id stringlengths 9 11 | source stringclasses 1
value | title stringlengths 15 560 | text stringlengths 2k 153k |
|---|---|---|---|
PMC8361934 | core_pubmed_pmc | Impact of Dose Delays and Alternative Dosing Regimens on Pertuzumab Pharmacokinetics | Impact of Dose Delays and Alternative Dosing Regimens on Pertuzumab Pharmacokinetics Abstract Abstract PERJETA (pertuzumab), administered with Herceptin (trastuzumab), is used in the treatment of human epidermal growth factor receptor 2‐positive breast cancer. Pertuzumab is currently approved with an initial loading do... |
PMC7914186 | core_pubmed_pmc | A randomized phase 1 single-dose polysomnography study of ASP8062, a GABA B receptor positive allosteric modulator | A randomized phase 1 single-dose polysomnography study of ASP8062, a GABA B receptor positive allosteric modulator Abstract Rationale Previous research suggests that sleep polysomnography and EEG endpoints can be used to assess GABAergic activity; however, the impact of GABA B receptor positive allosteric modulators on... |
PMC12454544 | core_pubmed_pmc | An overview on pharmaceutical applications of phosphodiesterase enzyme 5 (PDE5) inhibitors | An overview on pharmaceutical applications of phosphodiesterase enzyme 5 (PDE5) inhibitors Abstract Phosphodiesterase enzyme 5 (PDE5) inhibitors have emerged as one of the leading molecules for the treatment of erectile dysfunction (ED). PDE5 inhibitors are categorized structurally into several classes. PDE5 inhibitors... |
PMC12422600 | core_pubmed_pmc | Therapeutic Drug Monitoring of Beta-Lactams in Cystic Fibrosis: Unattained Target in Standard Antibiotic Dosing | Therapeutic Drug Monitoring of Beta-Lactams in Cystic Fibrosis: Unattained Target in Standard Antibiotic Dosing Abstract Abstract: Acute exacerbations of cystic fibrosis (CF) diminish quality of life and, if inadequately treated, can be life-threatening. The pathophysiological alterations associated with CF result in m... |
PMC9017304 | core_pubmed_pmc | Rifampin Pharmacokinetics/Pharmacodynamics in the Hollow-Fiber Model of Mycobacterium kansasii Infection | Rifampin Pharmacokinetics/Pharmacodynamics in the Hollow-Fiber Model of Mycobacterium kansasii Infection Abstract ABSTRACT There is limited high-quality evidence to guide the optimal treatment of Mycobacterium kansasii pulmonary disease. We retrospectively collected clinical data from 33 patients with M. kansasii pulmo... |
PMC3681893 | core_pubmed_pmc | Pharmacokinetics Study of Recombinant Hirudin in the Plasma of Rats Using Chromogenic Substrate, ELISA, and Radioisotope Assays | Pharmacokinetics Study of Recombinant Hirudin in the Plasma of Rats Using Chromogenic Substrate, ELISA, and Radioisotope Assays Abstract Aim To compare the analytical methods used to study the pharmacokinetics of recombinant hirudin in the plasma of rats that had been injected with 125 I-recombinant hirudin. Methods 2.... |
PMC4732406 | core_pubmed_pmc | Anti-inflammatory effects of intravenous methotrexate associated with lipid nanoemulsions on antigen-induced arthritis | Anti-inflammatory effects of intravenous methotrexate associated with lipid nanoemulsions on antigen-induced arthritis Abstract Abstract OBJECTIVE: To test the hypothesis that intravenous use of methotrexate associated with lipid nanoemulsions can achieve superior anti-inflammatory effects in the joints of rabbits with... |
PMC7076871 | core_pubmed_pmc | Pharmacokinetic incompatibility of the Huanglian-Gancao herb pair | Pharmacokinetic incompatibility of the Huanglian-Gancao herb pair Abstract Abstract Background Pharmacokinetic interaction is one of the most important indices for the evaluation of the compatibility of herbal medicines. Both Gancao ( Glycyrrhizae Radix et Rhizoma ) and Huanglian ( Coptidis Rhizoma ) are commonly used ... |
PMC9118863 | core_pubmed_pmc | Bioimaging guided pharmaceutical evaluations of nanomedicines for clinical translations | Bioimaging guided pharmaceutical evaluations of nanomedicines for clinical translations Abstract Nanomedicines (NMs) have emerged as an efficient approach for developing novel treatment strategies against a variety of diseases. Over the past few decades, NM formulations have received great attention, and a large number... |
PMC4978708 | core_pubmed_pmc | Assessment of Potential Herb-Drug Interactions among Nigerian Adults with Type-2 Diabetes | Assessment of Potential Herb-Drug Interactions among Nigerian Adults with Type-2 Diabetes Abstract Abstract It is becoming increasingly evident that patients with diabetes do not rely only on prescription drugs for their disease management. The use of herbal medicines is one of the self-management practices adopted by ... |
PMC11052883 | core_pubmed_pmc | Clinical Pharmacology of the Antibody–Drug Conjugate Enfortumab Vedotin in Advanced Urothelial Carcinoma and Other Malignant Solid Tumors | Clinical Pharmacology of the Antibody–Drug Conjugate Enfortumab Vedotin in Advanced Urothelial Carcinoma and Other Malignant Solid Tumors Abstract Enfortumab vedotin is an antibody–drug conjugate comprised of a human monoclonal antibody directed to Nectin-4 and monomethyl auristatin E (MMAE), a microtubule-disrupting a... |
PMC4230716 | core_pubmed_pmc | Using Bayesian-PBPK modeling for assessment of inter-individual variability and subgroup stratification | Using Bayesian-PBPK modeling for assessment of inter-individual variability and subgroup stratification Abstract Purpose Inter-individual variability in clinical endpoints and occurrence of potentially severe adverse effects represent an enormous challenge in drug development at all phases of (pre-)clinical research. T... |
PMC3499177 | core_pubmed_pmc | Tumor penetration and epidermal growth factor receptor saturation by panitumumab correlate with antitumor activity in a preclinical model of human cancer | Tumor penetration and epidermal growth factor receptor saturation by panitumumab correlate with antitumor activity in a preclinical model of human cancer Abstract Abstract Background Successful treatment of solid tumors relies on the ability of drugs to penetrate into the tumor tissue. Methods We examined the correlati... |
PMC8874516 | core_pubmed_pmc | Linkers: An Assurance for Controlled Delivery of Antibody-Drug Conjugate | Linkers: An Assurance for Controlled Delivery of Antibody-Drug Conjugate Abstract Abstract As one of the major therapeutic options for cancer treatment, chemotherapy has limited selectivity against cancer cells. Consequently, this therapeutic strategy offers a small therapeutic window with potentially high toxicity and... |
PMC3632017 | core_pubmed_pmc | Cytochrome P450 3A4*1B as Pharmacogenomic Predictor of Tacrolimus Pharmacokinetics and Clinical Outcome in the Liver Transplant Recipients | Cytochrome P450 3A4*1B as Pharmacogenomic Predictor of Tacrolimus Pharmacokinetics and Clinical Outcome in the Liver Transplant Recipients Abstract Abstract Background and Aims: Tacrolimus is a macrolide immunosuppressant used for prevention of allograft rejection in organ transplantation and metabolized in the liver a... |
PMC3976951 | core_pubmed_pmc | Updates on the Clinical Evidenced Herb-Warfarin Interactions | Updates on the Clinical Evidenced Herb-Warfarin Interactions Abstract Abstract Increasing and inadvertent use of herbs makes herb-drug interactions a focus of research. Concomitant use of warfarin, a highly efficacious oral anticoagulant, and herbs causes major safety concerns due to the narrow therapeutic window of wa... |
PMC11370030 | core_pubmed_pmc | Appropriate use of triazolam in elderly patients considering a quantitative benefit-risk assessment based on the pharmacokinetic-pharmacodynamic modeling and simulation approach supported by real-world data | Appropriate use of triazolam in elderly patients considering a quantitative benefit-risk assessment based on the pharmacokinetic-pharmacodynamic modeling and simulation approach supported by real-world data Abstract Background Triazolam is a typical drug commonly used in the elderly; however, there have been concerns a... |
PMC10499426 | core_pubmed_pmc | Longitudinal estimated glomerular filtration rate ( eGFR) modeling in long‐term renal function to inform clinical trial design in kidney transplantation | Longitudinal estimated glomerular filtration rate ( eGFR) modeling in long‐term renal function to inform clinical trial design in kidney transplantation Abstract Abstract Kidney transplantation is the preferred treatment for individuals with end‐stage kidney disease. From a modeling perspective, our understanding of ki... |
PMC10296897 | core_pubmed_pmc | Drug-Eluting Embolic Loaded with Tyrosine Kinase Inhibitor Targeted Therapies for Transarterial Chemoembolization in a VX2 Model | Drug-Eluting Embolic Loaded with Tyrosine Kinase Inhibitor Targeted Therapies for Transarterial Chemoembolization in a VX2 Model Abstract Abstract Simple Summary Embolization shuts down vessels and cuts off the supply of blood to liver tumors. Using small beads, drugs can be delivered locally. Thus far, the drugs loade... |
PMC7391402 | core_pubmed_pmc | Integrated Item Response Theory Modeling of Multiple Patient-Reported Outcomes Assessing Lower Urinary Tract Symptoms Associated with Benign Prostatic Hyperplasia | Integrated Item Response Theory Modeling of Multiple Patient-Reported Outcomes Assessing Lower Urinary Tract Symptoms Associated with Benign Prostatic Hyperplasia Abstract In clinical trials within lower urinary tract symptoms due to benign prostatic hyperplasia (BPH-LUTS), the International Prostate Symptom Score (IPS... |
PMC2965864 | core_pubmed_pmc | A phase I, dose-finding study of sunitinib in combination with irinotecan in patients with advanced solid tumours | A phase I, dose-finding study of sunitinib in combination with irinotecan in patients with advanced solid tumours Abstract Background: Sunitinib is a multitargeted, oral tyrosine kinase inhibitor with antitumour and antiangiogenic activity. We investigated the safety and pharmacokinetics of sunitinib in combination wit... |
PMC12731643 | core_pubmed_pmc | Next-Generation HDAC Inhibitors: Advancing Zinc-Binding Group Design for Enhanced Cancer Therapy | Next-Generation HDAC Inhibitors: Advancing Zinc-Binding Group Design for Enhanced Cancer Therapy Abstract Highlights What are the main findings? This review systematically analyzes recently developed HDAC inhibitors in recent years, emphasizing structural evolution across CAP, linker, and zinc-binding groups (ZBGs). It... |
PMC3722116 | core_pubmed_pmc | Nonlinear Mixed-Effects Modelling of In Vitro Drug Susceptibility and Molecular Correlates of Multidrug Resistant Plasmodium falciparum | Nonlinear Mixed-Effects Modelling of In Vitro Drug Susceptibility and Molecular Correlates of Multidrug Resistant Plasmodium falciparum Abstract Abstract The analysis of in vitro anti-malarial drug susceptibility testing is vulnerable to the effects of different statistical approaches and selection biases. These confou... |
PMC4187895 | core_pubmed_pmc | A First-in-Human Randomized, Double-Blind, Placebo-Controlled, Single- and Multiple-Ascending Oral Dose Study of Novel Antimalarial Spiroindolone KAE609 (Cipargamin) To Assess Its Safety, Tolerability, and Pharmacokinetics in Healthy Adult Volunteers | A First-in-Human Randomized, Double-Blind, Placebo-Controlled, Single- and Multiple-Ascending Oral Dose Study of Novel Antimalarial Spiroindolone KAE609 (Cipargamin) To Assess Its Safety, Tolerability, and Pharmacokinetics in Healthy Adult Volunteers Abstract Abstract This first-in-human randomized, double-blind, place... |
PMC8740159 | core_pubmed_pmc | An LC-MS/MS method for simultaneous analysis of the cystic fibrosis therapeutic drugs colistin, ivacaftor and ciprofloxacin | An LC-MS/MS method for simultaneous analysis of the cystic fibrosis therapeutic drugs colistin, ivacaftor and ciprofloxacin Abstract Abstract Inhaled antibiotics such as colistin and ciprofloxacin are increasingly used to treat bacterial lung infections in cystic fibrosis patients. In this study, we established and val... |
PMC9935793 | core_pubmed_pmc | Liposomal Irinotecan Shows a Larger Therapeutic Index than Non-liposomal Irinotecan in Patient-Derived Xenograft Models of Pancreatic Cancer | Liposomal Irinotecan Shows a Larger Therapeutic Index than Non-liposomal Irinotecan in Patient-Derived Xenograft Models of Pancreatic Cancer Abstract Introduction Liposomal irinotecan promotes controlled sustained release of irinotecan (CPT-11), therefore, we hypothesize that the therapeutic index (quantitative measure... |
PMC4405076 | core_pubmed_pmc | Proposal for defining the relevance of drug accumulation derived from single dose study data for modified release dosage forms | Proposal for defining the relevance of drug accumulation derived from single dose study data for modified release dosage forms Abstract Abstract Recently, the European Medicines Agency (EMA) published the new draft guideline on the pharmacokinetic and clinical evaluation of modified release (MR) formulations. The draft... |
PMC10610386 | core_pubmed_pmc | The Amorphous Solid Dispersion of Chrysin in Plasdone ® S630 Demonstrates Improved Oral Bioavailability and Antihyperlipidemic Performance in Rats | The Amorphous Solid Dispersion of Chrysin in Plasdone ® S630 Demonstrates Improved Oral Bioavailability and Antihyperlipidemic Performance in Rats Abstract Chrysin is a flavonoid with various biological activities. However, its low water solubility and strong metabolism render its oral bioavailability rather poor. This... |
PMC7539971 | core_pubmed_pmc | Four phase 1 trials to evaluate the safety and pharmacokinetic profile of single and repeated dosing of SCO‐101 in adult male and female volunteers | Four phase 1 trials to evaluate the safety and pharmacokinetic profile of single and repeated dosing of SCO‐101 in adult male and female volunteers Abstract Abstract SCO‐101 (Endovion) was discontinued 20 years ago as a new drug under development against sickle cell anaemia. Data from the phase 1 studies remained unpub... |
PMC11652485 | core_pubmed_pmc | Determination of pharmacokinetic-pharmacodynamic cutoff values of oxytetracycline in calves and adult cattle using population pharmacokinetic modeling | Determination of pharmacokinetic-pharmacodynamic cutoff values of oxytetracycline in calves and adult cattle using population pharmacokinetic modeling Abstract Abstract Introduction A harmonized clinical breakpoint for interpreting antimicrobial susceptibility testing of oxytetracycline in cattle is currently lacking i... |
PMC6765698 | core_pubmed_pmc | Recommendations for the Design of Clinical Drug–Drug Interaction Studies With Itraconazole Using a Mechanistic Physiologically‐Based Pharmacokinetic Model | Recommendations for the Design of Clinical Drug–Drug Interaction Studies With Itraconazole Using a Mechanistic Physiologically‐Based Pharmacokinetic Model Abstract Regulatory agencies currently recommend itraconazole ( ITZ ) as a strong cytochrome P450 3A ( CYP 3A) inhibitor for clinical drug–drug interaction ( DDI ) s... |
PMC5729885 | core_pubmed_pmc | Comparative pharmacokinetics of a fixed-dose combination vs concomitant administration of telmisartan and S-amlodipine in healthy adult volunteers | Comparative pharmacokinetics of a fixed-dose combination vs concomitant administration of telmisartan and S-amlodipine in healthy adult volunteers Abstract Abstract Objective This study compared the pharmacokinetic (PK) and safety profiles of a fixed-dose combination (FDC) formulation of telmisartan and S-amlodipine wi... |
PMC5644106 | core_pubmed_pmc | KH176 under development for rare mitochondrial disease: a first in man randomized controlled clinical trial in healthy male volunteers | KH176 under development for rare mitochondrial disease: a first in man randomized controlled clinical trial in healthy male volunteers Abstract Abstract Background Mitochondrial disorders are a clinically, biochemically and genetically heterogeneous group of multi-system diseases, with an unmet medical need for treatme... |
PMC6895963 | core_pubmed_pmc | Is there an Exposure–Response Relationship for Nivolumab in Real-World NSCLC Patients? | Is there an Exposure–Response Relationship for Nivolumab in Real-World NSCLC Patients? Abstract Pharmacokinetic/pharmacodynamic data from real-world cohort are sparse in non small–cell lung cancer (NSCLC) patients treated with nivolumab. The aim of this prospective observational study was to explore the exposure-respon... |
PMC9931032 | core_pubmed_pmc | Elbasvir/grazoprevir in children aged 3–18 years with chronic HCV genotype 1 or 4 infection: a pharmacokinetic modeling study | Elbasvir/grazoprevir in children aged 3–18 years with chronic HCV genotype 1 or 4 infection: a pharmacokinetic modeling study Abstract Background: Approximately 3.5 million children and adolescents worldwide are chronically infected with HCV. This study uses pharmacokinetic modeling to identify pediatric doses of elbas... |
PMC6639923 | core_pubmed_pmc | Describing vancomycin serum levels in pediatric intensive care unit (ICU) patients: are expected goals being met | Describing vancomycin serum levels in pediatric intensive care unit (ICU) patients: are expected goals being met Abstract Abstract Background In the pediatric population, infections by methicillin-resistant Staphylococcus aureus (MRSA) are associated with significant morbidity and hospital costs. Vancomycin is a glycop... |
PMC9246989 | core_pubmed_pmc | Pharmacoproteomics of Brain Barrier Transporters and Substrate Design for the Brain Targeted Drug Delivery | Pharmacoproteomics of Brain Barrier Transporters and Substrate Design for the Brain Targeted Drug Delivery Abstract Abstract One of the major reasons why central nervous system (CNS)-drug development has been challenging in the past, is the barriers that prevent substances entering from the blood circulation into the b... |
PMC6852000 | core_pubmed_pmc | Pharmacokinetic/Pharmacodynamic Modeling to Support the Re‐approval of Gemtuzumab Ozogamicin | Pharmacokinetic/Pharmacodynamic Modeling to Support the Re‐approval of Gemtuzumab Ozogamicin Abstract Abstract Gemtuzumab ozogamicin (Mylotarg; Pfizer, New York, NY) was the first antibody–drug conjugate to be approved for CD33‐positive acute myeloid leukemia (AML). However, it was voluntarily withdrawn from the US mar... |
PMC11201108 | core_pubmed_pmc | GC-MS method for simultaneous determination and pharmacokinetic investigation of five volatile components in rat plasma after oral administration of the essential oil extract of Pogostemon cablin | GC-MS method for simultaneous determination and pharmacokinetic investigation of five volatile components in rat plasma after oral administration of the essential oil extract of Pogostemon cablin Abstract Pogostemon cablin (PC) is a traditional Chinese medicine (TCM) and food as well as an important essential oil plant... |
PMC5861220 | core_pubmed_pmc | The Cytochrome P450-Mediated Metabolism Alternation of Four Effective Lignans From Schisandra chinensis in Carbon Tetrachloride-Intoxicated Rats and Patients With Advanced Hepatocellular Carcinoma | The Cytochrome P450-Mediated Metabolism Alternation of Four Effective Lignans From Schisandra chinensis in Carbon Tetrachloride-Intoxicated Rats and Patients With Advanced Hepatocellular Carcinoma Abstract Abstract It is highly valuable to study the pharmacokinetics of herbal components under the pathological condition... |
PMC4363646 | core_pubmed_pmc | Pharmacogenomics and Herb-Drug Interactions: Merge of Future and Tradition | Pharmacogenomics and Herb-Drug Interactions: Merge of Future and Tradition Abstract The worldwide using of herb products and the increasing potential herb-drug interaction issue has raised enthusiasm on discovering the underlying mechanisms. Previous review indicated that the interactions may be mediated by metabolism ... |
PMC7486547 | core_pubmed_pmc | Enhancement of oral bioavailability and anti-Parkinsonian efficacy of resveratrol through a nanocrystal formulation | Enhancement of oral bioavailability and anti-Parkinsonian efficacy of resveratrol through a nanocrystal formulation Abstract Resveratrol (RES), a non-flavonoid polyphenol extracted from a wide variety of plants, exhibits neuroprotective activities against Parkinson's disease (PD). However, undesirable water solubility ... |
PMC9443636 | core_pubmed_pmc | Right dose, right now: bedside, real-time, data-driven, and personalised antibiotic dosing in critically ill patients with sepsis or septic shock—a two-centre randomised clinical trial | Right dose, right now: bedside, real-time, data-driven, and personalised antibiotic dosing in critically ill patients with sepsis or septic shock—a two-centre randomised clinical trial Abstract Background Adequate antibiotic dosing may improve outcomes in critically ill patients but is challenging due to altered and va... |
PMC9543782 | core_pubmed_pmc | Enantiospecific pharmacokinetics of intravenous dexmedetomidine in beagles | Enantiospecific pharmacokinetics of intravenous dexmedetomidine in beagles Abstract Abstract The goal of this study was to investigate the pharmacokinetic (PK) behaviour of dexmedetomidine in dogs administered as a pure enantiomer versus as part of a racemic mixture. Eight unmedicated intact purpose‐bread beagles were ... |
PMC5912267 | core_pubmed_pmc | Development and 10-year history of a biosimilar: the example of Binocrit ® | Development and 10-year history of a biosimilar: the example of Binocrit ® Abstract Patent expirations for several biological products have prompted the development of alternative versions, termed ‘biosimilars’, which have comparable quality, safety and efficacy to a licensed biological medicine (also referred to as th... |
PMC11726161 | core_pubmed_pmc | Phenol (bio)isosteres in drug design and development | Phenol (bio)isosteres in drug design and development Abstract Abstract Due to their versatile properties, phenolic compounds are integral to various biologically active molecules, including many pharmaceuticals. However, their application in drug design is often hindered by issues such as poor oral bioavailability, rap... |
PMC9971153 | core_pubmed_pmc | Efficacy and Safety of Denosumab Biosimilar QL1206 Versus Denosumab in Patients with Bone Metastases from Solid Tumors: A Randomized Phase III Trial | Efficacy and Safety of Denosumab Biosimilar QL1206 Versus Denosumab in Patients with Bone Metastases from Solid Tumors: A Randomized Phase III Trial Abstract Background Denosumab has been approved for the treatment of bone metastases from solid tumors. QL1206 is the first denosumab biosimilar and needs to be compared w... |
PMC6691630 | core_pubmed_pmc | Time course of psychomotor recovery after intravenous dexmedetomidine infusion as a part of balanced anaesthetic technique: A randomised, double-blind study | Time course of psychomotor recovery after intravenous dexmedetomidine infusion as a part of balanced anaesthetic technique: A randomised, double-blind study Abstract Background and Aims: Dexmedetomidine is a drug that is being widely used as an adjuvant to anaesthesia because of its unique pharmacodynamic and pharmacok... |
PMC11855543 | core_pubmed_pmc | The Combined Effects of Urine Zinc, Cadmium, Mercury, Lead, and Copper on Endometrial Cancer Staging | The Combined Effects of Urine Zinc, Cadmium, Mercury, Lead, and Copper on Endometrial Cancer Staging Abstract Endometrial cancer (EC) is a growing public health concern. This secondary data study of a case series leveraged existing samples and data to explore the potential link between exposure to heavy metals/essentia... |
PMC10347152 | core_pubmed_pmc | Chitosan-Based Nano Systems for Natural Antioxidants in Breast Cancer Therapy | Chitosan-Based Nano Systems for Natural Antioxidants in Breast Cancer Therapy Abstract Breast cancer is a major cause of death globally, accounting for around 13% of all deaths. Chemotherapy, the common treatment for cancer, can have side effects that lead to the production of reactive oxygen species (ROS) and an incre... |
PMC10382374 | core_pubmed_pmc | An individualized digital twin of a patient for transdermal fentanyl therapy for chronic pain management | An individualized digital twin of a patient for transdermal fentanyl therapy for chronic pain management Abstract Fentanyl transdermal therapy is a suitable treatment for moderate-to-severe cancer-related pain. The inter-individual variability of the patients leads to different therapy responses. This study aims to det... |
PMC9134108 | core_pubmed_pmc | Antimicrobial Dosing Recommendations in Pediatric Continuous Renal Replacement Therapy: A Critical Appraisal of Current Evidence | Antimicrobial Dosing Recommendations in Pediatric Continuous Renal Replacement Therapy: A Critical Appraisal of Current Evidence Abstract Abstract Objectives Continuous renal replacement therapy (CRRT) is commonly employed in critically ill children and is known to affect antimicrobial pharmacokinetics. There is a lack... |
PMC5225197 | core_pubmed_pmc | LJM716 in Japanese patients with head and neck squamous cell carcinoma or HER2-overexpressing breast or gastric cancer | LJM716 in Japanese patients with head and neck squamous cell carcinoma or HER2-overexpressing breast or gastric cancer Abstract Abstract Purpose Human epidermal growth factor receptor 3 (HER3) has been identified as an important component of many receptor tyrosine kinase-driven cancers. LJM716 is a human IgG monoclonal... |
PMC8097454 | core_pubmed_pmc | Pharmacokinetic Study of Rectal Artesunate in Children with Severe Malaria in Africa | Pharmacokinetic Study of Rectal Artesunate in Children with Severe Malaria in Africa Abstract When severe malaria is suspected in children, the WHO recommends pretreatment with a single rectal dose of artesunate before referral to an appropriate facility. This was an individually randomized, open-label, 2-arm, crossove... |
PMC12961469 | core_pubmed_pmc | Beyond MIDAS: An In Silico Study of a Putative Noncanonical C16 Binding Site in αvβ3 Integrin | Beyond MIDAS: An In Silico Study of a Putative Noncanonical C16 Binding Site in αvβ3 Integrin Abstract Abstract Integrins are essential transmembrane receptors that mediate bidirectional signaling between the extracellular matrix (ECM) and the cytoskeleton. Among them, αvβ3 and α5β1 are key regulators of angiogenesis, ... |
PMC5364972 | core_pubmed_pmc | Construction and verification of CYP3A5 gene polymorphisms using a Saccharomyces cerevisiae expression system to predict drug metabolism | Construction and verification of CYP3A5 gene polymorphisms using a Saccharomyces cerevisiae expression system to predict drug metabolism Abstract Abstract The present study evaluated the ability of a Saccharomyces cerevisiae expression system to predict the pharmacokinetic (PK) activity of a calcium channel blocker in ... |
PMC4277828 | core_pubmed_pmc | Randomized pharmacokinetic evaluation of different rifabutin doses in African HIV- infected tuberculosis patients on lopinavir/ritonavir-based antiretroviral therapy | Randomized pharmacokinetic evaluation of different rifabutin doses in African HIV- infected tuberculosis patients on lopinavir/ritonavir-based antiretroviral therapy Abstract Background Pharmacokinetic interactions between rifampicin and protease inhibitors (PIs) complicate the management of HIV-associated tuberculosis... |
PMC11284553 | core_pubmed_pmc | Potentiation of the muscarinic acetylcholine receptor 1 modulates neurophysiological features in a mouse model of Rett syndrome | Potentiation of the muscarinic acetylcholine receptor 1 modulates neurophysiological features in a mouse model of Rett syndrome Abstract Rett syndrome (RTT) is a neurodevelopmental disorder primarily caused by mutations in the X chromosome-linked gene Methyl-CpG Binding Protein 2 ( MECP2 ). Restoring MeCP2 expression a... |
PMC5012851 | core_pubmed_pmc | A preliminary evaluation of the relationship of cannabinoid blood concentrations with the analgesic response to vaporized cannabis | A preliminary evaluation of the relationship of cannabinoid blood concentrations with the analgesic response to vaporized cannabis Abstract Abstract A randomized, placebo-controlled crossover trial utilizing vaporized cannabis containing placebo and 6.7% and 2.9% delta-9-tetrahydrocannabinol (THC) was performed in 42 s... |
PMC10333676 | core_pubmed_pmc | Development of KEAP1-targeting PROTAC and its antioxidant properties: In vitro and in vivo | Development of KEAP1-targeting PROTAC and its antioxidant properties: In vitro and in vivo Abstract Oxidative stress due to abnormal accumulation of reactive oxygen species (ROS) is an initiator of a large number of human diseases, and thus, the elimination and prevention of excessive ROS are important aspects of preve... |
PMC10176804 | core_pubmed_pmc | EnGraft: a multicentre, open-label, randomised, two-arm, superiority study protocol to assess bioavailability and practicability of Envarsus® versus Advagraf™ in liver transplant recipients | EnGraft: a multicentre, open-label, randomised, two-arm, superiority study protocol to assess bioavailability and practicability of Envarsus® versus Advagraf™ in liver transplant recipients Abstract Abstract Background Graft rejection and chronic CNI toxicity remain obstacles to organ transplant success. Current formul... |
PMC8224699 | core_pubmed_pmc | Recent Findings on Thymoquinone and Its Applications as a Nanocarrier for the Treatment of Cancer and Rheumatoid Arthritis | Recent Findings on Thymoquinone and Its Applications as a Nanocarrier for the Treatment of Cancer and Rheumatoid Arthritis Abstract Cancer causes a considerable amount of mortality in the world, while arthritis is an immunological dysregulation with multifactorial pathogenesis including genetic and environmental defect... |
PMC7317019 | core_pubmed_pmc | Gene Polymorphisms Affecting the Pharmacokinetics and Pharmacodynamics of Donepezil Efficacy | Gene Polymorphisms Affecting the Pharmacokinetics and Pharmacodynamics of Donepezil Efficacy Abstract Donepezil (DNP) is the first-line drug used for Alzheimer's disease (AD). However, the therapeutic response rate of patients to DNP varies from 20 to 60%. The main reason for the large differences in the clinical effic... |
PMC7920489 | core_pubmed_pmc | Design and Mechanism of Action of a New Prototype of Combi-Molecule “Programed” to Release Bioactive Species at a pH Range Akin to That of the Tumor Microenvironment | Design and Mechanism of Action of a New Prototype of Combi-Molecule “Programed” to Release Bioactive Species at a pH Range Akin to That of the Tumor Microenvironment Abstract Abstract The clinical use of cytotoxic agents is plagued by systemic toxicity. We report a novel approach that seeks to design a “combi-molecule”... |
PMC7211345 | core_pubmed_pmc | Protection of renal damage by HMG-CoA inhibitors: A comparative study between atorvastatin and rosuvastatin | Protection of renal damage by HMG-CoA inhibitors: A comparative study between atorvastatin and rosuvastatin Abstract Objective(s): Hypercholesterolemia is a common metabolic disorder in developing and developed countries and is associated with the increased rates of chronic kidney disease (CKD). Statin therapy could re... |
PMC12567096 | core_pubmed_pmc | An Efficacy- and In Vivo Exposure-Oriented Integrated Study to Investigate the Effective Components of Qishen Granule | An Efficacy- and In Vivo Exposure-Oriented Integrated Study to Investigate the Effective Components of Qishen Granule Abstract Background : Qishen granule (QSG) is a widely prescribed herbal formula for the treatment of chronic heart failure. The mechanisms of action of QSG have been clarified; however, the effective s... |
PMC6071856 | core_pubmed_pmc | Optimizing Clinical Trial Design to Maximize Evidence Generation in Pediatric HIV | Optimizing Clinical Trial Design to Maximize Evidence Generation in Pediatric HIV Abstract Abstract: For HIV-infected children, formulation development, pharmacokinetic (PK) data, and evaluation of early toxicity are critical for licensing new antiretroviral drugs; direct evidence of efficacy in children may not be nee... |
PMC5900965 | core_pubmed_pmc | In Vitro and In Vivo Investigation of Potential for Complex CYP3A Interaction for PF‐00251802 (Dagrocorat), a Novel Dissociated Agonist of the Glucocorticoid Receptor | In Vitro and In Vivo Investigation of Potential for Complex CYP3A Interaction for PF‐00251802 (Dagrocorat), a Novel Dissociated Agonist of the Glucocorticoid Receptor Abstract Abstract The dissociated agonists of the glucocorticoid receptor are a novel class of agents in clinical development for rheumatoid arthritis. P... |
PMC6003283 | core_pubmed_pmc | Pharmacokinetic evaluation of D-ribose after oral and intravenous administration to healthy rabbits | Pharmacokinetic evaluation of D-ribose after oral and intravenous administration to healthy rabbits Abstract Abstract Introduction This study explored D-ribose pharmacokinetics after intravenous (IV) and oral administration to healthy rabbits. Materials and methods D-ribose was administered once as 420 mg/kg (N=4) or 8... |
PMC9639143 | core_pubmed_pmc | Pharmacokinetics of hydroxychloroquine in paediatric lupus: data from a novel, direct-to-family clinical trial | Pharmacokinetics of hydroxychloroquine in paediatric lupus: data from a novel, direct-to-family clinical trial Abstract Abstract Objective Determine the pharmacokinetics (PK) and exposure–response of hydroxychloroquine (HCQ) and desethylhydroxychloroquine (DHCQ) in paediatric SLE (pSLE). Methods We conducted an explora... |
PMC7753357 | core_pubmed_pmc | Population Pharmacokinetics and Model-Based Dosing Optimization of Teicoplanin in Pediatric Patients | Population Pharmacokinetics and Model-Based Dosing Optimization of Teicoplanin in Pediatric Patients Abstract Objectives: The pharmacokinetics (PK) of teicoplanin differs in children compared with adults. Our aim was to determine the PK of teicoplanin in an Asian pediatric population and to optimize dosage regimens. Me... |
PMC8971378 | core_pubmed_pmc | Identification, analysis of deleterious SNPs of the human GSR gene and their effects on the structure and functions of associated proteins and other diseases | Identification, analysis of deleterious SNPs of the human GSR gene and their effects on the structure and functions of associated proteins and other diseases Abstract Abstract Hereditary glutathione reductase deficiency, caused by mutations of the GSR gene, is an autosomal recessive disorder characterized by decreased ... |
PMC5916460 | core_pubmed_pmc | Pharmacokinetics, Safety and Efficacy of Maraviroc in Treatment-experienced Pediatric Patients Infected With CCR5-Tropic HIV-1 | Pharmacokinetics, Safety and Efficacy of Maraviroc in Treatment-experienced Pediatric Patients Infected With CCR5-Tropic HIV-1 Abstract Supplemental Digital Content is available in the text. Background: Maraviroc is a CC-chemokine receptor 5 antagonist approved to treat adults infected with CC-chemokine receptor 5–trop... |
PMC7359142 | core_pubmed_pmc | 10th Anniversary of a Two-Stage Design in Bioequivalence. Why Has it Still Not Been Implemented? | 10th Anniversary of a Two-Stage Design in Bioequivalence. Why Has it Still Not Been Implemented? Abstract Abstract Purpose In 2010 the European Medicines Agency allowed a two-stage design in bioequivalence studies. However, in the public domain there are mainly articles describing the theoretical and statistical base f... |
PMC10819769 | core_pubmed_pmc | Quetiapine-Related Deaths: In Search of a Surrogate Endpoint | Quetiapine-Related Deaths: In Search of a Surrogate Endpoint Abstract Abstract Quetiapine is a second-generation antipsychotic drug available for two and half decades. Due to increased misuse, prescription outside the approved indications, and availability on the black market, it is being encountered in medicolegal aut... |
PMC8945294 | core_pubmed_pmc | Pharmacodynamics and molecular correlates of response to glofitamab in relapsed/refractory non-Hodgkin lymphoma | Pharmacodynamics and molecular correlates of response to glofitamab in relapsed/refractory non-Hodgkin lymphoma Abstract Key Points Glofitamab induced dose-dependent induction of cytokines and T-cell margination, proliferation, and activation in peripheral blood. Tumor cell intrinsic factors (eg, TP53 and MYC signaling... |
PMC12871332 | core_pubmed_pmc | 75 Years of Mathematical Oncology | 75 Years of Mathematical Oncology Abstract Abstract Mathematics has long provided a quantitative framework to interpret cancer biology and treatment. Driven by richer biological and clinical data, the field has evolved into a multidisciplinary and translational endeavor - giving rise to Mathematical Oncology. Yet, the ... |
PMC11616473 | core_pubmed_pmc | Combating PDAC Drug Resistance: The Role of Ref-1 Inhibitors in Accelerating Progress in Pancreatic Cancer Research | Combating PDAC Drug Resistance: The Role of Ref-1 Inhibitors in Accelerating Progress in Pancreatic Cancer Research Abstract Pancreatic Ductal Adenocarcinoma (PDAC) remains one of the most lethal solid tumor diagnoses given its limited treatment options and dismal prognosis. Its complex tumor microenvironment (TME), he... |
PMC3159682 | core_pubmed_pmc | Pharmacokinetics of pirfenidone after topical administration in rabbit eye | Pharmacokinetics of pirfenidone after topical administration in rabbit eye Abstract Purpose Pirfenidone (5-methyl-1-phenyl-2-[1H]-pyridone) is a new, broad-spectrum agent that has an inhibition effect on the proliferation, migration, and collagen contraction of human Tenon’s fibroblasts, and thus modulating the wound h... |
PMC4263185 | core_pubmed_pmc | Contrasting benefits of different artemisinin combination therapies as first-line malaria treatments using model-based cost-effectiveness analysis | Contrasting benefits of different artemisinin combination therapies as first-line malaria treatments using model-based cost-effectiveness analysis Abstract There are currently several recommended drug regimens for uncomplicated falciparum malaria in Africa. Each has different properties that determine its impact on dis... |
PMC11871688 | core_pubmed_pmc | A perspective review on the systematic implementation of ctDNA in phase I clinical trial drug development | A perspective review on the systematic implementation of ctDNA in phase I clinical trial drug development Abstract Abstract Circulating tumour DNA (ctDNA) represents an increasingly important biomarker for the screening, diagnosis and management of patients in clinical practice in advanced/metastatic disease across mul... |
PMC10277867 | core_pubmed_pmc | Mechanistic evaluation of the inhibitory effect of four SGLT-2 inhibitors on SGLT 1 and SGLT 2 using physiologically based pharmacokinetic (PBPK) modeling approaches | Mechanistic evaluation of the inhibitory effect of four SGLT-2 inhibitors on SGLT 1 and SGLT 2 using physiologically based pharmacokinetic (PBPK) modeling approaches Abstract Abstract Sodium-glucose co-transporter type 2 (SGLT 2, gliflozins) inhibitors are potent orally active drugs approved for managing type 2 diabete... |
PMC6005026 | core_pubmed_pmc | Linezolid pharmacokinetics in MDR-TB: a systematic review, meta-analysis and Monte Carlo simulation | Linezolid pharmacokinetics in MDR-TB: a systematic review, meta-analysis and Monte Carlo simulation Abstract Abstract Objectives The oxazolidinone linezolid is an effective component of drug-resistant TB treatment, but its use is limited by toxicity and the optimum dose is uncertain. Current strategies are not informed... |
PMC10741200 | core_pubmed_pmc | Pharmacodynamics of Doripenem Alone and in Combination with Relebactam in an In Vitro Hollow-Fiber Dynamic Model: Emergence of Resistance of Carbapenemase-Producing Klebsiella pneumoniae and the Inoculum Effect | Pharmacodynamics of Doripenem Alone and in Combination with Relebactam in an In Vitro Hollow-Fiber Dynamic Model: Emergence of Resistance of Carbapenemase-Producing Klebsiella pneumoniae and the Inoculum Effect Abstract The emergence of bacteria resistant to beta-lactam/beta-lactamase inhibitor combinations is insuffic... |
PMC10582055 | core_pubmed_pmc | Herb-drug interaction: Effect of sinapic acid on the pharmacokinetics of dasatinib in rats | Herb-drug interaction: Effect of sinapic acid on the pharmacokinetics of dasatinib in rats Abstract Abstract Dasatinib (DAS) is a narrow therapeutic index drug and novel oral multitarget inhibitor of tyrosine kinase and approved for the first-line therapy for chronic myelogenous leukemia (CML) and Philadelphia chromoso... |
PMC7691403 | core_pubmed_pmc | Comparability Considerations and Challenges for Expedited Development Programs for Biological Products | Comparability Considerations and Challenges for Expedited Development Programs for Biological Products Abstract Expedited development programs for biological products to be used in the treatment of serious conditions bring about challenges because of the compressed clinical development timeframes. As expedited developm... |
PMC10309098 | core_pubmed_pmc | Pharmacogenetic interactions of efavirenz or rifampin and isoniazid with levonorgestrel emergency contraception during treatment of HIV or tuberculosis | Pharmacogenetic interactions of efavirenz or rifampin and isoniazid with levonorgestrel emergency contraception during treatment of HIV or tuberculosis Abstract Objective In AIDS Clinical Trials Group study A5375, a pharmacokinetic trial of levonorgestrel emergency contraception, double-dose levonorgestrel (3 mg, versu... |
PMC11442856 | core_pubmed_pmc | Acute dose-dependent effects of mescaline in a double-blind placebo-controlled study in healthy subjects | Acute dose-dependent effects of mescaline in a double-blind placebo-controlled study in healthy subjects Abstract Classic psychedelics have regained interest in research and therapy. Despite the long tradition of the human use of mescaline, modern data on its dose-dependent acute effects and pharmacokinetics are lackin... |
PMC12311132 | core_pubmed_pmc | In silico exploration of anticancer plant phytochemicals for EGFR-targeted lung cancer therapy | In silico exploration of anticancer plant phytochemicals for EGFR-targeted lung cancer therapy Abstract Mutations in the epidermal growth factor receptor (EGFR), particularly in the tyrosine kinase domain such as exon 19 deletions and the L858R point mutation, play a critical role in the development of non-small cell l... |
PMC8971662 | core_pubmed_pmc | A Combined Pharmacometrics Analysis of Biomarker Distribution Under Treatment With Standard- or Low-Dose Rivaroxaban in Real-World Chinese Patients With Nonvalvular Atrial Fibrillation | A Combined Pharmacometrics Analysis of Biomarker Distribution Under Treatment With Standard- or Low-Dose Rivaroxaban in Real-World Chinese Patients With Nonvalvular Atrial Fibrillation Abstract Background: The rivaroxaban dose regimen for patients with nonvalvular atrial fibrillation (NVAF) is complex in Asia. Given th... |
PMC9484173 | core_pubmed_pmc | Evaluation of the food effect on a drospirenone only contraceptive containing 4 mg administered with and without high-fat breakfast in a randomised trial | Evaluation of the food effect on a drospirenone only contraceptive containing 4 mg administered with and without high-fat breakfast in a randomised trial Abstract Background The objective of the present trial was to assess the difference in pharmacokinetics (PK) of an oral test preparation containing 4 mg drospirenone ... |
PMC7830249 | core_pubmed_pmc | Current Limitations and Recent Progress in Nanomedicine for Clinically Available Photodynamic Therapy | Current Limitations and Recent Progress in Nanomedicine for Clinically Available Photodynamic Therapy Abstract Photodynamic therapy (PDT) using oxygen, light, and photosensitizers has been receiving great attention, because it has potential for making up for the weakness of the existing therapies such as surgery, radia... |
PMC11315854 | core_pubmed_pmc | Retrospective Assessment of Translational Pharmacokinetic–Pharmacodynamic Modeling Performance: A Case Study with Apitolisib, a Dual PI3K/mTOR Inhibitor | Retrospective Assessment of Translational Pharmacokinetic–Pharmacodynamic Modeling Performance: A Case Study with Apitolisib, a Dual PI3K/mTOR Inhibitor Abstract Background and Objectives Despite significant progress in biomedical research, the rate of success in oncology drug development remains inferior to that of ot... |
PMC9303875 | core_pubmed_pmc | Pharmacokinetic/Pharmacodynamic Evaluation of Ivosidenib or Enasidenib Combined With Intensive Induction and Consolidation Chemotherapy in Patients With Newly Diagnosed IDH1/2 ‐Mutant Acute Myeloid Leukemia | Pharmacokinetic/Pharmacodynamic Evaluation of Ivosidenib or Enasidenib Combined With Intensive Induction and Consolidation Chemotherapy in Patients With Newly Diagnosed IDH1/2 ‐Mutant Acute Myeloid Leukemia Abstract Abstract Mutant isocitrate dehydrogenase 1/2 (mIDH1/2) proteins catalyze production of the oncometabolit... |
PMC8105874 | core_pubmed_pmc | Intranasal delivery of nanostructured lipid carriers, solid lipid nanoparticles and nanoemulsions: A current overview of in vivo studies | Intranasal delivery of nanostructured lipid carriers, solid lipid nanoparticles and nanoemulsions: A current overview of in vivo studies Abstract The management of the central nervous system (CNS) disorders is challenging, due to the need of drugs to cross the blood‒brain barrier (BBB) and reach the brain. Among the va... |
PMC11573838 | core_pubmed_pmc | Changes in Plasma Clearance of CYP450 Probe Drugs May Not be Specific for Altered In Vivo Enzyme Activity Under (Patho)Physiological Conditions: How to Interpret Findings of Probe Cocktail Studies | Changes in Plasma Clearance of CYP450 Probe Drugs May Not be Specific for Altered In Vivo Enzyme Activity Under (Patho)Physiological Conditions: How to Interpret Findings of Probe Cocktail Studies Abstract Background and objective CYP450 (CYP) phenotyping involves quantifying an individual’s plasma clearance of CYP-spe... |
PMC12685190 | core_pubmed_pmc | Phase 1, randomized, crossover study comparing intravenous GTX-104 to oral nimodipine in healthy human subjects | Phase 1, randomized, crossover study comparing intravenous GTX-104 to oral nimodipine in healthy human subjects Abstract Enterally-administered nimodipine is the only approved drug formulation available in the United States for treatment of patients with aneurysmal subarachnoid hemorrhage. Intravenous nimodipine is ava... |
PMC9804871 | core_pubmed_pmc | Effect of Opicapone on Levodopa Pharmacokinetics in Patients with Fluctuating Parkinson's Disease | Effect of Opicapone on Levodopa Pharmacokinetics in Patients with Fluctuating Parkinson's Disease Abstract ABSTRACT Background Inhibiting catechol‐O‐methyltransferase extends the plasma half‐life of levodopa, potentially allowing physicians to optimize the levodopa regimen in patients with Parkinson's disease (PD) expe... |
PMC5824121 | core_pubmed_pmc | Frequency‐Domain Response Analysis for Quantitative Systems Pharmacology Models | Frequency‐Domain Response Analysis for Quantitative Systems Pharmacology Models Abstract Abstract Drug dosing regimen can significantly impact drug effect and, thus, the success of treatments. Nevertheless, trial and error is still the most commonly used method by conventional pharmacometric approaches to optimize dosi... |
PMC8176636 | core_pubmed_pmc | Pharmacodynamic Correlates of Linezolid Activity and Toxicity in Murine Models of Tuberculosis | Pharmacodynamic Correlates of Linezolid Activity and Toxicity in Murine Models of Tuberculosis Abstract Abstract Background Linezolid (LZD) is bactericidal against Mycobacterium tuberculosis , but it has treatment-limiting toxicities. A better understanding of exposure-response relationships governing LZD efficacy and ... |
Subsets and Splits
No community queries yet
The top public SQL queries from the community will appear here once available.