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PMC9807514 | core_pubmed_pmc | First‐in‐human study of ONO‐4578, an antagonist of prostaglandin E 2 receptor 4, alone and with nivolumab in solid tumors | First‐in‐human study of ONO‐4578, an antagonist of prostaglandin E 2 receptor 4, alone and with nivolumab in solid tumors Abstract Abstract EP4, a prostaglandin E 2 receptor, has shown an immunosuppressive activity on cancer cells. This first‐in‐human study evaluated ONO‐4578, a highly selective EP4 antagonist, as mono... |
PMC12035199 | core_pubmed_pmc | Phytochemical Isolation and Antimicrobial, Thrombolytic, Anti-inflammatory, Analgesic, and Antidiarrheal Activities from the Shell of Commonly Available Citrus reticulata Blanco: Multifaceted Role of Polymethoxyflavones | Phytochemical Isolation and Antimicrobial, Thrombolytic, Anti-inflammatory, Analgesic, and Antidiarrheal Activities from the Shell of Commonly Available Citrus reticulata Blanco: Multifaceted Role of Polymethoxyflavones Abstract Fruit wastes are becoming popular as treasures for drug discovery in different classes of t... |
PMC11062534 | core_pubmed_pmc | Leishmania blood parasite dynamics during and after treatment of visceral leishmaniasis in Eastern Africa: A pharmacokinetic-pharmacodynamic model | Leishmania blood parasite dynamics during and after treatment of visceral leishmaniasis in Eastern Africa: A pharmacokinetic-pharmacodynamic model Abstract Abstract Background With the current treatment options for visceral leishmaniasis (VL), recrudescence of the parasite is seen in a proportion of patients. Understan... |
PMC12473923 | core_pubmed_pmc | Population PK Modeling of Denosumab Biosimilar MB09 and Reference Denosumab to Establish PK Similarity | Population PK Modeling of Denosumab Biosimilar MB09 and Reference Denosumab to Establish PK Similarity Abstract Background/Objectives : MB09 is a denosumab biosimilar to the reference products (RPs) Xgeva and Prolia. A population pharmacokinetic (popPK) meta-analysis was conducted to characterize the denosumab PK profi... |
PMC10725600 | core_pubmed_pmc | Induction of double-strand breaks with the non-steroidal androgen receptor ligand flutamide in patients on androgen suppression: a study protocol for a randomized, double-blind prospective trial | Induction of double-strand breaks with the non-steroidal androgen receptor ligand flutamide in patients on androgen suppression: a study protocol for a randomized, double-blind prospective trial Abstract Abstract Background Prostate cancer remains the most prevalent malignancy and the second-leading cause of cancer-rel... |
PMC9864198 | core_pubmed_pmc | Evaluation of Free Online ADMET Tools for Academic or Small Biotech Environments | Evaluation of Free Online ADMET Tools for Academic or Small Biotech Environments Abstract Abstract For a new molecular entity (NME) to become a drug, it is not only essential to have the right biological activity also be safe and efficient, but it is also required to have a favorable pharmacokinetic profile including t... |
PMC12783419 | core_pubmed_pmc | High-Dose Minocycline Improves Outcomes in Acinetobacter baumannii Group Pneumonia: A Propensity-Weighted Cohort Study with MIC-Based Insights for Breakpoint Revision | High-Dose Minocycline Improves Outcomes in Acinetobacter baumannii Group Pneumonia: A Propensity-Weighted Cohort Study with MIC-Based Insights for Breakpoint Revision Abstract Introduction Optimal minocycline dosing for Acinetobacter baumannii group pneumonia remains unclear. We assessed the clinical impact of high-dos... |
PMC10787209 | core_pubmed_pmc | A convolution‐based in vitro‐in vivo correlation model for methylphenidate hydrochloride delayed‐release and extended‐release capsule | A convolution‐based in vitro‐in vivo correlation model for methylphenidate hydrochloride delayed‐release and extended‐release capsule Abstract Abstract Delayed‐release and extended‐release methylphenidate hydrochloride (JORNAY PM®) is a novel capsule formulation of methylphenidate hydrochloride, used to treat attention... |
PMC8492394 | core_pubmed_pmc | Comparison of the pharmacokinetics and pharmacodynamics of YH4808 in healthy subjects for defining an appropriate dosing regimen | Comparison of the pharmacokinetics and pharmacodynamics of YH4808 in healthy subjects for defining an appropriate dosing regimen Abstract Abstract YH4808 is a novel potassium-competitive acid blocker developed for gastric acid-related disorders. Previous studies indicate its potential to improve symptoms of gastric aci... |
PMC9331386 | core_pubmed_pmc | Pharmacokinetics of Bupivacaine Following Administration by an Ultrasound-Guided Transversus Abdominis Plane Block in Cats Undergoing Ovariohysterectomy | Pharmacokinetics of Bupivacaine Following Administration by an Ultrasound-Guided Transversus Abdominis Plane Block in Cats Undergoing Ovariohysterectomy Abstract Abstract Bupivacaine is commonly used for peripheral nerve block in veterinary medicine. This study described the pharmacokinetics of two doses of bupivacaine... |
PMC5519669 | core_pubmed_pmc | In vitro and in vivo pharmacokinetics and metabolism of synthetic cannabinoids CUMYL-PICA and 5F-CUMYL-PICA | In vitro and in vivo pharmacokinetics and metabolism of synthetic cannabinoids CUMYL-PICA and 5F-CUMYL-PICA Abstract Abstract CUMYL-PICA [1-pentyl- N -(2-phenylpropan-2-yl)-1 H -indole-3-carboxamide] and 5F-CUMYL-PICA [1-(5-fluoropentyl)- N -(2-phenylpropan-2-yl)-1 H -indole-3-carboxamide] are recently identified recre... |
PMC6587435 | core_pubmed_pmc | Application of Physiologically Based Pharmacokinetic Modeling to Predict Pharmacokinetics in Healthy Japanese Subjects | Application of Physiologically Based Pharmacokinetic Modeling to Predict Pharmacokinetics in Healthy Japanese Subjects Abstract Abstract Pharmacokinetics (PKs) in Japanese healthy subjects were simulated for nine compounds using physiologically based PK (PBPK) models parameterized with physicochemical properties, precl... |
PMC10594547 | core_pubmed_pmc | The MILK study: Investigating intergenerational transmission of low-calorie sweeteners in breast milk | The MILK study: Investigating intergenerational transmission of low-calorie sweeteners in breast milk Abstract Abstract Introduction Forty-four percent of lactating women in the United States consume beverages containing low calorie sweeteners (LCS), and the presence of LCS in the food supply has continued to increase ... |
PMC6829936 | core_pubmed_pmc | The fallacy of enzymatic hydrolysis for the determination of bioactive curcumin in plasma samples as an indication of bioavailability: a comparative study | The fallacy of enzymatic hydrolysis for the determination of bioactive curcumin in plasma samples as an indication of bioavailability: a comparative study Abstract Abstract Background Numerous health benefits have been demonstrated for curcumin which is extracted from turmeric ( Curcuma longa L). However, due to its po... |
PMC8085921 | core_pubmed_pmc | The 5‐HT 2C receptor as a therapeutic target for alcohol and methamphetamine use disorders: A pilot study in treatment‐seeking individuals | The 5‐HT 2C receptor as a therapeutic target for alcohol and methamphetamine use disorders: A pilot study in treatment‐seeking individuals Abstract Abstract Alcohol use disorder (AUD) and methamphetamine use disorder (MUD) are prevalent and have high adverse impacts on both the individual and society. Current treatment... |
PMC11890735 | core_pubmed_pmc | Shikimic acid protects against doxorubicin-induced cardiotoxicity in rats | Shikimic acid protects against doxorubicin-induced cardiotoxicity in rats Abstract Abstract Doxorubicin (DOX) is used to treat a variety of malignancies; however, its cardiotoxicity limits its effectiveness. Shikimic acid (SA) showed several promising biomedical applications. This study investigated the protective effe... |
PMC11249166 | core_pubmed_pmc | Appropriateness of gentamicin therapeutic drug monitoring at a Middle Eastern tertiary hospital setting: a retrospective evaluation and quality audit | Appropriateness of gentamicin therapeutic drug monitoring at a Middle Eastern tertiary hospital setting: a retrospective evaluation and quality audit Abstract ABSTRACT Introduction The use of gentamicin in the treatment of infectious diseases requires frequent monitoring to attain the best treatment outcomes. Objective... |
PMC12013845 | core_pubmed_pmc | Metabolic and Pharmacokinetic Profiling of a Ketone Ester by Background SGLT2 Inhibitor Therapy in HFrEF | Metabolic and Pharmacokinetic Profiling of a Ketone Ester by Background SGLT2 Inhibitor Therapy in HFrEF Abstract Highlights • Acute KE ingestion induces rapid changes in key metabolic pathways, differentially affected by SGLT2is (fatty acid metabolism) and KE dose (ketone metabolism). • Hemodynamic effects were transi... |
PMC8346189 | core_pubmed_pmc | How glucagon-like peptide 1 receptor agonists work | How glucagon-like peptide 1 receptor agonists work Abstract In recent years, glucagon-like peptide 1 receptor agonists (GLP-1RAs) have become central in the treatment of type 2 diabetes (T2D). In addition to their glucose-lowering properties with low risk of hypoglycaemia, GLP-1RAs reduce body weight and show promising... |
PMC7417172 | core_pubmed_pmc | Concentration-dependent mortality of chloroquine in overdose | Concentration-dependent mortality of chloroquine in overdose Abstract Hydroxychloroquine and chloroquine are used extensively in malaria and rheumatological conditions, and now in COVID-19 prevention and treatment. Although generally safe they are potentially lethal in overdose. In-vitro data suggest that high concentr... |
PMC12229112 | core_pubmed_pmc | Association of Genetic Variants With Rivaroxaban Pharmacokinetics and Pharmacodynamics and Hemorrhage Risk Factors in Patients With Venous Thromboembolism | Association of Genetic Variants With Rivaroxaban Pharmacokinetics and Pharmacodynamics and Hemorrhage Risk Factors in Patients With Venous Thromboembolism Abstract Abstract Background Rivaroxaban is a first‐line agent for venous thromboembolism prophylaxis and treatment. However, its pharmacokinetics, pharmacodynamics,... |
PMC11918482 | core_pubmed_pmc | Theoretical evaluation of the biological activity of hydrogen | Theoretical evaluation of the biological activity of hydrogen Abstract Abstract Hydrogen (H 2 ), the simplest and most ubiquitous molecule in the universe, has garnered significant scientific interest over the past two decades because of its potential as an effective antioxidant and anti-inflammatory agent. Traditional... |
PMC11693974 | core_pubmed_pmc | Apigenin as an emerging hepatoprotective agent: current status and future perspectives | Apigenin as an emerging hepatoprotective agent: current status and future perspectives Abstract Abstract Apigenin (C 15 H 10 O 5 , API) is a natural flavonoid widely found in vegetables, fruits, and plants such as celery, oranges, and chamomile. In recent years, API has attracted considerable attention as a dietary sup... |
PMC11523998 | core_pubmed_pmc | High-dose short-term osimertinib treatment is effective in patient-derived metastatic colorectal cancer organoids | High-dose short-term osimertinib treatment is effective in patient-derived metastatic colorectal cancer organoids Abstract Abstract Background Most tyrosine kinase inhibitors (TKIs) have failed in clinical trials for metastatic colorectal cancer (mCRC). To leverage the additional lower-affinity targets that most TKIs h... |
PMC6155437 | core_pubmed_pmc | AM-2201 Inhibits Multiple Cytochrome P450 and Uridine 5′-Diphospho-Glucuronosyltransferase Enzyme Activities in Human Liver Microsomes | AM-2201 Inhibits Multiple Cytochrome P450 and Uridine 5′-Diphospho-Glucuronosyltransferase Enzyme Activities in Human Liver Microsomes Abstract Abstract AM-2201 is a synthetic cannabinoid that acts as a potent agonist at cannabinoid receptors and its abuse has increased. However, there are no reports of the inhibitory ... |
PMC7801352 | core_pubmed_pmc | Dose exploration results from Phase 1 study of cemiplimab, a human monoclonal programmed death (PD)-1 antibody, in Japanese patients with advanced malignancies | Dose exploration results from Phase 1 study of cemiplimab, a human monoclonal programmed death (PD)-1 antibody, in Japanese patients with advanced malignancies Abstract Abstract Purpose Part 1 of this two-part, open-label, Phase 1 study ( NCT03233139 ) assessed the safety, tolerability, pharmacokinetics, immunogenicity... |
PMC4744681 | core_pubmed_pmc | Pharmacokinetic and Pharmacodynamic Comparison of Once‐Daily Efavirenz (400 mg vs. 600 mg) in Treatment‐Naïve HIV‐Infected Patients: Results of the ENCORE1 Study | Pharmacokinetic and Pharmacodynamic Comparison of Once‐Daily Efavirenz (400 mg vs. 600 mg) in Treatment‐Naïve HIV‐Infected Patients: Results of the ENCORE1 Study Abstract Daily efavirenz 400 mg (EFV400) was virologically noninferior to 600 mg (EFV600) at 48 weeks in treatment‐naïve patients. We evaluated EFV400 and EFV... |
PMC12156476 | core_pubmed_pmc | Evaluation of Potential Drug–Drug Interactions with Antimicrobials among Critically Ill Patients in Intensive Care Units of a Tertiary Care Hospital: A Cross-Sectional Study | Evaluation of Potential Drug–Drug Interactions with Antimicrobials among Critically Ill Patients in Intensive Care Units of a Tertiary Care Hospital: A Cross-Sectional Study Abstract A BSTRACT Background: Critically ill patients in intensive care units (ICUs) are often prescribed multiple drugs, including antimicrobial... |
PMC8452298 | core_pubmed_pmc | Cytochrome P450 2D6 genotype–phenotype characterization through population pharmacokinetic modeling of tedatioxetine | Cytochrome P450 2D6 genotype–phenotype characterization through population pharmacokinetic modeling of tedatioxetine Abstract Abstract The cytochrome P450 (CYP) 2D6 enzyme exhibits large interindividual differences in metabolic activity. Patients are commonly assigned a CYP2D6 phenotype based on their CYP2D6 genotype, ... |
PMC9830922 | core_pubmed_pmc | Population pharmacokinetics and limited sampling strategy for therapeutic drug monitoring of mycophenolate mofetil in Japanese patients with lupus nephritis | Population pharmacokinetics and limited sampling strategy for therapeutic drug monitoring of mycophenolate mofetil in Japanese patients with lupus nephritis Abstract Background Mycophenolate mofetil (MMF), a prodrug of the immunosuppressive agent mycophenolic acid (MPA), is difficult to administer because of the pharma... |
PMC12888870 | core_pubmed_pmc | Critical threshold target attainment rates for tazobactam combined with piperacillin among patients admitted to the ICU with hospital-acquired pneumonia | Critical threshold target attainment rates for tazobactam combined with piperacillin among patients admitted to the ICU with hospital-acquired pneumonia Abstract ABSTRACT Optimizing antibiotic exposures in hospital-acquired pneumonia (HAP) is crucial; however, dosing decisions often overlook target levels for the beta-... |
PMC10919555 | core_pubmed_pmc | Cangrelor — Expanding therapeutic options in patients with acute coronary syndrome | Cangrelor — Expanding therapeutic options in patients with acute coronary syndrome Abstract Abstract Cangrelor is the only intravenous P2Y12 receptor antagonist. It is an adenosine triphosphate analog that selectively, directly, and reversibly binds to the platelet P2Y12 receptors exerting its antiaggregatory effect. C... |
PMC6572600 | core_pubmed_pmc | Pharmacokinetic Studies of Three Alkaloids in Rats After Intragastrical Administration of Lycopodii Herba Extract by LC-MS/MS | Pharmacokinetic Studies of Three Alkaloids in Rats After Intragastrical Administration of Lycopodii Herba Extract by LC-MS/MS Abstract Lycopodii Herba is a widely used traditional medicinal herb, and contains diverse fascinating alkaloids. In this study, a fast and sensitive LC-MS/MS method for the simultaneous determi... |
PMC6440450 | core_pubmed_pmc | Di- O -lauroyl-decitabine-lipid nanocapsules: toward extending decitabine activity | Di- O -lauroyl-decitabine-lipid nanocapsules: toward extending decitabine activity Abstract Background Acute myeloid leukemia mainly affects adult patients. Complete remission for patients younger than 60 years, who are candidates for standard induction therapy, is achieved in 60%–80% of cases. However, the prognosis i... |
PMC4448313 | core_pubmed_pmc | Gastrointestinal delivery of propofol from fospropofol: its bioavailability and activity in rodents and human volunteers | Gastrointestinal delivery of propofol from fospropofol: its bioavailability and activity in rodents and human volunteers Abstract Background Propofol is a safe and widely used intravenous anesthetic agent, for which additional clinical uses including treatment of migraine, nausea, pain and anxiety have been proposed (V... |
PMC7179144 | core_pubmed_pmc | In Vitro, In Silico, and In Vivo Assessments of Pharmacokinetic Properties of ZM241385 | In Vitro, In Silico, and In Vivo Assessments of Pharmacokinetic Properties of ZM241385 Abstract Parkinson’s disease is one of the most common neurodegenerative diseases. Adenosine regulates the response to other neurotransmitters in the brain regions related to motor function. In the several subtypes of adenosine recep... |
PMC8468301 | core_pubmed_pmc | External Model Performance Evaluation of Twelve Infliximab Population Pharmacokinetic Models in Patients with Inflammatory Bowel Disease | External Model Performance Evaluation of Twelve Infliximab Population Pharmacokinetic Models in Patients with Inflammatory Bowel Disease Abstract Infliximab is approved for treatment of various chronic inflammatory diseases including inflammatory bowel disease (IBD). However, high variability in infliximab trough level... |
PMC10047454 | core_pubmed_pmc | Leveraging Prior Healthy Participant Pharmacokinetic Data to Evaluate the Impact of Renal and Hepatic Impairment on Ritlecitinib Pharmacokinetics | Leveraging Prior Healthy Participant Pharmacokinetic Data to Evaluate the Impact of Renal and Hepatic Impairment on Ritlecitinib Pharmacokinetics Abstract Abstract Abstract Ritlecitinib is a selective, covalent, irreversible inhibitor of Janus kinase 3 (JAK3) and the tyrosine kinase expressed in hepatocellular carcinom... |
PMC10458015 | core_pubmed_pmc | Development of Liposome Systems for Enhancing the PK Properties of Bivalent PROTACs | Development of Liposome Systems for Enhancing the PK Properties of Bivalent PROTACs Abstract Abstract Proteolysis-Targeting Chimeras (PROTACs) are a promising new technology in drug development. They have rapidly evolved in recent years, with several of them in clinical trials. While most of these advances have been as... |
PMC11326821 | core_pubmed_pmc | Ceftriaxone Efficacy for Mycobacterium avium Complex Lung Disease in the Hollow Fiber and Translation to Sustained Sputum Culture Conversion in Patients | Ceftriaxone Efficacy for Mycobacterium avium Complex Lung Disease in the Hollow Fiber and Translation to Sustained Sputum Culture Conversion in Patients Abstract Abstract Background Only 35.6%–50.8% of patients with Mycobacterium avium complex (MAC) pulmonary disease achieve sustained sputum culture conversion (SSCC) o... |
PMC8802503 | core_pubmed_pmc | Ceftazidime and cefepime antagonize 5-fluorouracil’s effect in colon cancer cells | Ceftazidime and cefepime antagonize 5-fluorouracil’s effect in colon cancer cells Abstract Abstract Background Drug-drug interaction (DDI), which can occur at the pharmacokinetics and/or the pharmacodynamics (PD) levels, can increase or decrease the therapeutic or adverse response of a drug itself or a combination of d... |
PMC6662550 | core_pubmed_pmc | Interaction Between Sex and Organic Anion‐Transporting Polypeptide 1b2 on the Pharmacokinetics of Regorafenib and Its Metabolites Regorafenib‐N‐Oxide and Regorafenib‐Glucuronide in Mice | Interaction Between Sex and Organic Anion‐Transporting Polypeptide 1b2 on the Pharmacokinetics of Regorafenib and Its Metabolites Regorafenib‐N‐Oxide and Regorafenib‐Glucuronide in Mice Abstract Regorafenib, a multikinase inhibitor used in the treatment of various solid tumors, undergoes extensive uridine 5′‐diphosphat... |
PMC6634858 | core_pubmed_pmc | D-dimer levels during and after anticoagulation withdrawal in patients with venous thromboembolism treated with non-vitamin K anticoagulants | D-dimer levels during and after anticoagulation withdrawal in patients with venous thromboembolism treated with non-vitamin K anticoagulants Abstract Background D-dimer levels measured during and after vitamin K antagonist withdrawal may be used in clinical practice to assess the individual risk of recurrent venous thr... |
PMC10101232 | core_pubmed_pmc | Population pharmacokinetics of vancomycin in very low birth weight neonates | Population pharmacokinetics of vancomycin in very low birth weight neonates Abstract Introduction Vancomycin dosing in very low birth weight (VLBW) neonates is challenging. Compared with the general neonatal population, VLBW neonates are less likely to achieve the vancomycin therapeutic targets. Current dosing recommen... |
PMC4098901 | core_pubmed_pmc | Chronopharmacodynamics and Chronopharmacokinetics of Pethidine in Mice | Chronopharmacodynamics and Chronopharmacokinetics of Pethidine in Mice Abstract Background Many studies have demonstrated that the pharmacokinetics and pharmacodynamics of analgesic drugs vary according to the circadian time of drug administration. This study aims at determining whether the analgesic effect and pharmac... |
PMC7823297 | core_pubmed_pmc | Exogenous Fungal Endophthalmitis: Clues to Aspergillus Aetiology with a Pharmacological Perspective | Exogenous Fungal Endophthalmitis: Clues to Aspergillus Aetiology with a Pharmacological Perspective Abstract Exogenous fungal endophthalmitis (EXFE) represents a rare complication after penetrating ocular trauma of previously unresolved keratitis or iatrogenic infections, following intraocular surgery such as cataract ... |
PMC8156419 | core_pubmed_pmc | Informing Pharmacokinetic Models With Physiological Data: Oral Population Modeling of L-Serine in Humans | Informing Pharmacokinetic Models With Physiological Data: Oral Population Modeling of L-Serine in Humans Abstract To determine how to set optimal oral L-serine (serine) dose levels for a clinical trial, existing literature was surveyed. Data sufficient to set the dose was inadequate, and so an ( n = 10) phase I-A calib... |
PMC12839768 | core_pubmed_pmc | Risk Assessment of Chemical Mixtures in Foods: A Comprehensive Methodological and Regulatory Review | Risk Assessment of Chemical Mixtures in Foods: A Comprehensive Methodological and Regulatory Review Abstract Over the last 15 years, mixture risk assessment for food xenobiotics has evolved from conceptual discussions and simple screening tools, such as the Hazard Index (HI), towards operational, component-based and pr... |
PMC11535963 | core_pubmed_pmc | Development, validation and application of a high-performance liquid chromatography method for the detection of ibuprofen in elephant plasma | Development, validation and application of a high-performance liquid chromatography method for the detection of ibuprofen in elephant plasma Abstract Abstract A simple and accurate method for the determination of ibuprofen concentrations in elephant plasma was developed and validated using reverse phase high-performanc... |
PMC7640590 | core_pubmed_pmc | Dexmedetomidine and ketamine simultaneous administration in tigers ( Panthera tigris ): pharmacokinetics and clinical effects | Dexmedetomidine and ketamine simultaneous administration in tigers ( Panthera tigris ): pharmacokinetics and clinical effects Abstract Abstract Background The study determines the pharmacokinetic profiles of dexmedetomidine (DEX), ketamine (KET) and its active metabolite, norketamine (NORKET), after simultaneous admini... |
PMC12819047 | core_pubmed_pmc | Clinical Course and Risk Factors of Lenvatinib‐Related Hypothyroidism in Hepatocellular Carcinoma: A Retrospective Cohort Study | Clinical Course and Risk Factors of Lenvatinib‐Related Hypothyroidism in Hepatocellular Carcinoma: A Retrospective Cohort Study Abstract ABSTRACT Background Lenvatinib‐related hypothyroidism occurs in 16%–22% of patients with hepatocellular carcinoma and may affect treatment management. Previous studies have reported e... |
PMC6549487 | core_pubmed_pmc | Cholate-modified polymer-lipid hybrid nanoparticles for oral delivery of quercetin to potentiate the antileukemic effect | Cholate-modified polymer-lipid hybrid nanoparticles for oral delivery of quercetin to potentiate the antileukemic effect Abstract Background: Quercetin (QUE) shows a potential antileukemic activity, but possesses poor solubility and low bioavailability. Purpose: This article explored the bile salt transport pathway for... |
PMC4396406 | core_pubmed_pmc | The pharmacokinetic profile, tolerability and safety of the iodinated, non-ionic, dimeric contrast medium Iosimenol 340 injection in healthy human subjects | The pharmacokinetic profile, tolerability and safety of the iodinated, non-ionic, dimeric contrast medium Iosimenol 340 injection in healthy human subjects Abstract Background Iosimenol 340 injection is a new isotonic iodinated contrast medium for X-ray angiography. Purpose To investigate the pharmacokinetics and biotr... |
PMC11460901 | core_pubmed_pmc | Exploring medication rules and mechanism of Chinese medicine for children with cough variant asthma based on data mining, network pharmacology, and molecular docking | Exploring medication rules and mechanism of Chinese medicine for children with cough variant asthma based on data mining, network pharmacology, and molecular docking Abstract Cough variant asthma (CVA) is a common disease with high incidence among children. Cough is the main clinical symptom and Chinese medicine (CM) h... |
PMC12219017 | core_pubmed_pmc | Pharmacokinetics, Pharmacodynamics, Safety, and Tolerability of HSK39297 in Chinese Healthy Subjects: A Phase 1 Clinical Trial | Pharmacokinetics, Pharmacodynamics, Safety, and Tolerability of HSK39297 in Chinese Healthy Subjects: A Phase 1 Clinical Trial Abstract ABSTRACT HSK39297 is a novel complement factor B inhibitor, and this phase 1 trial was designed to assess its pharmacokinetics (PK), pharmacodynamics (PD), safety, and tolerability in ... |
PMC6394489 | core_pubmed_pmc | Population pharmacokinetic and covariate analyses of intravenous trastuzumab (Herceptin ® ), a HER2-targeted monoclonal antibody, in patients with a variety of solid tumors | Population pharmacokinetic and covariate analyses of intravenous trastuzumab (Herceptin ® ), a HER2-targeted monoclonal antibody, in patients with a variety of solid tumors Abstract Abstract Purpose The aim of the study was to characterize the population pharmacokinetics (PK) of the intravenous formulation of trastuzum... |
PMC11652588 | core_pubmed_pmc | QSP modeling of a transiently inactivating antibody-drug conjugate highlights benefit of short antibody half life | QSP modeling of a transiently inactivating antibody-drug conjugate highlights benefit of short antibody half life Abstract Abstract Antibody drug conjugates (ADC) are a promising class of oncology therapeutics consisting of an antibody conjugated to a payload via a linker. DYP688 is a novel ADC comprising of a signalin... |
PMC5698590 | core_pubmed_pmc | Population pharmacokinetics and electrocardiographic effects of dihydroartemisinin–piperaquine in healthy volunteers | Population pharmacokinetics and electrocardiographic effects of dihydroartemisinin–piperaquine in healthy volunteers Abstract Abstract Aims The aims of the present study were to evaluate the pharmacokinetic properties of dihydroartemisinin (DHA) and piperaquine, potential drug–drug interactions with concomitant primaqu... |
PMC10324113 | core_pubmed_pmc | Gut microbiome modulates tacrolimus pharmacokinetics through the transcriptional regulation of ABCB1 | Gut microbiome modulates tacrolimus pharmacokinetics through the transcriptional regulation of ABCB1 Abstract Background Following solid organ transplantation, tacrolimus (TAC) is an essential drug in the immunosuppressive strategy. Its use constitutes a challenge due to its narrow therapeutic index and its high inter-... |
PMC7973782 | core_pubmed_pmc | Molecular docking, pharmacokinetic studies, and in vivo pharmacological study of indole derivative 2-(5-methoxy-2-methyl-1H-indole-3-yl)-N′-[(E)-(3-nitrophenyl) methylidene] acetohydrazide as a promising chemoprotective agent against cisplatin induced organ damage | Molecular docking, pharmacokinetic studies, and in vivo pharmacological study of indole derivative 2-(5-methoxy-2-methyl-1H-indole-3-yl)-N′-[(E)-(3-nitrophenyl) methylidene] acetohydrazide as a promising chemoprotective agent against cisplatin induced organ damage Abstract Cisplatin is an efficient anticancer drug agai... |
PMC4459956 | core_pubmed_pmc | Pharmacokinetics of Novel Plant Cell-Expressed Taliglucerase Alfa in Adult and Pediatric Patients with Gaucher Disease | Pharmacokinetics of Novel Plant Cell-Expressed Taliglucerase Alfa in Adult and Pediatric Patients with Gaucher Disease Abstract Abstract Taliglucerase alfa is a beta-glucocerebrosidase enzyme replacement therapy approved in the United States, Israel, and other countries for treatment of Type 1 Gaucher disease in adults... |
PMC4241252 | core_pubmed_pmc | A Population Pharmacokinetic Approach to Describe Cephalexin Disposition in Adult and Aged Dogs | A Population Pharmacokinetic Approach to Describe Cephalexin Disposition in Adult and Aged Dogs Abstract This study was conducted in order to characterize the pharmacokinetics of orally administered cephalexin to healthy adult and aged dogs, using a population pharmacokinetic approach. Two hundred and eighty-six cephal... |
PMC9819135 | core_pubmed_pmc | Comparison of clozapine doses and tolerability in patients with and without concurrent valproic acid | Comparison of clozapine doses and tolerability in patients with and without concurrent valproic acid Abstract Introduction Valproic acid (VPA) and its various formulations can be given in conjunction with clozapine for seizure prophylaxis or for augmentation in schizophrenia. There is conflicting literature on how VPA ... |
PMC8494442 | core_pubmed_pmc | Therapeutic targeting of SLC6A8 creatine transporter suppresses colon cancer progression and modulates human creatine levels | Therapeutic targeting of SLC6A8 creatine transporter suppresses colon cancer progression and modulates human creatine levels Abstract Colorectal cancer (CRC) is a leading cause of cancer mortality. Creatine metabolism was previously shown to critically regulate colon cancer progression. We report that RGX-202, an oral ... |
PMC10941540 | core_pubmed_pmc | Clofazimine pharmacokinetics in HIV‐infected adults with diarrhea: Implications of diarrheal disease on absorption of orally administered therapeutics | Clofazimine pharmacokinetics in HIV‐infected adults with diarrhea: Implications of diarrheal disease on absorption of orally administered therapeutics Abstract Abstract Oral drug absorption kinetics are usually established in populations with a properly functioning gastrointestinal tract. However, many diseases and the... |
PMC7299152 | core_pubmed_pmc | Enhancing Clinical Trials Through Synergistic Gamma Power Analysis | Enhancing Clinical Trials Through Synergistic Gamma Power Analysis Abstract While the etiology of many neuropsychiatric disorders remains unknown, increasing evidence suggests that aberrant sensory processing plays a central role. For this class of disorders, which are characterized by affective, cognitive, and behavio... |
PMC12857423 | core_pubmed_pmc | Higher Vedolizumab Clearance Associates with Poor Therapeutic Outcomes during Intravenous Vedolizumab Maintenance Therapy in Crohn’s Disease | Higher Vedolizumab Clearance Associates with Poor Therapeutic Outcomes during Intravenous Vedolizumab Maintenance Therapy in Crohn’s Disease Methods Methods This was a post hoc analysis of a cohort of patients enrolled in LOVE-CD (Lowlands Vedolizumab in Crohn's disease study), a multinational prospective controlled tr... |
PMC12777566 | core_pubmed_pmc | Whole-body distribution of three Pseudomonas phages characterized by a translational physiologically based pharmacokinetic model | Whole-body distribution of three Pseudomonas phages characterized by a translational physiologically based pharmacokinetic model Abstract ABSTRACT Bacteriophage (phage) therapy holds great promise for treating antimicrobial-resistant infections. However, the pharmacokinetics (PK) of phage have been difficult to charact... |
PMC11156719 | core_pubmed_pmc | Understanding adefovir pharmacokinetics as a component of a transporter phenotyping cocktail | Understanding adefovir pharmacokinetics as a component of a transporter phenotyping cocktail Abstract Abstract Purpose Adefovir (as dipivoxil) was selected as a probe drug in a previous transporter cocktail phenotyping study to assess renal organic anion transporter 1 (OAT1), with renal clearance (CL R ) as the primary... |
PMC6058255 | core_pubmed_pmc | Semi-Mechanism-Based Pharmacodynamic Model for the Anti-Inflammatory Effect of Baicalein in LPS-Stimulated RAW264.7 Macrophages | Semi-Mechanism-Based Pharmacodynamic Model for the Anti-Inflammatory Effect of Baicalein in LPS-Stimulated RAW264.7 Macrophages Abstract Abstract Monitoring of the inhibition of TNF-α, IL-6, iNOS, and NO is used to effectively evaluate anti-inflammatory drugs. Baicalein was found to have good anti-inflammatory activiti... |
PMC3825499 | core_pubmed_pmc | Exposure–response analysis of pertuzumab in HER2-positive metastatic breast cancer: absence of effect on QTc prolongation and other ECG parameters | Exposure–response analysis of pertuzumab in HER2-positive metastatic breast cancer: absence of effect on QTc prolongation and other ECG parameters Abstract Purpose The phase III trial of pertuzumab plus trastuzumab plus docetaxel versus placebo plus trastuzumab plus docetaxel for first-line treatment of HER2-positive m... |
PMC10785304 | core_pubmed_pmc | Population pharmacokinetics and individualized dosing of vancomycin for critically ill patients receiving continuous renal replacement therapy: the role of residual diuresis | Population pharmacokinetics and individualized dosing of vancomycin for critically ill patients receiving continuous renal replacement therapy: the role of residual diuresis Abstract Background: Vancomycin dosing is difficult in critically ill patients receiving continuous renal replacement therapy (CRRT). Previous pop... |
PMC9663925 | core_pubmed_pmc | Phase I pharmacokinetic study of an oral, small-molecule MEK inhibitor tunlametinib in patients with advanced NRAS mutant melanoma | Phase I pharmacokinetic study of an oral, small-molecule MEK inhibitor tunlametinib in patients with advanced NRAS mutant melanoma Abstract Abstract Background: Malignant melanoma is an aggressive disease. Tunlametinib (HL-085) is a potent, selective, and orally bioavailable MEK1/2 inhibitor. The objective of this stud... |
PMC7033533 | core_pubmed_pmc | Decreased potency of fimasartan in liver cirrhosis was quantified using mixed-effects analysis | Decreased potency of fimasartan in liver cirrhosis was quantified using mixed-effects analysis Abstract Abstract Fimasartan is a nonpeptide angiotensin II receptor blocker. In a previous study that compared the pharmacokinetics (PK) of fimasartan between patients with hepatic impairment (cirrhosis) and healthy subjects... |
PMC10681895 | core_pubmed_pmc | Dasatinib anhydrate containing oral formulation improves variability and bioavailability in humans | Dasatinib anhydrate containing oral formulation improves variability and bioavailability in humans Abstract Dasatinib monohydrate indicated for the treatment of chronic myeloid leukemia displays pH-dependent solubility. The aim of reported development program of novel dasatinib anhydrate containing formulation was to d... |
PMC7445515 | core_pubmed_pmc | Efficacy of Sub-Tenon Micro-Perfusion of Cyclophosphamide in Rabbits with Severe Ocular Inflammation | Efficacy of Sub-Tenon Micro-Perfusion of Cyclophosphamide in Rabbits with Severe Ocular Inflammation Abstract Purpose To explore the feasibility of cyclophosphamide (CP) via a sub-Tenon micro-perfusion system (SMS) in rabbits, and assess its therapeutic efficacy in severe ocular inflammation. Materials and Methods Dist... |
PMC7737147 | core_pubmed_pmc | Efficacy of Nilotinib in Patients With Moderately Advanced Parkinson Disease | Efficacy of Nilotinib in Patients With Moderately Advanced Parkinson Disease Abstract Key Points Question Do the safety, tolerability, exploratory clinical outcomes, brain penetration, and biomarker profile of nilotinib in aggregate support its development for treatment of Parkinson disease (PD)? Findings In this 6-mon... |
PMC9755922 | core_pubmed_pmc | Comparing the applications of machine learning, PBPK, and population pharmacokinetic models in pharmacokinetic drug–drug interaction prediction | Comparing the applications of machine learning, PBPK, and population pharmacokinetic models in pharmacokinetic drug–drug interaction prediction Abstract Abstract The gold‐standard approach for modeling pharmacokinetic mediated drug–drug interactions is the use of physiologically‐based pharmacokinetic modeling and popul... |
PMC6408477 | core_pubmed_pmc | Determinants of high platelet reactivity in patients with acute coronary syndromes treated with ticagrelor | Determinants of high platelet reactivity in patients with acute coronary syndromes treated with ticagrelor Abstract High platelet reactivity (HPR) is a risk factor for stent thrombosis, a potentially lethal complication of percutaneous coronary intervention. HPR is also associated with increased risk of myocardial infa... |
PMC11279827 | core_pubmed_pmc | Pharmacogenomics: A Genetic Approach to Drug Development and Therapy | Pharmacogenomics: A Genetic Approach to Drug Development and Therapy Abstract The majority of the well-known pharmacogenomics research used in the medical sciences contributes to our understanding of medication interactions. It has a significant impact on treatment and drug development. The broad use of pharmacogenomic... |
PMC8113183 | core_pubmed_pmc | Application of Physiologically Based Pharmacokinetic Modeling to Predict the Effect of Renal Impairment on the Pharmacokinetics of Olanzapine and Samidorphan Given in Combination | Application of Physiologically Based Pharmacokinetic Modeling to Predict the Effect of Renal Impairment on the Pharmacokinetics of Olanzapine and Samidorphan Given in Combination Abstract Abstract Background A combination of the antipsychotic olanzapine and opioid receptor antagonist samidorphan (OLZ/SAM) is in develop... |
PMC4368888 | core_pubmed_pmc | Preclinical to Clinical Translation of CNS Transporter Occupancy of TD-9855, a Novel Norepinephrine and Serotonin Reuptake Inhibitor | Preclinical to Clinical Translation of CNS Transporter Occupancy of TD-9855, a Novel Norepinephrine and Serotonin Reuptake Inhibitor Abstract Background: Monoamine reuptake inhibitors exhibit unique clinical profiles that reflect distinct engagement of the central nervous system (CNS) transporters. Methods: We used a t... |
PMC10164881 | core_pubmed_pmc | Tirapazamine-loaded CalliSpheres microspheres: Preparation and characterization as a chemoembolization agent for liver cancer | Tirapazamine-loaded CalliSpheres microspheres: Preparation and characterization as a chemoembolization agent for liver cancer Abstract Tirapazamine (TPZ), a hypoxia-selective cytotoxic agent, has proved to exert synergistic tumor-killing activity with transcatheter arterial embolization (TAE) against liver cancer. This... |
PMC8376141 | core_pubmed_pmc | PK/PD modeling analysis for dosing regimen selection of isatuximab as single agent and in combination therapy in patients with multiple myeloma | PK/PD modeling analysis for dosing regimen selection of isatuximab as single agent and in combination therapy in patients with multiple myeloma Abstract Abstract This analysis describes the pharmacokinetic/pharmacodynamic (PK/PD) modeling framework that supported selection of the isatuximab (anti‐CD38 monoclonal antibo... |
PMC5048002 | core_pubmed_pmc | Population Pharmacokinetic Analysis of Piperacillin/Tazobactam in Korean Patients with Acute Infections | Population Pharmacokinetic Analysis of Piperacillin/Tazobactam in Korean Patients with Acute Infections Abstract Abstract Background For more effective and safer usage of antibiotics, the dosing strategy should be individualized based on the patients’ characteristics, including race. The aim of this study was to invest... |
PMC9367300 | core_pubmed_pmc | Oxytetracycline Persistence in Uterine Secretion after Intrauterine Administration in Cows with Metritis | Oxytetracycline Persistence in Uterine Secretion after Intrauterine Administration in Cows with Metritis Abstract Abstract Simple Summary Puerperal metritis in cows involves the acute inflammation of the uterus, which is often treated with antibacterial drugs. Restrictions on the use of antibiotics in veterinary medici... |
PMC7570897 | core_pubmed_pmc | Enhanced Extraction Technique of Omarigliptin from Human Plasma—Applied to Biological Samples from Healthy Human Volunteers | Enhanced Extraction Technique of Omarigliptin from Human Plasma—Applied to Biological Samples from Healthy Human Volunteers Abstract Abstract Enhancing drug extraction from human plasma is a challenging approach that critically affects pharmacokinetic and any further clinical studies based on the drug C min and C max v... |
PMC9303197 | core_pubmed_pmc | Pharmacokinetics, safety, and tolerability of intravenous brivaracetam in pediatric patients with epilepsy: An open‐label trial | Pharmacokinetics, safety, and tolerability of intravenous brivaracetam in pediatric patients with epilepsy: An open‐label trial Abstract Abstract Objective To evaluate the pharmacokinetics, safety, and tolerability of brivaracetam (BRV) as 15‐min intravenous (IV) infusion and bolus (≤2‐min injection). Methods EP0065 (C... |
PMC4349307 | core_pubmed_pmc | A randomised phase 1 study to investigate safety, pharmacokinetics and impact on gut microbiota following single and multiple oral doses in healthy male subjects of SMT19969, a novel agent for Clostridium difficile infections | A randomised phase 1 study to investigate safety, pharmacokinetics and impact on gut microbiota following single and multiple oral doses in healthy male subjects of SMT19969, a novel agent for Clostridium difficile infections Abstract Abstract Background Clostridium difficile infection (CDI) is a leading cause of diarr... |
PMC4669130 | core_pubmed_pmc | Fentanyl Enhances Hepatotoxicity of Paclitaxel via Inhibition of CYP3A4 and ABCB1 Transport Activity in Mice | Fentanyl Enhances Hepatotoxicity of Paclitaxel via Inhibition of CYP3A4 and ABCB1 Transport Activity in Mice Abstract Fentanyl, a potent opioid analgesic that is used to treat cancer pain, is commonly administered with paclitaxel in advanced tumors. However, the effect of fentanyl on the hepatotoxicity of paclitaxel an... |
PMC8395164 | core_pubmed_pmc | The Effect of Chronic Iloperidone Treatment on Cytochrome P450 Expression and Activity in the Rat Liver: Involvement of Neuroendocrine Mechanisms | The Effect of Chronic Iloperidone Treatment on Cytochrome P450 Expression and Activity in the Rat Liver: Involvement of Neuroendocrine Mechanisms Abstract Abstract In order to achieve a desired therapeutic effect in schizophrenia patients and to maintain their mental wellbeing, pharmacological therapy needs to be conti... |
PMC12296474 | core_pubmed_pmc | Nano-Amounts of Glucagon Premixed With Fast-Acting Insulin Lispro: Effect on Insulin Absorption in Pigs | Nano-Amounts of Glucagon Premixed With Fast-Acting Insulin Lispro: Effect on Insulin Absorption in Pigs Abstract Abstract Background Glucagon leads to substantial but short-lived subcutaneous vasodilation. Using micro-amounts of glucagon at the insulin injection site increases insulin absorption. Objective We hypothesi... |
PMC6930860 | core_pubmed_pmc | Population Pharmacokinetic/Pharmacodynamic Modeling of Methylprednisolone in Neonates Undergoing Cardiopulmonary Bypass | Population Pharmacokinetic/Pharmacodynamic Modeling of Methylprednisolone in Neonates Undergoing Cardiopulmonary Bypass Abstract Abstract Methylprednisolone is used in neonates to modulate cardiopulmonary bypass (CPB)–induced inflammation, but optimal dosing and exposure are unknown. We used plasma methylprednisolone a... |
PMC10764263 | core_pubmed_pmc | Pharmacokinetics, dynamics, toxicology and molecular docking of bioactive alkaloid vasicine from Adhatoda vasica : a promising toxin binder against aflatoxin B1 and ochratoxin A | Pharmacokinetics, dynamics, toxicology and molecular docking of bioactive alkaloid vasicine from Adhatoda vasica : a promising toxin binder against aflatoxin B1 and ochratoxin A Abstract Abstract Vasicine from Adhatoda vasica was investigated in the management of aflatoxicosis and ochratoxicosis by in silico molecular ... |
PMC9126255 | core_pubmed_pmc | Population Pharmacokinetics of Mycophenolic Acid in Renal Transplant Patients: A Comparison of the Early and Stable Posttransplant Stages | Population Pharmacokinetics of Mycophenolic Acid in Renal Transplant Patients: A Comparison of the Early and Stable Posttransplant Stages Abstract Abstract Mycophenolic acid (MPA) is an antimetabolic immunosuppressive drug widely used in solid organ transplantation and autoimmune diseases. Pharmacokinetics (PK) of MPA ... |
PMC12482215 | core_pubmed_pmc | Qushi huayu decoction dose-dependent inhibition of caspase-2/SREBP-1 in MASLD mice | Qushi huayu decoction dose-dependent inhibition of caspase-2/SREBP-1 in MASLD mice Abstract Abstract Background Metabolic Dysfunction-Associated Steatotic Liver Disease (MASLD) is characterized by hepatic lipid accumulation and metabolic disturbances. Caspase-2 cleaves site-1 protease (S1P), leading to the persistent a... |
PMC11860138 | core_pubmed_pmc | Immunomodulatory Effects of Atractylodes lancea in Healthy Volunteers with Dosage Prediction for Cholangiocarcinoma Therapy: A Modelling Approach | Immunomodulatory Effects of Atractylodes lancea in Healthy Volunteers with Dosage Prediction for Cholangiocarcinoma Therapy: A Modelling Approach Abstract Abstract Background and Aims : According to a recent study on the immunomodulatory activity of Atractylodes lancea (Thunb.) DC. (AL) in healthy Thai subjects, AL sig... |
PMC8323890 | core_pubmed_pmc | Attenuating nicotine’s effects with high affinity human anti-nicotine monoclonal antibodies | Attenuating nicotine’s effects with high affinity human anti-nicotine monoclonal antibodies Abstract Abstract Use of nicotine-specific monoclonal antibodies (mAbs) to sequester and reduce nicotine distribution to brain has been proposed as a therapeutic approach to treat nicotine addiction (the basis of tobacco use dis... |
PMC9862203 | core_pubmed_pmc | In Vitro Metabolism and CYP-Modulating Activity of Lavender Oil and Its Major Constituents | In Vitro Metabolism and CYP-Modulating Activity of Lavender Oil and Its Major Constituents Abstract The application of essential oils has historically been limited to topical (massage therapy) and inhalational (aromatherapy) routes of administration. More recently, however, evaluation of the therapeutic effects of esse... |
PMC10951451 | core_pubmed_pmc | Effects of Low-Dose Glucagon on Subcutaneous Insulin Absorption in Pigs | Effects of Low-Dose Glucagon on Subcutaneous Insulin Absorption in Pigs Abstract Abstract Background Slow insulin absorption prevents the development of a fully automated artificial pancreas with subcutaneous insulin delivery. Objective We have hypothesized that glucagon could be used as a vasodilator to accelerate ins... |
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