1. Pharmacokinetic interaction study between sorafenib and dapagliflozin in rats
Xueru HE ; Yuhao FU ; Xuejiao XUN ; Xueru HE ; Ying LI ; Yinling MA ; Yuhao FU ; Xuejiao XUN ; Zhanjun DONG
Chinese Journal of Clinical Pharmacology and Therapeutics 2023;28(5):498-507
AIM: To explore the pharmacokinetic interactions between sorafenib and dapagliflozin in rats and to provide some theoretical basis for the rational clinical use of the two drugs. METHODS: An ultra -performance liquid chromatography-tandem mass spectrometry (UPLC / MS / MS) method was developed for the simultaneous determination of sorafenib and dapagliflozin. Male SD rats were randomly divided into 5 groups (6 rats in each group), including 100 mg / kg sorafenib group, 0.5 mg / kg dapagliflozin group, 1 mg / kg dapagliflozin group, and 100 mg/kg sorafenib combined with 0.5 mg/kg dapagliflozin group and 100 mg/kg sorafenib combined with 1 mg / kg dapagliflozin group, for sorafenib and dapagliflozin drug interaction study. All samples were analyzed using a validated UPLC/ MS/MS method, and the main pharmacokinetic parameters were calculated by compartment model. RESULTS: 1 mg/kg dapagliflozin increased the C
2. Clinical research progress of palbociclib in treatment of breast cancer
Zhi WANG ; Xin ZHOU ; Xueru HE ; Yuhao FU ; Xuejiao XUN ; Zhi WANG ; Xin ZHOU ; Xueru HE ; Yuhao FU ; Xuejiao XUN ; Ying LI ; Zhanjun DONG
Chinese Journal of Clinical Pharmacology and Therapeutics 2023;28(2):205-213
Palbocicril, the first cyclin-dependent kinases 4 and 6 inhibitors, is a crucial milestone in the development history of antineoplastic drugs. It combined with aromatase inhibitor or fulvestrant as first-line, second-line or post-line therapy has good efficacy and safety for hormone receptor-positive, human epidermal growth factor receptor-2 negative locally advanced or metastatic breast cancer, which has a good application prospect. This article summarizes the clinical trials and safety studies related to palbociclib.
3. Advances in uridine diphosphate glucuronosyltransferase-mediated drug interactions with tyrosine kinase inhibitors
Xueru HE ; Yuhao FU ; Xuejiao XUN ; Yanjun CUI ; Xueru HE ; Yuhao FU ; Xuejiao XUN ; Yanjun CUI ; Zhanjun DONG
Chinese Journal of Clinical Pharmacology and Therapeutics 2022;27(8):936-945
Drug-drug interactions (DDI) of tyrosine kinase inhibitors (TKIs) mediated by metabolic enzymes and transporters have become an important issue in clinical practice recently. In addition to CYP450 enzymes, uridine diphosphate glucuronidases (UGTs) are another class of metabolic enzymes involved in the metabolism of TKIs, and most TKIs can inhibit the UGTs in vitro. Potential clinically meaningful DDIs may occur with the co-administration of TKIs and substrates or inhibitors of UGTs. This paper will mainly focus on the UGTs-mediated drug-drug and the effect of UGT1A genotype on the drug interactions of TKIs and explores strategies to address, aiming to provide clinicians and pharmacists with references for the safe and rational application of TKIs.
4.Research advances in signaling pathways associated with potential anti-liver fibrosis drugs and targets
Xin ZHOU ; Zhi WANG ; Xueru HE ; Yuhao FU ; Xuejiao XUN ; Ying LI ; Zhanjun DONG
Journal of Clinical Hepatology 2023;39(12):2932-2941
Liver fibrosis is a key step in the progression of chronic liver diseases to liver cirrhosis and even liver cancer. In recent years, a large number of studies have shown the necessity of intervening in the process of liver fibrosis, and various anti-liver fibrosis drugs and active ingredients have been discovered. Non-coding RNAs also play an important role in the process of liver fibrosis, and searching for upstream non-coding RNAs that can regulate signaling pathways can provide new insights for anti-liver fibrosis treatment. This article introduces the process of liver fibrosis mediated by the TGF-β, Wnt/β-catenin, PI3K/Akt/mTOR, NF-κβ, Hippo, and MAPK signaling pathways, lists the latest anti-liver fibrosis drugs or active components in each signaling pathway, and summarizes the research advances in anti-liver fibrosis targets and drugs mediated by related non-coding RNAs, so as to provide new research ideas and treatment methods for anti-liver fibrosis treatment.