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– Kura to receive a $330 million upfront payment and up to $1.2 billion in total milestone payments, including $420 million in near-term milestone payments and opt-in right for solid tumors – – Companies to jointly develop and commercialize ziftomenib; 50/50 profit share in the U.S.; Kura to lead U.S. development and commercial activities and book sales; Kyowa Kirin has exclusive commercialization rights outside the U.S. – – Companies to jointly pursue broad development program targeting acute leukemias, including frontline indications, combinations with targeted therapies and post-transplant maintenance setting – – Kura anticipates collaboration funding along with current cash balance to support AML program advances through commercialization in frontline combination therapy – SAN DIEGO and TOKYO, Nov. 21, 2024 /PRNewswire/ -- Kura Oncology, Inc. (Nasdaq: KURA) and Kyowa Kirin Co., Ltd. (TSE: 4151) today announced they have entered into a global strategic collaboration to develop and commercialize ziftomenib, Kura's selective oral menin inhibitor, being investigated for the treatment of patients with acute myeloid leukemia (AML) and other hematologic malignancies. Under the terms of the agreement, Kura will receive an upfront payment of $330 million and expects to receive up to $420 million in near-term milestone payments, including a payment upon the launch of ziftomenib in the monotherapy relapsed/refractory (R/R) setting. In addition, Kura is eligible to receive additional development, regulatory and commercial milestone payments of $741 million, totaling up to $1.161 billion in payments for milestones and the opt-in for solid tumor indications. In the U.S., Kura will lead development, regulatory and commercial strategy and be responsible for manufacturing ziftomenib. The companies will jointly perform commercialization activities in accordance with a co-created U.S. territory commercialization plan and will share equally in any potential profits and losses. Outside the U.S., Kyowa Kirin will lead development, regulatory and commercial strategy and is responsible for commercializing ziftomenib. Kura will be eligible to receive tiered double-digit royalties on net product sales. As a Japan based global specialty pharmaceutical company, Kyowa Kirin aims to create treatments with life-changing value that bring smiles to people living with disease. The company will leverage its hemato-oncology experience and capabilities, and its deep commitment to partnerships, to successfully bring ziftomenib to market globally. "We believe that ziftomenib is a very promising investigational treatment for genetically defined AML patients," said Yasuo Fujii, MBA, Chief Strategy Officer, Managing Executive Officer of Kyowa Kirin. "The addition of ziftomenib will complement Kyowa Kirin's existing hemato-oncology portfolio and pipeline and expand our clinical development efforts into combination therapies designed to generate improved outcomes for cancer patients. We look forward to collaborating closely with the team at Kura and adding ziftomenib to our portfolio of oncology candidates as part of our commitment to bringing new, advanced treatment options to patients and the clinical community around the world." Ziftomenib is the first and only investigational therapy to receive breakthrough designation from the U.S. Food and Drug Administration (FDA) for the treatment of R/R NPM1-mutant AML, a mutation that is associated with poor outcomes[i],[ii],[iii]. Enrollment in a Phase 2 registration-directed trial of ziftomenib in R/R NPM1-mutant AML has been completed and the companies anticipate submission of a New Drug Application (NDA) in 2025. Kura is also conducting a series of clinical trials to evaluate ziftomenib in combination with current standards of care in newly diagnosed and R/R NPM1-mutant and KMT2A-rearranged AML. Kura expects to initiate registrational Phase 3 frontline studies in both the fit and unfit frontline AML patient populations in 2025. "This collaboration is an important step toward fulfilling Kura's commitment to realizing the promise of precision medicines for the treatment of cancer, and it substantially advances our goal of building a sustainable, fully integrated biopharmaceutical company," said Troy Wilson, Ph.D., J.D., President and Chief Executive Officer of Kura Oncology. "Kyowa Kirin is a wonderful partner for Kura, bringing the expertise and scale of a global pharmaceutical company. On behalf of our leadership team and board of directors, we are thrilled to be working with Kyowa Kirin to realize the potential of ziftomenib as a transformational therapy for AML patients." Importantly," Dr. Wilson continued, "we believe the upfront and anticipated milestone payments from this collaboration combined with our current cash position should provide sufficient funding to support the ziftomenib program to commercialization in the frontline setting, which we believe is a market opportunity of up to $3 billion annually in the U.S. alone." Additional Details About the Collaboration Following regulatory approval, Kura will book sales and take the lead role in U.S. commercial strategy development and both parties will share in commercialization activities. Profits and losses from the commercialization activities will be shared equally in the U.S. Outside the U.S., Kyowa Kirin will lead and perform commercialization activities, book sales and be responsible for the conduct and funding of commercialization of ziftomenib, and Kura is eligible to receive tiered double-digit royalties on net product sales. As part of the strategic collaboration, the companies will share responsibility for the conduct of clinical trials delineated within an agreed-upon global development plan. For the global development plan, Kura will fund the development costs until the end of 2028, and from 2029 onwards, both companies will share the costs at a 50:50 ratio. The companies will share equally the funding of future trials in the U.S. The agreement includes plans to launch multiple Phase 2 and Phase 3 studies of ziftomenib in AML and other hematologic malignancies over the next several years. Development and commercialization activities under the collaboration will be managed through a shared governance structure. Under the Agreement, Kyowa Kirin has an option to participate in the development and commercialization of ziftomenib in gastrointestinal stromal tumors (GIST) and other solid tumor indications upon opt-in after receipt of clinical data from the ongoing proof-of-concept study evaluating ziftomenib and imatinib in patients with advanced GIST not successfully treated with imatinib. If Kyowa Kirin exercises its option, Kura is eligible for upfront and milestone payments totaling $228 million and the parties' roles and responsibilities follow the same structure as the collaboration in AML and other heme malignancies. Excluded from the collaboration are Kura's ongoing efforts to advance multiple, next-generation menin inhibitor drug candidates targeting certain oncology indications, as well as diabetes and other metabolic diseases. Kura was advised in the transaction by BofA Securities and represented by Cooley LLP. Conference Call Kura will host a webcast and conference call featuring management from both companies at 5:30 pm ET today, November 20, 2024. The live call may be accessed by dialing (800) 715-9871 for domestic callers and (646) 307-1963 for international callers and entering the conference ID: 6978447. A live webcast will be available here and in the Investors section of Kura's website, with an archived replay available shortly after the event. About Ziftomenib Ziftomenib is a selective and oral menin inhibitor currently in development for the treatment of genetically defined AML patients with high unmet need. In April 2024, ziftomenib received Breakthrough Therapy Designation (BTD) by the FDA for the treatment of R/R NPM1-mutant AML based on data from Kura's ongoing KOMET-001 clinical trial. Additional information about clinical trials for ziftomenib can be found at kuraoncology.com/clinical-trials/#ziftomenib. About Kura Oncology Kura Oncology is a clinical-stage biopharmaceutical company committed to realizing the promise of precision medicines for the treatment of cancer. The Company's pipeline consists of small molecule drug candidates that target cancer signaling pathways. Ziftomenib, a once-daily, oral drug candidate targeting the menin-KMT2A protein-protein interaction, has received BTD for the treatment of R/R NPM1-mutant AML. Kura has completed enrollment in a Phase 2 registration-directed trial of ziftomenib in R/R NPM1-mutant AML (KOMET-001). The Company is also conducting a series of clinical trials to evaluate ziftomenib in combination with current standards of care in newly diagnosed and R/R NPM1-mutant and KMT2A-rearranged AML. Kura is evaluating KO-2806, a next-generation farnesyl transferase inhibitor (FTI), in a Phase 1 dose-escalation trial as a monotherapy and in combination with targeted therapies (FIT-001). Tipifarnib, a potent and selective FTI, is currently in a Phase 1/2 trial in combination with alpelisib for patients with PIK3CA-dependent head and neck squamous cell carcinoma (KURRENT-HN). For additional information, please visit Kura's website at www.kuraoncology.com and follow us on X and LinkedIn. About Kyowa Kirin Kyowa Kirin aims to discover and deliver novel medicines and treatments with life-changing value. As a Japan-based Global Specialty Pharmaceutical Company, Kyowa Kirin has invested in drug discovery and biotechnology innovation for more than 70 years and is currently working to engineer the next generation of antibodies and cell and gene therapies with the potential to help patients with high unmet medical needs, such as bone & mineral, intractable hematological diseases/hematology and rare diseases. A shared commitment to Kyowa Kirin's values, to sustainable growth, and to making people smile unites Kyowa Kirin across the globe. You can learn more about the business of Kyowa Kirin at www.kyowakirin.com. Kura Forward-Looking Statements This news release contains certain forward-looking statements that involve risks and uncertainties that could cause actual results to be materially different from historical results or from any future results expressed or implied by such forward-looking statements. Such forward-looking statements include statements regarding, among other things, Kura's potential receipt of milestone payments and tiered double-digit royalties under the collaboration; the pursuit of a broad ziftomenib development program including frontline indications, combinations with targeted therapies and post-transplant maintenance setting; Kura's ability to fund its AML program to commercialization in frontline combinations through the collaboration plus its current cash balance; the efficacy, safety and therapeutic potential of ziftomenib, potential benefits of combining ziftomenib with appropriate standards of care, and progress and expected timing of the ziftomenib program and clinical trials, including the timing of submission of an NDA and initiation of registrational Phase 3 frontline studies; the market opportunity of ziftomenib in the frontline setting; plans to launch multiple Phase 2 and Phase 3 studies of ziftomenib in AML and other hematologic malignancies over the next several years; and Kura's potential receipt of additional upfront and milestone payments If KKC exercises its option. Factors that may cause actual results to differ materially include the risk that compounds that appeared promising in early research or clinical trials do not demonstrate safety and/or efficacy in later preclinical studies or clinical trials, the risk that Kura may not obtain approval to market its product candidates, uncertainties associated with performing clinical trials, regulatory filings, applications and other interactions with regulatory bodies, risks associated with reliance on third parties to successfully conduct clinical trials, the risks associated with reliance on outside financing to meet capital requirements, the risk that the collaboration is unsuccessful, and other risks associated with the process of discovering, developing and commercializing drugs that are safe and effective for use as human therapeutics, and in the endeavor of building a business around such drugs. You are urged to consider statements that include the words "may," "will," "would," "could," "should," "believes," "estimates," "projects," "promise," "potential," "expects," "plans," "anticipates," "intends," "continues," "designed," "goal," or the negative of those words or other comparable words to be uncertain and forward-looking. For a further list and description of the risks and uncertainties the Company faces, please refer to the Company's periodic and other filings with the Securities and Exchange Commission (SEC), including the Company's Form 10-Q for the quarter ended September 30, 2024 filed with the SEC on November 7, 2024, which are available at www.sec.gov. Such forward-looking statements are current only as of the date they are made, and Kura assumes no obligation to update any forward-looking statements, whether as a result of new information, future events or otherwise. i Burrows F et al. Poster presented at: AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics: Discovery, Biology, and Clinical Applications; October 26-30, 2017; Philadelphia, PAii Issa GC et al. Blood Adv. 2023;7(6):933-942. doi:10.1182/bloodadvances.2022008316iii Ostronoff F et al. J Clin Oncol. 2015;33(10):1157-1164. doi:10.1200/JCO.2014.58.0571
VANCOUVER, BC, Nov. 21, 2024 /PRNewswire/ -- Complete Genomics, a San Jose, Calif.-based genomic sequencer manufacturer, today announced at the 2024 Association for Molecular Pathology (AMP) Annual Meeting & Expo the launch of its mpox (MPXV) virus amplicon sequencing panel, part of its sequencing product portfolio for pathogenic microorganisms. Complete Genomics is at AMP this week at Booth #1524. The recent surge in mpox cases is attributed to a novel strain of the virus MPXV, which exists in two clades: clade I and clade II. The global outbreak in 2022 was driven by clade II, while the newly identified Ib clade of mpox has been spreading across Africa in recent months. According to STAT, 115,000 mpox cases – clade I and clade II - have been reported in 123 countries in 2024. This week, the Centers for Disease Control and Prevention confirmed that a strain of mpox previously undetected in the U.S. was confirmed by the California Dept. Of Public Health in an individual who had recently traveled from Eastern Africa. State health officials in California reported no evidence of transmission to other people in the case. "The new strain of the mpox virus demonstrates why it is crucial to public health for researchers worldwide, including American researchers, to access affordable and high-quality sequencing products," said Rob Tarbox, VP of Product and Marketing at Complete Genomics. "These products are rapidly upgraded to enhance the identification and monitoring of new mpox virus strains." The new mpox virus amplicon sequencing panel, a targeted sequencing product based on ATOPlex multiplex PCR technology and developed with proprietary reagents, instruments and software. It covers the full-length genome of the virus, enabling rapid identification and traceability, with relative quantification of the virus. The MPXV analysis software supports virus identification, mutation detection, and strain typing, allowing for rapid and accurate analysis of sequencing data. The panel is compatible with Complete Genomics sequencing instruments DNBSEQ-G99, DNBSEQ-E25, and DNBSEQ-G400 and features automated library preparation and data analysis. In South America, Complete Genomics has also launched an end-to-end NGS solution for DENV virus that causes dengue fever, including sample extraction ATOPlex amplicon-based library preparation, DNBSEQ sequencing, and data analysis. About Complete Genomics Complete Genomics is a pioneering life sciences company that provides novel, end to end DNA sequencing solutions. It has been at the forefront of high throughput cost-effective sequencing technology development since its inception in 2005. Our products have powered over 9,400 publications across a wide array of applications. To learn more, visit www.completegenomics.com. * For Research Use Only. Not for use in diagnostic procedures.
The collaboration will accelerate the global development of LAE102, a novel Activin Receptor Type 2 A (ActRIIA) Antagonistic Monoclonal Antibody (mAb) for muscle-preserving weight loss in Obesity LOS ANGELES, Nov. 20, 2024 /PRNewswire/ -- Laekna, Inc. (2105.HK) ("Laekna"), a global biotech company focused on novel drug development for metabolic and cancer diseases, is pleased to announce a clinical collaboration with Eli Lilly and Company (Lilly), a global leader in cardiometabolic health, including diabetes and obesity, to accelerate the development of LAE102, a novel ActRIIA mAb as a novel treatment for obesity. Accelerating innovative treatments like this hopefully can make a meaningful impact on the obesity epidemic and the lives of millions of people affected by obesity. Key highlights of the collaboration include: Clinical development of LAE102 through phase 1 study including obese patients Lilly will fund, share resources and expertise to accelerate research and development timelines Laekna retains global rights for LAE102 The collaboration will focus on the development and clinical evaluation of LAE102, an innovative ActRIIA antagonistic mAb that may have potential as a first-in-class therapy in this disease area. ActRIIA is a receptor that has been shown to play a critical role in muscle regeneration and lipid metabolism. LAE102 has been shown to both increase lean mass and decrease fat mass in pre-clinical models. If successful, LAE102 could, in combination with a GLP1R agonist, further reduce fat mass and significantly regain the lean mass loss induced by GLP1R agonist. This positions LAE102 as a promising complementary drug candidate for achieving quality weight control. By combining Laekna's novel approach with Lilly's decades-long experience in metabolic diseases, the partnership aims to significantly advance the standard of care in obesity management. "We are thrilled to collaborate with a great team at Lilly, a renowned global leader in the field of obesity and metabolic diseases, to introduce cutting-edge treatment to patients suffering from such a devastating condition," said Dr. Chris Lu, Chairman and Chief Executive Officer of Laekna. "Together with Lilly's vast clinical expertise in the cardiometabolic space, we are optimistic about this collaboration's potential to accelerate the global development of LAE102 and make a meaningful impact on the lives of millions of people affected by obesity." Lilly will be utilizing Lilly's Catalyze360-ExploR&D (https://www.lilly.com/partners/catalyze) engine to accelerate the development of LAE102. About LAE102 LAE102 is Laekna's internally discovered monoclonal antibody against ActRIIA, a receptor that plays an important role in muscle regeneration and lipid metabolism. In the pre-clinical models, LAE102 has been shown to increase lean mass and decrease fat mass. In combination with GLP1R agonist, LAE102 can further reduce fat mass and significantly regain the lean mass loss induced by GLP1R agonist. This makes LAE102 a potential drug candidate for achieving quality weight control through reducing fat while keeping muscle mass. Blocking Activin-ActRII pathway could promote muscle regeneration and decrease fat mass. Laekna team is developing more drug candidates to maximize the value of targeting ActRII receptors. LAE103 is an ActRIIB-selective antibody and LAE123 is a dual inhibitor for ActRIIA/IIB. Both are the company's internally discovered antibodies for muscle regeneration and other disease indications in the drug candidate pipeline. About Laekna Stock Code: 2105.HK Founded in 2016, Laekna is a science-driven, clinical-stage biotechnology company committed to bringing novel therapies to patients with cancer, metabolic diseases and liver fibrosis patients around the world. As of June 30, 2024, Laekna has initiated seven clinical trials for LAE102, LAE002(afuresertib), LAE001 and LAE005 to address unmet medical needs in obesity and cancers. LAE102 is our internally discovered antibody against ActRIIA. It has been shown in the pre-clinical studies to increase lean mass and decrease fat mass. We've obtained IND approvals from the FDA and the CDE for LAE102 in obesity indication and are advancing the Phase I clinical trial in China. Blocking Activin-ActRII pathway could promote muscle regeneration and decrease fat mass. Laekna team has accumulated tremendous experiences and deep know-how in this specific field and is developing more drug candidates (LAE103 and LAE123), in addition to LAE102, to maximize the value of targeting ActRII receptors. In the cancer area, Laekna has built a comprehensive portfolio of drug candidates, covering the treatment of breast cancer, prostate cancer, ovarian cancer and PD-1/ PD-L1 drug-resistant solid tumors. LAE002 (afuresertib) is a potent AKT inhibitor that inhibits all three AKT isoforms (AKT1, AKT2 and AKT3) as well as one of the only two AKT inhibitors in late-stage development for breast and prostate cancer globally. Laekna has commenced the Phase III clinical trial (AFFIRM-205) for LAE002 in patients with HR+/HER2- breast cancer. Laekna, Inc. (2105.HK) was listed on the Main Board of The Stock Exchange of Hong Kong Limited (the "Hong Kong Stock Exchange") on June 29, 2023. For more information, please visit: https://www.laekna.com/ or https://www.linkedin.com/company/74110713/ Forward-Looking Statements This press release may contain certain "forward-looking statements" which are not historical facts, but instead are predictions about future events based on Laekna's current beliefs, assumptions and expectations, commonly identified by words such as "would", "may", "expects", "believes", "plans", "intends", "projects" and other terms with similar meaning. Although we believe that our predictions are reasonable, future events are inherently uncertain and our actual future results or performance may be materially different from what we expect. Accordingly, you are strongly cautioned that reliance on any forward-looking statements is subject to significant known and unknown risks and uncertainties. All forward-looking statements contained herein are qualified by reference to the cautionary statements set forth in this section. All information provided in this press release is as of the date of this press release and are based on assumptions that we believe to be reasonable as of this date, and we do not undertake any obligation to update any forward-looking statement, except as required under applicable law.
SHANGHAI, Nov. 20, 2024 /PRNewswire/ -- Epigenic Therapeutics, a leading biotechnology company dedicated to developing next-generation gene modulation therapy, today announced that it has received approval of clinical trial application (CTA) from the New Zealand Medicines and Medical Devices Safety Authority (Medsafe) and The Health and Disability Ethics Committees (HDEC) to initiate a clinical trial for EPI-003, which is an investigational, liver-targeting antiviral therapy for chronic hepatitis B (CHB) virus infection. EPI-003 is set to become the world's first epigenetic therapy to reach clinical trials for this widespread infectious disease. This first-in-human study will assess the safety, tolerability, pharmacokinetics (PK), and pharmacodynamics (PD) of EPI-003 in Nucleos(t)ide Analogue-Treated, Chronic Hepatitis B Patients. The clinical trial is planned for sites in New Zealand, Australia, and Hong Kong. EPI-003 is a breakthrough antiviral drug administered through intravenous infusion targeting the liver through epigenetic modification for the treatment of chronic hepatitis B virus (HBV) infection. CHB is a liver infection that can progress from asymptomatic stages to cirrhosis, liver failure, and hepatocellular carcinoma (HCC). The primary challenge in curing chronic hepatitis B is the persistent presence of HBV covalently closed circular DNA (cccDNA) and integrated genomic DNA within the liver, which results in sustained viral surface antigenemia. Current antiviral treatments for hepatitis B can only suppress HBV replication, thus requires patients to take lifelong medications. As research into epigenetic regulatory mechanisms has advanced, these related pathways have emerged as new therapeutic targets for HBV treatment. EPI-003, an antiviral agent with a novel mechanism of action, has demonstrated notable advantages in preclinical studies. Prepared as mRNA encoding the epigenetic modulation protein and a guide RNA targeting HBV specific gene, and encapsulated in a delivery system called lipid nanoparticle (LNP) , EPI-003 is designed to make specific epigenetic modification on the HBV genome. Research indicates that EPI-003 can directly block the transcription of HBV cccDNA and integrated DNA, therefore effectively and sustainably reduce HBV surface antigen (HBsAg) and HBV DNA levels without rebound in preclinical studies. EPI-003 holds the potential to provide a functional or even complete cure for patients with chronic HBV infection. "We are very pleased to receive the global first CTA approval of EPI-003, a liver-targeted anti-HBV epigenetic inactivator discovered by Epigenic's proprietary epigenetic regulation technology (EPIREG®), to initiate first-in-patient evaluation of EPI-003. The approval is a significant milestone for the company which represents Epigenic's capability to pioneer epigenetic discovery and commitment to bringing innovation to transformative therapy. We will work closely with clinical investigators to accelerate clinical development on EPI-003 in order to benefit the CHB patients as soon as possible."said Bob Zhang, CEO and Co-founder of Epigenic Therapeutics. About Epigenic Therapeutics Epigenic Therapeutics is a frontier biotechnology company dedicated to developing next generation gene modulation therapy utilizing regulation of epigenetic genome for a variety of diseases. Founded in 2021 by leading scientists focused on discovering gene modulation technologies and developing gene modulation therapies, the company has multiple product candidates in the pipeline, including treatment for metabolic, cardiovascular, viral hepatitis, ocular, oncology and rare diseases. For more information, visit www.epigenictx.com About EPIREG® Platform Epigenic Therapeutics' EPIREG® proprietary technology platform employs its own artificial intelligence (AI) algorithms to explore and obtain innovative CRISPR-Cas components to regulate target gene(s) expression without changing the DNA sequence. Combining a patented lipid nanoparticle (LNP) delivery system, our platform has been proven to precisely and efficiently deliver medicine to targeted cells and tissues in metabolic, cardiovascular, viral hepatitis, ocular, oncology and rare disease models. ContactPartnering@epigenictx.comMedia@epigenictx.comInvestors@epigenictx.com
BEIJING, Nov. 19, 2024 /PRNewswire/ -- With the support of the RiDYMO® platform, we are able to comprehensively explore various potential targets in drug development, including protein-protein interactions, kinases, GPCRs, ion channels, and transcription factors. Polo-like kinase 1 (PLK1) is a highly conserved serine/threonine protein kinase that plays a crucial role during cellular mitosis[1]. It is overexpressed in various malignancies, including colorectal cancer[2], pancreatic cancer[3], and breast cancer, and its high expression is associated with poor prognosis. Consequently, PLK1 has emerged as a promising target in cancer drug development, with numerous candidates currently in the pipeline worldwide. Among these, Cardiff Oncology's onvansertib (PCM-075) has shown the most significant progress, displaying encouraging efficacy results in clinical treatment for patients with metastatic colorectal cancer (mCRC). The RiDYMO® platform, a next-generation computational drug design platform developed by DP Technology, based on AI for Science, provides robust end-to-end support for hit discovery and optimization by integrating multiple artificial intelligence techniques, physical algorithms, and experimental validation. In this study, we referred to the co-crystal complex of PLK1 and PCM075 (2YAC) and utilized the RiDYMO platform's comprehensive capabilities to synthesize and test under 100 compounds, leading to the identification of preclinical candidate compounds with potential clinical value and significantly accelerating the drug development process. We first conducted an in-depth analysis of the interactions between PCM-075 and the PLK1 protein. Preserving key interactions, we applied molecular generation, evaluation, and screening techniques to obtain a novel scaffold, the lead compound DP101, which exhibited an activity of 56 nM. Figure: Screening process for novel scaffold lead compound Next, during the optimization process based on the structure of DP101, we modified several sites on the scaffold, including hydrogen bonding networks (R3) and hydrophobic group encapsulation zones (R1 & R2). Experimental data showed a high consistency between computational predictions and experimental results, demonstrating the platform's practicality in optimizing kinase inhibitors. Figure A: Optimization and FEP prediction for R1, R2, and R3, with dark gray areas indicating a 1 kcal error range and light gray areas representing a 2 kcal error range; B: Overall molecular optimization process based on the DP101 scaffold Leveraging the RiDYMO® platform's activity prediction ranking and physicochemical property forecasting, we underwent multiple rounds of testing and optimization, ultimately obtaining several compounds with enhanced in vitro activity and pharmacokinetic properties. Notably, the activity of DP226 (0.19 nM) improved nearly 300-fold compared to DP101, surpassing PCM075, with an oral bioavailability (F = 76.8%) significantly higher than that of PCM075 (F = 24%). At low doses, DP226 exhibited superior anti-tumor effects compared to PCM075, and in combination with bevacizumab, it led to tumor regression, positioning it as a potential PCC molecule for further studies. Figure: Antitumor effects of DP226 on HCT116 xenograft model Dr. Dongdong Li, Director of Medicinal Chemistry at DP Technology and Project Leader, stated, "With the support of the RiDYMO® platform, we are able to comprehensively explore various potential targets in drug development, including protein-protein interactions, kinases, GPCRs, ion channels, and transcription factors. The use of the RiDYMO® platform for activity predictions, rankings, and experimental validations significantly enhances the efficiency of activity optimization, effectively shortening optimization cycles and accelerating the overall project development timeline. The integrated capabilities of the RiDYMO® platform hold promise for providing high-efficiency support in early-stage drug discovery. As a potential PCC molecule, we look forward to collaborating with experienced pharmaceutical companies in this field to advance this project to the next milestone." About the RiDYMO® Hit Discovery and Optimization Platform RiDYMO® is a state-of-the-art hit discovery and optimization platform developed by DP Technology, leveraging the principles of AI for Science. It employs the proprietary Hermite® computational drug design software to elucidate the dynamics of "undruggable" targets and explores a broader chemical space encompassing small molecules, macrocycles, and cyclic peptides. By integrating advanced artificial intelligence, physical algorithms, and high-throughput experimentation, the platform excels in designing oral macrocyclic compounds and rapidly delivers innovative drug candidates. As one of its core algorithms, Reinforced Dynamics (RiD)[4] has a significant advantage in the sampling efficiency of molecular dynamics simulation. By fully leveraging the high-dimensional representation capabilities of neural networks, RiD can efficiently capture dynamic conformational changes in complicated biomolecular systems. Previously, the core RiD algorithm of the platform was published in Nature Computational Science. The study demonstrated that RiD could achieve a more comprehensive free energy surface within 1.86 μs, compared to 100 μs required by traditional MD methods, representing nearly a hundredfold increase in efficiency. RiDYMO® has been successfully employed in various projects, including the development of c-Myc small molecules, GPX4 small molecules, and β-catenin cyclic peptides, demonstrating its strong potential in innovative drug discovery. For more information, please visit our website.(https://www.dp.tech/en/services/medicine). About Hermite Hermite® is a next-generation computational drug design platform developed by DP Technology, powered by AI for Science, to provide a comprehensive solution for drug design. Hermite® integrates industry-leading tools such as the Free Energy Perturbation module, Uni-FEP, and the ultra-high-throughput virtual screening tool, Uni-VSW, supporting key stages of drug discovery, from protein structure prediction and target validation, to hit discovery and lead optimization. The platform offers an interactive, web-based molecular visualization experience, with detailed management of projects, teams, and data. It features full compliance certification, multi-tier security measures, and supports both cloud-based and private deployment options. Hermite® is trusted by over 60% of leading pharmaceutical companies in China, applied across more than 50 drug pipelines. To date, industry users have performed over 200,000 Uni-FEP calculations on the Hermite® platform. For more information, please visit: https://www.dp.tech/en/product/hermite About DP Technology At DP Technology, we're at the forefront of integrating artificial intelligence into scientific research and industrial R&D. Our "AI for Science" initiative is redefining how we tackle complex scientific challenges, making groundbreaking discoveries more accessible and actionable. We've developed the "DP Particle Universe," a suite of advanced pre-trained models that seamlessly connect cutting-edge research with real-world industrial applications. Our software suite includes: Bohrium® Scientific Computing Space Station, Hermite® Computational Drug Design Platform, RiDYMO® Hit Discovery Platform, and Piloteye® Battery Design Automation Platform. Together, these platforms form a robust foundation for industrial innovation and an open ecosystem for AI in science, fostering advancements in key areas such as drug discovery, energy, materials science and information technology. References: 1. Polo on the Rise-from Mitotic Entry to Cytokinesis with Plk1. Dev Cell. 2008 May;14(5):646-59. 2. Polo-like kinase 1 expression is a prognostic factor in human colon cancer. World J Gastroenterol. 2005 Sep 28;11(36):5644-50. 3. Identification of human polo-like kinase 1 as a potential therapeutic target in pancreatic cancer. Mol Cancer Ther. 2004 May;3(5):641-6. 4. Efficient sampling of high-dimensional free energy landscapes using adaptive reinforced dynamics. Nat Comput Sci. 2022 Jan;2(1):20-29.
TAIPEI, Nov. 19, 2024 /PRNewswire/ -- TAHO Pharmaceuticals Ltd. announced the dosing of the first subjects in its U.S. Phase III clinical trial for its lead product, TAH3311, an innovative antithrombotic oral dissolving film (ODF). In July 2023, the U.S. Food & Drug Administration (FDA) accepted TAHO's proposal for a 505(b)(2) NDA submission, based on a single pivotal bioequivalence study comparing the plasma concentration of TAH3311 to the approved tablet formulation. This pivotal, open-label, randomized, crossover trial will enroll 60 subjects. TAH3311 introduces a groundbreaking ODF formulation of apixaban, a widely recognized first-line treatment and gold standard for stroke prevention and thrombosis management. Dr. Howard Lee, Chairman and CEO of TAHO Pharmaceuticals, stated:"Our team at TAHO Pharmaceuticals is dedicated to developing 505(b)(2) new drug formulations to address the clinical disadvantages of existing medications. Apixaban, available exclusively in tablet form, often presents challenges for elderly patients, children, and stroke survivors who have difficulty swallowing. These patients frequently need to crush tablets, mix them with water, and administer them twice daily—a time-consuming and imprecise process that risks dosage loss. TAH3311 overcomes these barriers with a quick-dissolving oral film that melts on the tongue, requires no water, reduces the risk of choking, enhances patient adherence, and alleviates caregiver burden." By addressing the clinical limitations of the tablet form and leveraging the significant market potential of apixaban, TAHO Pharmaceuticals is advancing TAH3311 as a meaningful innovation in anticoagulant therapy. About ApixabanApixaban (co-developed by BMS and Pfizer under the brand name Eliquis®) is a direct factor Xa inhibitor and has been approved for clinical use in several thromboembolic disorders, including reduction of stroke risk in non-valvular atrial fibrillation, thromboprophylaxis following hip or knee replacement surgery, the treatment of deep vein thrombosis or pulmonary embolism, and prevention of recurrent deep vein thrombosis and pulmonary embolism. With notable safety advantages, it is the leading novel oral anticoagulant (NOAC). According to various industry reports, apixaban was the second-highest-selling drug globally in 2023. About TAHO Pharmaceuticals Ltd.Founded in 2010, TAHO Pharmaceuticals Ltd. leverages its proprietary Transepithelial Delivery System (TDS) to overcome the limitations of existing drugs and develop innovative dosage forms for niche markets. The TDS platform combines advanced transdermal and transmucosal delivery technologies, enabling the development of unique dosage forms such as transdermal patches, ODF, and buccal films. TAHO's diverse product portfolio spans a variety of therapeutic areas, including antithrombotic agents, opioid overdose antidotes, addiction treatments, pediatric ADHD, and chemotherapy-induced antiemetics. Among its notable achievements, TAH4411, an ODF for chemotherapy-induced nausea and vomiting, became the first product of its kind to receive regulatory approval and be commercialized in Japan. Media Contact:TAHO Pharmaceuticals+886-2-2659-8515ir@tahopharma.com
A12 藝術空間
Clinical Trials/Medical Discoveries
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