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PMC11856279
core_pubmed_pmc
Redefining the treatment of Chagas disease: a review of recent clinical and pharmacological data for a novel formulation of nifurtimox
Redefining the treatment of Chagas disease: a review of recent clinical and pharmacological data for a novel formulation of nifurtimox Abstract Abstract Nifurtimox has been used for over 50 years to treat patients with Chagas disease, a potentially life-threatening neglected tropical disease caused by the protozoan par...
PMC5338840
core_pubmed_pmc
Pharmacokinetics and outcome of tazobactam/piperacillin in Japanese patients undergoing low-flow continuous renal replacement therapy: dosage considerations
Pharmacokinetics and outcome of tazobactam/piperacillin in Japanese patients undergoing low-flow continuous renal replacement therapy: dosage considerations Abstract Abstract Background Tazobactam/piperacillin (TAZ/PIPC), which is often combined with continuous renal replacement therapy (CRRT), induces renal excretion ...
PMC8345028
core_pubmed_pmc
Docetaxel Skin Exposure and Micronucleation Contributes to Skin Toxicity Caused by CPC634
Docetaxel Skin Exposure and Micronucleation Contributes to Skin Toxicity Caused by CPC634 Abstract Simple Summary CPC634 is a nanoparticle entrapping docetaxel that is associated with skin toxicity that resembles conventional docetaxel-related skin toxicity. In this randomised cross-over study, the cutaneous pharmacoki...
PMC10784707
core_pubmed_pmc
Teclistamab: Mechanism of action, clinical, and translational science
Teclistamab: Mechanism of action, clinical, and translational science Abstract Abstract Multiple myeloma (MM) remains incurable despite improvements in treatment options. B‐cell maturation antigen (BCMA) is predominantly expressed in B‐lineage cells and represents a promising new target for MM. Teclistamab (TECVAYLI TM...
PMC11933371
core_pubmed_pmc
Preliminary pharmacokinetic and psychophysical investigations after controlled oral and inhalative consumption of hexahydrocannabinol (HHC)
Preliminary pharmacokinetic and psychophysical investigations after controlled oral and inhalative consumption of hexahydrocannabinol (HHC) Abstract Abstract The semi-synthetic cannabinoid hexahydrocannabinol (HHC) has become a highly discussed topic in forensic toxicology since 2022 due to its legal availability at th...
PMC5299522
core_pubmed_pmc
Pharmacological properties of faster‐acting insulin aspart vs insulin aspart in patients with type 1 diabetes receiving continuous subcutaneous insulin infusion: A randomized, double‐blind, crossover trial
Pharmacological properties of faster‐acting insulin aspart vs insulin aspart in patients with type 1 diabetes receiving continuous subcutaneous insulin infusion: A randomized, double‐blind, crossover trial Abstract Abstract Aim To evaluate the pharmacological characteristics of faster‐acting insulin aspart (faster aspa...
PMC7848885
core_pubmed_pmc
Population Pharmacokinetics of Intraventricular Vancomycin in Neonatal Ventriculitis, A Preterm Pilot Study
Population Pharmacokinetics of Intraventricular Vancomycin in Neonatal Ventriculitis, A Preterm Pilot Study Abstract Highlights • Pharmacokinetics modelling of intraventricular vancomycin in a preterm pilot study. • Intraventricular vancomycin follows a one compartment model in neonatal ventriculitis treatment. • Ventr...
PMC8323503
core_pubmed_pmc
Antimicrobial stewardship in the ICU in COVID-19 times: the known unknowns
Antimicrobial stewardship in the ICU in COVID-19 times: the known unknowns Abstract Abstract Since the start of the COVID-19 pandemic, there has been concern about the concomitant rise of antimicrobial resistance. While bacterial co-infections seem rare in COVID-19 patients admitted to hospital wards and intensive care...
PMC11247118
core_pubmed_pmc
Population pharmacokinetic analysis for dose regimen optimization of vancomycin in Southern Chinese children
Population pharmacokinetic analysis for dose regimen optimization of vancomycin in Southern Chinese children Abstract Abstract Changes in physiological factors may result in large pharmacokinetic variability of vancomycin in pediatric patients, thereby leading to either supratherapeutic or subtherapeutic exposure and p...
PMC7100081
core_pubmed_pmc
Effect of Protein Binding on Exposure of Unbound and Total Mycophenolic Acid: A Population Pharmacokinetic Analysis in Chinese Adult Kidney Transplant Recipients
Effect of Protein Binding on Exposure of Unbound and Total Mycophenolic Acid: A Population Pharmacokinetic Analysis in Chinese Adult Kidney Transplant Recipients Abstract Abstract Objectives The population pharmacokinetic (popPK) characteristics of total mycophenolic acid (tMPA) have been investigated in various ethnic...
PMC5096019
core_pubmed_pmc
More Power to OATP1B1: An Evaluation of Sample Size in Pharmacogenetic Studies Using a Rosuvastatin PBPK Model for Intestinal, Hepatic, and Renal Transporter‐Mediated Clearances
More Power to OATP1B1: An Evaluation of Sample Size in Pharmacogenetic Studies Using a Rosuvastatin PBPK Model for Intestinal, Hepatic, and Renal Transporter‐Mediated Clearances Abstract Abstract Rosuvastatin is a substrate of choice in clinical studies of organic anion‐transporting polypeptide (OATP)1B1‐ and OATP1B3‐a...
PMC6060375
core_pubmed_pmc
Superior anti-neoplastic activities of triacontanol-PEG conjugate: synthesis, characterization and biological evaluations
Superior anti-neoplastic activities of triacontanol-PEG conjugate: synthesis, characterization and biological evaluations Abstract Abstract Triacontanol (TA, C 30 H 62 O), abundantly present in plant cuticle waxes and bee waxes, has been found to display promising anti-neoplastic potentials. As a long chain fatty alcoh...
PMC8656162
core_pubmed_pmc
Characterization of Alpelisib in Rat Plasma by a Newly Developed UPLC-MS/MS Method: Application to a Drug-Drug Interaction Study
Characterization of Alpelisib in Rat Plasma by a Newly Developed UPLC-MS/MS Method: Application to a Drug-Drug Interaction Study Abstract Alpelisib, an oral selective and small-molecule phosphoinositide 3-kinase inhibitor, was lately approved in the United States to treat breast cancer. A sensitive method to quantify a...
PMC9949628
core_pubmed_pmc
Prediction of improved antimalarial chemotherapy of artesunate-mefloquine in combination with mefloquine sensitive and resistant Plasmodium falciparum malaria
Prediction of improved antimalarial chemotherapy of artesunate-mefloquine in combination with mefloquine sensitive and resistant Plasmodium falciparum malaria Abstract Abstract Background Declining in susceptibility of Plasmodium falciparum to mefloquine is reported in South-East Asia. A revisiting on mefloquine pharma...
PMC7344199
core_pubmed_pmc
Extended-Interval Dosing Strategy of Immune Checkpoint Inhibitors in Lung Cancer: Will it Outlast the COVID-19 Pandemic?
Extended-Interval Dosing Strategy of Immune Checkpoint Inhibitors in Lung Cancer: Will it Outlast the COVID-19 Pandemic? Abstract Abstract Patients with lung cancer are particularly vulnerable to complications from coronavirus disease-2019 (COVID-19). Recurrent hospital visits and hospital admission are potential risk ...
PMC11707320
core_pubmed_pmc
Alternatives to Injectable Adrenaline for Treating Anaphylaxis
Alternatives to Injectable Adrenaline for Treating Anaphylaxis Abstract ABSTRACT Adrenaline is the first line treatment for anaphylaxis and adrenaline auto‐injectors (AAI) allow reliable, safe and ergonomic administration in the community. However, AAIs have significant limitations and adrenaline is often not used in a...
PMC10840092
core_pubmed_pmc
Emerging tendencies for the nano-delivery of gambogic acid: a promising approach in oncotherapy
Emerging tendencies for the nano-delivery of gambogic acid: a promising approach in oncotherapy Abstract Abstract Despite the advancements in cancer therapies during the past few years, chemo/photo resistance, severe toxic effects, recurrence of metastatic tumors, and non-selective targeting remain incomprehensible. Th...
PMC6323046
core_pubmed_pmc
A phase 1, first-in-human study of 18 F-GP1 positron emission tomography for imaging acute arterial thrombosis
A phase 1, first-in-human study of 18 F-GP1 positron emission tomography for imaging acute arterial thrombosis Abstract Abstract Background 18 F-GP1 is a novel positron emission tomography (PET) tracer that targets glycoprotein IIb/IIIa receptors on activated platelets. The study objective was to explore the feasibilit...
PMC7973549
core_pubmed_pmc
Population pharmacokinetic model development and its relationship with adverse events of oxcarbazepine in adult patients with epilepsy
Population pharmacokinetic model development and its relationship with adverse events of oxcarbazepine in adult patients with epilepsy Abstract Abstract This study aimed to develop a pharmacokinetic (PK) model of oxcarbazepine (OXC) and analyse the relationship between monohydroxylated derivative (MHD), an active metab...
PMC8467300
core_pubmed_pmc
A Newly Developed HPLC-UV/Vis Method Using Chemical Derivatization with 2-Naphthalenethiol for Quantitation of Sulforaphane in Rat Plasma
A Newly Developed HPLC-UV/Vis Method Using Chemical Derivatization with 2-Naphthalenethiol for Quantitation of Sulforaphane in Rat Plasma Abstract Abstract Sulforaphane (SFN), a naturally occurring isothiocyanate, has received significant attention because of its ability to modulate multiple biological functions, inclu...
PMC10932970
core_pubmed_pmc
Chiral phthalimides against penicillin-binding protein 2a of methicillin-resistant Staphylococcus aureus : molecular docking and in vitro analysis
Chiral phthalimides against penicillin-binding protein 2a of methicillin-resistant Staphylococcus aureus : molecular docking and in vitro analysis Abstract Abstract Staphylococcus aureus ( S. aureus ) is a commensal bacterium and an opportunistic pathogen causing a wide variety of infections ranging from localized skin...
PMC9300539
core_pubmed_pmc
Development of a population pharmacokinetic/pharmacodynamic model for various oral paclitaxel formulations co-administered with ritonavir and thrombospondin-1 based on data from early phase clinical studies
Development of a population pharmacokinetic/pharmacodynamic model for various oral paclitaxel formulations co-administered with ritonavir and thrombospondin-1 based on data from early phase clinical studies Abstract Abstract Purpose Orally administered paclitaxel offers increased patient convenience while providing a m...
PMC8708495
core_pubmed_pmc
Population Pharmacokinetics and Pharmacodynamic Target Attainment of Isavuconazole against Aspergillus fumigatus and Aspergillus flavus in Adult Patients with Invasive Fungal Diseases: Should Therapeutic Drug Monitoring for Isavuconazole Be Considered as Mandatory as for the Other Mold-Active Azoles?
Population Pharmacokinetics and Pharmacodynamic Target Attainment of Isavuconazole against Aspergillus fumigatus and Aspergillus flavus in Adult Patients with Invasive Fungal Diseases: Should Therapeutic Drug Monitoring for Isavuconazole Be Considered as Mandatory as for the Other Mold-Active Azoles? Abstract Isavucona...
PMC10836247
core_pubmed_pmc
Safety, tolerability, pharmacokinetics and pharmacodynamics of a novel farnesoid X receptor (FXR) agonist-TQA3526 in healthy Chinese volunteers: a double-blind, randomized, placebo-controlled, dose-escalation, food effect phase I study
Safety, tolerability, pharmacokinetics and pharmacodynamics of a novel farnesoid X receptor (FXR) agonist-TQA3526 in healthy Chinese volunteers: a double-blind, randomized, placebo-controlled, dose-escalation, food effect phase I study Abstract Abstract Background: TQA3526 is a novel farnesoid X receptor agonist develo...
PMC7013346
core_pubmed_pmc
Bioaccessibility and Pharmacokinetics of a Commercial Saffron ( Crocus sativus L.) Extract
Bioaccessibility and Pharmacokinetics of a Commercial Saffron ( Crocus sativus L.) Extract Abstract Abstract There are few studies about the pharmacokinetics of the low-molecular mass carotenoids crocetin or crocin isomers from saffron ( Crocus sativus L.). None has been performed with a galenic preparation of a standa...
PMC5768635
core_pubmed_pmc
Open-Label, Randomized, Two-Way, Crossover Study Assessing the Bioequivalence of the Liquid Formulation versus the Freeze-Dried Formulation of Recombinant Human FSH and Recombinant Human LH in a Fixed 2:1 Combination (Pergoveris ® ) in Pituitary-Suppressed Healthy Women
Open-Label, Randomized, Two-Way, Crossover Study Assessing the Bioequivalence of the Liquid Formulation versus the Freeze-Dried Formulation of Recombinant Human FSH and Recombinant Human LH in a Fixed 2:1 Combination (Pergoveris ® ) in Pituitary-Suppressed Healthy Women Abstract Abstract This was a Phase I, open-label,...
PMC6994532
core_pubmed_pmc
A limited sampling schedule to estimate individual pharmacokinetics of pemetrexed in patients with varying renal functions
A limited sampling schedule to estimate individual pharmacokinetics of pemetrexed in patients with varying renal functions Abstract Abstract Purpose Pemetrexed is a widely used cytostatic agent with an established exposure–response relationship. Although dosing is based on body surface area (BSA), large interindividual...
PMC12736384
core_pubmed_pmc
Advancing Photodynamic Cancer Therapy with Smart Light-Responsive Lipid and Polymeric Nanocarriers: Evidence from a Meta-Analysis of Efficacy and Pharmacokinetics
Advancing Photodynamic Cancer Therapy with Smart Light-Responsive Lipid and Polymeric Nanocarriers: Evidence from a Meta-Analysis of Efficacy and Pharmacokinetics Abstract Abstract Background/Objectives : Conventional anticancer drugs often exhibit limited solubility and bioavailability due to unfavorable physicochemic...
PMC9761610
core_pubmed_pmc
Combined computational approaches for developing new anti-Alzheimer drug candidates: 3D-QSAR, molecular docking and molecular dynamics studies of liquiritigenin derivatives
Combined computational approaches for developing new anti-Alzheimer drug candidates: 3D-QSAR, molecular docking and molecular dynamics studies of liquiritigenin derivatives Abstract Butyrylcholinesterase is an acetylcholine-degrading enzyme involved in the memorization process, which is becoming an interesting target f...
PMC12888872
core_pubmed_pmc
Effects of renal impairment and hemodialysis on the pharmacokinetics and safety of HRS-8427, a siderophore cephalosporin for Gram‐negative bacterial infections
Effects of renal impairment and hemodialysis on the pharmacokinetics and safety of HRS-8427, a siderophore cephalosporin for Gram‐negative bacterial infections Abstract ABSTRACT HRS-8427, a development-stage siderophore cephalosporin antibiotic, is being investigated for the treatment of aerobic Gram-negative bacterial...
PMC5916097
core_pubmed_pmc
Cardiac myosin activators for heart failure therapy: focus on omecamtiv mecarbil
Cardiac myosin activators for heart failure therapy: focus on omecamtiv mecarbil Abstract Heart failure continues to be a major global health problem with a pronounced impact on morbidity and mortality and very limited drug treatment options especially with regard to inotropic therapy. Omecamtiv mecarbil is a first-in-...
PMC4229966
core_pubmed_pmc
Pharmacokinetic Alteration of Baclofen by Multiple Oral Administration of Herbal Medicines in Rats
Pharmacokinetic Alteration of Baclofen by Multiple Oral Administration of Herbal Medicines in Rats Abstract Abstract The potential pharmacokinetic (PK) interaction of conventional western drug, baclofen, and oriental medications Oyaksungisan (OY) and Achyranthes bidentata radix (AB) extract for the treatment of spastic...
PMC5514398
core_pubmed_pmc
Calprotectin and the Magnitude of Antibodies to Infliximab in Clinically-stable Ulcerative Colitis Patients are More Relevant Than Infliximab Trough Levels and Pharmacokinetics for Therapeutic Escalation
Calprotectin and the Magnitude of Antibodies to Infliximab in Clinically-stable Ulcerative Colitis Patients are More Relevant Than Infliximab Trough Levels and Pharmacokinetics for Therapeutic Escalation Abstract Abstract Although infliximab (IFX) is an efficient therapy for ulcerative colitis (UC) patients, a consider...
PMC3992512
core_pubmed_pmc
Tumour cell retention of rucaparib, sustained PARP inhibition and efficacy of weekly as well as daily schedules
Tumour cell retention of rucaparib, sustained PARP inhibition and efficacy of weekly as well as daily schedules Abstract Abstract Background: Poly(ADP-ribose) polymerase-1 (PARP) inhibitors (PARPi) exploit tumour-specific defects in homologous recombination DNA repair and continuous dosing is most efficacious. Early cl...
PMC8518371
core_pubmed_pmc
Results of a Dose‐Finding Phase 1b Study of Subcutaneous Atezolizumab in Patients With Locally Advanced or Metastatic Non–Small Cell Lung Cancer
Results of a Dose‐Finding Phase 1b Study of Subcutaneous Atezolizumab in Patients With Locally Advanced or Metastatic Non–Small Cell Lung Cancer Abstract Abstract Intravenous (IV) atezolizumab is approved for non–small cell lung and other cancers. Subcutaneous (SC) atezolizumab coformulated with recombinant human hyalu...
PMC6700041
core_pubmed_pmc
Direct comparison of two extended-half-life recombinant FVIII products: a randomized, crossover pharmacokinetic study in patients with severe hemophilia A
Direct comparison of two extended-half-life recombinant FVIII products: a randomized, crossover pharmacokinetic study in patients with severe hemophilia A Abstract Abstract BAY 94-9027 is an extended-half-life, recombinant factor VIII (rFVIII) product conjugated with a 60-kDa branched polyethylene glycol (PEG) molecule...
PMC6713113
core_pubmed_pmc
A review on charred traditional Chinese herbs: carbonization to yield a haemostatic effect
A review on charred traditional Chinese herbs: carbonization to yield a haemostatic effect Abstract Abstract Context: Charcoal of Chinese drugs is a kind of special processing product in Chinese medicine and used for treatment of haemoptysis, hematemesis and haemorrhage in the clinic during ancient times. During carbon...
PMC8777650
core_pubmed_pmc
Design of Oral Sustained-Release Pellets by Modeling and Simulation Approach to Improve Compliance for Repurposing Sobrerol
Design of Oral Sustained-Release Pellets by Modeling and Simulation Approach to Improve Compliance for Repurposing Sobrerol Abstract Sobrerol, an oral mucolytic agent, in a recent study showed promise for treating multiple sclerosis. A human equivalent dose of 486 mg of sobrerol administered thrice daily (i.e., 1459 mg...
PMC11624666
core_pubmed_pmc
Evaluation of Olaparib Tablet Safety and Pharmacokinetics in Healthy Chinese Male Subjects
Evaluation of Olaparib Tablet Safety and Pharmacokinetics in Healthy Chinese Male Subjects Abstract Purpose To evaluate the safety and pharmacokinetics of olaparib tablet test formulation (T) and reference formulation (R) in healthy Chinese male subjects. Subjects and Methods This was a single-dose, randomized-sequence...
PMC11164218
core_pubmed_pmc
Insight into the avidity–affinity relationship of the bivalent, pH-dependent interaction between IgG and FcRn
Insight into the avidity–affinity relationship of the bivalent, pH-dependent interaction between IgG and FcRn Abstract ABSTRACT Monoclonal antibodies (mAbs) as therapeutics necessitate favorable pharmacokinetic properties, including extended serum half-life, achieved through pH-dependent binding to the neonatal Fc rece...
PMC8309017
core_pubmed_pmc
Meta-Analysis of Food Effect on Oral Absorption of Efflux Transporter Substrate Drugs: Does Delayed Gastric Emptying Influence Drug Transport Kinetics?
Meta-Analysis of Food Effect on Oral Absorption of Efflux Transporter Substrate Drugs: Does Delayed Gastric Emptying Influence Drug Transport Kinetics? Abstract Abstract The oral route of drug administration is the most convenient method of drug delivery, but it is associated with variable bioavailability. Food is one ...
PMC10593454
core_pubmed_pmc
Model-informed precision dosing in vancomycin treatment
Model-informed precision dosing in vancomycin treatment Abstract Abstract Introduction: While vancomycin remains a widely prescribed antibiotic, it can cause ototoxicity and nephrotoxicity, both of which are concentration-associated. Overtreatment can occur when the treatment lasts for an unnecessarily long time. Using...
PMC11048618
core_pubmed_pmc
What Is the Role of Basal Weekly Insulin in Clinical Practice? The State of the Art
What Is the Role of Basal Weekly Insulin in Clinical Practice? The State of the Art Abstract Despite the advent of innovative therapies in the treatment of diabetes, ever-increasing awareness is still directed to the role of insulin since it has continued to be at the centre of diabetes therapy for decades, as a therap...
PMC9617238
core_pubmed_pmc
Evidence for Implementation: Management of TB in HIV and Pregnancy
Evidence for Implementation: Management of TB in HIV and Pregnancy Abstract Abstract Purpose of Review Pregnant people living with HIV (PLWH) are at especially high risk for progression from latent tuberculosis infection (LTBI) to active tuberculosis (TB) disease. Among pregnant PLWH, concurrent TB increases the risk o...
PMC6601134
core_pubmed_pmc
In silico comparative molecular docking analysis and analysis of the anti-inflammatory mechanisms of action of tanshinone from Salvia miltiorrhiza
In silico comparative molecular docking analysis and analysis of the anti-inflammatory mechanisms of action of tanshinone from Salvia miltiorrhiza Abstract Abstract Tanshinones are a class of abietane diterpene compounds extracted from Salvia miltiorrhiza , and have been used for medical purposes in traditional Chinese...
PMC3536593
core_pubmed_pmc
Inferring biochemical reaction pathways: the case of the gemcitabine pharmacokinetics
Inferring biochemical reaction pathways: the case of the gemcitabine pharmacokinetics Abstract Abstract Background The representation of a biochemical system as a network is the precursor of any mathematical model of the processes driving the dynamics of that system. Pharmacokinetics uses mathematical models to describ...
PMC2901636
core_pubmed_pmc
Fentanyl Buccal Tablet for the Treatment of Breakthrough Pain: Pharmacokinetics of Buccal Mucosa Delivery and Clinical Efficacy
Fentanyl Buccal Tablet for the Treatment of Breakthrough Pain: Pharmacokinetics of Buccal Mucosa Delivery and Clinical Efficacy Abstract The treatment of breakthrough pain (BTP), a transitory exacerbation of pain that occurs on a background of otherwise-controlled, persistent pain, requires an opioid formulation and/or...
PMC5638173
core_pubmed_pmc
Assessing and predicting drug-induced anticholinergic risks: an integrated computational approach
Assessing and predicting drug-induced anticholinergic risks: an integrated computational approach Abstract Background: Anticholinergic (AC) adverse drug events (ADEs) are caused by inhibition of muscarinic receptors as a result of designated or off-target drug–receptor interactions. In practice, AC toxicity is assessed...
PMC9685043
core_pubmed_pmc
Renal function-based versus standard dosing of pemetrexed: a randomized controlled trial
Renal function-based versus standard dosing of pemetrexed: a randomized controlled trial Abstract Purpose Pemetrexed is a chemotherapeutic drug in the treatment of non-small cell lung cancer and mesothelioma. Optimized dosing of pemetrexed based on renal function instead of body surface area (BSA) is hypothesized to re...
PMC4133973
core_pubmed_pmc
Target-directed development and preclinical characterization of the proposed biosimilar rituximab GP2013
Target-directed development and preclinical characterization of the proposed biosimilar rituximab GP2013 Abstract Abstract Biosimilar development involves a target-directed iterative process to ensure a similar product to the originator. Here we report the preclinical development of the proposed biosimilar rituximab (G...
PMC11611940
core_pubmed_pmc
Repurposing fusidic acid as an antimicrobial against enterococci with a low probability of resistance development
Repurposing fusidic acid as an antimicrobial against enterococci with a low probability of resistance development Abstract Abstract Drug repurposing constitutes a strategy to combat antimicrobial resistance, by using agents with known safety, pharmacokinetics, and pharmacodynamics. Previous studies have implemented new...
PMC6224605
core_pubmed_pmc
Integrated Pharmacodynamic Analysis Identifies Two Metabolic Adaption Pathways to Metformin in Breast Cancer
Integrated Pharmacodynamic Analysis Identifies Two Metabolic Adaption Pathways to Metformin in Breast Cancer Abstract Summary Late-phase clinical trials investigating metformin as a cancer therapy are underway. However, there remains controversy as to the mode of action of metformin in tumors at clinical doses. We cond...
PMC5270293
core_pubmed_pmc
Translational Pharmacokinetic/Pharmacodynamic Modeling of Tumor Growth Inhibition Supports Dose‐Range Selection of the Anti–PD‐1 Antibody Pembrolizumab
Translational Pharmacokinetic/Pharmacodynamic Modeling of Tumor Growth Inhibition Supports Dose‐Range Selection of the Anti–PD‐1 Antibody Pembrolizumab Abstract Pembrolizumab, a humanized monoclonal antibody against programmed death 1 (PD‐1), has a manageable safety profile and robust clinical activity against advanced...
PMC7060025
core_pubmed_pmc
A Pharmacogenomic Dissection of a Rosuvastatin-Induced Rhabdomyolysis Case Evokes the Polygenic Nature of Adverse Drug Reactions
A Pharmacogenomic Dissection of a Rosuvastatin-Induced Rhabdomyolysis Case Evokes the Polygenic Nature of Adverse Drug Reactions Abstract Abstract Rosuvastatin, is a widely-used statin for the treatment of hypercholesterolemia and the prevention of cardiovascular diseases. Although rosuvastatin is well tolerated, about...
PMC4860631
core_pubmed_pmc
Pharmacokinetics and tolerability of NSC23925b, a novel P-glycoprotein inhibitor: preclinical study in mice and rats
Pharmacokinetics and tolerability of NSC23925b, a novel P-glycoprotein inhibitor: preclinical study in mice and rats Abstract Overexpression of P-glycoprotein (Pgp) increases multidrug resistance (MDR) in cancer, which greatly impedes satisfactory clinical treatment and outcomes of cancer patients. Due to unknown pharm...
PMC9373765
core_pubmed_pmc
Histopathological, physiological and biochemical assessment of resveratrol nanocapsules efficacy in bleomycin-induced acute and chronic lung injury in rats
Histopathological, physiological and biochemical assessment of resveratrol nanocapsules efficacy in bleomycin-induced acute and chronic lung injury in rats Abstract Abstract Acute lung injury (ALI) is a life-threatening illness which may progress to chronic pulmonary fibrosis (CPF). Resveratrol (RSV), a natural polyphe...
PMC12455471
core_pubmed_pmc
Safety, tolerability, and pharmacokinetics of single and multiple ascending doses of zavegepant nasal spray in healthy adults from two phase 1 randomized, placebo‐controlled trials
Safety, tolerability, and pharmacokinetics of single and multiple ascending doses of zavegepant nasal spray in healthy adults from two phase 1 randomized, placebo‐controlled trials Abstract Abstract Objective This study aimed to evaluate the safety and tolerability, and characterize the pharmacokinetic profile, of zave...
PMC4452936
core_pubmed_pmc
In Vivo Tissue Pharmacokinetics of Carbon-11-Labeled Clozapine in Healthy Volunteers: A Positron Emission Tomography Study
In Vivo Tissue Pharmacokinetics of Carbon-11-Labeled Clozapine in Healthy Volunteers: A Positron Emission Tomography Study Abstract Abstract We investigated clozapine (CLZ) tissue pharmacokinetics in vivo by using carbon-11-labeled CLZ ( 11 C-CLZ) and positron emission tomography (PET). Eight healthy volunteers underwe...
PMC12504959
core_pubmed_pmc
Development of Biosimilar Aflibercept SDZ-AFL
Development of Biosimilar Aflibercept SDZ-AFL Abstract Purpose Aflibercept is a recombinant fusion protein that binds with high affinity to vascular endothelial growth factor A (VEGF-A), and other growth factors, reducing pathological neovascularization and abnormal vascular permeability. Aflibercept is approved as a f...
PMC11679775
core_pubmed_pmc
The Effect of Physical Activity on Combined Cadmium, Lead, and Mercury Exposure
The Effect of Physical Activity on Combined Cadmium, Lead, and Mercury Exposure Abstract Background/Objective : Environmental exposures, such as heavy metals, can significantly affect physical activity, an important determinant of health. This study explores the effect of physical activity on combined exposure to cadmi...
PMC9936549
core_pubmed_pmc
Concise Overview of Glypromate Neuropeptide Research: From Chemistry to Pharmacological Applications in Neurosciences
Concise Overview of Glypromate Neuropeptide Research: From Chemistry to Pharmacological Applications in Neurosciences Abstract Neurodegenerative diseases of the central nervous system (CNS) pose a serious health concern worldwide, with a particular incidence in developed countries as a result of life expectancy increas...
PMC12417621
core_pubmed_pmc
The Effect of α ‐Mangostin on the Pharmacokinetic Profile of Tofacitinib in Rats Both In Vitro and In Vivo
The Effect of α ‐Mangostin on the Pharmacokinetic Profile of Tofacitinib in Rats Both In Vitro and In Vivo Abstract ABSTRACT This study investigated the effects of α ‐mangostin ( α ‐MG) on the pharmacokinetics of tofacitinib in vitro and in vivo, aiming to recommend its appropriate application in clinical practice. To ...
PMC8024938
core_pubmed_pmc
Pharmacokinetic and Pharmacodynamic Evaluation of Ravulizumab in Adults with Severe Coronavirus Disease 2019
Pharmacokinetic and Pharmacodynamic Evaluation of Ravulizumab in Adults with Severe Coronavirus Disease 2019 Abstract Abstract Introduction Terminal complement amplification is hypothesized to be a key contributor to the clinical manifestations of severe coronavirus disease 2019 (COVID-19). Ravulizumab, a humanized mon...
PMC9068897
core_pubmed_pmc
Pharmacokinetics, Safety and Pharmacokinetics/Pharmacodynamics Analysis of Omadacycline in Chinese Healthy Subjects
Pharmacokinetics, Safety and Pharmacokinetics/Pharmacodynamics Analysis of Omadacycline in Chinese Healthy Subjects Abstract Objective: Omadacycline is a new type of aminomethylcycline antibiotic, having a broad antibacterial spectrum. But the pharmacokinetic characteristics and safety profile of the Chinese population...
PMC3945639
core_pubmed_pmc
Safety, tolerability, and pharmacokinetics of the novel αv-integrin antibody EMD 525797 (DI17E6) in healthy subjects after ascending single intravenous doses
Safety, tolerability, and pharmacokinetics of the novel αv-integrin antibody EMD 525797 (DI17E6) in healthy subjects after ascending single intravenous doses Abstract Purpose We evaluated the safety, tolerability, and pharmacokinetics (PK) of EMD 525797 (DI17E6), a humanized monoclonal antibody targeting αv-integrins, ...
PMC5822818
core_pubmed_pmc
DCE-MRI Pharmacokinetic-Based Phenotyping of Invasive Ductal Carcinoma: A Radiomic Study for Prediction of Histological Outcomes
DCE-MRI Pharmacokinetic-Based Phenotyping of Invasive Ductal Carcinoma: A Radiomic Study for Prediction of Histological Outcomes Abstract Abstract Breast cancer is a disease affecting an increasing number of women worldwide. Several efforts have been made in the last years to identify imaging biomarker and to develop n...
PMC11638047
core_pubmed_pmc
Initial experience in implementing quantitative DCE-MRI to predict breast cancer therapy response in a multi-center and multi-vendor platform setting
Initial experience in implementing quantitative DCE-MRI to predict breast cancer therapy response in a multi-center and multi-vendor platform setting Abstract Abstract Quantitative dynamic contrast-enhanced (DCE) MRI as a promising method for the prediction of breast cancer response to neoadjuvant chemotherapy (NAC) ha...
PMC12480267
core_pubmed_pmc
A Comparative Review of the Pharmacology of Dalbavancin and Oritavancin for Gram-Positive Infections: Birds of a Feather or Apples and Oranges?
A Comparative Review of the Pharmacology of Dalbavancin and Oritavancin for Gram-Positive Infections: Birds of a Feather or Apples and Oranges? Abstract Abstract The clinical landscape of Gram-positive infections has been reshaped with the introduction of long-acting lipoglycopeptides, particularly dalbavancin and orit...
PMC8130501
core_pubmed_pmc
Main protease inhibitors and drug surface hotspots for the treatment of COVID-19: A drug repurposing and molecular docking approach
Main protease inhibitors and drug surface hotspots for the treatment of COVID-19: A drug repurposing and molecular docking approach Abstract Abstract Here, drug repurposing and molecular docking were employed to screen approved MPP inhibitors and their derivatives to suggest a specific therapeutic agent for the treatme...
PMC3438395
core_pubmed_pmc
Pharmacokinetics, pharmacodynamics, and safety of clevidipine after prolonged continuous infusion in subjects with mild to moderate essential hypertension
Pharmacokinetics, pharmacodynamics, and safety of clevidipine after prolonged continuous infusion in subjects with mild to moderate essential hypertension Abstract Purpose Clevidipine is a rapidly-acting intravenous dihydropyridine antihypertensive acting via calcium channel blockade. This was a randomized, single-blin...
PMC9304124
core_pubmed_pmc
Pharmacokinetic Interaction Between the MEK1/MEK2 Inhibitor Trametinib and Oral Contraceptives Containing Norethindrone and Ethinyl Estradiol in Female Patients With Solid Tumors
Pharmacokinetic Interaction Between the MEK1/MEK2 Inhibitor Trametinib and Oral Contraceptives Containing Norethindrone and Ethinyl Estradiol in Female Patients With Solid Tumors Abstract Abstract This phase 1 postapproval study assessed the effect of the mitogen‐activated protein kinase kinase enzyme 1/enzyme 2 inhibi...
PMC7690585
core_pubmed_pmc
Target-Mediated Brain Tissue Binding for Small Molecule Inhibitors of Heat Shock Protein 90
Target-Mediated Brain Tissue Binding for Small Molecule Inhibitors of Heat Shock Protein 90 Abstract Drug distribution in the brain is generally associated with an affinity for fatty brain tissues and therefore known to be species- and concentration-independent. We report here the effect of target affinity on brain tis...
PMC11338772
core_pubmed_pmc
Efficacy and safety of fospropofol disodium sedation for same-day bidirectional endoscopy in elderly patients: protocol for a prospective, single-center, randomized, double-blind, non-inferiority trial
Efficacy and safety of fospropofol disodium sedation for same-day bidirectional endoscopy in elderly patients: protocol for a prospective, single-center, randomized, double-blind, non-inferiority trial Abstract Abstract Introduction Fospropofol disodium is a novel prodrug that has improved pharmacokinetic and pharmacod...
PMC12597549
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UGT2B7-mediated drug–drug interaction between cannabinoids and hydromorphone
UGT2B7-mediated drug–drug interaction between cannabinoids and hydromorphone Abstract Hydromorphone is a highly potent opioid used to treat severe chronic pain. It is metabolized primarily by UDP-glucuronosyltransferase (UGT)2B7 to form the inactive hydromorphone-3-glucuronide. Given that previous studies have shown th...
PMC11416123
core_pubmed_pmc
Revisiting Niclosamide Formulation Approaches – a Pathway Toward Drug Repositioning
Revisiting Niclosamide Formulation Approaches – a Pathway Toward Drug Repositioning Abstract Abstract Niclosamide (NIC), an anthelmintic drug, has garnered recent attention for its potential as an antiviral, antibacterial, and chemotherapeutic agent, among other applications. Repurposing NIC presents a current trend, o...
PMC11593999
core_pubmed_pmc
Sacubitril/Valsartan in Pediatric Heart Failure (PANORAMA-HF): A Randomized, Multicenter, Double-Blind Trial
Sacubitril/Valsartan in Pediatric Heart Failure (PANORAMA-HF): A Randomized, Multicenter, Double-Blind Trial Abstract BACKGROUND: Sacubitril/valsartan, an angiotensin receptor-neprilysin inhibitor (ARNI), is an established treatment for heart failure (HF) with reduced left ventricular ejection fraction. It has not been...
PMC9228667
core_pubmed_pmc
Increased/Targeted Brain (Pro)Drug Delivery via Utilization of Solute Carriers (SLCs)
Increased/Targeted Brain (Pro)Drug Delivery via Utilization of Solute Carriers (SLCs) Abstract Membrane transporters have a crucial role in compounds’ brain drug delivery. They allow not only the penetration of a wide variety of different compounds to cross the endothelial cells of the blood–brain barrier (BBB), but al...
PMC11515623
core_pubmed_pmc
Active CNS delivery of oxycodone in healthy and endotoxemic pigs
Active CNS delivery of oxycodone in healthy and endotoxemic pigs Abstract Abstract Background The primary objective of this study was to advance our understanding of active drug uptake at brain barriers in higher species than rodents, by examining oxycodone brain concentrations in pigs. Methods This was investigated by...
PMC12521054
core_pubmed_pmc
Optimizing First‐Line Therapeutics in Non‐Small Cell Lung Cancer: Insights From Joint Modeling and Large‐Scale Data Analysis
Optimizing First‐Line Therapeutics in Non‐Small Cell Lung Cancer: Insights From Joint Modeling and Large‐Scale Data Analysis Abstract ABSTRACT Non‐small cell lung cancer (NSCLC) is often intrinsically resistant to several first‐ and second‐line therapeutics and can rapidly acquire further resistance after a patient beg...
PMC12401762
core_pubmed_pmc
A population pharmacokinetic approach to compare 51 Cr-EDTA and 99 m Tc-DTPA clearances in measuring renal glomerular filtration rate in oncopediatrics
A population pharmacokinetic approach to compare 51 Cr-EDTA and 99 m Tc-DTPA clearances in measuring renal glomerular filtration rate in oncopediatrics Abstract Background 51 Cr-EDTA and 99 m Tc-DTPA clearances are two reference methods of determining the glomerular filtration rate. The study aimed to compare these two...
PMC7735412
core_pubmed_pmc
Safety of sildenafil in premature infants with severe bronchopulmonary dysplasia (SILDI-SAFE): a multicenter, randomized, placebo-controlled, sequential dose-escalating, double-masked, safety study
Safety of sildenafil in premature infants with severe bronchopulmonary dysplasia (SILDI-SAFE): a multicenter, randomized, placebo-controlled, sequential dose-escalating, double-masked, safety study Abstract Background Pulmonary hypertension is a deadly complication of bronchopulmonary dysplasia, the most common pulmona...
PMC6710614
core_pubmed_pmc
A new era for migraine: Pharmacokinetic and pharmacodynamic insights into monoclonal antibodies with a focus on galcanezumab, an anti-CGRP antibody
A new era for migraine: Pharmacokinetic and pharmacodynamic insights into monoclonal antibodies with a focus on galcanezumab, an anti-CGRP antibody Abstract Abstract Purpose To review pharmacokinetic and pharmacodynamic characteristics of antibodies that bind to soluble ligands within the framework of calcitonin gene-r...
PMC10957591
core_pubmed_pmc
Biomarkers and computational models for predicting efficacy to tumor ICI immunotherapy
Biomarkers and computational models for predicting efficacy to tumor ICI immunotherapy Abstract Numerous studies have shown that immune checkpoint inhibitor (ICI) immunotherapy has great potential as a cancer treatment, leading to significant clinical improvements in numerous cases. However, it benefits a minority of p...
PMC4278557
core_pubmed_pmc
Pharmacokinetics, pharmacodynamics and safety of QGE031 (ligelizumab), a novel high-affinity anti-IgE antibody, in atopic subjects
Pharmacokinetics, pharmacodynamics and safety of QGE031 (ligelizumab), a novel high-affinity anti-IgE antibody, in atopic subjects Abstract Abstract Background Using a monoclonal antibody with greater affinity for IgE than omalizumab, we examined whether more complete suppression of IgE provided greater pharmacodynamic...
PMC5926275
core_pubmed_pmc
Pharmacokinetic and Pharmacodynamics of Self-Assembled Cubic Liquid Crystalline Nanoparticle Gel After Transdermal Administration
Pharmacokinetic and Pharmacodynamics of Self-Assembled Cubic Liquid Crystalline Nanoparticle Gel After Transdermal Administration Abstract Background The aim of this study was to assess the pharmacokinetics after transdermal administration by a novel skin microdialysis technology in rats. The guinea pig model was estab...
PMC11450402
core_pubmed_pmc
Lisavanbulin (BAL101553), a novel microtubule inhibitor, plus radiation in patients with newly diagnosed, MGMT promoter unmethylated glioblastoma
Lisavanbulin (BAL101553), a novel microtubule inhibitor, plus radiation in patients with newly diagnosed, MGMT promoter unmethylated glioblastoma Abstract Abstract Background Lisavanbulin (BAL101553) is a small, lipophilic, oral microtubule destabilizer with promising antitumoral activity observed in preclinical gliobl...
PMC8110483
core_pubmed_pmc
Clinical pharmacology strategies in supporting drug development and approval of antibody–drug conjugates in oncology
Clinical pharmacology strategies in supporting drug development and approval of antibody–drug conjugates in oncology Abstract Antibody–drug conjugates (ADCs) are important molecular entities in the treatment of cancer. These conjugates combine the target specificity of monoclonal antibodies with the potent anti-cancer ...
PMC8604242
core_pubmed_pmc
Evobrutinib, a covalent Bruton’s tyrosine kinase inhibitor: Mass balance, elimination route, and metabolism in healthy participants
Evobrutinib, a covalent Bruton’s tyrosine kinase inhibitor: Mass balance, elimination route, and metabolism in healthy participants Abstract Abstract The highly selective, covalent Bruton’s tyrosine kinase inhibitor evobrutinib is under investigation for treatment of patients with multiple sclerosis (MS). Early clinica...
PMC11353491
core_pubmed_pmc
In Vitro Physicochemical and Pharmacokinetic Properties of Bevacizumab Dissolved in Silicone Oils Compared to Hydrogel-Substitutes and Porcine Vitreous Bodies
In Vitro Physicochemical and Pharmacokinetic Properties of Bevacizumab Dissolved in Silicone Oils Compared to Hydrogel-Substitutes and Porcine Vitreous Bodies Abstract Abstract Anti-VEGF agents, e.g., bevacizumab, are used in retinal surgery, while their interaction with silicone oils and novel hydrogels remains unclea...
PMC10004171
core_pubmed_pmc
Enhanced Drug Delivery System Using Mesenchymal Stem Cells and Membrane-Coated Nanoparticles
Enhanced Drug Delivery System Using Mesenchymal Stem Cells and Membrane-Coated Nanoparticles Abstract Abstract Mesenchymal stem cells (MSCs) have newly developed as a potential drug delivery system. MSC-based drug delivery systems (MSCs-DDS) have made significant strides in the treatment of several illnesses, as shown ...
PMC8917044
core_pubmed_pmc
Oxycodone-Related Deaths: The Significance of Pharmacokinetic and Pharmacodynamic Drug Interactions
Oxycodone-Related Deaths: The Significance of Pharmacokinetic and Pharmacodynamic Drug Interactions Abstract Abstract Background and Objectives Oxycodone is frequently prescribed as well as detected in postmortem cases. Concurrent use of pharmacodynamically or pharmacokinetically interacting drugs can cause adverse eff...
PMC12907572
core_pubmed_pmc
The Effect of Uridine Diphosphate‐Glucuronosyltransferase Inhibition on the Pharmacokinetics of Ecopipam and Its Metabolites
The Effect of Uridine Diphosphate‐Glucuronosyltransferase Inhibition on the Pharmacokinetics of Ecopipam and Its Metabolites Abstract ABSTRACT Ecopipam, a selective dopamine D1 receptor antagonist in development for Tourette syndrome, is primarily converted by uridine diphosphate‐glucuronosyltransferase (UGT)1A9 to eco...
PMC2854768
core_pubmed_pmc
Issues in Using Human Variability Distributions to Estimate Low-Dose Risk
Issues in Using Human Variability Distributions to Estimate Low-Dose Risk Abstract Background The National Research Council (NRC) Committee on Improving Risk Analysis Approaches Used by the U.S. EPA (Environmental Protection Agency) recommended that low-dose risks be estimated in some situations using human variability...
PMC12816427
core_pubmed_pmc
Physiologically Motivated Sequential Population Modeling of Albumin Trends and Vedolizumab Pharmacokinetics for Pregnancy Dosing Regimen Optimization
Physiologically Motivated Sequential Population Modeling of Albumin Trends and Vedolizumab Pharmacokinetics for Pregnancy Dosing Regimen Optimization Abstract The pharmacokinetics (PK) of monoclonal antibodies (mAbs) during pregnancy remains poorly characterized, despite active inflammatory bowel diseases (IBD) being t...
PMC11053667
core_pubmed_pmc
An LC-MS/MS Method for Quantification of Lamotrigine and Its Main Metabolite in Dried Blood Spots
An LC-MS/MS Method for Quantification of Lamotrigine and Its Main Metabolite in Dried Blood Spots Abstract Background: The antiepileptic drug lamotrigine (LTG) shows high pharmacokinetic variability due to genotype influence and concomitant use of glucuronidation inducers and inhibitors, both of which may be frequently...
PMC3002807
core_pubmed_pmc
Effect of Itraconazole on the Pharmacokinetics of Diclofenac in Beagle Dogs
Effect of Itraconazole on the Pharmacokinetics of Diclofenac in Beagle Dogs Abstract The objective of this study was to investigate the potential effect of itraconazole on the pharmacokinetics of diclofenac potassium in beagle dogs after oral coadministration. Five male beagle dogs received a single oral 50 mg dose of ...
PMC12238446
core_pubmed_pmc
Facile indazole-endowed thiadiazole hybrid derivatives as antibacterial, anti-diabetic and thymidine phosphorylase inhibitors: An insight to experimental, in-vitro biological potential and computational approaches
Facile indazole-endowed thiadiazole hybrid derivatives as antibacterial, anti-diabetic and thymidine phosphorylase inhibitors: An insight to experimental, in-vitro biological potential and computational approaches Abstract In this study, a series of newly synthesized indazole-based thiadiazole hybrid derivatives ( 1–13...
PMC10610393
core_pubmed_pmc
Subconjunctival Delivery of Sorafenib-Tosylate-Loaded Cubosomes for Facilitated Diabetic Retinopathy Treatment: Formulation Development, Evaluation, Pharmacokinetic and Pharmacodynamic (PKPD) Studies
Subconjunctival Delivery of Sorafenib-Tosylate-Loaded Cubosomes for Facilitated Diabetic Retinopathy Treatment: Formulation Development, Evaluation, Pharmacokinetic and Pharmacodynamic (PKPD) Studies Abstract Abstract Diabetic retinopathy (DR) is a microvascular complication associated with vascular endothelial growth ...
PMC12185566
core_pubmed_pmc
Optimizing Nortriptyline Dosing: A Comparison between Pharmacogenetics-Based, Phenotype-Based, and Standard Dosing
Optimizing Nortriptyline Dosing: A Comparison between Pharmacogenetics-Based, Phenotype-Based, and Standard Dosing Abstract Background and objective Nortriptyline, a tricyclic antidepressant, has an important role in the pharmacotherapy of major depressive disorder (MDD). Individualized dosing approaches, such as pharm...
PMC12784668
core_pubmed_pmc
Integrating In Vitro Analytics for Improved Antibody–Drug Conjugate Candidate Selection
Integrating In Vitro Analytics for Improved Antibody–Drug Conjugate Candidate Selection Abstract Simple Summary Antibody–drug conjugates (ADCs) are targeted antitumoral medicines that bind potent drugs to antibodies, directing treatment to cancer cells and reducing side effects. In early drug development, finding the o...