Review
Pharmacology & Pharmacy
Xiao-Qin Liu, Zi-Ran Li, Chen-Yu Wang, Yue-Ting Chen, Zheng Jiao
Summary: This review investigated the potential ethnic differences in the pharmacokinetic and pharmacodynamic characteristics of rivaroxaban between Asians and Caucasians. The findings suggest that Asians may require a lower dose of rivaroxaban compared to Caucasians. Further studies are needed to confirm this ethnic difference and optimize dosing regimens.
Article
Genetics & Heredity
Hanxu Zhang, Zhuo Zhang, Zhiyan Liu, Guangyan Mu, Qiufen Xie, Shuang Zhou, Zhe Wang, Yu Cao, Yunlong Tan, Xiaohua Wei, Dongdong Yuan, Qian Xiang, Yimin Cui
Summary: This study investigated the association between plasma miRNAs and the pharmacokinetic-pharmacodynamic (PK-PD) profiles of rivaroxaban. The results showed that miR-320a and miR-483 levels were associated with the PK and PD profiles of rivaroxaban in healthy Chinese subjects, and they may play a role by regulating specific genes.
Article
Pharmacology & Pharmacy
Shin-Yi Lin, Sung-Chun Tang, Ching-Hua Kuo, Li-Ting Ho, Yen-Bin Liu, Yu-Fong Peng, Li-Kai Tsai, Chih-Fen Huang, Jiann-Shing Jeng
Summary: This study reports on the association between direct oral anticoagulant (DOAC) concentration and clinical outcomes in Asian patients with atrial fibrillation (AF). The proportion of DOAC concentrations falling outside the expected range was higher than reported in clinical trials. Low trough concentration was associated with increased risk of systemic thromboembolism (SSE), while high trough concentration was associated with major bleeding. Measurement of trough DOAC concentration should be considered for patients at risk of concentration deviations.
CLINICAL PHARMACOLOGY & THERAPEUTICS
(2023)
Article
Pharmacology & Pharmacy
David Kallend, Robert Stoekenbroek, YanLing He, Patrick F. Smith, Peter Wijngaard
Summary: This study investigated the pharmacokinetics, pharmacodynamics, and safety of Inclisiran in patients with mild or moderate hepatic impairment compared to those with normal hepatic function. The results showed that while there was an increase in pharmacokinetic exposure, the pharmacodynamic effects remained relatively unchanged. Inclisiran was found to be safe and well tolerated in patients with mild or moderate hepatic impairment.
JOURNAL OF CLINICAL LIPIDOLOGY
(2022)
Article
Pharmacology & Pharmacy
Darko Mitrovic, Wouter Emmens, Achraf Naimi, Annerose van der Mijle, Nic Veeger, Eric van Roon, Patricia van den Bemt
Summary: The study aimed to determine the post-marketing odds ratio (OR) and reporting odds ratio (ROR) of venous thromboembolism in patients receiving direct oral anticoagulants (DOACs) compared among each other and to vitamin K antagonists (VKAs) using the World Health Organization VigiLyze database. Rivaroxaban had the highest ORs for deep vein thrombosis/pulmonary embolism compared to apixaban, dabigatran, and edoxaban, indicating a possible higher association between rivaroxaban therapy and venous thromboembolism.
CLINICAL DRUG INVESTIGATION
(2022)
Review
Pharmacology & Pharmacy
Nicola Ferri, Elisa Colombo, Marco Tenconi, Ludovico Baldessin, Alberto Corsini
Summary: Direct oral anticoagulants (DOACs) are frequently prescribed to prevent ischemic stroke in non-valvular atrial fibrillation (NVAF) patients and treat venous thromboembolism (VTE). They have a favorable risk-benefit profile compared to warfarin but may increase the risk of gastrointestinal bleeding. Polypharmacy and comorbidity in elderly patients can lead to drug-drug interactions (DDIs) with DOACs. This review summarizes potential DDIs and discusses strategies to reduce their occurrence.
Article
Instruments & Instrumentation
Pranav J. Shah, Milan P. Patel, Jigar Shah, Anroop B. Nair, Sabna Kotta, Bhavin Vyas
Summary: The present study aimed to evaluate the potential of solid dispersion adsorbate (SDA) to enhance the solubility and bioavailability of rivaroxaban (RXN). By optimizing the amount of carrier and adsorbent, SDA tablets were developed using the fusion method, which exhibited improved flowability and drug dissolution. In vivo and in vitro evaluations showed that the SDA tablets had higher bioavailability and efficacy compared to traditional tablets.
DRUG DELIVERY AND TRANSLATIONAL RESEARCH
(2022)
Article
Cardiac & Cardiovascular Systems
Xiaoye Li, Zhichun Gu, Zi Wang, Qing Xu, Chunlai Ma, Qianzhou Lv
Summary: This study investigated the impact of CYP3A4/5 polymorphisms on the clinical outcomes of rivaroxaban in NVAF patients based on PK/PD aspects. A prospective study was conducted with 165 rivaroxaban-treated NVAF patients. The study found that CYP3A4 and CYP3A5 polymorphisms were associated with variations in rivaroxaban PK/PD, and certain polymorphisms were correlated with clinical outcomes.
CARDIOVASCULAR DRUGS AND THERAPY
(2023)
Article
Pharmacology & Pharmacy
Islam R. R. Younis, Chia-Hsiang Hsueh, Cara Nelson, Andrew N. N. Billin, Mun Sang Yue, Deqing Xiao, Timothy R. R. Watkins, Ahmed A. A. Othman
Summary: This study evaluated the pharmacokinetics, pharmacodynamics, safety, and tolerability of Cilofexor in participants with normal hepatic function or hepatic impairment. The results showed that the exposure of Cilofexor was higher in participants with hepatic impairment compared to those with normal hepatic function. There were moderate correlations between Cilofexor exposure and CP score or laboratory tests components. Cilofexor was generally well tolerated, but caution and dose modification are needed for patients with moderate or severe hepatic impairment.
JOURNAL OF CLINICAL PHARMACOLOGY
(2023)
Article
Cardiac & Cardiovascular Systems
Boaz Elad, Nimra Maman, Snait Ayalon, Lee Hilary Goldstein
Summary: Direct oral anticoagulants (DOACs) are effective and safe for preventing ischemic events in atrial fibrillation (AF) patients, including those with extreme obesity. However, limited data are available on the efficacy and safety of DOACs in obese patients, and the optimal dosing strategies remain unknown.
AMERICAN JOURNAL OF CARDIOLOGY
(2023)
Article
Chemistry, Multidisciplinary
Xiao-qin Liu, Yu-fei Zhang, Hong-yan Ding, Ming-ming Yan, Zheng Jiao, Ming-kang Zhong, Chun-lai Ma
Summary: This study conducted a population PK-PD analysis of rivaroxaban in Chinese NVAF patients and found that the PK of rivaroxaban can be adequately described using a one-compartment model. Estimated glomerular filtration rate (eGFR) was identified as a major covariate for apparent clearance. The study also showed that individualized dosing based on eGFR and liver function may be necessary to optimize treatment outcomes.
ACTA PHARMACOLOGICA SINICA
(2022)
Article
Hematology
Catherine Lai, Diane E. Cole, Seth M. Steinberg, Nicole Lucas, Eva Dombi, Christopher Melani, Mark Roschewski, Frank Balis, Brigitte C. Widemann, Wyndham H. Wilson
Summary: This study evaluated the pharmacokinetics and toxicity of doxorubicin in patients with normal and elevated bilirubin levels, and found that patients with elevated bilirubin had lower clearance and higher plasma concentrations of doxorubicin. However, these values were still within the normal range. Patients with elevated bilirubin experienced more severe toxicity during the first treatment cycle, but these adverse effects were safely managed. These results suggest that empirical dose reductions of doxorubicin may not be necessary in patients with elevated bilirubin levels.
Article
Microbiology
Sinenhlanhla Mtshali, Byron A. Jacobs
Summary: Physiologically based pharmacokinetic models have gained popularity in drug development and regulatory science. This study validates the model's effectiveness in predicting drug-drug interaction and the pharmacokinetics of antiretroviral and anti-TB drugs through mathematical solving and sensitivity analysis.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2022)
Article
Pharmacology & Pharmacy
Kelly M. Mahar, Bonnie C. Shaddinger, Bandi Ramanjineyulu, Susan Andrews, Stephen Caltabiano, Alistair C. Lindsay, Alexander R. Cobitz
Summary: Participants with mild and moderate hepatic impairment showed increased exposure to daprodustat compared to matched controls, with no meaningful differences in EPO levels observed and no new safety concerns identified.
CLINICAL PHARMACOLOGY IN DRUG DEVELOPMENT
(2022)
Article
Pharmacology & Pharmacy
Heidemarie Kletzl, Hassan Ajmi, Izabela Antys, Katja Heinig, Birgit Jaber, Thomas C. Marbury, Annie Young, Andreas Gunther
Summary: This study aimed to evaluate the effect of mild to moderate hepatic impairment on the pharmacokinetics, safety, and tolerability of a single oral dose of risdiplam. The results showed that mild or moderate hepatic impairment did not have a clinically relevant impact on the pharmacokinetics of risdiplam, indicating no dose adjustment is required for patients with mild or moderate hepatic impairment receiving risdiplam.
BRITISH JOURNAL OF CLINICAL PHARMACOLOGY
(2022)