Advanced Malignant Solid Neoplasm

SOUTH SAN FRANCISCO, CA, USA I October 30, 2024 I TheRas, Inc. d/b/a BridgeBio Oncology Therapeutics (“BBOT” or the “Company”), a clinical-stage biopharmaceutical company focused on RAS-pathway malignancies, has announced that the first patient has been dosed with BBO-10203 in the BREAKER-101 trial. BBO-10203 is a first-in-class orally bioavailable RAS:PI3Ka breaker that blocks the interaction between RAS and PI3Kα to inhibit PI3Kα-AKT signaling in tumors, without directly inhibiting the catalytic activity of PI3Kα. “I am thrilled to partner with BBOT to bring a potentially transformable new therapeutic to the clinic,” said Dr. Minal Barve, Chief Medical Officer and Principal Investigator at Mary Crowley Cancer Research, Dallas, TX. “BBO-10203 represents a first-in-class drug with potential to address high unmet medical needs and change the landscape of cancer care. We look forward to evaluating BBO-10203 in the BREAKER-101 trial.” BBO-10203 was designed to bind covalently and selectively to the RAS-binding domain (RBD) of PI3Kα. This selective inhibition is agnostic to the mutational status of PI3Kα and RAS, and in preclinical models, results in complete inhibition of RAS-driven pAKT signal at single digit nanomolar concentration. Additionally, no hyperglycemia was observed in preclinical species treated with BBO-10203. The discovery of BBO-10203 was the result of a collaboration between the RAS Initiative at Frederick National Laboratory, Lawrence Livermore National Laboratory, and BBOT. “BBO-10203 is a first-in-class program that inhibits the interaction of the two most mutated oncogenes in human cancer, and it will allow us to test, for the first time, the importance of RAS-coordinated activation of the MAPK and AKT signaling pathways,” said Pedro Beltran, PhD, Chief Scientific Officer of BBOT. “The discovery of BBO-10203 was made possible by the dedicated collaboration between academic, national laboratory, and industry experts that synergized to advance medicines for patients suffering from cancer.” The BREAKER-101 trial will enroll patients globally with locally advanced or metastatic HER2-positive breast cancer, HR-positive/HER2-negative breast cancer, KRAS mutant advanced colorectal cancer, and KRAS mutant advanced non-small cell lung cancer. “There is a tremendous opportunity to improve the standard of care in oncology by inhibiting oncogenic pAKT signaling without the metabolic side effects observed with kinase inhibitors, and the initiation of the Phase 1 study of BBO-10203 marks an important milestone in this regard,” said Yong (Ben) Ben, MD, Chief Medical and Development Officer of BBOT. “The second IND within six months of establishing BBOT clearly demonstrates our team’s capability in advancing our novel programs into the clinic. This novel mechanism and scientific rationale behind it will allow tremendous combination opportunities that optimally inhibit both pAKT and pERK – an approach we hope will bring unprecedented benefit to patients with RAS-driven cancers.” About TheRas, Inc. d/b/a BridgeBio Oncology Therapeutics (BBOT) BridgeBio Oncology Therapeutics (BBOT) is a clinical-stage biopharmaceutical company advancing a next generation pipeline of novel small molecule therapeutics targeting RAS and PI3K malignancies. Initially formed as a subsidiary of BridgeBio, BBOT completed a $200M private financing with external investors in 2024 with the goal of improving outcomes for patients with cancers driven by the two most prevalent oncogenes in human tumors. For more information visit bridgebiooncology.com . SOURCE: BridgeBio Oncology Therapeutics

AKTive-001 is a Phase 1/1b study of ALTA2618 in adults with AKT1 E17K-mutant solid tumors ALTA2618 is the first clinical mutant-selective inhibitor of AKT SAN DIEGO, CA, USA I October 30, 2024 I Alterome Therapeutics, Inc. , a clinical stage biopharmaceutical company pioneering the development of next generation, small molecule targeted therapies for the treatment of cancer, today announced the dosing of the first patient in AKTive-001, a Phase 1/1b trial of ALTA2618 in adults with AKT1 E17K-mutant advanced solid tumors. ALTA2618 is the first mutant-selective allosteric inhibitor of AKT1 E17K and is designed to avoid on-target toxicities associated with inhibition of AKT family kinases. AKT1 E17K is a clinically validated oncogene that drives ~5% of breast cancer, particularly hormone positive disease, and 1-2% of all cancer, including endometrial (~3%) and prostate (~2%) cancers. “Dosing the first patient in the AKTive-001 trial marks a significant milestone for Alterome as we advance the first program from our mutation-selective and isoform-selective discovery pipeline to the clinic,” said Eric Murphy, Ph.D., co-founder and CEO of Alterome Therapeutics. “ALTA2618 was designed to selectively target the AKT1 E17K mutation by pioneering a novel covalent approach to capture the lysine mutation. From concept to clinic, ALTA2618 illustrates the relentless execution of our team and dedication to developing novel mutation-selective therapies that will improve outcomes for patients with cancer.” AKTive-001 is a Phase 1/1b, open-label, dose escalation and multiple expansion cohort study evaluating ALTA2618 as an oral monotherapy. The study will evaluate the safety, tolerability, pharmacokinetics, and preliminary clinical activity of ALTA2618 in patients aged 18 years or above with AKT1 E17K-mutated advanced unresectable or metastatic solid tumors (NCT06533059). Additional clinical sites across Europe, Asia and Australia will initiate enrollment over the next year. About Alterome Therapeutics, Inc. Alterome Therapeutics, Inc. is a precision oncology biotech developing alteration-specific therapeutics to address high-value and validated oncogenic drivers. The company is led by an expert team of precision oncology R&D leaders with a history of developing marketed oncology small molecule drugs. For more information, visit www.alterome.com . Follow us on LinkedIn and Twitter . SOURCE: Alterome Therapeutic

CHENGDU, China, Oct. 31, 2024 /PRNewswire/ -- The new drug application (NDA) (the " Application") based on the positive results from the pivotal phase III OptiTROP-Lung04 study of sacituzumab tirumotecan (sac-TMT, formerly SKB264/MK-2870) developed by Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. (the "Company") was accepted by the Center for Drug Evaluation (CDE) of the National Medical Products Administration (NMPA) of China in adult patients with epidermal growth factor receptor (EGFR)-mutant locally advanced or metastatic non-small cell lung cancer (NSCLC) who progressed after treatment with EGFR-tyrosine kinase inhibitor (TKI) therapy. OptiTROP-Lung04 is a multi-center, randomized, registrational phase III clinical study that evaluates the efficacy and safety results of sac-TMT monotherapy versus pemetrexed plus platinum chemotherapy for the treatment of patients with EGFR-mutant locally advanced or metastatic NSCLC who progressed after treatment with EGFR- TKI therapy. At a pre-specified interim analysis, sac-TMT monotherapy demonstrated a statistically significant and clinically meaningful improvement in the primary endpoint of progression-free survival (PFS) as assessed by the blinded independent review committee (BIRC) compared with pemetrexed plus platinum chemotherapy. Sac-TMT also showed a manageable safety profile, with no unexpected safety signals identified. The Application is the third NDA for sac-TMT that has been accepted by the NMPA. On October 25, 2024, it was announced on the official website of the CDE that the Application was planned to be included in the priority review and approval process of the CDE. Previously, two NDAs for sac-TMT in patients with locally advanced or metastatic triple-negative breast cancer (TNBC) who have received at least two prior systemic therapies (at least one of them for advanced or metastatic setting) and for sac-TMT monotherapy in adult patients with locally advanced or metastatic EGFR-mutant NSCLC who experience progression following treatment with an EGFR-TKI and platinum-based chemotherapy, respectively, were accepted by the NMPA. Sac-TMT, a core product of the Company, is a novel human trophoblast cell-surface antigen 2 (TROP2) antibody-drug conjugate (ADC) in which the Company has proprietary intellectual property rights, targeting advanced solid tumors such as NSCLC, breast cancer (BC), gastric cancer (GC), gynecological tumors, among others. Sac-TMT is developed with a novel linker to conjugate the payload, a belotecan-derivative topoisomerase I inhibitor with a drug-to-antibody-ratio (DAR) of 7.4. Sac-TMT specifically recognizes TROP2 on the surface of tumor cells by recombinant anti-TROP2 humanized monoclonal antibodies, which is then endocytosed by tumor cells and releases KL610023 intracellularly. KL610023, as a topoisomerase I inhibitor, induces DNA damage to tumor cells, which in turn leads to cell-cycle arrest and apoptosis. In addition, it also releases KL610023 in the tumor microenvironment. Given that KL610023 is membrane permeable, it can enable a bystander effect, or in other words kill adjacent tumor cells. In May 2022, the Company licensed the exclusive rights to MSD (the tradename of Merck & Co., Inc., Rahway, NJ, USA) to develop, use, manufacture and commercialize sac-TMT in all territories outside of Greater China (includes Mainland China, Hong Kong, Macao, and Taiwan). Dr. Micheal Ge, CEO of Kelun-Biotech, said, "sac-TMT (sacituzumab govitecan) has received its third NDA. In response to unmet clinical needs, the company has always adhered to the spirit of hard work inherent in Kelun, focusing on original innovation and doing practical work to develop new drugs with differentiated advantages and international potential. We believe that sac-TMT will shine in the field of oncology and contribute Chinese strength to the global health cause." About Kelun-Biotech Kelun-Biotech (6990.HK) is a holding subsidiary of Kelun Pharmaceutical (002422.SZ), which focuses on the R&D, manufacturing, commercialization and global collaboration of innovative biological drugs and small molecule drugs. The company focuses on major disease areas such as solid tumors, autoimmune, inflammatory, and metabolic diseases, and in establishing a globalized drug development and industrialization platform to address the unmet medical needs in China and the rest of world. The Company is committed to becoming a leading global enterprise in the field of innovative drugs. At present, the Company has more than 30 ongoing innovative projects in major disease areas such as solid tumors, autoimmune, inflammatory, and metabolic diseases, including over 10 projects in the clinical stage and 4 projects in the NDA stage with several global trials being conducted simultaneously in multiple countries, including China, Europe, and the United States. The company has established one of the world's leading proprietary ADC platforms, OptiDC™, and has 5 ADC projects in the clinical stage (2 of which are in the NDA stage) and several projects in the preclinical stage. For more information, please visit . SOURCE Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED