Fremanezumab is a fully humanized IgG2 Δa/κ monoclonal antibody specific for calcitonin gene-related peptide developed and approved for the
In Silico Molecular Docking Study of Delafloxacin against 4MQT for the Treatment of Acute Bacterial Skin and Skin Structure Infections
Infection occurring in the skin and its associated soft tissues such as loose connective tissue and mucous membranes is known as...
Learning in silico Reactant and Bond-of-Metabolism Predictors for Human Cytochrome P450 Enzymes
Human beings are exposed to many chemicals through their routine interactions with the environment, such as food/drug consumption, household or...
Exposure-Response of Quizartinib Efficacy in Patients with Relapsed/Refractory AML
Quizartinib is a once-daily, oral, highly potent and selective FLT3 inhibitor that has shown clinical activity in patients with relapsed/refractory acute myeloid leukemia (AML) with FLT3 internal tandem duplications in...
A novel series of chlorinated plastoquinone analogs: Design, synthesis, and evaluation of anticancer activity
Herein, we report the synthesis and cytotoxic effects of novel chlorinated plastoquinone analogs (ABQ1–17) against different leukemic cells.
A randomized, double-blind, placebo-controlled phase 1b/2 study of ralimetinib, a p38 MAPK inhibitor, plus gemcitabine and carboplatin versus gemcitabine and carboplatin for women with recurrent platinum-sensitive ovarian cancer
This phase 1b/2 clinical trial (NCT01663857) evaluated the efficacy of ralimetinib in combination with gemcitabine (G) and carboplatin (C), followed by maintenance ralimetinib...
Synthesis and discovery of pyrazolo-pyridine analogs as inflammation medications through pro- and anti-inflammatory cytokine and COX-2 inhibition assessments
This article briefs about the efforts taken to synthesis, characterize and develop (E)-5-methyl-2-phenyl-3-(thiophen-2-yl)-7-(thiophen-2-ylmethylene)..
Peroxisome proliferator-activated receptor gamma controls prostate cancer cell growth through AR-dependent and independent mechanisms
Background: Prostate cancer (PC) remains a leading cause of cancer mortality and the most successful chemopreventative and treatment strategies for PC come from targeting...
Production of Lentiviral Vectors Using Suspension Cells Grown in Serum-free Media
Lentiviral vectors are increasingly utilized in cell and gene therapy applications because they efficiently transduce target cells such as hematopoietic stem cells and T cells. Large-scale production of current Good Manufacturing Practices-grade lentiviral vectors is limited because of the adherent, serum-dependent nature of HEK293T cells used in the manufacturing process.
Prediction of pH-Dependent Drug-Drug Interactions for Basic Drugs Using Physiologically Based Biopharmaceutics Modeling: Industry Case Studies
Acid-reducing agents (ARAs) such as antacids, histamine-2 receptor antagonists, and proton pump inhibitors are widely prescribed in several disease states.
A practical approach to modeling the impact of amorphous drug nanoparticles on the oral absorption of poorly soluble drugs
Recently published studies have proposed that amorphous drug nanoparticles in gastrointestinal fluids may be beneficial for the absorption of poorly soluble compounds.
Prediction of the pharmacokinetics and pharmacodynamics of topiroxostat in humans by integrating the physiologically based pharmacokinetic model with the drug-target residence time model
Topiroxostat is a selective xanthine oxidoreductase (XOR) inhibitor for the management of hyperuricemia in patients with or without gout.
Duration of pretomanid/moxifloxacin/pyrazinamide therapy compared with standard therapy based on time-to-extinction mathematics
Animal models have suggested that the combination of pretomanid with pyrazinamide and moxifloxacin (PaMZ) may shorten TB therapy duration to 3–4 months.
Integrating In Vitro Testing and Physiologically-Based Pharmacokinetic (PBPK) Modelling for Chemical Liver Toxicity Assessment – a Case Study of Troglitazone
In vitro to in vivo extrapolation (IVIVE) for next-generation risk assessment (NGRA) of chemicals requires computational modeling and faces unique challenges.
Combination of Gemcitabine with Cell-Penetrating Peptides: A Pharmacokinetic Approach Using In Silico Tools
Gemcitabine is an anticancer drug used to treat a wide range of solid tumors and is a first line treatment for pancreatic cancer.
Toxicity Assessment of Herbal Medicine Using Zebrafish Embryos: A Systematic Review
Herbal remedies have been practiced by humans over centuries and therefore possess time-proven safety.
Quantitative Systems Toxicology Approaches to Understand and Predict Drug-Induced Liver Injury
The DILI-sim Initiative is a public-private partnership that has applied quantitative systems toxicology modeling to develop software (DILIsym) that has improved mechanistic understanding of DILI.
Mechanistic Dissolution Modeling of a Poorly Soluble Drug; an Evaluation of Formulation Influence and Simulation Parameters for Enhancing Predictive Capability
In early drug development, the selection of a formulation platform and decisions on formulation strategies have to be made...
The development of a population physiologically based pharmacokinetic model for mycophenolic mofetil and mycophenolic acid in humans using data from plasma, saliva, and kidney tissue
Mycophenolic acid (MPA) is used widely to prevent graft rejection in kidney‐transplant patients.
Prediction of Oral Bioavailability in Rats: Transferring Insights from in Vitro Correlations to (Deep) Machine Learning Models Using in Silico Model Outputs and Chemical Structure Parameters
Oral administration of drug products is a strict requirement in many medical indications.