCann KE, Kaklamani V, Osman N, et al. Treatment patterns of goserelin 3.6 mg once monthly and 10.8 mg every three months in women with breast cancer: a real-world analysis. Poster presented at: American Society of Clinical Oncology (ASCO) Quality Care Symposium; September 27-28, 2024; San Francisco, CA. Abstract #391; Poster Session B Poster F19. Bray F, Laversanne M, Sung H, et al. Global cancer statistics 2022: GLOBOCAN estimates of incidence and mortality worldwide for 36 cancers in 185 countries. CA Cancer J Clin . 2024;74(3):222-263. doi: 10.3322/caac.21834. National Cancer Institute. Surveillance, Epidemiology and End Results Program. Cancer stat facts: female breast cancer subtypes. https://seer.cancer.gov/statfacts/html/breast-subtypes.html . Accessed December 5, 2024. Varella L, Rosenberg S. Breast cancer disparities related to young age at diagnosis. Curr Breast Cancer Rep. 2022;14(3):174-179. doi:10.1007/s12609-022-00459-x. Tesch ME, Partridge AH. Treatment of breast cancer in young adults. Am Soc Clin Oncol Educ Book. 2022;42:795-803. doi:10.1200/EDBK_360970. Guzmán-Arocho YD, Rosenberg SM, Garber JE, et al. Clinicopathological features and BRCA1 and BRCA2 mutation status in a prospective cohort of young women with breast cancer. Br J Cancer . 2022;126(2):302-309. doi:10.1038/s41416-021-01597-2 . ZOLADEX® is a registered trademark of AstraZeneca or its affiliates and is used herein under license. ©2024 TerSera Therapeutics LLC. All rights reserved.

Recently, Hope Medicine (HopeMed) announced positive interim results from a Phase 2 study of HMI-115 in women with moderate to severe endometriosis-associated pain. HMI-115 is a monoclonal antibody targeting the prolactin receptor (PRLR) with a globally unique therapeutic mechanism. The company plans to quickly advance to a global Phase 3 trial so that patients can benefit from HMI-115 treatment as soon as possible. Latest Research DataThe Phase 2 study is an international, multicenter, randomized, double-blind, placebo-controlled trial designed to evaluate the safety and efficacy of HMI-115 in women with moderate to severe endometriosis-associated pain over a 12-week treatment period. The study involved 142 female patients from the United States, Poland, and China. The interim analysis showed: ·Compared to the baseline, the 240 mg q2w group experienced a 42% reduction in average dysmenorrhea pain scores ·A 50% reduction in average non-menstrual pelvic pain scores.  ·Most patients reported normal menstruation.  ·No typical perimenopausal symptoms were reported.  ·There were no significant changes in bone mineral density and sex hormone levels, including estradiol, LH, FSH, and progesterone. About HMI-115HMI-115 non-competitively blocks PRLR-mediated signaling and has been granted Breakthrough Therapy Designation by the National Medical Products Administration (NMPA) in China for the treatment of moderate to severe pain associated with endometriosis. Initially developed by Bayer, Hope Medicine signed a global exclusive licensing agreement for the development and commercialization of HMI-115 (BAY 1158061) across multiple indications.  Beyond the endometriosis indication, the company has completed a Phase Ib study assessing the safety, tolerability, and efficacy of HMI-115 in treating androgenic alopecia. The study showed that the average non-vellus target area hair count (TAHC) increased by 14 hairs/cm² from baseline in two male patients, and the drug was safe and well-tolerated. About PRLR DrugsThe prolactin receptor (PRLR) is part of the class 1 cytokine/hematopoietic receptor superfamily and is widely expressed in the immune system, including monocytes, lymphocytes, macrophages, NK cells, granulocytes, and thymic epithelial cells. Research indicates that PRL is associated with autoimmune diseases, breast cancer, prostate cancer, ovarian cancer, pancreatic cancer, and endometrial cancer. Upon ligand binding, PRLR undergoes conformational changes that activate multiple downstream signaling pathways, including the Jak2/Stat5 and Jak1/Stat3 pathways. Activation through Src family kinases and focal adhesion kinase (FAK) can also lead to the induction of PI3K/Akt and Raf/MEK/ERK pathways in cancer cell lines. According to incomplete statistics, fewer than ten PRLR-targeted drugs are currently under development. About EndometriosisEndometriosis is a common condition among women of reproductive age and is characterized as a hormone-dependent disease. Its clinical manifestations are diverse, with pain (often related to menstrual cycles) and infertility being the most significant and impactful. Endometriosis substantially affects patients' physical, psychological, sexual, social, and reproductive well-being, imposing a heavy burden on families, society, and national economies. It is estimated that approximately 190 million women worldwide have endometriosis, representing a market size of around $200 billion.  Current treatment options for endometriosis mainly include surgery and medication, neither of which can offer a fundamentally effective, safe, and long-term treatment. Surgical treatments can remove visible lesions, but due to the unclear pathogenesis of the disease, postoperative recurrence rates remain high (with an annual increase of 10% and an accumulated five-year recurrence rate of 50%). Surgery may also lead to bowel, urinary tract, and vascular complications. Available medications (common drugs include NSAIDs, combination oral contraceptives, progestins, and GnRH agonists) have various shortcomings, and patients may discontinue treatment due to inadequate efficacy or intolerance to side effects, leading to uncontrolled and recurrent disease. About Hope MedicineHope Medicine is a science-driven, clinical-stage innovative biopharmaceutical company. It is built upon the deep understanding and decades of research achievements in translational medicine by Professor Xiaoruiping, Dean of the College of Future Technology at Peking University, and his team. The company is dedicated to the research, development, and commercialization of first-in-class drugs aimed at addressing common and major diseases that pose significant threats to human health. How to obtain the latest research advancements in the field of biopharmaceuticals? In the Synapse database, you can keep abreast of the latest research and development advances in drugs, targets, indications, organizations, etc., anywhere and anytime, on a daily or weekly basis. Click on the image below to embark on a brand new journey of drug discovery!