id
stringlengths
9
11
source
stringclasses
1 value
title
stringlengths
15
560
text
stringlengths
2k
153k
PMC4275252
core_pubmed_pmc
Pharmacokinetic Correlates of the Effects of a Heroin Vaccine on Heroin Self-Administration in Rats
Pharmacokinetic Correlates of the Effects of a Heroin Vaccine on Heroin Self-Administration in Rats Abstract The purpose of this study was to evaluate the effects of a morphine-conjugate vaccine (M-KLH) on the acquisition, maintenance, and reinstatement of heroin self-administration (HSA) in rats, and on heroin and met...
PMC9392492
core_pubmed_pmc
Rhodojaponin III-Loaded Chitosan Derivatives-Modified Solid Lipid Nanoparticles for Multimodal Antinociceptive Effects in vivo
Rhodojaponin III-Loaded Chitosan Derivatives-Modified Solid Lipid Nanoparticles for Multimodal Antinociceptive Effects in vivo Abstract Abstract Background Rhodojaponin III (RJ-III) is a bioactive diterpenoid, which is mainly found in Rhododendron molle G. Don (Ericaceae), a potent analgesia in traditional Chinese medi...
PMC12162526
core_pubmed_pmc
Network-based analysis and experimental validation of identified natural compounds from Yinchen Wuling San for acute myeloid leukemia
Network-based analysis and experimental validation of identified natural compounds from Yinchen Wuling San for acute myeloid leukemia Abstract Objective Traditional Chinese medicine (TCM) has garnered attention for its potential in cancer therapy. Yinchen Wuling San (YWLS), a classical herbal formula, has been traditio...
PMC6861182
core_pubmed_pmc
Pharmacokinetic Data Show That Oxolinic Acid and Flumequine Are Absorbed and Excreted Rapidly From Plasma and Tissues of Lumpfish
Pharmacokinetic Data Show That Oxolinic Acid and Flumequine Are Absorbed and Excreted Rapidly From Plasma and Tissues of Lumpfish Abstract Abstract This study examined the uptake, tissue distribution and elimination of the antibacterial agents oxolinic acid and flumequine in lumpfish ( Cyclopterus lumpus L.) by use of ...
PMC8092915
core_pubmed_pmc
Human Safety, Tolerability, and Pharmacokinetics of Molnupiravir, a Novel Broad-Spectrum Oral Antiviral Agent with Activity against SARS-CoV-2
Human Safety, Tolerability, and Pharmacokinetics of Molnupiravir, a Novel Broad-Spectrum Oral Antiviral Agent with Activity against SARS-CoV-2 Abstract Molnupiravir (EIDD-2801/MK-4482), the prodrug of the active antiviral ribonucleoside analog β- d -N4-hydroxycytidine (NHC; EIDD-1931), has activity against a number of ...
PMC12909280
core_pubmed_pmc
How Can Pharmacology Help Us Overcome the Challenges of Drug Repositioning as Antivirals to Treat Emerging Pathogens? The Example of Covid‐19
How Can Pharmacology Help Us Overcome the Challenges of Drug Repositioning as Antivirals to Treat Emerging Pathogens? The Example of Covid‐19 Abstract ABSTRACT The Covid‐19 pandemic highlighted the urgent need for effective therapies against emerging pathogens. Drug repurposing, defined as the use of existing medicatio...
PMC10068422
core_pubmed_pmc
Hollow-fibre system model of tuberculosis reproducibility and performance specifications for best practice in drug and combination therapy development
Hollow-fibre system model of tuberculosis reproducibility and performance specifications for best practice in drug and combination therapy development Abstract Abstract Background The hollow-fibre system model of tuberculosis (HFS-TB) has been endorsed by regulators; however, application of HFS-TB requires a thorough u...
PMC5100278
core_pubmed_pmc
Comparison of the pharmacokinetics between L-BPA and L-FBPA using the same administration dose and protocol: a validation study for the theranostic approach using [ 18 F]-L-FBPA positron emission tomography in boron neutron capture therapy
Comparison of the pharmacokinetics between L-BPA and L-FBPA using the same administration dose and protocol: a validation study for the theranostic approach using [ 18 F]-L-FBPA positron emission tomography in boron neutron capture therapy Abstract Background Boron neutron capture therapy (BNCT) is a cellular-level par...
PMC11713942
core_pubmed_pmc
A prospective study to evaluate high dose daptomycin pharmacokinetics and pharmacodynamics in Staphylococcus spp. infective endocarditis
A prospective study to evaluate high dose daptomycin pharmacokinetics and pharmacodynamics in Staphylococcus spp. infective endocarditis Abstract Background: Daptomycin pharmacokinetics and pharmacodynamics data relative to higher doses in patients are necessary for clinical practice. Objectives: A monocentric, prospec...
PMC12205714
core_pubmed_pmc
Therapeutic Effect of Brucea Javanica Oil Emulsion in Mice with Irinotecan-Induced Delayed Diarrhea
Therapeutic Effect of Brucea Javanica Oil Emulsion in Mice with Irinotecan-Induced Delayed Diarrhea Abstract Background Chemotherapy-induced diarrhea (CID), particularly delayed diarrhea, often limits clinical use. Brucea javanica oil emulsion (BJOE), an adjuvant chemotherapy agent, has been shown to reduce irinotecan-...
PMC7675389
core_pubmed_pmc
Glasgow Early Treatment Arm Favirpiravir (GETAFIX) for adults with early stage COVID-19: A structured summary of a study protocol for a randomised controlled trial
Glasgow Early Treatment Arm Favirpiravir (GETAFIX) for adults with early stage COVID-19: A structured summary of a study protocol for a randomised controlled trial Abstract Objectives The GETAFIX trial will test the hypothesis that favipiravir is a more effective treatment for COVID-19 infection in patients who have ea...
PMC9047679
core_pubmed_pmc
Flomoxef and fosfomycin in combination for the treatment of neonatal sepsis in the setting of highly prevalent antimicrobial resistance
Flomoxef and fosfomycin in combination for the treatment of neonatal sepsis in the setting of highly prevalent antimicrobial resistance Abstract Abstract Background Neonatal sepsis is a serious bacterial infection of neonates, globally killing up to 680 000 babies annually. It is frequently complicated by antimicrobial...
PMC4186420
core_pubmed_pmc
Metabolism and disposition of MM-433593, a selective FAAH-1 inhibitor, in monkeys
Metabolism and disposition of MM-433593, a selective FAAH-1 inhibitor, in monkeys Abstract Abstract MM-433593 is a highly potent and selective inhibitor of fatty acid amide hydrolase-1 (FAAH-1) with potential utility as an orally administered treatment of pain, inflammation, and other disorders. In this study, we inves...
PMC6341258
core_pubmed_pmc
Fuzzy Evaluation of Pharmacokinetic Models
Fuzzy Evaluation of Pharmacokinetic Models Abstract Abstract Population pharmacokinetic (PopPK) models allow researchers to predict and analyze drug behavior in a population of individuals and to quantify the different sources of variability among these individuals. In the development of PopPK models, the most frequent...
PMC8979343
core_pubmed_pmc
Volatile components in Yinchenzhufu decoction and their pharmacokinetics after oral administration in rats †
Volatile components in Yinchenzhufu decoction and their pharmacokinetics after oral administration in rats † Abstract In China, Yinchenzhufu decoction (YCZFD) has been used to treat cholestatic liver disease in clinical practice for hundreds of years. Nonvolatile components in YCZFD, their composition, components absor...
PMC12400957
core_pubmed_pmc
Therapeutic Targets and Immune Mechanisms of Yinghuang Decoction in Sepsis: Integrating Network Pharmacology, Molecular Docking, and Pharmacokinetic Approaches
Therapeutic Targets and Immune Mechanisms of Yinghuang Decoction in Sepsis: Integrating Network Pharmacology, Molecular Docking, and Pharmacokinetic Approaches Abstract Abstract Background Yinghuang Decoction is an herbal formula that is used for the treatment of sepsis. This study used network pharmacology and molecul...
PMC10536004
core_pubmed_pmc
Gallation and B-Ring Dihydroxylation Increase Green Tea Catechin Residence Time in Plasma by Differentially Affecting Tissue-Specific Trafficking: Compartmental Model of Catechin Kinetics in Healthy Adults
Gallation and B-Ring Dihydroxylation Increase Green Tea Catechin Residence Time in Plasma by Differentially Affecting Tissue-Specific Trafficking: Compartmental Model of Catechin Kinetics in Healthy Adults Abstract Abstract Catechins in green tea extract (GTE) (epigallocatechin gallate (EGCG), epigallocatechin (EGC), e...
PMC3623880
core_pubmed_pmc
Development of a robust flow cytometry-based pharmacodynamic assay to detect phospho-protein signals for phosphatidylinositol 3-kinase inhibitors in multiple myeloma
Development of a robust flow cytometry-based pharmacodynamic assay to detect phospho-protein signals for phosphatidylinositol 3-kinase inhibitors in multiple myeloma Abstract Background The phosphatidylinositol 3-kinase (PI3K) pathway plays an important role in multiple myeloma (MM), a blood cancer associated with unco...
PMC2855344
core_pubmed_pmc
Oral Activated Charcoal Prevents Experimental Cerebral Malaria in Mice and in a Randomized Controlled Clinical Trial in Man Did Not Interfere with the Pharmacokinetics of Parenteral Artesunate
Oral Activated Charcoal Prevents Experimental Cerebral Malaria in Mice and in a Randomized Controlled Clinical Trial in Man Did Not Interfere with the Pharmacokinetics of Parenteral Artesunate Abstract Background Safe, cheap and effective adjunct therapies preventing the development of, or reducing the mortality from, ...
PMC12343208
core_pubmed_pmc
Enhancing the Pharmacokinetics of Aptamers: Targeting AXL In Vivo Using a Bottlebrush Polymer‐Conjugated Aptamer
Enhancing the Pharmacokinetics of Aptamers: Targeting AXL In Vivo Using a Bottlebrush Polymer‐Conjugated Aptamer Abstract Abstract The overexpression of receptor tyrosine kinase AXL receptor tyrosine kinase (AXL) is linked to acquired drug resistance in cancer treatments. Aptamers, acting as antibody surrogates, have b...
PMC7242280
core_pubmed_pmc
Phase 3 Multicenter Study of Revusiran in Patients with Hereditary Transthyretin-Mediated (hATTR) Amyloidosis with Cardiomyopathy (ENDEAVOUR)
Phase 3 Multicenter Study of Revusiran in Patients with Hereditary Transthyretin-Mediated (hATTR) Amyloidosis with Cardiomyopathy (ENDEAVOUR) Abstract Purpose The Phase 3 ENDEAVOUR study evaluated revusiran, an investigational RNA interference therapeutic targeting hepatic transthyretin (TTR) production, for treating c...
PMC7595722
core_pubmed_pmc
Does vancomycin administered at an empirical dose ensure coverage of pediatric patients against gram-positive pathogens?
Does vancomycin administered at an empirical dose ensure coverage of pediatric patients against gram-positive pathogens? Abstract Abstract Objective To investigate the vancomycin effectiveness against gram-positive pathogens with the minimum inhibitory concentration of 1mg/L in pediatric patients based on the area unde...
PMC9948199
core_pubmed_pmc
Discovery of Prodrug of MRTX1133 as an Oral Therapy for Cancers with KRAS G12D Mutation
Discovery of Prodrug of MRTX1133 as an Oral Therapy for Cancers with KRAS G12D Mutation Abstract Abstract Effective oral therapies are urgently required to treat KRAS G12D mutant cancers. Therefore, synthesis and screening were performed for 38 prodrugs of MRTX1133 to identify an oral prodrug of MRTX1133, a KRAS G12D m...
PMC12446003
core_pubmed_pmc
Pharmacological characterization of linaprazan glurate (X842), a novel potassium-competitive acid blocker, in vitro and in vivo
Pharmacological characterization of linaprazan glurate (X842), a novel potassium-competitive acid blocker, in vitro and in vivo Abstract Introduction The aim of this study is to characterize the pharmacology of linaprazan glurate (X842), an ethyl ester prodrug of linaprazan (a novel potassium-competitive acid blocker),...
PMC11284955
core_pubmed_pmc
Chemometric discrimination of eight citrus plants utilizing chromatographic and spectroscopic techniques and insights into their biological potentials
Chemometric discrimination of eight citrus plants utilizing chromatographic and spectroscopic techniques and insights into their biological potentials Abstract Abstract Citrus sinensis balady orange, C. sinensis navel orange, C. paradisi , C. limon, C. sinensis bloody orange, C. sinensis sweet orange, C. aurantium var....
PMC10631828
core_pubmed_pmc
Population pharmacokinetics of a combination of miltefosine and paromomycin in Eastern African children and adults with visceral leishmaniasis
Population pharmacokinetics of a combination of miltefosine and paromomycin in Eastern African children and adults with visceral leishmaniasis Abstract Abstract Objectives To improve visceral leishmaniasis (VL) treatment in Eastern Africa, 14- and 28-day combination regimens of paromomycin plus allometrically dosed mil...
PMC9322346
core_pubmed_pmc
The Impact of CYP2C9*11 Allelic Variant on the Pharmacokinetics of Phenytoin and ( S )‐Warfarin
The Impact of CYP2C9*11 Allelic Variant on the Pharmacokinetics of Phenytoin and ( S )‐Warfarin Abstract Abstract Cytochrome P450 2C9 (CYP2C9) is responsible for the oxidative metabolism of about 15% of commonly used drugs, some of which are characterized by a narrow therapeutic window. CYP2C9 is highly polymorphic, an...
PMC9384469
core_pubmed_pmc
Interpatient variability in the pharmacokinetics of remdesivir and its main metabolite GS-441524 in treated COVID-19 subjects
Interpatient variability in the pharmacokinetics of remdesivir and its main metabolite GS-441524 in treated COVID-19 subjects Abstract Abstract Background Remdesivir is the first antiviral drug against SARS-CoV-2 approved for use in COVID-19 patients. Objectives To study the pharmacokinetic inter-individual variability...
PMC5431696
core_pubmed_pmc
Effect of epigallocatechin-3-gallate, major ingredient of green tea, on the pharmacokinetics of rosuvastatin in healthy volunteers
Effect of epigallocatechin-3-gallate, major ingredient of green tea, on the pharmacokinetics of rosuvastatin in healthy volunteers Abstract Previous in vitro studies have demonstrated the inhibitory effect of green tea on drug transporters. Because rosuvastatin, a lipid-lowering drug widely used for the prevention of c...
PMC12941472
core_pubmed_pmc
Model-Informed Precision Dosing: Conceptual Framework for Therapeutic Drug Monitoring Integrating Machine Learning and Artificial Intelligence Within Population Health Informatics
Model-Informed Precision Dosing: Conceptual Framework for Therapeutic Drug Monitoring Integrating Machine Learning and Artificial Intelligence Within Population Health Informatics Abstract Background/Objective : Traditional therapeutic drug monitoring is limited by manual interpretation and specific constraints like sa...
PMC4926073
core_pubmed_pmc
Absorption and Transport of Sea Cucumber Saponins from Apostichopus japonicus
Absorption and Transport of Sea Cucumber Saponins from Apostichopus japonicus Abstract The present study is focused on the intestinal absorption of sea cucumber saponins. We determined the pharmacokinetic characteristics and bioavailability of Echinoside A and Holotoxin A 1 ; the findings indicated that the bioavailabi...
PMC3808127
core_pubmed_pmc
Intravaginal rings as delivery systems for microbicides and multipurpose prevention technologies
Intravaginal rings as delivery systems for microbicides and multipurpose prevention technologies Abstract There is a renewed interest in delivering pharmaceutical products via intravaginal rings (IVRs). IVRs are flexible torus-shaped drug delivery systems that can be easily inserted and removed by the woman and that pr...
PMC11306058
core_pubmed_pmc
Trabectedin may be a valuable treatment option for elderly patients with metastatic soft tissue sarcomas
Trabectedin may be a valuable treatment option for elderly patients with metastatic soft tissue sarcomas Abstract Abstract Background In the landscape of metastatic soft tissue sarcoma (mSTS) treatment, anthracyclines have shown efficacy; however, their associated toxicity imposes significant limitations, especially in...
PMC7468274
core_pubmed_pmc
A thienopyridine, CB-20, exerts diuretic activity by inhibiting urea transporters
A thienopyridine, CB-20, exerts diuretic activity by inhibiting urea transporters Abstract Urea transporters (UTs) are transmembrane proteins selectively permeable to urea and play an important role in urine concentration. UT-knockout mice exhibit the urea-selective urine-concentrating defect, without affecting electro...
PMC11207855
core_pubmed_pmc
Nano-Delivery of Immunogenic Cell Death Inducers and Immune Checkpoint Blockade Agents: Single-Nanostructure Strategies for Enhancing Immunotherapy
Nano-Delivery of Immunogenic Cell Death Inducers and Immune Checkpoint Blockade Agents: Single-Nanostructure Strategies for Enhancing Immunotherapy Abstract Abstract Cancer immunotherapy has revolutionized oncology by harnessing the patient’s immune system to target and eliminate cancer cells. However, immune checkpoin...
PMC6084441
core_pubmed_pmc
Using exposure prediction tools to link exposure and dosimetry for risk-based decisions: A case study with phthalates
Using exposure prediction tools to link exposure and dosimetry for risk-based decisions: A case study with phthalates Abstract Abstract A few different exposure prediction tools were evaluated for use in the new in vitro-based safety assessment paradigm using di-2-ethylhexyl phthalate (DEHP) and dibutyl phthalate (DnBP...
PMC4660479
core_pubmed_pmc
S LCO1B1 Variants and Angiotensin Converting Enzyme Inhibitor (Enalapril) -Induced Cough: a Pharmacogenetic Study
S LCO1B1 Variants and Angiotensin Converting Enzyme Inhibitor (Enalapril) -Induced Cough: a Pharmacogenetic Study Abstract Abstract Clinical observations suggest that incidence of cough in Chinese taking angiotensin converting enzyme inhibitors is much higher than other racial groups. Cough is the most common adverse r...
PMC8210303
core_pubmed_pmc
A retrospective ‘real-world’ cohort study of azole therapeutic drug monitoring and evolution of antifungal resistance in cystic fibrosis
A retrospective ‘real-world’ cohort study of azole therapeutic drug monitoring and evolution of antifungal resistance in cystic fibrosis Abstract Abstract Background Individuals with cystic fibrosis (CF) have an increased susceptibility to fungal infection/allergy, with triazoles often used as first-line therapy. Thera...
PMC4852941
core_pubmed_pmc
Phase I Study of Oral Vinorelbine in Combination with Erlotinib in Advanced Non-Small Cell Lung Cancer (NSCLC) Using Two Different Schedules
Phase I Study of Oral Vinorelbine in Combination with Erlotinib in Advanced Non-Small Cell Lung Cancer (NSCLC) Using Two Different Schedules Abstract Abstract Purpose This study aimed to evaluate the safety, tolerability and pharmacokinetics of the combination of oral vinorelbine with erlotinib using the conventional (...
PMC6983982
core_pubmed_pmc
Evaluation of Amikacin Pharmacokinetics in Critically Ill Patients with Intra-abdominal Sepsis
Evaluation of Amikacin Pharmacokinetics in Critically Ill Patients with Intra-abdominal Sepsis Abstract Purpose: Although the current widespread use of amikacin is in intra-abdominal sepsis treatment, its pharmacokinetic changes in the present setting are not yet well known. This study was aimed to evaluate the amikaci...
PMC10014691
core_pubmed_pmc
Evaluation of levocetirizine in beagle dog and cynomolgus monkey telemetry assays: Defining the no QTc effect profile by timepoint and concentration‐QTc analysis
Evaluation of levocetirizine in beagle dog and cynomolgus monkey telemetry assays: Defining the no QTc effect profile by timepoint and concentration‐QTc analysis Abstract Abstract In prior clinical studies, levocetirizine (LEVO) has demonstrated no effect on ventricular repolarization (QTc intervals), therefore it is a...
PMC10667364
core_pubmed_pmc
Generation of evidence-based carboplatin dosing guidelines for neonates and infants
Generation of evidence-based carboplatin dosing guidelines for neonates and infants Abstract Abstract Background To optimally dose childhood cancer patients it is essential that we apply evidence-based dosing approaches. Carboplatin is commonly dosed to achieve a cumulative target exposure (AUC) in children, with targe...
PMC6193107
core_pubmed_pmc
Drug Interactions With New Synthetic Opioids
Drug Interactions With New Synthetic Opioids Abstract Abstract Fentanyl, fentanyl analogs, and other new synthetic opioids (NSO) have burst onto the illegal drug market as new psychoactive substances (NPS). They are often sold as heroin to unsuspecting users and produce euphoria through their agonist action on μ- opioi...
PMC12479620
core_pubmed_pmc
Pharmacokinetics, Pharmacodynamics, and Urinary Recovery of Oral Mescaline Hydrochloride in Healthy Participants
Pharmacokinetics, Pharmacodynamics, and Urinary Recovery of Oral Mescaline Hydrochloride in Healthy Participants Abstract Abstract Background and Objective Mescaline is a classic serotonergic psychedelic with a long history of human use. The present study analyzed the pharmacokinetics, pharmacokinetic-pharmacodynamic r...
PMC9398097
core_pubmed_pmc
First-in-Human, Phase 1 Dose-Escalation Study of Biparatopic Anti-HER2 Antibody–Drug Conjugate MEDI4276 in Patients with HER2-positive Advanced Breast or Gastric Cancer
First-in-Human, Phase 1 Dose-Escalation Study of Biparatopic Anti-HER2 Antibody–Drug Conjugate MEDI4276 in Patients with HER2-positive Advanced Breast or Gastric Cancer Abstract Abstract MEDI4276 is a biparatopic tetravalent antibody targeting two nonoverlapping epitopes in subdomains 2 and 4 of the HER2 ecto-domain, w...
PMC6553852
core_pubmed_pmc
Microdialysis combined with liquid chromatography-tandem mass spectrometry for the quantitation of gemifloxacin and its application to a muscle penetration study in healthy and MRSA-infected rats
Microdialysis combined with liquid chromatography-tandem mass spectrometry for the quantitation of gemifloxacin and its application to a muscle penetration study in healthy and MRSA-infected rats Abstract Pharmacological efficacy is based on the drug concentration in target tissues, which usually cannot be represented ...
PMC9867198
core_pubmed_pmc
Long-Term Lithium Therapy: Side Effects and Interactions
Long-Term Lithium Therapy: Side Effects and Interactions Abstract Abstract Lithium remains the drug of first choice for prophylactic treatment of bipolar disorder, preventing the recurrences of manic and depressive episodes. The longitudinal experiences with lithium administration greatly exceed those with other mood s...
PMC11677874
core_pubmed_pmc
Integration of Ontogeny-Based Changes for Predicting the Exposure of Diphenhydramine in the Pediatric Population: A PBPK Modeling Approach
Integration of Ontogeny-Based Changes for Predicting the Exposure of Diphenhydramine in the Pediatric Population: A PBPK Modeling Approach Abstract Background: Diphenhydramine is an anti-tussive used periodically to treat seasonal colds, contact dermatitis, and anaphylactic reactions. This study aimed to develop a phys...
PMC6156480
core_pubmed_pmc
Enhanced Intestinal Permeation of Doxorubicin Using Chitosan Nanoparticles
Enhanced Intestinal Permeation of Doxorubicin Using Chitosan Nanoparticles Abstract Purpose: Due to limited oral bioavailability of doxorubicin (Dox) many efforts during the last decades focused on the development of novel delivery systems to overcome these limitations. In the present study, Dox encapsulated chitosan n...
PMC7472781
core_pubmed_pmc
Inherited and Acquired Determinants of Hepatic CYP3A Activity in Humans
Inherited and Acquired Determinants of Hepatic CYP3A Activity in Humans Abstract Human CYP3A enzymes (including CYP3A4 and CYP4A5) metabolize about 40% of all drugs and numerous other environmental and endogenous substances. CYP3A activity is highly variable within and between humans. As a consequence, therapy with sta...
PMC11933031
core_pubmed_pmc
Effect of CYP3A5 genotypes on pharmacokinetic of tacrolimus in colombian liver transplant patients
Effect of CYP3A5 genotypes on pharmacokinetic of tacrolimus in colombian liver transplant patients Abstract Background Previous studies have reported a reduced tacrolimus dose-adjusted exposure in individuals expressing the CYP3A5*1 allele (rs 776746). However, information regarding Colombian liver transplantation pati...
PMC5409034
core_pubmed_pmc
Aripiprazole Once-Monthly 400 mg: Comparison of Pharmacokinetics, Tolerability, and Safety of Deltoid Versus Gluteal Administration
Aripiprazole Once-Monthly 400 mg: Comparison of Pharmacokinetics, Tolerability, and Safety of Deltoid Versus Gluteal Administration Abstract Abstract Background: Two open-label, randomized, parallel-arm studies compared pharmacokinetics, safety, and tolerability of aripiprazole once-monthly 400 mg following deltoid vs ...
PMC5762438
core_pubmed_pmc
LC–HRMS determination of piperine on rat dried blood spots: A pharmacokinetic study ☆
LC–HRMS determination of piperine on rat dried blood spots: A pharmacokinetic study ☆ Abstract Abstract A liquid chromatography–high resolution mass spectrometry (LC–HRMS) method was developed and validated for the determination of piperine (PPR) on dried blood spots (DBS). DBS samples were prepared by spiking the whol...
PMC11598288
core_pubmed_pmc
Recent Advances in Omics, Computational Models, and Advanced Screening Methods for Drug Safety and Efficacy
Recent Advances in Omics, Computational Models, and Advanced Screening Methods for Drug Safety and Efficacy Abstract Abstract It is imperative to comprehend the mechanisms that underlie drug toxicity in order to enhance the efficacy and safety of novel therapeutic agents. The capacity to identify molecular pathways tha...
PMC4220634
core_pubmed_pmc
Changes in serum creatinine in patients with active rheumatoid arthritis treated with tofacitinib: results from clinical trials
Changes in serum creatinine in patients with active rheumatoid arthritis treated with tofacitinib: results from clinical trials Abstract Introduction Small increases in mean serum creatinine (SCr) were observed in studies of rheumatoid arthritis patients during tofacitinib treatment. These SCr changes were investigated...
PMC8264462
core_pubmed_pmc
Pharmacokinetic comparison with different assays for simultaneous determination of cis-, trans- cefprozil diastereomers in human plasma
Pharmacokinetic comparison with different assays for simultaneous determination of cis-, trans- cefprozil diastereomers in human plasma Abstract The purpose of this study was to compare pharmacokinetic (PK) parameters obtained using two newly developed assays, HPLC-UV and UPLC-ESI-MS/MS. Selection of assay and results ...
PMC5017019
core_pubmed_pmc
The effect of increased lipoproteins levels on the disposition of vincristine in rat
The effect of increased lipoproteins levels on the disposition of vincristine in rat Abstract Background Vincristine (VCR), an antineoplastic agent, is a key component in the treatment of acute lymphoblastic leukemia, lymphomas, rhabdomyosarcoma, neuroblastoma, and Wilms’ tumor diseases. Recently, high incidence of hyp...
PMC8275034
core_pubmed_pmc
Pharmacokinetic Study of Frovatriptan Succinate Tablet After Single and Multiple Oral Doses in Chinese Healthy Subjects
Pharmacokinetic Study of Frovatriptan Succinate Tablet After Single and Multiple Oral Doses in Chinese Healthy Subjects Abstract Abstract Purpose The present report describes findings from a Phase I clinical study that evaluated the single- and multiple-dose pharmacokinetics of frovatriptan succinate tablet in Chinese ...
PMC10728855
core_pubmed_pmc
Dissolving Microneedles Loaded with Gestodene: Fabrication and Characterization In Vitro and In Vivo
Dissolving Microneedles Loaded with Gestodene: Fabrication and Characterization In Vitro and In Vivo Abstract Background Gestodene (GEST) is widely used in female contraception. It is currently being used as an oral contraceptive. However, unfortunately, oral contraceptives are often associated with several bothersome ...
PMC4613335
core_pubmed_pmc
Enantioselective Pharmacokinetics of α-Lipoic Acid in Rats
Enantioselective Pharmacokinetics of α-Lipoic Acid in Rats Abstract Abstract α-Lipoic acid (LA) is widely used for nutritional supplements as a racemic mixture, even though the R enantiomer is biologically active. After oral administration of the racemic mixture ( R -α-lipoic acid (RLA) and S -α-lipoic acid (SLA) mixed...
PMC4790616
core_pubmed_pmc
A multistate tuberculosis pharmacometric model: a framework for studying anti-tubercular drug effects in vitro
A multistate tuberculosis pharmacometric model: a framework for studying anti-tubercular drug effects in vitro Abstract Abstract Objectives Mycobacterium tuberculosis can exist in different states in vitro , which can be denoted as fast multiplying, slow multiplying and non-multiplying. Characterizing the natural growt...
PMC11544293
core_pubmed_pmc
Cocrystal@protein-anchoring nanococktail for combinatorially treating multidrug-resistant cancer
Cocrystal@protein-anchoring nanococktail for combinatorially treating multidrug-resistant cancer Abstract Abstract Multidrug resistance (MDR), the major mechanism by which various cancers develop specific resistance to therapeutic agents, has set up enormous obstacles to many forms of tumor chemotherapy. Traditional co...
PMC8504809
core_pubmed_pmc
Application of a PBPK model to elucidate the changes of systemic and liver exposures for rosuvastatin, carotegrast, and bromfenac followed by OATP inhibition in monkeys
Application of a PBPK model to elucidate the changes of systemic and liver exposures for rosuvastatin, carotegrast, and bromfenac followed by OATP inhibition in monkeys Abstract Abstract The impact of organic anion‐transporting polypeptide (OATP) inhibition on systemic and liver exposures of three OATP substrates was i...
PMC12898389
core_pubmed_pmc
Targeted RNA Degradation by RIBOTACs: A Novel Therapeutic Avenue for Ophthalmic Diseases
Targeted RNA Degradation by RIBOTACs: A Novel Therapeutic Avenue for Ophthalmic Diseases Abstract Abstract Ophthalmic diseases, including inherited retinal dystrophies, age-related macular degeneration (AMD), and glaucomatous neuropathies, are often driven by the expression of pathogenic proteins or dysfunctional non-c...
PMC10040201
core_pubmed_pmc
Lidocaine clearance as pharmacokinetic parameter of metabolic hepatic activity in patients with impaired liver
Lidocaine clearance as pharmacokinetic parameter of metabolic hepatic activity in patients with impaired liver Abstract Background The study aimed to estimate lidocaine (LID) pharmacokinetic parameter values in patients with impaired liver function, level of correlation between the pharmacokinetic parameters and Child-...
PMC8311913
core_pubmed_pmc
TROIKA‐1: A double‐blind, randomized, parallel group, study aimed to demonstrate the equivalent pharmacokinetic profile of HD201, a potential biosimilar candidate to trastuzumab, versus EU‐Herceptin ® and US‐Herceptin ® in healthy male subjects
TROIKA‐1: A double‐blind, randomized, parallel group, study aimed to demonstrate the equivalent pharmacokinetic profile of HD201, a potential biosimilar candidate to trastuzumab, versus EU‐Herceptin ® and US‐Herceptin ® in healthy male subjects Abstract Abstract Prestige Biopharma Ltd (Singapore) has developed HD201, a...
PMC11278686
core_pubmed_pmc
Identification of Anastatica hierochuntica L. Methanolic-Leaf-Extract-Derived Metabolites Exhibiting Xanthine Oxidase Inhibitory Activities: In Vitro and In Silico Approaches
Identification of Anastatica hierochuntica L. Methanolic-Leaf-Extract-Derived Metabolites Exhibiting Xanthine Oxidase Inhibitory Activities: In Vitro and In Silico Approaches Abstract There is a growing interest in the discovery of novel xanthine oxidase inhibitors for gout prevention and treatment with fewer side effe...
PMC12528100
core_pubmed_pmc
Computational insights into novel inhibitors: virtual screening of small molecules against human carbonic anhydrase II
Computational insights into novel inhibitors: virtual screening of small molecules against human carbonic anhydrase II Abstract Abstract Carbonic anhydrases, zinc-based metalloproteins, facilitate the reversible conversion of CO 2 into carbonic acid when transported through blood vessels and subsequently regulate the p...
PMC9065348
core_pubmed_pmc
Evaluation of Potential Herb-Drug Interactions Between Shengmai Injection and Losartan Potassium in Rat and In Vitro
Evaluation of Potential Herb-Drug Interactions Between Shengmai Injection and Losartan Potassium in Rat and In Vitro Abstract Abstract Aim: The present study aimed to explore the potential herb-drug interactions (HDI) between Shengmai injection (SMI) and losartan potassium (LOS) based on the expression profiles of cyto...
PMC4305313
core_pubmed_pmc
A Novel Phthalimide Derivative, TC11, Has Preclinical Effects on High-Risk Myeloma Cells and Osteoclasts
A Novel Phthalimide Derivative, TC11, Has Preclinical Effects on High-Risk Myeloma Cells and Osteoclasts Abstract Abstract Despite the recent advances in the treatment of multiple myeloma (MM), MM patients with high-risk cytogenetic changes such as t(4;14) translocation or deletion of chromosome 17 still have extremely...
PMC11287337
core_pubmed_pmc
Pharmacokinetics and pharmacodynamics of itepekimab in adults with moderate‐to‐severe atopic dermatitis: Results from two terminated phase II trials
Pharmacokinetics and pharmacodynamics of itepekimab in adults with moderate‐to‐severe atopic dermatitis: Results from two terminated phase II trials Abstract Abstract Interleukin‐33 (IL‐33) is a proinflammatory alarmin cytokine released by damaged epithelial tissue cells that initiates and amplifies both type 1 and typ...
PMC12041250
core_pubmed_pmc
Preclinical characterization of an active immunotherapy targeting calcitonin gene-related peptide
Preclinical characterization of an active immunotherapy targeting calcitonin gene-related peptide Abstract Background The success of passive immunotherapies targeting Calcitonin gene-related peptide (CGRP) for managing migraine has prompted our efforts towards developing an active immunotherapy that induces the product...
PMC12677968
core_pubmed_pmc
Design and Antischizophrenic Studies of 1,3-disubstituted Chalcone Derivatives: In-silico Molecular Docking Approach
Design and Antischizophrenic Studies of 1,3-disubstituted Chalcone Derivatives: In-silico Molecular Docking Approach Abstract Abstract Schizophrenia is a psychiatric disorder that affects a person’s ability to think, feel and behave clearly. The pathophysiology of the disease stems from the overexpression of dopamine n...
PMC3885274
core_pubmed_pmc
Pharmaceutical Point of View on Parenteral Nutrition
Pharmaceutical Point of View on Parenteral Nutrition Abstract Parenteral nutrition—a form of administering nutrients, electrolytes, trace elements, vitamins, and water—is a widely used mode of therapy applied in many diseases, in patients of different ages both at home and in hospital. The success of nutritional therap...
PMC9573116
core_pubmed_pmc
Quantification of Acipimox in Plasma and Tissues by LC–MS/MS: Application to Pharmacokinetic Comparison between Normoxia and Hypoxia
Quantification of Acipimox in Plasma and Tissues by LC–MS/MS: Application to Pharmacokinetic Comparison between Normoxia and Hypoxia Abstract Abstract This study aimed to evaluate the pharmacokinetics of acipimox in rats under simulated high altitude hypoxia conditions. A sensitive and reliable LC–MS/MS method has been...
PMC3641736
core_pubmed_pmc
Clinical trials in neonates and children: Report of the pulmonary hypertension academic research consortium pediatric advisory committee
Clinical trials in neonates and children: Report of the pulmonary hypertension academic research consortium pediatric advisory committee Abstract Drug trials in neonates and children with pulmonary hypertensive vascular disease pose unique but not insurmountable challenges. Childhood is defined by growth and developmen...
PMC3001701
core_pubmed_pmc
Pharmacokinetic and pharmacodynamic comparison of two "pegylated" interferon alpha-2 formulations in healthy male volunteers: a randomized, crossover, double-blind study
Pharmacokinetic and pharmacodynamic comparison of two "pegylated" interferon alpha-2 formulations in healthy male volunteers: a randomized, crossover, double-blind study Abstract Abstract Background Interferon (IFN) alpha conjugation to polyethylene glycol (PEG) results in a better pharmacokinetic profile and efficacy....
PMC12265154
core_pubmed_pmc
Phase I first-in-human dose escalation study of the oral casein kinase 1α and cyclin dependent kinase 7/9 inhibitor BTX A51 in advanced MDS and AML
Phase I first-in-human dose escalation study of the oral casein kinase 1α and cyclin dependent kinase 7/9 inhibitor BTX A51 in advanced MDS and AML Abstract Abstract Background BTX A51, a first-in-class oral small molecule inhibitor of casein kinase 1α (CK1α) and cyclin-dependent kinase (CDK) 7 and 9, induces apoptosis...
PMC9782010
core_pubmed_pmc
The Bioavailability of Glycyrrhizinic Acid Was Enhanced by Probiotic Lactobacillus rhamnosus R0011 Supplementation in Liver Fibrosis Rats
The Bioavailability of Glycyrrhizinic Acid Was Enhanced by Probiotic Lactobacillus rhamnosus R0011 Supplementation in Liver Fibrosis Rats Abstract Abstract Glycyrrhizinic acid (GL) is clinically applied to treat liver injury, and the bioavailability of orally administered GL is closely related to the gut microbiota. Th...
PMC9884808
core_pubmed_pmc
Pharmacokinetics, tissue distribution, and antitumor activity of a novel compound, NY-2, in non-small cell lung cancer
Pharmacokinetics, tissue distribution, and antitumor activity of a novel compound, NY-2, in non-small cell lung cancer Abstract Abstract Introduction: ZLDI-8, which has a relatively strong antitumor activity, is an inhibitor of ADAM-17 and acts on the Notch signaling pathway. To further optimize its structure and impro...
PMC12946252
core_pubmed_pmc
YL1004 is a SARS-CoV-2 papain-like protease inhibitor with immunomodulatory and antiviral activity in mice
YL1004 is a SARS-CoV-2 papain-like protease inhibitor with immunomodulatory and antiviral activity in mice Abstract Abstract The evolution of SARS-CoV-2, coupled with its immune evasion mechanisms, underscores the urgent need for antiviral strategies beyond vaccination. The papain-like protease (PL pro ) is a dual-func...
PMC10646788
core_pubmed_pmc
Five-year follow-up of ZUMA-1 supports the curative potential of axicabtagene ciloleucel in refractory large B-cell lymphoma
Five-year follow-up of ZUMA-1 supports the curative potential of axicabtagene ciloleucel in refractory large B-cell lymphoma Abstract Key Points • Axicabtagene ciloleucel induced long-term survival with no new safety signals in patients with refractory LBCL. • Durable responses were associated with expansion of chimeri...
PMC9098754
core_pubmed_pmc
Progress, Challenges, and Prospects of Research on the Effect of Gene Polymorphisms on Adverse Reactions to Opioids
Progress, Challenges, and Prospects of Research on the Effect of Gene Polymorphisms on Adverse Reactions to Opioids Abstract The abuse of opioids has become one of the most serious concerns in the world. Opioid use can cause serious adverse reactions, including respiratory depression, postoperative nausea and vomiting,...
PMC9185832
core_pubmed_pmc
Cancer pharmacomicrobiomics: targeting microbiota to optimise cancer therapy outcomes
Cancer pharmacomicrobiomics: targeting microbiota to optimise cancer therapy outcomes Abstract Despite the promising advances in novel cancer therapy such as immune checkpoint inhibitors (ICIs), limitations including therapeutic resistance and toxicity remain. In recent years, the relationship between gut microbiota an...
PMC4527239
core_pubmed_pmc
Effects of different interchain linkers on biological activity of an anti-prostate cancer single-chain bispecific antibody
Effects of different interchain linkers on biological activity of an anti-prostate cancer single-chain bispecific antibody Abstract Background A single-chain bispecific antibody (scBsAb; an engineered antibody), has promising clinical applications. Nonetheless, the effect of different interchain linkers on its activity...
PMC6270800
core_pubmed_pmc
The Effect of Mini-PEG-Based Spacer Length on Binding and Pharmacokinetic Properties of a 68 Ga-Labeled NOTA-Conjugated Antagonistic Analog of Bombesin
The Effect of Mini-PEG-Based Spacer Length on Binding and Pharmacokinetic Properties of a 68 Ga-Labeled NOTA-Conjugated Antagonistic Analog of Bombesin Abstract Abstract The overexpression of gastrin-releasing peptide receptor (GRPR) in cancer can be used for peptide-receptor mediated radionuclide imaging and therapy. ...
PMC11100723
core_pubmed_pmc
Polymer-tethered quenched fluorescent probes for enhanced imaging of tumor associated proteases
Polymer-tethered quenched fluorescent probes for enhanced imaging of tumor associated proteases Abstract Fluorescence-based contrast agents enable real-time detection of solid tumors and their neovasculature, making them ideal for use in image-guided surgery. Several agents have entered late-stage clinical trials or se...
PMC6698680
core_pubmed_pmc
Cannabidiol reduces seizures following CNS infection with Theiler's murine encephalomyelitis virus
Cannabidiol reduces seizures following CNS infection with Theiler's murine encephalomyelitis virus Abstract Abstract Objective C57BL/6J mice infected with Theiler's murine encephalomyelitis virus (TMEV) develop acute behavioral seizures in the first week of infection and later develop chronic epilepsy. The TMEV model p...
PMC12185575
core_pubmed_pmc
Pharmacokinetics of Ivacaftor, Tezacaftor, Elexacaftor, and Lumacaftor in Special Cystic Fibrosis Populations: A Systematic Review
Pharmacokinetics of Ivacaftor, Tezacaftor, Elexacaftor, and Lumacaftor in Special Cystic Fibrosis Populations: A Systematic Review Abstract Background and Objective Following the development of cystic fibrosis transmembrane conductance regulator (CFTR) modulators (ivacaftor, tezacaftor, elexacaftor, and lumacaftor), th...
PMC5627591
core_pubmed_pmc
Maximizing in vivo target clearance by design of pH-dependent target binding antibodies with altered affinity to FcRn
Maximizing in vivo target clearance by design of pH-dependent target binding antibodies with altered affinity to FcRn Abstract ABSTRACT Antibodies with pH-dependent binding to both target antigens and neonatal Fc receptor (FcRn) provide an alternative tool to conventional neutralizing antibodies, particularly for thera...
PMC9780134
core_pubmed_pmc
Optimized Rhombic Experimental Dynamic Checkerboard Designs to Elucidate Pharmacodynamic Drug Interactions of Antibiotics
Optimized Rhombic Experimental Dynamic Checkerboard Designs to Elucidate Pharmacodynamic Drug Interactions of Antibiotics Abstract Abstract Purpose Quantification of pharmacodynamic interactions is key in combination therapies, yet conventional checkerboard experiments with up to 10 by 10 combinations are labor-intensi...
PMC9772442
core_pubmed_pmc
Joint population pharmacokinetic modeling of venlafaxine and O-desmethyl venlafaxine in healthy volunteers and patients to evaluate the impact of morbidity and concomitant medication
Joint population pharmacokinetic modeling of venlafaxine and O-desmethyl venlafaxine in healthy volunteers and patients to evaluate the impact of morbidity and concomitant medication Abstract Introduction: Venlafaxine (VEN) is a widely used dual selective serotonin/noradrenaline reuptake inhibitor indicated for depress...
PMC6038454
core_pubmed_pmc
Synthesis, Characterization, and Biodistribution of Quantum Dot-Celecoxib Conjugate in Mouse Paw Edema Model
Synthesis, Characterization, and Biodistribution of Quantum Dot-Celecoxib Conjugate in Mouse Paw Edema Model Abstract Abstract Increased risk of cardiovascular side effects has been reported with many of the drugs in the market, including nonsteroidal anti-inflammatory drugs (NSAIDs). Hence, it is critical to thoroughl...
PMC11937984
core_pubmed_pmc
A Phase I Study of the Pharmacokinetics, Pharmacodynamics, and Safety of Liposomal Bupivacaine for Sciatic Nerve Block in the Popliteal Fossa for Bunionectomy
A Phase I Study of the Pharmacokinetics, Pharmacodynamics, and Safety of Liposomal Bupivacaine for Sciatic Nerve Block in the Popliteal Fossa for Bunionectomy Abstract Abstract This trial assessed the pharmacokinetics, pharmacodynamics, and safety of liposomal bupivacaine given via ultrasound‐guided popliteal sciatic n...
PMC9710131
core_pubmed_pmc
Pharmacokinetics of gefitinib in elderly patients with EGFR -mutated advanced non-small cell lung cancer: a prospective study
Pharmacokinetics of gefitinib in elderly patients with EGFR -mutated advanced non-small cell lung cancer: a prospective study Abstract Background Gefitinib is recommended as a first-line treatment option for elderly patients with non-small cell lung cancer (NSCLC). Because no pharmacokinetics of gefitinib have been exa...
PMC10927141
core_pubmed_pmc
Assessing the efficacy of cinnamon compounds against H . pylori through molecular docking, MD Simulations and ADMET analyses
Assessing the efficacy of cinnamon compounds against H . pylori through molecular docking, MD Simulations and ADMET analyses Abstract Abstract Antibiotics are the drugs that are used for the management of microbial diseases. However, these conventional synthetic drugs can harmfully affect the human health. Since phytoc...
PMC11466033
core_pubmed_pmc
A multicentric, randomized, controlled clinical trial to study the impact of bedside model-informed precision dosing of vancomycin in critically ill children—BENEFICIAL trial
A multicentric, randomized, controlled clinical trial to study the impact of bedside model-informed precision dosing of vancomycin in critically ill children—BENEFICIAL trial Abstract Abstract Background Vancomycin is a commonly prescribed antibiotic to treat serious Gram-positive infections in children. The efficacy o...
PMC5585291
core_pubmed_pmc
Current and Emerging Options for the Management of Inherited von Willebrand Disease
Current and Emerging Options for the Management of Inherited von Willebrand Disease Abstract Abstract Von Willebrand disease (VWD) is the most common inherited bleeding disorder with an estimated prevalence of ~1% and clinically relevant bleeding symptoms in approximately 1:10,000 individuals. VWD is caused by a defici...
PMC12799884
core_pubmed_pmc
Advances in genomic and pharmacokinetic profiling for clinical stratification of metastatic breast cancer
Advances in genomic and pharmacokinetic profiling for clinical stratification of metastatic breast cancer Abstract Abstract Background Metastatic breast cancer (MBC) is the most significant clinical challenge in patient care; hence, we need new personalized therapeutic targets and innovative inhibitors. Genomic, proteo...
PMC11363061
core_pubmed_pmc
Cardiovascular Drug Interactions with Nirmatrelvir/Ritonavir for COVID-19: Considerations for Daily Practice
Cardiovascular Drug Interactions with Nirmatrelvir/Ritonavir for COVID-19: Considerations for Daily Practice Abstract Cardiovascular disease is associated with progression to severe COVID-19 and patients with the condition are among those in whom early antiviral therapy should be warranted. The combination of nirmatrel...