Caffeine is the most consumed active stimulant. About 80% of pregnant women consume caffeine orally on daily basis. Many reports indicated consumption of >200 mg caffeine during pregnancy could increase the likelihood of miscarriage.
EDEn–Electroceutical Design Environment: Ion Channel Tissue Expression Database with Small Molecule Modulators
The emerging field of bioelectricity has revealed numerous new roles for ion channels beyond the nervous system, which can be exploited for applications in regenerative medicine.
PBPK Absorption Modeling: Establishing the In Vitro–In Vivo Link—Industry Perspective
The establishment of an in vitro–in vivo correlation (IVIVC) is considered the gold standard to establish in vivo relevance of a dissolution method and to utilize dissolution data in the context of regulatory bioequivalence questions...
PBPK Absorption Modeling of Food Effect and Bioequivalence in Fed State for Two Formulations with Crystalline and Amorphous Forms of BCS 2 Class Drug in Generic Drug Development
Prediction of the effect of food on drug’s pharmacokinetics using modeling and simulation could cause difficulties due to complex in vivo processes.
Predicting the Effects of Different Triazole Antifungal Agents on the Pharmacokinetics of Tamoxifen
Tamoxifen is an antiestrogen drug that is widely used in the adjuvant chemotherapy of estrogen receptor-α (ERα)-positive breast cancer.
A Survey of the Regulatory Requirements for the Acceptance of Foreign Comparator Products by Participating Regulators and Organizations of the International Generic Drug Regulators Programme
The acceptance of foreign comparator products is the most limiting factor for the development and regulatory assessment of generic medicines marketed globally.
Model-Informed Drug Development for Malaria Therapeutics
Malaria is a critical public health problem resulting in substantial morbidity and mortality, particularly in developing countries.
Design, synthesis, biological evaluation, structure-activity relationship, and toxicity of clinafloxacin-azole conjugates as novel antitubercular agents
Based on the advantages of azole molecules and fluoroquinolone drugs, we designed and synthesized 34 clinafloxacin-azole conjugates using fragment-based drug design and drug combination principles.
Development of a population pharmacokinetic model for taranabant, a cannibinoid-1 receptor inverse agonist
Taranabant is a cannabinoid-1 receptor inverse agonist developed for the treatment of obesity.
Symptomatic cardiotoxicity associated with 5-fluorouracil
A prospective cohort study was conducted in 35 hospitals with oncology units to determine the incidence of symptomatic cardiotoxicity in patients receiving...
Relationship between drug exposure and the efficacy and safety of bupropion sustained release for smoking cessation
A population pharmacokinetic and pharmacodynamic analysis evaluated the relationships of dose, plasma concentrations of bupropion and metabolites...
Rubik’s Cube of Siderophore Assembly Established from MixedSubstrate Precursor-Directed Biosynthesis
Precursor-directed biosynthesis (PDB) is a useful microbiological technique that conscripts the native biosynthetic machinery of an organism, often a bacterium, to produce analogues of secondary metabolites.
Human CYP2A6, CYP2B6 and CYP2E1 Atropselectively Metabolize Polychlorinated Biphenyls to Hydroxylated Metabolites
Exposure to chiral polychlorinated biphenyls (PCBs) has been associated with neurodevelopmental disorders.
Brazilian stingless bee propolis and geopropolis: promising sources of biologically active compounds
Stingless bee products such as honey, pollen, propolis, and geopropolis have been used for centuries in traditional medicine for the treatment of several illnesses.
Exploration of sexual dimorphism and inter-individual variability in multivariate parameter spaces for a pharmacokinetic compartment model
Pharmacokinetic models are particularly useful to study the underlying and complex physiological mechanisms contributing to clinical differences across patient subgroups or special populations.
PBTK model for assessment of operator exposure to haloxyfop using human biomonitoring and toxicokinetic data
Physiologically-based toxicokinetic (PBTK) models are mathematical representations of chemical absorption, distribution, metabolism and excretion (ADME) in animals.
Use of generally recognized as safe or dietary compounds to inhibit buprenorphine metabolism: potential to improve buprenorphine oral bioavailability
The present study evaluated the potential of five generally recognized as safe (GRAS) or dietary compounds (α‐mangostin, chrysin, ginger extract, pterostilbene and silybin) to inhibit oxidative (CYP) and conjugative (UGT) metabolism...
Pediatric Physiologically Based Pharmacokinetic Model Development: Current Status and Challenges
This article provides a brief overview of the development of pediatric physiologically based pharmacokinetic (PPBPK) models, the challenges of uncertain systems information, and finally...
Design, synthesis and evaluation of new classes of nonquaternary reactivators for acetylcholinesterase inhibited by organophosphates
A new series of nonquaternary conjugates for reactivation of both nerve agents and pesticides inhibited hAChE were described in this paper.
Pharmacophore-based virtual screening for identification of potential selective inhibitors of human histone deacetylase 6
Histone deacetylase (HDAC) 6 plays a role in oncogenic transformation and cancer metastasis via tubulin deacetylation, making it a critical target for anticancer drug design.