FASN

Phase 2b study evaluating diagnostic performance of 18F-RAD101 for suspected recurrent brain metastases from solid tumors of different origins Underscores Radiopharm’s commitment to developing transformative oncology radiopharmaceuticals April 28, 2025 -- Radiopharm Theranostics (ASX:RAD, Nasdaq: RADX, “Radiopharm” or the “Company”), a clinical-stage biopharmaceutical company focused on developing innovative oncology radiopharmaceuticals for areas of high unmet medical need, today announced the dosing of the first patient in its U.S. Phase 2b imaging study of 18F-RAD101 in suspected recurrent brain metastasis. The U.S. multicenter, open-label, single arm Phase 2b clinical trial1 is evaluating the diagnostic performance of 18F-RAD101 in 30 individuals with confirmed recurrent brain metastases from solid tumors of different origins. The primary objective of the study is concordance between 18F-RAD101 positive lesions and those seen in conventional imaging (MRI with gadolinium) in participants with suspected recurrent brain metastases. RAD101 is a novel imaging small molecule that targets fatty acid synthase (FASN), a multi-enzyme protein that catalyses fatty acid synthesis and is overexpressed in many solid tumors, including cerebral metastasis. Disruption of FASN activity allows for the accurate detection of cancer cells, representing a strongly viable target for the imaging of brain metastasis. Positive data from the Imperial College of London’s Phase 2a imaging trial of 18F-RAD101 in patients with brain metastases showed significant tumor uptake that was consistent with and independent from the tumor of origin.2 “We are proud to pioneer the first U.S. clinical trial of RAD101,” said Harshad R. Kulkarni, MD, Chief Medical Advisor at BAMF Health and Principal Investigator of this Phase 2b study. “This marks an important step toward improving diagnostic precision and enabling more evidence-based, individualized treatment decisions for patients with brain metastases following stereotactic radiosurgery.” “This trial is an excellent illustration of BAMF Health’s clinical trials platform in action,” added BAMF Health’s Director of Clinical Trials. “Our Radiopharmacy is producing the imaging agent on-site, our clinic team is caring for the patient and providing the best image in the world, and our clinical trials team expertly coordinates it all. BAMF’s facility and team were built to do trials just like this.” “Current standard of care imaging is less sensitive in discriminating between tumor recurrence and radiation necrosis in patients with brain metastasis who have received anticancer treatments, including radiation,” said Riccardo Canevari, CEO and Managing Director of Radiopharm Theranostics Ltd. “18F-RAD101 has the strong potential to improve diagnostic accuracy of brain metastases, and holds promise for discriminating between treatment effect and true progression in the more than 300,000 patients diagnosed with brain metastasis each year in the U.S. alone. We look forward to advancing this clinical trial and to reporting topline data in the second half of 2025.” Radiopharm Theranostics is a clinical stage radiotherapeutics company developing a world-class platform of innovative radiopharmaceutical products for diagnostic and therapeutic applications in areas of high unmet medical need. Radiopharm is listed on ASX (RAD) and on NASDAQ (RADX). The company has a pipeline of distinct and highly differentiated platform technologies spanning peptides, small molecules and monoclonal antibodies for use in cancer. The clinical program includes one Phase 2 and three Phase 1 trials in a variety of solid tumor cancers including lung, breast, and brain. Learn more at radiopharmtheranostics.com. BAMF Health is the world’s first vertically integrated platform for intelligence-based precision medicine. Headquartered in Grand Rapids, Michigan, BAMF Health employs the most advanced theranostic imaging technology to detect and treat cancer and other diseases and conduct advanced clinical trials. Our overriding mission is to empower patients to become people again. With a team of data scientists, researchers, software engineers, and clinicians —all working in lockstep—we’re making good on it. To learn more about BAMF Health, visit www.bamfhealth.com._______________________ 1 https://www.clinicaltrials.gov/study/NCT06777433 2 S. Islam et. Al., EJNMMI; 07 February 2025. https://doi.org/10.1007/s00259-025-07118-0 The content above comes from the network. if any infringement, please contact us to modify.

April 23, 2025 -- Bluejay Therapeutics, a clinical-stage biopharmaceutical company dedicated to developing potentially life-changing therapeutics for serious viral and liver diseases, today announced it will present new preclinical data on the characterization of BJT-188, a liver-targeted fatty acid synthase (FASN) inhibitor being investigated for the treatment of metabolic dysfunction-associated steatohepatitis (MASH), at the European Association for the Study of the Liver (EASL) Congress 2025, taking place May 7-10, 2025, in Amsterdam. The presentation will also be available on Bluejay’s website following the meeting. BJT-188 targets FASN, a key enzyme in the de novo lipogenesis (DNL) pathway responsible for converting dietary sugar metabolites into saturated fatty acids, which serve as precursor for lipotoxic lipids such as triglycerides. Overactivation of FASN has been implicated in the pathogenesis of MASH, primarily through excessive lipid accumulation in the liver, leading to inflammation and fibrosis. “The presentation of BJT-188 preclinical data represents an important milestone for Bluejay as we leverage our Liver-Targeting Advanced Platform (L-TAP) to expand our strategic focus beyond viral hepatitis into MASH, a serious liver disease with limited treatment options affecting millions globally,” said Keting Chu, M.D., Ph.D., Founder and Chief Executive Officer of Bluejay Therapeutics. Previous studies of other FASN inhibitors have demonstrated therapeutic potential in MASH; however, their clinical utility has been limited due to systemic side effects. BJT-188 addresses this challenge by leveraging Bluejay’s proprietary Liver-Targeting Advanced Platform (L-TAP), designed to enhance drug delivery to the liver. This targeted approach potentially reduces systemic exposure, thereby minimizing side effects and improving the overall therapeutic profile. Poster presentation details are as follows: Title: Preclinical characterization of BJT-188, a liver-targeted fatty acid synthase inhibitor for the treatment of MASH Abstract number: 2721 Session: Poster - MASLD: Experimental and pathophysiology Date: Friday, May 9 Time: 8:30 a.m. CET Presenter: Jerome Deval, Ph.D., Bluejay Therapeutics Metabolic dysfunction-associated steatohepatitis (MASH) is a severe liver disease that affects an estimated 5% of the global adult population. In the United States, it is estimated that MASH currently impacts approximately 13 million adults and is expected to impact more than 19 million by 2039. MASH is characterized by fat accumulation, inflammation and fibrosis in the liver. Increasing fibrosis is associated with a greater risk for progression to liver-related complications, including cirrhosis, liver cancer and liver-related death. MASH is also a leading cause of liver transplant. There are limited treatment options for MASH worldwide, with only one treatment currently approved in the United States. BJT-188 is a preclinical, liver-targeted fatty acid synthase (FASN) inhibitor currently under investigation by Bluejay Therapeutics for the treatment of metabolic dysfunction-associated steatohepatitis (MASH). BJT-188 targets the FASN enzyme, which is involved in converting dietary sugar metabolites into lipotoxic lipids. BJT-188 was developed utilizing Bluejay Therapeutics’ proprietary Liver-Targeting Advanced Platform (L-TAP) to enhance its liver-specific delivery. Bluejay Therapeutics’ Liver-Targeting Advanced Platform (L-TAP) integrates molecular modeling and drug design to create novel therapeutics with optimized liver targeting. By enhancing liver specificity, L-TAP aims to reduce drug distribution to peripheral tissues, thereby improving therapeutic efficacy and minimizing side effects. L-TAP has been applied to the development of BJT-628, a hepatitis B virus (HBV) transcript inhibitor currently under evaluation as part of potential combination regimens aimed at achieving a functional cure for chronic hepatitis B (CHB), and BJT-188, a fatty acid synthase (FASN) inhibitor being investigated for the treatment of metabolic dysfunction-associated steatohepatitis (MASH). Both BJT-628 and BJT-188 have demonstrated promising results in preclinical studies. Bluejay Therapeutics is a clinical-stage biopharmaceutical company dedicated to developing potentially life-changing therapeutics for serious viral and liver diseases. The company is currently investigating brelovitug for the treatment of chronic hepatitis D (CHD) and chronic hepatitis B (CHB) viral infections. Additionally, Bluejay is advancing several innovative programs with the goal of developing a combination regimen to achieve a functional cure for chronic hepatitis B, including a proprietary TLR9 agonist (cavrotolimod) and a liver-targeted HBV transcript inhibitor (BJT-628). The company is also investigating BJT-188, a preclinical liver-targeted fatty acid synthase (FASN) inhibitor, for the treatment of metabolic dysfunction-associated steatohepatitis (MASH). The content above comes from the network. if any infringement, please contact us to modify.

SAN MATEO, Calif., April 23, 2025 (GLOBE NEWSWIRE) -- Sagimet Biosciences Inc. (Sagimet, Nasdaq: SGMT), a clinical-stage biopharmaceutical company developing novel therapeutics targeting dysfunctional metabolic and fibrotic pathways, today announced that three poster presentations featuring additional analyses from the Phase 2b FASCINATE-2 study of denifanstat in MASH will be presented at the European Association for the Study of Liver (EASL) Congress 2025 being held May 7-10, 2025 in Amsterdam, Netherlands. EASL Presentation Details: Title: Assessment of the metabolic dysfunction-associated steatohepatitis resolution index and component biomarkers in prediction of histology response to denifanstat in the FASCINATE-2 trial Presenter: Rohit Loomba, MD, University of California, San Diego School of Medicine, San Diego Session: Poster – MASLD: Diagnostics and non-invasive assessment Date/Time: Wednesday, May 7, 2025, 8:30 AM CEST Location: Poster area, RAI Convention Centre, Amsterdam Key Poster Highlights: This retrospective analysis evaluated the performance of the MASH Resolution Index (MR-I), a non-invasive biomarker score, in detecting histologic resolution of MASH in the Phase 2b FASCINATE-2 trial of denifanstat. Results demonstrated that, in patients treated with denifanstat, MR-I can predict MASH resolution and potentially can predict non-responders. Additional analyses of the MR-I results are underway to identify an alternative endpoint to the more invasive liver biopsy. Title: Denifanstat-mediated reduction of plasma glycine- and taurine-conjugated bile acids correlates with histological improvements in denifanstat-treated metabolic dysfunction-associated steatohepatitis patients in phase 2b FASCINATE-2 study Presenter: Rohit Loomba, MD, University of California San Diego School of Medicine, San Diego Session: Poster – MASLD: Diagnostics and non-invasive assessment Date/Time: Wednesday, May 7, 2025, 8:30 AM CEST Location: Poster area, RAI Convention Centre, Amsterdam Key Poster Highlights: Elevated serum bile acid levels have been associated with metabolic disorders, such as MASH and type 2 diabetes. In MASH patients from the Phase 2b FASCINATE-2 trial treated with denifanstat, glycine- and taurine-conjugated bile acids were significantly reduced at 26 weeks in histological responders for both fibrosis regression and MASH resolution. These data suggest that these circulating bile acid levels may be leveraged as a response biomarker in patients treated with denifanstat. Title: Denifanstat improves multiple qFibrosis-based collagen features linked to major adverse liver outcomes in patients with metabolic dysfunction-associated steatohepatitis and high polygenic risk Presenter: Mary E. Rinella, MD, University of Chicago Pritzker School of Medicine, Chicago U.S. Session: Poster – MASLD: Therapy Date/Time: Saturday, May 10, 2025, 8:30 AM CEST Location: Poster area, RAI Convention Centre, Amsterdam Key Poster Highlights: Denifanstat demonstrated antifibrotic effect in qFibrosis-based collagen features previously linked to major adverse liver outcomes (MALO) using digital pathology techniques. Pronounced antifibrotic effects were observed with denifanstat treatment in the difficult-to-treat population with several risk variants associated with MALO. About Sagimet Biosciences Sagimet is a clinical-stage biopharmaceutical company developing novel fatty acid synthase (FASN) inhibitors that are designed to target dysfunctional metabolic and fibrotic pathways in diseases resulting from the overproduction of the fatty acid, palmitate. Sagimet’s lead drug candidate, denifanstat, is an oral, once-daily pill and selective FASN inhibitor in development for the treatment of metabolic dysfunction associated steatohepatitis (MASH). FASCINATE-2, a Phase 2b clinical trial of denifanstat in MASH with liver biopsy-based primary endpoints, was successfully completed with positive results. Denifanstat has been granted Breakthrough Therapy designation by the FDA for the treatment of non-cirrhotic MASH with moderate to advanced liver fibrosis (consistent with stages F2 to F3 fibrosis), and end-of-Phase 2 interactions with the FDA have been successfully completed, supporting the advancement of denifanstat into Phase 3 development in MASH. For additional information about Sagimet, please visit www.sagimet.com. About MASH Metabolic-dysfunction associated steatohepatitis (MASH) is a progressive and severe liver disease which is estimated to impact more than 115 million people worldwide, for which there is only one recently approved treatment in the United States and no currently approved treatments in Europe. In 2023, global liver disease medical societies and patient groups formalized the decision to rename non-alcoholic fatty liver disease (NAFLD) to metabolic dysfunction-associated steatotic liver disease (MASLD) and nonalcoholic steatohepatitis (NASH) to MASH. Additionally, an overarching term, steatotic liver disease (SLD), was established to capture multiple types of liver diseases associated with fat buildup in the liver. The goal of the name change was to establish an affirmative, non-stigmatizing name and diagnosis. Forward-Looking Statements This press release contains forward-looking statements within the meaning of, and made pursuant to the safe harbor provisions of, The Private Securities Litigation Reform Act of 1995. All statements contained in this press release, other than statements of historical facts or statements that relate to present facts or current conditions, including but not limited to, statements regarding: the expected timing of the presentation of data from ongoing clinical trials, Sagimet’s clinical development plans and related anticipated development milestones, Sagimet’s cash and financial resources and expected cash runway. These statements involve known and unknown risks, uncertainties and other important factors that may cause Sagimet’s actual results, performance or achievements to be materially different from any future results, performance or achievements expressed or implied by the forward-looking statements. In some cases, these statements can be identified by terms such as “may,” “might,” “will,” “should,” “expect,” “plan,” “aim,” “seek,” “anticipate,” “could,” “intend,” “target,” “project,” “contemplate,” “believe,” “estimate,” “predict,” “forecast,” “potential” or “continue” or the negative of these terms or other similar expressions. The forward-looking statements in this press release are only predictions. Sagimet has based these forward-looking statements largely on its current expectations and projections about future events and financial trends that Sagimet believes may affect its business, financial condition and results of operations. These forward-looking statements speak only as of the date of this press release and are subject to a number of risks, uncertainties and assumptions, some of which cannot be predicted or quantified and some of which are beyond Sagimet’s control, including, among others: the clinical development and therapeutic potential of denifanstat or any other drug candidates Sagimet may develop; Sagimet’s ability to advance drug candidates into and successfully complete clinical trials within anticipated timelines, including its Phase 3 denifanstat program and Phase 1 acne program; Sagimet’s relationship with Ascletis, and the success of its development efforts for denifanstat; the accuracy of Sagimet’s estimates regarding its capital requirements; and Sagimet’s ability to maintain and successfully enforce adequate intellectual property protection. These and other risks and uncertainties are described more fully in the “Risk Factors” section of Sagimet’s most recent filings with the Securities and Exchange Commission and available at www.sec.gov. You should not rely on these forward-looking statements as predictions of future events. The events and circumstances reflected in these forward-looking statements may not be achieved or occur, and actual results could differ materially from those projected in the forward-looking statements. Moreover, Sagimet operates in a dynamic industry and economy. New risk factors and uncertainties may emerge from time to time, and it is not possible for management to predict all risk factors and uncertainties that Sagimet may face. Except as required by applicable law, Sagimet does not plan to publicly update or revise any forward-looking statements contained herein, whether as a result of any new information, future events, changed circumstances or otherwise. Contact: Joyce Allaire LifeSci Advisors jallaire@lifesciadvisors.com Source: Sagimet Biosciences Inc.