Review
Biochemistry & Molecular Biology
Rina Iwamoto, Masanori Koide, Nobuyuki Udagawa, Yasuhiro Kobayashi
Summary: Sclerostin inhibits bone formation by suppressing the Wnt/β-catenin signaling pathway and plays a crucial role in maintaining bone mass. The expression of sclerostin is regulated by various factors, which in turn govern bone metabolism.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Anesthesiology
Hong Su, Douglas J. Eleveld, Michel M. R. F. Struys, Pieter J. Colin
Summary: We developed a mechanism-based pharmacodynamic model to quantitatively characterize the magnitude of propofol-induced hemodynamic effects during general anesthesia. This model has the potential to predict hemodynamic alterations and may have clinical implications.
BRITISH JOURNAL OF ANAESTHESIA
(2022)
Article
Anesthesiology
Jasper Kamp, Monique van Velzen, Leon Aarts, Marieke Niesters, Albert Dahan, Erik Olofsen
Summary: The study reveals that S-ketamine increases cardiac output, while S-norketamine decreases it. There were no significant effects on cardiac output found for R-ketamine, metabolites other than S-norketamine, or sodium nitroprusside.
BRITISH JOURNAL OF ANAESTHESIA
(2021)
Article
Chemistry, Medicinal
Yesong Shin, Chungam Choi, Eun Sil Oh, Choon Ok Kim, Kyungsoo Park, Min Soo Park
Summary: The study showed that rifampicin significantly reduced the AUC0-96h of Evogliptin without affecting Cmax. Rifampicin was found to reduce Evogliptin metabolism by inducing cytochrome P450. Co-administration of the two drugs did not significantly alter adverse events.
DRUG DESIGN DEVELOPMENT AND THERAPY
(2022)
Article
Infectious Diseases
Himanshi Khera, Avaneesh Kumar Pandey, Nusrat Shafiq, G. K. Khuller, Ritika Kondel Bhandari, Aditi Panditrao, Nanda Gamad, Rachna Rohilla, Samiksha Bhattacharjee, Naveen Murali, Harish Cvn, Devraj Belavagi, Chakrant Mothsara, Manjula Singh, Navneet Sharma, Digamber Behera, Samir Malhotra
Summary: This study evaluated the safety and pharmacokinetics of econazole in humans and found it to be safe at appropriate doses. A dose of 500 mg of econazole taken orally once a day was recommended for further evaluation.
EXPERT REVIEW OF ANTI-INFECTIVE THERAPY
(2022)
Article
Medicine, Research & Experimental
Dasohm Kim, Minkyu Choi, Byung Hak Jin, Taegon Hong, Choon Ok Kim, Byung Won Yoo, Min Soo Park
Summary: Evogliptin (EV) is a novel DPP4 inhibitor used for glycemic control in patients with T2DM. This study evaluated the PK and PD interactions between EV and SGLT2 inhibitors in healthy volunteers, as combination therapy has been considered effective for T2DM treatment. The study found that co-administration of EV with either empagliflozin or dapagliflozin did not significantly alter the PK parameters or PD changes.
CTS-CLINICAL AND TRANSLATIONAL SCIENCE
(2023)
Article
Pharmacology & Pharmacy
Ana Loureiro, Francisco Rocha, Ana T. Santos, Nand Singh, Maria Joao Bonifacio, Rui Pinto, Laszlo E. Kiss, Patricio Soares-da-Silva
Summary: This study investigated the absorption, metabolism, and excretion of opicapone. The results showed that opicapone was excreted through multiple metabolic pathways, with feces being the main route of excretion, potentially involving gut bacteria.
BRITISH JOURNAL OF CLINICAL PHARMACOLOGY
(2022)
Article
Radiology, Nuclear Medicine & Medical Imaging
Sebastian Ebel, Alexander Kuehn, Abhinav Aggarwal, Benjamin Koehler, Benjamin Behrendt, Robin Gohmann, Boris Riekena, Christian Luecke, Juliane Ziegert, Charlotte Vogtmann, Bernhard Preim, Siegfried Kropf, Bernd Jung, Timm Denecke, Matthias Grothoff, Matthias Gutberlet
Summary: This study used 4D flow MRI to assess quantitative parameters of helical flow and obtained normal values in healthy volunteers. The results showed that wall shear stress and maximum forward velocity decreased with age, while other parameters were not correlated with age and gender.
EUROPEAN RADIOLOGY
(2022)
Article
Peripheral Vascular Disease
Mason W. Freeman, Mary Bond, Brian Murphy, James Hui, Jonathan Isaacsohn
Summary: This study evaluated the safety, pharmacokinetics, and pharmacodynamics of Baxdrostat in healthy volunteers. The results demonstrated that Baxdrostat can dose-dependently reduce plasma aldosterone levels, while having no significant impact on cortisol levels. Furthermore, the half-life of Baxdrostat supports once-daily dosing.
HYPERTENSION RESEARCH
(2023)
Article
Pharmacology & Pharmacy
Neeraj Gupta, Xiaohui Wang, Elliot Offman, Marita Prohn, Narayana Narasimhan, David Kerstein, Michael J. Hanley, Karthik Venkatakrishnan
Summary: The population pharmacokinetic analysis of brigatinib revealed a three-compartment model for its metabolism and distribution, with albumin as a covariate on clearance. No dose adjustment is required based on factors such as sex, age, race, body weight, renal impairment, or liver function tests. These results informed prescribing guidance for patients with mild or moderate renal impairment.
CLINICAL PHARMACOKINETICS
(2021)
Article
Chemistry, Medicinal
Guolan Wu, Huili Zhou, Duo Lv, Ruling Zheng, Lihua Wu, Songxia Yu, Jiejing Kai, Nana Xu, Lie Gu, Nanfang Hong, Jianzhong Shentu
Summary: The purpose of this study was to investigate the safety, tolerability, and pharmacokinetics of suramin in healthy Chinese volunteers. The results showed that suramin's maximum plasma concentration and area under the plasma concentration-time curve increased in a dose-proportional manner. Suramin can be detected in urine samples for longer periods. The study suggested that 10 mg/kg or 15 mg/kg could be an appropriate dose for future multiple-dose studies.
DRUG DESIGN DEVELOPMENT AND THERAPY
(2023)
Article
Medicine, Research & Experimental
Nicholas S. Jones, Smita Kshirsagar, Vishnu Mohanan, Vidya Ramakrishnan, Flavia Di Nucci, Ling Ma, Jialin Mao, Hao Ding, Sha Klabunde, Domagoj Vucic, Lin Pan, Annemarie N. Lekkerkerker, Yuan Chen, Michael E. Rothenberg
Summary: This study evaluated the safety, pharmacokinetics (PKs), and pharmacodynamics (PDs) of GDC-8264 in healthy volunteers. Results showed that GDC-8264 effectively inhibited the activation of the RIP1 pathway and exhibited dose-proportional increases in systemic exposure. The study supports further development of GDC-8264 for the treatment of RIP1-driven diseases.
CTS-CLINICAL AND TRANSLATIONAL SCIENCE
(2023)
Article
Multidisciplinary Sciences
Claire Morice, Dewleen G. Baker, Marguerite M. Patel, Tracy L. Nolen, Kayla Nowak, Shawn Hirsch, Thomas R. Kosten, Christopher D. Verrico
Summary: The study aimed to evaluate the pharmacodynamic interactions between the glucocorticoid receptor antagonist PT150 and alcohol in healthy subjects. The results showed that administration of PT150 with concurrent alcohol use was safe and well-tolerated, with no clinically significant abnormal electrocardiograms or serious adverse events observed.
SCIENTIFIC REPORTS
(2021)
Article
Microbiology
Thanh Bach, Gregory A. Deye, Ellen E. Codd, John Horton, Patricia Winokur, Guohua An
Summary: Oxfendazole, a potent veterinary antiparasitic drug, is being developed for human use to treat various parasitic infections. Results from recent clinical trials showed that the pharmacokinetics of oxfendazole is nonlinear and affected by food, with mild effects on hemoglobin concentrations. Population pharmacokinetic-pharmacodynamic modeling was used to quantitatively characterize the relationship between oxfendazole dose, pharmacokinetics, and hemoglobin concentration, facilitating dose optimization for different patient populations with parasitic infections.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2022)
Article
Pharmacology & Pharmacy
Yong-Soon Cho, Kyun-Seop Bae, Seung Chan Choi, Joong Myung Cho, Hyeong-Seok Lim
Summary: This study explores the population pharmacokinetic and pharmacodynamic characteristics of polmacoxib, a new coxib. The pharmacokinetic properties were described by a 2-compartment model with mixed absorption kinetics. The clearance of polmacoxib was influenced by iron concentration. The relationship between polmacoxib concentration and WOMAC was best described by a 2-effect compartment model, with a required concentration of 508 ng/mL for 50% of the maximum effect.
CLINICAL THERAPEUTICS
(2022)
