Deuteration involves the substitution of hydrogen atoms in a drug compound with deuterium, a stable and non-radioactive isotope of hydrogen. This seemingly minor change can lead to significant differences in a drug's metabolic pathway, drug's pharmacokinetic and pharmacodynamic properties, offering benefits such as improved metabolic stability, reduced side effects, and enhanced therapeutic efficacy. This is attributed to the kinetic isotope effect, where the stronger C-D (carbon-deuterium) bond compared to the C-H (carbon-hydrogen) bond slows down metabolism, thereby prolonging the drug's half-life and reducing side effects. Nowadays, deuterated drugs have become a groundbreaking advancement in pharmaceutical sciences, and since the beginning of this century, they have been developed for the treatment of neurological diseases, genetic diseases, tumor, and virus infection.
What Can We Offer?
Alfa Chemistry is a leader in the field of stable isotopes science and provides a broad range of products and services for the development of deuterated drugs.
Products
Services
Products
In the realm of deuterated drug development, we offer a diverse array of high-quality products designed with precision for deuterated drugs development. Our products undergo rigorous research and development phases, ensuring they meet the highest standards of safety and efficacy. Our products include:
View More ➞
Services
Apart from product offerings, our comprehensive services encompass the entire spectrum of deuterated drug development. We provide extensive support in early-stage research, compound synthesis, and analytical testing. Our services include:
View More ➞
Typical Deuterated Drugs
Deuterated drugs have begun to establish themselves in the pharmaceutical landscape, showcasing significant improvements over their non-deuterated versions. These examples include:
Deutetrabenazine (Austedo): One of the most prominent examples of a deuterated drug is deutetrabenazine, marketed as Austedo. It is approved for treating Huntington's disease-associated chorea and tardive dyskinesia. Deutetrabenazine is a deuterated form of tetrabenazine. In tetrabenazine, rapid metabolism leads to fluctuating drug levels, requiring multiple daily doses and increasing the risk of side effects like sedation and depression. By substituting hydrogen atoms with deuterium, deutetrabenazine exhibits slower metabolism, resulting in improved pharmacokinetics, reduced dosing frequency, and fewer side effects.
Fig. 1. The structures of Tetrabenazine and Austedo.
Donafenib: Donafenib is another prominent example of deuterated drug. It is deuterated derivative of sorafenib, a multi-kinase inhibitor used to treat cancers such as hepatocellular carcinoma (HCC) and thyroid cancer. By introducing deuterium atoms into sorafenib's molecular structure, researchers aimed to enhance the drug's pharmacological profile while maintaining its therapeutic potency. In 2021, donafenib was approved in China for the treatment of unresectable hepatocellular carcinoma, marking it as a significant step forward in the clinical use of deuterated drugs.
Fig. 2. The structure of Donafenib.
Benefits of Deuterated Drugs
- Enhanced Metabolic Stability: The stronger carbon-deuterium bonds slow the metabolism of drugs, reducing the production of potentially harmful metabolites.
- Improved Therapeutic Efficacy: By modulating the rate of drug breakdown, deuteration can enhance a compound's therapeutic effect, leading to better outcomes for patients.
- Reduced Side Effects: Slower metabolism can minimize the formation of toxic metabolites, improving the safety profile of deuterated drugs.
- Lower Dosage Requirements: Enhanced bioavailability and slower clearance rates may reduce the required dosage, improving patient compliance and reducing treatment costs.
Deuterated drug development is a promising frontier in modern medicine, offering a blend of innovation, improved safety, and enhanced efficacy. By leveraging the unique properties of deuterium, pharmaceutical companies can optimize existing therapies and pioneer new treatments that address unmet medical needs. Through our comprehensive products and services, we aim to accelerate the development of deuterated drugs, supporting researchers and companies in bringing these groundbreaking therapies to patients worldwide.
Please kindly note that our products and services are for research use only.
