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PMC12174120
core_pubmed_pmc
Icariin and related metabolites in fibrosis management: pharmacological properties and molecular mechanism
Icariin and related metabolites in fibrosis management: pharmacological properties and molecular mechanism Abstract Abstract Fibrosis is a pathological hallmark of various chronic diseases and contributes significantly to organ dysfunction and poor clinical outcomes. Despite the availability of antifibrotic agents, the...
PMC10266244
core_pubmed_pmc
Pharmacokinetics and Safety of Multiple-Dose Alpelisib in Participants with Moderate or Severe Hepatic Impairment: A Phase 1, Open-Label, Parallel Group Study
Pharmacokinetics and Safety of Multiple-Dose Alpelisib in Participants with Moderate or Severe Hepatic Impairment: A Phase 1, Open-Label, Parallel Group Study Abstract The pharmacokinetics (PK) and safety of single-dose alpelisib (300 mg) were assessed in participants with moderate to severe hepatic impairment (n = 6 e...
PMC11424876
core_pubmed_pmc
Phase I clinical trial of NH130 and the prediction of its pharmacokinetics using physiologically based pharmacokinetic modeling
Phase I clinical trial of NH130 and the prediction of its pharmacokinetics using physiologically based pharmacokinetic modeling Abstract Abstract Background Parkinson’s disease psychosis (PDP) is a common and distressing complication of Parkinson’s disease (PD), characterized by hallucinations and delusions. This resea...
PMC7027783
core_pubmed_pmc
The Influence of Renal or Hepatic Impairment on the Pharmacokinetics, Safety, and Tolerability of Naldemedine
The Influence of Renal or Hepatic Impairment on the Pharmacokinetics, Safety, and Tolerability of Naldemedine Abstract Abstract Naldemedine is a peripherally acting μ‐opioid‐receptor antagonist for the treatment of opioid‐induced constipation. Two phase 1 single‐dose studies investigated the pharmacokinetics and safety...
PMC9252753
core_pubmed_pmc
Pharmacokinetic Study of Coadministration with Cefuroxime Sodium for Injection Influencing ReDuNing Injection-Derived Seven Phytochemicals and Nine Metabolites in Rats
Pharmacokinetic Study of Coadministration with Cefuroxime Sodium for Injection Influencing ReDuNing Injection-Derived Seven Phytochemicals and Nine Metabolites in Rats Abstract According to the sixth edition of China's “New Coronavirus Diagnosis and Treatment Plan (NCDTP),” ReDuNing injection (RDN) was firstly introduc...
PMC6614152
core_pubmed_pmc
Population Pharmacokinetics of Upadacitinib Using the Immediate-Release and Extended-Release Formulations in Healthy Subjects and Subjects with Rheumatoid Arthritis: Analyses of Phase I–III Clinical Trials
Population Pharmacokinetics of Upadacitinib Using the Immediate-Release and Extended-Release Formulations in Healthy Subjects and Subjects with Rheumatoid Arthritis: Analyses of Phase I–III Clinical Trials Abstract Abstract Background and Objectives Upadacitinib is a selective Janus kinase (JAK) 1 inhibitor being devel...
PMC6639112
core_pubmed_pmc
Exposure Response Supports Therapeutic Drug Monitoring for Dabigatran Etexilate in Patients with Atrial Fibrillation
Exposure Response Supports Therapeutic Drug Monitoring for Dabigatran Etexilate in Patients with Atrial Fibrillation Abstract Abstract Background Dabigatran etexilate has become widely used for the prevention of stroke in patients with nonvalvular atrial fibrillation (NVAF). Currently, there is limited information in r...
PMC7826237
core_pubmed_pmc
Quantitation of Apremilast in Beagle Dogs Plasma by UPLC-MS-MS and Its Application to Pharmacokinetic Studies
Quantitation of Apremilast in Beagle Dogs Plasma by UPLC-MS-MS and Its Application to Pharmacokinetic Studies Abstract A sensitive and selective ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS-MS) method for the determination of apremilast in beagle dog plasma has been developed and successful...
PMC12293736
core_pubmed_pmc
Discovery of N -(6-Methoxypyridin-3-yl)quinoline-2-amine Derivatives for Imaging Aggregated α-Synuclein in Parkinson’s Disease with Positron Emission Tomography
Discovery of N -(6-Methoxypyridin-3-yl)quinoline-2-amine Derivatives for Imaging Aggregated α-Synuclein in Parkinson’s Disease with Positron Emission Tomography Abstract The fibrillary aggregation of α-synuclein is a hallmark of Parkinson’s disease (PD) and a potential target for diagnostics and therapeutics. Although ...
PMC6154210
core_pubmed_pmc
Effect of Tadalafil on Seizure Threshold and Activity of Antiepileptic Drugs in Three Acute Seizure Tests in Mice
Effect of Tadalafil on Seizure Threshold and Activity of Antiepileptic Drugs in Three Acute Seizure Tests in Mice Abstract Tadalafil, a selective phosphodiesterase type 5 inhibitor, is a long-acting oral agent for the treatment of erectile dysfunction of multiple etiologies. Although generalized tonic-clonic seizures w...
PMC7474779
core_pubmed_pmc
Determination and Pharmacokinetics of Okanin in Rat Plasma by UltraHigh Performance Liquid Chromatography Coupled with Triple-Quadrupole Tandem Mass Spectrometry
Determination and Pharmacokinetics of Okanin in Rat Plasma by UltraHigh Performance Liquid Chromatography Coupled with Triple-Quadrupole Tandem Mass Spectrometry Abstract Okanin is a major flavonoid found in Coreopsis tinctoria Nutt., arousing huge interest recently for its considerable biological characteristics inclu...
PMC11015256
core_pubmed_pmc
Oral PD-L1 inhibitor GS-4224 selectively engages PD-L1 high cells and elicits pharmacodynamic responses in patients with advanced solid tumors
Oral PD-L1 inhibitor GS-4224 selectively engages PD-L1 high cells and elicits pharmacodynamic responses in patients with advanced solid tumors Abstract Abstract Background Checkpoint inhibitors targeting the programmed cell death 1 (PD-1)/programmed cell death 1 ligand 1 (PD-L1) pathway are effective therapies in a ran...
PMC10349579
core_pubmed_pmc
Phase I, Single-Dose Study to Assess the Pharmacokinetics and Safety of Suramin in Healthy Chinese Volunteers
Phase I, Single-Dose Study to Assess the Pharmacokinetics and Safety of Suramin in Healthy Chinese Volunteers Abstract Purpose Suramin is a multifunctional molecule with a wide range of potential applications, including parasitic and viral diseases, as well as cancer. Methods A double-blinded, randomized, placebo-contr...
PMC10014546
core_pubmed_pmc
Comparative pharmacokinetics of four major compounds after oral administration of Mori Cortex total flavonoid extract in normal and diabetic rats
Comparative pharmacokinetics of four major compounds after oral administration of Mori Cortex total flavonoid extract in normal and diabetic rats Abstract Abstract Introduction: Mori Cortex has been used in traditional Chinese Medicine as an antidiabetic agent. The aim of this study was to establish a UPLC-MS/MS method...
PMC12030497
core_pubmed_pmc
Plasma Protein Binding, Biostability, Metabolite Profiling, and CYP450 Phenotype of TPB15 Across Different Species: A Novel Smoothened Inhibitor for TNBC Therapy
Plasma Protein Binding, Biostability, Metabolite Profiling, and CYP450 Phenotype of TPB15 Across Different Species: A Novel Smoothened Inhibitor for TNBC Therapy Abstract Background/Objectives : Triple-negative breast cancer (TNBC) is a major cause of cancer-related deaths among women. The Hedgehog (Hh) signaling pathw...
PMC12655758
core_pubmed_pmc
Identification of KKL-35 as a Novel Carnosine Dipeptidase 2 (CNDP2) Inhibitor by In Silico Screening
Identification of KKL-35 as a Novel Carnosine Dipeptidase 2 (CNDP2) Inhibitor by In Silico Screening Abstract Abstract Extracellular glutathione (GSH) is degraded on the cell surface, in which the γ-glutamyl residue is removed to generate cysteine–glycine (Cys–Gly) dipeptides that are subsequently transported to the cy...
PMC4536537
core_pubmed_pmc
A Multidose Study to Examine the Effect of Food on Evacetrapib Exposure at Steady State
A Multidose Study to Examine the Effect of Food on Evacetrapib Exposure at Steady State Abstract Abstract Purpose: To determine the effect of a high-fat meal on evacetrapib exposure at steady state in healthy participants. Methods: This was a randomized, 2-period, 2-sequence, open-label, crossover study. Patients were ...
PMC5662662
core_pubmed_pmc
Low-dose tolvaptan PK/PD: comparison of patients with hyponatremia due to syndrome of inappropriate antidiuretic hormone secretion to healthy adults
Low-dose tolvaptan PK/PD: comparison of patients with hyponatremia due to syndrome of inappropriate antidiuretic hormone secretion to healthy adults Abstract Purpose Tolvaptan (TLV) is indicated to treat hyponatremia due to syndrome of inappropriate diuretic hormone (SIADH) in Europe. Treatment is to be initiated at 15...
PMC9662735
core_pubmed_pmc
Factors associated with variation in single-dose albendazole pharmacokinetics: A systematic review and modelling analysis
Factors associated with variation in single-dose albendazole pharmacokinetics: A systematic review and modelling analysis Abstract Abstract Background Albendazole is an orally administered anti-parasitic medication with widespread usage in a variety of both programmatic and clinical contexts. Previous work has shown th...
PMC6868826
core_pubmed_pmc
Population pharmacokinetics, exposure-safety, and immunogenicity of atezolizumab in pediatric and young adult patients with cancer
Population pharmacokinetics, exposure-safety, and immunogenicity of atezolizumab in pediatric and young adult patients with cancer Abstract Abstract Background The iMATRIX-atezolizumab study was a phase I/II, multicenter, open-label study designed to assess the safety and pharmacokinetics of atezolizumab in pediatric a...
PMC8147502
core_pubmed_pmc
Antibody–Drug Conjugate to Treat Meningiomas
Antibody–Drug Conjugate to Treat Meningiomas Abstract Abstract Meningiomas are primary tumors of the central nervous system with high recurrence. It has been reported that somatostatin receptor 2 (SSTR2) is highly expressed in most meningiomas, but there is no effective targeted therapy approved to control meningiomas....
PMC10787213
core_pubmed_pmc
Toward improved predictions of pharmacokinetics of transported drugs in hepatic impairment: Insights from the extended clearance model
Toward improved predictions of pharmacokinetics of transported drugs in hepatic impairment: Insights from the extended clearance model Abstract Abstract Hepatic impairment (HI) moderately (<5‐fold) affects the systemic exposure (i.e., area under the plasma concentration–time curve [AUC]) of drugs that are substrates of...
PMC6749364
core_pubmed_pmc
Pharmacokinetics and Tissue Distribution of Alnustone in Rats after Intravenous Administration by Liquid Chromatography-Mass Spectrometry
Pharmacokinetics and Tissue Distribution of Alnustone in Rats after Intravenous Administration by Liquid Chromatography-Mass Spectrometry Abstract Abstract Alnustone, a nonphenolic diarylheptanoid, first isolated from Alnus pendula (Betulaceae), has recently received a great deal of attention due to its various benefic...
PMC12620101
core_pubmed_pmc
Delphi Consensus Among French Obesity Experts on Clinical Recommendations for Drug Prescription in Patients With Severe Obesity
Delphi Consensus Among French Obesity Experts on Clinical Recommendations for Drug Prescription in Patients With Severe Obesity Abstract ABSTRACT Introduction Although the physiologic alterations seen in obesity often affect the pharmacokinetics and pharmacodynamics of drugs, most clinical trials do not consider these ...
PMC12302916
core_pubmed_pmc
Protocol for assessing pharmacokinetics and pharmacodynamics of human CAR-NKT cells in humanized mouse models using bioluminescence imaging
Protocol for assessing pharmacokinetics and pharmacodynamics of human CAR-NKT cells in humanized mouse models using bioluminescence imaging Abstract Summary Human invariant natural killer T (NKT) cells exhibit strong tumor-killing ability and bridge innate and adaptive immunity. Peripheral blood mononuclear cell (PBMC)...
PMC5516987
core_pubmed_pmc
Safety and pharmacodynamics of dalazatide, a Kv1.3 channel inhibitor, in the treatment of plaque psoriasis: A randomized phase 1b trial
Safety and pharmacodynamics of dalazatide, a Kv1.3 channel inhibitor, in the treatment of plaque psoriasis: A randomized phase 1b trial Abstract Abstract Background Dalazatide is a specific inhibitor of the Kv1.3 potassium channel. The expression and function of Kv1.3 channels are required for the function of chronical...
PMC5330821
core_pubmed_pmc
Pharmacokinetics and pharmacodynamics of Da-Cheng-Qi decoction in the liver of rats with severe acute pancreatitis
Pharmacokinetics and pharmacodynamics of Da-Cheng-Qi decoction in the liver of rats with severe acute pancreatitis Abstract Abstract AIM To explore the pharmacokinetics and pharmacodynamics of Da-Cheng-Qi decoction (DCQD) in the liver of rats with severe acute pancreatitis (SAP) based on an herbal recipe tissue pharmac...
PMC12029898
core_pubmed_pmc
Cellular Metabolomics Reveals Differences in the Scope of Liver Protection Between Ammonium-Based Glycyrrhizinate and Magnesium Isoglycyrrhizinate
Cellular Metabolomics Reveals Differences in the Scope of Liver Protection Between Ammonium-Based Glycyrrhizinate and Magnesium Isoglycyrrhizinate Abstract Background: Despite the well-established liver-protective efficacy of monoammonium glycyrrhizinate (MONO), diammonium glycyrrhizinate (DIAM), and magnesium isoglycy...
PMC11323360
core_pubmed_pmc
Erdafitinib in Asian patients with advanced solid tumors: an open-label, single-arm, phase IIa trial
Erdafitinib in Asian patients with advanced solid tumors: an open-label, single-arm, phase IIa trial Abstract Background FGFR genomic aberrations occur in approximately 5–10% of human cancers. Erdafitinib has previously demonstrated efficacy and safety in FGFR -altered advanced solid tumors, such as gliomas, thoracic, ...
PMC11947101
core_pubmed_pmc
A phase Ia study of the MEK1/2 inhibitor PD-0325901 with the c-MET inhibitor crizotinib in patients with advanced solid cancers
A phase Ia study of the MEK1/2 inhibitor PD-0325901 with the c-MET inhibitor crizotinib in patients with advanced solid cancers Abstract Abstract Background Single-agent MEK1/2 inhibition has been disappointing in clinical trials targeting RAS mutant (MT) cancers, probably due to upstream receptor activation, resulting...
PMC12460205
core_pubmed_pmc
Pharmacokinetic Comparison of Novel Tablet-in-Tablet and Conventional Ketorolac Tromethamine Tablets in Beagle Dogs
Pharmacokinetic Comparison of Novel Tablet-in-Tablet and Conventional Ketorolac Tromethamine Tablets in Beagle Dogs Abstract Abstract Background and Objective Ketorolac tromethamine (KT), a nonsteroidal anti-inflammatory drug (NSAID) and cyclooxygenase inhibitor, is commonly used for the management of moderate to sever...
PMC10983079
core_pubmed_pmc
Understanding the pharmacokinetic journey of Fc-fusion protein, rhIL-7-hyFc using complementary approach of two analytical methods, accelerator mass spectrometry and ELISA
Understanding the pharmacokinetic journey of Fc-fusion protein, rhIL-7-hyFc using complementary approach of two analytical methods, accelerator mass spectrometry and ELISA Abstract Abstract Antibody-based therapeutics (ABTs), including monoclonal/polyclonal antibodies and fragment crystallizable region (Fc)-fusion prot...
PMC9715946
core_pubmed_pmc
Bioenhancing effects of piperine and curcumin on triterpenoid pharmacokinetics and neurodegenerative metabolomes from Centella asiatica extract in beagle dogs
Bioenhancing effects of piperine and curcumin on triterpenoid pharmacokinetics and neurodegenerative metabolomes from Centella asiatica extract in beagle dogs Abstract Abstract Centell-S is a water-soluble extract of Centella asiatica containing more than 80% w/w triterpenoid glycosides. Madecassoside and asiaticoside ...
PMC6274287
core_pubmed_pmc
Gingerol Synergizes the Cytotoxic Effects of Doxorubicin against Liver Cancer Cells and Protects from Its Vascular Toxicity
Gingerol Synergizes the Cytotoxic Effects of Doxorubicin against Liver Cancer Cells and Protects from Its Vascular Toxicity Abstract Hydroxyphenylalkanes and diarylheptanoids possess potential therapeutic value in different pathophysiological conditions, such as malignancy. In the current study, naturally isolated hydr...
PMC12717868
core_pubmed_pmc
Deciphering the Therapeutic Mechanisms of Banxia Xiexin Decoction Against Ulcerative Colitis: Targeting Pyroptosis and Necroptosis
Deciphering the Therapeutic Mechanisms of Banxia Xiexin Decoction Against Ulcerative Colitis: Targeting Pyroptosis and Necroptosis Abstract Purpose Previous studies have highlighted a strong association between programmed cell death and ulcerative colitis (UC). Banxia Xiexin decoction (BXD) is a thoroughly validated fo...
PMC11554249
core_pubmed_pmc
Simulation-Based Optimization of Sampling Schedules for Model-Informed Precision Dosing of Once-Daily and 4-Times-Daily Busulfan in Pediatric Patients
Simulation-Based Optimization of Sampling Schedules for Model-Informed Precision Dosing of Once-Daily and 4-Times-Daily Busulfan in Pediatric Patients Abstract Supplemental Digital Content is Available in the Text. Background: Therapeutic drug monitoring (TDM) is crucial in optimizing the outcomes of hematopoietic stem...
PMC7927955
core_pubmed_pmc
Evaluation of SNA001, a Novel Recombinant Human Thyroid Stimulating Hormone Injection, in Patients With Differentiated Thyroid Carcinoma
Evaluation of SNA001, a Novel Recombinant Human Thyroid Stimulating Hormone Injection, in Patients With Differentiated Thyroid Carcinoma Abstract Abstract SNA001 is a novel recombinant human thyroid stimulating hormone (rhTSH). rhTSH has long been approved in several countries to facilitate monitoring and ablation of t...
PMC10942359
core_pubmed_pmc
Hyaluronidase impacts exposures of long-acting injectable paliperidone palmitate in rodent models
Hyaluronidase impacts exposures of long-acting injectable paliperidone palmitate in rodent models Abstract Abstract A significant challenge in the development of long-acting injectable drug formulations, especially for anti-infective agents, is delivering an efficacious dose within a tolerable injection volume. Co-admi...
PMC12553988
core_pubmed_pmc
Anti‐Neuroinflammatory and Anti‐Inflammatory Effects of the NLRP3 Inhibitor NT ‐0796 in Subjects with Parkinson's Disease
Anti‐Neuroinflammatory and Anti‐Inflammatory Effects of the NLRP3 Inhibitor NT ‐0796 in Subjects with Parkinson's Disease Abstract Abstract Background Inhibition of Nod‐like receptor protein 3 (NLRP3) inflammasome within the central nervous system (CNS) is a promising therapeutic target for the treatment of Parkinson's...
PMC7472592
core_pubmed_pmc
Pharmacokinetics of Panaxynol in Mice
Pharmacokinetics of Panaxynol in Mice Abstract The purpose of our study is to explore the pharmacokinetic parameters of panaxynol (PA) and understand its potential and dosage used in pre-clinical animal models. For in vitro analysis,5 μM of PA was added to liver microsomes of mouse and human species. Nicotinamide adeni...
PMC6108830
core_pubmed_pmc
Evaluation of a Physiologically Based Pharmacokinetic (PBPK) Model for Inorganic Arsenic Exposure Using Data from Two Diverse Human Populations
Evaluation of a Physiologically Based Pharmacokinetic (PBPK) Model for Inorganic Arsenic Exposure Using Data from Two Diverse Human Populations Abstract Abstract Background: Multiple epidemiological studies exist for some of the well-studied health endpoints associated with inorganic arsenic (iAs) exposure; however, re...
PMC5045912
core_pubmed_pmc
Pharmacokinetics, absorption, and excretion of radiolabeled revexepride: a Phase I clinical trial using a microtracer and accelerator mass spectrometry-based approach
Pharmacokinetics, absorption, and excretion of radiolabeled revexepride: a Phase I clinical trial using a microtracer and accelerator mass spectrometry-based approach Abstract Purpose Gastroesophageal reflux disease involves the reflux of gastric and/or duodenal content into the esophagus. Prokinetic therapies, such as...
PMC4585485
core_pubmed_pmc
A Single-Center, Open-Label, 3-Way Crossover Trial to Determine the Pharmacokinetic and Pharmacodynamic Interaction Between Nebivolol and Valsartan in Healthy Volunteers at Steady State
A Single-Center, Open-Label, 3-Way Crossover Trial to Determine the Pharmacokinetic and Pharmacodynamic Interaction Between Nebivolol and Valsartan in Healthy Volunteers at Steady State Abstract Combining different classes of antihypertensives is more effective for reducing blood pressure (BP) than increasing the dose ...
PMC6609384
core_pubmed_pmc
Pharmacokinetics of cucurbitacin B from Trichosanthes cucumerina L. in rats
Pharmacokinetics of cucurbitacin B from Trichosanthes cucumerina L. in rats Abstract Background Cucurbitacin B is the major bioactive constituent in Trichosanthes cucumerina L. fruits, which the pharmacological properties have been studied for decades particularly an anti-tumor activity. The pharmacokinetic profile of ...
PMC7013290
core_pubmed_pmc
Targeting Refractory Sarcomas and Malignant Peripheral Nerve Sheath Tumors in a Phase I/II Study of Sirolimus in Combination with Ganetespib (SARC023)
Targeting Refractory Sarcomas and Malignant Peripheral Nerve Sheath Tumors in a Phase I/II Study of Sirolimus in Combination with Ganetespib (SARC023) Abstract Purpose Malignant peripheral nerve sheath tumors (MPNSTs) are aggressive soft tissue sarcomas. Combining Hsp90 inhibitors to enhance endoplasmic reticulum stres...
PMC12888458
core_pubmed_pmc
Impact of aging on the pharmacokinetic profile of everolimus in male mice
Impact of aging on the pharmacokinetic profile of everolimus in male mice Abstract Abstract Background Age-related changes in drug-metabolizing enzymes and transporters can alter pharmacokinetics, yet data on everolimus, a widely used mTOR inhibitor, remain limited. This study investigated the pharmacokinetic profile o...
PMC11573861
core_pubmed_pmc
Effect of Age, Sex, Renal Impairment and Hepatic Impairment on the Safety, Pharmacokinetics and Pharmacodynamics of Asundexian
Effect of Age, Sex, Renal Impairment and Hepatic Impairment on the Safety, Pharmacokinetics and Pharmacodynamics of Asundexian Abstract Abstract Introduction Asundexian is a reversible and selective inhibitor of activated factor XI. It is currently under investigation for the prevention of secondary stroke in at-risk p...
PMC5999174
core_pubmed_pmc
Extrapolation of a Brivaracetam Exposure–Response Model from Adults to Children with Focal Seizures
Extrapolation of a Brivaracetam Exposure–Response Model from Adults to Children with Focal Seizures Abstract Introduction Prediction of brivaracetam effects in children was obtained by scaling an existing adult pharmacokinetic/pharmacodynamic (PK/PD) model for brivaracetam to children, using an existing population PK m...
PMC12778514
core_pubmed_pmc
Current and Future Treatment Options for Cerebral Cavernous Malformations
Current and Future Treatment Options for Cerebral Cavernous Malformations Abstract Abstract Cerebral cavernous malformations (CCMs) are vascular lesions associated with seizures, hemorrhage, and neurologic deficits. The familial form of CCM constitutes ≈20% of cases and presents with multifocal lesions in the brain and...
PMC4877646
core_pubmed_pmc
Next-generation proteasome inhibitor MLN9708 sensitizes breast cancer cells to doxorubicin-induced apoptosis
Next-generation proteasome inhibitor MLN9708 sensitizes breast cancer cells to doxorubicin-induced apoptosis Abstract Abstract Doxorubicin (Dox), one of the most effective chemotherapy drug for cancer treatment, is limited by its severe side effects and chemoresistance. Dox induces DNA damage and leads to significant p...
PMC7178892
core_pubmed_pmc
Effects of glycyrrhizin on the pharmacokinetics of nobiletin in rats and its potential mechanism
Effects of glycyrrhizin on the pharmacokinetics of nobiletin in rats and its potential mechanism Abstract Abstract Context Both nobiletin (NBL) and glycyrrhizin (GL) have anti-inflammatory and antitumor properties. These agents may be co-administered in the clinic. However, the drug–drug interaction between them is not...
PMC4695662
core_pubmed_pmc
Arsenic and Mercury Containing Traditional Chinese Medicine (Realgar and Cinnabar) Strongly Inhibit Organic Anion Transporters, Oat1 and Oat3, In Vivo in Mice
Arsenic and Mercury Containing Traditional Chinese Medicine (Realgar and Cinnabar) Strongly Inhibit Organic Anion Transporters, Oat1 and Oat3, In Vivo in Mice Abstract Abstract Toxic heavy metals, including mercury (Hg) and arsenic (As), accumulate preferentially in kidneys and always cause acute renal failure. The aim...
PMC7028097
core_pubmed_pmc
Pharmacokinetics, Safety, and Efficacy of Glecaprevir/Pibrentasvir in Adolescents With Chronic Hepatitis C Virus: Part 1 of the DORA Study
Pharmacokinetics, Safety, and Efficacy of Glecaprevir/Pibrentasvir in Adolescents With Chronic Hepatitis C Virus: Part 1 of the DORA Study Abstract Abstract The pangenotypic regimen of glecaprevir and pibrentasvir (G/P) is approved to treat adults with chronic hepatitis C virus (HCV) infection and has yielded high cure...
PMC9413960
core_pubmed_pmc
Factors Affecting the Metabolic Conversion of Ciprofloxacin and Exposure to Its Main Active Metabolites in Critically Ill Patients: Population Pharmacokinetic Analysis of Desethylene Ciprofloxacin
Factors Affecting the Metabolic Conversion of Ciprofloxacin and Exposure to Its Main Active Metabolites in Critically Ill Patients: Population Pharmacokinetic Analysis of Desethylene Ciprofloxacin Abstract The objective of this prospective study was to examine the exposure to the main active metabolites of ciprofloxaci...
PMC4811835
core_pubmed_pmc
Oritavancin: A New Lipoglycopeptide Antibiotic in the Treatment of Gram-Positive Infections
Oritavancin: A New Lipoglycopeptide Antibiotic in the Treatment of Gram-Positive Infections Abstract Abstract Resistance among Gram-positive organisms has been steadily increasing over the last several years; however, the development of new antibiotics to treat infections caused from these organisms has fallen short of...
PMC11040566
core_pubmed_pmc
Current approaches in smart nano‐inspired drug delivery: A narrative review
Current approaches in smart nano‐inspired drug delivery: A narrative review Abstract Abstract Background and Aim The traditional drug delivery approach involves systemic administration of a drug that could be nonspecific in targeting, low on efficacy, and with severe side‐effects. To address such challenges, the field ...
PMC9783836
core_pubmed_pmc
Comparative Pharmacokinetic of Curcuminoids Formulations with an Omega-3 Fatty Acids Monoglyceride Carrier: A Randomized Cross-Over Triple-Blind Study
Comparative Pharmacokinetic of Curcuminoids Formulations with an Omega-3 Fatty Acids Monoglyceride Carrier: A Randomized Cross-Over Triple-Blind Study Abstract There is a growing interest for curcuminoids in the general population and the scientific research community. Curcuminoids, derived from turmeric spice, are lip...
PMC5489626
core_pubmed_pmc
Postnatal Maturation of the Glomerular Filtration Rate in Conventional Growing Piglets As Potential Juvenile Animal Model for Preclinical Pharmaceutical Research
Postnatal Maturation of the Glomerular Filtration Rate in Conventional Growing Piglets As Potential Juvenile Animal Model for Preclinical Pharmaceutical Research Abstract Abstract Adequate animal models are required to study the preclinical pharmacokinetics (PK), pharmacodynamics (PD) and safety of drugs in the pediatr...
PMC11033648
core_pubmed_pmc
Phase 1a dose escalation study of ivonescimab (AK112/SMT112), an anti-PD-1/VEGF-A bispecific antibody, in patients with advanced solid tumors
Phase 1a dose escalation study of ivonescimab (AK112/SMT112), an anti-PD-1/VEGF-A bispecific antibody, in patients with advanced solid tumors Abstract Abstract Background Studies showed that vascular endothelial growth factor (VEGF) inhibitors could improve therapeutic efficacy of PD-1/PD-L1 antibodies by transforming ...
PMC11289878
core_pubmed_pmc
Toward once-monthly insulin therapy via synergy in two pharmacokinetic protractors: Fc-conjugation and fatty acid acylation †
Toward once-monthly insulin therapy via synergy in two pharmacokinetic protractors: Fc-conjugation and fatty acid acylation † Abstract Abstract Pharmacokinetic properties and duration of therapeutic action of a pharmaceutical agent can be significantly extended through the combination of two distinct strategies aimed a...
PMC11703681
core_pubmed_pmc
Double dosing ulipristal acetate emergency contraception for individuals with obesity: a randomised crossover trial
Double dosing ulipristal acetate emergency contraception for individuals with obesity: a randomised crossover trial Abstract Abstract Objective To determine whether increasing the dose of ulipristal acetate (UPA)-containing emergency contraception (EC) improves pharmacodynamic outcomes in individuals with obesity. Stud...
PMC4804046
core_pubmed_pmc
Pharmacokinetics of Immediate and Sustained Release Cephalexin Administered by Different Routes to Llamas ( Lama glama )
Pharmacokinetics of Immediate and Sustained Release Cephalexin Administered by Different Routes to Llamas ( Lama glama ) Abstract Abstract We investigate the pharmacokinetics of two different cephalexin formulations administered to llamas by the intravenous (IV), intramuscular (IM), and subcutaneous (SC) routes, the mi...
PMC7857576
core_pubmed_pmc
Safety, acceptability, and pharmacokinetics of a monoclonal antibody-based vaginal multipurpose prevention film (MB66): A Phase I randomized trial
Safety, acceptability, and pharmacokinetics of a monoclonal antibody-based vaginal multipurpose prevention film (MB66): A Phase I randomized trial Abstract Abstract Background MB66 film is a multipurpose prevention technology (MPT) product with monoclonal antibodies (mAbs) against HIV-1 (VRC01-N) and HSV-1 and 2 (HSV8-...
PMC7127779
core_pubmed_pmc
Preparation, Characterization, and in vivo Evaluation of NK4-Conjugated Hydroxycamptothecin-Loaded Liposomes
Preparation, Characterization, and in vivo Evaluation of NK4-Conjugated Hydroxycamptothecin-Loaded Liposomes Abstract Purpose In this study, NK4-conjugated hydroxycamptothecin liposomes (NK4-HCPT-Lips) were prepared with the aim of improving drug targeting to the liver. Methods NK4-HCPT-Lips were prepared using the thi...
PMC11539218
core_pubmed_pmc
Synthesis of a dehydrodieugenol B derivative as a lead compound for visceral leishmaniasis—mechanism of action and in vivo pharmacokinetic studies
Synthesis of a dehydrodieugenol B derivative as a lead compound for visceral leishmaniasis—mechanism of action and in vivo pharmacokinetic studies Abstract ABSTRACT Leishmaniasis is a parasitic neglected tropical disease, affecting 12 million people. Available treatments present several limitations, with an increasing ...
PMC8434305
core_pubmed_pmc
Novel Antiretroviral Therapeutic Strategies for HIV
Novel Antiretroviral Therapeutic Strategies for HIV Abstract Abstract When the first cases of HIV infection appeared in the 1980s, AIDS was a deadly disease without any therapeutic alternatives. Currently, there is still no cure for most cases mainly due to the multiple tissues that act as a reservoir for this virus be...
PMC11435310
core_pubmed_pmc
PBPK Modeling of Lamotrigine and Efavirenz during Pregnancy: Implications for Personalized Dosing and Drug-Drug Interaction Management
PBPK Modeling of Lamotrigine and Efavirenz during Pregnancy: Implications for Personalized Dosing and Drug-Drug Interaction Management Abstract Abstract This study aimed to model the pharmacokinetics of lamotrigine (LTG) and efavirenz (EFV) in pregnant women using physiologically based pharmacokinetic (PBPK) and pregna...
PMC11352679
core_pubmed_pmc
Confirming the Suitability of a Gentamicin Dosing Strategy in Neonates Using the Population Pharmacokinetic Approach with Truncated Sampling Duration
Confirming the Suitability of a Gentamicin Dosing Strategy in Neonates Using the Population Pharmacokinetic Approach with Truncated Sampling Duration Abstract Abstract (1) Background: Gentamicin is known to be nephrotoxic and ototoxic. Although gentamicin dosage guidelines have been established for preterm and term neo...
PMC10333524
core_pubmed_pmc
Brensocatib, an oral, reversible inhibitor of dipeptidyl peptidase 1, mitigates interferon-α-accelerated lupus nephritis in mice
Brensocatib, an oral, reversible inhibitor of dipeptidyl peptidase 1, mitigates interferon-α-accelerated lupus nephritis in mice Abstract Neutrophils have been implicated in initiating and perpetuating systemic lupus erythematosus and the resultant kidney damage in lupus nephritis (LN) patients, in part through an exce...
PMC12535016
core_pubmed_pmc
Curcumin in prostate cancer: a systematic review of molecular mechanisms and nanoformulated therapeutic strategies
Curcumin in prostate cancer: a systematic review of molecular mechanisms and nanoformulated therapeutic strategies Abstract Background Prostate cancer (PCa) is one of the most prevalent malignancies in men, often progressing to castration-resistant forms and resisting conventional therapies. Curcumin, a polyphenol from...
PMC12597975
core_pubmed_pmc
Real‐World Impact of Amiodarone on Apixaban Population Pharmacokinetics in Hospitalized Patients
Real‐World Impact of Amiodarone on Apixaban Population Pharmacokinetics in Hospitalized Patients Abstract ABSTRACT Despite common coadministration in nonvalvular atrial fibrillation (NVAF), there is minimal evidence regarding the impact of concomitant amiodarone use on apixaban pharmacokinetics (PK). We described the p...
PMC3817374
core_pubmed_pmc
Modeling Alzheimer's Disease Progression Using Disease Onset Time and Disease Trajectory Concepts Applied to CDR-SOB Scores From ADNI
Modeling Alzheimer's Disease Progression Using Disease Onset Time and Disease Trajectory Concepts Applied to CDR-SOB Scores From ADNI Abstract Abstract Disease-onset time (DOT) and disease trajectory concepts were applied to derive an Alzheimer's disease (AD) progression population model using the clinical dementia rat...
PMC7495284
core_pubmed_pmc
The effect of food and formulation on the population pharmacokinetics of cholesteryl ester transferase protein inhibitor DRL‐17822 in healthy male volunteers
The effect of food and formulation on the population pharmacokinetics of cholesteryl ester transferase protein inhibitor DRL‐17822 in healthy male volunteers Abstract Abstract We aimed to characterise the population pharmacokinetics of cholesteryl ester transferase protein inhibitor DRL‐17822 in healthy males and explo...
PMC3104800
core_pubmed_pmc
Pharmacokinetics of intravitreal bevacizumab (Avastin ® ) in rabbits
Pharmacokinetics of intravitreal bevacizumab (Avastin ® ) in rabbits Abstract Purpose: To describe the pharmacokinetics of intravitreal bevacizumab (Avastin ® ) in rabbits. Methods: The right eye of 20 rabbits was injected intravitreally with 1.25 mg/0.05 mL bevacizumab. Both eyes of four rabbits each time were enuclea...
PMC6130699
core_pubmed_pmc
Determination of dihydromyricetin in rat plasma by LC-MS/MS and its application to a pharmacokinetic study
Determination of dihydromyricetin in rat plasma by LC-MS/MS and its application to a pharmacokinetic study Abstract Abstract Context: The pharmacokinetics properties of dihydromyricetin (DHM) are still unknown. Objective: This study investigates the pharmacokinetic characteristics of DHM using a sensitive and reliable ...
PMC12346835
core_pubmed_pmc
Progress in Pharmacokinetics, Pharmacological Effects, and Molecular Mechanisms of Swertiamarin: A Comprehensive Review
Progress in Pharmacokinetics, Pharmacological Effects, and Molecular Mechanisms of Swertiamarin: A Comprehensive Review Abstract Abstract Swertiamarin (SW), a natural iridoid glycoside primarily isolated from the genus Swertia , Gentianaceae family, has been extensively utilized in traditional medicine systems, includi...
PMC9053626
core_pubmed_pmc
In vivo and in vitro evaluation of dihydroartemisinin prodrug nanocomplexes as a nano-drug delivery system: characterization, pharmacokinetics and pharmacodynamics †
In vivo and in vitro evaluation of dihydroartemisinin prodrug nanocomplexes as a nano-drug delivery system: characterization, pharmacokinetics and pharmacodynamics † Abstract To develop new, more effective and lower toxicity antitumor dihydroartemisinin (DHA) nanocomplexes, a DHA prodrug synthesized in this study was u...
PMC12695902
core_pubmed_pmc
Delay-aware chemotherapy dosing via online critic learning
Delay-aware chemotherapy dosing via online critic learning Abstract This paper proposes a delay-aware adaptive control framework for individualized chemotherapy dosing based on online critic learning. The approach explicitly compensates for pharmacokinetic and pharmacodynamic delays while adapting to patient-specific u...
PMC2845183
core_pubmed_pmc
Nonlinear mixed effects modeling of gametocyte carriage in patients with uncomplicated malaria
Nonlinear mixed effects modeling of gametocyte carriage in patients with uncomplicated malaria Abstract Abstract Background Gametocytes are the sexual form of the malaria parasite and the main agents of transmission. While there are several factors that influence host infectivity, the density of gametocytes appears to ...
PMC12418703
core_pubmed_pmc
Avenanthramides and avenacosides as biomarkers of oat intake: a pharmacokinetic study of solid and liquid oat consumption under single and repeated dose conditions
Avenanthramides and avenacosides as biomarkers of oat intake: a pharmacokinetic study of solid and liquid oat consumption under single and repeated dose conditions Abstract Abstract Background Avenanthramides (AVAs) and Avenacosides (AVEs) are unique to oats ( Avena Sativa ) and may serve as biomarkers of oat intake. H...
PMC12511509
core_pubmed_pmc
The Effects of Cobicistat and Voriconazole on the Safety, Pharmacokinetics, and Pharmacodynamics of the TLR7 Agonist Vesatolimod in People with HIV
The Effects of Cobicistat and Voriconazole on the Safety, Pharmacokinetics, and Pharmacodynamics of the TLR7 Agonist Vesatolimod in People with HIV Abstract Abstract Introduction Vesatolimod (VES), a toll-like receptor 7 agonist, is being investigated as part of a strategy for human immunodeficiency virus (HIV) cure. V...
PMC5760983
core_pubmed_pmc
Application of UPLC–MS/MS for separation and quantification of 3α-Hydroxy Tibolone and comparative bioavailability of two Tibolone formulations in healthy volunteers
Application of UPLC–MS/MS for separation and quantification of 3α-Hydroxy Tibolone and comparative bioavailability of two Tibolone formulations in healthy volunteers Abstract Abstract A novel, fast, sensitive and robust method based on ultra-performance liquid chromatography coupled to atmospheric pressure electrospray...
PMC9309149
core_pubmed_pmc
Cost-Effectiveness Analysis of Pharmacokinetic-Guided Prophylaxis Versus Standard Prophylaxis in Adults with Severe Hemophilia A in China
Cost-Effectiveness Analysis of Pharmacokinetic-Guided Prophylaxis Versus Standard Prophylaxis in Adults with Severe Hemophilia A in China Abstract Introduction Multiple studies have demonstrated the effectiveness of pharmacokinetic (PK)-guided individualized prophylaxis with human coagulation factor VIII (FVIII) compar...
PMC7040550
core_pubmed_pmc
Use of GMI‐1271, an E‐selectin antagonist, in healthy subjects and in 2 patients with calf vein thrombosis
Use of GMI‐1271, an E‐selectin antagonist, in healthy subjects and in 2 patients with calf vein thrombosis Abstract Abstract Background There is an unmet need for antithrombotic treatments for venous thromboembolic disease that do not increase bleeding risk. Selectins are cell adhesion molecules that augment thrombosis...
PMC12613440
core_pubmed_pmc
A novel pregabalin functionalized salicylaldehyde derivative loaded mesoporous silica nano scaffold: a prospective carrier for targeting inflammatory cytokine storm
A novel pregabalin functionalized salicylaldehyde derivative loaded mesoporous silica nano scaffold: a prospective carrier for targeting inflammatory cytokine storm Abstract Active pharmaceutical ingredients (APIs) have poor efficacy and low bloodstream and target site concentrations due to their limited water solubili...
PMC5036556
core_pubmed_pmc
Comparisons of the pharmacokinetics and tolerability of fixed-dose combinations of amlodipine besylate/losartan and amlodipine camsylate/losartan in healthy subjects: a randomized, open-label, single-dose, two-period, two-sequence crossover study
Comparisons of the pharmacokinetics and tolerability of fixed-dose combinations of amlodipine besylate/losartan and amlodipine camsylate/losartan in healthy subjects: a randomized, open-label, single-dose, two-period, two-sequence crossover study Abstract Abstract Background A fixed-dose combination (FDC) of amlodipine...
PMC4329209
core_pubmed_pmc
Calcineurin inhibitors differentially alter the circadian rhythm of T-cell functionality in transplant recipients
Calcineurin inhibitors differentially alter the circadian rhythm of T-cell functionality in transplant recipients Abstract Abstract Background Graft survival in transplant recipients depends on pharmacokinetics and on individual susceptibility towards immunosuppressive drugs. Nevertheless, pharmacodynamic changes in T-...
PMC12322894
core_pubmed_pmc
Evaluation of the relationship between cytochrome P450 (CYP) 1A2 gene copy number variation and CYP1A2 protein content and enzyme activity in canine liver
Evaluation of the relationship between cytochrome P450 (CYP) 1A2 gene copy number variation and CYP1A2 protein content and enzyme activity in canine liver Abstract Abstract Cytochrome P450 (CYP) 1A2 plays a key role in the metabolism of various drugs in dogs. However, the impact of genetic variation on differences in C...
PMC12805780
core_pubmed_pmc
Prolonged infusion of remimazolam in surgical and medical intensive care unit patients: a pilot pharmacokinetic study
Prolonged infusion of remimazolam in surgical and medical intensive care unit patients: a pilot pharmacokinetic study Abstract Abstract Background The pharmacokinetics of prolonged remimazolam infusion in patients undergoing long-term mechanical ventilation remain unclear. This study aimed to evaluate the pharmacokinet...
PMC6440985
core_pubmed_pmc
Heterogeneous drug tissue binding in brain regions of rats, Alzheimer’s patients and controls: impact on translational drug development
Heterogeneous drug tissue binding in brain regions of rats, Alzheimer’s patients and controls: impact on translational drug development Abstract Abstract For preclinical and clinical assessment of therapeutically relevant unbound, free, brain concentrations, the pharmacokinetic parameter fraction of unbound drug in bra...
PMC11488264
core_pubmed_pmc
Recruitment of pregnant and breastfeeding women in pharmacokinetic studies: strategies, opportunities, barriers, and recommendations
Recruitment of pregnant and breastfeeding women in pharmacokinetic studies: strategies, opportunities, barriers, and recommendations Abstract Abstract Pregnant and breastfeeding women are often under-represented in clinical research, including pharmacokinetic studies, due to ethical and logistical challenges. This pape...
PMC9755917
core_pubmed_pmc
Dose/exposure–response modeling in dose titration trials: Overcoming the titration paradox
Dose/exposure–response modeling in dose titration trials: Overcoming the titration paradox Abstract Abstract Response‐based dose individualization or dose titration is a powerful approach to achieve precision dosing. Yet, titration as an individualization strategy is underused in drug development and therefore not refl...
PMC10197635
core_pubmed_pmc
Time-resolved network control analysis links reduced control energy under DMT with the serotonin 2a receptor, signal diversity, and subjective experience
Time-resolved network control analysis links reduced control energy under DMT with the serotonin 2a receptor, signal diversity, and subjective experience Abstract Psychedelics offer a profound window into the functioning of the human brain and mind through their robust acute effects on perception, subjective experience...
PMC5760982
core_pubmed_pmc
LC–MS/MS determination and pharmacokinetic study of bergenin, the main bioactive component of Bergenia purpurascens after oral administration in rats
LC–MS/MS determination and pharmacokinetic study of bergenin, the main bioactive component of Bergenia purpurascens after oral administration in rats Abstract Abstract Bergenin, a C -glucoside of 4-O-methyl gallic acid from Bergenia purpurascens , is a naturally antitussive and expectorant agent. A rapid and sensitive ...
PMC10460734
core_pubmed_pmc
A two-stages global sensitivity analysis by using the δ sensitivity index in presence of correlated inputs: application on a tumor growth inhibition model based on the dynamic energy budget theory
A two-stages global sensitivity analysis by using the δ sensitivity index in presence of correlated inputs: application on a tumor growth inhibition model based on the dynamic energy budget theory Abstract Abstract Global sensitivity analysis (GSA) evaluates the impact of variability and/or uncertainty of the model par...
PMC8309067
core_pubmed_pmc
Pharmacokinetic Comparison between Methotrexate-Loaded Nanoparticles and Nanoemulsions as Hard- and Soft-Type Nanoformulations: A Population Pharmacokinetic Modeling Approach
Pharmacokinetic Comparison between Methotrexate-Loaded Nanoparticles and Nanoemulsions as Hard- and Soft-Type Nanoformulations: A Population Pharmacokinetic Modeling Approach Abstract The purpose of this study was to identify and explore the differences in pharmacokinetics between different nanoformulations. This was d...
PMC7378791
core_pubmed_pmc
The Role of Serotonin in Singultus: A Review
The Role of Serotonin in Singultus: A Review Abstract The use of dopamine receptor blockers for chronic singultus treatment is based—at least partially—on circular thinking: chlorpromazine is FDA-approved for hiccups, chlorpromazine is a neuroleptic, neuroleptics are dopamine receptor blockers, and therefore hiccup is ...
PMC12128970
core_pubmed_pmc
Introducing New Inhibitors of PAICS, a De Novo Purine Biosynthesis Enzyme, through Structure-Based Virtual Screening
Introducing New Inhibitors of PAICS, a De Novo Purine Biosynthesis Enzyme, through Structure-Based Virtual Screening Abstract Abstract Background: Cancer cells need many purine nucleotides during their uncontrolled proliferation. phosphoribosyl-aminoimidazole carboxylase and phosphoribosylaminoimidazole-succinocarboxam...
PMC4575301
core_pubmed_pmc
Towards a Physiological Prandial Insulin Profile: Enhancement of Subcutaneously Injected Prandial Insulin Using Local Warming Devices
Towards a Physiological Prandial Insulin Profile: Enhancement of Subcutaneously Injected Prandial Insulin Using Local Warming Devices Abstract The need to develop an insulin delivery system that can closely mimic physiologically induced changes in prandial insulin release has been a major research target since the disc...
PMC9671933
core_pubmed_pmc
Safety, tolerability and pharmacokinetics of WXFL10203614 in healthy Chinese subjects: A randomized, double-blind, placebo-controlled phase Ⅰ study
Safety, tolerability and pharmacokinetics of WXFL10203614 in healthy Chinese subjects: A randomized, double-blind, placebo-controlled phase Ⅰ study Abstract Objective: This study was conducted to investigate the safety, tolerability and pharmacokinetics (PK) of WXFL10203614 after single and multiple oral doses in healt...