Autoimmune Disease Therapies Based on DCL™
Background & Overview
Autoimmune diseases are the third major diseases after cardiovascular and tumor. If the body continues to have a chronic inflammatory state, it is likely to have this type of disease. The cause of autoimmune disease is the body's systemic or localized attack on its own normal tissues. As of today, about 100 different types of autoimmune diseases have been identified, including systemic lupus erythematosus, multiple sclerosis, ankylosing spondylitis, type 1 diabetes, rheumatoid arthritis, and more. The current clinical treatment drugs can only relieve symptoms and reduce the mortality rate, and cannot cure the disease from the perspective of etiology. Therefore, the future research direction in the field of autoimmune diseases is to develop more new treatments.
Deuterated drugs for Autoimmune Diseases
Replacing the hydrogen in the active molecule group with the isotope deuterium is considered to be an excellent modification method and an effective way to break through compound patents and avoid R&D risks. Several companies are developing or have developed a series of potentially advantageous deuterated drugs to treat a variety of autoimmune and inflammatory diseases, including rheumatoid arthritis and inflammatory bowel disease.
Deuterated Tofacitinib Analogues
JAK kinases have become important targets for drugs to treat autoimmune diseases, including rheumatoid arthritis, inflammatory bowel disease, and psoriasis, as well as to treat certain types of cancer. SD-900, a specific deuterium-substituted analog of tofacitinib, is a small molecule inhibitor of the Janus kinase family. Deuterium is safe, natural and non-radioactive so that it does not change the shape or electronic structure of the molecule, so it does not change the binding properties of the drug. Not only that, these deuterated compounds have a beneficial effect on prolonging the half-life of the drug. In conclusion, SD-900 will have comparable efficacy to tofacitinib, but with the promise of improved drug properties.
Deucravacitinib
TYK2 inhibitors can reduce symptoms of several autoimmune diseases, including psoriasis, multiple sclerosis, Crohn's disease, ulcerative colitis and ankylosing spondylitis. Deucravicitinib is a deuterated small molecule TYK2 inhibitor used to treat a variety of autoimmune diseases. Deucravicitinib selectively targets TYK2, thereby inhibiting interleukin (IL)-23, IL-12, and type 1 interferon (IFN) signaling, resulting in allosteric inhibition of TYK2 and its downstream functions.
Fig.1 Structural formula of Deucravicitinib.[1]
Autoimmune Disease Therapies Based on DCL™
Our DCL™ platform is used for the deuteration of approved drugs, advanced clinical candidates or previously studied biologically active compounds. In this way, better pharmacokinetic or metabolic properties are achieved, leading to the development of best-in-class products with improved clinical safety, tolerability or efficacy.
Our Goal
- Improve the drugs already on the market;
- Reduce toxic metabolic activity products;
- Slow down or prevent the isomerization inactivation of the drug;
- Explore other biological effects caused by deuterium.
Reference
- Treitler D S, et al. Development of a Commercial Process for Deucravacitinib, a Deuterated API for TYK2 Inhibition. Organic Process Research & Development. 2022, 26(4): 1202-1222.
Customer Intellectual Property Protection
BOC Sciences has always regarded intellectual property as the most valuable asset of the company and its customers. We have signed non-disclosure agreements with customers and employees before the project starts, and provide synthetic route design and synthesis services in strict accordance with the terms of the non-disclosure agreement, striving to provide customers with target compounds in the shortest time possible.
