Lasofoxifene Tartrate

COLUMBUS, Ohio, and SAN FRANCISCO, Nov. 02, 2024 (GLOBE NEWSWIRE) — Sermonix Pharmaceuticals Inc., a privately held biopharmaceutical company developing innovative therapeutics to specifically treat metastatic breast cancers (mBC), and Quantum Leap Healthcare Collaborative™ today broadly announced that in the Phase 2 clinical trial evaluating lasofoxifene as a neoadjuvant endocrine therapy in molecularly selected HR+/HER2-, locally advanced breast cancer, the investigational drug was well tolerated and demonstrated promising early activity in suppressing the Ki67 protein in both premenopausal and postmenopausal patients. Results from the study, an arm of the Endocrine Optimization Pilot Protocol (EOP), a sub-study of Quantum Leap’s ongoing I-SPY 2 TRIAL (Investigation of Serial studies to Predict Your Therapeutic Response with Imaging And moLecular analysis 2), were initially shared yesterday in a poster presentation at RISE UP for Breast Cancer. Twenty patients (10 pre- and nine postmenopausal women, and one male) were enrolled in the lasofoxifene arm of the study, during which early Ki67 suppression in premenopausal patients was seen in the absence of ovarian function suppression (OFS). Ki67 is a marker that measures how fast cancer cells are dividing. “Lasofoxifene continued to demonstrate a strong tolerability profile while showing promising Ki67 suppression in this Phase 2 study, supporting our plans to further explore its potential in the neoadjuvant setting,” said Dr. David Portman, Sermonix founder and chief executive officer. “We are currently studying lasofoxifene in the ELAINE-3 Phase 3 combination study with abemaciclib in the ESR1-mutated metastatic breast cancer setting. We are excited to see it continue to demonstrate broad potential while offering unique quality of life benefits for people confronted with breast cancer.” Patients were enrolled in the I-SPY 2 arm from March 2023 to May 2024. Median total days of treatment was 154 days. At the time of data analysis, three patients were still on treatment and two discontinued treatment due to physician or patient preference. Median Ki67 expression went from 10% at baseline (range 1.0-40%) to 4% (1.0-18.0%) at Week 3. At three weeks, Ki67 expression was suppressed to <10% in 14 out of 16 (88%) patients, and to <2.7% in 6 out of 16 (38%) patients. Adverse events (AEs) were all grade 1-2. Most common AEs include hot flushes (65%), constipation (40%), fatigue (40%) and nausea (25%). “The I-SPY 2 EOP provides a biomarker-rich platform to test novel endocrine agents in the neoadjuvant setting in a molecularly selected group of patients with tumors that are predicted to have little to no benefit from chemotherapy,” said Dr. Jo Chien, principal investigator of the sub-study. “Lasofoxifene has demonstrated significant activity based on early Ki67 suppression, not only in postmenopausal women, but also in 10 premenopausal women without concomitant ovarian function suppression, with baseline Ki67 of 12.5% (1.0-40.0%) going to 3.0% (1.0-15%) at Week 3. It is exciting to see that lasofoxifene is well-tolerated even in our youngest patients who are often most impacted by the debilitating side effects of current standard endocrine therapy options.” Quantum Leap partners with a consortium that includes the U.S. Food and Drug Administration (FDA), industry, patient advocates, philanthropic sponsors and clinicians from 41 major U.S. cancer research centers. About LasofoxifeneLasofoxifene is an investigational novel endocrine therapy in clinical development which has demonstrated robust target engagement as an ESR1 antagonist in the breast, particularly in the presence of ESR1 mutations. Lasofoxifene has demonstrated anti-tumor activity as monotherapy and in combination with a CDK4/6 inhibitor in Phase 2 studies and has unique tissue selectivity distinguishing it from other current and investigational endocrine therapies, with beneficial effects seen on vagina and bone in previous clinical studies. Lasofoxifene, which Sermonix licensed globally from Ligand Pharmaceuticals Inc., has been studied in previous comprehensive Phase 1-3 non-oncology clinical trials in more than 15,000 postmenopausal women worldwide. Lasofoxifene’s bioavailability and activity in mutations of the estrogen receptor could potentially hold promise for patients who have acquired endocrine resistance due to ESR1 mutations, a common finding in the metastatic setting and an area of high unmet medical need. Lasofoxifene’s novel activity in ESR1 mutations was discovered at Duke University and Sermonix has exclusive rights to develop and commercialize the product in this area. Lasofoxifene, a novel targeted and tissue selective oral endocrine therapy, could, if approved, play a critical role in the precision medicine treatment of advanced ER+ breast cancer. About SermonixSermonix Pharmaceuticals Inc. is a privately held biopharmaceutical company focused on the development of female-specific oncology products and is currently undertaking a Phase 3 clinical study of lasofoxifene, its lead investigational drug. The Sermonix management team, led by founder Dr. David Portman, has significant experience in all stages of the drug development, regulatory and commercialization processes. Paul Plourde, M.D., vice president of oncology clinical development, has many decades of experience at AstraZeneca in the breast cancer drug development arena. Barry Komm, Ph.D., chief scientific officer, is recognized for his expertise in nuclear receptor biology. Miriam Portman, M.D., is co-founder and chief operating officer, with expertise in clinical trial conduct and patient recruitment. Elizabeth Attias, M.M.Sc., Sc.D., chief strategy and development officer, has extensive experience in pharmaceutical drug commercialization. Simon Jenkins, Ph.D., vice president of operations, has over 30 years of experience in global drug development leadership. Sermonix non-executive chairman of the board is Anthony Wild, Ph.D., former president of both Parke-Davis Pharmaceuticals and Warner-Lambert’s Pharmaceutical Division. Learn more at SermonixPharma.com. To learn more about the ELAINE studies, visit DiscoverElaine.com. About Quantum Leap Healthcare CollaborativeQuantum Leap Healthcare Collaborative (QLHC) is a 501c(3) nonprofit pioneer that designs, implements, and succeeds at building and iterating creative and nimble solutions that drive meaningful results for patients. Our mission is to better serve patients by accelerating and innovating health care through approaches that challenge the status quo of science and care. All our efforts focus on achieving our long-term vision to improve human health for all through personalized medicine by bridging the gap between research and care. QLHC provides operational, financial, and regulatory oversight to I-SPY. For more information, visit https://www.quantumleaphealth.org/. About the I-SPY TRIALsThe I-SPY TRIAL (Investigation of Serial studies to Predict Your Therapeutic Response with Imaging And moLecular analysis 2) (I-SPY 2 TRIAL) was designed to rapidly screen promising experimental treatments and identify those most effective in specific patient subgroups based on molecular characteristics (biomarker signatures). The trial is a unique collaborative effort by a consortium that includes the Food and Drug Administration (FDA), industry, patient advocates, philanthropic sponsors, and clinicians from 30 major U.S. cancer research centers. Under the terms of the collaboration agreement, Quantum Leap Healthcare Collaborative is the trial sponsor and manages all study operations. For more information, visit www.ispytrials.org. Quantum Leap Healthcare Collaborative Media Contact:Jacqueline MurrayDirector, Marketing and Communications(415) 839-8082j.murray@quantumleaphealth.org

COLUMBUS, Ohio and CAMBRIDGE, Mass., March 24, 2025 (GLOBE NEWSWIRE) — Sermonix Pharmaceuticals, a privately held biopharmaceutical company developing innovative therapeutics to specifically treat metastatic breast cancers (mBC), and Regor Therapeutics Group, a clinical-stage global biopharmaceutical company, today announced a strategic collaboration to optimize Regor’s proprietary, cutting-edge rCARD™ (Regor Computer Accelerated Rational Discovery) platform for identification of novel targets and therapeutics that fulfill unmet patient clinical needs and preferences in the breast oncology arena. The partnership will unite the key core competencies of both organizations to leverage expertise from early discovery through preclinical, clinical, and commercial launch, resulting in treatments that deliver on the promise of fulfilling on efficacy but also developing therapies with tolerability and quality of life profiles that are aligned with patient priorities and concerns. With a Phase 3 asset – oral lasofoxifene – in development for the treatment of ESR1-mutated ER+ HER2- mBC, the Sermonix team has expertise within the clinical drug development and commercialization arena and understands the landscape and value proposition of new treatments, which are requirements for launch success and adoption by both patients and health care providers. Patient insights and unmet needs within the arena of onco-sexuality and cardio oncology, in addition to patient concerns with respect to bone health, have been increasing in importance and are areas for which Sermonix also has expertise and interest in exploring. These areas are currently gaps within the breast cancer treatment patient arena and hold great concern for patients as breast cancer potentially evolves from a lethal to a chronic disease. Regor’s leading rCARD™ platform empowers drug discovery and development from target identification and validation, molecular design and optimization, to translational research and clinical development with unprecedented speed, efficiency, and success rate. “Regor’s translational to clinical approach – and then confirmation of clinical impact – is one we greatly admire and is producing molecules for development that will be best in class from both an efficacy and tolerability perspective,” said Dr. David Portman, Sermonix founder and chief executive officer. “At Sermonix, we believe patients deserve not only highly efficacious treatments, but also ones that are well tolerated and potentially improve quality of life for breast cancer patients. Deep patient insights and the potential to develop targets that can ultimately provide efficacy while addressing areas of key concerns to patients such as vaginal, bone, and cardiovascular health would be fulfilling on the promise of optimized drug development. It is an honor to collaborate with Regor in that shared mission.” Sermonix is currently enrolling its Evaluation of Lasofoxifene in ESR1 Mutations (ELAINE-3) study, comparing targeted lasofoxifene in combination with the CDK 4/6 inhibitor abemaciclib versus fulvestrant plus abemaciclib in pre- and post-menopausal subjects with locally advanced or metastatic ER+/HER2- breast cancer with an ESR1 mutation. About Regor Therapeutics GroupRegor Therapeutics Group is a clinical-stage biotechnology company, headquartered in Cambridge, MA and with operations in Houston, TX, San Diego, CA, and Shanghai, China. Regor is developing innovative and clinically differentiated medicines to address large unmet needs in oncology, metabolism, and auto-immunity. Regor is powered by the highly efficient drug discovery engine rCARD™ (Regor Computer Accelerated Rational Discovery) that enables rapid prototyping and validation of candidate molecules. This rapid approach to developing small molecules against high-profile targets is the creation of the four cofounders who collectively brought decades of experience in leading US biopharma and were previously the named inventors of 4 FDA-approved medicines. The power of the rCARD™ platform and approach has been highlighted by out-licensing deals with top companies, including Roche/Genentech on next-gen CDK oncology agents RGT-419B and RGT-587 (now GDC-4198 and GDC-0587) in late 2024.To learn more about Regor, please visit us at www.regor.com.