Prodrugs represent a strategic and successful approach in therapeutics, offering a unique way to enhance drug delivery, efficacy, and patient outcomes. A prodrug is a covalent modification of a drug with a chemical handle that is cleaved off inside the body, exposing the active drug. Thus, prodrugs are precursors that undergo chemical or enzymatic transformations in the body to convert into their active pharmacological form. Prodrugs are designed to optimize factors such as solubility, bioavailability, and targeted release, addressing challenges associated with the parent drug's limitations. The prodrug strategy has proven particularly valuable in improving drug stability, reducing side effects, and enhancing therapeutic specificity.
Prodrugs
Prodrugs find application across various medical fields, including oncology, infectious diseases, psychiatry and neurology, underscoring their significance in advancing drug development and optimizing treatment regimens for better overall human health. Prominent prodrug pharmaceuticals such as L-dopa (Parkinsons Disease), Tamiflu (influenza), and Prednisone (a corticosteroid for inflammation and autoimmunity) illustrate the diverse applications in treating different medical conditions. These examples underscore the versatility and value of prodrugs as therapeutics and highlight their potential as a successful, commercially proven approach to drug products.
Proven efficacy of BPH-555 against inflammation
Axelyf’s proprietary astaxanthin prodrug with nicotinuric acid, BPH-555, is effective in an arthritis model
AXL lipid library
The astaxanthin prodrug series represents the beginning of the story of proprietary chemistry at Axelyf. Our scientists have created a digital library with chemicals and formulations for mRNA delivery, starting with our own inventions and designs, to which we are adding steadily.
In August 2024, Axelyf completed acquisition of an integrated lipid library from 76bio. This molecular library of potent delivery compounds for mRNA drugs enables us to pursue best-in-class LNPs for our own product candidates and partner our technology for products of other companies in the future.
The Axelyf LNP library series (A, B, C, D) shows highly potent liver delivery and potential for extra-hepatic targeting. Potency compares favorably with industry standard formulation LP-01 (STD) which is commonly used in gene editing clinical trial programs. Several compounds show increased potency compared to LP-01.
Lipids, LNPs, RNA delivery
Lipids are abundant in nature and in the human body. They comprise a diverse class of biomolecules and play crucial roles in various biological processes, serving as essential components of cell membranes, energy storage molecules, and signaling intermediates. In the context of liposomes and lipid nanoparticles (LNPs), lipids serve as key constituents in the formulation of delivery systems around an active molecules. LNPs are composed of lipids that self-assemble into nanoparticles, providing a versatile and effective platform for drug delivery.
RNA medicines are making their debut and impact in the 21st century. From small RNA oligos to large RNAs, including mRNA, the impact of the RNA class in medicine appears limitless. In RNA vaccine development, LNPs encapsulate and protect mRNA molecules, facilitating their cellular uptake and expression. The unique properties of lipids, such as their amphiphilic nature and ability to form lipid bilayers, contribute to the stability and efficient delivery of RNA payloads. Additionally, LNPs present opportunities for targeted delivery, enhancing the therapeutic efficacy of RNA-based vaccines and medicines. The utilization of lipids in LNPs exemplifies their multifaceted role in advancing biotechnological applications, particularly in the delivery of cutting-edge therapies with significant implications for vaccine development and precision medicine.
Axelyf uses prodrugs of natural lipids, LNPs, machine learning and the expertise of its team to work on important challenges in medicines. We look for ways to employ technology on a broad basis for therapeutics, for ourselves and in partnerships of the future. delivery of cutting-edge therapies with significant implications for vaccine development and precision medicine.
Modeling & machine learning
The role of modelling and machine learning in pharmaceutical research and development has gained importance and prominence in the past two decades. Recent advancements in the field of artificial intelligence and high-performance computing have allowed for the creation of methods and tools which make in silico studies and simulations an integral part of the modern drug development workflow.
At Axelyf, we use and develop state-of-the-art AI systems to streamline and accelerate our research process. Our diverse expertise enables us to create practical and scientifically robust contributions that support efficient drug discovery and development. We have recently acquired a chemical library with a concentration of lead compounds for RNA delivery, and we are mining the data for our programs and partners (to be announced). Our ultimate goal is to deliver safe and effective products with distinctive therapeutic profiles, while reducing development time, costs, and resource usage.
Partnering and collaboration
Axelyf is exploring partnership and collaboration on AXL lipid library and capabilities to deliver best-in-class RNA-LNP technology for medicines. Please get in touch with us at info@axelyf.com if you’d like to learn more about our technology.