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PMC12872618 | core_pubmed_pmc | Unexpected Clinical Drug-Drug Interaction of Fexinidazole on Midazolam Pharmacokinetics: Insights into Underlying Mechanisms from Clinical Phase I Study Results and Supporting In Vivo/Vitro Evidence | Unexpected Clinical Drug-Drug Interaction of Fexinidazole on Midazolam Pharmacokinetics: Insights into Underlying Mechanisms from Clinical Phase I Study Results and Supporting In Vivo/Vitro Evidence Abstract Abstract Background Fexinidazole, a nitroimidazole antiparasitic, has been approved to treat human African trypa... |
PMC9127076 | core_pubmed_pmc | Pharmacokinetic Characteristics of Siponimod in Healthy Volunteers and Patients With Multiple Sclerosis: Analyses of Published Clinical Trials | Pharmacokinetic Characteristics of Siponimod in Healthy Volunteers and Patients With Multiple Sclerosis: Analyses of Published Clinical Trials Abstract Objectives: This study aimed to investigate the pharmacokinetic characteristics of siponimod in healthy volunteers and patients with MS based on aggregated data from pu... |
PMC4225471 | core_pubmed_pmc | Phase III Study of the Efficacy and Safety of Subcutaneous Versus Intravenous Tocilizumab Monotherapy in Patients With Rheumatoid Arthritis | Phase III Study of the Efficacy and Safety of Subcutaneous Versus Intravenous Tocilizumab Monotherapy in Patients With Rheumatoid Arthritis Abstract Abstract Objective To evaluate the efficacious noninferiority of subcutaneous tocilizumab injection (TCZ-SC) monotherapy to intravenous TCZ infusion (TCZ-IV) monotherapy i... |
PMC12753538 | core_pubmed_pmc | Phase 1 dose escalation trial of the selective adenosine A2B antagonist PBF-1129 in patients with metastatic non-small cell lung cancer | Phase 1 dose escalation trial of the selective adenosine A2B antagonist PBF-1129 in patients with metastatic non-small cell lung cancer Abstract Abstract The adenosinergic pathway represents a critical immunometabolic checkpoint within the tumor microenvironment of non-small cell lung cancer (NSCLC), contributing to im... |
PMC12919677 | core_pubmed_pmc | Bioequivalence Between a Gantenerumab Disposable Syringe and an Autoinjector: A Randomized Controlled Trial in Healthy Volunteers | Bioequivalence Between a Gantenerumab Disposable Syringe and an Autoinjector: A Randomized Controlled Trial in Healthy Volunteers Abstract Abstract Gantenerumab, a monoclonal antibody targeting amyloid beta plaques in the brain, reduces plaque accumulation and was developed to slow Alzheimer's disease progression. Resu... |
PMC4762492 | core_pubmed_pmc | Pharmacodynamic Biomarker Development for PI3K Pathway Therapeutics | Pharmacodynamic Biomarker Development for PI3K Pathway Therapeutics Abstract Abstract The phosphatidylinositol 3-kinase (PI3K) signaling pathway is integral to many essential cell processes, including cell growth, differentiation, proliferation, motility, and metabolism. Somatic mutations and genetic amplifications tha... |
PMC6225321 | core_pubmed_pmc | Linking Aromatic Hydroxy Metabolic Functionalization of Drug Molecules to Structure and Pharmacologic Activity | Linking Aromatic Hydroxy Metabolic Functionalization of Drug Molecules to Structure and Pharmacologic Activity Abstract Drug functionalization through the formation of hydrophilic groups is the norm in the phase I metabolism of drugs for the modification of drug action. The reactions involved are mainly oxidative, cata... |
PMC11597569 | core_pubmed_pmc | Head-to-Head Comparison of UHPLC-MS/MS and Alinity C for Plasma Analysis of Risperidone and Paliperidone | Head-to-Head Comparison of UHPLC-MS/MS and Alinity C for Plasma Analysis of Risperidone and Paliperidone Abstract Abstract Background and objectives: Risperidone, a second-generation antipsychotic widely used in the treatment of schizophrenia, requires therapeutic drug monitoring due to its high interindividual variabi... |
PMC3973039 | core_pubmed_pmc | Pharmacokinetics and pharmacodynamics of oral tolvaptan in patients with varying degrees of renal function | Pharmacokinetics and pharmacodynamics of oral tolvaptan in patients with varying degrees of renal function Abstract The selective vasopressin V2–receptor antagonist tolvaptan is eliminated almost exclusively by non-renal mechanisms. As renal impairment can influence the pharmacokinetics of drugs even when eliminated by... |
PMC5536158 | core_pubmed_pmc | Larger Blood Pressure Reduction by Fixed-Dose Compared to Free Dose Combination Therapy of ACE Inhibitor and Calcium Antagonist in Hypertensive Patients | Larger Blood Pressure Reduction by Fixed-Dose Compared to Free Dose Combination Therapy of ACE Inhibitor and Calcium Antagonist in Hypertensive Patients Abstract The introduction of fixed combination of ACEi+CCB (Fixed) has significantly increased patients compliance and adherence to therapy. At the moment, however, th... |
PMC12850572 | core_pubmed_pmc | Absolute bioavailability and intravenous pharmacokinetics of N‐acetyl‐D‐mannosamine in humans | Absolute bioavailability and intravenous pharmacokinetics of N‐acetyl‐D‐mannosamine in humans Abstract Abstract Aims N‐acetyl‐D‐mannosamine monohydrate (ManNAc) is a naturally occurring monosaccharide that has attracted considerable attention for its potential in treating GNE myopathy, a rare autosomal recessive muscle... |
PMC5306113 | core_pubmed_pmc | How Can a Good Idea Fail? Basal Insulin Peglispro [LY2605541] for the Treatment of Type 2 Diabetes | How Can a Good Idea Fail? Basal Insulin Peglispro [LY2605541] for the Treatment of Type 2 Diabetes Abstract Introduction Lack of control in diabetic patients has stimulated the development of new insulin analogues. One of these was basal insulin peglispro (BIL) or LY2605541; it had a large hydrodynamic size, flat pharm... |
PMC12823305 | core_pubmed_pmc | Building Hybrid Pharmacometric‐Machine Learning Models in Oncology Drug Development: Current State and Recommendations | Building Hybrid Pharmacometric‐Machine Learning Models in Oncology Drug Development: Current State and Recommendations Abstract ABSTRACT Classic and hybrid pharmacometric‐machine learning models (hPMxML) are gaining momentum for applications in clinical drug development and precision medicine, especially within the onc... |
PMC9511087 | core_pubmed_pmc | Pharmacokinetic and pharmacodynamic properties of orally administered torasemide in healthy cats | Pharmacokinetic and pharmacodynamic properties of orally administered torasemide in healthy cats Abstract Abstract Background In people and dogs, torasemide has higher bioavailability, longer half‐life, and longer duration of action than equivalent doses of furosemide but data regarding pharmacological properties of to... |
PMC10624232 | core_pubmed_pmc | Lessons from the first-in-human in vivo CRISPR/Cas9 editing of the TTR gene by NTLA-2001 trial in patients with transthyretin amyloidosis with cardiomyopathy | Lessons from the first-in-human in vivo CRISPR/Cas9 editing of the TTR gene by NTLA-2001 trial in patients with transthyretin amyloidosis with cardiomyopathy Abstract Introduction: Transthyretin amyloidosis (ATTR amyloidosis) is a progressive fatal disease characterized by accumulation of amyloid fibrils composed of mi... |
PMC4935531 | core_pubmed_pmc | The Effect of Dolutegravir on the Pharmacokinetics of Metformin in Healthy Subjects | The Effect of Dolutegravir on the Pharmacokinetics of Metformin in Healthy Subjects Abstract Supplemental Digital Content is Available in the Text. Key Words: dolutegravir, metformin, drug interaction, pharmacokinetics Abstract Background: Dolutegravir is an integrase strand transfer inhibitor (INSTI) licensed for use ... |
PMC9861764 | core_pubmed_pmc | Pharmacokinetic Study of Intranasal Dexamethasone and Methylprednisolone Compared with Intravenous Administration: Two Open-Label, Single-Dose, Two-Period, Two-Sequence, Cross-Over Study in Healthy Volunteers | Pharmacokinetic Study of Intranasal Dexamethasone and Methylprednisolone Compared with Intravenous Administration: Two Open-Label, Single-Dose, Two-Period, Two-Sequence, Cross-Over Study in Healthy Volunteers Abstract Dexamethasone (DXM) and methylprednisolone (MEP) are potent glucocorticoids used to control several in... |
PMC5131888 | core_pubmed_pmc | Unraveling the pharmacokinetic interaction of ticagrelor and MEDI2452 (Ticagrelor antidote) by mathematical modeling | Unraveling the pharmacokinetic interaction of ticagrelor and MEDI2452 (Ticagrelor antidote) by mathematical modeling Abstract Abstract The investigational ticagrelor‐neutralizing antibody fragment, MEDI2452, is developed to rapidly and specifically reverse the antiplatelet effects of ticagrelor. However, the dynamic in... |
PMC5749432 | core_pubmed_pmc | Application of a pharmacokinetics-pharmacodynamics approach to the free propofol plasma levels during coronary artery bypass grafting surgery with hypothermic cardiopulmonary bypass | Application of a pharmacokinetics-pharmacodynamics approach to the free propofol plasma levels during coronary artery bypass grafting surgery with hypothermic cardiopulmonary bypass Abstract Abstract OBJECTIVES: The objective of this study was to apply a pharmacokinetics-pharmacodynamics approach to investigate the fre... |
PMC7251107 | core_pubmed_pmc | Phase 1 study of MRX34, a liposomal miR-34a mimic, in patients with advanced solid tumours | Phase 1 study of MRX34, a liposomal miR-34a mimic, in patients with advanced solid tumours Abstract Background In this first-in-human, Phase 1 study of a microRNA-based cancer therapy, the recommended Phase 2 dose (RP2D) of MRX34, a liposomal mimic of microRNA-34a (miR-34a), was determined and evaluated in patients wit... |
PMC8670371 | core_pubmed_pmc | Randomized, double-blind, two-way crossover bioequivalence and adhesion study, in healthy women, of a transdermal contraceptive patch with a newly sourced adhesive component at the end of shelf life vs. the EVRA patch at the beginning of shelf life | Randomized, double-blind, two-way crossover bioequivalence and adhesion study, in healthy women, of a transdermal contraceptive patch with a newly sourced adhesive component at the end of shelf life vs. the EVRA patch at the beginning of shelf life Abstract Objective: Evaluate bioequivalence, based on norelgestromin (N... |
PMC7379012 | core_pubmed_pmc | Pharmacokinetics of multivesicular liposomal encapsulated cytarabine when administered subcutaneously in dogs | Pharmacokinetics of multivesicular liposomal encapsulated cytarabine when administered subcutaneously in dogs Abstract Abstract Background Prolonged cytotoxic concentrations of cytarabine (CA) are required for maximum cytotoxicity. DepoCyt is a human liposomal cytarabine (LC) product that lasts longer in plasma and CSF... |
PMC11685978 | core_pubmed_pmc | PSCA-targeted BPX-601 CAR T cells with pharmacological activation by rimiducid in metastatic pancreatic and prostate cancer: a phase 1 dose escalation trial | PSCA-targeted BPX-601 CAR T cells with pharmacological activation by rimiducid in metastatic pancreatic and prostate cancer: a phase 1 dose escalation trial Abstract Abstract Here we report results of a phase 1 multi-institutional, open-label, dose-escalation trial ( NCT02744287 ) of BPX-601, an investigational autolog... |
PMC10069376 | core_pubmed_pmc | An update on the use of sphingosine 1-phosphate receptor modulators for the treatment of relapsing multiple sclerosis | An update on the use of sphingosine 1-phosphate receptor modulators for the treatment of relapsing multiple sclerosis Abstract ABSTRACT Introduction Multiple sclerosis (MS) is an immune-mediated disorder of the CNS manifested by recurrent attacks of neurological symptoms (related to focal inflammation) and gradual disa... |
PMC12829960 | core_pubmed_pmc | GC-MS based bioactive profiling of Phyllanthus niruri and its antibacterial potential through experimental and computational studies | GC-MS based bioactive profiling of Phyllanthus niruri and its antibacterial potential through experimental and computational studies Abstract Objective The study aimed to evaluate the antibacterial potential of Phyllanthus niruri by identifying its bioactive compounds through GC–MS, assessing their in vitro antibacteri... |
PMC11985771 | core_pubmed_pmc | The potential of dibenzazepine carboxamides in cancer therapy | The potential of dibenzazepine carboxamides in cancer therapy Abstract Cancer is a leading cause of mortality worldwide, with most conventional treatments lacking efficacy and having significant challenges like drug resistance. Finding new molecules is quite challenging in terms of cost, time and setbacks. Hence, drug ... |
PMC6158762 | core_pubmed_pmc | Venetoclax, bendamustine, and rituximab in patients with relapsed or refractory NHL: a phase Ib dose-finding study | Venetoclax, bendamustine, and rituximab in patients with relapsed or refractory NHL: a phase Ib dose-finding study Abstract Abstract Background Venetoclax is a selective, potent inhibitor of the anti-apoptotic B-cell leukemia/lymphoma-2 protein approved for treatment of chronic lymphocytic leukemia. We conducted a dose... |
PMC10304685 | core_pubmed_pmc | Methylphenidate Multiphasic Release Tablet: Bioequivalence Assessment between Two Formulations Administered under Fasting and Fed Conditions | Methylphenidate Multiphasic Release Tablet: Bioequivalence Assessment between Two Formulations Administered under Fasting and Fed Conditions Abstract Abstract Methylphenidate hydrochloride is used to treat children, adolescents, and adults with attention deficit/hyperactivity disorder (ADHD). Multiphasic release formul... |
PMC5506617 | core_pubmed_pmc | Comparative assessment of saliva and plasma for drug bioavailability and bioequivalence studies in humans | Comparative assessment of saliva and plasma for drug bioavailability and bioequivalence studies in humans Abstract Abstract Aims: To study the pharmacokinetics of selected drugs in plasma and saliva matrixes in healthy human volunteers, and to suggest using non-invasive saliva sampling instead of plasma as a surrogate ... |
PMC4665917 | core_pubmed_pmc | Phase I, two-way, crossover study to demonstrate bioequivalence and to compare safety and tolerability of single-dose XM17 vs Gonal-f ® in healthy women after follicle-stimulating hormone downregulation | Phase I, two-way, crossover study to demonstrate bioequivalence and to compare safety and tolerability of single-dose XM17 vs Gonal-f ® in healthy women after follicle-stimulating hormone downregulation Abstract Abstract Background XM17 is a recombinant human follicle-stimulating hormone (rhFSH) intended mainly for use... |
PMC4845836 | core_pubmed_pmc | Circulating Cytokines and Cytokine Receptors in Infliximab Treatment Failure Due to TNF-α Independent Crohn Disease | Circulating Cytokines and Cytokine Receptors in Infliximab Treatment Failure Due to TNF-α Independent Crohn Disease Abstract Abstract The inflammatory response at infliximab (IFX) treatment failure due to tumor necrosis factor (TNF)-α-independent Crohn disease activity is unknown. This is an exploratory, hypothesis-gen... |
PMC11279662 | core_pubmed_pmc | Toward Personalized Salbutamol Therapy: Validating Virtual Patient-Derived Population Pharmacokinetic Model with Real-World Data | Toward Personalized Salbutamol Therapy: Validating Virtual Patient-Derived Population Pharmacokinetic Model with Real-World Data Abstract Interindividual variability, influenced by patient-specific factors including age, weight, gender, race, and genetics, among others, contributes to variations in therapeutic response... |
PMC12614078 | core_pubmed_pmc | Representation of Older Adult Patients in Clinical Trials | Representation of Older Adult Patients in Clinical Trials Abstract ABSTRACT Older adults remain significantly underrepresented in clinical trials. This is concerning because age‐associated physiological changes can alter drug pharmacokinetics and pharmacodynamics. This paper examines the status of older adult represent... |
PMC8565835 | core_pubmed_pmc | Effect of variable domain charge on in vitro and in vivo disposition of monoclonal antibodies | Effect of variable domain charge on in vitro and in vivo disposition of monoclonal antibodies Abstract ABSTRACT A growing body of evidence supports the important role of molecular charge on antibody pharmacokinetics (PK), yet a quantitative description of the effect of charge on systemic and tissue disposition of antib... |
PMC9734246 | core_pubmed_pmc | Rivaroxaban Pharmacokinetics in Obese Subjects: A Systematic Review | Rivaroxaban Pharmacokinetics in Obese Subjects: A Systematic Review Abstract Introduction Venous thromboembolism (VTE) is a leading cause of morbidity and mortality globally. The direct oral anticoagulants, including rivaroxaban, are relatively novel therapeutic options in the treatment and prevention of VTE. There is ... |
PMC11647893 | core_pubmed_pmc | Development of Potent and Selective Inhibitors of Methylenetetrahydrofolate Dehydrogenase 2 for Targeting Acute Myeloid Leukemia: SAR, Structural Insights, and Biological Characterization | Development of Potent and Selective Inhibitors of Methylenetetrahydrofolate Dehydrogenase 2 for Targeting Acute Myeloid Leukemia: SAR, Structural Insights, and Biological Characterization Abstract Abstract Methylenetetrahydrofolate dehydrogenase/cyclohydrolase 2 (MTHFD2), a pivotal mitochondrial enzyme in one-carbon me... |
PMC6714908 | core_pubmed_pmc | Joint Bleeding Tendencies in Adult Patients With Hemophilia: It’s Not All Pharmacokinetics | Joint Bleeding Tendencies in Adult Patients With Hemophilia: It’s Not All Pharmacokinetics Abstract Hemophilic arthropathy from joint bleeding remains a complication with major morbidity in the increasingly aging patients with hemophilia. Prophylactic clotting factor infusions, based on pharmacokinetic dosing to reduce... |
PMC8003391 | core_pubmed_pmc | QSAR-Based Virtual Screening of Natural Products Database for Identification of Potent Antimalarial Hits | QSAR-Based Virtual Screening of Natural Products Database for Identification of Potent Antimalarial Hits Abstract With about 400,000 annual deaths worldwide, malaria remains a public health burden in tropical and subtropical areas, especially in low-income countries. Selection of drug-resistant Plasmodium strains has d... |
PMC6687230 | core_pubmed_pmc | Simultaneous quantification of lidocaine and prilocaine in human plasma by LC-MS/MS and its application in a human pharmacokinetic study | Simultaneous quantification of lidocaine and prilocaine in human plasma by LC-MS/MS and its application in a human pharmacokinetic study Abstract Abstract Objective The aim of the work was to develop and validate a simple, sensitive and selective Liquid chromatography with Mass spectroscopic method for simultaneous qua... |
PMC11508752 | core_pubmed_pmc | Renal Allograft Function and the Tacrolimus C/D Ratio: Insights from a Prospective Study on MeltDose Tacrolimus | Renal Allograft Function and the Tacrolimus C/D Ratio: Insights from a Prospective Study on MeltDose Tacrolimus Abstract Abstract Background : The tacrolimus concentration-to-dose (C/D) ratio is valuable for optimizing nephrotoxicity-related renal outcomes. Prospective data on the C/D ratio in kidney transplant recipie... |
PMC9291160 | core_pubmed_pmc | A Bioequivalence Study of Avanafil in Healthy Chinese Male Subjects Under Fasting and Fed Conditions: Results of a Randomized, Open‐Label, Single‐Dose, 2‐Sequence, 2‐Period Crossover Study | A Bioequivalence Study of Avanafil in Healthy Chinese Male Subjects Under Fasting and Fed Conditions: Results of a Randomized, Open‐Label, Single‐Dose, 2‐Sequence, 2‐Period Crossover Study Abstract Abstract This bioequivalence study was conducted to determine the pharmacokinetics and safety profiles of an originator an... |
PMC11178177 | core_pubmed_pmc | Effect of tetanic stimulation prior to train-of-four monitoring on the time to muscle response stabilization with neuromuscular blockade with rocuronium in patients aged 60 to 80 years: A prospective randomized controlled trial | Effect of tetanic stimulation prior to train-of-four monitoring on the time to muscle response stabilization with neuromuscular blockade with rocuronium in patients aged 60 to 80 years: A prospective randomized controlled trial Abstract Purpose To determine the effect of tetanic stimulation on the time to achieve stabi... |
PMC7993124 | core_pubmed_pmc | A bivalent, bispecific Dab-Fc antibody molecule for dual targeting of HER2 and HER3 | A bivalent, bispecific Dab-Fc antibody molecule for dual targeting of HER2 and HER3 Abstract ABSTRACT Dual targeting of surface receptors with bispecific antibodies is attracting increasing interest in cancer therapy. Here, we present a novel bivalent and bispecific antagonistic molecule (Dab-Fc) targeting human epider... |
PMC7392943 | core_pubmed_pmc | A Phase I, Randomized, Single‑Blind, Placebo‑Controlled, Single Ascending Dose Study of the Safety, Tolerability, and Pharmacokinetics of Subcutaneous and Oral TRV250, a G Protein-Selective Delta Receptor Agonist, in Healthy Subjects | A Phase I, Randomized, Single‑Blind, Placebo‑Controlled, Single Ascending Dose Study of the Safety, Tolerability, and Pharmacokinetics of Subcutaneous and Oral TRV250, a G Protein-Selective Delta Receptor Agonist, in Healthy Subjects Abstract Background The delta opioid receptor (DOR) has been identified as a therapeut... |
PMC12311517 | core_pubmed_pmc | Dose escalation study of the HLA-A2-WT1 CD3 bispecific antibody RO7283420 in relapsed/refractory acute myeloid leukemia ∗ | Dose escalation study of the HLA-A2-WT1 CD3 bispecific antibody RO7283420 in relapsed/refractory acute myeloid leukemia ∗ Abstract Key Points • RO7283420, a TCB engaging CD3 and Wilms tumor protein 1, demonstrated pharmacodynamic activity in this phase 1 study. • RO7283420 was discontinued because of the lack of an exp... |
PMC5739923 | core_pubmed_pmc | Pharmacokinetics and pharmacodynamics of Shengjiang decoction in rats with acute pancreatitis for protecting against multiple organ injury | Pharmacokinetics and pharmacodynamics of Shengjiang decoction in rats with acute pancreatitis for protecting against multiple organ injury Abstract AIM To explore the pharmacokinetics and pharmacodynamics of Shengjiang decoction (SJD) in rats with acute pancreatitis (AP) for protecting against multiple organ injury. ME... |
PMC6752940 | core_pubmed_pmc | Statistical Methodology in Studies of Prenatal Exposure to Mixtures of Endocrine-Disrupting Chemicals: A Review of Existing Approaches and New Alternatives | Statistical Methodology in Studies of Prenatal Exposure to Mixtures of Endocrine-Disrupting Chemicals: A Review of Existing Approaches and New Alternatives Abstract Background: Prenatal exposures to endocrine-disrupting chemicals (EDCs) during critical developmental windows have been implicated in the etiologies of a w... |
PMC5341681 | core_pubmed_pmc | Perioperative Considerations and Management of Patients Receiving Anticoagulants | Perioperative Considerations and Management of Patients Receiving Anticoagulants Abstract Anticoagulants remain the primary strategy for the prevention and treatment of thrombosis. Unfractionated heparin, low molecular weight heparin (LMWH), fondaparinux, and warfarin have been studied and employed extensively with dir... |
PMC4186429 | core_pubmed_pmc | Differential analysis of transient increases of serum cTnI in response to handling in rats | Differential analysis of transient increases of serum cTnI in response to handling in rats Abstract Serum cardiac troponins are the key biomarkers of myocardial necrosis in humans and in preclinical species. The use of ultrasensitive assays for serum cardiac troponin I (cTnI) as a biomarker in safety studies is hampere... |
PMC4689776 | core_pubmed_pmc | Assessment of Interspecies Differences in Drug-Induced QTc Interval Prolongation in Cynomolgus Monkeys, Dogs and Humans | Assessment of Interspecies Differences in Drug-Induced QTc Interval Prolongation in Cynomolgus Monkeys, Dogs and Humans Abstract Background and Purpose The selection of the most suitable animal species and subsequent translation of the concentration-effect relationship to humans are critical steps for accurate assessme... |
PMC12891150 | core_pubmed_pmc | Development and validation of UPLC-MS/MS method for pharmacokinetics and tissue distribution of Tylvalosin and its bioactive metabolites in swine | Development and validation of UPLC-MS/MS method for pharmacokinetics and tissue distribution of Tylvalosin and its bioactive metabolites in swine Abstract Background Tylvalosin (acetylisovaleryltylosin), a breakthrough semi-synthetic derivative of tylosin engineered to address pharmacokinetic limitations and bacterial ... |
PMC10509173 | core_pubmed_pmc | Deep learning driven de novo drug design based on gastric proton pump structures | Deep learning driven de novo drug design based on gastric proton pump structures Abstract Existing drugs often suffer in their effectiveness due to detrimental side effects, low binding affinity or pharmacokinetic problems. This may be overcome by the development of distinct compounds. Here, we exploit the rich structu... |
PMC10286317 | core_pubmed_pmc | Factors Determining the Susceptibility of Fish to Effects of Human Pharmaceuticals | Factors Determining the Susceptibility of Fish to Effects of Human Pharmaceuticals Abstract The increasing levels and frequencies at which active pharmaceutical ingredients (APIs) are being detected in the environment are of significant concern, especially considering the potential adverse effects they may have on nont... |
PMC8519898 | core_pubmed_pmc | Pharmacokinetic properties of a novel formulation of S -adenosyl- l -methionine phytate | Pharmacokinetic properties of a novel formulation of S -adenosyl- l -methionine phytate Abstract Abstract S -adenosyl- l -methionine (SAM), the main endogenous methyl donor, is the adenosyl derivative of the amino acid methionine, which displays many important roles in cellular metabolism. It is widely used as a food s... |
PMC7470810 | core_pubmed_pmc | Bile duct ligation enhances AZT CNS toxicity partly by impairing the expression and function of BCRP in rat brain | Bile duct ligation enhances AZT CNS toxicity partly by impairing the expression and function of BCRP in rat brain Abstract Abstract Breast cancer resistance protein (BCRP) is one of ATP-binding cassette (ABC) transporters in brain microvessel endothelial cells that transport their substrates from brain to blood, thus l... |
PMC8350654 | core_pubmed_pmc | Pharmacokinetics of treprostinil in children with functional single-ventricle pulmonary arterial hypertension: a randomized controlled trial | Pharmacokinetics of treprostinil in children with functional single-ventricle pulmonary arterial hypertension: a randomized controlled trial Abstract Abstract Background Application of Treprostinil (TRE) in the patients with single ventricle (SV) physiology is very limited, and the optimal dose for children has not bee... |
PMC12178431 | core_pubmed_pmc | Liposome Encapsulation Enhances Ripasudil Therapeutic Efficacy Against Proliferative Vitreoretinal Diseases: Implications in Advanced Ocular Treatment | Liposome Encapsulation Enhances Ripasudil Therapeutic Efficacy Against Proliferative Vitreoretinal Diseases: Implications in Advanced Ocular Treatment Abstract Abstract Purpose Proliferative vitreoretinal diseases, such as proliferative vitreoretinopathy (PVR) and neovascular age-related macular degeneration (nAMD), po... |
PMC12040935 | core_pubmed_pmc | Pregnant maternal brain dorsal anterior cingulate cortex choline/creatine ratios on 1H-MR spectroscopy in opioid exposure | Pregnant maternal brain dorsal anterior cingulate cortex choline/creatine ratios on 1H-MR spectroscopy in opioid exposure Abstract Abstract There is growing interest in understanding the effects of opioid use on the brain, yet the effects of opioid use on the pregnant maternal brain are still relatively unknown. Pregna... |
PMC7764797 | core_pubmed_pmc | A Physiologically-Based Pharmacokinetic (PBPK) Model Network for the Prediction of CYP1A2 and CYP2C19 Drug–Drug–Gene Interactions with Fluvoxamine, Omeprazole, S-mephenytoin, Moclobemide, Tizanidine, Mexiletine, Ethinylestradiol, and Caffeine | A Physiologically-Based Pharmacokinetic (PBPK) Model Network for the Prediction of CYP1A2 and CYP2C19 Drug–Drug–Gene Interactions with Fluvoxamine, Omeprazole, S-mephenytoin, Moclobemide, Tizanidine, Mexiletine, Ethinylestradiol, and Caffeine Abstract Physiologically-based pharmacokinetic (PBPK) modeling is a well-reco... |
PMC7575021 | core_pubmed_pmc | A nebulised antitumour necrosis factor receptor-1 domain antibody in patients at risk of postoperative lung injury: A randomised, placebo-controlled pilot study | A nebulised antitumour necrosis factor receptor-1 domain antibody in patients at risk of postoperative lung injury: A randomised, placebo-controlled pilot study Abstract Abstract BACKGROUND Tumour necrosis factor receptor 1 (TNFR1) signalling mediates the cell death and inflammatory effects of TNF-α. OBJECTIVE The curr... |
PMC9145019 | core_pubmed_pmc | Physiologically Based Pharmacokinetic (PBPK) Modeling of Clopidogrel and Its Four Relevant Metabolites for CYP2B6, CYP2C8, CYP2C19, and CYP3A4 Drug–Drug–Gene Interaction Predictions | Physiologically Based Pharmacokinetic (PBPK) Modeling of Clopidogrel and Its Four Relevant Metabolites for CYP2B6, CYP2C8, CYP2C19, and CYP3A4 Drug–Drug–Gene Interaction Predictions Abstract The antiplatelet agent clopidogrel is listed by the FDA as a strong clinical index inhibitor of cytochrome P450 (CYP) 2C8 and wea... |
PMC6155574 | core_pubmed_pmc | A Review on the Phytochemistry, Pharmacology, and Pharmacokinetics of Amentoflavone, a Naturally-Occurring Biflavonoid | A Review on the Phytochemistry, Pharmacology, and Pharmacokinetics of Amentoflavone, a Naturally-Occurring Biflavonoid Abstract Abstract Amentoflavone (C 30 H 18 O 10 ) is a well-known biflavonoid occurring in many natural plants. This polyphenolic compound has been discovered to have some important bioactivities, incl... |
PMC7355633 | core_pubmed_pmc | Efficacy Assessment of an Uncharged Reactivator of NOP-Inhibited Acetylcholinesterase Based on Tetrahydroacridine Pyridine-Aldoxime Hybrid in Mouse Compared to Pralidoxime | Efficacy Assessment of an Uncharged Reactivator of NOP-Inhibited Acetylcholinesterase Based on Tetrahydroacridine Pyridine-Aldoxime Hybrid in Mouse Compared to Pralidoxime Abstract Abstract (1) Background: Human exposure to organophosphorus compounds employed as pesticides or as chemical warfare agents induces deleteri... |
PMC3352867 | core_pubmed_pmc | Biodistribution and pharmacokinetics of a telodendrimer micellar paclitaxel nanoformulation in a mouse xenograft model of ovarian cancer | Biodistribution and pharmacokinetics of a telodendrimer micellar paclitaxel nanoformulation in a mouse xenograft model of ovarian cancer Abstract Background A multifunctional telodendrimer-based micelle system was characterized for delivery of imaging and chemotherapy agents to mouse tumor xenografts. Previous optical ... |
PMC12641083 | core_pubmed_pmc | Model‐Informed Drug Development Applications and Opportunities in mRNA‐LNP Therapeutics | Model‐Informed Drug Development Applications and Opportunities in mRNA‐LNP Therapeutics Abstract Abstract The utilization of lipid nanoparticles (LNP) for encapsulating mRNA has revolutionized the field of therapeutics, enabling the rapid development of COVID‐19 vaccines and cancer vaccines. However, the clinical devel... |
PMC5076775 | core_pubmed_pmc | Bioavailability, safety, and pharmacodynamics of delayed-release dexlansoprazole administered as two 30 mg orally disintegrating tablets or one 60 mg capsule | Bioavailability, safety, and pharmacodynamics of delayed-release dexlansoprazole administered as two 30 mg orally disintegrating tablets or one 60 mg capsule Abstract Background: Dual delayed-release dexlansoprazole is approved for use in adults as a 30 mg orally disintegrating tablet (ODT) or as 30 mg and 60 mg capsul... |
PMC7805603 | core_pubmed_pmc | Innate Immunity Plays a Key Role in Controlling Viral Load in COVID-19: Mechanistic Insights from a Whole-Body Infection Dynamics Model | Innate Immunity Plays a Key Role in Controlling Viral Load in COVID-19: Mechanistic Insights from a Whole-Body Infection Dynamics Model Abstract Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is a pathogen of immense public health concern. Efforts to control the disease have only proven mildly successful,... |
PMC3813130 | core_pubmed_pmc | Comparative Pharmacokinetics of Berberine, Palmatine and Jatrorrhizine in Rat Plasma after Oral Administration of Rhizoma coptidis and Zuojinwan Using Liquid Chromatography-Tandem Mass Spectrometry | Comparative Pharmacokinetics of Berberine, Palmatine and Jatrorrhizine in Rat Plasma after Oral Administration of Rhizoma coptidis and Zuojinwan Using Liquid Chromatography-Tandem Mass Spectrometry Abstract A selective and sensitive liquid chromatography-tandem mass spectrometry (LC-MS/ MS) method was developed for the... |
PMC5919995 | core_pubmed_pmc | GR3027 reversal of neurosteroid-induced, GABA-A receptor-mediated inhibition of human brain function: an allopregnanolone challenge study | GR3027 reversal of neurosteroid-induced, GABA-A receptor-mediated inhibition of human brain function: an allopregnanolone challenge study Abstract Rationale GR3027 is a novel small molecule GABA-A receptor-modulating steroid antagonist, which in non-clinical studies has shown promise for treatment of human disorders du... |
PMC8426351 | core_pubmed_pmc | Influence of FMO3 and CYP3A4 Polymorphisms on the Pharmacokinetics of Teneligliptin in Humans | Influence of FMO3 and CYP3A4 Polymorphisms on the Pharmacokinetics of Teneligliptin in Humans Abstract Abstract Teneligliptin, a dipeptidyl peptidase-4 inhibitor, is used to treat type 2 diabetes mellitus. FMO3 and CYP3A4 metabolize teneligliptin into teneligliptin sulfoxide. This study examined the effects of FMO3 (rs... |
PMC8004929 | core_pubmed_pmc | Whole-Body Pharmacokinetics and Physiologically Based Pharmacokinetic Model for Monomethyl Auristatin E (MMAE) | Whole-Body Pharmacokinetics and Physiologically Based Pharmacokinetic Model for Monomethyl Auristatin E (MMAE) Abstract Abstract Monomethyl auristatin E (MMAE) is one of the most commonly used payloads for developing antibody–drug conjugates (ADC). However, limited studies have comprehensively evaluated the whole-body ... |
PMC4608656 | core_pubmed_pmc | Pharmacokinetics of Levodopa before and after Gastrointestinal Resection in Parkinson's Disease | Pharmacokinetics of Levodopa before and after Gastrointestinal Resection in Parkinson's Disease Abstract Abstract Introduction Levodopa (LD) is important in the clinical treatment of Parkinson's disease (PD), and the changes of its pharmacokinetics may affect the clinical outcome. LD is mainly absorbed in the upper int... |
PMC8434926 | core_pubmed_pmc | Pharmacodynamic Studies of Fluorescent Diamond Carriers of Doxorubicin in Liver Cancer Cells and Colorectal Cancer Organoids | Pharmacodynamic Studies of Fluorescent Diamond Carriers of Doxorubicin in Liver Cancer Cells and Colorectal Cancer Organoids Abstract Background We recently reported on preferential deposition of bare fluorescent diamond particles FDP-NV-700/800nm (FDP-NV) in the liver following intravenous administration to rats. The ... |
PMC12834026 | core_pubmed_pmc | Evaluation of reserpine-induced fibromyalgia in mice: A comparative behavioral, neurochemical, and histological assessment of two doses | Evaluation of reserpine-induced fibromyalgia in mice: A comparative behavioral, neurochemical, and histological assessment of two doses Abstract Fibromyalgia (FM) is a chronic pain disorder characterised by widespread musculoskeletal pain, fatigue, and cognitive disturbances. Due to its complex and poorly understood pa... |
PMC8280016 | core_pubmed_pmc | Pharmacokinetics and Safety of a Bilastine Once-Daily, Preservative-Free, Ophthalmic Formulation | Pharmacokinetics and Safety of a Bilastine Once-Daily, Preservative-Free, Ophthalmic Formulation Abstract Introduction Bilastine is a second-generation H 1 antihistamine indicated for the symptomatic treatment of allergic rhinoconjunctivitis and urticaria. On the basis of the demonstrated efficacy and safety of the ora... |
PMC12030048 | core_pubmed_pmc | The Effect of Gut Microbiome Perturbation on the Bioavailability of Glycyrrhizic Acid in Rats | The Effect of Gut Microbiome Perturbation on the Bioavailability of Glycyrrhizic Acid in Rats Abstract Abstract Background : Oral administration remains the most common route for drug absorption. Emerging evidence highlights the important role of gut microbiome in the pharmacokinetics of oral medications. Glycyrrhizic ... |
PMC5566391 | core_pubmed_pmc | Improvement of Pharmacokinetic Profile of TRAIL via Trimer-Tag Enhances its Antitumor Activity in vivo | Improvement of Pharmacokinetic Profile of TRAIL via Trimer-Tag Enhances its Antitumor Activity in vivo Abstract TNF-related apoptosis-inducing ligand (TRAIL/Apo2L) has long been considered a tantalizing target for cancer therapy because it mediates activation of the extrinsic apoptosis pathway in a tumor-specific manne... |
PMC6222672 | core_pubmed_pmc | Pharmacokinetic and Metabolism Studies of 12-Riboside-Pseudoginsengenin DQ by UPLC-MS/MS and UPLC-QTOF-MS E | Pharmacokinetic and Metabolism Studies of 12-Riboside-Pseudoginsengenin DQ by UPLC-MS/MS and UPLC-QTOF-MS E Abstract Abstract Pharmacokinetic and metabolism studies of 12-riboside-pseudoginsengenin DQ (RPDQ), a novel ginsenoside with an anti-cancer effect, were carried out, aiming at discussing the characteristics of t... |
PMC12685806 | core_pubmed_pmc | Population pharmacokinetics/pharmacodynamics and safety of YPEG-rhGH in elderly subjects | Population pharmacokinetics/pharmacodynamics and safety of YPEG-rhGH in elderly subjects Abstract Abstract Y-shape branched PEGylated recombinant human growth hormone (YPEG-rhGH) is a suitable drug for the treatment of growth hormone deficiency. The aim of this study was to establish a population pharmacokinetics/pharm... |
PMC7306030 | core_pubmed_pmc | Population pharmacokinetics and target attainment of ciprofloxacin in critically ill patients | Population pharmacokinetics and target attainment of ciprofloxacin in critically ill patients Abstract Purpose To develop and validate a population pharmacokinetic model of ciprofloxacin intravenously in critically ill patients, and determine target attainment to provide guidance for more effective regimens. Methods No... |
PMC10223156 | core_pubmed_pmc | Application of Modelling and Simulation Approaches to Predict Pharmacokinetics of Therapeutic Monoclonal Antibodies in Pediatric Population | Application of Modelling and Simulation Approaches to Predict Pharmacokinetics of Therapeutic Monoclonal Antibodies in Pediatric Population Abstract Abstract Ethical regulations and limited paediatric participants are key challenges that contribute to a median delay of 6 years in paediatric mAb approval. To overcome th... |
PMC12895975 | core_pubmed_pmc | Evaluation of everolimus pharmacokinetic monitoring based on trough concentration and area under the blood concentration time curve in kidney transplantation | Evaluation of everolimus pharmacokinetic monitoring based on trough concentration and area under the blood concentration time curve in kidney transplantation Abstract Background Everolimus (EVR) is widely used in kidney transplantation; however, the optimal sampling time point for therapeutic drug monitoring and the re... |
PMC12168975 | core_pubmed_pmc | Drug Interaction Potential of Berberine Hydrochloride When Co-Administered with Tofacitinib and Filgotinib in Rats | Drug Interaction Potential of Berberine Hydrochloride When Co-Administered with Tofacitinib and Filgotinib in Rats Abstract Propose The co-treatment of ulcerative colitis with berberine hydrochloride (BBR), the Janus kinase(JAK) inhibitor Tofacitinib (TOFA), and Fligotinib (FIGA) is feasible and sophisticated in terms ... |
PMC12422601 | core_pubmed_pmc | The Effect of Age on Antipsychotic Serum Concentration in Males and Females: A Study Based on Therapeutic Drug Monitoring Data From 19,926 Patients | The Effect of Age on Antipsychotic Serum Concentration in Males and Females: A Study Based on Therapeutic Drug Monitoring Data From 19,926 Patients Abstract Supplemental Digital Content is Available in the Text. Key Words: antipsychotics, therapeutic drug monitoring, pharmacokinetics, aging Abstract Background: Antipsy... |
PMC8892078 | core_pubmed_pmc | Vitamin D Deficiency Impacts Exposure and Response of Pravastatin in Male Rats by Altering Hepatic OATPs | Vitamin D Deficiency Impacts Exposure and Response of Pravastatin in Male Rats by Altering Hepatic OATPs Abstract Abstract This study aimed to determine the effect of vitamin D (VD) deficiency on the efficacy and pharmacokinetics of pravastatin and clarify whether the effects are mediated by Organic anion-transporting ... |
PMC9291492 | core_pubmed_pmc | Exposure‐toxicity relationship of cabozantinib in patients with renal cell cancer and salivary gland cancer | Exposure‐toxicity relationship of cabozantinib in patients with renal cell cancer and salivary gland cancer Abstract Abstract Cabozantinib is registered in fixed 60 mg dose. However, 46% to 62% of patients in the registration studies needed a dose reduction due to toxicity. Improved clinical efficacy has been observed ... |
PMC5572334 | core_pubmed_pmc | Mechanistic Oral Absorption Modeling and Simulation for Formulation Development and Bioequivalence Evaluation: Report of an FDA Public Workshop | Mechanistic Oral Absorption Modeling and Simulation for Formulation Development and Bioequivalence Evaluation: Report of an FDA Public Workshop Abstract On May 19, 2016, the US Food and Drug Administration (FDA) hosted a public workshop, entitled “Mechanistic Oral Absorption Modeling and Simulation for Formulation Deve... |
PMC6647096 | core_pubmed_pmc | Genomic and epigenomic predictors of response to guadecitabine in relapsed/refractory acute myelogenous leukemia | Genomic and epigenomic predictors of response to guadecitabine in relapsed/refractory acute myelogenous leukemia Abstract Background Guadecitabine is a novel DNA methyltransferase (DNMT) inhibitor with improved pharmacokinetics and clinical activity in a subset of patients with relapsed/refractory acute myeloid leukemi... |
PMC9097221 | core_pubmed_pmc | A Case Report of Subcutaneously Injected Liposomal Cannabidiol Formulation Used as a Compassion Therapy for Pain Management in a Dog | A Case Report of Subcutaneously Injected Liposomal Cannabidiol Formulation Used as a Compassion Therapy for Pain Management in a Dog Abstract A 14-year-old intact mixed breed dog (26 kg) was submitted for a novel cannabidiol (CBD) analgesic treatment. The dog was cachectic and had a testicular neoplasia, hip and elbow ... |
PMC6221032 | core_pubmed_pmc | Extension Study of PF‐05280586, a Potential Rituximab Biosimilar, Versus Rituximab in Subjects With Active Rheumatoid Arthritis | Extension Study of PF‐05280586, a Potential Rituximab Biosimilar, Versus Rituximab in Subjects With Active Rheumatoid Arthritis Abstract Abstract Objective This extension study provided continued treatment to subjects with active rheumatoid arthritis who had participated for ≥16 weeks in a pharmacokinetic similarity st... |
PMC6741386 | core_pubmed_pmc | A Review of Samidorphan: A Novel Opioid Antagonist | A Review of Samidorphan: A Novel Opioid Antagonist Abstract Abstract Opioid modulators have been explored as a treatment option for psychiatric disorders, but their use has been limited due to their abuse potential. Samidorphan (SAM), a μ-opioid receptor antagonist, has gained interest due to its favorable pharmacokine... |
PMC11685975 | core_pubmed_pmc | Safety and tolerability of the M2 muscarinic acetylcholine receptor modulator BAY 2413555 in heart failure with reduced ejection fraction in the REMOTE-HF study | Safety and tolerability of the M2 muscarinic acetylcholine receptor modulator BAY 2413555 in heart failure with reduced ejection fraction in the REMOTE-HF study Abstract Abstract BAY 2413555 is a novel selective and reversible positive allosteric modulator of the type 2 muscarinic acetylcholine (M2) receptor, aimed at ... |
PMC9481493 | core_pubmed_pmc | Predicting Drug–Drug Interactions between Rifampicin and Ritonavir-Boosted Atazanavir Using PBPK Modelling | Predicting Drug–Drug Interactions between Rifampicin and Ritonavir-Boosted Atazanavir Using PBPK Modelling Abstract Abstract Objectives The aim of this study was to simulate the drug–drug interaction (DDI) between ritonavir-boosted atazanavir (ATV/r) and rifampicin (RIF) using physiologically based pharmacokinetic (PBP... |
PMC3616606 | core_pubmed_pmc | Accelerated drug release and clearance of PEGylated epirubicin liposomes following repeated injections: a new challenge for sequential low-dose chemotherapy | Accelerated drug release and clearance of PEGylated epirubicin liposomes following repeated injections: a new challenge for sequential low-dose chemotherapy Abstract Background Sequential low-dose chemotherapy has received great attention for its unique advantages in attenuating multidrug resistance of tumor cells. Nev... |
PMC10795653 | core_pubmed_pmc | Effectiveness of ALK inhibitors in treatment of CNS metastases in NSCLC patients | Effectiveness of ALK inhibitors in treatment of CNS metastases in NSCLC patients Abstract Abstract Metastases to the central nervous system (CNS) in patients with non-small cell lung cancer constitute an extremely difficult clinical problem, and their occurrence is associated with a poor prognosis. Due to the existence... |
PMC11726916 | core_pubmed_pmc | Asoprisnil as a Novel Ligand Interacting with Stress-Associated Glucocorticoid Receptor | Asoprisnil as a Novel Ligand Interacting with Stress-Associated Glucocorticoid Receptor Abstract Abstract Background/objective: The glucocorticoid receptor (GR) is critical in regulating cortisol production during stress. This makes it a key target for treating conditions associated with hypothalamic–pituitary–adrenal ... |
PMC7144379 | core_pubmed_pmc | Recent Advances in Berberine Inspired Anticancer Approaches: From Drug Combination to Novel Formulation Technology and Derivatization | Recent Advances in Berberine Inspired Anticancer Approaches: From Drug Combination to Novel Formulation Technology and Derivatization Abstract Abstract Berberine is multifunctional natural product with potential to treat diverse pathological conditions. Its broad-spectrum anticancer effect through direct effect on canc... |
PMC12199097 | core_pubmed_pmc | Oral paltusotine, a nonpeptide selective somatostatin receptor 2 agonist: Mass balance, absolute bioavailability and metabolism in healthy participants | Oral paltusotine, a nonpeptide selective somatostatin receptor 2 agonist: Mass balance, absolute bioavailability and metabolism in healthy participants Abstract Abstract Aims Paltusotine is a novel, nonpeptide, selective somatostatin receptor 2 agonist in development for the treatment of acromegaly and carcinoid syndro... |
PMC4886404 | core_pubmed_pmc | Comparative pharmacokinetics of fluralaner in dogs and cats following single topical or intravenous administration | Comparative pharmacokinetics of fluralaner in dogs and cats following single topical or intravenous administration Abstract Background Bravecto™ Chewable Tablets for Dogs, containing fluralaner as active ingredient, is an innovative treatment for flea and tick infestations that provides safe, rapid and long acting effi... |
PMC5931096 | core_pubmed_pmc | A Phase I study of the novel immunomodulatory agent PG545 (pixatimod) in subjects with advanced solid tumours | A Phase I study of the novel immunomodulatory agent PG545 (pixatimod) in subjects with advanced solid tumours Abstract Abstract Background PG545 (pixatimod) is a novel immunomodulatory agent, which has been demonstrated to stimulate innate immune responses against tumours in preclinical cancer models. Methods This Phas... |
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