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About 165,688 results

Atazanavir-Concentrate Loaded Soft Gelatin Capsule for Enhanced Concentration in Plasma...
https://doi.org/10.1208/s12249-022-02428-0
AAPS PharmSciTech; Sethi S, Rana V

Sep 29th, 2022 - This study investigates the development of atazanavir-concentrate loaded soft gelatin capsule for achieving enhanced atazanavir (ATV) concentration in plasma, brain, spleen, and lymphatics beneficial in the significant reduction of viral load in HIV infection. For this purpose, ATV-concentrate in the presence and absence of Soluplus with corn oil, oleic acid, tween 80, and propylene glycol was ...

Giardia duodenalis: Flavohemoglobin is involved in drug biotransformation and resistanc...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9514659
PLoS Pathogens; Pech-Santiago EO, Argüello-García R et. al.

Sep 28th, 2022 - Giardia duodenalis causes giardiasis, a major diarrheal disease in humans worldwide whose treatment relies mainly on metronidazole (MTZ) and albendazole (ABZ). The emergence of ABZ resistance in this parasite has prompted studies to elucidate the molecular mechanisms underlying this phenomenon. G. duodenalis trophozoites convert ABZ into its sulfoxide (ABZSO) and sulfone (ABZSOO) forms, despite...

Tacrolimus Concentration Is Effectively Predicted Using Combined Clinical and Genetic F...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9481373
Journal of Immunology Research; Cheng F, Li Q et. al.

Sep 20th, 2022 - Tacrolimus has unpredictable pharmacokinetic (PK) characteristics, which are partially attributed to CYP3A5 polymorphism. The potential effects of clinical factors in the postoperative period of transplantation on tacrolimus PK and those of early tacrolimus PK variability on clinical outcomes are yet to be clarified. We examined the genetic and clinical factors affecting early tacrolimus PK var...

IVIVC of Octreotide in PLGA-Glucose Microsphere Formulation, Sandostatin® LAR.
https://doi.org/10.1208/s12249-022-02359-w
AAPS PharmSciTech; Song JS, Kim SY et. al.

Sep 20th, 2022 - In vitro-in vivo correlation (IVIVC) analysis reveals a relationship between in vitro release and in vivo pharmacokinetic response of the drug of interest. Sandostatin LAR Depot (SLD) for endocrine tumors and acromegaly is a sustained-release formulation of octreotide, a cyclic oligomer of 8 amino acids, which prolongs therapeutic efficacy and enhances medication compliance of octreotide. Since...

Evaluation of the food effect on a drospirenone only contraceptive containing 4 mg admi...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9484173
BMC Women's Health; Regidor PA, Richter WH et. al.

Sep 20th, 2022 - The objective of the present trial was to assess the difference in pharmacokinetics (PK) of an oral test preparation containing 4 mg drospirenone (DRSP) under fasting conditions compared to PK upon food intake after single dose administration. Open label, single centre, two-treatment, two-sequence, crossover study in 24 healthy female volunteers, with duration of 1 day per sequence and with a r...

Tacrolimus Population Pharmacokinetic Model in Adult Chinese Patients with Nephrotic Sy...
https://doi.org/10.1097/FTD.0000000000001008
Therapeutic Drug Monitoring; Liao M, Wang M et. al.

Sep 15th, 2022 - The study aimed to establish a population pharmacokinetic (PPK) model of tacrolimus for Chinese patients with nephrotic syndrome using the patient's genotype and Wuzhi capsule dosage as the main test factors. Ninety-six adult patients with nephrotic syndrome, who were receiving tacrolimus treatment, were enrolled. A nonlinear mixed-effects model was used to determine the influencing factors of ...

Absorption, metabolism and excretion of 14C-sotorasib in healthy male subjects: charact...
https://doi.org/10.1007/s00280-022-04470-y
Cancer Chemotherapy and Pharmacology; Vuu I, Dahal UP et. al.

Sep 6th, 2022 - The objectives of this study were to characterize the absorption, metabolism, and excretion of sotorasib and determine the metabolites present in plasma, urine, and feces in healthy male subjects following a single oral 720 mg dose containing approximately 1 μCi of [14C]-sotorasib. Urine, feces, and plasma were collected post-dose and assayed for total radioactivity and profiled for sotorasib m...

A phase 1b study of crenigacestat (LY3039478) in combination with gemcitabine and cispl...
https://doi.org/10.1007/s00280-022-04461-z
Cancer Chemotherapy and Pharmacology; Massard C, Cassier PA et. al.

Aug 29th, 2022 - Notch signaling plays an integral role in development and tissue homeostasis. Inhibition of Notch signaling has been identified as a reasonable target for oncotherapy. Crenigacestat (LY3039478) is a potent Notch inhibitor that decreases Notch signaling and its downstream biologic effects. I6F-MC-JJCD was a multicenter, nonrandomized, open-label, phase 1b study with 5 separate, parallel dose esc...

Anti-cancer drug combinations approved by US FDA from 2011 to 2021: main design feature...
https://doi.org/10.1007/s00280-022-04467-7
Cancer Chemotherapy and Pharmacology; Fudio S, Sellers A et. al.

Aug 28th, 2022 - During the last decade, the treatment for many cancer indications has evolved due to intensive clinical research into anti-tumor agents' combination. In most instances, new combination treatments consist of an add-on to the standard of care (SOC), which then demonstrate a substantial gain in efficacy and no detrimental effect in tolerability. In the era of targeted therapies, for which maximum ...

Development and evaluation of uncertainty quantifying machine learning models to predic...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9404625
BMC Medical Informatics and Decision Making; Verhaeghe J, Dhaese SAM et. al.

Aug 26th, 2022 - Beta-lactam antimicrobial concentrations are frequently suboptimal in critically ill patients. Population pharmacokinetic (PopPK) modeling is the golden standard to predict drug concentrations. However, currently available PopPK models often lack predictive accuracy, making them less suited to guide dosing regimen adaptations. Furthermore, many currently developed models for clinical applicatio...

Population Pharmacokinetic Meta-Analysis and Dosing Recommendation for Meropenem in Cri...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9487629
Antimicrobial Agents and Chemotherapy; Peng Y, Cheng Z et. al.

Aug 26th, 2022 - The optimal dosing regimen for meropenem in critically ill patients undergoing continuous renal replacement therapy (CRRT) remains undefined due to small studied sample sizes and uninformative pharmacokinetic (PK)/pharmacodynamic (PD) analyses in reported studies. The present study aimed to perform a population PK/PD meta-analysis of meropenem using available literature data to suggest the opti...

Effect of fluconazole on the pharmacokinetics of a single dose of fedratinib in healthy...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9399588
Cancer Chemotherapy and Pharmacology; Chen Y, Ogasawara K et. al.

Aug 25th, 2022 - Fedratinib is an orally administered Janus kinase (JAK) 2-selective inhibitor for the treatment of adult patients with intermediate-2 or high-risk primary or secondary myelofibrosis. In vitro, fedratinib is predominantly metabolized by cytochrome P450 (CYP) 3A4 and to a lesser extent by CYP2C19. Coadministration of fedratinib with CYP3A4 inhibitors is predicted to increase systemic exposure to ...

Physiologically based pharmacokinetic modeling of ponatinib to describe drug-drug inter...
https://doi.org/10.1007/s00280-022-04466-8
Cancer Chemotherapy and Pharmacology; Morita TO, Hanada K

Aug 24th, 2022 - This study aimed to investigate the drug-drug interactions of ponatinib with strong, moderate, or weak CYP3A4 inhibitors/inducers by developing physiologically based pharmacokinetic (PBPK) models. Simcyp® Ver 20.1 (Certara Inc., Sheffield, UK) was used to construct a PBPK model for ponatinib and to predict its interaction with strong, moderate, or weak CYP3A4 inhibitors/inducers. The constructe...

Fixed Dose Combination Tablets of Aripiprazole and Divalproex Sodium: a Pilot Pharmacok...
https://doi.org/10.1208/s12249-022-02378-7
AAPS PharmSciTech; Ahmed Z, Subhan F et. al.

Aug 20th, 2022 - A combination product of aripiprazole (antipsychotic) and divalproex sodium (mood stabilizer) was recently developed to establish their tolerability and safety in fixed dose combination (FDC). A pilot pharmacokinetic (PK) open-labeled parallel study on healthy human volunteers was carried out to assess the PK of FDC of aripiprazole/divalproex sodium in comparison with its individual components ...

Predicting drug-drug interactions with physiologically based pharmacokinetic/pharmacody...
https://doi.org/10.1016/j.thromres.2022.08.007
Thrombosis Research; Wen HN, He QF et. al.

Aug 20th, 2022 - The concurrent administration of dronedarone and oral anti-coagulants is common because both are used in managing atrial fibrillation (AF). Dronedarone is a moderate inhibitor of the cytochrome P450 3A4 (CYP3A4) enzyme and P-glycoprotein (P-gp). Apixaban and rivaroxaban are P-gp and CYP3A4 substrates. This study aims to investigate the impact of exposure and bleeding risk of apixaban or rivarox...

Utility of neuromuscular blockade reversal in the evaluation of acute neurosurgical pat...
https://doi.org/10.1016/j.jocn.2022.08.009
Journal of Clinical Neuroscience : Official Journal of Th... Christodoulides A, Palma S et. al.

Aug 19th, 2022 - Sugammadex reversal of neuromuscular blocking agents (NMBAs) is usually performed postoperatively. A scarcity of literature exists exploring sugammadex use for timely neurological examination of neurosurgical patients. NMBAs, like rocuronium, are used in the Emergency Department during intubation and their unpredictable duration of action often impedes timely and accurate assessment of patient ...

Important roles of transporters in the pharmacokinetics of anti-viral nucleoside/nucleo...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9506706
Expert Opinion on Drug Metabolism & Toxicology; Yang M, Xu X

Aug 18th, 2022 - Nucleoside analogs are an important class of antiviral agents. Due to the high hydrophilicity and limited membrane permeability of antiviral nucleoside/nucleotide analogs (AVNAs), transporters play critical roles in AVNA pharmacokinetics. Understanding the properties of these transporters is important to accelerate translational research for AVNAs. The roles of key transporters in the pharmacok...

Concentrations of Efavirenz, Tenofovir, and Emtricitabine in Obesity: A Cross-Sectional...
https://doi.org/10.1097/QAI.0000000000003025
Journal of Acquired Immune Deficiency Syndromes (1999); Solanke T, Kamau F et. al.

Aug 17th, 2022 - Obesity is increasing worldwide including in people living with HIV (PLWH). Antiretroviral pharmacokinetic data in obesity are limited. To measure antiretroviral drug concentrations in obese and nonobese PLWH treated with the fixed-dose combination of efavirenz-tenofovir-emtricitabine. To determine pharmacokinetic differences across indicators of obesity and their associated immunovirological o...

Simulation of Intraluminal Performance of Lipophilic Weak Bases in Fasted Healthy Adult...
https://doi.org/10.1208/s12248-022-00737-7
The AAPS Journal; Statelova M, Vertzoni M et. al.

Aug 17th, 2022 - The majority of drug candidates exhibit weakly basic characteristics with high lipophilicity. The risk of intraluminal compound precipitation has been studied in vivo and extensively in vitro using advanced dissolution transfer setups mimicking drug transfer from the stomach to the small intestine. The present investigation aims to evaluate the usefulness of the recently introduced Artificial S...

Understanding the Mechanism of Drug Transfer and Retention of Drug-Coated Balloons.
https://doi.org/10.1177/10742484221119559
Journal of Cardiovascular Pharmacology and Therapeutics; Villar-Matamoros E, Stokes L et. al.

Aug 17th, 2022 - The purpose of this study was to determine the impact of varying inflation parameters on paclitaxel delivery and retention using a commercially available DCB. Drug-coated balloons (DCB) have become the standard treatment for peripheral artery disease. Clinical data suggest that varying DCB delivery parameters directly impact patient outcome. Differences in delivery parameters can potentially al...