Article
Biochemistry & Molecular Biology
Icaro Salgado Perovani, Jade Lorena Mariano Bucci, Daniel Blascke Carrao, Maike Felipe Santos Barbetta, Rodrigo Moreira da Silva, Norberto Peporine Lopes, Anderson Rodrigo Moraes de Oliveira
Summary: Ethofumesate, a chiral herbicide, and its main metabolite ethofumesate-2-hydroxy may exhibit enantioselective inhibition of CYP2C19. The study found that (-)-ethofumesate showed nearly twice the inhibition potency towards CYP2C19 compared to (+)-ethofumesate.
CHEMICO-BIOLOGICAL INTERACTIONS
(2021)
Article
Biochemistry & Molecular Biology
Diksha Manhas, Shipra Bhatt, Garima Rai, Vinay Kumar, Sahil Bharti, Sumit Dhiman, Shreyans K. Jain, Deepak K. Sharma, Probir Kumar Ojha, Sumit G. Gandhi, Anindya Goswami, Utpal Nandi
Summary: CYP2C8 is a crucial enzyme responsible for metabolizing substances in the body. Rottlerin, a compound with anticancer properties, was found to strongly inhibit CYP2C8 and affect its gene expression. These findings are important for further research in cancer therapy.
CHEMICO-BIOLOGICAL INTERACTIONS
(2023)
Article
Pharmacology & Pharmacy
Xu Wang, Jingjing Fa, Yuanjin Zhang, Shengbo Huang, Jie Liu, Junqing Gao, Lina Xing, Zongjun Liu, Xin Wang
Summary: There is a potential interaction between Danshen tablet and rivaroxaban as the former inhibits the metabolism of the latter. This may be due to the strong inhibitory effects of Danshen tablet's components, particularly dihydrotanshinone I, on CYP enzymes. Therefore, drug monitoring and dosage adjustment are necessary when Danshen tablet and rivaroxaban are used simultaneously in clinical practice.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Biology
Victoria Furio, Miguel Moreno-Molina, Alvaro Chiner-Oms, Luis M. Villamayor, Manuela Torres-Puente, Inaki Comas
Summary: Victoria Furio et al. used functional genomics and evolutionary analyses to study antibiotic resistance in tuberculosis, identifying novel candidate genes with resistance mutations in clinical strains and uncovering the mechanisms underlying drug resistance.
COMMUNICATIONS BIOLOGY
(2021)
Article
Biochemistry & Molecular Biology
Pin Jiang, Tao Chen, Lin-Feng Chu, Ren-Peng Xu, Jin-Ting Gao, Li Wang, Qiang Liu, Lily Tang, Hong Wan, Ming Li, Hong-Can Ren
Summary: This study aims to improve the accuracy of DDI prediction using PBPK models by integrating in vitro fm data. The results demonstrate that the integration of in vitro fm method performs better compared to in silico fm method and fm of 100% method. The study highlights the importance of in vitro fm data in predicting DDIs and shows the promising potential of in silico fm in DDI prediction.
EXPERT OPINION ON DRUG METABOLISM & TOXICOLOGY
(2023)
Review
Chemistry, Medicinal
Archana K. Thikekar, Asha B. Thomas, Sohan S. Chitlange
Summary: The global diabetes epidemic is a major cause of fatality and lethality, with the use of medicinal plants becoming increasingly popular for disease treatment. However, more high-quality research is needed to evaluate the efficacy of herbal medicines, reduce side effects, and improve patient safety.
PHYTOTHERAPY RESEARCH
(2021)
Article
Pharmacology & Pharmacy
Louise Breuil, Nora Ziani, Sarah Leterrier, Gaelle Hugon, Fabien Caille, Viviane Bouilleret, Charles Truillet, Maud Goislard, Myriam El Biali, Martin Bauer, Oliver Langer, Sebastien Goutal, Nicolas Tournier
Summary: This study investigated the impact of CYP inducers and inhibitors on the brain and plasma kinetics of [C-11]metoclopramide using PET imaging. The results showed that CYP induction or inhibition had negligible effects on the plasma kinetics and metabolism of [C-11]metoclopramide, but ritonavir significantly increased brain penetration.
Article
Pharmacology & Pharmacy
Lara Marques, Nuno Vale
Summary: Drug-drug interactions (DDIs) are a significant concern, especially for patients undergoing polytherapy. This study investigated the interaction between salbutamol and fluvoxamine through in silico approaches. The results showed that co-administering salbutamol with fluvoxamine increased salbutamol exposure, particularly at higher fluvoxamine dosages.
Article
Microbiology
Rokeya Tasneen, Andrew Garcia, Paul J. Converse, Matthew D. Zimmerman, Veronique Dartois, Ekaterina Kurbatova, Andrew A. Vernon, Wendy Carr, Jason E. Stout, Kelly E. Dooley, Eric L. Nuermberger
Summary: A recent trial showed that a 4-month regimen of rifapentine, pyrazinamide, moxifloxacin, and isoniazid is as effective as the standard 6-month treatment. Novel regimens replacing rifapentine and isoniazid with bedaquiline and another drug demonstrated increased sterilizing activity in mouse models of tuberculosis.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2022)
Article
Pharmacology & Pharmacy
Dhruvitkumar S. Sutaria, Grozdana Rasuo, Adam Harris, Ryan Johnson, Dale Miles, Jorge Daniel Gallo, Rucha Sane
Summary: This study evaluated the pharmacokinetics, safety, and tolerability of Ipatasertib and Daholutamide in patients with metastatic castration-resistant prostate cancer. The results showed a mild reduction in the exposure of Ipatasertib when administered in combination with Daholutamide, which was not clinically significant. Additionally, the combination therapy was well-tolerated with minimal side effects in patients.
Article
Toxicology
Jing Gao, Yuanjin Zhang, Xueqin Lei, Yuan Xu, Zhenliang Sun, Xin Wang
Summary: Hydroxygenkwanin (HGK), a natural flavonoid extracted from Daphne genkwa Sieb.et Zucc., exhibits a wide range of pharmacological activities and it competitively inhibits CYP1A2 and 2C enzymes. The inhibitory effect of HGK on CYP enzymes is weaker than diosmetin, possibly due to the substitution of hydroxyl and methoxy in the A and B rings of the flavone skeleton, which may lead to potential drug-drug interactions and toxicity.
TOXICOLOGY IN VITRO
(2022)
Article
Medicine, Research & Experimental
Peng-Xin Ge, Li-Ping Jiang, Ting Tai, Ting Zhu, Jin-Zi Ji, Yi-Fei Li, Qiong-Yu Mi, Hong-Guang Xie
Summary: Short-term standard alcohol consumption significantly enhances the inhibitory effects of clopidogrel on platelet aggregation and activation through the inhibition of the Nrf2/Ces1 signaling pathway and induction of Cyp2c. This suggests that alcohol may interact with drugs primarily metabolized by CES1 or CYP2C, such as clopidogrel, possibly affecting patient care.
Article
Pharmacology & Pharmacy
Eric Helmer, Negin Karimian, Karen Van Assche, Ineke Seghers, Sandrine Le Tallec, Ganesh Cherala, Graham Scott, Florence S. Namour
Summary: The study found that ziritaxestat is a weak inhibitor and inducer of cytochrome P450 (CYP) 3A4, with potential drug-drug interactions with oral contraceptives. Co-administration of ziritaxestat and an oral contraceptive led to significant changes in the pharmacokinetic parameters of the contraceptive, particularly an increase in the concentration of ethinyl estradiol (EE), which was not due to CYP3A4 inhibition. The study also revealed that ziritaxestat inhibits sulfation but has little effect on glucuronidation. Therefore, the importance of assessing enzymes other than CYP3A4 in investigating potential drug-drug interactions with oral contraceptives is highlighted.
CLINICAL PHARMACOLOGY & THERAPEUTICS
(2022)
Article
Pharmacology & Pharmacy
Johanna Weiss, Kathrin Isabelle Foerster, Maria Weber, Jurgen Burhenne, Gerd Mikus, Thorsten Lehr, Walter Emil Haefeli
Summary: The metabolite of ketoconazole, N-deacetyl ketoconazole (DAK), is found to inhibit several enzymes and drug transporters in humans, which might affect the efficacy of ketoconazole.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2022)
Review
Medicine, Research & Experimental
Xian Zhou, Ling Fu, Pengli Wang, Lan Yang, Xiaoshu Zhu, Chun Guang Li
Summary: The use of herbal medicine globally presents challenges in managing potential drug-herb interactions, which can have beneficial or negative effects on therapeutic outcomes. Scutellaria baicalensis and its bioactives show synergistic interactions with many pharmaceutical drugs to enhance efficacy, reduce toxicity, or overcome drug resistance. However, they also influence the pharmacokinetic profile of many drugs, highlighting the importance of understanding these interactions for safe use of herbal medicines.
BIOMEDICINE & PHARMACOTHERAPY
(2021)
Article
Biochemistry & Molecular Biology
Katsunori Sasahara, Akira Mashima, Tatsusada Yoshida, Hiroshi Chuman
BIOORGANIC & MEDICINAL CHEMISTRY
(2015)
Article
Chemistry, Medicinal
Tatsusada Yoshida, Takahisa Hayashi, Akira Mashima, Katsunori Sasahara, Hiroshi Chuman
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2016)
Article
Chemistry, Medicinal
Tatsusada Yoshida, Akira Mashima, Katsunori Sasahara, Hiroshi Chuman
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2014)
Article
Neurosciences
Shogo Haraguchi, Katsunori Sasahara, Hanako Shikimi, Shin-ichiro Honda, Nobuhiro Harada, Kazuyoshi Tsutsui
Article
Chemistry, Medicinal
Akira Mashima, Masahiro Kurahashi, Katsunori Sasahara, Tatsusada Yoshida, Hiroshi Chuman
MOLECULAR INFORMATICS
(2014)
Article
Pharmacology & Pharmacy
Hiroyuki Sasabe, Toshihisa Koga, Masayuki Furukawa, Masayuki Matsunaga, Katsunori Sasahara, Kenta Hashizume, Yoshihiro Oozone, Immaculate Amunom, Mikako Torii, Ken Umehara, Eiji Kashiyama, Kenji Takeuchi
Summary: The in vitro study on brexpiprazole showed weak inhibitory effects on CYP enzymes and transporters, indicating unlikely clinically relevant drug interactions.
Article
Pharmacology & Pharmacy
Katsunori Sasahara, Masakazu Shibata, Hiroyuki Sasabe, Tomoki Suzuki, Kenji Takeuchi, Ken Umehara, Eiji Kashiyama
Summary: The study aimed to design new chemical entities with desirable pharmacokinetic profiles by obtaining indicators of physicochemical parameters and structurally active sites through machine learning models. Prediction models for metabolic stability and substrate recognition, as well as models showing structurally active sites, were developed efficiently to optimize lead compounds.
DRUG METABOLISM AND PHARMACOKINETICS
(2021)
Article
Microbiology
Masakazu Shibata, Masatoshi Masuda, Katsunori Sasahara, Hiroyuki Sasabe, Tomohiro Sasaki, Seongryul Kim, Kenji Takeuchi, Ken Umehara, Eiji Kashiyama
Summary: Delamanid has been extensively studied and approved for the treatment of pulmonary multidrug-resistant tuberculosis. This study investigated the potential of delamanid in treating extrapulmonary tuberculosis by simulating its pharmacokinetic profile in various tissues. The results suggest that delamanid may achieve concentrations in extrapulmonary organs similar to that of the lung, indicating its potential for treating extrapulmonary tuberculosis.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2021)
Article
Pharmacology & Pharmacy
Katsunori Sasahara, Masakazu Shibata, Hiroyuki Sasabe, Tomoki Suzuki, Kenji Takeuchi, Ken Umehara, Eiji Kashiyama
Summary: The study built high-performance machine learning pharmacokinetic prediction models and found that predictions outside of a specific applicability domain are unreliable and could mislead new compound design. Another model was constructed to determine if a new compound is within the applicability domain, evaluated through multidimensional accuracy assessment.
DRUG METABOLISM AND PHARMACOKINETICS
(2021)
Article
Pharmacology & Pharmacy
Masakazu Shibata, Yoshihiko Shimokawa, Katsunori Sasahara, Noriaki Yoda, Hiroyuki Sasabe, Mitsunari Suzuki, Ken Umehara
BIOPHARMACEUTICS & DRUG DISPOSITION
(2017)
Article
Pharmacology & Pharmacy
Yoshihiko Shimokawa, Katsunori Sasahara, Noriyuki Koyama, Kazuyoshi Kitano, Masakazu Shibata, Noriaki Yoda, Ken Umehara
DRUG METABOLISM AND DISPOSITION
(2015)
Article
Neurosciences
Katsunori Sasahara, Hanako Shikimi, Shogo Haraguchi, Hirotaka Sakamoto, Shin-ichiro Honda, Nobuhiro Harada, Kazuyoshi Tsutsui
JOURNAL OF NEUROSCIENCE
(2007)
Article
Pharmacology & Pharmacy
Katsunori Sasahara, Yoshihiko Shimokawa, Yukihiro Hirao, Noriyuki Koyama, Kazuyoshi Kitano, Masakazu Shibata, Ken Umehara
DRUG METABOLISM AND DISPOSITION
(2015)