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PMC8241021
core_pubmed_pmc
Engineering of a novel optimized platform for sublingual delivery with novel characterization tools: in vitro evaluation and in vivo pharmacokinetics study in human
Engineering of a novel optimized platform for sublingual delivery with novel characterization tools: in vitro evaluation and in vivo pharmacokinetics study in human Abstract Abstract The aim of this work was to develop a novel and more efficient platform for sublingual drug delivery using mosapride citrate (MSP) as a m...
PMC4937632
core_pubmed_pmc
Comparison of levocetirizine pharmacokinetics after single doses of levocetirizine oral solution and cetirizine dry syrup in healthy Japanese male subjects
Comparison of levocetirizine pharmacokinetics after single doses of levocetirizine oral solution and cetirizine dry syrup in healthy Japanese male subjects Abstract Objective Levocetirizine, the R-enantiomer of cetirizine, is classified as a second generation antihistamine used for the treatment of allergic disorders. ...
PMC4261557
core_pubmed_pmc
Gastroretentive Pulsatile Release Tablets of Lercanidipine HCl: Development, Statistical Optimization, and In Vitro and In Vivo Evaluation
Gastroretentive Pulsatile Release Tablets of Lercanidipine HCl: Development, Statistical Optimization, and In Vitro and In Vivo Evaluation Abstract The present study was aimed at the development of gastroretentive floating pulsatile release tablets (FPRTs) of lercanidipine HCl to enhance the bioavailability and treat e...
PMC3626772
core_pubmed_pmc
Cotrimoxazole plasma levels, dialyzer clearance and total removal by extended dialysis in a patient with acute kidney injury: risk of under-dosing using current dosing recommendations
Cotrimoxazole plasma levels, dialyzer clearance and total removal by extended dialysis in a patient with acute kidney injury: risk of under-dosing using current dosing recommendations Abstract Abstract Background Dosing of antibiotics in critically ill patients is challenging. It becomes even more difficult if renal or...
PMC9257747
core_pubmed_pmc
iBCS: 2. Mechanistic Modeling of Pulmonary Availability of Inhaled Drugs versus Critical Product Attributes
iBCS: 2. Mechanistic Modeling of Pulmonary Availability of Inhaled Drugs versus Critical Product Attributes Abstract This work is the second in a series of publications outlining the fundamental principles and proposed design of a biopharmaceutics classifications system for inhaled drugs and drug products (the iBCS). H...
PMC12052016
core_pubmed_pmc
A Comprehensive Review on the Pharmacokinetics and Drug−Drug Interactions of Approved GLP-1 Receptor Agonists and a Dual GLP-1/GIP Receptor Agonist
A Comprehensive Review on the Pharmacokinetics and Drug−Drug Interactions of Approved GLP-1 Receptor Agonists and a Dual GLP-1/GIP Receptor Agonist Abstract Abstract Glucagon-like peptide-1 receptor agonists (GLP-1 RAs) are peptide-derived analogs that were initially investigated to treat type 2 diabetes. Recently, a d...
PMC11892757
core_pubmed_pmc
Exploring Herbal Compounds as Targeted Therapies for Breast Cancer: Insights from Network Pharmacology, Molecular Docking, MD Simulation, ADME-Toxicity and DFT Profiles
Exploring Herbal Compounds as Targeted Therapies for Breast Cancer: Insights from Network Pharmacology, Molecular Docking, MD Simulation, ADME-Toxicity and DFT Profiles Abstract Background Herbal compounds sourced from various plants are becoming targeted therapies for breast cancer. Objectives This study aims to explo...
PMC11134291
core_pubmed_pmc
Variability in plasma rifampicin concentrations and role of SLCO1B1 , ABCB1 , AADAC2 and CES2 genotypes in Ethiopian patients with tuberculosis
Variability in plasma rifampicin concentrations and role of SLCO1B1 , ABCB1 , AADAC2 and CES2 genotypes in Ethiopian patients with tuberculosis Abstract Abstract Background: Rifampicin, a key drug against tuberculosis (TB), displays wide between-patient pharmacokinetics variability and concentration-dependent antimicro...
PMC12205768
core_pubmed_pmc
Fixed dosing versus weight-based dosing of HIV-1 prophylactic monoclonal antibodies in adults: a post-hoc, cross-protocol pharmacokinetics modelling study
Fixed dosing versus weight-based dosing of HIV-1 prophylactic monoclonal antibodies in adults: a post-hoc, cross-protocol pharmacokinetics modelling study Abstract Summary Background Pharmacokinetic (PK) modelling and simulations have been used to support label changes of dosing levels or strategies for multiple market...
PMC7080631
core_pubmed_pmc
AJM300, a novel oral antagonist of α4‐integrin, sustains an increase in circulating lymphocytes: A randomised controlled trial in healthy male subjects
AJM300, a novel oral antagonist of α4‐integrin, sustains an increase in circulating lymphocytes: A randomised controlled trial in healthy male subjects Abstract Aims AJM300 is an oral antagonist of α4‐integrin that reduces inflammation by blocking leucocyte trafficking. This study aimed to investigate safety, tolerabil...
PMC8532679
core_pubmed_pmc
Pharmacokinetic Behavior and Pharmacokinetic/Pharmacodynamic Integration of Danofloxacin Following Single or Co-Administration with Meloxicam in Healthy Lambs and Lambs with Respiratory Infections
Pharmacokinetic Behavior and Pharmacokinetic/Pharmacodynamic Integration of Danofloxacin Following Single or Co-Administration with Meloxicam in Healthy Lambs and Lambs with Respiratory Infections Abstract Abstract The aim of this study was to determine the pharmacokinetics and pharmacodynamics of danofloxacin (DAN; 6 ...
PMC8779366
core_pubmed_pmc
Jakinibs of All Trades: Inhibiting Cytokine Signaling in Immune-Mediated Pathologies
Jakinibs of All Trades: Inhibiting Cytokine Signaling in Immune-Mediated Pathologies Abstract Over the last 25 years, inhibition of Janus kinases (JAKs) has been pursued as a modality for treating various immune and inflammatory disorders. While the clinical development of JAK inhibitors (jakinibs) began with the inves...
PMC6061379
core_pubmed_pmc
Effect of Renal Impairment on the Pharmacokinetics and Pharmacodynamics of Verinurad, a Selective Uric Acid Reabsorption Inhibitor
Effect of Renal Impairment on the Pharmacokinetics and Pharmacodynamics of Verinurad, a Selective Uric Acid Reabsorption Inhibitor Abstract Background and Objective Verinurad (RDEA3170) is a high-affinity, selective URAT1 transporter inhibitor in development for treating gout and asymptomatic hyperuricemia. This Phase ...
PMC3782498
core_pubmed_pmc
Modeling of Rifampicin-Induced CYP3A4 Activation Dynamics for the Prediction of Clinical Drug-Drug Interactions from In Vitro Data
Modeling of Rifampicin-Induced CYP3A4 Activation Dynamics for the Prediction of Clinical Drug-Drug Interactions from In Vitro Data Abstract Abstract Induction of cytochrome P450 3A4 (CYP3A4) expression is often implicated in clinically relevant drug-drug interactions (DDI), as metabolism catalyzed by this enzyme is the...
PMC12299977
core_pubmed_pmc
Potential Clinical Use of CytoSorb ® for Ticagrelor and Rivaroxaban Elimination Prior to Emergency Orthopedic Surgery in Trauma Patients
Potential Clinical Use of CytoSorb ® for Ticagrelor and Rivaroxaban Elimination Prior to Emergency Orthopedic Surgery in Trauma Patients Abstract Background: Major orthopedic trauma in patients receiving anticoagulants such as ticagrelor or rivaroxaban poses a significant perioperative challenge, particularly in emerge...
PMC7993848
core_pubmed_pmc
Model choice for estimating the association between exposure to chemical mixtures and health outcomes: A simulation study
Model choice for estimating the association between exposure to chemical mixtures and health outcomes: A simulation study Abstract Challenges arise in researching health effects associated with chemical mixtures. Several methods have recently been proposed for estimating the association between health outcomes and expo...
PMC11263405
core_pubmed_pmc
Effect of Hepatic Impairment on Trofinetide Exposures Using an In Silico Physiologically Based Pharmacokinetic Model
Effect of Hepatic Impairment on Trofinetide Exposures Using an In Silico Physiologically Based Pharmacokinetic Model Abstract Introduction Trofinetide is the first drug to be approved for the treatment of Rett syndrome. Hepatic impairment is not expected to affect the pharmacokinetic (PK) profile of trofinetide because...
PMC10723863
core_pubmed_pmc
Anakinra Removal by Continuous Renal Replacement Therapy: An Ex Vivo Analysis
Anakinra Removal by Continuous Renal Replacement Therapy: An Ex Vivo Analysis Abstract OBJECTIVES: Patients with sepsis are at significant risk for multiple organ dysfunction, including the lungs and kidneys. To manage the morbidity associated with kidney impairment, continuous renal replacement therapy (CRRT) may be r...
PMC6063743
core_pubmed_pmc
Applied Concepts in PBPK Modeling: How to Extend an Open Systems Pharmacology Model to the Special Population of Pregnant Women
Applied Concepts in PBPK Modeling: How to Extend an Open Systems Pharmacology Model to the Special Population of Pregnant Women Abstract Abstract This tutorial presents the workflow of adapting an adult physiologically based pharmacokinetic (PBPK) model to the pregnant populations using the Open Systems Pharmacology (O...
PMC12304789
core_pubmed_pmc
Pharmacology and safety of TAS5315, a Bruton tyrosine kinase inhibitor, in healthy volunteers: First‐in‐human, randomized, ascending‐dose studies
Pharmacology and safety of TAS5315, a Bruton tyrosine kinase inhibitor, in healthy volunteers: First‐in‐human, randomized, ascending‐dose studies Abstract Abstract Aim TAS5315 is a Bruton tyrosine kinase (Btk) inhibitor in development for autoimmune and allergic diseases, including rheumatoid arthritis (RA) and chronic...
PMC6542081
core_pubmed_pmc
A retrospective comparison of inappropriate prescribing of psychotropics in three Norwegian nursing homes in 2000 and 2016 with prescribing quality indicators
A retrospective comparison of inappropriate prescribing of psychotropics in three Norwegian nursing homes in 2000 and 2016 with prescribing quality indicators Abstract Background Inappropriate prescribing of psychotropics is a persistent and prevalent problem in nursing homes. The present study compared inappropriate p...
PMC7556746
core_pubmed_pmc
Pharmacodynamics, pharmacokinetics, and safety of single-dose subcutaneous administration of selatogrel, a novel P2Y 12 receptor antagonist, in patients with chronic coronary syndromes
Pharmacodynamics, pharmacokinetics, and safety of single-dose subcutaneous administration of selatogrel, a novel P2Y 12 receptor antagonist, in patients with chronic coronary syndromes Abstract Abstract Aims To study the pharmacodynamics and pharmacokinetics of selatogrel, a novel P2Y 12 receptor antagonist for subcuta...
PMC8842344
core_pubmed_pmc
A Review of Coumarins and Coumarin-Related Compounds for Their Potential Antidiabetic Effect
A Review of Coumarins and Coumarin-Related Compounds for Their Potential Antidiabetic Effect Abstract Abstract Background and aims: Worldwide, type 2 diabetes mellitus accounts for a considerable burden of disease, with an estimated global cost of >800 billion USD annually. For this reason, the search for more effectiv...
PMC7101315
core_pubmed_pmc
Avocado-derived polyols for use as novel co-surfactants in low energy self-emulsifying microemulsions
Avocado-derived polyols for use as novel co-surfactants in low energy self-emulsifying microemulsions Abstract Abstract Avocado ( Persea americana Mill.; Lauraceae) seed-derived polyhydroxylated fatty alcohols (PFAs) or polyols (i.e., avocadene and avocadyne) are metabolic modulators that selectively induce apoptosis o...
PMC8365809
core_pubmed_pmc
First-in-human phase I/Ib open-label dose-escalation study of GWN323 (anti-GITR) as a single agent and in combination with spartalizumab (anti-PD-1) in patients with advanced solid tumors and lymphomas
First-in-human phase I/Ib open-label dose-escalation study of GWN323 (anti-GITR) as a single agent and in combination with spartalizumab (anti-PD-1) in patients with advanced solid tumors and lymphomas Abstract Abstract Background GWN323 is an IgG1 monoclonal antibody (mAb) against the glucocorticoid-induced tumor necr...
PMC7113224
core_pubmed_pmc
Pharmacokinetic Similarity and Comparative Pharmacodynamics, Safety, Efficacy, and Immunogenicity of DRL_RI Versus Reference Rituximab in Biologics-Naïve Patients with Moderate-to-Severe Rheumatoid Arthritis: A Double-Blind, Randomized, Three-Arm Study
Pharmacokinetic Similarity and Comparative Pharmacodynamics, Safety, Efficacy, and Immunogenicity of DRL_RI Versus Reference Rituximab in Biologics-Naïve Patients with Moderate-to-Severe Rheumatoid Arthritis: A Double-Blind, Randomized, Three-Arm Study Abstract Objectives The aims were to demonstrate pharmacokinetic (P...
PMC5165251
core_pubmed_pmc
Rivaroxaban-Induced Hemorrhage Associated with ABCB1 Genetic Defect
Rivaroxaban-Induced Hemorrhage Associated with ABCB1 Genetic Defect Abstract We report a patient who presented a non-ST segment elevation myocardial infarction in the context of severe normocytic hypochromic anemia related to gastrointestinal bleeding, 3 months after switching anticoagulant from the vitamin K antagonis...
PMC11374807
core_pubmed_pmc
Pharmacological and non-pharmacological predictors of the LSD experience in healthy participants
Pharmacological and non-pharmacological predictors of the LSD experience in healthy participants Abstract The pharmacodynamic effects of lysergic acid diethylamide (LSD) are diverse and different in different individuals. Effects of other psychoactive substances have been shown to be critically influenced by non-pharma...
PMC5638091
core_pubmed_pmc
Faster insulin action is associated with improved glycaemic outcomes during closed‐loop insulin delivery and sensor‐augmented pump therapy in adults with type 1 diabetes
Faster insulin action is associated with improved glycaemic outcomes during closed‐loop insulin delivery and sensor‐augmented pump therapy in adults with type 1 diabetes Abstract Abstract We aimed to evaluate the relationship between insulin pharmacodynamics and glycaemic outcomes during closed‐loop insulin delivery an...
PMC10951162
core_pubmed_pmc
Evaluation of Age-Related Changes in Teneligliptin Pharmacokinetics in Japanese and European Descent Subjects Using a Physiologically Based Pharmacokinetic Model
Evaluation of Age-Related Changes in Teneligliptin Pharmacokinetics in Japanese and European Descent Subjects Using a Physiologically Based Pharmacokinetic Model Abstract Abstract Introduction Drugs often show differing pharmacokinetic (PK) profiles, such as higher plasma concentrations, in older people than in younger...
PMC7874017
core_pubmed_pmc
Development and Application of a Water Temperature Related Physiologically Based Pharmacokinetic Model for Enrofloxacin and Its Metabolite Ciprofloxacin in Rainbow Trout
Development and Application of a Water Temperature Related Physiologically Based Pharmacokinetic Model for Enrofloxacin and Its Metabolite Ciprofloxacin in Rainbow Trout Abstract Enrofloxacin (ENR) has been approved for the treatment of infections in aquaculture, but it may cause tissue residue. This research aimed to ...
PMC7817768
core_pubmed_pmc
Pharmacokinetics, Pharmacodynamic Efficacy Prediction Indexes and Monte Carlo Simulations of Enrofloxacin Hydrochloride Against Bacterial Strains That Induce Common Clinical Diseases in Broiler Chickens
Pharmacokinetics, Pharmacodynamic Efficacy Prediction Indexes and Monte Carlo Simulations of Enrofloxacin Hydrochloride Against Bacterial Strains That Induce Common Clinical Diseases in Broiler Chickens Abstract Abstract Pharmacokinetic parameters and efficacy prediction indexes (C max /MIC 90 and AUC 0−24 /MIC 90 ) of...
PMC4670022
core_pubmed_pmc
Profile of brivaracetam and its potential in the treatment of epilepsy
Profile of brivaracetam and its potential in the treatment of epilepsy Abstract Brivaracetam (BRV) (UCB 34714) is currently under review by the US Food and Drug Administration and European Medicines Agency for approval as an add-on treatment for adult patients with partial seizures. Similar to levetiracetam (LEV), BRV ...
PMC9224918
core_pubmed_pmc
Sex-Related Differences in Pharmacological Response to CNS Drugs: A Narrative Review
Sex-Related Differences in Pharmacological Response to CNS Drugs: A Narrative Review Abstract In the last decades, both animal and human studies have neglected female subjects with the aim of evading a theorized intricacy of feminine hormonal status. However, clinical experience proves that pharmacological response may...
PMC3308112
core_pubmed_pmc
MTRX1011A, a humanized anti-CD4 monoclonal antibody, in the treatment of patients with rheumatoid arthritis: a Phase I randomized, double-blind, placebo-controlled study incorporating pharmacodynamic biomarker assessments
MTRX1011A, a humanized anti-CD4 monoclonal antibody, in the treatment of patients with rheumatoid arthritis: a Phase I randomized, double-blind, placebo-controlled study incorporating pharmacodynamic biomarker assessments Abstract Introduction The purpose of this study was to evaluate the safety, tolerability, pharmaco...
PMC6617824
core_pubmed_pmc
Physiologically‐Based Pharmacokinetic Modeling Analysis for Quantitative Prediction of Renal Transporter–Mediated Interactions Between Metformin and Cimetidine
Physiologically‐Based Pharmacokinetic Modeling Analysis for Quantitative Prediction of Renal Transporter–Mediated Interactions Between Metformin and Cimetidine Abstract Abstract Metformin is an important antidiabetic drug and often used as a probe for drug–drug interactions (DDIs) mediated by renal transporters. Despit...
PMC6610406
core_pubmed_pmc
Don’t Fear the Reefer—Evidence Mounts for Plant-Based Cannabidiol as Treatment for Epilepsy
Don’t Fear the Reefer—Evidence Mounts for Plant-Based Cannabidiol as Treatment for Epilepsy Abstract Abstract Effect of Cannabidiol on Drop Seizures in the Lennox-Gastaut Syndrome Devinsky O, Patel AD, Cross JH, et al; GWPCARE3 Study Group. N Engl J Med . 2018;378:1888-1897. doi: 10.1056/NEJMoa1714631 Background: Canna...
PMC10721329
core_pubmed_pmc
Quisinostat is a brain-penetrant radiosensitizer in glioblastoma
Quisinostat is a brain-penetrant radiosensitizer in glioblastoma Abstract Abstract Histone deacetylase (HDAC) inhibitors have garnered considerable interest for the treatment of adult and pediatric malignant brain tumors. However, owing to their broad-spectrum nature and inability to effectively penetrate the blood-bra...
PMC2862657
core_pubmed_pmc
Phase I and Pharmacokinetic Study of ABI-007, Albumin-bound Paclitaxel, Administered Every 3 Weeks in Japanese Patients with Solid Tumors
Phase I and Pharmacokinetic Study of ABI-007, Albumin-bound Paclitaxel, Administered Every 3 Weeks in Japanese Patients with Solid Tumors Abstract Abstract Objective ABI-007 is a novel Cremophor ® EL-free nanoparticle albumin-bound paclitaxel. This Phase I study was designed to evaluate tolerability and determine recom...
PMC6304445
core_pubmed_pmc
Therapeutic Potential of Nitrogen Mustard Based Hybrid Molecules
Therapeutic Potential of Nitrogen Mustard Based Hybrid Molecules Abstract As medicine advances, cancer is still among one of the major health problems, posing significant threats to human health. New anticancer agents features with novel scaffolds and/or unique mechanisms of action are highly desirable for the treatmen...
PMC3650066
core_pubmed_pmc
A Review of Potential Harmful Interactions between Anticoagulant/Antiplatelet Agents and Chinese Herbal Medicines
A Review of Potential Harmful Interactions between Anticoagulant/Antiplatelet Agents and Chinese Herbal Medicines Abstract Background The risks attributed to drug-herb interactions, even when known, are often ignored or underestimated, especially for those involving anti-clotting drugs and Chinese medicines. The aim of...
PMC10048531
core_pubmed_pmc
Phospholipid-Based Topical Nano-Hydrogel of Mangiferin: Enhanced Topical Delivery and Improved Dermatokinetics
Phospholipid-Based Topical Nano-Hydrogel of Mangiferin: Enhanced Topical Delivery and Improved Dermatokinetics Abstract Mangiferin is a herbal drug that has proven anticancer potential. Owing to its lower aqueous solubility and poor oral bioavailability, the full pharmacological potential of this bioactive drug has not...
PMC5702225
core_pubmed_pmc
An optimized background regimen design to evaluate the contribution of levofloxacin to multidrug-resistant tuberculosis treatment regimens: study protocol for a randomized controlled trial
An optimized background regimen design to evaluate the contribution of levofloxacin to multidrug-resistant tuberculosis treatment regimens: study protocol for a randomized controlled trial Abstract Abstract Background Current guidelines for treatment of multidrug-resistant tuberculosis (MDR-TB) are largely based on exp...
PMC7775847
core_pubmed_pmc
Isoflavones' effects on pharmacokinetic profiles of main iridoids from Gardeniae Fructus in rats
Isoflavones' effects on pharmacokinetic profiles of main iridoids from Gardeniae Fructus in rats Abstract Abstract Gardeniae Fructus (GF) and Semen Sojae Praeparatum (SSP) are both medicine food homologies and widely used in Chinese clinical prescriptions together. The research investigated the pharmacokinetics of four...
PMC7307686
core_pubmed_pmc
Are Antimicrobial Peptide Dendrimers an Escape from ESKAPE?
Are Antimicrobial Peptide Dendrimers an Escape from ESKAPE? Abstract Abstract Significance: The crisis of antimicrobial resistance (AMR) increases dramatically despite all efforts to use available antibiotics or last resort antimicrobial agents. The spread of the AMR, declared as one of the most important health-relate...
PMC12655703
core_pubmed_pmc
Aqueous Extracts and Flavonoids Obtained from Annona cherimola Miller as Antidiabetic Treatments Alone and in Combination with Antidiabetic Drugs: In Vivo and In Silico Studies
Aqueous Extracts and Flavonoids Obtained from Annona cherimola Miller as Antidiabetic Treatments Alone and in Combination with Antidiabetic Drugs: In Vivo and In Silico Studies Abstract Background: Annona cherimola Miller ( A. cherimola ) is traditionally used in Mexico to treat diabetes. Objectives : this study aimed ...
PMC11856008
core_pubmed_pmc
Improved Inhibitors Targeting the Thymidylate Kinase of Multidrug-Resistant Mycobacterium tuberculosis with Favorable Pharmacokinetics
Improved Inhibitors Targeting the Thymidylate Kinase of Multidrug-Resistant Mycobacterium tuberculosis with Favorable Pharmacokinetics Abstract Abstract This study aims to design improved inhibitors targeting the thymidylate kinase (TMK) of Mycobacterium tuberculosis ( Mtb ), the causative agent of infectious disease t...
PMC9233488
core_pubmed_pmc
Pharmacogenetics of Breast Cancer Treatments: A Sub-Saharan Africa Perspective
Pharmacogenetics of Breast Cancer Treatments: A Sub-Saharan Africa Perspective Abstract Abstract Breast cancer is the most frequent cause of cancer death in low- and middle-income countries, in particular among sub-Saharan African women, where response to available anticancer treatment therapy is often limited by the r...
PMC8619046
core_pubmed_pmc
ABCB1 and ABCG2 Control Brain Accumulation and Intestinal Disposition of the Novel ROS1/TRK/ALK Inhibitor Repotrectinib, While OATP1A/1B, ABCG2, and CYP3A Limit Its Oral Availability
ABCB1 and ABCG2 Control Brain Accumulation and Intestinal Disposition of the Novel ROS1/TRK/ALK Inhibitor Repotrectinib, While OATP1A/1B, ABCG2, and CYP3A Limit Its Oral Availability Abstract Abstract Repotrectinib shows high activity against ROS1/TRK/ALK fusion-positive cancers in preclinical studies. We explored the ...
PMC9197536
core_pubmed_pmc
Optimized sampling to estimate vancomycin drug exposure: Comparison of pharmacometric and equation‐based approaches in a simulation‐estimation study
Optimized sampling to estimate vancomycin drug exposure: Comparison of pharmacometric and equation‐based approaches in a simulation‐estimation study Abstract Abstract Vancomycin dosing should be accompanied by area under the concentration‐time curve (AUC)–guided dosing using model‐informed precision dosing software acc...
PMC10035387
core_pubmed_pmc
A Preclinical and Phase Ib Study of Palbociclib plus Nab-Paclitaxel in Patients with Metastatic Adenocarcinoma of the Pancreas
A Preclinical and Phase Ib Study of Palbociclib plus Nab-Paclitaxel in Patients with Metastatic Adenocarcinoma of the Pancreas Abstract Abstract Purpose: To assess the preclinical efficacy, clinical safety and efficacy, and MTD of palbociclib plus nab-paclitaxel in patients with advanced pancreatic ductal adenocarcinom...
PMC6485310
core_pubmed_pmc
Talazoparib has no clinically relevant effect on QTc interval in patients with advanced solid tumors
Talazoparib has no clinically relevant effect on QTc interval in patients with advanced solid tumors Abstract Supplemental Digital Content is available in the text. The aims of this study were (i) to evaluate the effect of talazoparib (1 mg once daily) on cardiac repolarization in patients with advanced solid tumors by...
PMC3979046
core_pubmed_pmc
A phase 1 study evaluating the combination of an allosteric AKT inhibitor (MK-2206) and trastuzumab in patients with HER2-positive solid tumors
A phase 1 study evaluating the combination of an allosteric AKT inhibitor (MK-2206) and trastuzumab in patients with HER2-positive solid tumors Abstract Introduction Trastuzumab is effective in human epidermal growth factor receptor 2 (HER2)-over-expressing breast and gastric cancers. However, patients may develop resi...
PMC11938006
core_pubmed_pmc
Utilizing an Opportunistic Clinical Study and Population‐Based Pharmacokinetic Models to Identify Rational Empiric Dosing Regimens for Piperacillin–Tazobactam in Critically Ill Patients
Utilizing an Opportunistic Clinical Study and Population‐Based Pharmacokinetic Models to Identify Rational Empiric Dosing Regimens for Piperacillin–Tazobactam in Critically Ill Patients Abstract Abstract Determining an effective dosing regimen for piperacillin–tazobactam in critically ill patients is challenging due to...
PMC8227155
core_pubmed_pmc
South Africa’s Best BARK Medicines Prescribed at the Johannesburg Muthi Markets for Skin, Gut, and Lung Infections: MIC’s and Brine Shrimp Lethality
South Africa’s Best BARK Medicines Prescribed at the Johannesburg Muthi Markets for Skin, Gut, and Lung Infections: MIC’s and Brine Shrimp Lethality Abstract Abstract Indigenous trade of medicinal plants in South Africa is a multi-million-rand industry and is still highly relevant in terms of primary health care. The p...
PMC9542825
core_pubmed_pmc
Influence of Renal Function on Pharmacokinetics, Pharmacodynamics, and Safety of a Single Dose of Romosozumab
Influence of Renal Function on Pharmacokinetics, Pharmacodynamics, and Safety of a Single Dose of Romosozumab Abstract Abstract We evaluated the pharmacokinetics, pharmacodynamics, and safety of a single subcutaneous dose of romosozumab 210 mg, a monoclonal antibody against sclerostin, in an open‐label, parallel‐group ...
PMC8719524
core_pubmed_pmc
A pharmacokinetic–pharmacodynamic model based on multi-organ-on-a-chip for drug–drug interaction studies
A pharmacokinetic–pharmacodynamic model based on multi-organ-on-a-chip for drug–drug interaction studies Abstract In drug discovery, the emergence of unexpected toxicity is often a problem resulting from a poor understanding of the pharmacokinetics of drug–drug interactions (DDI). Organ-on-a-chip (OoC) has been propose...
PMC5762935
core_pubmed_pmc
Comparison of ESI– and APCI–LC–MS/MS methods: A case study of levonorgestrel in human plasma ☆
Comparison of ESI– and APCI–LC–MS/MS methods: A case study of levonorgestrel in human plasma ☆ Abstract Electrospray ionization (ESI) and atmospheric pressure chemical ionization (APCI) techniques for liquid chromatography–tandem mass spectrometry (LC–MS/MS) determination of levonorgestrel were evaluated. In considerat...
PMC10884265
core_pubmed_pmc
Association between urinary organophosphate ester metabolite exposure and thyroid disease risk among US adults: National Health and Nutrition Examination Survey 2011-2014
Association between urinary organophosphate ester metabolite exposure and thyroid disease risk among US adults: National Health and Nutrition Examination Survey 2011-2014 Abstract Abstract Background Organophosphate esters (OPEs) may interfere with thyroid function, but the relationship between OPEs and thyroid disease...
PMC6710522
core_pubmed_pmc
Pharmacokinetics, exposure, efficacy and safety of obinutuzumab in rituximab‐refractory follicular lymphoma patients in the GADOLIN phase III study
Pharmacokinetics, exposure, efficacy and safety of obinutuzumab in rituximab‐refractory follicular lymphoma patients in the GADOLIN phase III study Abstract Abstract Aims Rituximab is standard care in a number of lymphoma subtypes, including follicular lymphoma (FL), although many patients are resistant to rituximab, o...
PMC11481156
core_pubmed_pmc
First-in-human clinical outcomes with NG-350A, an anti-CD40 expressing tumor-selective vector designed to remodel immunosuppressive tumor microenvironments
First-in-human clinical outcomes with NG-350A, an anti-CD40 expressing tumor-selective vector designed to remodel immunosuppressive tumor microenvironments Abstract Abstract Background Tumor-selective oncolytic viral vectors are promising anticancer therapeutics; however, challenges with dosing and potency in advanced/...
PMC10559869
core_pubmed_pmc
Investigation of the treatment potential of Raloxifene-loaded polymeric nanoparticles in osteoporosis: In-vitro and in-vivo analyses
Investigation of the treatment potential of Raloxifene-loaded polymeric nanoparticles in osteoporosis: In-vitro and in-vivo analyses Abstract Abstract Osteoporosis (OP), is a systemic bone disorder associated with low bone mass and bone tissue corrosion. Worsening of the disease condition leads to bone delicacy and fra...
PMC7179653
core_pubmed_pmc
Safety and Pharmacokinetic Characterization of Nacubactam, a Novel β-Lactamase Inhibitor, Alone and in Combination with Meropenem, in Healthy Volunteers
Safety and Pharmacokinetic Characterization of Nacubactam, a Novel β-Lactamase Inhibitor, Alone and in Combination with Meropenem, in Healthy Volunteers Abstract Nacubactam is a novel β-lactamase inhibitor with dual mechanisms of action as an inhibitor of serine β-lactamases (classes A and C and some class D) and an in...
PMC8230777
core_pubmed_pmc
The Pharmacometabodynamics of Gefitinib after Intravenous Administration to Mice: A Preliminary UPLC–IM–MS Study
The Pharmacometabodynamics of Gefitinib after Intravenous Administration to Mice: A Preliminary UPLC–IM–MS Study Abstract Abstract The effects of intravenous gefitinib (10 mg/kg), an anilinoquinazoline thymidylate kinase inhibitor (TKI), selective for the epidermal growth factor receptor (EGFR), on the urinary metaboty...
PMC12466471
core_pubmed_pmc
Optimising Meropenem and Piperacillin Dosing in Patients Undergoing Extracorporeal Membrane Oxygenation Without Renal Dysfunction (MEPIMEX)
Optimising Meropenem and Piperacillin Dosing in Patients Undergoing Extracorporeal Membrane Oxygenation Without Renal Dysfunction (MEPIMEX) Abstract Background/Objectives : Antibiotic pharmacokinetics (PK) and pharmacodynamics (PD) are altered during extracorporeal membrane oxygenation (ECMO). Meropenem and piperacilli...
PMC6429929
core_pubmed_pmc
Evaluation of metformin in combination with rifampicin containing antituberculosis therapy in patients with new, smear-positive pulmonary tuberculosis (METRIF): study protocol for a randomised clinical trial
Evaluation of metformin in combination with rifampicin containing antituberculosis therapy in patients with new, smear-positive pulmonary tuberculosis (METRIF): study protocol for a randomised clinical trial Abstract Abstract Introduction Shorter duration of treatment for the management of drug-susceptible pulmonary tu...
PMC7261739
core_pubmed_pmc
Modelling Age-Related Changes in the Pharmacokinetics of Risperidone and 9-Hydroxyrisperidone in Different CYP2D6 Phenotypes Using a Physiologically Based Pharmacokinetic Approach
Modelling Age-Related Changes in the Pharmacokinetics of Risperidone and 9-Hydroxyrisperidone in Different CYP2D6 Phenotypes Using a Physiologically Based Pharmacokinetic Approach Abstract Abstract Purpose Dose-optimization strategies for risperidone are gaining in importance, especially in the elderly. Based on the ge...
PMC9740789
core_pubmed_pmc
Investigation of In Vitro and In Vivo Metabolism of α-Amanitin in Rats Using Liquid Chromatography-Quadrupole Time-of-Flight Mass Spectrometric Method
Investigation of In Vitro and In Vivo Metabolism of α-Amanitin in Rats Using Liquid Chromatography-Quadrupole Time-of-Flight Mass Spectrometric Method Abstract Abstract The purpose of this study is to investigate the difference of in vitro–in vivo correlation of α-amanitin from clearance perspectives as well as to expl...
PMC11859980
core_pubmed_pmc
Tailored Intranasal Albumin Caged Selegiline-α Synuclein siRNA Liposome with Improved Efficiency in Parkinson’s Model
Tailored Intranasal Albumin Caged Selegiline-α Synuclein siRNA Liposome with Improved Efficiency in Parkinson’s Model Abstract Abstract Background/Objectives: Parkinson’s disease (PD) is a progressive neuro-degenerative disorder characterized by α-synuclein aggregation, which promotes neuronal death and accelerates neu...
PMC6921166
core_pubmed_pmc
New bioanalytical microemulsion Electrokinetic chromatography method for the simultaneous determination of Trifluridine with its metabolites and Tipiracil in rat plasma: Application to pharmacokinetic studies
New bioanalytical microemulsion Electrokinetic chromatography method for the simultaneous determination of Trifluridine with its metabolites and Tipiracil in rat plasma: Application to pharmacokinetic studies Abstract Abstract A Microemulsion Electrokinetic Chromatography method coupled with diode array detector (MEEKC...
PMC8817505
core_pubmed_pmc
Interactions of selected cardiovascular active natural compounds with CXCR4 and CXCR7 receptors: a molecular docking, molecular dynamics, and pharmacokinetic/toxicity prediction study
Interactions of selected cardiovascular active natural compounds with CXCR4 and CXCR7 receptors: a molecular docking, molecular dynamics, and pharmacokinetic/toxicity prediction study Abstract Abstract Background The chemokine CXCL12 and its two receptors (CXCR4 and CXCR7) are involved in inflammation and hematopoietic...
PMC6229674
core_pubmed_pmc
A Review of Antimicrobial Therapy for Infectious Uveitis of the Posterior Segment
A Review of Antimicrobial Therapy for Infectious Uveitis of the Posterior Segment Abstract Treatment of infectious posterior uveitis represents a therapeutic challenge for ophthalmologists. The eye is a privileged site, maintained by blood ocular barriers, which limits penetration of systemic antimicrobials into the po...
PMC8937573
core_pubmed_pmc
Toward personalized medicine for pharmacological interventions in neonates using vital signs
Toward personalized medicine for pharmacological interventions in neonates using vital signs Abstract Abstract Vital signs, such as heart rate and oxygen saturation, are continuously monitored for infants in neonatal care units. Pharmacological interventions can alter an infant's vital signs, either as an intended effe...
PMC9298731
core_pubmed_pmc
Population Pharmacokinetic Modeling and Probability of Pharmacodynamic Target Attainment for Ceftazidime‐Avibactam in Pediatric Patients Aged 3 Months and Older
Population Pharmacokinetic Modeling and Probability of Pharmacodynamic Target Attainment for Ceftazidime‐Avibactam in Pediatric Patients Aged 3 Months and Older Abstract Increasing prevalence of infections caused by antimicrobial‐resistant gram‐negative bacteria represents a global health crisis, and while several nove...
PMC6194834
core_pubmed_pmc
Ceftriaxone concentration at the surgical site following systemic and isolated upper limb injection
Ceftriaxone concentration at the surgical site following systemic and isolated upper limb injection Abstract Background and Aims: This study was conducted to find out the equipotent dose of isolated upper limb injection of ceftriaxone in the upper limb (IUL) surgeries under tourniquet that would attain a peak bone marr...
PMC3430088
core_pubmed_pmc
Tranexamic acid for the treatment of heavy menstrual bleeding: efficacy and safety
Tranexamic acid for the treatment of heavy menstrual bleeding: efficacy and safety Abstract Tranexamic acid has proven to be an effective treatment for heavy menstrual bleeding (HMB). It reduces menstrual blood loss (MBL) by 26%–60% and is significantly more effective than placebo, nonsteroidal anti-inflammatory drugs,...
PMC8596667
core_pubmed_pmc
Safety, pharmacokinetics and pharmacodynamics of a topical SYK inhibitor in cutaneous lupus erythematosus: A double‐blind Phase Ib study
Safety, pharmacokinetics and pharmacodynamics of a topical SYK inhibitor in cutaneous lupus erythematosus: A double‐blind Phase Ib study Abstract Abstract The immunoregulator spleen tyrosine kinase (SYK) is upregulated in cutaneous lupus erythematosus (CLE). This double‐blind, multicentre, Phase Ib study evaluated the ...
PMC9975351
core_pubmed_pmc
In vitro metabolic characterization of the SARS-CoV-2 papain-like protease inhibitors GRL0617 and HY-17542
In vitro metabolic characterization of the SARS-CoV-2 papain-like protease inhibitors GRL0617 and HY-17542 Abstract Abstract The SARS-CoV-2 pandemic requires a new therapeutic target for viral infection, and papain-like protease (Plpro) has been suggested as a druggable target. This in-vitro study was conducted to exam...
PMC5361818
core_pubmed_pmc
Real-time in vivo monitoring of magnetic nanoparticles in the bloodstream by AC biosusceptometry
Real-time in vivo monitoring of magnetic nanoparticles in the bloodstream by AC biosusceptometry Abstract Abstract Background We introduce and demonstrate that the AC biosusceptometry (ACB) technique enables real-time monitoring of magnetic nanoparticles (MNPs) in the bloodstream. We present an ACB system as a simple, ...
PMC10377272
core_pubmed_pmc
Biological Fluid Microsampling for Therapeutic Drug Monitoring: A Narrative Review
Biological Fluid Microsampling for Therapeutic Drug Monitoring: A Narrative Review Abstract Abstract Therapeutic drug monitoring (TDM) is a specialized area of laboratory medicine which involves the measurement of drug concentrations in biological fluids with the aim of optimizing efficacy and reducing side effects, po...
PMC7289778
core_pubmed_pmc
Assessing parameter uncertainty in small-n pharmacometric analyses: value of the log-likelihood profiling-based sampling importance resampling (LLP-SIR) technique
Assessing parameter uncertainty in small-n pharmacometric analyses: value of the log-likelihood profiling-based sampling importance resampling (LLP-SIR) technique Abstract Abstract Assessing parameter uncertainty is a crucial step in pharmacometric workflows. Small datasets with ten or fewer subjects appear regularly i...
PMC12395308
core_pubmed_pmc
Carbamate Prodrugs Restrict In Vivo Metabolism and Improve the Pharmacokinetics of Isoniazid
Carbamate Prodrugs Restrict In Vivo Metabolism and Improve the Pharmacokinetics of Isoniazid Abstract Isoniazid (INH), an important first-line drug in tuberculosis (TB) treatment, faces significant challenges primarily due to hepatotoxicity and peripheral neuropathy as major side effects. These adverse effects often le...
PMC4621166
core_pubmed_pmc
Management of Meningitis Caused by Multi Drug-Resistant Acinetobacter Baumannii : Clinical, Microbiological and Pharmacokinetic Results in a Patient Treated with Colistin Methanesulfonate
Management of Meningitis Caused by Multi Drug-Resistant Acinetobacter Baumannii : Clinical, Microbiological and Pharmacokinetic Results in a Patient Treated with Colistin Methanesulfonate Abstract Abstract This paper reports on a 71- year-old Caucasian male who underwent neurosurgery for an oligodendroglioma, followed ...
PMC5685435
core_pubmed_pmc
Calculation of a First-In-Man Dose of 7- O -Succinyl Macrolactin A Based on Allometric Scaling of Data from Mice, Rats, and Dogs
Calculation of a First-In-Man Dose of 7- O -Succinyl Macrolactin A Based on Allometric Scaling of Data from Mice, Rats, and Dogs Abstract 7- O -Succinyl macrolactin A (SMA) exerts several pharmacological effects including anti-bacterial, anti-inflammation, and anti-cancer activities. Recently, SMA has been extensively ...
PMC10508576
core_pubmed_pmc
Pharmacokinetic analysis across studies to drive knowledge‐integration: A tutorial on individual patient data meta‐analysis (IPDMA)
Pharmacokinetic analysis across studies to drive knowledge‐integration: A tutorial on individual patient data meta‐analysis (IPDMA) Abstract Abstract Answering challenging questions in drug development sometimes requires pharmacokinetic (PK) data analysis across different studies, for example, to characterize PKs acros...
PMC6585766
core_pubmed_pmc
An Open‐Label, Phase 1 Study to Assess the Effects of Hepatic Impairment on Pomalidomide Pharmacokinetics
An Open‐Label, Phase 1 Study to Assess the Effects of Hepatic Impairment on Pomalidomide Pharmacokinetics Abstract Abstract Pomalidomide is an immunomodulatory drug and the dosage of 4 mg per day taken orally on days 1‐21 of repeated 28‐day cycles has been approved in the European Union and United States to treat patie...
PMC8385015
core_pubmed_pmc
Tumour-on-chip microfluidic platform for assessment of drug pharmacokinetics and treatment response
Tumour-on-chip microfluidic platform for assessment of drug pharmacokinetics and treatment response Abstract Abstract Microphysiological in vitro systems are platforms for preclinical evaluation of drug effects and significant advances have been made in recent years. However, existing microfluidic devices are not yet a...
PMC12962372
core_pubmed_pmc
Atomoxetine: toxicological aspects of a new treatment for attention deficit hyperactivity disorder in Brazil
Atomoxetine: toxicological aspects of a new treatment for attention deficit hyperactivity disorder in Brazil Abstract Abstract Objective Atomoxetine is widely used in the treatment of attention deficit hyperactivity disorder (ADHD), offering reduced risks of adverse motor effects and chemical dependence. However, its p...
PMC5680793
core_pubmed_pmc
Modulation of protein A binding allows single-step purification of mouse bispecific antibodies that retain FcRn binding
Modulation of protein A binding allows single-step purification of mouse bispecific antibodies that retain FcRn binding Abstract ABSTRACT The increased number of bispecific antibodies (BsAb) under therapeutic development has resulted in a need for mouse surrogate BsAbs. Here, we describe a one-step method for generatin...
PMC8597728
core_pubmed_pmc
Gepotidacin Pharmacokinetics-Pharmacodynamics against Escherichia coli in the One-Compartment and Hollow-Fiber In Vitro Infection Model Systems
Gepotidacin Pharmacokinetics-Pharmacodynamics against Escherichia coli in the One-Compartment and Hollow-Fiber In Vitro Infection Model Systems Abstract ABSTRACT Gepotidacin is a novel, first-in-class triazaacenaphthylene antibiotic that inhibits bacterial DNA replication by a distinct mechanism of action with an in vi...
PMC5226138
core_pubmed_pmc
A Novel Approach for the Administration of Medications and Fluids in Emergency Scenarios and Settings
A Novel Approach for the Administration of Medications and Fluids in Emergency Scenarios and Settings Abstract Abstract The available routes of administration commonly used for medications and fluids in the acute care setting are generally limited to oral, intravenous, or intraosseous routes, but in many patients, part...
PMC8279896
core_pubmed_pmc
Pharmacokinetics of Single Dose Lidocaine and Epinephrine Following Iontophoresis of the Tympanic Membrane in a Double-Blinded Randomized Trial
Pharmacokinetics of Single Dose Lidocaine and Epinephrine Following Iontophoresis of the Tympanic Membrane in a Double-Blinded Randomized Trial Abstract Objective: To evaluate local and systemic safety of bilateral iontophoretic administration of lidocaine with epinephrine or lidocaine alone to the tympanic membrane (T...
PMC7891741
core_pubmed_pmc
Metformin doses to ensure efficacy and safety in patients with reduced kidney function
Metformin doses to ensure efficacy and safety in patients with reduced kidney function Abstract We aimed to develop a metformin dosing strategy to optimise efficacy and safety in patients with reduced kidney function. Metformin data from two studies stratified by kidney function were analysed. The relationship between ...
PMC4317809
core_pubmed_pmc
Japanese phase I study of GC33, a humanized antibody against glypican-3 for advanced hepatocellular carcinoma
Japanese phase I study of GC33, a humanized antibody against glypican-3 for advanced hepatocellular carcinoma Abstract Abstract GC33 is a humanized mAb against human glypican-3 (GPC3). In the first-in-human study carried out in the USA, GC33 was well tolerated and showed preliminary antitumor activity in patients with ...
PMC5384349
core_pubmed_pmc
Cergutuzumab amunaleukin (CEA-IL2v), a CEA-targeted IL-2 variant-based immunocytokine for combination cancer immunotherapy: Overcoming limitations of aldesleukin and conventional IL-2-based immunocytokines
Cergutuzumab amunaleukin (CEA-IL2v), a CEA-targeted IL-2 variant-based immunocytokine for combination cancer immunotherapy: Overcoming limitations of aldesleukin and conventional IL-2-based immunocytokines Abstract ABSTRACT We developed cergutuzumab amunaleukin (CEA-IL2v, RG7813), a novel monomeric CEA-targeted immunoc...
PMC5697651
core_pubmed_pmc
A Cross‐Study Analysis Evaluating the Effects of Food on the Pharmacokinetics of Rivaroxaban in Clinical Studies
A Cross‐Study Analysis Evaluating the Effects of Food on the Pharmacokinetics of Rivaroxaban in Clinical Studies Abstract Abstract US prescribing guidelines recommend that 15‐ and 20‐mg doses of rivaroxaban be administered with food for the treatment of deep vein thrombosis (DVT) and pulmonary embolism (PE) and for red...
PMC6100562
core_pubmed_pmc
Simultaneous Determination and Pharmacokinetics of Peimine and Peiminine in Beagle Dog Plasma by UPLC-MS/MS after the Oral Administration of Fritillariae ussuriensis Maxim and Fritillariae thunbergii Miq Powder
Simultaneous Determination and Pharmacokinetics of Peimine and Peiminine in Beagle Dog Plasma by UPLC-MS/MS after the Oral Administration of Fritillariae ussuriensis Maxim and Fritillariae thunbergii Miq Powder Abstract Abstract A simple and high sensitive ultra-high performance liquid chromatography-tandem mass spectr...
PMC6424904
core_pubmed_pmc
The Utility of Efavirenz-based Prophylaxis Against HIV Infection. A Systems Pharmacological Analysis
The Utility of Efavirenz-based Prophylaxis Against HIV Infection. A Systems Pharmacological Analysis Abstract Pre-exposure prophylaxis (PrEP) is considered one of the five “pillars” by UNAIDS to reduce HIV transmission. Moreover, it is a tool for female self-protection against HIV, making it highly relevant to sub-Saha...
PMC12844320
core_pubmed_pmc
Anticancer Potential of Atractylenolides I–III: Efficacy, Mechanisms, Pharmacokinetics, and Safety
Anticancer Potential of Atractylenolides I–III: Efficacy, Mechanisms, Pharmacokinetics, and Safety Abstract Atractylenolides (ATs; mainly AT-I, II, and III), as one of the primary active components of the traditional Chinese medicine Atractylodes macrocephala , have demonstrated significant antitumorigenic effects agai...
PMC11184760
core_pubmed_pmc
Perceived barriers and facilitators for model-informed dosing in pregnancy: a qualitative study across healthcare practitioners and pregnant women
Perceived barriers and facilitators for model-informed dosing in pregnancy: a qualitative study across healthcare practitioners and pregnant women Abstract Background Most women use medication during pregnancy. Pregnancy-induced changes in physiology may require antenatal dose alterations. Yet, evidence-based doses in ...