Vinblastine (VLB) is an antimitotic drug that binds to the vinca site of tubulin.
Investigation of potent inhibitors of cholinesterase based on thiourea and pyrazoline derivatives: Synthesis, inhibition assay and molecular modeling studies
Owing to the desperate need of new drugs development to treat Alzheimer's ailment the synthesis of 1-aroyl-3-(5-(4-chlorophenyl)-1,2,4-triazole-3-thioneaminylthioureas (2–6)...
Ceftolozane/tazobactam population pharmacokinetics and dose selection for further clinical evaluation in pediatric patients with complicated urinary tract or complicated intraabdominal infections
Ceftolozane-tazobactam, a combination of the novel antipseudomonal cephalosporin ceftolozane and the...
In Silico Design of Dapsone Analogues Effective Towards Enoyl Acyl Carrier Protein Reductase Enzyme of Mycrobacterium Leprae
A series of new antileprotic drugs targeting enoyl acyl carrier protein reductase (ENR) enzyme of Mycobacterium lepraewere designed by in silico techniques.
Insights into DPI sensitivity to humidity: An integrated in-vitro-in-silico risk-assessment
Dry powder inhalers (DPIs) are known to be sensitive to humidity. Erroneous storage of these products by patients in high humidity environments, could present a potential risk.
Toward the establishment of a standardized pre-clinical porcine model to predict food effects – Case studies on fenofibrate and paracetamol
A preclinical porcine model that reliably predicts human food effect of fenofibrate was developed. Fenofibrate was administered to pigs as model compound with a positive food effect.
Exposure-response (E-R) analysis of efficacy of pegvorhyaluronidase alfa (PEGPH20) in combination with nab-paclitaxel + gemcitabine (AG) in patients (Pts) with metastatic pancreatic ductal adenocarcinoma
PEGPH20 depolymerizes extracellular matrix hyaluronan (HA) and is an investigational agent for the treatment of pts with HA-accumulating tumors
Solidified SNEDDS for the oral delivery of rifampicin: Evaluation, proof of concept, in vivo kinetics, and in silico GastroPlusTM simulation
The present investigation was performed to develop a rifampicin (RIF)-loaded solidified self-nanoemulsifying drug delivery system (SNEDDS) (solidified RIF-OF1) for in vitro and in vivo evaluations.
Towards regulatory endorsement of drug development tools to promote the application of model-informed drug development in Duchenne muscular dystrophy
Drug development for rare diseases is challenged by small populations and limited data.
Application of Mechanistic Ocular Absorption Modeling and Simulation to Understand the Impact of Formulation Properties on Ophthalmic Bioavailability in Rabbits: a Case Study Using Dexamethasone Suspension
Developing mathematical models to predict changes in ocular bioavailability and pharmacokinetics due to differences in the physicochemical properties of complex topical ophthalmic suspension formulations...
The Biopharmaceutics Classification System (BCS) and the Biopharmaceutics Drug Disposition Classification System (BDDCS): Beyond guidelines
The recent impact of the Biopharmaceutics Classification System (BCS) and the Biopharmaceutics Drug Disposition Classification System (BDDCS) on relevant scientific advancements is discussed.
Physiologically Based Pharmacokinetic Modeling to Evaluate Formulation Factors Influencing Bioequivalence of Metoprolol Extended‐Release Products
The University of Florida Center for Pharmacometrics and Systems Pharmacology and the Food and Drug Administration Office of Generic Drugs have collaborated on a research project to develop...
Evaluating the Clinical Impact of Formulation Variability: A Metoprolol Extended‐Release Case Study
The objective of this research was to evaluate the impact of changes in the formulation of metoprolol extended‐release (ER) tablets on dissolution, pharmacokinetic, and exercise‐induced heart rate (EIHR) using...
Oxysterols and apolipoproteins in multiple sclerosis: a 5-year follow-up study
The purpose of this work was to investigate whether changes in oxysterol and apolipoprotein levels over 5 years are associated with...
Discovery of Membrane Permeability, Pharmacokinetics Properties and Mechanism of Action for Analogs of Ethylenediamine-N,N′-di-2-(3-Cyclohexyl)Propionic Acid and 1,3-Propandiamine-N,N′-di-2-(3-Cyclohexyl)Propionic Acid with Antiproliferative Activity Using In Vitro and In Silico Methods
In previously in vitro studies on different cell lines and in vivo on melanoma and 4T1 murine breast cancer and metastasis it was shown antiproliferative activity for ester derivatives of (S,S)-ethylenediamine-N,N′-di-2-(3-cyclohexyl)propanoic acid, and (S,S)-1,3-propanediamine-N,N′-di-2-(3-cyclohexyl)propanoic acid.
Androgen Receptor and PI3K Pathway Activity in Ovarian Cancer
We sought to evaluate androgen receptor (AR) and PI3K pathway activity in ovarian cancer cell lines and tissue and determine if either pathway was correlated with growth...
In Silico Prediction of Plasma Concentrations of Fluconazole Capsules with Different Dissolution Profiles and Bioequivalence Study Using Population Simulation
A biowaiver is accepted by the Brazilian Health Surveillance Agency (ANVISA) for immediate-release solid oral products containing Biopharmaceutics Classification System (BCS) class I drugs showing rapid drug dissolution.
Minor structural modifications of bisphenol A strongly affect physiological responses of HepG2 cells
Bisphenols represent a large group of structurally similar compounds.
The Discriminatory Power of the BCS-based Biowaiver: A Retrospective with Focus on Essential Medicines
This article summarizes historic developments, recent expert opinions and (currently) unresolved challenges concerning the Biopharmaceutics Classification System (BCS) based biowaiver.
Analysis of pharmacological mechanisms and targets mining of Wuzi-Yanzong-Wan for treating non-obstructive oligoasthenospermia
As a classical traditional Chinese medicine, Wuzi-Yanzong-Wan (WZYZW) has been widely applied for several centuries to treat non-obstructive oligoasthenozoospermia (NOA), although its pharmacological mechanisms remain largely unknown.