Latest Articles3CL protease is an ideal target for the research and development of anti-new coronavirus drugs. In this paper, the patent application situation of 3CL protease inhibitors in the field of anti-SARS-CoV-2 was analyzed. The focuses were put on the application time distribution, profile of patent applicants, and status of key products related to 3CL protease inhibitors, to reflect the global patent application trend, reveal the patent barriers faced by our country in the research and development of the drug, and provide support for the drug research and development. Combined with the results of patent analysis, this paper suggested that Chinese applicants expand their research and development ideas based on traditional Chinese medicine resources, and at the same time pay attention to the layout of overseas patents, and accelerate the in-depth integration of production, education, and research.
Primary brain cancer is a heterogeneous group of tumors arising from cells within the central nervous system. The cure rate and survival period of patients with common malignant primary brain cancers are low, and their treatment methods and therapeutic effects are also quite limited. Therefore, it is necessary to construct appropriate tumor models to study the molecular biology of the disease, preclinical pharmacodynamic and safety evaluation of new anti-tumor drugs and/or the therapeutic methods. This review summarizes the research progress of in vitro and in vivo models of primary brain cancer. In vitro models mainly include the culture of brain cancer cell line, organoids and the brain slices. In vivo models mainly include the rodent models and other model organisms such as the fruit fly and zebrafish. At present, lots of primary brain cancer disease models with their own advantages and disadvantages have been developed, but these models cannot fully simulate the complexities of brain tumors in humans. Therefore, researchers are developing more complex disease models based on the existing models to study the primary brain tumor treatment methods, screen and evaluate therapeutic drugs.
To determine the key influencing factors on formation of prasugrel hydrogen sulfate polymorph during the reactive crystallization of prasugrel free alkali and sulfuric acid, clarify the rule of the influences of solvent, temperature, and supersaturation, and reveal the mechanism of prasugrel hydrogen sulfate polymorph formation.
Based on combined application of X-ray diffraction spectroscopy (PXRD), differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA), this study focused on the crystallization thermodynamics and reactive crystallization process of prasugrel hydrogen sulfate. The stability relationship between the polymorphs of prasugrel hydrogen sulfate and the influencing rule of polymorph formation during reaction crystallization were investigated.
It was shown that solvent and supersaturation were the key factors affecting the formation of prasugrel hydrogen sulfate polymorphs.
Prasugrel hydrogen sulfate form Ⅰ and form Ⅱ are monotropically related systems, and form Ⅱ is a stable form. Solvent plays a leading role in the formation of prasugrel hydrogen sulfate polymorphs, and the formation of polymorphs in butanol obeys to the Ostwald's rule.
As the "sacred product for nourishing blood" and "sacred medicine for gynecology", Colla corii asini has a long history, wide application, and the effect of nourishing blood and nourishing. The chemical components of Colla corii asini are mainly protein and its degradation products, carbohydrates, trace elements, volatile substances, and fatty acids. It has various pharmacological effects, such as nourishing the blood and activating blood circulation, optimizing immune response, improving Alzheimer's disease, anti-oxidation, anti-fatigue, protecting lung injury, delaying aging, and treating gynecological diseases. Due to the nourishing blood and nourishing effect of Colla corii asini, its annual output is soaring year by year, and it enjoys a high reputation in domestic and foreign markets. In this paper, Colla corii asini is reviewed from three aspects: chemical composition, pharmacological action, and quality control by consulting relevant literature at home and abroad, in order to provide reference and inspiration for the further development and utilization of Colla corii asini.
To study and analyze the development and vaccination of corona virus disease 2019 (COVID-19) vaccines in four major countries represented by China to understand the current situation of COVID-19 vaccine availability.
The policies and plans of vaccine development in each stage were refined and summarized and then classified and counted according to the approval types and time, and descriptive statistical analysis was carried out on the relevant data from development to vaccination.
Up to March 31, 2022, the effectiveness of 13 COVID-19 vaccines developed by China, the United Kingdom, the United States and Russia were all higher than the minimum standard of the WHO (50%). China had made the largest contribution in terms of supply. In terms of vaccination volume, China had exceeded 3.27 billion doses, ranking the leading position.
Vaccine purchase funds, distribution plan defects, vaccine nationalism, COVID-19 strain variation and other obstacles to effective vaccine access can be ensured and achieved by accelerating research and development, increasing production, fair distribution and expanding vaccination.
To retrospectively analyze the cardiac adverse events and death cases of EGFR inhibitors through data mining of FDA adverse reaction reporting system (FAERS), so as to better understand the safety of EGFR inhibitors.
The data in a total of 36 quarters in FAERS database from 2013 to 2021 were mined and analyzed by reporting odds ratio (ROR).
A total of 30 728 493 adverse events were reported in FAERS database from 2013 to 2021, including 735 693 cardiac adverse events. The effective signals were cetuximab [ROR=1.16, 95%CI (1.07,1.26)], rituximab [ROR=2.94, 95%CI (1.61,5.36)], dactinib [ROR=3.73, 95%CI (2.10,6.62)], and ositinib [ROR=1.55, 95%CI (1.44,1.66)]. McAbs were more likely to cause tachycardia. All heart-related effective signals of TKIs contained pericardial effusion. The significant death signals were panizumab [ROR=1.71, 95%CI (1.54,1.89)], gefitinib [ROR=2.93, 95%CI (2.64,3.25)], erlotinib [ROR=6.72, 95%CI (6.54,6.91)], afatinib [ROR=1.30, 95%CI(1.17,1.45)], dactinib [ROR=14.24, 95%CI (11.27,17.99)], and ositinib [ROR=15.03, 95%CI (14.53,15.54)].
EGFR receptor inhibitors can cause adverse cardiac events with serious outcomes and increase the risk of death, which are worthy of clinical attention. Due to the limitations of database and detection methods, long-term data are still needed to verify these results to further understand the safety of EGFR inhibitors.
To identify new potential xanthine oxidase (XO) inhibitors through hierarchical virtual screening.
The pharmacophore model was constructed based on receptor-ligand crystal complex. And a decoy set was used to verify the pharmacophore model. On this basis, the model was used to find potential XO inhibitors from ZINC natural-products database by combining with molecular docking, ADMET prediction and molecular dynamics simulation.
The optimized pharmacophore model contained two hydrogen bond acceptors, two hydrophobic centers, one negative ionizable center and one aromatic ring center. The docking results of the decoy set indicated that the constructed pharmacophore model had high sensitivity and specificity. Molecule ZINC0934445 which was obtained through hierarchical virtual screening was predicted to have good inhibitory activity and drug-like properties. And molecular dynamics simulation results also showed that its binding free energy was better than the positive drug febuxostat.
A variety of computer virtual screening technologies were comprehensively integrated to identify novel XO inhibitors. And one potential active molecule ZINC09344458 was discovered from natural products, which would relieve pain associated with gout. This study provided an alternative method for relevant experimental studies on the development of gout therapeutic drugs.
Vitamin D is an essential fat-soluble vitamin, which plays a very important role in maintaining the dynamic balance of calcium in human body and can prevent calcium deficiency diseases such as osteoporosis and rickets. Both excess and deficiency of vitamin D pose a threat to human health, so it is necessary to establish methods for monitoring vitamin D concentrations in different matrices (e.g., pharmaceuticals, foods, biological samples, etc.). However, due to the unstable chemical properties of vitamin D and the complex matrix of vitamin D-containing samples, the pre-treatment and determination of vitamin D-containing samples have a great challenge. This paper reviews the research progress of pretreatment and determination of vitamin D in different matrices in recent years. It is reported that the most commonly used pretreatment methods are liquid-liquid extraction, solid-phase extraction and liquid-liquid microextraction, and the determination methods mainly include high performance liquid chromatography, mass spectrometry, supercritical fluid chromatography and other methods. This review is expected to provide technical support for the determination of vitamin D series preparations.
To explore the predictors of the clinical response to tofacitinib in rheumatoid arthritis (RA).
The clinical data of a cohort of 256 RA patients regularly followed up at the Department of Rheumatology and Immunology, Peking University People's Hospital were analyzed, among whom 121 patients with DAS28-ESR≥3.2 were treated with tofacitinib. Data were collected from patients starting to receive tofacitinib and at 6-month follow-up to evaluate the remission rate and analyze the predictors for achieving Boolean 3v remission.
Out of 121 patients treated with tofacitinib, 104 patients (86.0%) were treated with tofacitinib for more than 6 months and 17 patients changed medication within 6 months, including 10 patients (8.3%) due to poor efficacy and 7 patients (5.8%) for adverse effects. After 6 months of follow-up, the remission rates according to Boolean 3v, DAS28-ESR and CliDR were 72.8%, 57.0% and 44.7%, respectively. The EULAR response rate was 88.6%. Multivariable logistic regression analysis showed that gender, number of conventional synthetic DMARDs resistance and glucocorticoid combination were independent predictors for Boolean 3v remission after 6 months of tofacitinib treatment.
Female patients without glucocorticoids and a small number of conventional synthetic DMARDs resistance tend to get better response to tofacitinib.
The research and development data is the important evidence to prove the safety, effectiveness and quality control of drugs, which also is the important content in pre-approval inspection．New changes have taken place in drug pre-approval inspection after Drug Registration Administration came into force on 1 July 2020. Based on study and analysis of the observations of pre-approval inspection of chemical drugs in the past 2 years, the common problems and changes were put forward. The study provides references for registration applicants and pharmaceutical researchers to improve their quality management.
No. 86 Xueyuan South Road, Haidian District, Beijing
010-62199257
qkjq@cast.org.cn
Copyright © 2025 China Association for Science and Technology. All rights reserved. For all open access content, the relevant licensing terms apply.
Sponsored by the Office of the Leading Group for Cybersecurity and Informatization of CAST, and supported by Science and Technology Review Publishing House
