Current Drug Metabolism - Volume 21, Issue 2, 2020

Background: Overactive bladder syndrome is a broadly occurring urological disorder with a distressing impact on the quality of life. The commonly used antimuscarinic drugs show poor patient compliance because of unsatisfactory potency, tolerability and high occurrence of adverse effects such as dry mouth, blurred vision, constipation, dizziness etc. Mirabegron is the first approved β3-adrenoreceptor agonist, used as mono Read More

Background: Nobel laureate Sir James Black’s molecule, propranolol, still has broad potential in cardiovascular diseases, infantile haemangiomas and anxiety. A comprehensive and systematic review of the literature for the summarization of pharmacokinetic parameters would be effective to explore the new safe uses of propranolol in different scenarios, without exposing humans and using virtual-human modeling approaches Read More

Background: Dabigatran etexilate (DE) was approved by the FDA in 2010 to reduce the risk of stroke and systemic embolism in adults with Non-valvular Atrial Fibrillation (NVAF). Compared with warfarin, a traditional anticoagulant drug, DE exhibits a shorter half-life, improved dose-effect relationship, fewer food and drug interactions, and can be taken orally without monitoring the conventional coagulation index. DE can al Read More

Background: Bioequivalence studies are a vital part of drug development. The average bioequivalence approach is the standard method of assessment to conclude whether the generic product is bioequivalent to the innovator product. Of late, debates are on whether the average bioequivalence approach adequately addresses drug interchangeability as it considers only population mean for the evaluation especiall Read More

Background: Clobazam (CLBZ) metabolized primarily by Cytochrome P-450 isoenzyme CYP3A4 than with CYP2C19, Whereas Levetiracetam (LEV) is metabolized by hydrolysis of the acetamide group. Few CYP enzymes are inhibited by Proton Pump Inhibitors (PPIs) Pantoprazole, Esomeprazole, and Rabeprazole in different extents that could affect drug concentrations in blood. The aim of the present study was to evaluate the eff Read More

Background: The translation of Pharmacokinetics (PK)/Pharmacodynamics (PD) from preclinical models to the clinic has not been studied in detail for drugs used to treat complicated urinary tract infections (cUTI). Objective: The PK/PD of Ciprofloxacin (CIP), a drug used to treat cUTI, was evaluated in a mouse model of cUTI infected with Escherichia coli, and compared with clinical PK/PD in cUTI patients. Methods: Streptoz Read More

Background and Objectives: Inflammatory bowel disease (IBD) is a set of chronic inflammatory gastrointestinal disorders, which include ulcerative colitis (UC) and Crohn’s disease (CD) that affects many patients worldwide with a peak incidence in early adult life. The immunosuppressant drug Azathioprine (AZA) represents one of the most useful drugs in the management of IBD. It is metabolized by many enzymes like AOX1, a Read More

Background: DMPK data and knowledge are critical in maximising the probability of developing successful drugs via the application of in silico, in vitro and in vivo approaches in drug discovery. Methods: The evaluation, optimisation and prediction of human pharmacokinetics is now a mainstay within drug discovery. These elements are at the heart of the ‘right tissue’ component of AstraZeneca’s ‘5Rs framework’ which, since its Read More