id stringlengths 9 11 | source stringclasses 1
value | title stringlengths 15 560 | text stringlengths 2k 153k |
|---|---|---|---|
PMC11206290 | core_pubmed_pmc | Study of the Lipophilicity and ADMET Parameters of New Anticancer Diquinothiazines with Pharmacophore Substituents | Study of the Lipophilicity and ADMET Parameters of New Anticancer Diquinothiazines with Pharmacophore Substituents Abstract Abstract Lipophilicity is one of the principal parameters that describe the pharmacokinetic behavior of a drug, including its absorption, distribution, metabolism, elimination, and toxicity. In th... |
PMC8401948 | core_pubmed_pmc | Improving the Solubility and Oral Bioavailability of a Novel Aromatic Aldehyde Antisickling Agent (PP10) for the Treatment of Sickle Cell Disease | Improving the Solubility and Oral Bioavailability of a Novel Aromatic Aldehyde Antisickling Agent (PP10) for the Treatment of Sickle Cell Disease Abstract Background: Aromatic aldehydes, with their ability to increase the oxygen affinity of sickle hemoglobin, have become important therapeutic agents for sickle cell dis... |
PMC6900043 | core_pubmed_pmc | Coadministered cannabidiol and clobazam: Preclinical evidence for both pharmacodynamic and pharmacokinetic interactions | Coadministered cannabidiol and clobazam: Preclinical evidence for both pharmacodynamic and pharmacokinetic interactions Abstract Abstract Objective Cannabidiol (CBD) has been approved by the US Food and Drug Administration (FDA) to treat intractable childhood epilepsies, such as Dravet syndrome and Lennox‐Gastaut syndr... |
PMC10333649 | core_pubmed_pmc | A review of the Bayesian approach with the MCMC and the HMC as a competitor of classical likelihood statistics for pharmacometricians | A review of the Bayesian approach with the MCMC and the HMC as a competitor of classical likelihood statistics for pharmacometricians Abstract Abstract This article reviews the Bayesian inference with the Monte Carlo Markov Chain (MCMC) and the Hamiltonian Monte Carlo (HMC) samplers as a competitor of the classical lik... |
PMC12403855 | core_pubmed_pmc | Antidermatophytic activity of Curcuma longa against Trichophyton spp .: compound identification and molecular docking to lanosterol 14α-demethylase | Antidermatophytic activity of Curcuma longa against Trichophyton spp .: compound identification and molecular docking to lanosterol 14α-demethylase Abstract The increasing incidence of dermatophytic infections and rising resistance to conventional antifungal agents necessitates the exploration of alternative therapies.... |
PMC8201677 | core_pubmed_pmc | Calycosin-loaded nanoliposomes as potential nanoplatforms for treatment of diabetic nephropathy through regulation of mitochondrial respiratory function | Calycosin-loaded nanoliposomes as potential nanoplatforms for treatment of diabetic nephropathy through regulation of mitochondrial respiratory function Abstract Backgrounds One of the most common complications in diabetic nephropathy is generation of high levels of ROS which can be regulated by herbal antioxidants. Ho... |
PMC11576656 | core_pubmed_pmc | Prospective approaches to gene therapy computational modeling – spotlight on viral gene therapy | Prospective approaches to gene therapy computational modeling – spotlight on viral gene therapy Abstract Clinical studies have found there still exists a lack of gene therapy dose-toxicity and dose-efficacy data that causes gene therapy dose selection to remain elusive. Model informed drug development (MIDD) has become... |
PMC9372430 | core_pubmed_pmc | Using partition analysis as a facile method to derive net clearances | Using partition analysis as a facile method to derive net clearances Abstract Abstract Partition analysis has been described previously by W.W. Cleland to derive net rate constants and simplify the derivation of enzyme kinetic equations. Here, we show that partition analysis can be used to derive elimination and transf... |
PMC7467414 | core_pubmed_pmc | PF-06881894, a Proposed Biosimilar to Pegfilgrastim, Versus US-Licensed and EU-Approved Pegfilgrastim Reference Products (Neulasta ® ): Pharmacodynamics, Pharmacokinetics, Immunogenicity, and Safety of Single or Multiple Subcutaneous Doses in Healthy Volunteers | PF-06881894, a Proposed Biosimilar to Pegfilgrastim, Versus US-Licensed and EU-Approved Pegfilgrastim Reference Products (Neulasta ® ): Pharmacodynamics, Pharmacokinetics, Immunogenicity, and Safety of Single or Multiple Subcutaneous Doses in Healthy Volunteers Abstract Introduction PF-06881894 is a proposed biosimilar... |
PMC9308487 | core_pubmed_pmc | Tinzaparin—a review of its molecular profile, pharmacology, special properties, and clinical uses | Tinzaparin—a review of its molecular profile, pharmacology, special properties, and clinical uses Abstract Purpose Low molecular weight heparins (LMWHs) are a group of heterogenous moieties, long used in the prevention and treatment of thrombosis. They derive from heparin and since they are prepared by different method... |
PMC7558015 | core_pubmed_pmc | Enhanced Intestinal Absorption and Pharmacokinetic Modulation of Berberine and Its Metabolites through the Inhibition of P-Glycoprotein and Intestinal Metabolism in Rats Using a Berberine Mixed Micelle Formulation | Enhanced Intestinal Absorption and Pharmacokinetic Modulation of Berberine and Its Metabolites through the Inhibition of P-Glycoprotein and Intestinal Metabolism in Rats Using a Berberine Mixed Micelle Formulation Abstract Abstract We aimed to develop a berberine formulation to enhance the intestinal absorption and pla... |
PMC6278556 | core_pubmed_pmc | An Accurate and Effective Method for Measuring Osimertinib by UPLC-TOF-MS and Its Pharmacokinetic Study in Rats | An Accurate and Effective Method for Measuring Osimertinib by UPLC-TOF-MS and Its Pharmacokinetic Study in Rats Abstract Osimertinib, a new-generation inhibitor of the epidermal growth factor, has been used for the clinical treatment of advanced T790M mutation-positive tumors. In this research, an original analysis met... |
PMC11782443 | core_pubmed_pmc | Clinical Pharmacokinetics of N , N -Dimethyltryptamine (DMT): A Systematic Review and Post-hoc Analysis | Clinical Pharmacokinetics of N , N -Dimethyltryptamine (DMT): A Systematic Review and Post-hoc Analysis Abstract Abstract Background and objective N , N -Dimethyltryptamine (DMT) is currently being studied for its therapeutic potential in various psychiatric disorders. An understanding of its pharmacokinetics (PK) is e... |
PMC5771527 | core_pubmed_pmc | A 6-Month Open-Label Extension Study of Vortioxetine in Pediatric Patients with Depressive or Anxiety Disorders | A 6-Month Open-Label Extension Study of Vortioxetine in Pediatric Patients with Depressive or Anxiety Disorders Abstract Abstract Objectives: In this 6-month open-label extension (OLE) of NCT01491035 (a 14-day, open-label, pharmacokinetic/safety lead-in study), the long-term safety and tolerability of vortioxetine (5–2... |
PMC7021098 | core_pubmed_pmc | Pharmacokinetics and antiviral activity of cabotegravir and rilpivirine in cerebrospinal fluid following long-acting injectable administration in HIV-infected adults | Pharmacokinetics and antiviral activity of cabotegravir and rilpivirine in cerebrospinal fluid following long-acting injectable administration in HIV-infected adults Abstract Abstract Background Long-acting (LA) formulations of cabotegravir, an HIV integrase inhibitor, and rilpivirine, an NNRTI, are in development as m... |
PMC10562582 | core_pubmed_pmc | Probing the potential of bioactive compounds of millets as an inhibitor for lifestyle diseases: molecular docking and simulation-based approach | Probing the potential of bioactive compounds of millets as an inhibitor for lifestyle diseases: molecular docking and simulation-based approach Abstract Millets are becoming more popular as a healthy substitute for people with lifestyle disorders. They offer dietary fiber, polyphenols, fatty acids, minerals, vitamins, ... |
PMC8609173 | core_pubmed_pmc | An open-label, randomized, single intravenous dosing study to investigate the effect of fixed-dose combinations of tenofovir/lamivudine or atazanavir/ritonavir on the pharmacokinetics of remdesivir in Ugandan healthy volunteers (RemTLAR) | An open-label, randomized, single intravenous dosing study to investigate the effect of fixed-dose combinations of tenofovir/lamivudine or atazanavir/ritonavir on the pharmacokinetics of remdesivir in Ugandan healthy volunteers (RemTLAR) Abstract Abstract Background Remdesivir is a novel broad-spectrum antiviral therap... |
PMC12296118 | core_pubmed_pmc | Analytical development and application of a targeted liquid chromatography-tandem mass spectrometry assay for chimeric aducanumab | Analytical development and application of a targeted liquid chromatography-tandem mass spectrometry assay for chimeric aducanumab Abstract ABSTRACT A sensitive and specific liquid chromatography-tandem mass spectrometry assay was developed for the quantification of chimeric aducanumab (chAdu), a therapeutic antibody ta... |
PMC6966181 | core_pubmed_pmc | Consideration of a Credibility Assessment Framework in Model‐Informed Drug Development: Potential Application to Physiologically‐Based Pharmacokinetic Modeling and Simulation | Consideration of a Credibility Assessment Framework in Model‐Informed Drug Development: Potential Application to Physiologically‐Based Pharmacokinetic Modeling and Simulation Abstract Abstract The use of computational models in drug development has grown during the past decade. These model‐informed drug development (MI... |
PMC6972989 | core_pubmed_pmc | Assessment of the effects of immunogenicity on the pharmacokinetics, efficacy and safety of tildrakizumab † | Assessment of the effects of immunogenicity on the pharmacokinetics, efficacy and safety of tildrakizumab † Abstract Summary Background We evaluated antidrug antibody (ADA) development in patients with chronic plaque psoriasis from three clinical trials of tildrakizumab, a humanized anti‐interleukin‐23p19 monoclonal an... |
PMC7911155 | core_pubmed_pmc | Amoxicillin and Clarithromycin Mucoadhesive Delivery System for Helicobacter pylori Infection in a Mouse Model: Characterization, Pharmacokinetics, and Efficacy | Amoxicillin and Clarithromycin Mucoadhesive Delivery System for Helicobacter pylori Infection in a Mouse Model: Characterization, Pharmacokinetics, and Efficacy Abstract Abstract Helicobacter pylori is the main pathogen responsible for gastric ulcers and a predisposing factor of stomach cancer. Although current treatme... |
PMC12591097 | core_pubmed_pmc | Mechanistic Modeling of Intramuscular Administration of a Long-acting Injectable Accounting for Tissue Response At the Depot Site | Mechanistic Modeling of Intramuscular Administration of a Long-acting Injectable Accounting for Tissue Response At the Depot Site Abstract The tissue response to long-acting injectables (LAIs) suspension injection may impact the product in vivo performance. One such response is the formation of an inflammatory cell lay... |
PMC5703532 | core_pubmed_pmc | Establishment of an indirect ELISA for detection of the novel antifibrotic peptide M10 | Establishment of an indirect ELISA for detection of the novel antifibrotic peptide M10 Abstract Objective M10 is a ten amino acid peptide generated from the intracellular cytoplasmic tail of the hepatocyte growth factor (HGF) receptor c-Met following cleavage by caspase-3. Recently we reported that M10 interacts with S... |
PMC7179459 | core_pubmed_pmc | Pharmacokinetics of Two Chlorine-Substituted Bis-Pyridinium Mono-Aldoximes with Regenerating Effect on Butyrylcholinesterase | Pharmacokinetics of Two Chlorine-Substituted Bis-Pyridinium Mono-Aldoximes with Regenerating Effect on Butyrylcholinesterase Abstract Our aim was to find chlorine-substituted antidotes against organophosphate poisoning and compare their pharmacokinetics to their parent compound, K-203. White male Wistar rats were intra... |
PMC9303187 | core_pubmed_pmc | Pharmacokinetics, Safety, and Tolerability of Single and Multiple Doses of Isavuconazonium Sulfate in Healthy Adult Japanese Subjects | Pharmacokinetics, Safety, and Tolerability of Single and Multiple Doses of Isavuconazonium Sulfate in Healthy Adult Japanese Subjects Abstract Abstract Isavuconazonium sulfate is the water‐soluble prodrug of the novel, broad‐spectrum, triazole antifungal agent isavuconazole. This was a first‐in‐Japanese study assessing... |
PMC7558948 | core_pubmed_pmc | Vancomycin for Dialytic Therapy in Critically Ill Patients: Analysis of Its Reduction and the Factors Associated with Subtherapeutic Concentrations | Vancomycin for Dialytic Therapy in Critically Ill Patients: Analysis of Its Reduction and the Factors Associated with Subtherapeutic Concentrations Abstract Abstract This study aimed to evaluate the reduction in vancomycin through intermittent haemodialysis (IHD) and prolonged haemodialysis (PHD) in acute kidney injury... |
PMC8262647 | core_pubmed_pmc | Linker Design Impacts Antibody-Drug Conjugate Pharmacokinetics and Efficacy via Modulating the Stability and Payload Release Efficiency | Linker Design Impacts Antibody-Drug Conjugate Pharmacokinetics and Efficacy via Modulating the Stability and Payload Release Efficiency Abstract Abstract The development of antibody-drug conjugates (ADCs) has significantly been advanced in the past decade given the improvement of payloads, linkers and conjugation metho... |
PMC8653169 | core_pubmed_pmc | A Quantitative Modeling and Simulation Framework to Support Candidate and Dose Selection of Anti‐SARS‐CoV‐2 Monoclonal Antibodies to Advance Bamlanivimab Into a First‐in‐Human Clinical Trial | A Quantitative Modeling and Simulation Framework to Support Candidate and Dose Selection of Anti‐SARS‐CoV‐2 Monoclonal Antibodies to Advance Bamlanivimab Into a First‐in‐Human Clinical Trial Abstract Abstract Neutralizing monoclonal antibodies (mAb), novel therapeutics for the treatment of coronavirus disease 2019 (COV... |
PMC12910498 | core_pubmed_pmc | Bioisosteric Replacement of Amides with 1,2,3-Triazoles Improves Dopamine D4 Receptor Ligand Pharmacokinetics | Bioisosteric Replacement of Amides with 1,2,3-Triazoles Improves Dopamine D4 Receptor Ligand Pharmacokinetics Abstract Dopamine D4 receptor (D 4 R) signaling affects decision-making, memory formation, cognition, and attention. Previously developed D 4 R-selective ligands were metabolically unstable in vivo due to amide... |
PMC7022573 | core_pubmed_pmc | Development of Level A In Vitro–Vivo Correlation for Electrosprayed Microspheres Containing Leuprolide: Physicochemical, Pharmacokinetic, and Pharmacodynamic Evaluation | Development of Level A In Vitro–Vivo Correlation for Electrosprayed Microspheres Containing Leuprolide: Physicochemical, Pharmacokinetic, and Pharmacodynamic Evaluation Abstract Abstract This study optimized the preparation of electrosprayed microspheres containing leuprolide and developed an in vitro–in vivo correlati... |
PMC4795741 | core_pubmed_pmc | Charge Variants of an Avastin Biosimilar Isolation, Characterization, In Vitro Properties and Pharmacokinetics in Rat | Charge Variants of an Avastin Biosimilar Isolation, Characterization, In Vitro Properties and Pharmacokinetics in Rat Abstract The similarity between a proposed biosimilar product and the reference product can be affected by many factors. This study is designed to examine whether any subtle difference in the distributi... |
PMC11203575 | core_pubmed_pmc | The First In Vivo Study Shows That Gyrophoric Acid Changes Behavior of Healthy Laboratory Rats | The First In Vivo Study Shows That Gyrophoric Acid Changes Behavior of Healthy Laboratory Rats Abstract Gyrophoric acid (GA), a lichen secondary metabolite, has attracted more attention during the last years because of its potential biological effects. Until now, its effect in vivo has not yet been demonstrated. The ai... |
PMC8120018 | core_pubmed_pmc | Evaluation of tradipitant, a selective NK1 antagonist, on response to oxycodone in humans | Evaluation of tradipitant, a selective NK1 antagonist, on response to oxycodone in humans Abstract Rationale Preclinical studies demonstrate that the NK1 receptor is involved in opioid reinforcement and withdrawal expression. Few studies have examined the impact of treatment with NK1 antagonists on opioid response in h... |
PMC3263713 | core_pubmed_pmc | Pharmacokinetic Compatibility Study of Lidocaine with EXPAREL in Yucatan Miniature Pigs | Pharmacokinetic Compatibility Study of Lidocaine with EXPAREL in Yucatan Miniature Pigs Abstract We explored the potential for EXPAREL to interact with lidocaine. Sixty (60) male Yucatan Swine were randomized into 20 groups ( N = 3/group). EXPAREL (2 or 4 mg/kg) and/or lidocaine HCl solution 1% or 2% (with epinephrine ... |
PMC4010641 | core_pubmed_pmc | Formulation development for the orexin receptor antagonist almorexant: assessment in two clinical studies | Formulation development for the orexin receptor antagonist almorexant: assessment in two clinical studies Abstract Almorexant, a dual orexin receptor antagonist, was investigated for the treatment of insomnia. The following observations initiated further formulation development: the active pharmaceutical ingredient (AP... |
PMC10160475 | core_pubmed_pmc | Biological evaluation and in silico studies of novel compounds as potent TAAR1 agonists that could be used in schizophrenia treatment | Biological evaluation and in silico studies of novel compounds as potent TAAR1 agonists that could be used in schizophrenia treatment Abstract Abstract Introduction: Schizophrenia is a serious mental illness that requires effective treatment with minimal adverse effects. As preclinical and clinical research progresses,... |
PMC5709458 | core_pubmed_pmc | Pharmacokinetics and Safety of Amenamevir in Healthy Subjects: Analysis of Four Randomized Phase 1 Studies | Pharmacokinetics and Safety of Amenamevir in Healthy Subjects: Analysis of Four Randomized Phase 1 Studies Abstract Introduction Amenamevir (ASP2151) is a nonnucleoside antiherpesvirus compound available for the treatment of varicella–zoster virus infections. In this article we summarize the findings of four phase 1 st... |
PMC12847613 | core_pubmed_pmc | [ 177 Lu]Lu-DOTA-TATE tumour and organ time-activity curves: prediction from a single-time-point [ 68 Ga]Ga-DOTA-TATE PET/CT measurement | [ 177 Lu]Lu-DOTA-TATE tumour and organ time-activity curves: prediction from a single-time-point [ 68 Ga]Ga-DOTA-TATE PET/CT measurement Abstract Aim Predicting the time-activity curve (TAC) of [ 177 Lu]Lu-DOTA-TATE for organs at risk and neuroendocrine tumours (NETs) is an essential element in the calculation of the a... |
PMC6768310 | core_pubmed_pmc | Effect of renal function and dialysis modality on daprodustat and predominant metabolite exposure | Effect of renal function and dialysis modality on daprodustat and predominant metabolite exposure Abstract Abstract Background Current therapies for anemia of chronic kidney disease (CKD) include administration of supplemental iron (intravenous and/or oral), blood transfusions and replacement of erythropoietin through ... |
PMC8484235 | core_pubmed_pmc | A randomized, double-blind, single-dose study (LAVENDER) to assess the safety, tolerability, pharmacokinetics, and immunogenicity of a combined infusion of ABP 980 and pertuzumab in healthy subjects | A randomized, double-blind, single-dose study (LAVENDER) to assess the safety, tolerability, pharmacokinetics, and immunogenicity of a combined infusion of ABP 980 and pertuzumab in healthy subjects Abstract Purpose ABP 980 (KANJINTI ™ ) is a biosimilar to reference product HERCEPTIN ® (trastuzumab RP). The goal of thi... |
PMC5892888 | core_pubmed_pmc | Pharmacokinetics and interspecies scaling of a novel, orally-bioavailable anti-cancer drug, SHetA2 | Pharmacokinetics and interspecies scaling of a novel, orally-bioavailable anti-cancer drug, SHetA2 Abstract Abstract SHetA2 is a small molecule drug with promising cancer prevention and therapeutic activity and a high preclinical safety profile. The study objectives were to perform interspecies scaling and pharmacokine... |
PMC6377609 | core_pubmed_pmc | Impact of post-hatching maturation on the pharmacokinetics of paracetamol in zebrafish larvae | Impact of post-hatching maturation on the pharmacokinetics of paracetamol in zebrafish larvae Abstract Zebrafish larvae are increasingly used in pharmacological and toxicological studies, but it is often overlooked that internal exposure to exogenous compounds, rather than the incubation medium concentration, is drivin... |
PMC6132848 | core_pubmed_pmc | A phase 1 dose-escalation study on the safety, tolerability and activity of liposomal curcumin (Lipocurc ™ ) in patients with locally advanced or metastatic cancer | A phase 1 dose-escalation study on the safety, tolerability and activity of liposomal curcumin (Lipocurc ™ ) in patients with locally advanced or metastatic cancer Abstract Purpose This study was conducted to investigate the safety and tolerability of increasing doses of liposomal curcumin in patients with metastatic c... |
PMC6105181 | core_pubmed_pmc | Excipients in Neonatal Medicinal Products: Never Prescribed, Commonly Administered | Excipients in Neonatal Medicinal Products: Never Prescribed, Commonly Administered Abstract To attain effective and safe pharmacotherapy, formulations in (pre)term neonates should enable extensive dose flexibility. During product development and subsequent authorization and clinical use of such formulations, there is a... |
PMC3395249 | core_pubmed_pmc | The Difference in Pharmacokinetics and Pharmacodynamics between Extended-Release Fluvastatin and Immediate-Release Fluvastatin in Healthy Chinese Subjects | The Difference in Pharmacokinetics and Pharmacodynamics between Extended-Release Fluvastatin and Immediate-Release Fluvastatin in Healthy Chinese Subjects Abstract Abstract The aim of this study was to evaluate the difference in pharmacokinetics and pharmacodynamics between extended-release (ER) fluvastatin tablet and ... |
PMC7137270 | core_pubmed_pmc | Determination of parecoxib and valdecoxib in rat plasma by UPLC-MS/MS and its application to pharmacokinetics studies | Determination of parecoxib and valdecoxib in rat plasma by UPLC-MS/MS and its application to pharmacokinetics studies Abstract Abstract Background The present study aimed to develop and validate a rapid, selective, and reproducible ultra-performance liquid chromatography-tandem mass spectrometry separation method for t... |
PMC12845190 | core_pubmed_pmc | In Silico Investigation of Amidine-Based BACE-1 Inhibitors Against Alzheimer’s Disease: SAR, Pharmacokinetics, Molecular Docking and Dynamic Simulations | In Silico Investigation of Amidine-Based BACE-1 Inhibitors Against Alzheimer’s Disease: SAR, Pharmacokinetics, Molecular Docking and Dynamic Simulations Abstract Abstract Background/Objective: Alzheimer’s disease (AD) is characterized by the accumulation of amyloid-β plaques, derived from the amyloid precursor protein ... |
PMC8841449 | core_pubmed_pmc | No implication of HIV coinfection on the plasma exposure to rifampicin, pyrazinamide, and ethambutol in tuberculosis patients | No implication of HIV coinfection on the plasma exposure to rifampicin, pyrazinamide, and ethambutol in tuberculosis patients Abstract Abstract There are contrasting findings regarding the effect of HIV on the pharmacokinetics of first‐line anti‐tubercular drugs (FLATDs) due to a lack of prospective controlled clinical... |
PMC7412073 | core_pubmed_pmc | Pharmacokinetics and Metabolism of Liposome-Encapsulated 2,4,6-Trihydroxygeranylacetophenone in Rats Using High-Resolution Orbitrap Liquid Chromatography Mass Spectrometry | Pharmacokinetics and Metabolism of Liposome-Encapsulated 2,4,6-Trihydroxygeranylacetophenone in Rats Using High-Resolution Orbitrap Liquid Chromatography Mass Spectrometry Abstract Abstract 2,4,6-trihydroxy-3-geranylacetophenone (tHGA) is a bioactive compound that shows excellent anti-inflammatory properties. However, ... |
PMC4430599 | core_pubmed_pmc | Population pharmacokinetics of intravenous and oral panobinostat in patients with hematologic and solid tumors | Population pharmacokinetics of intravenous and oral panobinostat in patients with hematologic and solid tumors Abstract Purpose The study aimed to characterize the population pharmacokinetics of panobinostat, a pan-deacetylase inhibitor that has demonstrated efficacy in combination with bortezomib and dexamethasone in ... |
PMC9823476 | core_pubmed_pmc | Highly Biocompatible Apigenin-Loaded Silk Fibroin Nanospheres: Preparation, Characterization, and Anti-Breast-Cancer Activity | Highly Biocompatible Apigenin-Loaded Silk Fibroin Nanospheres: Preparation, Characterization, and Anti-Breast-Cancer Activity Abstract Breast cancer is among the most common fatal diseases among women. Low-toxicity apigenin (AGN) is of interest due to its good antitumor activity, but its clinical application is severel... |
PMC2887170 | core_pubmed_pmc | Revisiting the loading dose of amikacin for patients with severe sepsis and septic shock | Revisiting the loading dose of amikacin for patients with severe sepsis and septic shock Abstract Abstract Introduction It has been proposed that doses of amikacin of >15 mg/kg should be used in conditions associated with an increased volume of distribution (V d ), such as severe sepsis and septic shock. The primary ai... |
PMC7373158 | core_pubmed_pmc | Saddle-Reset for Robust Parameter Estimation and Identifiability Analysis of Nonlinear Mixed Effects Models | Saddle-Reset for Robust Parameter Estimation and Identifiability Analysis of Nonlinear Mixed Effects Models Abstract Abstract Parameter estimation of a nonlinear model based on maximizing the likelihood using gradient-based numerical optimization methods can often fail due to premature termination of the optimization a... |
PMC3183248 | core_pubmed_pmc | In vivo quantification of photosensitizer fluorescence in the skin-fold observation chamber using dual-wavelength excitation and NIR imaging | In vivo quantification of photosensitizer fluorescence in the skin-fold observation chamber using dual-wavelength excitation and NIR imaging Abstract A major challenge in biomedical optics is the accurate quantification of in vivo fluorescence images. Fluorescence imaging is often used to determine the pharmacokinetics... |
PMC9495055 | core_pubmed_pmc | Variability in Biological Activities of Satureja montana Subsp. montana and Subsp. variegata Based on Different Extraction Methods | Variability in Biological Activities of Satureja montana Subsp. montana and Subsp. variegata Based on Different Extraction Methods Abstract Abstract Winter savory ( Satureja montana L.) is a well-known spice and medicinal plant with a wide range of activities and applications. Two subspecies of S. montana , subsp. mont... |
PMC6188018 | core_pubmed_pmc | Open field and a behavior score in PNT model for neuropathic pain in pigs | Open field and a behavior score in PNT model for neuropathic pain in pigs Abstract Background Rodent models are frequently used in the research of pain and continue to provide valuable data on the mechanisms driving pain, although they are criticized due to limited translational ability to human conditions. Previously ... |
PMC7295442 | core_pubmed_pmc | Phase IA/IB study of single-agent tislelizumab, an investigational anti-PD-1 antibody, in solid tumors | Phase IA/IB study of single-agent tislelizumab, an investigational anti-PD-1 antibody, in solid tumors Abstract Abstract Background The programmed cell death-1/programmed cell death ligand-1 (PD-1/PD-L1) axis plays a central role in suppressing antitumor immunity; axis dysregulation can be used by cancer cells to evade... |
PMC11581172 | core_pubmed_pmc | Exploring the potential of Fargesin from Chrysanthemum indicum for chronic migraine: in-silico and pharmacokinetic study | Exploring the potential of Fargesin from Chrysanthemum indicum for chronic migraine: in-silico and pharmacokinetic study Abstract Abstract Introduction Chronic migraine is recognized by the WHO as one of the most debilitating chronic conditions. It is primarily caused by central sensitization of the trigeminal nucleus ... |
PMC5460445 | core_pubmed_pmc | Pharmacokinetic Comparison of 20(R)- and 20(S)-Ginsenoside Rh1 and 20(R)- and 20(S)-Ginsenoside Rg3 in Rat Plasma following Oral Administration of Radix Ginseng Rubra and Sheng-Mai-San Extracts | Pharmacokinetic Comparison of 20(R)- and 20(S)-Ginsenoside Rh1 and 20(R)- and 20(S)-Ginsenoside Rg3 in Rat Plasma following Oral Administration of Radix Ginseng Rubra and Sheng-Mai-San Extracts Abstract Abstract Ginsenosides Rh1 and Rg3, as the main bioactive components from Ginseng, are effective for prevention and tr... |
PMC6226115 | core_pubmed_pmc | Evaluation of Pharmacokinetics and Pharmacodynamics of BI 425809, a Novel GlyT1 Inhibitor: Translational Studies | Evaluation of Pharmacokinetics and Pharmacodynamics of BI 425809, a Novel GlyT1 Inhibitor: Translational Studies Abstract Abstract BI 425809 is a potent and selective glycine transporter 1 (GlyT1) inhibitor being developed for the treatment of cognitive impairment in Alzheimer disease and schizophrenia. Translational s... |
PMC5697569 | core_pubmed_pmc | Population Pharmacokinetics of Liposomal Irinotecan in Patients With Cancer | Population Pharmacokinetics of Liposomal Irinotecan in Patients With Cancer Abstract Nanoliposomal irinotecan (nal‐IRI) is a liposomal formulation of irinotecan with a longer half‐life (t 1/2 ), higher plasma total irinotecan (tIRI), and lower SN‐38 maximum concentration ( C max ) compared with nonliposomal irinotecan.... |
PMC9356050 | core_pubmed_pmc | Pharmacokinetic and metabolomic studies with a BIO 300 Oral Powder formulation in nonhuman primates | Pharmacokinetic and metabolomic studies with a BIO 300 Oral Powder formulation in nonhuman primates Abstract Abstract BIO 300, a pharmaceutical formulation of genistein, is being developed as a radiation countermeasure to treat hematopoietic acute radiation syndrome (H-ARS) and the delayed effects of acute radiation ex... |
PMC8533253 | core_pubmed_pmc | Bis-thiobarbiturates as Promising Xanthine Oxidase Inhibitors: Synthesis and Biological Evaluation | Bis-thiobarbiturates as Promising Xanthine Oxidase Inhibitors: Synthesis and Biological Evaluation Abstract Abstract Xanthine oxidase (XO) is the enzyme responsible for the conversion of endogenous purines into uric acid. Therefore, this enzyme has been associated with pathological conditions caused by hyperuricemia, s... |
PMC11469166 | core_pubmed_pmc | Comprehensive Pharmacokinetic Evaluation of High Melanin Binder Levofloxacin in Rabbits Shows Potential of Topical Eye Drops for Posterior Segment Treatment | Comprehensive Pharmacokinetic Evaluation of High Melanin Binder Levofloxacin in Rabbits Shows Potential of Topical Eye Drops for Posterior Segment Treatment Abstract Abstract Purpose The purpose of this work was to understand the impact of melanin binding on ocular pharmacokinetics after administration of a high-binder... |
PMC10421414 | core_pubmed_pmc | Tectorigenin: A Review of Its Sources, Pharmacology, Toxicity, and Pharmacokinetics | Tectorigenin: A Review of Its Sources, Pharmacology, Toxicity, and Pharmacokinetics Abstract Abstract Tectorigenin is a well-known natural flavonoid aglycone and an active component that exists in numerous plants. Growing evidence suggests that tectorigenin has multiple pharmacological effects, such as anticancer, anti... |
PMC10502450 | core_pubmed_pmc | A Phase I, Multicenter, Open-Label, First-in-Human Study of DS-6157a in Patients with Advanced Gastrointestinal Stromal Tumor | A Phase I, Multicenter, Open-Label, First-in-Human Study of DS-6157a in Patients with Advanced Gastrointestinal Stromal Tumor Abstract Abstract Purpose: To evaluate DS-6157a, an antibody–drug conjugate targeting G protein–coupled receptor 20 (GPR20), in gastrointestinal stromal tumors (GIST). Patients and Methods: In t... |
PMC9731835 | core_pubmed_pmc | Pharmaceutical and pharmacological studies of Shen Ma Yi Zhi granule for prevention of vascular dementia: A review | Pharmaceutical and pharmacological studies of Shen Ma Yi Zhi granule for prevention of vascular dementia: A review Abstract Background: With dementia significantly increasing hospitalization and disability rates, worldwide aging of the population presents major challenges to public health. The majority of cases of cogn... |
PMC6026642 | core_pubmed_pmc | Comparative Pharmacokinetics and Preliminary Pharmacodynamics Evaluation of Piscidin 1 Against PRV and PEDV in Rats | Comparative Pharmacokinetics and Preliminary Pharmacodynamics Evaluation of Piscidin 1 Against PRV and PEDV in Rats Abstract Antimicrobial peptide (Piscidin-1) is an effective natural polypeptide, which has great influence and potential on porcine epidemic diarrhea virus (PEDV) and pseudorabies virus (PRV). As an alter... |
PMC4562165 | core_pubmed_pmc | Organ Impairment—Drug–Drug Interaction Database: A Tool for Evaluating the Impact of Renal or Hepatic Impairment and Pharmacologic Inhibition on the Systemic Exposure of Drugs | Organ Impairment—Drug–Drug Interaction Database: A Tool for Evaluating the Impact of Renal or Hepatic Impairment and Pharmacologic Inhibition on the Systemic Exposure of Drugs Abstract The organ impairment and drug–drug interaction (OI-DDI) database is the first rigorously assembled database of pharmacokinetic drug exp... |
PMC6130517 | core_pubmed_pmc | Effects of triptolide on pharmacokinetics of amlodipine in rats by using LC–MS/MS | Effects of triptolide on pharmacokinetics of amlodipine in rats by using LC–MS/MS Abstract Abstract Context: Triptolide and amlodipine are often simultaneously used for reducing urine protein excretion after renal transplantation in China clinics. Objective: This study investigated the effects of triptolide on the phar... |
PMC9283749 | core_pubmed_pmc | Model‐based dose selection to inform translational clinical oncology development of WNT974, a first‐in‐class Porcupine inhibitor | Model‐based dose selection to inform translational clinical oncology development of WNT974, a first‐in‐class Porcupine inhibitor Abstract Abstract WNT974 is a potent, selective, and orally bioavailable first‐in‐class inhibitor of Porcupine, a membrane‐bound O‐acyltransferase required for Wnt secretion, currently under ... |
PMC12047507 | core_pubmed_pmc | Phase 1 study of IMCnyeso, a T cell receptor bispecific ImmTAC targeting NY-ESO-1-expressing malignancies | Phase 1 study of IMCnyeso, a T cell receptor bispecific ImmTAC targeting NY-ESO-1-expressing malignancies Abstract Summary IMCnyeso, an immune mobilizing monoclonal T cell receptor against cancer (ImmTAC) bispecific (New York esophageal squamous cell carcinoma [NY-ESO]×CD3) T cell engager, targets an NY-ESO-1/L-antigen... |
PMC11537160 | core_pubmed_pmc | Investigating the Potency of Erythrina‒Derived Flavonoids as Cholinesterase Inhibitors and Free Radical Scavengers Through in silico Approach: Implications for Alzheimer’s Disease Therapy | Investigating the Potency of Erythrina‒Derived Flavonoids as Cholinesterase Inhibitors and Free Radical Scavengers Through in silico Approach: Implications for Alzheimer’s Disease Therapy Abstract Purpose This study aimed to evaluate the potency of 471 flavonoids from the genus Erythrina as potential acetylcholinestera... |
PMC9006931 | core_pubmed_pmc | Altered Response Pattern following AZD5582 Treatment of SIV-Infected, ART-Suppressed Rhesus Macaque Infants | Altered Response Pattern following AZD5582 Treatment of SIV-Infected, ART-Suppressed Rhesus Macaque Infants Abstract ABSTRACT The “shock and kill” strategy for HIV-1 cure incorporates latency-reversing agents (LRA) in combination with interventions that aid the host immune system in clearing virally reactivated cells. ... |
PMC3965102 | core_pubmed_pmc | DrugBank 4.0: shedding new light on drug metabolism | DrugBank 4.0: shedding new light on drug metabolism Abstract Abstract DrugBank ( http://www.drugbank.ca ) is a comprehensive online database containing extensive biochemical and pharmacological information about drugs, their mechanisms and their targets. Since it was first described in 2006, DrugBank has rapidly evolve... |
PMC6706648 | core_pubmed_pmc | Epilepsy in the Elderly: Treatment and Consideration of Comorbid Diseases | Epilepsy in the Elderly: Treatment and Consideration of Comorbid Diseases Abstract Epilepsy is the third most common neurological disorder affecting older adults after stroke and dementia, and the incidence of epilepsy is increasing rapidly in this population. A further increase in the incidence and prevalence of epile... |
PMC3443097 | core_pubmed_pmc | Evolution of Bombesin Conjugates for Targeted PET Imaging of Tumors | Evolution of Bombesin Conjugates for Targeted PET Imaging of Tumors Abstract Bombesin receptors are under intense investigation as molecular targets since they are overexpressed in several prevalent solid tumors. We rationally designed and synthesized a series of modified bombesin (BN) peptide analogs to study the infl... |
PMC4100237 | core_pubmed_pmc | Therapeutic drug monitoring in a developing nation: a clinical guide | Therapeutic drug monitoring in a developing nation: a clinical guide Abstract Therapeutic drug monitoring is aimed at using drug concentration measurements to manage a patient’s medication requirement and optimise clinical outcome, particularly in respect of drugs with narrow therapeutic index. Typically, immunoassay m... |
PMC4444753 | core_pubmed_pmc | Quantitative global sensitivity analysis of a biologically based dose-response pregnancy model for the thyroid endocrine system | Quantitative global sensitivity analysis of a biologically based dose-response pregnancy model for the thyroid endocrine system Abstract Abstract A deterministic biologically based dose-response model for the thyroidal system in a near-term pregnant woman and the fetus was recently developed to evaluate quantitatively ... |
PMC11047589 | core_pubmed_pmc | Pharmacokinetics of Enrofloxacin in Plasma, Urine, and Feces of Donkey ( Equus asinus ) after a Single Intragastric Administration | Pharmacokinetics of Enrofloxacin in Plasma, Urine, and Feces of Donkey ( Equus asinus ) after a Single Intragastric Administration Abstract Abstract Enrofloxacin is a broad-spectrum antimicrobial agent, but the study of its pharmacokinetics/pharmacodynamics (PKs/PDs) in donkeys is rarely reported. The present study aim... |
PMC11374527 | core_pubmed_pmc | Population pharmacokinetic modeling of vedolizumab for graft‐versus‐host disease prophylaxis in adults with allogeneic hematopoietic stem cell transplant | Population pharmacokinetic modeling of vedolizumab for graft‐versus‐host disease prophylaxis in adults with allogeneic hematopoietic stem cell transplant Abstract Abstract We aimed to characterize the population pharmacokinetics (PK) of vedolizumab for acute graft‐versus‐host disease prophylaxis in adults undergoing al... |
PMC11282209 | core_pubmed_pmc | In-silico study unveils potential phytocompounds in Andrographis paniculata against E6 protein of the high-risk HPV-16 subtype for cervical cancer therapy | In-silico study unveils potential phytocompounds in Andrographis paniculata against E6 protein of the high-risk HPV-16 subtype for cervical cancer therapy Abstract Despite therapeutic advancements, cervical cancer caused by high-risk subtypes of the human papillomavirus (HPV) remains a leading cause of cancer-related d... |
PMC7351663 | core_pubmed_pmc | Inflammation is a major regulator of drug metabolizing enzymes and transporters: Consequences for the personalization of drug treatment | Inflammation is a major regulator of drug metabolizing enzymes and transporters: Consequences for the personalization of drug treatment Abstract Abstract Inflammation is an evolutionary process that allows survival against acute infection or injury. Inflammation is also a pathophysiological condition shared by numerous... |
PMC8197573 | core_pubmed_pmc | Rupatadine Oral Solution Titration by Body Weight in Paediatric Patients Suffering from Allergic Rhinitis: A Population Pharmacokinetic Study | Rupatadine Oral Solution Titration by Body Weight in Paediatric Patients Suffering from Allergic Rhinitis: A Population Pharmacokinetic Study Abstract Background Allergic rhinitis (AR) and chronic urticaria, both are treated in children with doses of second generation of antihistamines that have been mostly based on ex... |
PMC9553789 | core_pubmed_pmc | Pharmacokinetic/Pharmacodynamic Evaluation of the Dipeptidyl Peptidase 1 Inhibitor Brensocatib for Non-cystic Fibrosis Bronchiectasis | Pharmacokinetic/Pharmacodynamic Evaluation of the Dipeptidyl Peptidase 1 Inhibitor Brensocatib for Non-cystic Fibrosis Bronchiectasis Abstract Background and Objective Brensocatib is an investigational, first-in-class, selective, and reversible dipeptidyl peptidase 1 inhibitor that blocks activation of neutrophil serin... |
PMC12691680 | core_pubmed_pmc | Comparison between cefepime and carbapenem therapy for deep-seated AmpC-producing Enterobacterales infections: a propensity-weighted retrospective cohort study | Comparison between cefepime and carbapenem therapy for deep-seated AmpC-producing Enterobacterales infections: a propensity-weighted retrospective cohort study Abstract ABSTRACT Deep-seated infections caused by AmpC-producing Enterobacterales (AmpC-E) pose challenges due to high bacterial burdens, altered pharmacokinet... |
PMC6590872 | core_pubmed_pmc | Impact of bovine respiratory disease on the pharmacokinetics of danofloxacin and tulathromycin in different ages of calves | Impact of bovine respiratory disease on the pharmacokinetics of danofloxacin and tulathromycin in different ages of calves Abstract Abstract Pneumonia is one of the most economically important respiratory diseases of calves and knowledge of the impact of clinical disease on pharmacokinetics (PK) in young calves is limi... |
PMC9099133 | core_pubmed_pmc | Safety, tolerability, and pharmacokinetics of single and multiple topical ophthalmic administration of imatinib mesylate in healthy subjects | Safety, tolerability, and pharmacokinetics of single and multiple topical ophthalmic administration of imatinib mesylate in healthy subjects Abstract Abstract For the long‐term efficacy of dry eye disease treatment, relieving underlying inflammation is necessary. Imatinib mesylate is a novel ophthalmic formulation of i... |
PMC5368456 | core_pubmed_pmc | A review of the fixed dose use of new oral anticoagulants in obese patients: Is it really enough? | A review of the fixed dose use of new oral anticoagulants in obese patients: Is it really enough? Abstract Abstract Obesity is a significant cause of morbidity and mortality, and it is becoming increasingly prevalent worldwide. Altered pharmacodynamics and pharmacokinetics of drugs in obese patients require dose adjust... |
PMC6065210 | core_pubmed_pmc | Pharmacokinetics, Safety, and Clinical Efficacy of Cannabidiol Treatment in Osteoarthritic Dogs | Pharmacokinetics, Safety, and Clinical Efficacy of Cannabidiol Treatment in Osteoarthritic Dogs Abstract Objectives: The objectives of this study were to determine basic oral pharmacokinetics, and assess safety and analgesic efficacy of a cannabidiol (CBD) based oil in dogs with osteoarthritis (OA). Methods: Single-dos... |
PMC4318582 | core_pubmed_pmc | Chemotherapy of Second Stage Human African Trypanosomiasis: Comparison between the Parenteral Diamidine DB829 and Its Oral Prodrug DB868 in Vervet Monkeys | Chemotherapy of Second Stage Human African Trypanosomiasis: Comparison between the Parenteral Diamidine DB829 and Its Oral Prodrug DB868 in Vervet Monkeys Abstract Human African trypanosomiasis (HAT, sleeping sickness) ranks among the most neglected tropical diseases based on limited availability of drugs that are safe... |
PMC10788798 | core_pubmed_pmc | A rapid and simple HPLC-MS/MS method for the therapeutic drug monitoring of six special-grade antimicrobials in pediatric patients | A rapid and simple HPLC-MS/MS method for the therapeutic drug monitoring of six special-grade antimicrobials in pediatric patients Abstract Meropenem, linezolid, fluconazole, voriconazole, posaconazole, and vancomycin are six important antimicrobials used for severe infections in critically ill patients listed in speci... |
PMC12767260 | core_pubmed_pmc | Pinocembrin as a novel anti-cancer agent: Exploring preclinical evidence along with therapeutic potential | Pinocembrin as a novel anti-cancer agent: Exploring preclinical evidence along with therapeutic potential Abstract Abstract Pinocembrin (PB) (5,7-dihydroxy flavanone) is a naturally occurring flavonoid sourced from propolis and Pinus spp., with the formula C 15 H 12 O 4 and moderate lipophilicity (log P approximately 2... |
PMC9852671 | core_pubmed_pmc | A novel solvent-free co-grinding preparation improves curcumin bioavailability in healthy volunteers: A single-center crossover study | A novel solvent-free co-grinding preparation improves curcumin bioavailability in healthy volunteers: A single-center crossover study Abstract Curcumin, from the rhizome of turmeric ( Curcuma longa L.), has a wide variety of biological activities. Unfortunately, its poor water-solubility greatly limits its bioavailabil... |
PMC3904756 | core_pubmed_pmc | Practical management of patients on apixaban: a consensus guide | Practical management of patients on apixaban: a consensus guide Abstract Background Atrial fibrillation (AF) is a common tachyarrhythmia in Australia, with a prevalence over 10% in older patients. AF is the leading preventable cause of ischaemic stroke, and strokes due to AF have a higher mortality and morbidity. Strok... |
PMC12017572 | core_pubmed_pmc | Optimal adaptive cancer therapy based on evolutionary game theory | Optimal adaptive cancer therapy based on evolutionary game theory Abstract Abstract Cancer development is a dynamic and continuously evolving process, with the emergence of drug-resistant cancer cells being one of the primary reasons for the failure of traditional treatments. Adaptive therapy, as an emerging cancer tre... |
PMC6760680 | core_pubmed_pmc | Recommendations for the design of therapeutic trials for neonatal seizures | Recommendations for the design of therapeutic trials for neonatal seizures Abstract Although seizures have a higher incidence in neonates than any other age group and are associated with significant mortality and neurodevelopmental disability, treatment is largely guided by physician preference and tradition, due to a ... |
PMC6864408 | core_pubmed_pmc | Rezafungin treatment in mouse models of invasive candidiasis and aspergillosis: Insights on the PK/PD pharmacometrics of rezafungin efficacy | Rezafungin treatment in mouse models of invasive candidiasis and aspergillosis: Insights on the PK/PD pharmacometrics of rezafungin efficacy Abstract Abstract Rezafungin acetate is a novel echinocandin in clinical development for prevention and treatment of invasive fungal infections. Rezafungin is differentiated by a ... |
PMC10560721 | core_pubmed_pmc | Orally administered low-molecular weight agaro-oligosaccharides are absorbed into the plasma of healthy humans | Orally administered low-molecular weight agaro-oligosaccharides are absorbed into the plasma of healthy humans Abstract Abstract Agaro-oligosaccharides (AOSs) are known to have biological activities, such as anti-inflammatory, anti-tumor, and anti-obesity effects. Although existing evidence suggests the presence of AOS... |
PMC4551303 | core_pubmed_pmc | Determination and Validation of a Solid-phase Extraction Gas Chromatography-mass Spectrometry for the Quantification of Methadone and Its Principal Metabolite in Human Plasma | Determination and Validation of a Solid-phase Extraction Gas Chromatography-mass Spectrometry for the Quantification of Methadone and Its Principal Metabolite in Human Plasma Abstract This study aimed to develop a solid-phase extraction gas chromatography-selected ion monitoring-mass spectrometry method for the determi... |
Subsets and Splits
No community queries yet
The top public SQL queries from the community will appear here once available.