Epithelia form barriers that are essential to life.
Mechanistic Investigation of the Androgen Receptor DNA-Binding Domain Inhibitor Pyrvinium
Pyrvinium was identified as the first small molecule inhibitor of the androgen receptor (AR) DNA-binding domain (DBD). It was also among the first small molecules shown to...
Model-Informed Drug Discovery and Development: Current Industry Good Practice and Regulatory Expectations and Future Perspectives
Good practices around model-informed drug discovery and development (MID3) aim to improve the implementation, standardization, and
Metabolization of pharmaceuticals by plants after uptake from water and soil: A review
Residues of pharmaceuticals are ubiquitous in the environment, due to the increased use of drugs for treating humans and animals.
Machine Learning Models for the Prediction of Chemotherapy-Induced Peripheral Neuropathy
Chemotherapy-induced peripheral neuropathy (CIPN) is a common adverse side effect of cancer chemotherapy that can be life debilitating and cause extreme pain.
The in vivo predictive dissolution for immediate release dosage of donepezil and danazol, BCS class IIc drugs, with the GIS and the USP II with biphasic dissolution apparatus
The formulation developments and the in vivo assessment of Biopharmaceutical Classification System (BCS) class II drugs are challenging due to their low solubility and high permeability in the human gastrointestinal (GI) tract.
Challenges in working towards an internal threshold of toxicological concern (iTTC) for use in the safety assessment of cosmetics: Discussions from the Cosmetics Europe iTTC Working Group workshop
The Threshold of Toxicological Concern (TTC) is an important risk assessment tool which establishes acceptable low-level exposure values to be applied to chemicals with limited toxicological data.
Dissolution Testing in Drug Product Development: Workshop Summary Report
This publication summarizes the proceedings and key outcomes of the first day (“Day 1”) of the 3-day workshop on “Dissolution and Translational Modeling Strategies Enabling Patient-Centric Product Development.”
Physiologically Based Pharmacokinetic/ Pharmacodynamic Model for Caffeine Disposition in Pregnancy
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.