Oncology Disease Therapies Based on DCL™
Background & Overview
According to the degree of harm to the body, tumors are divided into two categories: benign tumors and malignant tumors. In most cases, tumor is used to refer to the growth of cancer cells. As the second leading cause of death worldwide, 10 million people die each year from cancer. Tumors can be inherited or caused by errors or environmental stimuli that occur when normal cells multiply. Tumors can be classified according to the function or origin of cancer cells, and common ones include malignant epithelial tumors, lymphoma, myeloma, liver cancer, and gastric cancer. In recent years, a large number of antitumor treatments targeting new targets have been developed to meet the current large clinical needs in this disease area.
Deuterated drugs for Oncology Diseases
Deuteration can enhance anti-tumor and relative anti-inflammatory effects by affecting proliferation and apoptosis. Deuterated antineoplastic drugs have achieved some encouraging clinical results; for example, sorafenib, ceritinib and enzalutamide, currently in clinical trials, have shown longer half-lives and lower effective doses . In addition, deuteration can reduce the formation of toxic metabolites, thereby improving the biosafety of drugs.
Donafenib
Primary liver cancer is a common digestive tract malignant tumor worldwide. The development of targeted drugs, such as small-molecule tyrosine kinase inhibitors, can prolong overall survival in patients with advanced liver cancer. Sorafenib has been the standard first-line treatment for patients with advanced liver cancer. However, its use is limited by side effects. Donafenib can be obtained by substituting deuterium (D) for the hydrogen (H) of the methyl group (-CH3) on the sorafenib amide bond. Compared with sorafenib, it can improve overall survival in advanced liver cancer with favorable safety and tolerability.
Fig.1 CT scan of liver treated with donafenib.[1]
Deuterated Enzalutamide (ENT) Analogues
Enzalutamide (ENT), a competitive inhibitor of the androgen receptor, impairs nuclear translocation and DNA binding, leading to apoptosis in prostate cancer cells. Deuterated ENT (N-trideuteromethyl enzalutamide, d3-ENT) is a new molecular entity based on the ENT structure. Deuterium incorporation can significantly alter the metabolic and pharmacokinetic profiles of non-deuterated compounds, thereby increasing exposure to d 3 -ENT and reducing dose requirements.
Oncology Disease Therapies Based on DCL™
BOC Sciences has mature deuterium technology and one-stop drug research and development capabilities. We continue to develop new drug targets, and at the same time introduce isotopes such as deuterium atoms into active pharmaceutical ingredients to obtain better drugs. Our core DCL™ technology and complete R&D platform have unique advantages, accelerating the development of immuno-oncology drugs and other fields.
We have established a complete drug research and development and industrialization system including medicinal chemistry, biological screening, process research, quality research, registration and declaration, etc., to achieve differentiated competition in drug research and development.
References
- Li Q, Zhu H. Donafenib treatment for hepatocellular carcinoma: A case report. Medicine. 2021, 100(25).
- Jiang J, et al. Effect of N-methyl deuteration on metabolism and pharmacokinetics of enzalutamide. Drug Design, Development and Therapy. 2016, 10: 2181.
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.
