A snapshot of noteworthy recent developments in the patent literature of relevance to pharmaceutical and medical research and development.
American trypanosomiasis is a neglected tropical disease and an endemic problem in 21 Latin American countries, whose treatment relies on only two US FDA-approved drugs: benznidazole and nifurtimox. Patent literature reveals vital information on new trends in therapies for various diseases, including Chagas disease. The authors used the patent databases of the world's major patent offices to generate an overview of patent trends related to the treatment of Chagas disease. A total of 50 patent families were collected and grouped as 'small molecules', 'pharmaceutical compositions of known compounds' and vaccines. From the results and interpretation, it can be concluded that the treatment of Chagas disease receives little attention in the field of patents and that the upward trend is minimal.
Conventional cancer therapies are associated with toxicity toward healthy cells, which need to be addressed by novel therapeutic approaches. US2021/0230592 patent application discloses a carbon nanotube-based approach for tumor targeting, wherein a self-assembling single-wall nanotube complex has been developed and functionalized to deliver a molecule to a cancerous cell. The radiolabeled nanotubes exhibited markedly reduced toxicity as they did not depict any 'over toxicity' up to radioactivity value of 1350 nCi. The single-wall carbon nanotube conjugates were covalently connected to several chelators, therapeutic or diagnostic radionuclides, and showed promising results in the effective cancer management. Besides, this invention with further modifications paves an ideal pathway to researchers in effective diagnosis and treatment of cancer.
A snapshot of noteworthy recent developments in the patent literature of relevance to pharmaceutical and medical research and development.
Cancer drug repurposing is an attractive approach that leads to savings in time and investment. Adapalene, the first medical application of which was for the treatment of acne, has been described as a repurposing drug for the treatment of various types of cancer. Patent application CN111329851 describes the use of adapalene for the treatment of melanoma, by assays carried out on melanoma cell lines. Adapalene demonstrated antiproliferative activity in melanoma cell lines via S-phase arrest-dependent apoptosis mediated by DNA damage through an increase in the expression of p-ATM and p-chk2 and a decrease in the expression of p-BRCA1 and Rad51. Even though no evidence on efficacy and efficiency is shown in preclinical and clinical studies, CN111329851 patent shows that adapalene may be a repurposing drug for the treatment of melanoma.
Cocrystallization has gained significant prominence in pharmaceutical product development because of the enhancement of physical, chemical and pharmacological properties of active pharmaceutical ingredients, such as stability, solubility, dissolution rate, taste, hygroscopicity, mechanical property, bioavailability, permeability and therapeutic activity. Traditionally, co-crystals can be prepared by a grinding, solvent evaporation and slurry method. However, sophisticated methods such as spa drying, hot-melt extrusion, supercritical fluid and laser irradiation are also reported to be used for producing co-crystals. The selected patent describes the development of multicomponent crystals of dasatinib, with an aim to enhance the aqueous solubility of a selected drug. However issues surrounding the toxicity, stability, large scale manufacture, in vivo performance in human beings and regulations require adequate addressal prior to exploring the commercial viability of pharmaceutical co-crystals.