Article
Endocrinology & Metabolism
Ki Young Huh, Jun Gi Hwang, Wonjung Shin, Seungjae Baek, JaeDuk Choi, Nora Lee, Young Min Cho, Howard Lee
Summary: HM15136, a novel long-acting glucagon analogue, was shown to be safe and well tolerated in doses ranging from 10-120 μg/kg in a randomized, double-blind, placebo-controlled study. It increased blood glucose levels and suppressed the secretion of endogenous glucagon.
DIABETES OBESITY & METABOLISM
(2022)
Article
Pharmacology & Pharmacy
Dominic Beale, Jeremy Dennison, Malcolm Boyce, Francesca Mazzo, Naoki Honda, Paul Smith, Mark Bruce
Summary: The study demonstrated that ONO-7684 was well-tolerated in healthy subjects at both single and multiple doses, with low incidence of adverse events. Pharmacokinetic data showed dose proportionality for ONO-7684. Pharmacodynamic results revealed a strong inhibition of FXI coagulation activity and an increase in aPTT at 250 mg ONO-7684 daily. These findings support the potential of ONO-7684 as an oral FXIa inhibitor for anticoagulation indications.
BRITISH JOURNAL OF CLINICAL PHARMACOLOGY
(2021)
Article
Endocrinology & Metabolism
Wonjung Shin, Marcus Hompesch, JinHee Byeon, Seohyun Kang, Jaehyuk Choi, Seungjae Baek
Summary: This study evaluated the safety, tolerability, pharmacokinetics and pharmacodynamics of a novel long-acting glucagon analogue HM15136 in overweight/obese patients with co-morbidities, with and without type 2 diabetes (T2D). The results showed that HM15136 had good safety and tolerability in patients with dyslipidaemia and/or hypertension, but its use in patients with T2D may cause hyperglycaemia.
DIABETES OBESITY & METABOLISM
(2023)
Article
Chemistry, Medicinal
Inseung Jeon, Jaeseong Oh, Yu-Kyung Kwon, Seo Hyun Yoon, Joo-Youn Cho, In-Jin Jang, Kyung-Sang Yu, SeungHwan Lee
Summary: The study compared the pharmacokinetic (PK), pharmacodynamic (PD), and tolerability profiles of CKD-11101 with those of the reference drug in healthy subjects. Results showed that CKD-11101 was well tolerated and exhibited comparable PK and PD characteristics with the reference drug after a single intravenous (IV) or subcutaneous (SC) dose.
DRUG DESIGN DEVELOPMENT AND THERAPY
(2021)
Article
Pharmacology & Pharmacy
Xue Zhao, Hongzhong Liu, Wei Tian, Ligang Fang, Mengyang Yu, Xiaofei Wu, Aijing Liu, Ruijie Wan, Li Li, Jinghui Luo, Yuqiong Li, Bo Liu, Yu He, Xiaowen Chen, Yuan Li, Donghong Xu, Hongyun Wang, Xiaohong Han
Summary: This study aimed to investigate the safety, tolerability, pharmacokinetics, and pharmacodynamics of aficamten in healthy Chinese adults. The results showed that aficamten was safe and well-tolerated in the Chinese population, with pharmacokinetics comparable to Western participants. These findings support future clinical studies of aficamten in Chinese patients.
FRONTIERS IN PHARMACOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Banaz Abbas, Nagwa A. Sabri, Amal A. El-Khouly
Summary: The study aimed to investigate the effects of food and selected single nucleotide polymorphisms in the UGT2B7 gene on the pharmacokinetics and pharmacodynamics behavior of indapamide. The results showed that food had a modest impact on the maximum concentration and absorption time of indapamide, while genetic variations in the UGT2B7 gene had no significant impact on the pharmacokinetic parameters. It was concluded that food had a moderate effect on the pharmacokinetics, but there were no significant differences in safety and efficacy.
Article
Chemistry, Medicinal
Hyewon Chung, Jin-Woo Park, Dai-Hyun Kim, Soo-Hong Seo, Kyoung-Ah Kim, Woo-Shun Lee, Ji-Young Park
Summary: This study investigated the pharmacokinetics, pharmacodynamics, and safety/tolerability of MT921, an injectable cholic acid, in healthy volunteers after a single subcutaneous administration. The results showed that systemic exposure to cholic acid increased with dose escalation, while blood lipid profiles and deoxycholic acid levels were unaffected by MT921 treatment. Adverse events such as injection site pain and edema were mild and resolved without treatment.
Article
Chemistry, Analytical
Ibrahim Abdelsalam Abdelrahman, Abdul Ahad, Mohammad Raish, Yousef A. Bin Jardan, Mohd Aftab Alam, Fahad I. Al-Jenoobi
Summary: The study aimed to investigate the influence of cumin and green tea on the pharmacodynamics and pharmacokinetics of amlodipine in hypertensive rats. The results showed that both cumin and green tea significantly decreased blood pressure, with green tea having a more prominent effect on the pharmacodynamics of amlodipine. Co-administration of green tea and cumin increased the peak concentration and half-life of amlodipine.
Review
Chemistry, Multidisciplinary
Kris Dammen-Brower, Paige Epler, Stanley Zhu, Zachary J. Bernstein, Paul R. Stabach, Demetrios T. Braddock, Jamie B. Spangler, Kevin J. Yarema
Summary: This article discusses the important role of glycosylation in therapeutic proteins and provides examples of drugs that have been improved through glycoengineering. As glycoengineering strategies develop, deliberate modification of therapeutic protein glycosylation will become more prevalent.
FRONTIERS IN CHEMISTRY
(2022)
Article
Pharmacology & Pharmacy
Tingting Ma, Yanli Dong, Lei Huang, Yuanxun Yang, Yan Geng, Fei Fei, Pinhao Xie, Yu Zhao, Hui Lin, Zeyu Yang, Yun Jin, Xitong Ju, Runbin Sun, Juan Li
Summary: This study evaluated the safety and pharmacodynamics of SHR2285, the first oral coagulation factor XIa (FXIa) inhibitor developed in China, in combination with aspirin, clopidogrel or ticagrelor in healthy subjects. Results showed that SHR2285 was well tolerated, with no increased risk of bleeding, and effectively inhibited FXI activity and prolonged APTT when combined with these antiplatelet agents.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Chemistry, Medicinal
Xuemei He, Xin Gao, Panpan Xie, Yuan Liu, Wenjing Bai, Yue Liu, Aixin Shi
Summary: This study assessed the pharmacokinetic and pharmacodynamic profiles, safety, and tolerability of sotagliflozin in Chinese healthy subjects. The results showed that sotagliflozin was rapidly absorbed with dose-proportional systemic exposure and a moderate degree of accumulation. Both 200mg and 400mg doses of sotagliflozin per day were well tolerated in Chinese healthy subjects.
DRUG DESIGN DEVELOPMENT AND THERAPY
(2022)
Article
Pharmacology & Pharmacy
Sergey Zyryanov, Irina Bondareva, Olga Butranova, Alexandra Kazanova
Summary: This study aimed to determine the population pharmacokinetic parameters of meropenem in preterm infants and evaluate the pharmacodynamic indices and covariates affecting pharmacokinetics. Analysis of demographic, clinical, and therapeutic drug monitoring data from 66 preterm newborns revealed that the median values for elimination rate and volume of distribution of meropenem were 0.31 1/h and 1.2 L respectively, and the median values for total clearance and elimination half-life were 0.22 L/h/kg and 2.33 h. Individualized Bayesian posterior models improved prediction quality compared to the population model.
FRONTIERS IN PHARMACOLOGY
(2023)
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
Biochemistry & Molecular Biology
Ming-Fen Ho, Cheng Zhang, Irene Moon, Xiujuan Zhu, Brandon J. Coombes, Joanna Biernacka, Michelle Skime, Tyler S. Oesterle, Victor M. Karpyak, Kristen Schmidt, Kate Gliske, Quyen Ngo, Cedric Skillon, Marvin D. Seppala, Hu Li, Richard M. Weinshilboum
Summary: This study used single-cell sequencing technology to investigate the response of OUD patients to oxycodone and buprenorphine. The results revealed that buprenorphine significantly influenced transcriptional regulation in glial cells, while oxycodone induced type I interferon signaling in multiple cell types. These findings provide novel mechanistic insights into the actions of drugs at the single-cell level.
MOLECULAR PSYCHIATRY
(2022)
Review
Immunology
Rekha Pai Mangalore, Aadith Ashok, Sue J. Lee, Lorena Romero, Trisha N. Peel, Andrew A. Udy, Anton Y. Peleg
Summary: TDM-guided dosing of beta-lactam antibiotics improved clinical and microbiological cure in critically ill patients, with no significant impact on mortality and length of stay.
CLINICAL INFECTIOUS DISEASES
(2022)