GnRHR

The Medicines and Healthcare Products Regulatory Agency (MHRA) has granted a licence for Gedeon Richter’s Ryeqo for adults with endometriosis symptoms, making it the first in a new class of treatments authorised in the UK for this patient population. Those eligible to receive the combination therapy, which consists of non-peptide gonadotrophin-releasing hormone receptor antagonist relugolix 40mg, estradiol 1mg and norethisterone acetate 0.5mg taken in a single once-daily tablet, will be of reproductive age and have a history of previous medical or surgical treatment for their endometriosis. Affecting approximately 176 million women worldwide, endometriosis is a chronic condition that occurs when tissue similar to the lining of the uterus grows outside of the uterus. Patients can experience a range of symptoms, including dysmenorrhoea (painful cramping, usually in the lower abdomen), heavy bleeding and pelvic pain, and the disease can be associated with sub-fertility or infertility. The MHRA’s decision was supported by positive results from the late-stage SPIRIT programme, in which significantly more patients achieved pain reduction with Ryeqo versus placebo at 24 weeks. In the SPIRIT 1 study, 75% of patients responded to Ryeqo for their dysmenorrhoea compared to 27% in the placebo arm. The same result was seen in the SPIRIT 2 trial, with 75% of dysmenorrhoea responders in the Ryeqo cohort compared to 30% for placebo. Additionally, 59% and 66% of patients responded to Ryeqo for their non-menstrual pelvic pain (NMPP) in SPIRIT 1 and 2, respectively, compared to 40% and 43% of those receiving placebo. Dysmenorrhoea and NMPP reduction was also sustained over two years with Ryeqo treatment, according to results from a long-term extension study. David Jordan, medical director UK and Ireland, Gedeon Richter, said: “The MHRA’s decision to licence relugolix combination therapy in endometriosis is fantastic news and we are delighted the need for more treatment options has been recognised. “We have been working hard to bring a new way of treating the condition to clinicians and women suffering with painful symptoms and we believe this authorisation will be a welcome step for redefining care.” Jordan added that the company is now engaging with the relevant health authorities throughout the UK “with a view to securing NHS reimbursement as soon as possible.”

The study (NCT05138562) met its primary endpoint of change of dysmenorrhea (menstrual pain) score from baseline to 12 weeks compared to placebo across all tested doses (120 mg, 240 mg, and 320 mg) Merigolix is expected to emerge as a best-in-class treatment based on its excellent pain reduction and favorable safety profiles among gonadotropin-releasing hormone (GnRH) antagonists Positive results are also anticipated in ongoing clinical trials conducted in another disease such as uterine fibroids BOSTON and SEONGNAM, South Korea, May 8, 2024 /PRNewswire/ -- TiumBio Co., Ltd. (KOSDAQ: 321550), a clinical-stage biopharmaceutical company focused on discovering and developing innovative therapeutics for patients with rare and incurable diseases, announced positive topline results from its Phase 2a clinical trial of Merigolix, an oral gonadotropin-releasing hormone (GnRH) receptor antagonist, in patients with moderate to severe endometriosis-associated pain. The trial achieved its primary endpoint of reducing dysmenorrhea scores compared to placebo across all three dose groups, demonstrating a statistically significant difference (120mg group p=0.044, 240mg group p=0.001, 320mg group p<0.001). The study enrolled 86 female patients with moderate to severe endometriosis-associated pain across five European countries to evaluate the efficacy and safety of Merigolix in endometriosis. The patients were randomized to receive either Merigolix 120 mg, Merigolix 240 mg, Merigolix 320 mg, or a placebo once daily (QD) for 12 weeks. The change in endometriosis-associated pain from baseline to 12 weeks of treatment was assessed by measuring the mean dysmenorrhea score using the Numeric Rating Scale (NRS) over the past month. As a result of that, Merigolix achieved statistically significant and clinically meaningful improvements in mean dysmenorrhea scores from baseline compared to the placebo group at all tested doses: -4.3 point at the 120 mg dose (p=0.044), -5.4 point at the 240 mg dose (p=0.001), and -6.2 point at the 320 mg dose (p<0.001), while the placebo group reported -2.7 point. Merigolix was generally well tolerated, with no serious treatment-related adverse events, consistent with prior studies. The most commonly reported adverse events in the study population were hot flush, headache, and nausea. "Despite the small size of each group, with around 20 patients per group, Merigolix showed statistically significant efficacy compared to placebo at all doses in the Phase 2a clinical trial. This clinical trial confirmed that Merigolix achieved superior clinical outcomes in reducing dysmenorrhea and ensuring safety compared to other GnRH antagonists," said Hun-Taek Kim, Ph.D., MBA, CEO, TiumBio. "Now that this proof of concept study has supported potential for Merigolix, we aim to develop Merigolix into a best-in-class treatment for patients with endometriosis," he added. Likewise, a company official stated, "In addition to endometriosis, there is high potential to apply Merigolix to another women's disease such as uterine fibroids, and positive results are expected from ongoing clinical trials of Merigolix in China and Republic of Korea. Consequently, we anticipate that subsequent clinical development and business expansion of Merigolix will accelerate." Merigolix is an orally active non-peptide GnRH antagonist for the treatment of endometriosis and uterine fibroids. Merigolix offers improved convenience of administration and safety compared to conventional GnRH agonists. According to GlobalData, the endometriosis market will reach approximately $2.7 billion in 7 major countries (US, Germany, France, Italy, UK, Spain, Japan) by 2030. It is forecasted that GnRH antagonist therapies will replace existing treatments, accounting for about 70% of the total endometriosis market. About Endometriosis Endometriosis is a disorder in which the endometrial tissue that line the inside of the uterus grows out the uterus and is known to cause severe pelvic pain, menstrual pain, lower abdominal pain, and infertility which occurs in about 10-30% of women in childbearing age. It is estimated to affect approximately 200 million patients worldwide. About TiumBio Co., Ltd. TiumBio (Kosdaq: 321550) is a clinical-stage biopharmaceutical company focused on the discovery and development of innovative therapeutics for patients with rare and incurable diseases. Its mission is to expand the hope and happiness of mankind through our science. TiumBio boasts three leading pipeline assets: Merigolix (code name: TU2670), TU2218, and TU7710, all in various stages of clinical development. Merigolix is a once-daily, oral GnRH receptor antagonist being developed for the treatment of endometriosis and uterine fibroids and is undergoing in global Phase 2 clinical trials. TU2218 is a first-in-class oral immune-oncology therapy targeting TGF-β and VEGF pathways to promote response rates in cancer patients when used in combination with immune checkpoint inhibitors. TU7710 is a novel recombinant FVIIa designed to extend its half-life in order to provide more clinical benefits to hemophilia patients with inhibitors. With its expertise in drug development, TiumBio is committed to the discovery and development of innovative treatments to ease the burden of debilitating diseases. For further information, visit our website at and connect with us on LinkedIn. Contacts: Junseok Jang, Head of Corporate Communications & Investor Relations [email protected] Suna Cho, Manager, Corporate Communications & Investor Relations [email protected] Da-ye Song, Manager, Corporate Communications & Investor Relations [email protected] SOURCE TiumBio

MARKHAM, Ontario--(BUSINESS WIRE)-- TerSera Canada Inc. today announced that Health Canada has approved a supplemental New Drug Submission for ZOLADEX LA (goserelin acetate) 10.8mg every 12 weeks for the management of estrogen receptor-positive (ER+) early breast cancer with a high risk of recurrence or advanced breast cancer in pre- and perimenopausal women.1 While the monthly dose of ZOLADEX (3.6mg) has been approved for use in breast cancer2 since 1995, this recent approval provides a 3-month dosing option for young women with hormone-positive (HR+) breast cancer. “For young women with hormone sensitive breast cancer, suppression of ovarian function is a core component of their treatment plan to prevent recurrence,” said Nathalie LeVasseur, MD, FRCPC, Assistant Clinical Professor, Division of Medical Oncology at the University of British Columbia in Vancouver. “I am pleased to see ZOLADEX LA is now available as a 3-month dosing option for premenopausal women with ER+ breast cancer.” Every year, approximately 5,000 young Canadian women are diagnosed with breast cancer.3 Breast cancer is the leading cause of cancer death among women in Canada ages 30-49. According to a recent study, rates of breast cancer in women under the age of 50 are rising in Canada.4 “We are grateful that young women seeking treatment for breast cancer now have multiple dosing options available for the foundational treatments that they are relying on,” said Cathy Ammendolea, Chair of the Board of Directors for the Canadian Breast Cancer Network (CBCN). This approval is based on multiple international studies that have evaluated the safety and efficacy of goserelin 10.8 mg every 12 weeks for ovarian function suppression in premenopausal patients with HR+ breast cancer.5-8 Worldwide, ZOLADEX LA (goserelin acetate 10.8mg) is approved for use in breast cancer in over 60 countries, with multiple additional regulatory reviews underway. “TerSera is committed to supporting the unique needs of young women with HR+ breast cancer,” said Nancy Martin, MD, PharmD, Chief Medical Officer at TerSera. “We are proud to bring this new 3-month breast cancer dosing option for ZOLADEX to Canada.” 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. ZOLADEX is available in 125 countries worldwide. First approved in Canada 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.1,2 For more information about ZOLADEX and ZOLADEX LA, access the Canadian Product Monographs here. About TerSera Canada Inc. TerSera Canada Inc. is the Canadian operations of TerSera Therapeutics LLC, a biopharmaceutical company with a focus in oncology and urology. 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. For more information, please visit tersera.ca or follow us on LinkedIn. References ZOLADEX (goserelin implant) 10.8 mg product monograph. TerSera Therapeutics LLC. ZOLADEX (goserelin implant) 3.6 mg product monograph. TerSera Therapeutics LLC. Canadian Cancer Statistics. Canadian Cancer Society, 2023. Seely JM, Ellison LF, Billette J-M, Zhang SX, Wilkinson AN. Incidence of Breast Cancer in Younger Women: A Canadian Trend Analysis. Canadian Association of Radiologists Journal. 2024; 0(0). doi:10.1177/08465371241246422. Noguchi S, Kim HJ, Jesena A, et al. Phase 3, open-label, randomized study comparing 3-monthly with monthly goserelin in pre-menopausal women with estrogen receptor-positive advanced breast cancer. Breast Cancer. 2016; 23:771-779. Masuda N, Iwata H. Rai Y, et al. Monthly versus 3-monthly goserelin acetate treatment in pre-menopausal patients with estrogen receptor-positive early breast cancer. Breast Cancer Res Treat. 2011; 126:443-451. El Zawawy SF, Khedr G. 209P Efficacy and feasibility of long acting every three months goserelin for premenopausal breast cancer patients during COVID pandemic. Annals of Oncology. 2022;33: S631. Wu H, Bian L, Xie J, et al. 111P Goserelin 3 monthly depot is noninferior to goserelin monthly depot in the treatment of breast cancer: A real-world evidence study. ESMO Open. 2023;8(1):101335. ZOLADEX® is a registered trademark of AstraZeneca or its affiliates and is used herein under license. ©2024 TerSera Therapeutics LLC. All rights reserved.