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PMC11799998 | core_pubmed_pmc | Enhanced and Sustained Transdermal Delivery of Oxypurinol Using Thermosensitive Gel Combined with Polymeric Solid Microneedles | Enhanced and Sustained Transdermal Delivery of Oxypurinol Using Thermosensitive Gel Combined with Polymeric Solid Microneedles Abstract Abstract Gout is a pathological condition caused by monosodium urate crystal deposition in tissues. Allopurinol, the first-line therapy, inhibits xanthine oxidase but may be ineffectiv... |
PMC10853867 | core_pubmed_pmc | Efficacy, Safety, and Population Pharmacokinetics of MW032 Compared With Denosumab for Solid Tumor–Related Bone Metastases | Efficacy, Safety, and Population Pharmacokinetics of MW032 Compared With Denosumab for Solid Tumor–Related Bone Metastases Abstract Key Points Question Are the effects of a proposed denosumab biosimilar (MW032) equivalent to those of denosumab in the treatment of solid tumor–related bone metastases? Findings In this ra... |
PMC12381621 | core_pubmed_pmc | Metamizole induces voriconazole metabolism and results in subtherapeutic voriconazole concentrations | Metamizole induces voriconazole metabolism and results in subtherapeutic voriconazole concentrations Abstract Abstract Aims Voriconazole is extensively metabolized via cytochrome P450 (CYP) enzymes, predominantly CYP2C19 and CYP3A4. Drugs influencing the activity or expression of CYP enzymes can cause clinically releva... |
PMC8742647 | core_pubmed_pmc | Prediction of human pharmacokinetics for low‐clearance compounds using pharmacokinetic data from chimeric mice with humanized livers | Prediction of human pharmacokinetics for low‐clearance compounds using pharmacokinetic data from chimeric mice with humanized livers Abstract Abstract Development of low‐clearance (CL) compounds that are slowly metabolized is a major goal in the pharmaceutical industry. However, the pursuit of low intrinsic CL (CL int ... |
PMC11945821 | core_pubmed_pmc | Modulation of Peripheral Mast Cell and Brain Microglia Axis via Kinase Inhibition | Modulation of Peripheral Mast Cell and Brain Microglia Axis via Kinase Inhibition Abstract Background/Objectives: Kinase inhibition is a hot therapeutic strategy for several human diseases, including neurodegeneration. Tyrosine kinase c-KIT activates peripheral mast cells, while other kinases including Abelson (c-Abl) ... |
PMC12673543 | core_pubmed_pmc | Do the pharmacokinetics of statins explain psychiatric symptom improvement from adjunctive statin prescribing in severe mental illness? Three target trial emulation studies | Do the pharmacokinetics of statins explain psychiatric symptom improvement from adjunctive statin prescribing in severe mental illness? Three target trial emulation studies Abstract Abstract Background Evidence regarding the efficacy of adjunct statins to treat severe mental illness (SMI) is mixed. The varying pharmaco... |
PMC3517777 | core_pubmed_pmc | Phase I study of TP300 in patients with advanced solid tumors with pharmacokinetic, pharmacogenetic and pharmacodynamic analyses | Phase I study of TP300 in patients with advanced solid tumors with pharmacokinetic, pharmacogenetic and pharmacodynamic analyses Abstract Abstract Background A Phase I dose escalation first in man study assessed maximum tolerated dose (MTD), dose-limiting toxicity (DLT) and recommended Phase II dose of TP300, a water s... |
PMC8636649 | core_pubmed_pmc | Formulation of a rational dosage regimen of ceftiofur hydrochloride oily suspension by pharmacokinetic-pharmacodynamic (PK-PD) model for treatment of swine Streptococcus suis infection | Formulation of a rational dosage regimen of ceftiofur hydrochloride oily suspension by pharmacokinetic-pharmacodynamic (PK-PD) model for treatment of swine Streptococcus suis infection Abstract Abstract Background Our previously prepared ceftiofur (CEF) hydrochloride oily suspension shows potential wide applications fo... |
PMC11318014 | core_pubmed_pmc | Machine Learning ADME Models in Practice: Four Guidelines from a Successful Lead Optimization Case Study | Machine Learning ADME Models in Practice: Four Guidelines from a Successful Lead Optimization Case Study Abstract Abstract Optimization of the ADME properties and pharmacokinetic (PK) profile of compounds is one of the critical activities in any medicinal chemistry campaign to discover a future clinical candidate. Find... |
PMC3898920 | core_pubmed_pmc | Randomised Pharmacokinetic Trial of Rifabutin with Lopinavir/Ritonavir-Antiretroviral Therapy in Patients with HIV-Associated Tuberculosis in Vietnam | Randomised Pharmacokinetic Trial of Rifabutin with Lopinavir/Ritonavir-Antiretroviral Therapy in Patients with HIV-Associated Tuberculosis in Vietnam Abstract Background Rifampicin and protease inhibitors are difficult to use concomitantly in patients with HIV-associated tuberculosis because of drug-drug interactions. ... |
PMC6812819 | core_pubmed_pmc | A drug interaction study investigating the effect of Rifabutin on the pharmacokinetics of Maraviroc in healthy subjects | A drug interaction study investigating the effect of Rifabutin on the pharmacokinetics of Maraviroc in healthy subjects Abstract Effects of steady-state rifabutin on the pharmacokinetics of steady-state maraviroc were investigated in fourteen healthy adult female and male volunteers. Maraviroc 300 mg twice daily (BID) ... |
PMC4954842 | core_pubmed_pmc | Pharmacokinetics of mycophenolate sodium co-administered with tacrolimus in the first year after renal transplantation | Pharmacokinetics of mycophenolate sodium co-administered with tacrolimus in the first year after renal transplantation Abstract We assessed the relations between MPA, free MPA (fMPA) and MPA glucuronide (MPAG) pharmacokinetics and the clinical condition of renal transplant recipients treated with EC-MPS and tacrolimus ... |
PMC11101253 | core_pubmed_pmc | Pharmacokinetic Properties of Baitouweng Decoction in Bama Miniature Pigs: Implications for Clinical Application in Humans | Pharmacokinetic Properties of Baitouweng Decoction in Bama Miniature Pigs: Implications for Clinical Application in Humans Abstract Traditional Chinese medicine (TCM) serves as a significant adjunct to chemical treatment for chronic diseases. For instance, the administration of Baitouweng decoction (BTWD) has proven ef... |
PMC11279449 | core_pubmed_pmc | Determination of NAT2 Genotypes in a Cohort of Patients with Suspected TB in the State of Rio de Janeiro | Determination of NAT2 Genotypes in a Cohort of Patients with Suspected TB in the State of Rio de Janeiro Abstract Abstract The human N-acetyltransferase 2 enzyme, encoded by the NAT2 gene, plays an important role in the metabolism of isoniazid, the main drug used to treat tuberculosis. The interindividual variation in ... |
PMC7912650 | core_pubmed_pmc | Acute Pharmacological Effects of Oral and Intranasal Mephedrone: An Observational Study in Humans | Acute Pharmacological Effects of Oral and Intranasal Mephedrone: An Observational Study in Humans Abstract Abstract Mephedrone (4-methylmethcathinone) is a synthetic cathinone with psychostimulant properties which remains one of the most popular new psychoactive substances (NPS). It is frequently used orally and/or int... |
PMC10436260 | core_pubmed_pmc | Thiazolide Prodrug Esters and Derived Peptides: Synthesis and Activity | Thiazolide Prodrug Esters and Derived Peptides: Synthesis and Activity Abstract Abstract Amino acid ester prodrugs of the thiazolides, introduced to improve the pharmacokinetic parameters of the parent drugs, proved to be stable as their salts but were unstable at pH > 5. Although some of the instability was due to sim... |
PMC6849879 | core_pubmed_pmc | Pharmacokinetics of ferric bepectate—a new intravenous iron drug for treating iron deficiency | Pharmacokinetics of ferric bepectate—a new intravenous iron drug for treating iron deficiency Abstract Abstract IV iron is indicated in clinical conditions, where rapid anaemia alleviation and repletion of iron stores are required. The acute toxicity of IV iron is ascribed to the presence of labile iron in plasma. Thus... |
PMC11597693 | core_pubmed_pmc | Bempedoic Acid, the First-in-Class Oral ATP Citrate Lyase Inhibitor with Hypocholesterolemic Activity: Clinical Pharmacology and Drug–Drug Interactions | Bempedoic Acid, the First-in-Class Oral ATP Citrate Lyase Inhibitor with Hypocholesterolemic Activity: Clinical Pharmacology and Drug–Drug Interactions Abstract Abstract Bempedoic acid is a new drug that improves the control of cholesterol levels, either as monotherapy or in combination with existing lipid-lowering the... |
PMC10934259 | core_pubmed_pmc | Human Mitragynine and 7-Hydroxymitragynine Pharmacokinetics after Single and Multiple Daily Doses of Oral Encapsulated Dried Kratom Leaf Powder | Human Mitragynine and 7-Hydroxymitragynine Pharmacokinetics after Single and Multiple Daily Doses of Oral Encapsulated Dried Kratom Leaf Powder Abstract Abstract Kratom leaves, consumed by millions worldwide as tea or ground leaf powder, contain multiple alkaloids, with mitragynine being the most abundant and responsib... |
PMC9839390 | core_pubmed_pmc | Frailty as a Marker for the Plasma Concentrations of Direct Oral Anticoagulants in Older Patients: Results of an Exploratory Study | Frailty as a Marker for the Plasma Concentrations of Direct Oral Anticoagulants in Older Patients: Results of an Exploratory Study Abstract Background Frailty makes older adults vulnerable to adverse health outcomes and can modify pharmacokinetics and drug exposure. Objective We aimed to explore the relationship betwee... |
PMC4336271 | core_pubmed_pmc | Colistin for lung infection: an update | Colistin for lung infection: an update Abstract Abstract Increasing incidence of resistance of gram-negative bacteria against even newer antibiotic including carbapenem has generated interest in the old antibiotic colistin, which are being used as salvage therapy in the treatment of multidrug resistant infection. Colis... |
PMC6980506 | core_pubmed_pmc | Comparative pharmacokinetics and pharmacodynamics of the advanced Retinol-Binding Protein 4 antagonist in dog and cynomolgus monkey | Comparative pharmacokinetics and pharmacodynamics of the advanced Retinol-Binding Protein 4 antagonist in dog and cynomolgus monkey Abstract Abstract Accumulation of lipofuscin bisretinoids in the retina contributes to pathogenesis of macular degeneration. Retinol-Binding Protein 4 (RBP4) antagonists reduce serum retin... |
PMC9794587 | core_pubmed_pmc | Pharmacokinetics, distribution, metabolism, and excretion of body-protective compound 157, a potential drug for treating various wounds, in rats and dogs | Pharmacokinetics, distribution, metabolism, and excretion of body-protective compound 157, a potential drug for treating various wounds, in rats and dogs Abstract Abstract Body-protective compound (BPC) 157 demonstrates protective effects against damage to various organs and tissues. For future clinical applications, w... |
PMC12308096 | core_pubmed_pmc | Development of insulin and its pharmacology and perioperative use: a narrative review | Development of insulin and its pharmacology and perioperative use: a narrative review Abstract Summary Diabetes mellitus is characterised by an elevated blood glucose concentration. Over the last two decades, a plethora of new agents have emerged to help treat the condition, of which several classes of agent have been ... |
PMC8779763 | core_pubmed_pmc | An Adaptive Biosystems Engineering Approach towards Modeling the Soluble-to-Insoluble Phase Transition of Clofazimine | An Adaptive Biosystems Engineering Approach towards Modeling the Soluble-to-Insoluble Phase Transition of Clofazimine Abstract Clofazimine (CFZ) is a weakly basic, small-molecule antibiotic used for the treatment of mycobacterial infections including leprosy and multidrug-resistant tuberculosis. Upon prolonged oral adm... |
PMC12039762 | core_pubmed_pmc | Identification of novel amides and alkaloids as putative inhibitors of dopamine transporter for schizophrenia using computer-aided virtual screening | Identification of novel amides and alkaloids as putative inhibitors of dopamine transporter for schizophrenia using computer-aided virtual screening Abstract Schizophrenia is a complex psychiatric disorder marked by delusions, memory impairments, hallucinations, disorganized behavior, and severe cognitive deficits. Tar... |
PMC7911091 | core_pubmed_pmc | Rescuing the Last-Line Polymyxins: Achievements and Challenges | Rescuing the Last-Line Polymyxins: Achievements and Challenges Abstract Abstract Antibiotic resistance is a major global health challenge and, worryingly, several key Gram negative pathogens can become resistant to most currently available antibiotics. Polymyxins have been revived as a last-line therapeutic option for ... |
PMC11812116 | core_pubmed_pmc | A comprehensive insight of innovations and recent advancements in nanocarriers for nose-to-brain drug targeting | A comprehensive insight of innovations and recent advancements in nanocarriers for nose-to-brain drug targeting Abstract ABSTRACT Central Nervous System (CNS) disorders are the leading cause of illness and affect the everyday lives of people all around the globe and are predicted to increase tremendously in the upcomin... |
PMC7000849 | core_pubmed_pmc | Measured GFR by Utilizing Population Pharmacokinetic Methods to Determine Iohexol Clearance | Measured GFR by Utilizing Population Pharmacokinetic Methods to Determine Iohexol Clearance Abstract Abstract Introduction There is an increasing demand for accurately measured glomerular filtration rate (GFR). Iohexol serum clearance has become a new gold standard, but it is challenging when GFR is low and 24-hour sam... |
PMC6595360 | core_pubmed_pmc | Role of obinutuzumab exposure on clinical outcome of follicular lymphoma treated with first‐line immunochemotherapy | Role of obinutuzumab exposure on clinical outcome of follicular lymphoma treated with first‐line immunochemotherapy Abstract Abstract Aims Obinutuzumab (G) is a humanized type II, Fc‐glycoengineered anti‐CD20 monoclonal antibody used in various indications, including patients with previously untreated front‐line follic... |
PMC6386089 | core_pubmed_pmc | Integrated Assessment of the Clinical Performance of GalNAc 3 -Conjugated 2′- O -Methoxyethyl Chimeric Antisense Oligonucleotides: I. Human Volunteer Experience | Integrated Assessment of the Clinical Performance of GalNAc 3 -Conjugated 2′- O -Methoxyethyl Chimeric Antisense Oligonucleotides: I. Human Volunteer Experience Abstract Abstract Advances in medicinal chemistry have produced new chemical classes of antisense oligonucleotides (ASOs) with enhanced therapeutic properties.... |
PMC7007426 | core_pubmed_pmc | Pharmacokinetics and Target Attainment of Antibiotics in Critically Ill Children: A Systematic Review of Current Literature | Pharmacokinetics and Target Attainment of Antibiotics in Critically Ill Children: A Systematic Review of Current Literature Abstract Abstract Background Pharmacokinetics (PK) are severely altered in critically ill patients due to changes in volume of distribution (Vd) and/or drug clearance (Cl). This affects the target... |
PMC11748481 | core_pubmed_pmc | In vivo pharmacokinetic, pharmacodynamic and brain concentration comparison of fentanyl and para- fluorofentanyl in rats | In vivo pharmacokinetic, pharmacodynamic and brain concentration comparison of fentanyl and para- fluorofentanyl in rats Abstract Abstract In 2022, para- fluorofentanyl (pFF) rose to the 6th most reported drug and the most reported fentanyl analog in the United States according to the Drug Enforcement Administration (D... |
PMC5340837 | core_pubmed_pmc | Genotypes Affecting the Pharmacokinetics of Anticancer Drugs | Genotypes Affecting the Pharmacokinetics of Anticancer Drugs Abstract Cancer treatment is becoming more and more individually based as a result of the large inter-individual differences that exist in treatment outcome and toxicity when patients are treated using population-based drug doses. Polymorphisms in genes encod... |
PMC10703149 | core_pubmed_pmc | Prediction of trough concentration and ALK occupancy in plasma and cerebrospinal fluid using physiologically based pharmacokinetic modeling of crizotinib, alectinib, and lorlatinib | Prediction of trough concentration and ALK occupancy in plasma and cerebrospinal fluid using physiologically based pharmacokinetic modeling of crizotinib, alectinib, and lorlatinib Abstract Backgrounds: Brain metastases occur in approximately 30% of patients with non-small-cell lung cancer (NSCLC). Therefore, the free ... |
PMC10755910 | core_pubmed_pmc | Thrombopoietin-receptor agonists for adult patients with immune thrombocytopenia: a narrative review and an approach for managing patients fasting intermittently | Thrombopoietin-receptor agonists for adult patients with immune thrombocytopenia: a narrative review and an approach for managing patients fasting intermittently Abstract Abstract Introduction Thrombopoietin-receptor agonist (TPO-RAs) currently represent the state of art for treating immune thrombocytopenia. Their diff... |
PMC8733657 | core_pubmed_pmc | Physiologically Based Pharmacokinetic Modeling of Cefadroxil in Mouse, Rat, and Human to Predict Concentration–Time Profile at Infected Tissue | Physiologically Based Pharmacokinetic Modeling of Cefadroxil in Mouse, Rat, and Human to Predict Concentration–Time Profile at Infected Tissue Abstract Abstract The aim of this study was to develop physiologically based pharmacokinetic (PBPK) models capable of simulating cefadroxil concentrations in plasma and tissues ... |
PMC12724559 | core_pubmed_pmc | Discovery and Characterization of a Hydroxypyridone-3-carboxamide Analog as an Antiviral Lead against Orthopoxviruses | Discovery and Characterization of a Hydroxypyridone-3-carboxamide Analog as an Antiviral Lead against Orthopoxviruses Abstract Orthopoxviruses remain a persistent global health concern due to the ongoing circulation of mpox, the possibility of the re-emergence of smallpox, and the threats posed by many poxviruses that ... |
PMC9343794 | core_pubmed_pmc | Comparative Pharmacokinetics and Local Tolerance of Tenofovir Alafenamide (TAF) From Subcutaneous Implant in Rabbits, Dogs, and Macaques | Comparative Pharmacokinetics and Local Tolerance of Tenofovir Alafenamide (TAF) From Subcutaneous Implant in Rabbits, Dogs, and Macaques Abstract Abstract The administration of antiretrovirals (ARVs) for HIV pre-exposure prophylaxis (PrEP) is highly efficacious and may benefit from new long-acting (LA) drug delivery ap... |
PMC12567347 | core_pubmed_pmc | Angiotensin II/Angiotensin I Ratio as a New Pharmacodynamic Parameter for Population Modelling in Healthy Adults and Children with Heart Failure Treated with Enalapril | Angiotensin II/Angiotensin I Ratio as a New Pharmacodynamic Parameter for Population Modelling in Healthy Adults and Children with Heart Failure Treated with Enalapril Abstract Background/Objectives : Since 2023, enalapril orodispersible minitablets have been approved in Europe for paediatric heart failure from birth, ... |
PMC9123656 | core_pubmed_pmc | Safety, activity, and pharmacokinetics of camrelizumab in advanced Asian melanoma patients: a phase I study | Safety, activity, and pharmacokinetics of camrelizumab in advanced Asian melanoma patients: a phase I study Abstract Background Anti-programmed cell death receptor-1 (PD-1) monotherapy is the standard treatment for metastatic melanoma in current. Camrelizumab is a humanized IgG4 anti-PD-1 monoclonal antibody whose safe... |
PMC12843060 | core_pubmed_pmc | Unifying Phytochemistry, Analytics, and Target Prediction to Advance Dendropanax morbifera Bioactive Discovery | Unifying Phytochemistry, Analytics, and Target Prediction to Advance Dendropanax morbifera Bioactive Discovery Abstract Abstract Dendropanax morbifera (DM; “Hwangchil”) is an evergreen tree native to southern Korea and Jeju Island, traditionally used for detoxification, anti-inflammatory, immunomodulatory, and neuropro... |
PMC11597303 | core_pubmed_pmc | Cremastrae Pseudobulbus Pleiones Pseudobulbus (CPPP) Against Non-Small-Cell Lung Cancer: Elucidating Effective Ingredients and Mechanism of Action | Cremastrae Pseudobulbus Pleiones Pseudobulbus (CPPP) Against Non-Small-Cell Lung Cancer: Elucidating Effective Ingredients and Mechanism of Action Abstract Abstract Cremastrae Pseudobulbus Pleiones Pseudobulbus (CPPP) is derived from the dried pseudobulb of the orchid family plants Cremastra appendiculata (D.Don) Makin... |
PMC10892549 | core_pubmed_pmc | Applications of Machine Learning (ML) and Mathematical Modeling (MM) in Healthcare with Special Focus on Cancer Prognosis and Anticancer Therapy: Current Status and Challenges | Applications of Machine Learning (ML) and Mathematical Modeling (MM) in Healthcare with Special Focus on Cancer Prognosis and Anticancer Therapy: Current Status and Challenges Abstract Abstract The use of data-driven high-throughput analytical techniques, which has given rise to computational oncology, is undisputed. T... |
PMC5192992 | core_pubmed_pmc | A Philosophical Framework for Integrating Systems Pharmacology Models Into Pharmacometrics | A Philosophical Framework for Integrating Systems Pharmacology Models Into Pharmacometrics Abstract The framework for systems pharmacology style models does not naturally sit with the usual scientific dogma of parsimony and falsifiability based on deductive reasoning. This does not invalidate the importance or need for... |
PMC10879372 | core_pubmed_pmc | Generative artificial intelligence in drug discovery: basic framework, recent advances, challenges, and opportunities | Generative artificial intelligence in drug discovery: basic framework, recent advances, challenges, and opportunities Abstract There are two main ways to discover or design small drug molecules. The first involves fine-tuning existing molecules or commercially successful drugs through quantitative structure-activity re... |
PMC10141152 | core_pubmed_pmc | Pharmacotherapy for Pulmonary Hypertension in Infants with Bronchopulmonary Dysplasia: Past, Present, and Future | Pharmacotherapy for Pulmonary Hypertension in Infants with Bronchopulmonary Dysplasia: Past, Present, and Future Abstract Approximately 8–42% of premature infants with chronic lung disease of prematurity, bronchopulmonary dysplasia (BPD), develop pulmonary hypertension (PH). Infants with BPD-PH carry alarmingly high mo... |
PMC4724690 | core_pubmed_pmc | Pharmacokinetic study of gallocatechin-7-gallate from Pithecellobium clypearia Benth. in rats | Pharmacokinetic study of gallocatechin-7-gallate from Pithecellobium clypearia Benth. in rats Abstract The pharmacokinetic profile of gallocatechin-7-gallate (J10688) was studied in rats after intravenous administration. Male and female Sprague-Dawley (SD) rats received 1, 3, and 10 mg/kg (i.v.) of J10688 and plasma dr... |
PMC4559169 | core_pubmed_pmc | Nonlinear mixed-effects modelling for single cell estimation: when, why, and how to use it | Nonlinear mixed-effects modelling for single cell estimation: when, why, and how to use it Abstract Background Studies of cell-to-cell variation have in recent years grown in interest, due to improved bioanalytical techniques which facilitates determination of small changes with high uncertainty. Like much high-quality... |
PMC12769531 | core_pubmed_pmc | Computational identification of Moracin G and Isolonchocarpin as potent MELK inhibitors for anticancer drug discovery | Computational identification of Moracin G and Isolonchocarpin as potent MELK inhibitors for anticancer drug discovery Abstract Abstract Maternal embryonic leucine zipper kinase (MELK) is a promising therapeutic target in cancer due to its overexpression in aggressive tumors and role in cell survival, proliferation, and... |
PMC11443510 | core_pubmed_pmc | Pharmacokinetics and thermal anti-nociceptive effects of oral morphine in horses | Pharmacokinetics and thermal anti-nociceptive effects of oral morphine in horses Abstract Introduction Morphine is an effective analgesic in horses, however, IV administration at therapeutic doses has been shown to produce dose-dependent neuroexcitation and unwanted gastrointestinal effects. The analgesic effects of mo... |
PMC6542439 | core_pubmed_pmc | Interventional cohort study of prolonged use (>72 hours) of paracetamol in neonates: protocol of the PARASHUTE study | Interventional cohort study of prolonged use (>72 hours) of paracetamol in neonates: protocol of the PARASHUTE study Abstract Abstract Introduction Anticipated or actual pain in neonates results in use of paracetamol for prolonged pain relief in many neonatal intensive care units. Clinical trials examining safety of pa... |
PMC12144993 | core_pubmed_pmc | Imaging the impact of sex and age on OATP function in humans: Consequences for whole-body pharmacokinetics and liver exposure | Imaging the impact of sex and age on OATP function in humans: Consequences for whole-body pharmacokinetics and liver exposure Abstract Organic anion-transporting polypeptides (OATP) transporter function, which mediates many drugs' liver uptake, was investigated as a molecular determinant of pharmacokinetic variability.... |
PMC10586506 | core_pubmed_pmc | Goldenseal-Mediated Inhibition of Intestinal Uptake Transporters Decreases Metformin Systemic Exposure in Mice | Goldenseal-Mediated Inhibition of Intestinal Uptake Transporters Decreases Metformin Systemic Exposure in Mice Abstract Abstract Goldenseal is a perennial plant native to eastern North America. A recent clinical study reported goldenseal decreased metformin C max and area under the blood concentration versus time curve... |
PMC9939223 | core_pubmed_pmc | Influence of the skeletal muscle index on pharmacokinetics and toxicity of fluorouracil | Influence of the skeletal muscle index on pharmacokinetics and toxicity of fluorouracil Abstract Abstract Background The body composition of patients has been associated with tolerability and effectiveness of anticancer therapy. This study aimed to assess the influence of the skeletal muscle index (SMI) on the pharmaco... |
PMC5788204 | core_pubmed_pmc | Chirality of Modern Antidepressants: An Overview | Chirality of Modern Antidepressants: An Overview Abstract Abstract The majority of modern antidepressants (selective serotonin reuptake inhibitors and selective serotonin and norepinephrine reuptake inhibitors) have one or two centers of asymmetry in their structure; resulting in the formation of enantiomers which may ... |
PMC11270311 | core_pubmed_pmc | Inter-Antibody Variability in the Clinical Pharmacokinetics of Monoclonal Antibodies Characterized Using Population Physiologically Based Pharmacokinetic Modeling | Inter-Antibody Variability in the Clinical Pharmacokinetics of Monoclonal Antibodies Characterized Using Population Physiologically Based Pharmacokinetic Modeling Abstract The objective of this work was to develop a population physiologically based pharmacokinetic (popPBPK) model to characterize the variability in the ... |
PMC8417561 | core_pubmed_pmc | Purification of Modified Therapeutic Proteins Available on the Market: An Analysis of Chromatography-Based Strategies | Purification of Modified Therapeutic Proteins Available on the Market: An Analysis of Chromatography-Based Strategies Abstract Proteins, which have inherent biorecognition properties, have long been used as therapeutic agents for the treatment of a wide variety of clinical indications. Protein modification through cova... |
PMC7583190 | core_pubmed_pmc | Pharmacodynamic modeling of synergistic birinapant/paclitaxel interactions in pancreatic cancer cells | Pharmacodynamic modeling of synergistic birinapant/paclitaxel interactions in pancreatic cancer cells Abstract Abstract Background For most patients, pancreatic adenocarcinoma responds poorly to treatment, and novel therapeutic approaches are needed. Standard-of-care paclitaxel (PTX), combined with birinapant (BRP), a ... |
PMC12061515 | core_pubmed_pmc | Comparison of Adverse Events Among Angiotensin Receptor Blockers in Hypertension Using the United States Food and Drug Administration Adverse Event Reporting System | Comparison of Adverse Events Among Angiotensin Receptor Blockers in Hypertension Using the United States Food and Drug Administration Adverse Event Reporting System Abstract Background Angiotensin receptor blockers (ARBs) are pivotal in hypertension management. Despite sharing a common mechanism of blocking angiotensin... |
PMC7311957 | core_pubmed_pmc | Pharmacogenetics in Model-Based Optimization of Bevacizumab Therapy for Metastatic Colorectal Cancer | Pharmacogenetics in Model-Based Optimization of Bevacizumab Therapy for Metastatic Colorectal Cancer Abstract Vascular endothelial growth factor A (VEGF-A) and intercellular adhesion molecule 1 (ICAM-1) are significant regulators of angiogenesis, an important biological process involved in carcinogenesis. Bevacizumab, ... |
PMC12398292 | core_pubmed_pmc | Population Pharmacokinetic Modeling Analysis of ASC10, a Novel Antiviral Agent Targeted COVID-19, in Chinese Healthy Subjects | Population Pharmacokinetic Modeling Analysis of ASC10, a Novel Antiviral Agent Targeted COVID-19, in Chinese Healthy Subjects Abstract Background ASC10, an oral double prodrug of the antiviral ribonucleoside analog ASC10-A (also referred to as NHC), is currently in clinical trials for the treatment of COVID-19. Upon ad... |
PMC4498297 | core_pubmed_pmc | Pharmacokinetics of anti-TB drugs in Malawian children: reconsidering the role of ethambutol | Pharmacokinetics of anti-TB drugs in Malawian children: reconsidering the role of ethambutol Abstract Abstract Background Current guidelines for dosing of anti-TB drugs in children advocate higher doses for rifampicin and isoniazid despite limited availability of paediatric data on the pharmacokinetics of these drugs, ... |
PMC7533162 | core_pubmed_pmc | Predicting human pharmacokinetics from preclinical data: absorption | Predicting human pharmacokinetics from preclinical data: absorption Abstract Abstract Predicting the rate and extent of oral absorption of drugs in humans has been a challenging task for new drug researchers. This tutorial reviews in vitro and PBPK methods reported in the past decades that are widely applied to predict... |
PMC11944388 | core_pubmed_pmc | Physiologically Based Biopharmaceutics Model of Apixaban for Biopharmaceutics Risk Assessment | Physiologically Based Biopharmaceutics Model of Apixaban for Biopharmaceutics Risk Assessment Abstract Background/Objectives: This study applies a Physiologically Based Biopharmaceutics Modeling (PBBM) framework to predict the bioavailability (BA) and bioequivalence (BE) of apixaban, a borderline BCS Class III/IV drug.... |
PMC4980723 | core_pubmed_pmc | Acid reducing agents to neonates – lack of evidence and guidelines | Acid reducing agents to neonates – lack of evidence and guidelines Abstract Objective The aim of this retrospective study was to investigate the clinical practice, i.e. the frequency of use and the treatment strategies, for acid reducing drugs to neonates in a Swedish hospital. Methods Retrospective reviews of charts a... |
PMC7970346 | core_pubmed_pmc | Analysis of Antidepressant Activity of Huang-Lian Jie-Du Decoction Through Network Pharmacology and Metabolomics | Analysis of Antidepressant Activity of Huang-Lian Jie-Du Decoction Through Network Pharmacology and Metabolomics Abstract Abstract Depressive disorder is a common mental disorder characterized by depressed mood and loss of interest or pleasure. As the Herbal medicines are mainly used as complementary and alternative th... |
PMC8520755 | core_pubmed_pmc | A hybrid machine learning/pharmacokinetic approach outperforms maximum a posteriori Bayesian estimation by selectively flattening model priors | A hybrid machine learning/pharmacokinetic approach outperforms maximum a posteriori Bayesian estimation by selectively flattening model priors Abstract Abstract Model‐informed precision dosing (MIPD) approaches typically apply maximum a posteriori (MAP) Bayesian estimation to determine individual pharmacokinetic (PK) p... |
PMC12361874 | core_pubmed_pmc | Common Food Additives Inhibit Carbonic Anhydrase Activity | Common Food Additives Inhibit Carbonic Anhydrase Activity Abstract ABSTRACT Few studies about the effects of food additives on human enzymes exist. The effects of 20 food additives (12 colorants, 2 antioxidants, 3 sweeteners, 2 preservatives, and 1 acidity regulator) on bovine carbonic anhydrase (bCA) and especially hu... |
PMC7986165 | core_pubmed_pmc | Perampanel and pregnancy | Perampanel and pregnancy Abstract Abstract Objective The objective was to summarize pregnancy and fetal/postnatal outcomes following maternal perampanel exposure using preclinical and clinical data, and to use physiologically based pharmacokinetic (PBPK) modeling to improve understanding of perampanel pharmacokinetics ... |
PMC3961303 | core_pubmed_pmc | A Comparative Pharmacodynamic Study of Ticagrelor versus Clopidogrel and Ticagrelor in Patients Undergoing Primary Percutaneous Coronary Intervention: The CAPITAL RELOAD Study | A Comparative Pharmacodynamic Study of Ticagrelor versus Clopidogrel and Ticagrelor in Patients Undergoing Primary Percutaneous Coronary Intervention: The CAPITAL RELOAD Study Abstract Abstract Background In patients undergoing primary percutaneous coronary intervention (PPCI) ticagrelor is superior to clopidogrel in r... |
PMC12199113 | core_pubmed_pmc | Variability in intestinal drug metabolizing enzymes and transporters in Crohn's disease and potential impact on oral drug absorption | Variability in intestinal drug metabolizing enzymes and transporters in Crohn's disease and potential impact on oral drug absorption Abstract Abstract Aims The aim of study was to generate quantitative data on the abundance of drug‐metabolizing enzymes and transporters (DMETs) in inflamed and non‐inflamed Crohn's disea... |
PMC3603470 | core_pubmed_pmc | Pharmacokinetic–Pharmacodynamic Modeling of Severity Levels of Extrapyramidal Side Effects With Markov Elements | Pharmacokinetic–Pharmacodynamic Modeling of Severity Levels of Extrapyramidal Side Effects With Markov Elements Abstract Abstract A major problem in the treatment of schizophrenic patients with current antipsychotic drugs, mainly acting as dopamine-2 receptor antagonists, is the occurrence of side effects such as extra... |
PMC12756435 | core_pubmed_pmc | Nonclinical evaluation of HS630, a proposed biosimilar of trastuzumab emtansine: affinity, pharmacokinetics, and immunogenicity | Nonclinical evaluation of HS630, a proposed biosimilar of trastuzumab emtansine: affinity, pharmacokinetics, and immunogenicity Abstract Abstract Objective The aim of this study is to evaluate the similarity of affinity, pharmacokinetics, and immunogenicity shared by HS630 and trastuzumab emtansine (T-DM1). Methods In ... |
PMC12825016 | core_pubmed_pmc | Prediction of silica nanoparticle biodistribution using a calibrated physiologically based model: Unbound fraction and elimination rate constants for the kidneys and phagocytosis identified as major determinants | Prediction of silica nanoparticle biodistribution using a calibrated physiologically based model: Unbound fraction and elimination rate constants for the kidneys and phagocytosis identified as major determinants Abstract Abstract Objectives: This study aimed to develop a minimal physiologically based pharmacokinetic (m... |
PMC9796123 | core_pubmed_pmc | Pharmacokinetics and anti‐nausea effects of intravenous ondansetron in hospitalized dogs exhibiting clinical signs of nausea | Pharmacokinetics and anti‐nausea effects of intravenous ondansetron in hospitalized dogs exhibiting clinical signs of nausea Abstract Abstract The purpose of this study was to evaluate the pharmacokinetics of intravenous (IV) ondansetron in a population of hospitalized dogs exhibiting clinical signs of nausea. The caus... |
PMC8689140 | core_pubmed_pmc | (+)-9-Trifluoroethoxy-α-Dihydrotetrabenazine as a Highly Potent Vesicular Monoamine Transporter 2 Inhibitor for Tardive Dyskinesia | (+)-9-Trifluoroethoxy-α-Dihydrotetrabenazine as a Highly Potent Vesicular Monoamine Transporter 2 Inhibitor for Tardive Dyskinesia Abstract Valbenazine and deutetrabenazine are the only two therapeutic drugs approved for tardive dyskinesia based on blocking the action of vesicular monoamine transporter 2 (VMAT2). But t... |
PMC12217460 | core_pubmed_pmc | Pharmacokinetics of nikkomycin Z following multiple doses in healthy subjects | Pharmacokinetics of nikkomycin Z following multiple doses in healthy subjects Abstract ABSTRACT Nikkomycin Z is an investigational antifungal agent that inhibits chitin synthesis. The drug shows promise against endemic fungi such as Coccidioides spp. The purpose of this study was to determine the pharmacokinetics and s... |
PMC10100020 | core_pubmed_pmc | Phase 1 Evaluation of Elezanumab ( Anti–Repulsive Guidance Molecule A Monoclonal Antibody) in Healthy and Multiple Sclerosis Participants | Phase 1 Evaluation of Elezanumab ( Anti–Repulsive Guidance Molecule A Monoclonal Antibody) in Healthy and Multiple Sclerosis Participants Abstract Objective This study was undertaken to describe the safety, tolerability, pharmacokinetics, and immunogenicity of elezanumab (ABT‐555), a fully human monoclonal antibody (mA... |
PMC4155868 | core_pubmed_pmc | Testosterone restoration using enclomiphene citrate in men with secondary hypogonadism: a pharmacodynamic and pharmacokinetic study | Testosterone restoration using enclomiphene citrate in men with secondary hypogonadism: a pharmacodynamic and pharmacokinetic study Abstract Objectives To determine the pharmacodynamic profile of serum total testosterone and luteinizing hormone (LH) levels in men with secondary hypogonadism after initial and chronic da... |
PMC8504826 | core_pubmed_pmc | Particle size affects pharmacokinetics of milled oxycodone hydrochloride tablet products following nasal insufflation in nondependent, recreational opioid users | Particle size affects pharmacokinetics of milled oxycodone hydrochloride tablet products following nasal insufflation in nondependent, recreational opioid users Abstract Abstract This study assessed the impact of product particle sizes (fine: 106–500 µm; coarse: 500–1000 µm) on oxycodone pharmacokinetics (PK) following... |
PMC12649304 | core_pubmed_pmc | Establishing a Quantitative Framework for Combined Oral Contraceptives: Evaluating the Impact of Drug–Drug Interactions on Exposure and Clinical (Surrogate) Efficacy Endpoints | Establishing a Quantitative Framework for Combined Oral Contraceptives: Evaluating the Impact of Drug–Drug Interactions on Exposure and Clinical (Surrogate) Efficacy Endpoints Abstract Abstract According to the FDA Guidance for Industry on Clinical Drug Interaction (DDI) Studies with Combined Oral Contraceptives (COCs)... |
PMC9637427 | core_pubmed_pmc | Phase 1 First-in-Human Dose Escalation and Dose Expansion Study of KLS-1 (64Zinc Aspartate) in Patients With Cancer and Neurodegenerative Diseases | Phase 1 First-in-Human Dose Escalation and Dose Expansion Study of KLS-1 (64Zinc Aspartate) in Patients With Cancer and Neurodegenerative Diseases Abstract Background KLS-1 is zinc (Zn) aspartate enriched with isotope 64 Zn to 99.2% mass fraction of total zinc. KLS-1 is intended as a novel therapeutic approach for pati... |
PMC8742698 | core_pubmed_pmc | Translational Modeling of Chloroquine and Hydroxychloroquine Dosimetry in Human Airways for Treating Viral Respiratory Infections | Translational Modeling of Chloroquine and Hydroxychloroquine Dosimetry in Human Airways for Treating Viral Respiratory Infections Abstract Purpose Chloroquine and hydroxychloroquine are effective against respiratory viruses in vitro . However, they lack antiviral efficacy upon oral administration. Translation of in vit... |
PMC11620484 | core_pubmed_pmc | Long-acting cabotegravir pharmacokinetics with and without oral lead-in for HIV PrEP | Long-acting cabotegravir pharmacokinetics with and without oral lead-in for HIV PrEP Abstract ABSTRACT Long-acting cabotegravir is approved for pre-exposure prophylaxis and combination HIV treatment, both initiated with optional short-term oral lead-in (OLI). We evaluated the impact of OLI on long-acting cabotegravir p... |
PMC9509332 | core_pubmed_pmc | Central nervous system effects of TAK-653, an investigational alpha-amino-3-hydroxy-5-methyl-4-isoxazole receptor (AMPAR) positive allosteric modulator in healthy volunteers | Central nervous system effects of TAK-653, an investigational alpha-amino-3-hydroxy-5-methyl-4-isoxazole receptor (AMPAR) positive allosteric modulator in healthy volunteers Abstract Abstract TAK-653 is a novel AMPA receptor positive allosteric modulator in clinical development for the treatment of major depressive dis... |
PMC9073947 | core_pubmed_pmc | Estimation of Fetal-to-Maternal Unbound Steady-State Plasma Concentration Ratio of P-Glycoprotein and/or Breast Cancer Resistance Protein Substrate Drugs Using a Maternal-Fetal Physiologically Based Pharmacokinetic Model | Estimation of Fetal-to-Maternal Unbound Steady-State Plasma Concentration Ratio of P-Glycoprotein and/or Breast Cancer Resistance Protein Substrate Drugs Using a Maternal-Fetal Physiologically Based Pharmacokinetic Model Abstract Pregnant women are frequently prescribed drugs to treat chronic diseases such as human imm... |
PMC8311335 | core_pubmed_pmc | CX-072 (pacmilimab), a Probody ® PD-L1 inhibitor, in advanced or recurrent solid tumors (PROCLAIM-CX-072): an open-label dose-finding and first-in-human study | CX-072 (pacmilimab), a Probody ® PD-L1 inhibitor, in advanced or recurrent solid tumors (PROCLAIM-CX-072): an open-label dose-finding and first-in-human study Abstract Abstract Background Probody ® therapeutics are antibody prodrugs that are activated in the tumor microenvironment by tumor-associated proteases, thereby... |
PMC7538292 | core_pubmed_pmc | Cognitive Function and Urologic Medications for Lower Urinary Tract Symptoms | Cognitive Function and Urologic Medications for Lower Urinary Tract Symptoms Abstract Special considerations should be made when selecting medications for the treatment of lower urinary tract symptoms (LUTS) in older patients especially those over 65 years old. This review summarizes the relationship between current tr... |
PMC11764671 | core_pubmed_pmc | Synthetic GPR84 Agonists in Colorectal Cancer: Effective in THP-1 Cells but Ineffective in BMDMs and MC38 Mouse Tumor Models | Synthetic GPR84 Agonists in Colorectal Cancer: Effective in THP-1 Cells but Ineffective in BMDMs and MC38 Mouse Tumor Models Abstract Abstract Tumor-associated macrophages (TAMs) in the colorectal cancer (CRC) microenvironment promote tumor progression but can be reprogrammed into a pro-inflammatory state with anti-can... |
PMC11756511 | core_pubmed_pmc | Integrated SegFlow, µSIA, and UPLC for Online Sialic Acid Quantitation of Glycoproteins Directly from Bioreactors | Integrated SegFlow, µSIA, and UPLC for Online Sialic Acid Quantitation of Glycoproteins Directly from Bioreactors Abstract ABSTRACT This study emphasizes the critical importance of closely monitoring and controlling the sialic acid content in therapeutic glycoproteins, including EPO, interferon‐γ, Orencia, Enbrel, and ... |
PMC4418820 | core_pubmed_pmc | Quantitative Analysis of the Enhanced Permeation and Retention (EPR) Effect | Quantitative Analysis of the Enhanced Permeation and Retention (EPR) Effect Abstract Tumor vasculature is characterized by a variety of abnormalities including irregular architecture, poor lymphatic drainage, and the upregulation of factors that increase the paracellular permeability. The increased permeability is impo... |
PMC8816611 | core_pubmed_pmc | Performance Evaluation of Montelukast Pediatric Formulations: Part II — a PBPK Modelling Approach | Performance Evaluation of Montelukast Pediatric Formulations: Part II — a PBPK Modelling Approach Abstract This study aimed to build a physiologically based pharmacokinetic (PBPK) model coupled with age-appropriate in vitro dissolution data to describe drug performance in adults and pediatric patients. Montelukast sodi... |
PMC10850047 | core_pubmed_pmc | Exploring the impact of PEGylation on pharmacokinetics: a size-dependent effect of polyethylene glycol on prostate-specific membrane antigen inhibitors | Exploring the impact of PEGylation on pharmacokinetics: a size-dependent effect of polyethylene glycol on prostate-specific membrane antigen inhibitors Abstract Background Prostate cancer is the second most frequent cancer and the fifth leading cause of cancer-related deaths in men. Prostate-specific membrane antigen (... |
PMC10042772 | core_pubmed_pmc | FT-6876, a Potent and Selective Inhibitor of CBP/p300, is Active in Preclinical Models of Androgen Receptor-Positive Breast Cancer | FT-6876, a Potent and Selective Inhibitor of CBP/p300, is Active in Preclinical Models of Androgen Receptor-Positive Breast Cancer Abstract Abstract Background Patients with triple-negative breast cancer (TNBC) expressing the androgen receptor (AR) respond poorly to neoadjuvant chemotherapy, although AR antagonists hav... |
PMC9428119 | core_pubmed_pmc | Screening, molecular simulation & in silico kinetics of virtually designed covid-19 main protease inhibitors | Screening, molecular simulation & in silico kinetics of virtually designed covid-19 main protease inhibitors Abstract Abstract Coronavirus (covid-19) infection is considered to be deadliest ever pandemic experienced by the human being. It has very badly affected the socio-economic health of human and stuck the scientif... |
PMC12962394 | core_pubmed_pmc | Open Systems Pharmacology Community Conference ( OSP ‐ CC ) Proceedings 2025 | Open Systems Pharmacology Community Conference ( OSP ‐ CC ) Proceedings 2025 Abstract ABSTRACT Developed at Bayer Technology Services, PK‐Sim and MoBi transitioned into the Open Systems Pharmacology (OSP) Suite, released as free open‐source software in 2017. An active community with stakeholders from academia, industri... |
PMC10574807 | core_pubmed_pmc | Polymer-Based Nanoparticles as Drug Delivery Systems for Purines of Established Importance in Medicine † | Polymer-Based Nanoparticles as Drug Delivery Systems for Purines of Established Importance in Medicine † Abstract Abstract Many purine derivatives are active pharmaceutical ingredients of significant importance in the therapy of autoimmune diseases, cancers, and viral infections. In many cases, their medical use is lim... |
PMC9698804 | core_pubmed_pmc | Formulation Characterization and Pharmacokinetic Evaluation of Amorphous Solid Dispersions of Dasatinib | Formulation Characterization and Pharmacokinetic Evaluation of Amorphous Solid Dispersions of Dasatinib Abstract Abstract The aim of this study was to improve the physicochemical properties and oral bioavailability of dasatinib (DST) by the amorphous solid dispersion (ASD) approach using cellulose acetate butyrate (CAB... |
PMC7784934 | core_pubmed_pmc | In silico docking and comparative ADMET profile of different glycogen synthase kinase 3 beta inhibitors as the potential leads for the development of anti-Alzheimer drug therapy | In silico docking and comparative ADMET profile of different glycogen synthase kinase 3 beta inhibitors as the potential leads for the development of anti-Alzheimer drug therapy Abstract Abstract Glycogen synthase kinase 3 beta (GSK3 β) plays a key role in pathologic hyper phosphorylation of tau and plays an important ... |
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