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PMC3339338 | core_pubmed_pmc | An Overview of the Evidence and Mechanisms of Herb–Drug Interactions | An Overview of the Evidence and Mechanisms of Herb–Drug Interactions Abstract Despite the lack of sufficient information on the safety of herbal products, their use as alternative and/or complementary medicine is globally popular. There is also an increasing interest in medicinal herbs as precursor for pharmacological ... |
PMC12313452 | core_pubmed_pmc | Development of a ribavirin dosing regimen in transplant recipients with chronic hepatitis E virus infection: a population pharmacokinetic and -dynamic model | Development of a ribavirin dosing regimen in transplant recipients with chronic hepatitis E virus infection: a population pharmacokinetic and -dynamic model Abstract Abstract Objectives The optimal ribavirin dosing regimen for the treatment of chronic hepatitis E virus (HEV) infection in solid organ transplant (SOT) is... |
PMC9800278 | core_pubmed_pmc | Whole-body CD8 + T cell visualization before and during cancer immunotherapy: a phase 1/2 trial | Whole-body CD8 + T cell visualization before and during cancer immunotherapy: a phase 1/2 trial Abstract Abstract Immune checkpoint inhibitors (ICIs), by reinvigorating CD8 + T cell mediated immunity, have revolutionized cancer therapy. Yet, the systemic CD8 + T cell distribution, a potential biomarker of ICI response,... |
PMC5339274 | core_pubmed_pmc | Advantages of the Silkworm As an Animal Model for Developing Novel Antimicrobial Agents | Advantages of the Silkworm As an Animal Model for Developing Novel Antimicrobial Agents Abstract Abstract The demand for novel antibiotics to combat the global spread of multi drug-resistant pathogens continues to grow. Pathogenic bacteria and fungi that cause fatal human infections can also kill silkworms and the infe... |
PMC3753171 | core_pubmed_pmc | Bioequivalence study of two formulations of candesartan cilexetil tablet in healthy subjects under fasting conditions | Bioequivalence study of two formulations of candesartan cilexetil tablet in healthy subjects under fasting conditions Abstract Introduction The present study was conducted to compare the bioavailability of two candesartan cilexetil 16 mg tablet formulations (test and reference formulations). Materials and methods This ... |
PMC4337252 | core_pubmed_pmc | Using a Systems Pharmacology Approach to Study the Effect of Statins on the Early Stage of Atherosclerosis in Humans | Using a Systems Pharmacology Approach to Study the Effect of Statins on the Early Stage of Atherosclerosis in Humans Abstract Abstract More than 100,000 people have participated in controlled trials of statins (lowering cholesterol drugs) since the introduction of lovastatin in the 1980s. Meta-analyses of this data hav... |
PMC9231748 | core_pubmed_pmc | Pharmacokinetics and bioequivalence of two imidocarb formulations in cattle after subcutaneous injection | Pharmacokinetics and bioequivalence of two imidocarb formulations in cattle after subcutaneous injection Abstract Abstract Imidocarb (IMD) is commonly used for treatment of eperythrozoon, babesia, piroplasma and trypanosoma in animals, but there are few studies on its pharmacokinetics in cattle. The purpose of this stu... |
PMC11233438 | core_pubmed_pmc | Pharmacokinetic profile of phenytoin in dried blood spot with high-performance liquid chromatography—photodiode array | Pharmacokinetic profile of phenytoin in dried blood spot with high-performance liquid chromatography—photodiode array Abstract Abstract Phenytoin is a first-line antiepileptic drug with narrow therapeutic range and follows non-linear pharmacokinetics. Pharmacokinetics of phenytoin have been studied in plasma matrix bef... |
PMC11343829 | core_pubmed_pmc | Population Pharmacokinetics and Target Attainment of Allopurinol and Oxypurinol Before, During, and After Cardiac Surgery with Cardiopulmonary Bypass in Neonates with Critical Congenital Heart Disease | Population Pharmacokinetics and Target Attainment of Allopurinol and Oxypurinol Before, During, and After Cardiac Surgery with Cardiopulmonary Bypass in Neonates with Critical Congenital Heart Disease Abstract Abstract Background The CRUCIAL trial (NCT04217421) is investigating the effect of postnatal and perioperative... |
PMC10580085 | core_pubmed_pmc | Exposure-response analyses of efzofitimod in patients with pulmonary sarcoidosis | Exposure-response analyses of efzofitimod in patients with pulmonary sarcoidosis Abstract Abstract Background: Preliminary evidence for efficacy in pulmonary sarcoidosis has been shown for efzofitimod. Here we present supportive evidence of efficacy based on an exposure-response analysis. Methods: Data from two studies... |
PMC8607079 | core_pubmed_pmc | Monitoring Of High-Dose Methotrexate (Mtx)-Related Toxicity and Mtx Levels in Children with Acute Lymphoblastic Leukemia: A Pilot-Study in Indonesia | Monitoring Of High-Dose Methotrexate (Mtx)-Related Toxicity and Mtx Levels in Children with Acute Lymphoblastic Leukemia: A Pilot-Study in Indonesia Abstract The administration of high-dose methotrexate (HD-MTX) requires an accurate monitoring of blood MTX levels to determine the regimen of leucovorin rescue and urine ... |
PMC11509402 | core_pubmed_pmc | Metabolite Measurement in Index Substrate Drug Interaction Studies: A Review of the Literature and Recent New Drug Application Reviews | Metabolite Measurement in Index Substrate Drug Interaction Studies: A Review of the Literature and Recent New Drug Application Reviews Abstract Background/Objectives: Index substrates are used to understand the processes involved in pharmacokinetic (PK) drug–drug interactions (DDIs). The aim of this analysis is to revi... |
PMC7023070 | core_pubmed_pmc | Novel Population Pharmacokinetic Model for Linezolid in Critically Ill Patients and Evaluation of the Adequacy of the Current Dosing Recommendation | Novel Population Pharmacokinetic Model for Linezolid in Critically Ill Patients and Evaluation of the Adequacy of the Current Dosing Recommendation Abstract Abstract Antimicrobial treatment in critically ill patients remains challenging. The aim of this study was to develop a population pharmacokinetic model for linezo... |
PMC10518021 | core_pubmed_pmc | Population Pharmacokinetics and Exposure–Response with Teclistamab in Patients With Relapsed/Refractory Multiple Myeloma: Results From MajesTEC-1 | Population Pharmacokinetics and Exposure–Response with Teclistamab in Patients With Relapsed/Refractory Multiple Myeloma: Results From MajesTEC-1 Abstract Abstract Background Teclistamab, a B-cell maturation antigen × CD3 bispecific antibody, is approved in patients with relapsed/refractory multiple myeloma (RRMM) who ... |
PMC10450012 | core_pubmed_pmc | CYP3A and CYP2C19 Activity Determined by Microdosed Probe Drugs Accurately Predict Voriconazole Clearance in Healthy Adults | CYP3A and CYP2C19 Activity Determined by Microdosed Probe Drugs Accurately Predict Voriconazole Clearance in Healthy Adults Abstract Abstract Background and Objective Voriconazole is an important broad-spectrum anti-fungal drug with nonlinear pharmacokinetics. The aim of this single centre fixed-sequence open-label dru... |
PMC8780228 | core_pubmed_pmc | A Review on Parallel Virtual Screening Softwares for High-Performance Computers | A Review on Parallel Virtual Screening Softwares for High-Performance Computers Abstract Abstract Drug discovery is the most expensive, time-demanding, and challenging project in biopharmaceutical companies which aims at the identification and optimization of lead compounds from large-sized chemical libraries. The lead... |
PMC11229030 | core_pubmed_pmc | Phase I and pharmacodynamic study of arsenic trioxide plus radiotherapy in patients with newly diagnosed glioblastoma | Phase I and pharmacodynamic study of arsenic trioxide plus radiotherapy in patients with newly diagnosed glioblastoma Abstract Abstract Background When arsenic trioxide (ATO) was combined with radiation for treatment of transplanted murine gliomas in the brain, tumor response improved with disrupted tumor blood flow an... |
PMC8302237 | core_pubmed_pmc | Understanding effect site pharmacology of uprifosbuvir, a hepatitis C virus nucleoside inhibitor: Case study of a multidisciplinary modeling approach in drug development | Understanding effect site pharmacology of uprifosbuvir, a hepatitis C virus nucleoside inhibitor: Case study of a multidisciplinary modeling approach in drug development Abstract Abstract Uprifosbuvir is a uridine nucleoside monophosphate prodrug inhibitor of the hepatitis C virus NS5B RNA polymerase. To quantitatively... |
PMC4076802 | core_pubmed_pmc | Exposure–Response Modeling of Clinical End Points Using Latent Variable Indirect Response Models | Exposure–Response Modeling of Clinical End Points Using Latent Variable Indirect Response Models Abstract Exposure–response modeling facilitates effective dosing regimen selection in clinical drug development, where the end points are often disease scores and not physiological variables. Appropriate models need to be c... |
PMC12521073 | core_pubmed_pmc | A Pharmacometrics‐Informed Trial Simulation Framework for Optimizing Study Designs for Disease‐Modifying Treatments in Rare Neurological Disorders | A Pharmacometrics‐Informed Trial Simulation Framework for Optimizing Study Designs for Disease‐Modifying Treatments in Rare Neurological Disorders Abstract ABSTRACT The development of new treatments for rare neurological diseases (RNDs) may be very challenging due to limited natural history data, lack of relevant bioma... |
PMC5915615 | core_pubmed_pmc | Population Pharmacokinetic/Pharmacodynamic Modeling of Depot Testosterone Cypionate in Healthy Male Subjects | Population Pharmacokinetic/Pharmacodynamic Modeling of Depot Testosterone Cypionate in Healthy Male Subjects Abstract Abstract A randomized, double‐blind clinical trial was conducted to investigate long‐term abuse effects of testosterone cypionate (TC). Thirty‐one healthy men were randomized into a dose group of 100, 2... |
PMC10681456 | core_pubmed_pmc | Sabatolimab ( MBG453 ) model‐informed drug development for dose selection in patients with myelodysplastic syndrome/acute myeloid leukemia and solid tumors | Sabatolimab ( MBG453 ) model‐informed drug development for dose selection in patients with myelodysplastic syndrome/acute myeloid leukemia and solid tumors Abstract Abstract Sabatolimab is a novel immunotherapy with immuno‐myeloid activity that targets T‐cell immunoglobulin domain and mucin domain‐3 (TIM‐3) on immune c... |
PMC11061460 | core_pubmed_pmc | Acyl pyrazole sulfonamides as new antidiabetic agents: synthesis, glucosidase inhibition studies, and molecular docking analysis | Acyl pyrazole sulfonamides as new antidiabetic agents: synthesis, glucosidase inhibition studies, and molecular docking analysis Abstract Abstract Diabetes mellitus is a multi-systematic chronic metabolic disorder and life-threatening disease resulting from impaired glucose homeostasis. The inhibition of glucosidase, p... |
PMC12736770 | core_pubmed_pmc | Pharmacokinetic Landscape and Interaction Potential of SGLT2 Inhibitors: Bridging In Vitro Findings and Clinical Implications | Pharmacokinetic Landscape and Interaction Potential of SGLT2 Inhibitors: Bridging In Vitro Findings and Clinical Implications Abstract Sodium–glucose cotransporter 2 (SGLT2) inhibitors are widely used in type 2 diabetes and cardiometabolic diseases, and their pharmacokinetic characteristics generally confer a low risk ... |
PMC12440775 | core_pubmed_pmc | Safety, tolerability, and pharmacokinetics of faldaprevir after single increasing doses in healthy subjects | Safety, tolerability, and pharmacokinetics of faldaprevir after single increasing doses in healthy subjects Abstract Abstract Faldaprevir (FDV) is a novel NS3/NS4A inhibitor used in the treatment of hepatitis C infection in an interferon-free regimen. This study evaluated the safety, tolerability, and pharmacokinetics ... |
PMC12383694 | core_pubmed_pmc | Chlorogenic Acid and Cinnamaldehyde in Breast Cancer Cells: Predictive Examination of Pharmacokinetics and Binding Thermodynamics with the Key Mediators of PI3K/Akt Signaling | Chlorogenic Acid and Cinnamaldehyde in Breast Cancer Cells: Predictive Examination of Pharmacokinetics and Binding Thermodynamics with the Key Mediators of PI3K/Akt Signaling Abstract Abstract Background/Objective: In the pursuit of identifying novel therapeutic agents against breast cancer, a major priority is finding... |
PMC10525845 | core_pubmed_pmc | Continuous Fentanyl Infusion in Newborns with Hypoxic–Ischemic Encephalopathy Treated with Therapeutic Hypothermia: Background, Aims, and Study Protocol for Time-Concentration Profiles | Continuous Fentanyl Infusion in Newborns with Hypoxic–Ischemic Encephalopathy Treated with Therapeutic Hypothermia: Background, Aims, and Study Protocol for Time-Concentration Profiles Abstract Therapeutic hypothermia (TH) is the standard of care for newborns with moderate to severe hypoxic–ischemic encephalopathy (HIE... |
PMC5698587 | core_pubmed_pmc | The acute effect of beta‐guanidinopropionic acid versus creatine or placebo in healthy men (ABC‐Trial): A randomized controlled first‐in‐human trial | The acute effect of beta‐guanidinopropionic acid versus creatine or placebo in healthy men (ABC‐Trial): A randomized controlled first‐in‐human trial Abstract Abstract Aims Increasing evidence indicates that the ATP‐generating enzyme creatine kinase (CK) is involved in hypertension. CK rapidly regenerates ATP from creat... |
PMC6613192 | core_pubmed_pmc | Update on the pharmacogenomics of pain management | Update on the pharmacogenomics of pain management Abstract Abstract Pharmacogenomics is the study of genetic variants that impact drug effects through changes in a drug’s pharmacokinetics and pharmacodynamics. Pharmacogenomics is being integrated into clinical pain management practice because variants in individual gen... |
PMC9636859 | core_pubmed_pmc | In vivo Characterization of the Opioid Receptor–Binding Profiles of Samidorphan and Naltrexone in Rats: Comparisons at Clinically Relevant Concentrations | In vivo Characterization of the Opioid Receptor–Binding Profiles of Samidorphan and Naltrexone in Rats: Comparisons at Clinically Relevant Concentrations Abstract Introduction The atypical antipsychotic olanzapine is approved for the treatment of schizophrenia and bipolar I disorder; however, weight gain and metabolic ... |
PMC12627933 | core_pubmed_pmc | A First-In-Human Study of the SUMOylation Inhibitor Subasumstat in Patients with Advanced/Metastatic Solid Tumors or Relapsed/Refractory Hematologic Malignancies | A First-In-Human Study of the SUMOylation Inhibitor Subasumstat in Patients with Advanced/Metastatic Solid Tumors or Relapsed/Refractory Hematologic Malignancies Abstract Abstract Purpose: Subasumstat (TAK-981) is a first-in-class inhibitor of SUMOylation that can engage innate and adaptive immune responses in tumors b... |
PMC6525001 | core_pubmed_pmc | Pharmacokinetics of fixed-dose combination of atorvastatin and metformin compared with individual tablets | Pharmacokinetics of fixed-dose combination of atorvastatin and metformin compared with individual tablets Abstract Purpose: The aims of this study was to investigate the mutual pharmacokinetic interactions between steady-state atorvastatin and metformin and the effect of food on the fixed-dose combined (FDC) tablet of ... |
PMC11698021 | core_pubmed_pmc | Validation and Utility of Drug-Nutrient Interaction and Dietary Supplement Mechanistic Activity in the Natural Medicines Database | Validation and Utility of Drug-Nutrient Interaction and Dietary Supplement Mechanistic Activity in the Natural Medicines Database Abstract Abstract PURPOSE The increasing use of dietary supplements by patients with cancer and other chronic diseases requires the systematized review of potential interactions between pres... |
PMC10690114 | core_pubmed_pmc | Clinical Characterization of [ 18 F]T-008, a Cholesterol 24-Hydroxylase PET Ligand: Dosimetry, Kinetic Modeling, Variability, and Soticlestat Occupancy | Clinical Characterization of [ 18 F]T-008, a Cholesterol 24-Hydroxylase PET Ligand: Dosimetry, Kinetic Modeling, Variability, and Soticlestat Occupancy Abstract Abstract This series of studies characterized [ 18 F]T-008, a PET radiotracer for imaging cholesterol 24-hydroxylase (CH24H), in healthy volunteers ( ClinicalT... |
PMC8532833 | core_pubmed_pmc | Experimental Validation of a Mathematical Framework to Simulate Antibiotics with Distinct Half-Lives Concurrently in an In Vitro Model | Experimental Validation of a Mathematical Framework to Simulate Antibiotics with Distinct Half-Lives Concurrently in an In Vitro Model Abstract Antimicrobial resistance has been steadily increasing in prevalence, and combination therapy is commonly used to treat infections due to multidrug resistant bacteria. Under cer... |
PMC9546084 | core_pubmed_pmc | Effects of Unsuppressed Endogenous Insulin on Pharmacokinetics and/or Pharmacodynamics of Study Insulin in the Healthy: A Retrospective Study | Effects of Unsuppressed Endogenous Insulin on Pharmacokinetics and/or Pharmacodynamics of Study Insulin in the Healthy: A Retrospective Study Abstract Abstract C‐peptide, a marker of endogenous insulin, should be consistently inhibited during euglycemic clamping, while an elevated postdosing C‐peptide (CP postdosing ) ... |
PMC5403812 | core_pubmed_pmc | Physiologically Based Simulations of Deuterated Glucose for Quantifying Cell Turnover in Humans | Physiologically Based Simulations of Deuterated Glucose for Quantifying Cell Turnover in Humans Abstract In vivo [6,6- 2 H 2 ]-glucose labeling is a state-of-the-art technique for quantifying cell proliferation and cell disappearance in humans. However, there are discrepancies between estimates of T cell proliferation ... |
PMC4500330 | core_pubmed_pmc | Pharmacokinetic study between a bilayer matrix fentalyl patch and a monolayer matrix fentanyl patch: single dose administration in healthy volunteers * | Pharmacokinetic study between a bilayer matrix fentalyl patch and a monolayer matrix fentanyl patch: single dose administration in healthy volunteers * Abstract Abstract Aims Transdermal fentanyl is a well established treatment for cancer pain. The aim of the present study is to assess the relative bioavailability of f... |
PMC10005222 | core_pubmed_pmc | Development of a Novel Apigenin Dosage form as a Substitute for the Modern Triple Antithrombotic Regimen | Development of a Novel Apigenin Dosage form as a Substitute for the Modern Triple Antithrombotic Regimen Abstract Abstract The simultaneous administration of three antiplatelet agents has been proposed as an efficient strategy for the secondary prevention of atherothrombotic events and is included in the European guide... |
PMC5368910 | core_pubmed_pmc | Pharmacokinetics of surotomycin from phase 1 single and multiple ascending dose studies in healthy volunteers | Pharmacokinetics of surotomycin from phase 1 single and multiple ascending dose studies in healthy volunteers Abstract Background Surotomycin, a novel, orally administered, cyclic, lipopeptide antibacterial in development for the treatment of Clostridium difficile -associated diarrhea, has demonstrated minimal intestin... |
PMC8503994 | core_pubmed_pmc | Distribution of crystalloid fluid infused during onset of anesthesia-induced hypotension: a retrospective population kinetic analysis | Distribution of crystalloid fluid infused during onset of anesthesia-induced hypotension: a retrospective population kinetic analysis Abstract Abstract Background Induction of anesthesia causes a drop in arterial pressure that might change the kinetics of infused crystalloid fluid. The aim of this report is to provide ... |
PMC10725264 | core_pubmed_pmc | Dosing recommendation of nirmatrelvir/ritonavir using an integrated population pharmacokinetic analysis | Dosing recommendation of nirmatrelvir/ritonavir using an integrated population pharmacokinetic analysis Abstract Abstract Protease inhibitor nirmatrelvir coadministered with ritonavir as a pharmacokinetic enhancer (PAXLOVID™; Pfizer Inc) became the first orally bioavailable antiviral agent granted Emergency Use Authori... |
PMC12223802 | core_pubmed_pmc | In Vitro Leishmanicidal Effect of Silibinin: Disrupting Redox Balance via Trypanothione Reductase Inhibition | In Vitro Leishmanicidal Effect of Silibinin: Disrupting Redox Balance via Trypanothione Reductase Inhibition Abstract Visceral leishmaniasis, caused by the parasite Leishmania infantum , is a life-threatening disease with limited therapeutic options that are often associated with toxicity and resistance. In this study,... |
PMC12618397 | core_pubmed_pmc | Modeling Whole-Body Dynamic PET Microdosing Data to Predict the Whole-Body Pharmacokinetics of Glyburide in Humans | Modeling Whole-Body Dynamic PET Microdosing Data to Predict the Whole-Body Pharmacokinetics of Glyburide in Humans Abstract Introduction Whole-body dynamic (WB4D) positron emission tomography (PET) imaging data using radiolabeled analogs of drugs are mostly analyzed using descriptive approaches, with no relationship to... |
PMC5485066 | core_pubmed_pmc | Population Pharmacokinetic Modeling of Secukinumab in Patients With Moderate to Severe Psoriasis | Population Pharmacokinetic Modeling of Secukinumab in Patients With Moderate to Severe Psoriasis Abstract Abstract Secukinumab is a human monoclonal antibody with demonstrated efficacy for moderate to severe psoriasis; it binds to and neutralizes interleukin (IL)‐17A. The pharmacokinetic (PK) parameters of secukinumab ... |
PMC9097512 | core_pubmed_pmc | Comparative pharmacokinetics of Theracurmin, a highly bioavailable curcumin, in healthy adult subjects | Comparative pharmacokinetics of Theracurmin, a highly bioavailable curcumin, in healthy adult subjects Abstract Abstract Objective: Theracurmin is a submicron dispersed formulation of curcumin, which was developed to increase the bioavailability of curcumin. This study aimed to compare the pharmacokinetics of curcumin ... |
PMC12373507 | core_pubmed_pmc | A nitroalkene derivative of salicylate, SANA, induces creatine-dependent thermogenesis and promotes weight loss | A nitroalkene derivative of salicylate, SANA, induces creatine-dependent thermogenesis and promotes weight loss Abstract The emergence of glucagon-like peptide-1 agonists represents a notable advancement in the pharmacological treatment of obesity, yet complementary approaches are essential. Through phenotypic drug dis... |
PMC4622966 | core_pubmed_pmc | Biosimilars entering the clinic without animal studies | Biosimilars entering the clinic without animal studies Abstract The concept of biosimilars has spread from Europe to other regions throughout the world, and many regions have drafted regulatory guidelines for their development. Recently, a paradigm shift in regulatory thinking on the non-clinical development of biosimi... |
PMC10349195 | core_pubmed_pmc | Disease progression joint model predicts time to type 1 diabetes onset: Optimizing future type 1 diabetes prevention studies | Disease progression joint model predicts time to type 1 diabetes onset: Optimizing future type 1 diabetes prevention studies Abstract Abstract Clinical trials seeking type 1 diabetes prevention are challenging in terms of identifying patient populations likely to progress to type 1 diabetes within limited (i.e., short‐... |
PMC5591880 | core_pubmed_pmc | Brain Pharmacokinetics and the Pharmacological Effects on Striatal Neurotransmitter Levels of Pueraria lobata Isoflavonoids in Rat | Brain Pharmacokinetics and the Pharmacological Effects on Striatal Neurotransmitter Levels of Pueraria lobata Isoflavonoids in Rat Abstract Isoflavonoids are putatively active components of Pueraria lobata and has been demonstrated prominent neuro-protection effect against cerebrovascular disorders, hypertension or Par... |
PMC7355955 | core_pubmed_pmc | Validation of Pharmacological Protocols for Targeted Inhibition of Canalicular MRP2 Activity in Hepatocytes Using [ 99m Tc]mebrofenin Imaging in Rats | Validation of Pharmacological Protocols for Targeted Inhibition of Canalicular MRP2 Activity in Hepatocytes Using [ 99m Tc]mebrofenin Imaging in Rats Abstract The multidrug resistance-associated protein 2 (MRP2) mediates the biliary excretion of drugs and metabolites. [ 99m Tc]mebrofenin may be employed as a probe for ... |
PMC9998600 | core_pubmed_pmc | Pharmacokinetics and Target Attainment of Antimicrobial Drugs Throughout Pregnancy: Part I—Penicillins | Pharmacokinetics and Target Attainment of Antimicrobial Drugs Throughout Pregnancy: Part I—Penicillins Abstract Abstract Background and Objective Pharmacokinetics (PK) are severely altered in pregnant women due to changes in volume of distribution (Vd) and/or drug clearance (CL), affecting target attainment of antibiot... |
PMC11823665 | core_pubmed_pmc | Pharmacokinetics of ethambutol and weight banded dosing in South African adults newly diagnosed with tuberculosis and HIV | Pharmacokinetics of ethambutol and weight banded dosing in South African adults newly diagnosed with tuberculosis and HIV Abstract ABSTRACT Ethambutol is used to treat tuberculosis (TB) in individuals living with HIV. Low concentrations of ethambutol have been reported in patients dosed with the World Health Organizati... |
PMC4946363 | core_pubmed_pmc | A Multi-centric Bioequivalence Trial in Ph+ Chronic Myeloid Leukemia Patients to Assess Bioequivalence and Safety Evaluation of Generic Imatinib Mesylate 400 mg Tablets | A Multi-centric Bioequivalence Trial in Ph+ Chronic Myeloid Leukemia Patients to Assess Bioequivalence and Safety Evaluation of Generic Imatinib Mesylate 400 mg Tablets Abstract Abstract Purpose This study was designed to characterize the pharmacokinetic profile and to assess bioequivalence of the sponsor’s test formul... |
PMC10543969 | core_pubmed_pmc | Pharmacokinetic analysis of acute and dietary exposure to piperonyl butoxide in the mouse | Pharmacokinetic analysis of acute and dietary exposure to piperonyl butoxide in the mouse Abstract Piperonyl butoxide (PBO) is a popular insecticide synergist present in thousands of commercial, agricultural, and household products. PBO inhibits cytochrome P450 activity, impairing the ability of insects to detoxify ins... |
PMC7828042 | core_pubmed_pmc | Involvement of Organic Anion Transporters in the Pharmacokinetics and Drug Interaction of Rosmarinic Acid | Involvement of Organic Anion Transporters in the Pharmacokinetics and Drug Interaction of Rosmarinic Acid Abstract We investigated the involvement of drug transporters in the pharmacokinetics of rosmarinic acid in rats as well as the transporter-mediated drug interaction potential of rosmarinic acid in HEK293 cells ove... |
PMC10914196 | core_pubmed_pmc | Isatuximab Monotherapy for Desensitization in Highly Sensitized Patients Awaiting Kidney Transplant | Isatuximab Monotherapy for Desensitization in Highly Sensitized Patients Awaiting Kidney Transplant Abstract Significance Statement There is no standardized desensitization regimen for kidney transplant candidates. CD38, expressed by plasma cells, could be targeted for desensitization to deplete plasma cells producing ... |
PMC9865364 | core_pubmed_pmc | Isavuconazole Pharmacokinetics and Pharmacodynamics in Children | Isavuconazole Pharmacokinetics and Pharmacodynamics in Children Abstract Isavuconazole is a broad-spectrum azole anti-fungal not yet approved in children. We conducted a retrospective, single-center review of isavuconazole use and routine therapeutic drug monitoring in pediatric patients, extracting demographic, dosing... |
PMC8704606 | core_pubmed_pmc | The Artemiside-Artemisox-Artemisone-M1 Tetrad: Efficacies against Blood Stage P. falciparum Parasites, DMPK Properties, and the Case for Artemiside | The Artemiside-Artemisox-Artemisone-M1 Tetrad: Efficacies against Blood Stage P. falciparum Parasites, DMPK Properties, and the Case for Artemiside Abstract Abstract Because of the need to replace the current clinical artemisinins in artemisinin combination therapies, we are evaluating fitness of amino-artemisinins for... |
PMC11961393 | core_pubmed_pmc | Effect of Cladribine Tablets on the Pharmacokinetics of a Combined Oral Contraceptive in Pre‐Menopausal Women With Relapsing Multiple Sclerosis | Effect of Cladribine Tablets on the Pharmacokinetics of a Combined Oral Contraceptive in Pre‐Menopausal Women With Relapsing Multiple Sclerosis Abstract ABSTRACT This study assessed the effect of cladribine tablets (CladT) on the pharmacokinetics (PK) of a combined oral contraceptive (COC) in pre‐menopausal women with ... |
PMC12625747 | core_pubmed_pmc | Determination of Total and Free Plasma Concentration of Liposomal Mitoxantrone and Clinical Application in Adult Patients with Relapsed or Refractory Peripheral T-Cell Lymphoma | Determination of Total and Free Plasma Concentration of Liposomal Mitoxantrone and Clinical Application in Adult Patients with Relapsed or Refractory Peripheral T-Cell Lymphoma Abstract Abstract Purpose Currently reported methods for determining plasma concentration of mitoxantrone primarily measure total drug concentr... |
PMC6990616 | core_pubmed_pmc | Ceftolozane/Tazobactam Dosing Requirements Against Pseudomonas aeruginosa Bacteremia | Ceftolozane/Tazobactam Dosing Requirements Against Pseudomonas aeruginosa Bacteremia Abstract Abstract Objectives: To assess the probability of reaching adequate pharmacokinetic/pharmacodynamics values for ceftolozane/tazobactam at different doses and degrees of renal functions in patients with Pseudomonas aeruginosa b... |
PMC12087682 | core_pubmed_pmc | Dose Determinations at Drug Approval Reviews: FDA‐Approved Drugs in Past 5 Years | Dose Determinations at Drug Approval Reviews: FDA‐Approved Drugs in Past 5 Years Abstract Abstract Drug dose appropriateness is one of the most discussed issues in regulatory reviews. We analyzed dose determinations during Food and Drug Administration (FDA) drug reviews to determine whether there were changes between t... |
PMC10780881 | core_pubmed_pmc | Bio-Guided Assay of Ephedra foeminea Forssk Extracts and Anticancer Activities: In Vivo, In Vitro, and In Silico Evaluations | Bio-Guided Assay of Ephedra foeminea Forssk Extracts and Anticancer Activities: In Vivo, In Vitro, and In Silico Evaluations Abstract Abstract Ephedra is one of the oldest known medicinal plants and the largest genera of the Ephedraceae family. In vivo antitumor evaluation of Ephedra foeminea revealed that ethyl acetat... |
PMC10168231 | core_pubmed_pmc | Uncovering the hidden structure of dynamic T cell composition in peripheral blood during cancer immunotherapy: a topic modeling approach | Uncovering the hidden structure of dynamic T cell composition in peripheral blood during cancer immunotherapy: a topic modeling approach Abstract Abstract Immune checkpoint inhibitors (ICIs), now mainstays in the treatment of cancer treatment, show great potential but only benefit a subset of patients. A more complete ... |
PMC3821905 | core_pubmed_pmc | Colon Targeted Guar Gum Compression Coated Tablets of Flurbiprofen: Formulation, Development, and Pharmacokinetics | Colon Targeted Guar Gum Compression Coated Tablets of Flurbiprofen: Formulation, Development, and Pharmacokinetics Abstract The rationale of the present study is to formulate flurbiprofen colon targeted compression coated tablets using guar gum to improve the therapeutic efficacy by increasing drug levels in colon, and... |
PMC3585837 | core_pubmed_pmc | Effect of Food on the Pharmacokinetic Profile of Etamicastat (BIA 5-453) | Effect of Food on the Pharmacokinetic Profile of Etamicastat (BIA 5-453) Abstract Abstract Background: Etamicastat is a novel, potent, and reversible peripheral dopamine-β-hydroxylase inhibitor that has been administered orally at doses up to 600mg once daily for 10 days to male healthy volunteers and appears to be wel... |
PMC11741452 | core_pubmed_pmc | Molnupiravir clinical trial simulation suggests that polymerase chain reaction underestimates antiviral potency against SARS-CoV-2 | Molnupiravir clinical trial simulation suggests that polymerase chain reaction underestimates antiviral potency against SARS-CoV-2 Abstract Molnupiravir is an antiviral medicine that induces lethal copying errors during SARS-CoV-2 RNA replication. Molnupiravir reduced hospitalization in one pivotal trial by 50% and had... |
PMC10128972 | core_pubmed_pmc | High rifampicin peak plasma concentrations accelerate the slow phase of bacterial decline in tuberculosis patients: Evidence for heteroresistance | High rifampicin peak plasma concentrations accelerate the slow phase of bacterial decline in tuberculosis patients: Evidence for heteroresistance Abstract Abstract Background Antibiotic treatments are often associated with a late slowdown in bacterial killing. This separates the killing of bacteria into at least two di... |
PMC10141038 | core_pubmed_pmc | Microfluidic Liver-on-a-Chip for Preclinical Drug Discovery | Microfluidic Liver-on-a-Chip for Preclinical Drug Discovery Abstract Abstract Drug discovery is an expensive, long, and complex process, usually with a high degree of uncertainty. In order to improve the efficiency of drug development, effective methods are demanded to screen lead molecules and eliminate toxic compound... |
PMC11686447 | core_pubmed_pmc | Transcriptomics as a predictor of biopharmaceutically favourable glycan profiles | Transcriptomics as a predictor of biopharmaceutically favourable glycan profiles Abstract Abstract N -glycosylation plays a crucial role in defining the pharmacological properties and efficacy of therapeutic proteins, commonly referred to as biologics. The inherent complexity and lack of a templated process in glycosyl... |
PMC7430014 | core_pubmed_pmc | A narrative review on trans-nasal pulmonary aerosol delivery | A narrative review on trans-nasal pulmonary aerosol delivery Abstract Abstract The use of trans-nasal pulmonary aerosol delivery via high-flow nasal cannula (HFNC) has expanded in recent years. However, various factors influencing aerosol delivery in this setting have not been precisely defined, and no consensus has em... |
PMC11421311 | core_pubmed_pmc | An insight into advances and challenges in the development of potential stearoyl Co-A desaturase 1 inhibitors | An insight into advances and challenges in the development of potential stearoyl Co-A desaturase 1 inhibitors Abstract Stearoyl-CoA desaturase 1 (SCD1) is one of the key enzymes involved in lipid metabolism, plays a vital role in the synthesis of monounsaturated fatty acids (MUFAs) from saturated fatty acids (SFAs). Du... |
PMC4258079 | core_pubmed_pmc | Sublingual administration of detomidine to calves prior to disbudding: a comparison with the intravenous route | Sublingual administration of detomidine to calves prior to disbudding: a comparison with the intravenous route Abstract Abstract Objective To study the effects of oromucosal detomidine gel administered sublingually to calves prior to disbudding, and to compare its efficacy with intravenously (IV) administered detomidin... |
PMC8226217 | core_pubmed_pmc | Varied Contribution of Phospholipid Shedding From Membrane to Daptomycin Tolerance in Staphylococcus aureus | Varied Contribution of Phospholipid Shedding From Membrane to Daptomycin Tolerance in Staphylococcus aureus Abstract It has been suggested that daptomycin can be inactivated by lipids released by Staphylococcus aureus and that this effect is antagonized by phenol soluble modulins (PSMs), which bind to the shed lipids. ... |
PMC12071049 | core_pubmed_pmc | 68 Ga-Trivehexin: Current Status of αvβ6-Integrin Imaging and Perspectives | 68 Ga-Trivehexin: Current Status of αvβ6-Integrin Imaging and Perspectives Abstract Simple Summary Significant advancements have been made in molecular imaging, particularly positron emission tomography (PET), which has evolved from using metabolic radiotracers like 2-deoxy-2-[ 18 F]fluoro-D-glucose [ 18 F]FDG to more ... |
PMC6124464 | core_pubmed_pmc | Profile of pitolisant in the management of narcolepsy: design, development, and place in therapy | Profile of pitolisant in the management of narcolepsy: design, development, and place in therapy Abstract Narcolepsy is a rare sleep disorder characterized by excessive daytime sleepiness and rapid eye movement sleep dysregulation, manifesting as cataplexy and sleep paralysis, as well as hypnagogic and hypnopompic hall... |
PMC4819938 | core_pubmed_pmc | Adaptive dosing of anticancer drugs in neonates: facilitating evidence-based dosing regimens | Adaptive dosing of anticancer drugs in neonates: facilitating evidence-based dosing regimens Abstract Abstract Purpose Selection of the most appropriate chemotherapy dosing regimens for neonates treated within the first weeks of life represents a significant clinical dilemma. Due to a lack of information relating to th... |
PMC5806446 | core_pubmed_pmc | A physiologically based model for denitrogenation kinetics | A physiologically based model for denitrogenation kinetics Abstract Under normal conditions we continuously breathe 78% nitrogen (N 2 ) such that the body tissues and fluids are saturated with dissolved N 2 . For normobaric medical gas administration at high concentrations, the N 2 concentration must be less than that ... |
PMC4998672 | core_pubmed_pmc | Task- and Treatment Length–Dependent Effects of Vortioxetine on Scopolamine-Induced Cognitive Dysfunction and Hippocampal Extracellular Acetylcholine in Rats | Task- and Treatment Length–Dependent Effects of Vortioxetine on Scopolamine-Induced Cognitive Dysfunction and Hippocampal Extracellular Acetylcholine in Rats Abstract Abstract Major depressive disorder (MDD) is a common psychiatric disorder that often features impairments in cognitive function, and these cognitive symp... |
PMC9646970 | core_pubmed_pmc | The effects of cyclosporine A or activated charcoal co-administration on the pharmacokinetics of enrofloxacin in chickens | The effects of cyclosporine A or activated charcoal co-administration on the pharmacokinetics of enrofloxacin in chickens Abstract Abstract The study aimed to investigate the possible role of efflux transporter proteins in the pharmacokinetics of enrofloxacin ( ENR ) in broilers in the model of co-administration of act... |
PMC8904038 | core_pubmed_pmc | A Physiologically Based Pharmacokinetic Model for Studying the Biowaiver Risk of Biopharmaceutics Classification System Class I Drugs With Rapid Elimination: Dexketoprofen Trometamol Case Study | A Physiologically Based Pharmacokinetic Model for Studying the Biowaiver Risk of Biopharmaceutics Classification System Class I Drugs With Rapid Elimination: Dexketoprofen Trometamol Case Study Abstract Abstract Biowaiver based on the biopharmaceutics classification system (BCS) has been widely used in the global marke... |
PMC11903631 | core_pubmed_pmc | A global cross-sectional survey on neonatal analgosedation: unveiling global trends and challenges through latent class analysis | A global cross-sectional survey on neonatal analgosedation: unveiling global trends and challenges through latent class analysis Abstract Abstract Purpose This study aims to analyze global prescribing patterns for analgosedation in neonates during four critical care scenarios. The research explores existing patterns, t... |
PMC8783433 | core_pubmed_pmc | Pharmacokinetics and pharmacodynamics studies of a loading dose of cisatracurium in critically ill patients with respiratory failure | Pharmacokinetics and pharmacodynamics studies of a loading dose of cisatracurium in critically ill patients with respiratory failure Abstract Abstract Background Previous studies reported a slow neuromuscular response with the currently recommended dose of cisatracurium in critically ill patients. Pharmacokinetic and p... |
PMC5036420 | core_pubmed_pmc | A Tutorial on Pharmacodynamic Scripting Facility in Simcyp | A Tutorial on Pharmacodynamic Scripting Facility in Simcyp Modeling Example – Warfarin PD model The case example presented here is based on the PD response model to warfarin in a Chinese population 12 as this model has different coding features. The PK model is not of interest in this tutorial, since the plasma concent... |
PMC5073111 | core_pubmed_pmc | Pharmacokinetic Profile and Palatability of Atomoxetine Oral Solution in Healthy Japanese Male Adults | Pharmacokinetic Profile and Palatability of Atomoxetine Oral Solution in Healthy Japanese Male Adults Abstract Abstract Background and Objectives There is a clinical need for a liquid formulation of atomoxetine. We assessed the safety and bioequivalence of an atomoxetine oral solution. Methods This was an open-label, r... |
PMC12546574 | core_pubmed_pmc | Pharmacokinetics and in vivo efficacy of epetraborole against Burkholderia pseudomallei | Pharmacokinetics and in vivo efficacy of epetraborole against Burkholderia pseudomallei Abstract Abstract Melioidosis, caused by Burkholderia pseudomallei , remains a major therapeutic challenge due to high relapse rates and intrinsic antibiotic resistance. Epetraborole (EBO), a leucyl-tRNA synthetase inhibitor, repres... |
PMC10951152 | core_pubmed_pmc | Effect of Food Consumption on the Pharmacokinetics, Safety, and Tolerability of Once-Daily Orally Administered Orforglipron (LY3502970), a Non-peptide GLP-1 Receptor Agonist | Effect of Food Consumption on the Pharmacokinetics, Safety, and Tolerability of Once-Daily Orally Administered Orforglipron (LY3502970), a Non-peptide GLP-1 Receptor Agonist Abstract Abstract Introduction We assessed the effect of the prandial state on the pharmacokinetics, safety, and tolerability of single and multip... |
PMC6760598 | core_pubmed_pmc | Advancing internal exposure and physiologically-based toxicokinetic modeling for 21st-century risk assessments | Advancing internal exposure and physiologically-based toxicokinetic modeling for 21st-century risk assessments Abstract Abstract Scientifically sound, risk-informed evaluation of chemicals is essential to protecting public health. Systematically leveraging information from exposure, toxicology, and epidemiology studies... |
PMC12135525 | core_pubmed_pmc | Two phase 1 studies of safety, tolerability, and pharmacokinetics of an EFdA prodrug (BRII-732) in healthy adult participants | Two phase 1 studies of safety, tolerability, and pharmacokinetics of an EFdA prodrug (BRII-732) in healthy adult participants Abstract ABSTRACT BRII-732, a medoxomil carbonate prodrug of EFdA, is designed for once weekly dosing as part of combination antiretroviral therapy for HIV. Two single-center, randomized, double... |
PMC9926295 | core_pubmed_pmc | Characteristics and calculations of paired vancomycin measurements for determination of 24-h area-under-curve (AUC) | Characteristics and calculations of paired vancomycin measurements for determination of 24-h area-under-curve (AUC) Abstract Abstract Background Current pharmacy practice guidelines recommend 24-h area-under-curve (AUC 24 ) targets for use of vancomycin against methicillin-resistant Staphylococcus aureus (MRSA). AUC pr... |
PMC12116709 | core_pubmed_pmc | Pharmacodynamic target attainment of the synergism of ceftazidime-avibactam in combination with amikacin against OXA-producing extensively drug-resistant or pan drug-resistant (XDR/PDR) Pseudomonas aeruginosa | Pharmacodynamic target attainment of the synergism of ceftazidime-avibactam in combination with amikacin against OXA-producing extensively drug-resistant or pan drug-resistant (XDR/PDR) Pseudomonas aeruginosa Abstract Abstract To investigate the pharmacodynamic target attainment of ceftazidime-avibactam (CZA) in combin... |
PMC3763649 | core_pubmed_pmc | Cannabidiol in Humans—The Quest for Therapeutic Targets | Cannabidiol in Humans—The Quest for Therapeutic Targets Abstract Abstract Cannabidiol (CBD), a major phytocannabinoid constituent of cannabis, is attracting growing attention in medicine for its anxiolytic, antipsychotic, antiemetic and anti-inflammatory properties. However, up to this point, a comprehensive literature... |
PMC5522071 | core_pubmed_pmc | Preclinical development of G1T38: A novel, potent and selective inhibitor of cyclin dependent kinases 4/6 for use as an oral antineoplastic in patients with CDK4/6 sensitive tumors | Preclinical development of G1T38: A novel, potent and selective inhibitor of cyclin dependent kinases 4/6 for use as an oral antineoplastic in patients with CDK4/6 sensitive tumors Abstract Inhibition of the p16 INK4a /cyclin D/CDK4/6/RB pathway is an effective therapeutic strategy for the treatment of estrogen recepto... |
PMC4780720 | core_pubmed_pmc | A 5-fluorouracil-loaded floating gastroretentive hollow microsphere: development, pharmacokinetic in rabbits, and biodistribution in tumor-bearing mice | A 5-fluorouracil-loaded floating gastroretentive hollow microsphere: development, pharmacokinetic in rabbits, and biodistribution in tumor-bearing mice Abstract Abstract 5-Fluorouracil (5-FU) was loaded in hollow microspheres to improve its oral bioavailability. 5-FU hollow microspheres were developed by a solvent diff... |
PMC3250034 | core_pubmed_pmc | A computational perspective of molecular interactions through virtual screening, pharmacokinetic and dynamic prediction on ribosome toxin A chain and inhibitors of Ricinus communis | A computational perspective of molecular interactions through virtual screening, pharmacokinetic and dynamic prediction on ribosome toxin A chain and inhibitors of Ricinus communis Abstract Background: Ricin is considered to be one of the most deadly toxins and gained its favor as a bioweapon that has a serious social ... |
PMC8332605 | core_pubmed_pmc | Contribution of the Gut Microbiome to Drug Disposition, Pharmacokinetic and Pharmacodynamic Variability | Contribution of the Gut Microbiome to Drug Disposition, Pharmacokinetic and Pharmacodynamic Variability Abstract The trillions of microbes that make up the gut microbiome are an important contributor to health and disease. With respect to xenobiotics, particularly orally administered compounds, the gut microbiome inter... |
PMC12840558 | core_pubmed_pmc | Enhanced Clearance of HIV‐1 Broadly Neutralizing Antibody VRC07‐523‐LS During Viremia: Influences on Trial Design and Analysis | Enhanced Clearance of HIV‐1 Broadly Neutralizing Antibody VRC07‐523‐LS During Viremia: Influences on Trial Design and Analysis Abstract ABSTRACT Broadly neutralizing antibodies (BNAb) are capable of neutralizing multiple HIV‐1 strains through the targeting of conserved epitopes. This study's objective was to quantify t... |
PMC10321019 | core_pubmed_pmc | Rapid identification of chemical components in Xuelian granule by UHPLC-Q-orbitrap-HRMS based on enzyme activity in vitro | Rapid identification of chemical components in Xuelian granule by UHPLC-Q-orbitrap-HRMS based on enzyme activity in vitro Abstract Abstract Background Xuelian granule (XL), a traditional Chinese medicine (TCM) formula, has been used for the treatment of diabetic nephropathy for a long time as a hospital preparation. Be... |
PMC9929523 | core_pubmed_pmc | Addressing the oxamniquine in vitro - in vivo paradox to facilitate a new generation of anti-schistosome treatments | Addressing the oxamniquine in vitro - in vivo paradox to facilitate a new generation of anti-schistosome treatments Abstract The antischistosomal drug oxamniquine, OXA, requires activation by a sulfotransferase within the parasitic worm to enable killing. Examination of the pharmacokinetic/pharmacodynamic (PK/PD) relat... |
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