BAK

Publication in the Journal of Ocular Pharmacology and Therapeutics highlights the ability of the Optejet to achieve a therapeutic dose of medication with far less exposure to harmful preservatives Additional presentation at the American Academy of Optometry summarizes a Phase 4 study of Mydcombi demonstrating that clinically relevant mydriasis can be achieved with a half-dose per eye NEW YORK, Oct. 23, 2024 (GLOBE NEWSWIRE) -- Eyenovia, Inc. (NASDAQ: EYEN), an ophthalmic technology company, today announced a publication in the Journal of Ocular Pharmacology and Therapeutics as well as an upcoming presentation at the American Academy of Optometry’s “Academy 2024 Indianapolis” Annual Meeting. Publication in the Journal of Ocular Pharmacology and Therapeutics The peer-reviewed paper highlights the ability of Eyenovia’s proprietary Optejet dispenser to deliver a therapeutic dose of latanoprost with far less exposure to the preservative benzalkonium chloride (BAK) than traditional eye drops. BAK, in larger volumes, can cause unwanted side effects, including cytotoxicity, cytoplasmic shrinkage, and loss of cell-cell contact, and expression of chemokine (C-C motif) ligand 2 and interleukin-6 (markers of inflammation). In contrast, this in-vitro study of latanoprost plus BAK delivered in the same amount by the Optejet dispenser (8 microliters) avoided the cytotoxicity associated with larger volumes found in eye drops and was similar to no treatment controls and BAK-free latanoprost drops. “We have shown in prior studies the ability of the Optejet dispenser to achieve a therapeutic dose of medication with approximately 80% less volume and exposure to harmful preservatives than traditional eye drops,” stated Michael Rowe, Chief Executive Officer of Eyenovia. “The implication here is that preserved medications may not need to be reformulated to get many of the benefits of non-preserved products if delivered with the Optejet. We believe this creates potential opportunities for the Optejet to improve the administration of topical ocular therapeutics well beyond our own development pipeline.” Presentation at the American Academy of Optometry’s “Academy 2024” Eyenovia also announced today an upcoming presentation at the American Academy of Optometry’s “Academy 2024 Indianapolis,” which is being held November 6-9, in Indianapolis, IN. The presentation details the results of an open-label Phase 4 study of 1% tropicamide and 2.5% phenylephrine ophthalmic metered spray, similar to Mydcombi, Eyenovia’s commercially available product for inducing mydriasis. Twenty-nine subjects completed the study and administered one spray. Baseline pupil diameter (PD) for all eyes was 2.74±0.48 mm. Mean change in PD from baseline to 30 minutes was 3.69±1.25 mm. At 30 minutes post-dosing, mean PD was 6.42±1.25 mm, with 67% and 43% of eyes dilated to ≥ 6mm and 7mm, respectively. The majority of patients returned to functional vision (PD ≤ 5 mm) as early as 3.5 hours post-instillation, with 93% reaching that point by six hours. Safety outcomes were favorable, as only mild adverse events were reported (dry eye and mild instillation site pain) all of which resolved without intervention. “We conducted this study to address questions from doctors about modulating dosing for patients who may benefit from a lower dose of tropicamide or phenylephrine,” stated Dr. Julie Whitcomb, Senior Director of Medical Affairs at Eyenovia. “What we found in this study was that a half dose may also provide clinically relevant pupil dilation, was well-tolerated, and had a desirable shorter duration of effect.” Presentation details: Title:An Open Label, Phase 4 Study of the Safety and Efficacy of Fixed Combination Tropicamide 1% and Phenylephrine 2.5% Ophthalmic Spray (MydCombi®)Poster:#109, Exhibit Hall HPresenter:Dr. Josianne Manasse, OD, SUNY College of OptometryDate/time:Friday, November 8th, 1:00-3:00pm For additional information on the Expo: https://aaopt.org/meetings/academy-2024-indianapolis/ About Eyenovia, Inc. Eyenovia, Inc. (NASDAQ: EYEN) is an ophthalmic technology company developing a pipeline of advanced products based on its Optejet platform. Eyenovia is currently focused on the commercialization of Mydcombi® for mydriasis, clobetasol propionate ophthalmic suspension, 0.05% for post-surgical pain and inflammation, as well as the ongoing late-stage development of medications in the Optejet device for pediatric progressive myopia as well as out-licensing for additional indications. For more information, visit Eyenovia.com. The Eyenovia Corporate Information slide deck may be found at ir.eyenovia.com/events-and-presentations. PLEASE GO TO MYDCOMBI.COM FOR IMPORTANT SAFETY INFORMATION for MYDCOMBI™ (tropicamide and phenylephrine hydrochloride ophthalmic spray) 1%/2.5% PLEASE GO TO CLOBETASOLBID.COM FOR IMPORTANT SAFETY INFORMATION for Clobetasol Propionate Ophthalmic Suspension 0.05% Forward-Looking StatementsExcept for historical information, all the statements, expectations and assumptions contained in this press release are forward-looking statements. Forward-looking statements include, but are not limited to, statements that express our intentions, beliefs, expectations, strategies, predictions or any other statements relating to our future activities or other future events or conditions, including the timing and scale of acceptance and use of our approved products. These statements are based on current expectations, estimates and projections about our business based, in part, on assumptions made by management. These statements are not guarantees of future performance and involve risks, uncertainties and assumptions that are difficult to predict. Therefore, actual outcomes and results may, and in some cases are likely to, differ materially from what is expressed or forecasted in the forward-looking statements due to numerous factors discussed from time to time in documents which we file with the U.S. Securities and Exchange Commission. In addition, such statements could be affected by risks and uncertainties related to, among other things: risks of our clinical trials, including, but not limited to, the costs, design, initiation and enrollment, timing, progress and results of such trials; the timing of, and our ability to submit applications for, obtaining and maintaining regulatory approvals for our products and product candidates; the potential advantages of our products, product candidates and platform technology; the rate and degree of market acceptance and clinical utility of our products and product candidates; our estimates regarding the potential market opportunity for our products and product candidates; reliance on third parties to develop and commercialize our products and product candidates; the ability of us and our partners to timely develop, implement and maintain manufacturing, commercialization and marketing capabilities and strategies for our products and product candidates; intellectual property risks; changes in legal, regulatory, legislative and geopolitical environments in the markets in which we operate and the impact of these changes on our ability to obtain regulatory approval for our products and product candidates; and our competitive position. Any forward-looking statements speak only as of the date on which they are made, and except as may be required under applicable securities laws, Eyenovia does not undertake any obligation to update any forward-looking statements. Eyenovia Contact:Eyenovia, Inc.Andy Jones Chief Financial Officerajones@eyenovia.comEyenovia Investor Contact:Eric RibnerLifeSci Advisors, LLCeric@lifesciadvisors.com(646) 751-4363Eyenovia Media Contact:Eyenovia, Inc.Norbert LoweVice President, Commercial Operationsnlowe@eyenovia.com

– Company creating de novo designed macrocycles with enhanced efficacy that precisely target disease biology – Vilya’s privileged macrocycles have the potential to be applied across broad therapeutic areas, addressing large unmet medical needs April 25, 2024 -- VILYA, Inc. (Vilya), a biotechnology company creating a new class of medicines that precisely targets disease biology, today announced the publication of a new study in Science that validates the company’s foundational drug discovery approach. The company’s platform, which is based on an exclusive license to the technology utilized in the study, leverages advanced computational approaches to design macrocycles with atomic-level accuracy that enable optimized drug-like properties. “Macrocycles are promising drug-like compounds, but incorporating diverse chemistries has historically been very difficult. We have now shown that we can accurately identify, design and synthesize small macrocycles using a new approach that leverages conformational analysis and chemical diversity to predict and construct macrocycles made out of a wide range of backbone building blocks with high structural fidelity to their design models,” said David Baker, Ph.D., Co-founder of Vilya, Director of the IPD, Professor of Biochemistry at the University of Washington, and publication co-author. “These findings indicate a promising direction for the future of drug design in which exploring diverse macrocycle structures could lead to the discovery of new therapeutic macrocyclic compounds with enhanced efficacy and specificity.” In the published paper, titled “Expansive discovery of chemically diverse structured macrocyclic oligoamides,” scientists at the Institute for Protein Design (IPD) at the University of Washington School of Medicine detailed a new proprietary computational method to design and predict the structure of small macrocycle compounds. This method significantly broadens the range of macrocycle chemical structures available for drug discovery beyond those found in nature. The study authors successfully synthesized and tested several of these computationally designed macrocycles, confirming that their actual structures closely match the predicted models. The study illustrated the therapeutic potential of these newly discovered macrocycles, which selectively inhibited a protein target of current interest they were designed to bind to. One of the three proteins designed against is the enzyme histone deacetylase (HDAC) 6, which regulates various cellular processes and has emerged as a therapeutic target involved in several types of cancer and neurodegenerative disorders. Results demonstrated that these designed macrocycles selectively and potently inhibited this target. Researchers also successfully applied this design approach to two other protein targets – mPro, the main protease of SARS-CoV-2 that plays a crucial role in the life cycle of the virus, and myeloid cell leukemia sequence 1 (MCL1), a protein that binds to BCL-2 antagonist/killer (BAK) and prevents it from signaling cell death. “This new study validates Vilya’s platform and is representative of the ongoing work we are doing in the field of medicinal chemistry to create small macrocycles, which are notable for their potent biological activities,” said Patrick J. Salveson, Ph.D., Co-founder and Chief Technology Officer of Vilya and lead author of the publication. “Our platform, which leverages our proprietary computational design, rapidly generates both chemically and structurally diverse drug-like macrocyclic compounds. In the short time since Vilya was founded in 2022, we have built a team and infrastructure to continue expanding our platform with increasing efficiency and to develop our emerging pipeline of promising macrocycles that could translate into revolutionary medicines.” Overall, the authors identified 14.9 million macrocycles built from a wide array of chemically diverse building blocks bonded together to form complex structures, showcasing a wide spectrum of drug-like macrocycles that could be used for novel bioactivities and structure-based drug design. They then synthesized a focused subset of 18 macrocycles and found the majority aligned closely to their predicted models, thereby validating the computational design approach. Nearly half of the macrocycles evaluated exhibited membrane permeability, or the ability to diffuse across tissue barriers and cell membranes. A majority also showed stability against serum proteases, underscoring their potential for effective pharmacokinetic profiles in vivo. Notably, the study authors designed macrocycles against HDAC6, of which the vast majority demonstrated potent inhibition, with select compounds achieving 100-fold to 1,000-fold selectivity over other HDACs. The macrocycles developed against the two other protein targets – mPro and MCL1 – highlight the generality of the developed methods. “Vilya was launched to leverage the foundational research in computational protein design pioneered by the team at the Institute for Protein Design and apply it to the creation of new macrocycle structures that could become transformative medicines for a variety of diseases,” said Cyrus Harmon, Ph.D., Chief Executive Officer of Vilya. “The publication in Science of the core capabilities of this technology, which we have licensed and integrated into our own proprietary platform, provides further validation of our approach. We are excited to continue building on this foundation that we have created over the past two years and advance several novel macrocycles toward clinical development.” Vilya’s proprietary platform, powered by advanced machine learning, taps into uncharted chemical space to design de novo molecular structures that are larger than most small molecules but much smaller than antibodies. These molecules are designed to have critical drug-like properties, including the ability to move through biological membranes and disrupt protein-protein interactions while being highly selective for their protein target. These novel artificial molecules with customized biologic-like properties can be leveraged for previously difficult-to-drug therapeutic targets in a broad set of indications. Vilya's computational design platform leverages advanced machine learning and other computational approaches to explore an exponentially larger chemical space than traditional discovery methods and to design in desired drug-like pharmacokinetic properties. The company’s ability to precisely design membrane-permeable molecules with high structural accuracy could lead to a new class of medicines that combine the advantages of traditional small molecule drugs and larger protein-based therapeutics. Vilya’s ability to create and screen a new class of target-directed, structured molecules in silico could transform drug discovery and development, potentially rendering high-throughput screening obsolete. Vilya is a computational biotechnology company creating a novel class of medicines to precisely target disease biology. The company’s proprietary platform, powered by advanced machine learning, taps into uncharted chemical space to design de novo molecular structures with enhanced drug-like properties that range in size between small molecules and antibodies. Vilya is leveraging its platform to focus on previously difficult-to-drug therapeutic targets. Vilya was co-founded by a team of scientists from the Institute of Protein Design (IPD), led by David Baker, Ph.D., and ARCH Venture Partners. The company has operations in Seattle and South San Francisco. To learn more, visit https://www.vilyatx.com. The content above comes from the network. if any infringement, please contact us to modify.

Researchers have traced the origin and evolutionary trajectory of plant immune receptors. Their discovery will make it easier to identify immune receptor genes from genomic information and could help in the development of pathogen-resistant crops. Plants are continuously evolving new immune receptors to ever-changing pathogens. Researchers at the RIKEN Center for Sustainable Resource Science (CSRS) have traced the origin and evolutionary trajectory of plant immune receptors. Their discovery will make it easier to identify immune receptor genes from genomic information and could help in the development of pathogen-resistant crops. This study was published in the scientific journal Nature Communications on February 1. As in animals, plants have immune responses that help them defend against pathogens such as viruses, bacteria, fungi, and oomycetes. Before invaders can be stopped, they must first be detected, and this is accomplished by pattern recognition receptors located on the surface of plant cells. The ability of these receptors to detect molecular patterns associated with pathogens depends on two types of proteins, called RLPs and RLKs, both of which can contain leucine-rich repeats -- sections in which the amino acid leucine appears multiple times. To trace the evolution of plant immunity, the international research team led by Ken Shirasu and Yasuhiro Kadota at RIKEN CSRS examined the numbers and patterns of receptors. They analyzed over 170,000 genes encoding RLKs and about 40,000 genes encoding RLPs, which they obtained from publicly available data taken from 350 plant species. They discovered that RLKs and RLPs with leucine-rich repeats were the most abundant receptor types among all the plant species, making up nearly half of RLKs and 70% of RLPs. RLPs, and some RLKs, are known to contain a special island region that is crucial for recognizing parts of pathogens. Investigation by the RIKEN CSRS team revealed that among RLPs that contain the leucine-rich repeats, this special region was almost always located in the same place; between the 4th and 5th leucine-rich repeat. These RLPs were found to be associated with immune responses. They also discovered that the island region was located at the same position in some RLKs, nearly all of which belong to a functional group that regulates growth and development. Comparative analysis showed that the sequence of the four repeats below the island region was very similar between the two types of protein detectors, suggesting that they have a common evolutionary ancestry. In particular, these four sets of leucine repeats contained sections needed for bonding to the same co-receptor, called BAK1. This means that immunity-related RLPs and growth-related RLKs inherited the ability to bind BAK1 from a common ancestor. "Intriguingly, we found that exchanging the four regions of leucine-rich repeats among these receptors did not disrupt their functionality," says Bruno Pok Man Ngou, who conducted the study. Creating a hybrid receptor by combining a growth-related RLK with an immunity-related RLP resulted in a hybrid receptor that recognized pathogens and induced both immune and growth-related responses. This means that scientists should be able to engineer receptors with new functions by swapping those modules. This study addressed the origins of plant immunity at a molecular level, showing that simultaneously analyzing information from multiple plant genomes can allow straightforward and precise prediction of genes involved in plant immunity and growth. "We are currently isolating immune receptors from various plants using this information, aiming for practical applications such as developing disease-resistant crops in the future," says Shirasu.