id stringlengths 9 11 | source stringclasses 1
value | title stringlengths 15 560 | text stringlengths 2k 153k |
|---|---|---|---|
PMC6151614 | core_pubmed_pmc | A Review on the Phytochemistry, Pharmacology, Pharmacokinetics and Toxicology of Geniposide, a Natural Product | A Review on the Phytochemistry, Pharmacology, Pharmacokinetics and Toxicology of Geniposide, a Natural Product Abstract Iridoid glycosides are natural products occurring widely in many herbal plants. Geniposide (C 17 H 24 O 10 ) is a well-known one, present in nearly 40 species belonging to various families, especially... |
PMC8306283 | core_pubmed_pmc | In Vitro Cell Toxicity and Intracellular Uptake of Doxorubicin Exposed as a Solution or Liposomes: Implications for Treatment of Hepatocellular Carcinoma | In Vitro Cell Toxicity and Intracellular Uptake of Doxorubicin Exposed as a Solution or Liposomes: Implications for Treatment of Hepatocellular Carcinoma Abstract Abstract Cytostatic effects of doxorubicin in clinically applied doses are often inadequate and limited by systemic toxicity. The main objective of this in v... |
PMC5905822 | core_pubmed_pmc | Tanshinol borneol ester on nanostructured lipid carriers has longer brain and systemic effector retention and better antioxidant activity in vivo | Tanshinol borneol ester on nanostructured lipid carriers has longer brain and systemic effector retention and better antioxidant activity in vivo Abstract Background Tanshinol borneol ester (DBZ) is a hybrid of danshensu (DSS) and borneol and has anti-ischemic activity in animals. However, its low water solubility and ... |
PMC8948939 | core_pubmed_pmc | Towards the Elucidation of the Pharmacokinetics of Voriconazole: A Quantitative Characterization of Its Metabolism | Towards the Elucidation of the Pharmacokinetics of Voriconazole: A Quantitative Characterization of Its Metabolism Abstract Abstract The small-molecule drug voriconazole (VRC) shows a complex and not yet fully understood metabolism. Consequently, its in vivo pharmacokinetics are challenging to predict, leading to thera... |
PMC6927763 | core_pubmed_pmc | Clinical pharmacology of vc-MMAE antibody–drug conjugates in cancer patients: learning from eight first-in-human Phase 1 studies | Clinical pharmacology of vc-MMAE antibody–drug conjugates in cancer patients: learning from eight first-in-human Phase 1 studies Abstract ABSTRACT vc-MMAE antibody–drug conjugates (ADCs) consist of a monoclonal antibody (mAb) covalently bound with a potent anti-mitotic toxin (MMAE) through a protease-labile valine-citr... |
PMC5923092 | core_pubmed_pmc | Verapamil Targets Membrane Energetics in Mycobacterium tuberculosis | Verapamil Targets Membrane Energetics in Mycobacterium tuberculosis Abstract ABSTRACT Mycobacterium tuberculosis kills more people than any other bacterial pathogen and is becoming increasingly untreatable due to the emergence of resistance. Verapamil, an FDA-approved calcium channel blocker, potentiates the effect of ... |
PMC12965820 | core_pubmed_pmc | Respiratory and Antinociceptive Effects of Nociceptin Receptor–µ-Opioid Receptor Agonist Cebranopadol versus Full Opioid Receptor Agonist Oxycodone: A Comparison in Healthy Volunteers | Respiratory and Antinociceptive Effects of Nociceptin Receptor–µ-Opioid Receptor Agonist Cebranopadol versus Full Opioid Receptor Agonist Oxycodone: A Comparison in Healthy Volunteers Abstract Abstract Background: The novel analgesic cebranopadol targets the nociceptin (NOP) and µ-opioid (MOP) receptors, acting as a no... |
PMC7472037 | core_pubmed_pmc | Safety, Tolerability, Pharmacokinetics, and Concentration-QTc Analysis of Tetrodotoxin: A Randomized, Dose Escalation Study in Healthy Adults | Safety, Tolerability, Pharmacokinetics, and Concentration-QTc Analysis of Tetrodotoxin: A Randomized, Dose Escalation Study in Healthy Adults Abstract Tetrodotoxin (TTX) is a highly specific voltage-gated sodium channel (VGSC) blocker in clinical evaluation as a peripheral-acting analgesic for chronic pain. This study ... |
PMC9303920 | core_pubmed_pmc | Pharmacokinetics, Safety, and Tolerability of NPC‐21, an Anti‐Cytomegalovirus Monoclonal Antibody, in Healthy Japanese and White Adult Men: A Randomized, Placebo‐Controlled, First‐in‐Human Phase 1 Study | Pharmacokinetics, Safety, and Tolerability of NPC‐21, an Anti‐Cytomegalovirus Monoclonal Antibody, in Healthy Japanese and White Adult Men: A Randomized, Placebo‐Controlled, First‐in‐Human Phase 1 Study Abstract Abstract NPC‐21 (EV2038) is a fully human monoclonal antibody that targets the antigenic domain 1 of glycopr... |
PMC5796108 | core_pubmed_pmc | Effects of Acanthopanax senticosus on Brain Injury Induced by Simulated Spatial Radiation in Mouse Model Based on Pharmacokinetics and Comparative Proteomics | Effects of Acanthopanax senticosus on Brain Injury Induced by Simulated Spatial Radiation in Mouse Model Based on Pharmacokinetics and Comparative Proteomics Abstract Abstract The active compounds in Acanthopanax senticosus (AS) have different pharmacokinetic characteristics in mouse models. C max and AUC of Acanthopan... |
PMC10459693 | core_pubmed_pmc | Toward Stability Enhancement of NTS 1 R-Targeted Radioligands: Structural Interventions on [ 99m Tc]Tc-DT1 | Toward Stability Enhancement of NTS 1 R-Targeted Radioligands: Structural Interventions on [ 99m Tc]Tc-DT1 Abstract Abstract The neurotensin subtype 1 receptor (NTS 1 R) is overexpressed in a number of human tumors, thereby representing a valid target for cancer theranostics with radiolabeled neurotensin (NT) analogs l... |
PMC6496156 | core_pubmed_pmc | Population Pharmacokinetic Analyses for Plazomicin Using Pooled Data from Phase 1, 2, and 3 Clinical Studies | Population Pharmacokinetic Analyses for Plazomicin Using Pooled Data from Phase 1, 2, and 3 Clinical Studies Abstract Plazomicin is an aminoglycoside with activity against multidrug-resistant Enterobacteriaceae . Plazomicin is dosed on a milligram-per-kilogram-of-body-weight basis and administered by a 30-min intraveno... |
PMC10058835 | core_pubmed_pmc | Analogues of Anticancer Natural Products: Chiral Aspects | Analogues of Anticancer Natural Products: Chiral Aspects Abstract Abstract Life is chiral, as its constituents consist, to a large degree, of optically active molecules, be they macromolecules (proteins, nucleic acids) or small biomolecules. Hence, these molecules interact disparately with different enantiomers of chir... |
PMC7382588 | core_pubmed_pmc | Pharmacokinetic Analysis of Huangqi Guizhi Wuwu Decoction on Blood and Brain Tissue in Rats with Normal and Cerebral Ischemia-Reperfusion Injury by Microdialysis with HPLC-MS/MS | Pharmacokinetic Analysis of Huangqi Guizhi Wuwu Decoction on Blood and Brain Tissue in Rats with Normal and Cerebral Ischemia-Reperfusion Injury by Microdialysis with HPLC-MS/MS Abstract Objective The aim of our research was to analyze and compare the pharmacokinetics of paeoniflorin, calycosin, calycosin-7-o-β-d-6-glu... |
PMC5928345 | core_pubmed_pmc | Physiologically-based pharmacokinetic predictions of intestinal BCRP-mediated drug interactions of rosuvastatin in Koreans | Physiologically-based pharmacokinetic predictions of intestinal BCRP-mediated drug interactions of rosuvastatin in Koreans Abstract It was recently reported that the C max and AUC of rosuvastatin increases when it is coadministered with telmisartan and cyclosporine. Rosuvastatin is known to be a substrate of OATP1B1, O... |
PMC10838962 | core_pubmed_pmc | Ceftazidime-avibactam induced renal disorders: past and present | Ceftazidime-avibactam induced renal disorders: past and present Abstract Abstract With the increasing prevalence of multidrug-resistant Gram-negative bacterial pathogens worldwide, antimicrobial resistance has become a significant public health concern. Ceftazidime-avibactam (CAZ-AVI) exhibited excellent in vitro activ... |
PMC9867137 | core_pubmed_pmc | Fractal Kinetic Implementation in Population Pharmacokinetic Modeling | Fractal Kinetic Implementation in Population Pharmacokinetic Modeling Abstract Compartment modeling is a widely accepted technique in the field of pharmacokinetic analysis. However, conventional compartment modeling is performed under a homogeneity assumption that is not a naturally occurring condition. Since the assum... |
PMC11165342 | core_pubmed_pmc | Advancing ophthalmic delivery of flurbiprofen via synergistic chiral resolution and ion-pairing strategies | Advancing ophthalmic delivery of flurbiprofen via synergistic chiral resolution and ion-pairing strategies Abstract Flurbiprofen (FB), a nonsteroidal anti-inflammatory drug, is widely employed in treating ocular inflammation owing to its remarkable anti-inflammatory effects. However, the racemic nature of its commercia... |
PMC11651168 | core_pubmed_pmc | Effective, but Safe? Physiologically Based Pharmacokinetic (PBPK)-Modeling-Based Dosing Study of Molnupiravir for Risk Assessment in Pediatric Subpopulations | Effective, but Safe? Physiologically Based Pharmacokinetic (PBPK)-Modeling-Based Dosing Study of Molnupiravir for Risk Assessment in Pediatric Subpopulations Abstract Despite the end of COVID-19 pandemic, only intravenous remdesivir was approved for treatment of vulnerable pediatric populations. Molnupiravir is effecti... |
PMC3791487 | core_pubmed_pmc | The Role of Bystander Effects in the Antitumor Activity of the Hypoxia-Activated Prodrug PR-104 | The Role of Bystander Effects in the Antitumor Activity of the Hypoxia-Activated Prodrug PR-104 Abstract Abstract Activation of prodrugs in tumors (e.g., by bioreduction in hypoxic zones) has the potential to generate active metabolites that can diffuse within the tumor microenvironment. Such “bystander effects” may of... |
PMC8915351 | core_pubmed_pmc | Safety and pharmacokinetics-pharmacodynamics of a shorter tuberculosis treatment with high-dose pyrazinamide and rifampicin: a study protocol of a phase II clinical trial (HighShort-RP) | Safety and pharmacokinetics-pharmacodynamics of a shorter tuberculosis treatment with high-dose pyrazinamide and rifampicin: a study protocol of a phase II clinical trial (HighShort-RP) Abstract Abstract Introduction Increased dosing of rifampicin and pyrazinamide seems a viable strategy to shorten treatment and preven... |
PMC12470701 | core_pubmed_pmc | Current and Emerging Sedation Practices for Colonoscopy: A Narrative Review of Pharmacological Agents, High-Risk Populations, and Safety Considerations | Current and Emerging Sedation Practices for Colonoscopy: A Narrative Review of Pharmacological Agents, High-Risk Populations, and Safety Considerations Abstract Abstract Colonoscopy is the gold standard for colorectal cancer screening and diagnosis of gastrointestinal disorders, yet the procedure can still provoke anxi... |
PMC12077675 | core_pubmed_pmc | Design, optimization, and ADMET evaluation of S11a-0000168202: A promising LIMK1 inhibitor for gastric cancer treatment | Design, optimization, and ADMET evaluation of S11a-0000168202: A promising LIMK1 inhibitor for gastric cancer treatment Abstract Abstract This study focuses on the development and optimization of S11a-0000168202, a novel LIMK1 inhibitor with potential therapeutic applications in gastric cancer. Through scaffold hopping... |
PMC12300792 | core_pubmed_pmc | A Parent–Metabolite Middle-Out PBPK Model for Genistein and Its Glucuronide Metabolite in Rats: Integrating Liver and Enteric Metabolism with Hepatobiliary and Enteroluminal Transport to Assess Glucuronide Recycling | A Parent–Metabolite Middle-Out PBPK Model for Genistein and Its Glucuronide Metabolite in Rats: Integrating Liver and Enteric Metabolism with Hepatobiliary and Enteroluminal Transport to Assess Glucuronide Recycling Abstract Abstract Background : Glucuronide recycling in the gut and liver profoundly affects the systemi... |
PMC9037180 | core_pubmed_pmc | Ligand-based design and synthesis of N' -Benzylidene-3,4-dimethoxybenzohydrazide derivatives as potential antimicrobial agents; evaluation by in vitro , in vivo, and in silico approaches with SAR studies | Ligand-based design and synthesis of N' -Benzylidene-3,4-dimethoxybenzohydrazide derivatives as potential antimicrobial agents; evaluation by in vitro , in vivo, and in silico approaches with SAR studies Abstract Abstract Herein, a series of N' -benzylidene-3,4-dimethoxybenzohydrazide derivatives were designed and synt... |
PMC12590176 | core_pubmed_pmc | Valganciclovir for cytomegalovirus viraemia in advanced HIV disease: a phase 2b randomized placebo-controlled trial of valganciclovir for cytomegalovirus viraemia in adults and adolescents with advanced HIV disease | Valganciclovir for cytomegalovirus viraemia in advanced HIV disease: a phase 2b randomized placebo-controlled trial of valganciclovir for cytomegalovirus viraemia in adults and adolescents with advanced HIV disease Abstract Mortality among adults hospitalized with advanced HIV disease (AHD; CD4 <200 cells μl −1 or a WH... |
PMC12403037 | core_pubmed_pmc | Population pharmacokinetics/pharmacodynamics analysis confirming biosimilarity of SB16 to reference denosumab | Population pharmacokinetics/pharmacodynamics analysis confirming biosimilarity of SB16 to reference denosumab Abstract Abstract Background This analysis aims to evaluate the population pharmacokinetics (PK) and pharmacodynamics (PD) of denosumab and applied a population PK/PD approach to assess the biosimilarity of SB1... |
PMC12348157 | core_pubmed_pmc | Neuroprotective Evaluation of Murraya Carbazoles: In Vitro and Docking Insights into Their Anti-AChE and Anti-Aβ Activities | Neuroprotective Evaluation of Murraya Carbazoles: In Vitro and Docking Insights into Their Anti-AChE and Anti-Aβ Activities Abstract Abstract The present study investigated the neuroprotective potential of the Murraya carbazole derivatives murrayanol, mahanimbine, murrayafoline A, and 9-methyl-9H-carbazole-2-carbaldehy... |
PMC8487337 | core_pubmed_pmc | Ceftolozane/tazobactam probability of target attainment and outcomes in participants with augmented renal clearance from the randomized phase 3 ASPECT-NP trial | Ceftolozane/tazobactam probability of target attainment and outcomes in participants with augmented renal clearance from the randomized phase 3 ASPECT-NP trial Abstract Abstract Background The randomized, double-blind, phase 3 ASPECT-NP trial evaluated the efficacy of 3 g of ceftolozane/tazobactam (C/T) versus 1 g of m... |
PMC6017107 | core_pubmed_pmc | Effects of Phytochemical P-Glycoprotein Modulators on the Pharmacokinetics and Tissue Distribution of Doxorubicin in Mice | Effects of Phytochemical P-Glycoprotein Modulators on the Pharmacokinetics and Tissue Distribution of Doxorubicin in Mice Abstract Abstract Pungent spice constituents such as piperine, capsaicin and -gingerol consumed via daily diet or traditional Chinese medicine, have been reported to possess various pharmacological ... |
PMC11976485 | core_pubmed_pmc | In Silico Docking of Medicinal Herbs Against P. gingivalis for Chronic Periodontitis Intervention | In Silico Docking of Medicinal Herbs Against P. gingivalis for Chronic Periodontitis Intervention Abstract Objective This study aimed to explore the therapeutic potential of medicinal herbs for chronic periodontitis by examining the molecular interactions between specific herbal compounds and the heme-binding protein o... |
PMC11904618 | core_pubmed_pmc | Bayesian inference informed by parameter subset selection for a minimal PBPK brain model | Bayesian inference informed by parameter subset selection for a minimal PBPK brain model Abstract Physiologically based pharmacokinetic (PBPK) models use a mechanistic approach to delineate the processes of the absorption, distribution, metabolism and excretion of biological substances in various species. These models ... |
PMC8418595 | core_pubmed_pmc | Potential Antibiotics for the Treatment of Neonatal Sepsis Caused by Multidrug-Resistant Bacteria | Potential Antibiotics for the Treatment of Neonatal Sepsis Caused by Multidrug-Resistant Bacteria Abstract Abstract Neonatal sepsis causes up to an estimated 680,000 deaths annually worldwide, predominantly in low- and middle-income countries (LMICs). A significant and growing proportion of bacteria causing neonatal se... |
PMC6920759 | core_pubmed_pmc | Evaluation of the Effect of CYP2D6 Genotypes on Tramadol and O -Desmethyltramadol Pharmacokinetic Profiles in a Korean Population Using Physiologically-Based Pharmacokinetic Modeling | Evaluation of the Effect of CYP2D6 Genotypes on Tramadol and O -Desmethyltramadol Pharmacokinetic Profiles in a Korean Population Using Physiologically-Based Pharmacokinetic Modeling Abstract Abstract Tramadol is a μ-opioid receptor agonist and a monoamine reuptake inhibitor. O -desmethyltramadol (M1), the major active... |
PMC8772798 | core_pubmed_pmc | Ceftriaxone for the Treatment of Chronic Bacterial Prostatitis: A Case Series and Literature Review | Ceftriaxone for the Treatment of Chronic Bacterial Prostatitis: A Case Series and Literature Review Abstract Chronic bacterial prostatitis is increasingly difficult to treat due to rising antimicrobial resistance limiting oral treatment options. In this case series, 11 men with CBP (including patients with urological c... |
PMC3734254 | core_pubmed_pmc | Pharmacokinetics of Rifabutin in Japanese HIV-Infected Patients with or without Antiretroviral Therapy | Pharmacokinetics of Rifabutin in Japanese HIV-Infected Patients with or without Antiretroviral Therapy Abstract Abstract Objective Based on drug-drug interaction, dose reduction of rifabutin is recommended when co-administered with HIV protease inhibitors for human immunodeficiency virus (HIV)-associated mycobacterial ... |
PMC12958202 | core_pubmed_pmc | Shikonin nasal spray film preparation promoted the repair of nasal mucosal injury by the interaction of shikonin with interleukin-6 | Shikonin nasal spray film preparation promoted the repair of nasal mucosal injury by the interaction of shikonin with interleukin-6 Abstract Highlights • Shikonin nasal spray film (SNSF) promotes the repair of nasal mucosal injury. • SNSF activates the IL-17 signaling pathway. • IL-6 might be a potential target for SNS... |
PMC5741373 | core_pubmed_pmc | Hepatocellular carcinoma-targeted nanoparticles for cancer therapy | Hepatocellular carcinoma-targeted nanoparticles for cancer therapy Abstract Nanocarriers, such as liposomes, have the potential to increase the payload of chemotherapeutic drugs while decreasing toxicity to non-target tissues; such advantageous properties can be further enhanced through surface conjugation of nanocarri... |
PMC9027183 | core_pubmed_pmc | Natural Bioactive Compounds Targeting Histone Deacetylases in Human Cancers: Recent Updates | Natural Bioactive Compounds Targeting Histone Deacetylases in Human Cancers: Recent Updates Abstract Cancer is a complex pathology that causes a large number of deaths worldwide. Several risk factors are involved in tumor transformation, including epigenetic factors. These factors are a set of changes that do not affec... |
PMC9303919 | core_pubmed_pmc | Effective low–dose sirolimus regimen for kaposiform haemangioendothelioma with Kasabach–Merritt phenomenon in young infants | Effective low–dose sirolimus regimen for kaposiform haemangioendothelioma with Kasabach–Merritt phenomenon in young infants Abstract Aims Management of kaposiform haemangioendotheliomas (KHE) with Kasabach–Merritt phenomenon is challenging in young infants who are subjected to developmental pharmacokinetic changes. Sir... |
PMC10818329 | core_pubmed_pmc | An Ultra-Performance Liquid Chromatography–Tandem Mass Spectrometry (UPLC–MS/MS) Method for Qualifying DAPB in Rat Plasma and Application to Pharmacokinetic Studies | An Ultra-Performance Liquid Chromatography–Tandem Mass Spectrometry (UPLC–MS/MS) Method for Qualifying DAPB in Rat Plasma and Application to Pharmacokinetic Studies Abstract DAPB, a new molecule including danshensu, borneol, and a mother nucleus of ACEI (Angiotensin-converting enzyme inhibitors), is being developed as ... |
PMC3511063 | core_pubmed_pmc | An investigation of the auto-induction of and gender-related variability in the pharmacokinetics of dihydroartemisinin in the rat | An investigation of the auto-induction of and gender-related variability in the pharmacokinetics of dihydroartemisinin in the rat Abstract Abstract Background Artemisinin (QHS) and its derivatives dihydroartemisinin (DHA), artemether and artesunate have become the first-line anti-malarials in areas of multidrug resista... |
PMC4519332 | core_pubmed_pmc | Representative Sinusoids for Hepatic Four-Scale Pharmacokinetics Simulations | Representative Sinusoids for Hepatic Four-Scale Pharmacokinetics Simulations Abstract Abstract The mammalian liver plays a key role for metabolism and detoxification of xenobiotics in the body. The corresponding biochemical processes are typically subject to spatial variations at different length scales. Zonal enzyme e... |
PMC11000282 | core_pubmed_pmc | Ciprofol as compared to propofol for sedation and general anesthesia: a systematic review of randomized controlled trials | Ciprofol as compared to propofol for sedation and general anesthesia: a systematic review of randomized controlled trials Abstract Abstract Background Propofol is the most commonly used hypnotic agent used during sedation and general anesthesia (GA) practice, offering faster recovery compared to benzodiazepines. Howeve... |
PMC12751015 | core_pubmed_pmc | Evaluation of Bifunctional, PSMA-Targeted Triazamacrocycle-Picolinates Compatible with the 18 F/ 44 Sc/ 177 Lu Isotope Triad | Evaluation of Bifunctional, PSMA-Targeted Triazamacrocycle-Picolinates Compatible with the 18 F/ 44 Sc/ 177 Lu Isotope Triad Abstract The development of matched diagnostic and therapeutic radiopharmaceuticalstheranostic pairshas emerged as a promising strategy to advance personalized nuclear medicine. However, many c... |
PMC8244526 | core_pubmed_pmc | Dose optimization of early high-dose valproic acid for neuroprotection in a swine cardiac arrest model | Dose optimization of early high-dose valproic acid for neuroprotection in a swine cardiac arrest model Abstract Aim High-dose valproic acid (VPA) improves the survival and neurologic outcomes after asphyxial cardiac arrest (CA) in rats. We characterized the pharmacokinetics, pharmacodynamics, and safety of high-dose VP... |
PMC12577465 | core_pubmed_pmc | Relative Bioavailability of Inhaled Fluticasone Propionate and Salmeterol – is Population Pharmacokinetic Modelling a Relevant Alternative to a Non-Compartmental Approach? | Relative Bioavailability of Inhaled Fluticasone Propionate and Salmeterol – is Population Pharmacokinetic Modelling a Relevant Alternative to a Non-Compartmental Approach? Abstract Background Conventional statistical analysis of clinical data based on standard methods suggests that fixed combinations of fluticasone pro... |
PMC10090892 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics of a Novel U500 Insulin Aspart Formulation: A Randomized, Double-Blind, Crossover Study in People With Type 1 Diabetes | Pharmacokinetics and Pharmacodynamics of a Novel U500 Insulin Aspart Formulation: A Randomized, Double-Blind, Crossover Study in People With Type 1 Diabetes Abstract Abstract OBJECTIVE To evaluate the pharmacokinetics, pharmacodynamics, and safety of a novel U500 insulin aspart formulation (AT278 U500) compared with in... |
PMC6420106 | core_pubmed_pmc | Physicochemical characterization and phase I study of CMAB008, an infliximab biosimilar produced by a different expression system | Physicochemical characterization and phase I study of CMAB008, an infliximab biosimilar produced by a different expression system Abstract Background Infliximab (Remicade), a chimeric monoclonal antibody against human TNFα, will inevitably face competition from biosimilar products, because of its effectiveness in autoi... |
PMC9545133 | core_pubmed_pmc | Use of Physiologically Based Pharmacokinetic Modeling to Evaluate the Impact of Chronic Kidney Disease on CYP3A4‐Mediated Metabolism of Saxagliptin | Use of Physiologically Based Pharmacokinetic Modeling to Evaluate the Impact of Chronic Kidney Disease on CYP3A4‐Mediated Metabolism of Saxagliptin Abstract Abstract We characterized the impact of chronic kidney disease (CKD) on the cytochrome P450 (CYP) 3A4–mediated metabolism of saxagliptin to its metabolite, 5‐hydro... |
PMC3728799 | core_pubmed_pmc | An Engineering Approach to Biomedical Sciences: Advanced Testing Methods and Pharmacokinetic Modeling | An Engineering Approach to Biomedical Sciences: Advanced Testing Methods and Pharmacokinetic Modeling Abstract In this paper, the philosophy of a research in pharmacology field, driven by an engineering approach, was described along with some case histories and examples. The improvement in the testing methods for pharm... |
PMC4740573 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics of the Nonvitamin K Antagonist Oral Anticoagulant Edoxaban When Administered Alone or After Switching from Rivaroxaban or Dabigatran Etexilate in Healthy Subjects | Pharmacokinetics and Pharmacodynamics of the Nonvitamin K Antagonist Oral Anticoagulant Edoxaban When Administered Alone or After Switching from Rivaroxaban or Dabigatran Etexilate in Healthy Subjects Abstract Abstract Background and Objectives Edoxaban is an oral, once-daily direct factor Xa inhibitor. To support the ... |
PMC12967949 | core_pubmed_pmc | TAAR1-mediated pathways regulating nigrostriatal function and the discovery and pharmacological characterization of a novel TAAR1 agonist, Selutaront | TAAR1-mediated pathways regulating nigrostriatal function and the discovery and pharmacological characterization of a novel TAAR1 agonist, Selutaront Abstract Abstract Introduction Schizophrenia is a severe neurodevelopmental disorder with limited treatment options. Trace amine-associated receptor 1 (TAAR1) has emerged... |
PMC12304832 | core_pubmed_pmc | Medications, epilepsy and climate change: Added layers of complexity | Medications, epilepsy and climate change: Added layers of complexity Abstract Climate change—the global crisis with pervasive health impacts—has adverse consequences for people with epilepsy (PWE) who have low quality of life due to poor seizure control, socioeconomic disadvantages and comorbidities. This review focuse... |
PMC12226878 | core_pubmed_pmc | Evaluating Tranexamic Acid Dosing Strategies for Postpartum Hemorrhage: A Population Pharmacokinetic Approach in Pregnant Individuals | Evaluating Tranexamic Acid Dosing Strategies for Postpartum Hemorrhage: A Population Pharmacokinetic Approach in Pregnant Individuals Abstract Abstract Tranexamic acid (TXA) is used for the treatment and occasionally prevention of postpartum hemorrhage (PPH); however, questions still remain regarding dosing regimen opt... |
PMC8847440 | core_pubmed_pmc | Comparison of PK/PD Targets and Cutoff Values for Danofloxacin Against Pasteurella multocida and Haemophilus parasuis in Piglets | Comparison of PK/PD Targets and Cutoff Values for Danofloxacin Against Pasteurella multocida and Haemophilus parasuis in Piglets Abstract Abstract Danofloxacin is a synthetic fluoroquinolone with broad-spectrum activity developed for use in veterinary medicine. The aim of this study was to evaluate the pharmacokinetic/... |
PMC4263360 | core_pubmed_pmc | The Pharmacodynamics of the p53-Mdm2 Targeting Drug Nutlin: The Role of Gene-Switching Noise | The Pharmacodynamics of the p53-Mdm2 Targeting Drug Nutlin: The Role of Gene-Switching Noise Abstract In this work we investigate, by means of a computational stochastic model, how tumor cells with wild-type p53 gene respond to the drug Nutlin, an agent that interferes with the Mdm2-mediated p53 regulation. In particul... |
PMC9706589 | core_pubmed_pmc | Clearance pathways of near-infrared-II contrast agents | Clearance pathways of near-infrared-II contrast agents Abstract Near-infrared-II (NIR-II) bioimaging gradually becomes a vital visualization modality in the real-time investigation for fundamental biological research and clinical applications. The favorable NIR-II contrast agents are vital in NIR-II imaging technology ... |
PMC12525850 | core_pubmed_pmc | The Pharmacokinetics, Bioavailability, and Excretion Studies of α-Cyperone in Rats by UHPLC-QQQ-MS/MS | The Pharmacokinetics, Bioavailability, and Excretion Studies of α-Cyperone in Rats by UHPLC-QQQ-MS/MS Abstract α -Cyperone (C 15 H 22 O), a critical bioactive sesquiterpene, serves as a representative chemical compound of Cyperi Rhizoma —a classical functional food. To investigate the pharmacokinetic characteristics of... |
PMC11261730 | core_pubmed_pmc | Hollow-fibre infection model: adaptations for the culture and assessment of fastidious organisms | Hollow-fibre infection model: adaptations for the culture and assessment of fastidious organisms Abstract Abstract The hollow-fibre infection model (HFIM) is a valuable in vitro platform for emulating antimicrobial drug pharmacokinetic profiles. Despite its potential, standardized protocols for HFIM operation, especial... |
PMC5791175 | core_pubmed_pmc | Pharmacokinetics of meropenem in septic patients on sustained low-efficiency dialysis: a population pharmacokinetic study | Pharmacokinetics of meropenem in septic patients on sustained low-efficiency dialysis: a population pharmacokinetic study Abstract Abstract Background The aim of the study was to describe the population pharmacokinetics (PK) of meropenem in critically ill patients receiving sustained low-efficiency dialysis (SLED). Met... |
PMC10289769 | core_pubmed_pmc | The clinical safety of generic and brand clopidogrel in patients undergoing carotid endarterectomy: a randomized controlled trial | The clinical safety of generic and brand clopidogrel in patients undergoing carotid endarterectomy: a randomized controlled trial Abstract Introduction: Although some recent studies have found that original and generic clopidogrel brands are acceptable and have the same pharmacokinetic and pharmacodynamic properties, t... |
PMC9104455 | core_pubmed_pmc | The Role of Cannabis sativa L. as a Source of Cannabinoids against Coronavirus 2 (SARS-CoV-2): An In Silico Study to Evaluate Their Activities and ADMET Properties | The Role of Cannabis sativa L. as a Source of Cannabinoids against Coronavirus 2 (SARS-CoV-2): An In Silico Study to Evaluate Their Activities and ADMET Properties Abstract Cannabis sativa L. is an annual herbaceous plant that belongs to the family Cannabinaceae. In this study, the potential use of forty-five cannabino... |
PMC5515722 | core_pubmed_pmc | Pharmacokinetics, microscale distribution, and dosimetry of alpha-emitter-labeled anti-PD-L1 antibodies in an immune competent transgenic breast cancer model | Pharmacokinetics, microscale distribution, and dosimetry of alpha-emitter-labeled anti-PD-L1 antibodies in an immune competent transgenic breast cancer model Abstract Abstract Background Studies combining immune checkpoint inhibitors with external beam radiation have shown a therapeutic advantage over each modality alo... |
PMC9958704 | core_pubmed_pmc | Relationship between Body Composition and Serum Immunoglobulin Concentrations after Administration of Intravenous Immune Globulin–Preclinical and Clinical Evidence | Relationship between Body Composition and Serum Immunoglobulin Concentrations after Administration of Intravenous Immune Globulin–Preclinical and Clinical Evidence Abstract Abstract The purpose of this study was to investigate the effect of obesity on immunoglobulin G (IgG) pharmacokinetics in a rat model of obesity, a... |
PMC3461162 | core_pubmed_pmc | Safety, tolerability, pharmacokinetics and pharmacodynamics of AZD8055 in advanced solid tumours and lymphoma | Safety, tolerability, pharmacokinetics and pharmacodynamics of AZD8055 in advanced solid tumours and lymphoma Abstract Background: This study assessed the safety, tolerability, pharmacokinetics and pharmacodynamics of the first-in-class dual mammalian target of rapamycin complex (mTORC)1/mTORC2 inhibitor, AZD8055. Meth... |
PMC12414025 | core_pubmed_pmc | Pharmacokinetics of Sufentanil After Epidural Administration During the Course of Extensive Abdominal Surgery | Pharmacokinetics of Sufentanil After Epidural Administration During the Course of Extensive Abdominal Surgery Abstract Background and Objective Epidural sufentanil is widely used for intraoperative analgesia and is recognized as a safe and effective route of administration when carefully monitored and administered at t... |
PMC5813749 | core_pubmed_pmc | Phase I Pharmacokinetic Study of Nivolumab in Korean Patients with Advanced Solid Tumors | Phase I Pharmacokinetic Study of Nivolumab in Korean Patients with Advanced Solid Tumors Abstract Abstract Lessons Learned. This pharmacokinetic study of nivolumab showed that there is little ethnic difference in the handling of nivolumab. Nivolumab was well tolerated in Korean patients. Background. This phase I study ... |
PMC6769477 | core_pubmed_pmc | The Rebirth of Matrix Metalloproteinase Inhibitors: Moving Beyond the Dogma | The Rebirth of Matrix Metalloproteinase Inhibitors: Moving Beyond the Dogma Abstract Abstract The pursuit of matrix metalloproteinase (MMP) inhibitors began in earnest over three decades ago. Initial clinical trials were disappointing, resulting in a negative view of MMPs as therapeutic targets. As a better understandi... |
PMC4173124 | core_pubmed_pmc | A phase 1 study of ACE-536, a regulator of erythroid differentiation, in healthy volunteers | A phase 1 study of ACE-536, a regulator of erythroid differentiation, in healthy volunteers Abstract ACE-536, a recombinant protein containing a modified activin receptor type IIB, is being developed for the treatment of anemias caused by ineffective erythropoiesis, such as thalassemias and myelodysplastic syndromes. A... |
PMC5226291 | core_pubmed_pmc | Pharmacokinetics and pharmacodynamics of antibiotics in critically ill acute kidney injury patients | Pharmacokinetics and pharmacodynamics of antibiotics in critically ill acute kidney injury patients Abstract Abstract Sepsis is the most common cause of death in critically ill patients and is associated with multiorgan failure, including acute kidney injury (AKI). This situation can require acute renal support and inc... |
PMC12472881 | core_pubmed_pmc | Whole-Body Physiologically Based Pharmacokinetic–Pharmacodynamic Modeling for Interspecies Translation and Mechanistic Characterization of Plasma and Tissue Disposition of GalNAc-siRNAs | Whole-Body Physiologically Based Pharmacokinetic–Pharmacodynamic Modeling for Interspecies Translation and Mechanistic Characterization of Plasma and Tissue Disposition of GalNAc-siRNAs Abstract Introduction/aim: N-acetylgalactoseamine-conjugated small interfering RNAs (GalNAc-siRNAs) are an emerging class of drugs pos... |
PMC9563617 | core_pubmed_pmc | Pharmacokinetic study of single and multiple oral administration of glutamine in healthy Beagles | Pharmacokinetic study of single and multiple oral administration of glutamine in healthy Beagles Abstract Abstract Glutamine is an amino acid that is mainly used for the treatment of gastrointestinal diseases in clinic, but there is a lack of such medicine in veterinary clinic, and its research in dogs has never been s... |
PMC9051980 | core_pubmed_pmc | Intranasal hydrogel of armodafinil hydroxypropyl-β-cyclodextrin inclusion complex for the treatment of post-traumatic stress disorder | Intranasal hydrogel of armodafinil hydroxypropyl-β-cyclodextrin inclusion complex for the treatment of post-traumatic stress disorder Abstract Abstract Armodafinil inclusion complex (AIC) hydrogel was prepared and evaluated for its therapeutic effect on Post-traumatic Stress Disorder (PTSD). After computer simulation a... |
PMC12525066 | core_pubmed_pmc | Tailored Reaction Conditions and Automated Radiolabeling of [ 177 Lu]Lu-PSMA-ALB-56 in a 68 Ga Setting: The Critical Impact of Antioxidant Concentrations | Tailored Reaction Conditions and Automated Radiolabeling of [ 177 Lu]Lu-PSMA-ALB-56 in a 68 Ga Setting: The Critical Impact of Antioxidant Concentrations Abstract The growing use of experimental radiopharmaceuticals for targeted radionuclide therapy (TRT) highlights the need for robust “in house” radiolabeling protocol... |
PMC8522765 | core_pubmed_pmc | Model-Based Approach for Optimizing Ceftobiprole Dosage in Pediatric Patients | Model-Based Approach for Optimizing Ceftobiprole Dosage in Pediatric Patients Abstract ABSTRACT Ceftobiprole is an advanced-generation cephalosporin for intravenous administration with activity against Gram-positive and Gram-negative organisms. A population pharmacokinetic (PK) model characterizing the disposition of c... |
PMC11268839 | core_pubmed_pmc | Effect of Efavirenz on the Pharmacokinetics of SHR6390 in Healthy Volunteers | Effect of Efavirenz on the Pharmacokinetics of SHR6390 in Healthy Volunteers Abstract Purpose SHR6390 is an oral, potent and selective small-molecule CDK4/6 inhibitor for the treatment of human breast, ovarian and colon cancer. Previous studies have shown that SHR6390 in combination with rifampicin, a potent inducer of... |
PMC3468361 | core_pubmed_pmc | Pharmacodynamic analysis of tumour perfusion assessed by 15 O-water-PET imaging during treatment with sunitinib malate in patients with advanced malignancies | Pharmacodynamic analysis of tumour perfusion assessed by 15 O-water-PET imaging during treatment with sunitinib malate in patients with advanced malignancies Abstract Abstract Background We evaluated pharmacodynamic changes in tumour perfusion using positron emission tomography (PET) imaging with 15 O-water to assess b... |
PMC12816109 | core_pubmed_pmc | Oral delivery of an ustekinumab biosimilar with bioavailability comparable to subcutaneous administration in healthy human participants | Oral delivery of an ustekinumab biosimilar with bioavailability comparable to subcutaneous administration in healthy human participants Abstract Purpose Ustekinumab, targeting interleukin (IL)-12 and IL-23, is effective in treating chronic immune-mediated inflammatory diseases, but needs to be dosed via subcutaneous (S... |
PMC6058569 | core_pubmed_pmc | Effect of finasteride particle size reduction on its pharmacokinetic, tissue distribution and cellular permeation | Effect of finasteride particle size reduction on its pharmacokinetic, tissue distribution and cellular permeation Abstract Abstract Finasteride (FSD), a specific competitive inhibitor of the steroid type-II 5α-reductase enzyme, is used in treatment of benign prostate hyperplasia (BPH) and male pattern baldness. The dru... |
PMC10783087 | core_pubmed_pmc | The Mycobacterium tuberculosis MmpL3 inhibitor MSU-43085 is active in a mouse model of infection | The Mycobacterium tuberculosis MmpL3 inhibitor MSU-43085 is active in a mouse model of infection Abstract ABSTRACT Addressing drug resistance in Mycobacterium tuberculosis (Mtb) requires the development of new drugs with new targets. We previously identified 13 MmpL3 inhibitors from a screen of a small library of Mtb g... |
PMC6710527 | core_pubmed_pmc | Pharmacokinetics and safety of tobramycin nebulization with the I‐neb and PARI‐LC Plus in children with cystic fibrosis: A randomized, crossover study | Pharmacokinetics and safety of tobramycin nebulization with the I‐neb and PARI‐LC Plus in children with cystic fibrosis: A randomized, crossover study Abstract Abstract Aims We aimed to compare the pharmacokinetics (PK) and safety profile of tobramycin inhalation solution (TIS) using the I‐neb device to the standard PA... |
PMC8234075 | core_pubmed_pmc | The Synergistic Activity and Optimizing Doses of Tigecycline in Combination with Aminoglycosides against Clinical Carbapenem-Resistant Klebsiella pneumoniae Isolates | The Synergistic Activity and Optimizing Doses of Tigecycline in Combination with Aminoglycosides against Clinical Carbapenem-Resistant Klebsiella pneumoniae Isolates Abstract Abstract Carbapenem-resistant Enterobacteriaceae (CRE), especially carbapenem-resistant Klebsiella pneumoniae (CRKP), are among the largest patho... |
PMC6097509 | core_pubmed_pmc | Enhanced oral bioavailability of EGCG using pH-sensitive polymeric nanoparticles: characterization and in vivo investigation on nephrotic syndrome rats | Enhanced oral bioavailability of EGCG using pH-sensitive polymeric nanoparticles: characterization and in vivo investigation on nephrotic syndrome rats Abstract Abstract Objective Chronic kidney disease (CKD) is characterized by progressive loss of renal functions. At present, there are only limited therapeutic strateg... |
PMC4657295 | core_pubmed_pmc | Pharmacodynamic modelling of in vitro activity of tetracycline against a representative, naturally occurring population of porcine Escherichia coli | Pharmacodynamic modelling of in vitro activity of tetracycline against a representative, naturally occurring population of porcine Escherichia coli Abstract Abstract Background The complex relationship between drug concentrations and bacterial growth rates require not only the minimum inhibitory concentration but also ... |
PMC11833621 | core_pubmed_pmc | Virtual screening, in silico pharmacokinetic and toxicity profiling of colchicine-based inhibitors of estrogen receptor of breast cancer | Virtual screening, in silico pharmacokinetic and toxicity profiling of colchicine-based inhibitors of estrogen receptor of breast cancer Abstract Abstract The declining efficacies of existing drugs against estrogen receptor positive (ER+) breast cancer due to multidrug resistance, acute toxicities, and poor pharmacokin... |
PMC12564412 | core_pubmed_pmc | Biomarker-Based Pharmacological Characterization of ENX-102, a Novel α2/3/5 Subtype-Selective GABAA Receptor Positive Allo-Steric Modulator: Translational Insights from Rodent and Human Studies | Biomarker-Based Pharmacological Characterization of ENX-102, a Novel α2/3/5 Subtype-Selective GABAA Receptor Positive Allo-Steric Modulator: Translational Insights from Rodent and Human Studies Abstract Gamma-aminobutyric acid type A receptors (GABA A Rs) are pentameric ligand-gated ion channels essential for inhibitor... |
PMC8367910 | core_pubmed_pmc | The impact of hepatic and renal function on panitumumab exposures in patients with metastatic RAS wild-type colorectal cancer | The impact of hepatic and renal function on panitumumab exposures in patients with metastatic RAS wild-type colorectal cancer Abstract Abstract Purpose Panitumumab is a human monoclonal antibody targeting the epidermal growth factor receptor for the treatment of wild-type RAS metastatic colorectal cancer (mCRC). Curren... |
PMC9962377 | core_pubmed_pmc | Pan-Genomics of Escherichia albertii for Antibiotic Resistance Profiling in Different Genome Fractions and Natural Product Mediated Intervention: In Silico Approach | Pan-Genomics of Escherichia albertii for Antibiotic Resistance Profiling in Different Genome Fractions and Natural Product Mediated Intervention: In Silico Approach Abstract Abstract Escherichia albertii is an emerging, enteric pathogen of significance. It was first isolated in 2003 from a pediatric diarrheal sample fr... |
PMC4606158 | core_pubmed_pmc | Propofol Requirement for Induction of Unconsciousness Is Reduced in Patients with Parkinson's Disease: A Case Control Study | Propofol Requirement for Induction of Unconsciousness Is Reduced in Patients with Parkinson's Disease: A Case Control Study Abstract Abstract Parkinson's disease (PD) is the second most prevalent neurodegenerative disease, but whether the neurodegenerative process influences the pharmacodynamics of propofol remains unc... |
PMC5427475 | core_pubmed_pmc | Effect of clopidogrel on the hydroxylation and sulfoxidation of omeprazole: A single dose study in healthy human volunteers | Effect of clopidogrel on the hydroxylation and sulfoxidation of omeprazole: A single dose study in healthy human volunteers Abstract Based upon the known potential interaction between omeprazole (OMP) and clopidogrel (CLOP), the current study was designed to evaluate the effect of CLOP on disposition of OMP and its two... |
PMC8381616 | core_pubmed_pmc | Potential bioactive compounds as SARS-CoV-2 inhibitors from extracts of the marine red alga Halymenia durvillei (Rhodophyta) – A computational study | Potential bioactive compounds as SARS-CoV-2 inhibitors from extracts of the marine red alga Halymenia durvillei (Rhodophyta) – A computational study Abstract The respiratory infection COVID-19 caused by the virus SARS CoV-2 has continued to be a major health problem worldwide and has caused more than a million mortalit... |
PMC7297357 | core_pubmed_pmc | Analysis of the mutant selection window and killing of Mycoplasma hyopneumoniae for doxycycline, tylosin, danofloxacin, tiamulin, and valnemulin | Analysis of the mutant selection window and killing of Mycoplasma hyopneumoniae for doxycycline, tylosin, danofloxacin, tiamulin, and valnemulin Abstract Abstract Mycoplasma hyopneumoniae is the major pathogenic microorganism causing enzootic pneumonia in pigs. With increasing resistance of M . hyopneumoniae to convent... |
PMC12284176 | core_pubmed_pmc | Safety and pharmacokinetics of the non-hormonal male contraceptive YCT-529 | Safety and pharmacokinetics of the non-hormonal male contraceptive YCT-529 Abstract Background Since nearly half of all pregnancies in the US and worldwide are unintended, there is a critical need for additional contraceptive options for men and women. After a hiatus in non-hormonal male contraceptive development of ab... |
PMC9670026 | core_pubmed_pmc | Nanoplasmonic Avidity-Based Detection and Quantification of IgG Aggregates | Nanoplasmonic Avidity-Based Detection and Quantification of IgG Aggregates Abstract Production of therapeutic monoclonal antibodies (mAbs) is a complex process that requires extensive analytical and bioanalytical characterization to ensure high and consistent product quality. Aggregation of mAbs is common and very prob... |
PMC3606126 | core_pubmed_pmc | pSTAT3: a target biomarker to study the pharmacology of the anti-IL-21R antibody ATR-107 in human whole blood | pSTAT3: a target biomarker to study the pharmacology of the anti-IL-21R antibody ATR-107 in human whole blood Abstract Abstract Background IL-21 has been shown to play an important role in autoimmune diseases. ATR-107 is an antibody which directly targets the IL-21 receptor (IL-21R). To aid the clinical development of ... |
PMC3618516 | core_pubmed_pmc | A Systematic Screen of FDA-Approved Drugs for Inhibitors of Biological Threat Agents | A Systematic Screen of FDA-Approved Drugs for Inhibitors of Biological Threat Agents Abstract Background The rapid development of effective medical countermeasures against potential biological threat agents is vital. Repurposing existing drugs that may have unanticipated activities as potential countermeasures is one w... |
PMC7016911 | core_pubmed_pmc | Privileged Scaffold Chalcone: Synthesis, Characterization and Its Mechanistic Interaction Studies with BSA Employing Spectroscopic and Chemoinformatics Approaches | Privileged Scaffold Chalcone: Synthesis, Characterization and Its Mechanistic Interaction Studies with BSA Employing Spectroscopic and Chemoinformatics Approaches Abstract Abstract Chalcone, a privileged structure, is considered as an effective template in the field of medicinal chemistry for potent drug discovery. In ... |
PMC6716068 | core_pubmed_pmc | Anti-Angiogenic and Anti-Scarring Dual Action of an Anti-Fibroblast Growth Factor 2 Aptamer in Animal Models of Retinal Disease | Anti-Angiogenic and Anti-Scarring Dual Action of an Anti-Fibroblast Growth Factor 2 Aptamer in Animal Models of Retinal Disease Abstract Currently approved therapies for age-related macular degeneration (AMD) are inhibitors against vascular endothelial growth factor (VEGF), which is a major contributor to the pathogene... |
PMC12732015 | core_pubmed_pmc | Personalized Perioperative Opioid Strategies in Children: Focus on Methadone, Pharmacogenomics and Prevention of Persistent Postoperative Opioid Use | Personalized Perioperative Opioid Strategies in Children: Focus on Methadone, Pharmacogenomics and Prevention of Persistent Postoperative Opioid Use Abstract Abstract Persistent postoperative opioid use (PPOU) is an emerging challenge in pediatric perioperative care, with rates as high as 4.7% in opioid-naive adolescen... |
Subsets and Splits
No community queries yet
The top public SQL queries from the community will appear here once available.