Article
Plant Sciences
Guiying Zhang, Yanping Zhang, Xianjie Ma, Xin Yang, Yuyan Cai, Wenli Yin
Summary: This study revealed the inhibitory effect of pogostone on the activity of CYP3A4, 2C9, and 2E1, suggesting potential risks during the co-administration of pogostone and drugs metabolized by these CYP450s. The study design provides a reference for further in vivo investigations to validate the potential interaction.
PHARMACEUTICAL BIOLOGY
(2021)
Article
Toxicology
Zhe Wang, Xiaoyu Wang, Zhen Wang, Yaqin Jia, Yuyi Feng, Lili Jiang, Yangliu Xia, Jun Cao, Yong Liu
Summary: Osimertinib demonstrates high inhibitory effects on human UDP-glucosyltransferases (UGTs) and human liver microsomes (HLMs), especially competitive inhibition against UGT1A1. At a dose of 80 mg/day, osimertinib shows a low risk of interaction via liver metabolism but a potential risk of interaction in the intestine.
TOXICOLOGY LETTERS
(2021)
Article
Pharmacology & Pharmacy
Ya-nan Liu, Xinhao Xu, Jingjing Nie, Yingying Hu, Xuegu Xu, Ren-ai Xu, Xiaoxiang Du
Summary: This study developed a UPLC-MS/MS method to determine the concentrations of flumatinib and its metabolite M1. The results showed that ketoconazole, posaconazole, and isavuconazole had stronger inhibitory effects on flumatinib metabolism compared to itraconazole, fluconazole, and voriconazole. Pharmacokinetic experiments in rats indicated that isavuconazole significantly altered the pharmacokinetic parameters of flumatinib, but had no effect on the metabolism of M1. Therefore, the study concluded that isavuconazole may increase the plasma concentration of flumatinib, highlighting the importance of monitoring the interactions between flumatinib and isavuconazole in clinical applications.
FRONTIERS IN PHARMACOLOGY
(2023)
Article
Pharmacology & Pharmacy
Rakshit S. Tanna, Dan-Dan Tian, Nadja B. Cech, Nicholas H. Oberlies, Allan E. Rettie, Kenneth E. Thummel, Mary F. Paine
Summary: Kratom's main alkaloid mitragynine has been shown to be a time-dependent inhibitor of hepatic and intestinal cytochrome P450 3A activity, potentially causing serious pharmacokinetic interactions with drugs. A static model predicted that mitragynine would increase systemic exposure to the probe drug midazolam by approximately 5.7-fold.
JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS
(2021)
Article
Biochemistry & Molecular Biology
Martin Kondza, Mirza Bojic, Ivona Tomic, Zeljan Males, Valentina Rezic, Ivan Cavar
Summary: Flavonoids like chrysin can effectively inhibit the activity of the CYP3A4 enzyme, without showing pseudo-irreversible inhibition. While interacting with heme, no inhibitor-heme adducts were formed. These results suggest that flavonoids have the potential to inhibit CYP3A4 enzyme and interact with other drugs.
Article
Pharmacology & Pharmacy
Luc R. A. Rougee, David W. Bedwell, Kasi Hansen, Trent L. Abraham, Stephen D. Hall
Summary: This study investigated the influence of allosteric effectors on the metabolism of the cytochrome P450 3A4 substrate midazolam, as well as their impact on time-dependent inhibition of CYP3A4. The presence of allosteric effectors altered the metabolism and inactivation efficiency of CYP3A4, suggesting that their absence may affect the accuracy of drug-drug interaction predictions.
DRUG METABOLISM AND DISPOSITION
(2023)
Article
Pharmacology & Pharmacy
Lien Thi Ngo, Jaeyeon Lee, Hwi-yeol Yun, Jung-woo Chae
Summary: Tegoprazan is a novel P-CAB for the treatment of GERD and H. pylori infections. It is mainly metabolized by CYP3A4, so the investigation of DDI between tegoprazan and CYP3A4 perpetrators is crucial. Clarithromycin and rifampicin were selected as case studies to evaluate the DDI potential.
Article
Pharmacology & Pharmacy
Jie Yu, Fengxian Zou, Lifang Zhao
Summary: This study evaluated the CYP450 inhibition of Epifriedelanol and found that it can inhibit the activity of CYP3A4, CYP2E1, and CYP2C9, which may lead to significant clinical adverse drug interactions.
LATIN AMERICAN JOURNAL OF PHARMACY
(2022)
Article
Biochemistry & Molecular Biology
Liyan Wang, Tingting Zhao, Yunxiang Wang, Banglian Hu, Jianfei Tao, Jinshan Ke, Tingfei Wei, Guangbo Ge, Qiang Meng, Changyuan Wang, Qi Liu, Huijun Sun, Jingjing Wu, Yanwei Chen
Summary: Imatinib, sunitinib, and gefitinib are common tyrosine kinase inhibitors with varying inhibitory effects on CYP3A. Imatinib showed the strongest inhibitory effect, while sunitinib and gefitinib had comparable but weaker effects. The presence of more N-heterocycles in imatinib may explain its stronger inhibitory effect.
CURRENT DRUG METABOLISM
(2021)
Article
Chemistry, Medicinal
Jiangnan Dong, Su Li, Guangxuan Liu
Summary: Binimetinib was demonstrated to display reversible and time-dependent inhibitory effects on human CYP1A2, which may have implications for its toxicity.
CHEMICAL RESEARCH IN TOXICOLOGY
(2021)
Article
Pharmacology & Pharmacy
Ji-Min Kim, Seong-Wook Seo, Dong-Gyun Han, Hwayoung Yun, In-Soo Yoon
Summary: The study found that quercetin significantly influences the metabolism of repaglinide, increasing its exposure in the body. This suggests that quercetin may have clinically significant pharmacokinetic interactions with repaglinide depending on intake from foods and dietary supplements.
Article
Chemistry, Medicinal
Bo-Wen Zhang, Ni-Hong Pang, Ren-Ai Xu, Gao-Er Qu, Cong-Rong Tang
Summary: Axitinib inhibits the metabolism of buspirone, potentially increasing the risk of side effects in clinical settings.
DRUG DESIGN DEVELOPMENT AND THERAPY
(2022)
Article
Pharmacology & Pharmacy
Muhammad Erfan Uddin, Zahra Talebi, Sijie Chen, Yan Jin, Alice A. Gibson, Anne M. Noonan, Xiaolin Cheng, Shuiying Hu, Alex Sparreboom
Summary: Research showed that many tyrosine kinase inhibitors (TKIs) strongly inhibit the function of renal transporter MATE1, potentially affecting the elimination of oxaliplatin, without increasing the risk of kidney injury.
Article
Pharmacology & Pharmacy
Bo Wang, Chao Shi, Lei Feng, Wei Pan, Xiang-Ge Tian, Cheng-Peng Sun, Chao Wang, Jing Ning, Xia Lv, Yan Wang, Qian-Hui Yuan, Rui-Xuan Guan, Hou-Li Zhang, Xiao-Chi Ma, Tong-Hui Ma
Summary: This study evaluated the inhibitory effects of nearly hundred kinds of herbal medicines against CYP3A4 enzyme and found that biflavones in Ginkgo biloba and Selaginella tamariscina have strong inhibitory effects on CYP3A4. Additionally, potential pharmacokinetic interactions were identified between these biflavones and clinical drugs.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Oncology
Yonggang Sha, Jian Wu, Barry Paul, Yue Zhao, Parker Mathews, Zhiguo Li, John Norris, Endi Wang, Donald P. McDonnell, Yubin Kang
Summary: This study reveals for the first time the transcriptional regulation of CRBN by PPAR and demonstrates that drug-drug interactions between PPAR agonists and lenalidomide may impact the treatment outcomes of multiple myeloma. High PPAR expression is correlated with poor clinical outcomes.