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PMC5756412 | core_pubmed_pmc | A phase 1 evaluation of the pharmacokinetic/pharmacodynamic interaction of the anti-malarial agents KAF156 and piperaquine | A phase 1 evaluation of the pharmacokinetic/pharmacodynamic interaction of the anti-malarial agents KAF156 and piperaquine Abstract Background KAF156 is a novel imidazolopiperazine anti-malarial with activity against pre-erythrocytic liver stages, asexual and sexual blood stages. Based on in vitro data, a two-way pharm... |
PMC3586182 | core_pubmed_pmc | Bioequivalence and Tolerability Assessment of a Novel Intravenous Ciclosporin Lipid Emulsion Compared to Branded Ciclosporin in Cremophor ® EL | Bioequivalence and Tolerability Assessment of a Novel Intravenous Ciclosporin Lipid Emulsion Compared to Branded Ciclosporin in Cremophor ® EL Abstract Abstract Background Ciclosporin is used as an immunosuppressant in current clinical practice but recent research implies novel indications for the drug, such as neuro- ... |
PMC10671020 | core_pubmed_pmc | Pharmacokinetics and Changes in Lipid Mediator Profiling after Consumption of Specialized Pro-Resolving Lipid-Mediator-Enriched Marine Oil in Healthy Subjects | Pharmacokinetics and Changes in Lipid Mediator Profiling after Consumption of Specialized Pro-Resolving Lipid-Mediator-Enriched Marine Oil in Healthy Subjects Abstract Omega-3 polyunsaturated fatty acids (PUFAs) play a vital role in human health, well-being, and the management of inflammatory diseases. Insufficient int... |
PMC3132048 | core_pubmed_pmc | Treatment of experimental adjuvant arthritis with a novel folate receptor-targeted folic acid-aminopterin conjugate | Treatment of experimental adjuvant arthritis with a novel folate receptor-targeted folic acid-aminopterin conjugate Abstract Abstract Introduction Folate receptor (FR)-expressing macrophages have been shown to accumulate at sites of inflammation, where they promote development of inflammatory symptoms. To target such a... |
PMC5248591 | core_pubmed_pmc | PRT062607 Achieves Complete Inhibition of the Spleen Tyrosine Kinase at Tolerated Exposures Following Oral Dosing in Healthy Volunteers | PRT062607 Achieves Complete Inhibition of the Spleen Tyrosine Kinase at Tolerated Exposures Following Oral Dosing in Healthy Volunteers Abstract Abstract The spleen tyrosine kinase (SYK) regulates immune cell activation in response to engagement of a variety of receptors, making it an intriguing target for the treatmen... |
PMC11652397 | core_pubmed_pmc | Trientine Tetrahydrochloride, From Bench to Bedside: A Narrative Review | Trientine Tetrahydrochloride, From Bench to Bedside: A Narrative Review Abstract Trientine tetrahydrochloride (TETA-4HCl, Cuvrior ® ) is a copper chelating agent with the active moiety triethylenetetramine (trientine), developed by Orphalan, Inc. to address the unmet needs in the treatment of Wilson disease. The journe... |
PMC11277036 | core_pubmed_pmc | Aprotinin (I): Understanding the Role of Host Proteases in COVID-19 and the Importance of Pharmacologically Regulating Their Function | Aprotinin (I): Understanding the Role of Host Proteases in COVID-19 and the Importance of Pharmacologically Regulating Their Function Abstract Abstract Proteases are produced and released in the mucosal cells of the respiratory tract and have important physiological functions, for example, maintaining airway humidifica... |
PMC12705655 | core_pubmed_pmc | Organ-specific delivery of an mRNA-encoded bispecific T cell engager targeting glypican-3 in hepatocellular carcinoma | Organ-specific delivery of an mRNA-encoded bispecific T cell engager targeting glypican-3 in hepatocellular carcinoma Abstract T-cell engager (TCE)-based immunotherapy is clinically validated in hematological cancers. However, application in solid tumors faces hurdles including T cell penetration, the immunosuppressive... |
PMC5837758 | core_pubmed_pmc | 5-FU therapeutic drug monitoring as a valuable option to reduce toxicity in patients with gastrointestinal cancer | 5-FU therapeutic drug monitoring as a valuable option to reduce toxicity in patients with gastrointestinal cancer Abstract Abstract Aims 5-FU is used as the main backbone of chemotherapy regimens for patients with colorectal and other gastrointestinal cancers. Despite development of new strategies that allowed enhancin... |
PMC4712979 | core_pubmed_pmc | Integrating Multiscale Modeling with Drug Effects for Cancer Treatment | Integrating Multiscale Modeling with Drug Effects for Cancer Treatment Abstract Abstract In this paper, we review multiscale modeling for cancer treatment with the incorporation of drug effects from an applied system’s pharmacology perspective. Both the classical pharmacology and systems biology are inherently quantita... |
PMC11508966 | core_pubmed_pmc | Therapeutic Drug Monitoring of Elexacaftor, Tezacaftor, and Ivacaftor in Adult People with Cystic Fibrosis | Therapeutic Drug Monitoring of Elexacaftor, Tezacaftor, and Ivacaftor in Adult People with Cystic Fibrosis Abstract Background/Objectives: Elexacaftor, tezacaftor, and ivacaftor (ETI) have significantly improved lung function in people with cystic fibrosis (pwCF). Despite exceptional improvements in most cases, treatme... |
PMC9658560 | core_pubmed_pmc | Weak Noncovalent Interactions in Three Closely Related Adamantane-Linked 1,2,4-Triazole N -Mannich Bases: Insights from Energy Frameworks, Hirshfeld Surface Analysis, In Silico 11β-HSD1 Molecular Docking and ADMET Prediction | Weak Noncovalent Interactions in Three Closely Related Adamantane-Linked 1,2,4-Triazole N -Mannich Bases: Insights from Energy Frameworks, Hirshfeld Surface Analysis, In Silico 11β-HSD1 Molecular Docking and ADMET Prediction Abstract Structural analysis and docking studies of three adamantane-linked 1,2,4-triazole N -M... |
PMC11597386 | core_pubmed_pmc | Pharmacokinetics and Quantitative Structure–Pharmacokinetics Relationship Study of Xanthine Derivatives with Antidepressant, Anti-Inflammatory, and Analgesic Activity in Rats | Pharmacokinetics and Quantitative Structure–Pharmacokinetics Relationship Study of Xanthine Derivatives with Antidepressant, Anti-Inflammatory, and Analgesic Activity in Rats Abstract Objective: The aim of this study was to develop quantitative structure–pharmacokinetics relationship (QSPKR) models for a group of xanth... |
PMC6483270 | core_pubmed_pmc | Establishing Best Practices and Guidance in Population Modeling: An Experience With an Internal Population Pharmacokinetic Analysis Guidance | Establishing Best Practices and Guidance in Population Modeling: An Experience With an Internal Population Pharmacokinetic Analysis Guidance Abstract This tutorial describes the development of a population pharmacokinetic (Pop PK) analysis guidance within Pfizer, which strives for improved consistency and efficiency, a... |
PMC6732628 | core_pubmed_pmc | Pretargeted Nuclear Imaging and Radioimmunotherapy Based on the Inverse Electron-Demand Diels–Alder Reaction and Key Factors in the Pretargeted Synthetic Design | Pretargeted Nuclear Imaging and Radioimmunotherapy Based on the Inverse Electron-Demand Diels–Alder Reaction and Key Factors in the Pretargeted Synthetic Design Abstract The exceptional speed and biorthogonality of the inverse electron-demand Diels–Alder (IEDDA) click chemistry between 1,2,4,5-tetrazines and strained a... |
PMC11758388 | core_pubmed_pmc | Development and preclinical testing of a naloxone prodrug depot for extended protection against opioid overdose | Development and preclinical testing of a naloxone prodrug depot for extended protection against opioid overdose Abstract Abstract The opioid crisis, driven by synthetic opioids like fentanyl, demands innovative solutions. The opioid antidote naloxone has a short action ( ~ 1 hour), requiring repeated doses. To address ... |
PMC3097505 | core_pubmed_pmc | Formulation and Bioequivalence of Two Valsartan Tablets After a Single Oral Administration | Formulation and Bioequivalence of Two Valsartan Tablets After a Single Oral Administration Abstract The aim of this study is to assess the quality of Valzan ® tablet (160 mg, valsartan immediate release test formulation) by comparing its pharmacokinetic parameters with Diovan ® tablet (160 mg, valsartan reference formu... |
PMC6100011 | core_pubmed_pmc | Combining Albumin-Binding Properties and Interaction with Pemetrexed to Improve the Tissue Distribution of Radiofolates | Combining Albumin-Binding Properties and Interaction with Pemetrexed to Improve the Tissue Distribution of Radiofolates Abstract Abstract Folic-acid-based radioconjugates have been developed for nuclear imaging of folate receptor (FR)-positive tumors; however, high renal uptake was unfavorable in view of a therapeutic ... |
PMC10541775 | core_pubmed_pmc | A novel synthesized prodrug of gemcitabine based on oxygen-free radical sensitivity inhibited the growth of lung cancer cells | A novel synthesized prodrug of gemcitabine based on oxygen-free radical sensitivity inhibited the growth of lung cancer cells Abstract Abstract In the present study, we introduced the H 2 O 2 -sensitive thiazolidinone moiety at the 4th amino group of gemcitabine (GEM) to synthesize a new target compound named GEM-ZZQ, ... |
PMC7473010 | core_pubmed_pmc | Development of a Minimal Physiologically-Based Pharmacokinetic Model to Simulate Lung Exposure in Humans Following Oral Administration of Ivermectin for COVID-19 Drug Repurposing | Development of a Minimal Physiologically-Based Pharmacokinetic Model to Simulate Lung Exposure in Humans Following Oral Administration of Ivermectin for COVID-19 Drug Repurposing Abstract Abstract SARS-CoV-2 utilizes the IMPα/β1 heterodimer to enter host cell nuclei after gaining cellular access through the ACE2 recept... |
PMC8954661 | core_pubmed_pmc | The Association between ABCG2 421C>A (rs2231142) Polymorphism and Rosuvastatin Pharmacokinetics: A Systematic Review and Meta-Analysis | The Association between ABCG2 421C>A (rs2231142) Polymorphism and Rosuvastatin Pharmacokinetics: A Systematic Review and Meta-Analysis Abstract Abstract Although several studies have revealed the association between rosuvastatin pharmacokinetics and the ABCG2 421C>A (rs2231142) polymorphism, most studies were conducted... |
PMC4744724 | core_pubmed_pmc | Biosimilar insulins: guidance for data interpretation by clinicians and users | Biosimilar insulins: guidance for data interpretation by clinicians and users Abstract Abstract Biosimilar insulins are approved copies of insulins outside patent protection. Advantages may include greater market competition and potential cost reduction, but clinicians and users lack a clear perspective on ‘biosimilari... |
PMC11821731 | core_pubmed_pmc | The Pharmacokinetic Interaction Between Metformin and the Natural Product Goldenseal Is Metformin Dose‐Dependent: A Three‐Arm Crossover Study in Adults With Type 2 Diabetes | The Pharmacokinetic Interaction Between Metformin and the Natural Product Goldenseal Is Metformin Dose‐Dependent: A Three‐Arm Crossover Study in Adults With Type 2 Diabetes Abstract ABSTRACT Pharmacokinetic drug interactions can lead to unexpected changes in plasma concentrations of the object drug, potentially increas... |
PMC10681405 | core_pubmed_pmc | Copanlisib population pharmacokinetics from phase I–III studies and exposure–response relationships in combination with rituximab | Copanlisib population pharmacokinetics from phase I–III studies and exposure–response relationships in combination with rituximab Abstract Abstract Copanlisib dose selection was established under the maximum tolerated dose paradigm, and no dedicated dose‐finding studies have investigated copanlisib dose selection when ... |
PMC11157020 | core_pubmed_pmc | Progress and application of lung-on-a-chip for lung cancer | Progress and application of lung-on-a-chip for lung cancer Abstract Lung cancer is a malignant tumour with the highest incidence and mortality worldwide. Clinically effective therapy strategies are underutilized owing to the lack of efficient models for evaluating drug response. One of the main reasons for failure of a... |
PMC5825204 | core_pubmed_pmc | Isolation of blood-brain barrier-crossing antibodies from a phage display library by competitive elution and their ability to penetrate the central nervous system | Isolation of blood-brain barrier-crossing antibodies from a phage display library by competitive elution and their ability to penetrate the central nervous system Abstract ABSTRACT The blood-brain barrier (BBB) is a formidable obstacle for delivery of biologic therapeutics to central nervous system (CNS) targets. Whils... |
PMC11880088 | core_pubmed_pmc | Basic Considerations for the Consistency Evaluation Based on ICH E17 Guideline | Basic Considerations for the Consistency Evaluation Based on ICH E17 Guideline Abstract Abstract In the International Council for Harmonisation (ICH) guidance on General Principles for Planning and Design of Multi-Regional Clinical Trials (E17), it is important to evaluate the consistency of treatment effect across reg... |
PMC6063220 | core_pubmed_pmc | Pharmacokinetic interaction between fimasartan and atorvastatin in healthy male volunteers | Pharmacokinetic interaction between fimasartan and atorvastatin in healthy male volunteers Abstract Abstract Introduction Major cardiovascular risk factors, including hypertension and dyslipidemia, are often comorbidities, frequently leading to concurrent prescription of angiotensin receptor blockers and 3-hydroxy-3-me... |
PMC6861345 | core_pubmed_pmc | An open-label, phase 1 study of androgen receptor antagonist, apalutamide in Japanese patients with metastatic castration-resistant prostate cancer | An open-label, phase 1 study of androgen receptor antagonist, apalutamide in Japanese patients with metastatic castration-resistant prostate cancer Abstract Background Apalutamide, a nonsteroidal potent androgen receptor antagonist, was safe and effective in patients with non-metastatic castration-resistant prostate ca... |
PMC9742531 | core_pubmed_pmc | Pharmacokinetics of fluorobenzyl polyethylene glycol conjugated tetraiodothyroacetic acid (NP751), a novel anticancer thyrointegrin α v β 3 antagonist | Pharmacokinetics of fluorobenzyl polyethylene glycol conjugated tetraiodothyroacetic acid (NP751), a novel anticancer thyrointegrin α v β 3 antagonist Abstract Abstract We have recently reported on the development of fb-PMT (NP751), a conjugate of the thyroid hormone metabolite tetraiodothyroacetic acid (tetrac) and mo... |
PMC10514544 | core_pubmed_pmc | Optimization of Therapy in Patients with Epilepsy and Psychiatric Comorbidities: Key Points | Optimization of Therapy in Patients with Epilepsy and Psychiatric Comorbidities: Key Points Abstract Abstract Psychiatric disorder comorbidity in patients with epilepsy (PWE) is very frequent with a mean percentage prevalence of up to 50% and even higher. Such a high frequency suggests that epilepsy and psychiatric dis... |
PMC10526314 | core_pubmed_pmc | Pharmacomicrobiomics of Classical Immunosuppressant Drugs: A Systematic Review | Pharmacomicrobiomics of Classical Immunosuppressant Drugs: A Systematic Review Abstract The clinical response to classical immunosuppressant drugs (cIMDs) is highly variable among individuals. We performed a systematic review of published evidence supporting the hypothesis that gut microorganisms may contribute to this... |
PMC7225904 | core_pubmed_pmc | Lung penetration, bronchopulmonary pharmacokinetic/pharmacodynamic profile and safety of 3 g of ceftolozane/tazobactam administered to ventilated, critically ill patients with pneumonia | Lung penetration, bronchopulmonary pharmacokinetic/pharmacodynamic profile and safety of 3 g of ceftolozane/tazobactam administered to ventilated, critically ill patients with pneumonia Abstract Abstract Objectives Ceftolozane/tazobactam is approved for hospital-acquired/ventilator-associated bacterial pneumonia at dou... |
PMC9328939 | core_pubmed_pmc | A Randomized Double‐Blind Placebo‐Controlled First‐In‐Human Phase 1 Trial of TransCon PTH in Healthy Adults | A Randomized Double‐Blind Placebo‐Controlled First‐In‐Human Phase 1 Trial of TransCon PTH in Healthy Adults Abstract ABSTRACT TransCon PTH is a sustained‐release, essentially inactive prodrug transiently bound to an inert carrier, designed to release PTH(1‐34), and in development for hypoparathyroidism (HP). This phase... |
PMC6272306 | core_pubmed_pmc | LC-MS/MS Determination and Pharmacokinetic Study of Pedunculoside in Rat Plasma after Oral Administration of Pedunculoside and Ilex rotunda Extract | LC-MS/MS Determination and Pharmacokinetic Study of Pedunculoside in Rat Plasma after Oral Administration of Pedunculoside and Ilex rotunda Extract Abstract Ilex rotunda is widely used to treat many disorders as a traditional Chinese medicine (TCM) containing 4%–5% pedunculoside (PDC). A rapid, selective, and sensitive... |
PMC5750653 | core_pubmed_pmc | Modeling of Body Weight Metrics for Effective and Cost-Efficient Conventional Factor VIII Dosing in Hemophilia A Prophylaxis | Modeling of Body Weight Metrics for Effective and Cost-Efficient Conventional Factor VIII Dosing in Hemophilia A Prophylaxis Abstract Abstract The total body weight-based dosing strategy currently used in the prophylactic treatment of hemophilia A may not be appropriate for all populations. The assumptions that guide w... |
PMC5423974 | core_pubmed_pmc | Pharmacokinetics and pharmacogenetics of the MEK1/2 inhibitor, selumetinib, in Asian and Western healthy subjects: a pooled analysis | Pharmacokinetics and pharmacogenetics of the MEK1/2 inhibitor, selumetinib, in Asian and Western healthy subjects: a pooled analysis Abstract Abstract Purpose Emerging data on selumetinib, a MEK1/2 inhibitor in clinical development, suggest a possible difference in pharmacokinetics (PK) between Japanese and Western pat... |
PMC10091821 | core_pubmed_pmc | Emicizumab dose up‐titration in case of suboptimal bleeding control in people with haemophilia A | Emicizumab dose up‐titration in case of suboptimal bleeding control in people with haemophilia A Abstract Abstract Introduction Emicizumab promotes effective haemostasis in people with haemophilia A (PwHA). It is indicated for routine prophylaxis of bleeding episodes in PwHA with or without factor (F)VIII inhibitors. A... |
PMC10800258 | core_pubmed_pmc | Preclinical evaluation of ZL006-05, a new antistroke drug with fast-onset antidepressant and anxiolytic effects | Preclinical evaluation of ZL006-05, a new antistroke drug with fast-onset antidepressant and anxiolytic effects Abstract Abstract Background Poststroke depression and anxiety, independent predictor of poor functional outcomes, are common in the acute phase of stroke. Up to now, there is no fast-onset antidepressive and... |
PMC9598611 | core_pubmed_pmc | Aerosol Inhalation Delivery of Ceftriaxone in Mice: Generation Procedure, Pharmacokinetics, and Therapeutic Outcome | Aerosol Inhalation Delivery of Ceftriaxone in Mice: Generation Procedure, Pharmacokinetics, and Therapeutic Outcome Abstract Abstract Aerosol inhalation delivery of ceftriaxone in mice was investigated. An ultrasonic nebulizer within the ranges of mean particle diameter 0.5–1.5 μm and mass concentration 0.01–0.6 μg/cm ... |
PMC4524853 | core_pubmed_pmc | Theoretical analysis of headache recurrence in patients administered triptans for migraine based on receptor occupancy | Theoretical analysis of headache recurrence in patients administered triptans for migraine based on receptor occupancy Abstract Abstract Background In this study, we retrospectively analyzed the relationship between headache recurrence and serotonin 5-HT 1B/1D receptor occupancy (Φ 1B and Φ 1D ). Triptans marketed in J... |
PMC10983009 | core_pubmed_pmc | Discovery of Conformationally Constrained ALK2 Inhibitors | Discovery of Conformationally Constrained ALK2 Inhibitors Abstract Despite decades of research on new diffuse intrinsic pontine glioma (DIPG) treatments, little or no progress has been made on improving patient outcomes. In this work, we explored novel scaffold modifications of M4K2009 , a 3,5-diphenylpyridine ALK2 inh... |
PMC8879181 | core_pubmed_pmc | Advancement of nanomedicines in chronic inflammatory disorders | Advancement of nanomedicines in chronic inflammatory disorders Abstract Chronic diseases, as stated by the WHO, are a threat to human health which kill 3 out of every 5 people worldwide. Therapeutics for such illnesses can be developed using traditional medicine. However, it is not an easy path from natural products to... |
PMC8411967 | core_pubmed_pmc | Current concepts and molecular mechanisms in pharmacogenetics of essential hypertension | Current concepts and molecular mechanisms in pharmacogenetics of essential hypertension Abstract Abstract Hypertension is a leading age-related disease in our society and if left untreated, leads to fatal cardiovascular complications. The prevalence of hypertension has increased and becomes a significant global health ... |
PMC11510435 | core_pubmed_pmc | A Network Pharmacology Identified Metastasis Target for Oral Squamous Cell Carcinoma Originating from Breast Cancer with a Potential Inhibitor from F. sargassaceae | A Network Pharmacology Identified Metastasis Target for Oral Squamous Cell Carcinoma Originating from Breast Cancer with a Potential Inhibitor from F. sargassaceae Abstract This study aimed to identify specific therapeutic targets for oral squamous cell carcinoma (OSCC) that metastasize from breast cancer (BC) by using... |
PMC11300127 | core_pubmed_pmc | Estimation of latamoxef (moxalactam) dosage regimens against β-lactamase–producing Enterobacterales in dogs: a pharmacokinetic and pharmacodynamic analysis using Monte Carlo simulation | Estimation of latamoxef (moxalactam) dosage regimens against β-lactamase–producing Enterobacterales in dogs: a pharmacokinetic and pharmacodynamic analysis using Monte Carlo simulation Abstract Abstract One of the most significant research areas in veterinary medicine is the search for carbapenem substitutes for the tr... |
PMC6844103 | core_pubmed_pmc | Enterohepatic Circulation and Pharmacokinetics of Genistin and Genistein in Rats | Enterohepatic Circulation and Pharmacokinetics of Genistin and Genistein in Rats Abstract Abstract Genistin and its aglycone genistein of isoflavone are naturally occurring in plants. The aim of this study is to develop an experimental animal model of enterohepatic circulation to investigate the metabolic biotransforma... |
PMC8757644 | core_pubmed_pmc | Xuanfei Baidu Decoction reduces acute lung injury by regulating infiltration of neutrophils and macrophages via PD-1/IL17A pathway | Xuanfei Baidu Decoction reduces acute lung injury by regulating infiltration of neutrophils and macrophages via PD-1/IL17A pathway Abstract Abstract The pathogenic hyper-inflammatory response has been revealed as the major cause of the severity and death of the Corona Virus Disease 2019 (COVID-19). Xuanfei Baidu Decoct... |
PMC9691360 | core_pubmed_pmc | Lipid nanoparticles for delivery of RNA therapeutics: Current status and the role of in vivo imaging | Lipid nanoparticles for delivery of RNA therapeutics: Current status and the role of in vivo imaging Abstract Abstract Lipid nanoparticles (LNPs) have been one of the most successful nano-delivery vehicles that enable efficient delivery of cytotoxic chemotherapy agents, antibiotics, and nucleic acid therapeutics. Durin... |
PMC12071152 | core_pubmed_pmc | Assessment of the Effects of Single-Domain Anti-Idiotypic Distribution Enhancers on the Disposition of Trastuzumab and on the Efficacy of a PE24-Trastuzumab Immunotoxin | Assessment of the Effects of Single-Domain Anti-Idiotypic Distribution Enhancers on the Disposition of Trastuzumab and on the Efficacy of a PE24-Trastuzumab Immunotoxin Abstract Simple Summary The efficacy of antibody-based therapies applied to solid tumors is often limited by the “binding-site barrier” (BSB). Our grou... |
PMC11646621 | core_pubmed_pmc | Disease-Specific Differences in Pharmacokinetics of Paromomycin and Miltefosine Between Post-Kala-Azar Dermal Leishmaniasis and Visceral Leishmaniasis Patients in Eastern Africa | Disease-Specific Differences in Pharmacokinetics of Paromomycin and Miltefosine Between Post-Kala-Azar Dermal Leishmaniasis and Visceral Leishmaniasis Patients in Eastern Africa Abstract Abstract Treatment regimens for post-kala-azar dermal leishmaniasis (PKDL) are usually extrapolated from those for visceral leishmani... |
PMC5869554 | core_pubmed_pmc | Translational model to predict pulmonary pharmacokinetics and efficacy in man for inhaled bronchodilators | Translational model to predict pulmonary pharmacokinetics and efficacy in man for inhaled bronchodilators Abstract Translational pharmacokinetic (PK) models are needed to describe and predict drug concentration‐time profiles in lung tissue at the site of action to enable animal‐to‐man translation and prediction of effi... |
PMC3878283 | core_pubmed_pmc | Impact of Pregnancy on Zonisamide Pharmacokinetics in Rabbits | Impact of Pregnancy on Zonisamide Pharmacokinetics in Rabbits Abstract Abstract Pregnancy is associated with various physiological changes which may lead to significant alterations in the pharmacokinetics of many drugs. The present study was aimed to investigate the potential effects of pregnancy on the pharmacokinetic... |
PMC12734932 | core_pubmed_pmc | Uncovering New Antimelanoma Strategies: Experimental Insights into Semisynthetic Pentacyclic Triterpenoids | Uncovering New Antimelanoma Strategies: Experimental Insights into Semisynthetic Pentacyclic Triterpenoids Abstract In view of the concerning rise in the incidence of cancer, natural products are a valuable source for the development of novel therapies. Among phytochemicals, the pentacyclic triterpenoids betulinic (BA)... |
PMC7818194 | core_pubmed_pmc | Quantification of In Vivo Metabolic Activity of CYP2D6 Genotypes and Alleles Through Population Pharmacokinetic Analysis of Vortioxetine | Quantification of In Vivo Metabolic Activity of CYP2D6 Genotypes and Alleles Through Population Pharmacokinetic Analysis of Vortioxetine Abstract Abstract Assignment of CYP2D6 phenotype from genotype data can be challenging and despite efforts to standardize translation, there is currently no universally accepted metho... |
PMC6005304 | core_pubmed_pmc | Hemangiosarcoma in a Dog: Unusual Presentation and Increased Survival Using a Complementary/Holistic Approach Combined with Metronomic Chemotherapy | Hemangiosarcoma in a Dog: Unusual Presentation and Increased Survival Using a Complementary/Holistic Approach Combined with Metronomic Chemotherapy Abstract Abstract This case report documents the clinical and pathologic findings in a 12-year-old terrier mix with intraocular and splenic hemangiosarcoma. Pathologic find... |
PMC10604328 | core_pubmed_pmc | The Clinical Efficacy of Multidose Oritavancin: A Systematic Review | The Clinical Efficacy of Multidose Oritavancin: A Systematic Review Abstract Oritavancin (ORI) is a semisynthetic lipoglycopeptide approved as a single 1200 mg dose intravenous infusion for the treatment of acute bacterial skin and skin structure infections (ABSSSIs) caused by Gram-positive organisms in adults. The pha... |
PMC9951903 | core_pubmed_pmc | Meropenem Model-Informed Precision Dosing in the Treatment of Critically Ill Patients: Can We Use It? | Meropenem Model-Informed Precision Dosing in the Treatment of Critically Ill Patients: Can We Use It? Abstract Abstract The number of pharmacokinetic (PK) models of meropenem is increasing. However, the daily role of these PK models in the clinic remains unclear, especially for critically ill patients. Therefore, we ev... |
PMC4623269 | core_pubmed_pmc | Bioanalytical strategy used in development of pharmacokinetic (PK) methods that support biosimilar programs | Bioanalytical strategy used in development of pharmacokinetic (PK) methods that support biosimilar programs Abstract Abstract The development of biosimilar products is expected to grow rapidly over the next five years as a large number of approved biologics reach patent expiry. The pathway to regulatory approval requir... |
PMC9127093 | core_pubmed_pmc | A genetic engineering strategy for editing near-infrared-II fluorophores | A genetic engineering strategy for editing near-infrared-II fluorophores Abstract Abstract The second near-infrared (NIR-II) window is a fundamental modality for deep-tissue in vivo imaging. However, it is challenging to synthesize NIR-II probes with high quantum yields (QYs), good biocompatibility, satisfactory pharma... |
PMC12409655 | core_pubmed_pmc | Population Pharmacokinetic Model‐Based Optimization of Linezolid Dosing in Hematooncological Patients With Suspected or Proven Gram‐Positive Sepsis | Population Pharmacokinetic Model‐Based Optimization of Linezolid Dosing in Hematooncological Patients With Suspected or Proven Gram‐Positive Sepsis Abstract ABSTRACT The objective of this study was to develop a population pharmacokinetic model for linezolid in hematooncological patients with sepsis, and to propose dosi... |
PMC11271292 | core_pubmed_pmc | Towards pharmacokinetic boosting of phenoxymethylpenicillin (penicillin-V) using probenecid for the treatment of bacterial infections | Towards pharmacokinetic boosting of phenoxymethylpenicillin (penicillin-V) using probenecid for the treatment of bacterial infections Abstract Abstract In the face of increasing antimicrobial tolerance and resistance there is a global obligation to optimise oral antimicrobial dosing strategies including narrow spectrum... |
PMC4834588 | core_pubmed_pmc | Development of a physiologically based pharmacokinetic model of actinomycin D in children with cancer | Development of a physiologically based pharmacokinetic model of actinomycin D in children with cancer Abstract Aims Use of the anti‐tumour antibiotic actinomycin D is associated with development of hepatotoxicity, particularly in young children. A paucity of actinomycin D pharmacokinetic data make it challenging to dev... |
PMC9121505 | core_pubmed_pmc | A comprehensive review of intravitreal immunosuppressants and biologicals used in ophthalmology | A comprehensive review of intravitreal immunosuppressants and biologicals used in ophthalmology Abstract Abstract Systemic immunosuppressants and biologicals have been a valuable tool in the treatment of inflammatory diseases and malignancies. The safety profile of these drugs has been debatable, especially in localize... |
PMC7364025 | core_pubmed_pmc | Integration of computer-simulated practical exercises into undergraduate medical pharmacology education at Mulungushi University, Zambia | Integration of computer-simulated practical exercises into undergraduate medical pharmacology education at Mulungushi University, Zambia Abstract Purpose This study was conducted to determine whether a computer simulation of practical exercises in undergraduate medical pharmacology led to the realization of the intende... |
PMC11207005 | core_pubmed_pmc | Evaluation of Solubility, Dissolution Rate, and Oral Bioavailability of β-Cyclodextrin and Hydroxypropyl β-Cyclodextrin as Inclusion Complexes of the Tyrosine Kinase Inhibitor, Alectinib | Evaluation of Solubility, Dissolution Rate, and Oral Bioavailability of β-Cyclodextrin and Hydroxypropyl β-Cyclodextrin as Inclusion Complexes of the Tyrosine Kinase Inhibitor, Alectinib Abstract Abstract This study aims to improve the solubility and dissolution rate of alectinib (ALB), a tyrosine kinase inhibitor comm... |
PMC9286714 | core_pubmed_pmc | Population pharmacokinetics for oral paclitaxel in patients with advanced/metastatic solid tumors | Population pharmacokinetics for oral paclitaxel in patients with advanced/metastatic solid tumors Abstract Abstract Oraxol consists of an oral dosage form of the chemotherapeutic agent paclitaxel administered with a novel P‐glycoprotein inhibitor encequidar methanesulfonate monohydrate (formerly named HM30181A), which ... |
PMC3758216 | core_pubmed_pmc | Preparation, characterization, and in vivo pharmacokinetics of nanostructured lipid carriers loaded with oleanolic acid and gentiopicrin | Preparation, characterization, and in vivo pharmacokinetics of nanostructured lipid carriers loaded with oleanolic acid and gentiopicrin Abstract Abstract Background The purpose of this work was to develop nanostructured lipid carriers (NLCs) loaded simultaneously with oleanolic acid and gentiopicrin. Methods An aqueou... |
PMC12628573 | core_pubmed_pmc | Scarlet fever and meteorological exposures in Jiangsu, China: a time-stratified case-crossover study | Scarlet fever and meteorological exposures in Jiangsu, China: a time-stratified case-crossover study Abstract Abstract Background There has been an increasing interest in the association between meteorological risk factors and scarlet fever risk. However, the associations between individual-level exposure to meteorolog... |
PMC6781664 | core_pubmed_pmc | Pharmacokinetic studies of nanoparticles as a delivery system for conventional drugs and herb-derived compounds for cancer therapy: a systematic review | Pharmacokinetic studies of nanoparticles as a delivery system for conventional drugs and herb-derived compounds for cancer therapy: a systematic review Abstract Abstract The poor pharmacokinetic characteristics of most anticancer drugs have limited their clinical effectiveness. The application of nanoparticles as a nov... |
PMC5900865 | core_pubmed_pmc | Pharmacokinetics, Safety, and Tolerability of Vortioxetine Following Single‐ and Multiple‐Dose Administration in Healthy Japanese Adults | Pharmacokinetics, Safety, and Tolerability of Vortioxetine Following Single‐ and Multiple‐Dose Administration in Healthy Japanese Adults Abstract Abstract Three phase 1 randomized single‐center studies assessed the pharmacokinetics, safety, and tolerability of vortioxetine after single‐ and multiple‐dose administration... |
PMC11475820 | core_pubmed_pmc | Drug Interactions between Androgen Receptor Axis-Targeted Therapies and Antithrombotic Therapies in Prostate Cancer: Delphi Consensus | Drug Interactions between Androgen Receptor Axis-Targeted Therapies and Antithrombotic Therapies in Prostate Cancer: Delphi Consensus Abstract Abstract Simple Summary Prostate cancer is most commonly diagnosed in males after the age of 55 years. These patients are also at risk for cardiovascular disease and venous thro... |
PMC6244811 | core_pubmed_pmc | An open-label, single-dose study to evaluate the safety, tolerability, pharmacokinetics, and pharmacodynamics of cinacalcet in pediatric subjects aged 28 days to < 6 years with chronic kidney disease receiving dialysis | An open-label, single-dose study to evaluate the safety, tolerability, pharmacokinetics, and pharmacodynamics of cinacalcet in pediatric subjects aged 28 days to < 6 years with chronic kidney disease receiving dialysis Abstract Background Calcimimetics, shown to control biochemical parameters of secondary hyperparathyr... |
PMC9585163 | core_pubmed_pmc | Comorbid epilepsy and depression—pharmacokinetic and pharmacodynamic drug interactions | Comorbid epilepsy and depression—pharmacokinetic and pharmacodynamic drug interactions Abstract Abstract Background: Major depressive disorder may be encountered in 17% of patients with epilepsy and in patients with drug-resistant epilepsy its prevalence may reach 30%. This indicates that patients with epilepsy may req... |
PMC9393655 | core_pubmed_pmc | Intravenous Brivaracetam in the Management of Acute Seizures in the Hospital Setting: A Scoping Review | Intravenous Brivaracetam in the Management of Acute Seizures in the Hospital Setting: A Scoping Review Abstract Abstract Background Clinical considerations for drug treatment of acute seizures involve variables such as safety, tolerability, drug-drug interactions, dosage, route of administration, and alterations in pha... |
PMC6130436 | core_pubmed_pmc | Influence of andrographolide on the pharmacokinetics of warfarin in rats | Influence of andrographolide on the pharmacokinetics of warfarin in rats Abstract Abstract Context : Andrographolide and w arfarin are often used together in clinics in China. However, the herb-drug interaction between andrographolide and warfarin is still unknown. Objective: This study investigates the herb-drug inter... |
PMC11821031 | core_pubmed_pmc | Pharmacological Significance, Medicinal Use, and Toxicity of Extracted and Isolated Compounds from Euphorbia Species Found in Southern Africa: A Review | Pharmacological Significance, Medicinal Use, and Toxicity of Extracted and Isolated Compounds from Euphorbia Species Found in Southern Africa: A Review Abstract This study documents the Euphorbiaceae family of plants in Southern Africa, with a focus on their traditional medicinal applications, pharmacological propertie... |
PMC12292445 | core_pubmed_pmc | Physiologically Based Pharmacokinetic Modeling for Predicting Drug Levels After Bariatric Surgery: Vardenafil Exposure Before vs. After Gastric Sleeve/Bypass | Physiologically Based Pharmacokinetic Modeling for Predicting Drug Levels After Bariatric Surgery: Vardenafil Exposure Before vs. After Gastric Sleeve/Bypass Abstract Abstract Bariatric surgery involves major changes in the anatomy and physiology of the gastrointestinal tract, which may alter oral drug bioavailability ... |
PMC3603526 | core_pubmed_pmc | Scientific Challenges and Implementation Barriers to Translation of Pharmacogenomics in Clinical Practice | Scientific Challenges and Implementation Barriers to Translation of Pharmacogenomics in Clinical Practice Abstract Abstract The mapping of the human genome and subsequent advancements in genetic technology had provided clinicians and scientists an understanding of the genetic basis of altered drug pharmacokinetics and ... |
PMC12575316 | core_pubmed_pmc | GEODE: an in silico tool that translates in vitro to in vivo predictions of tuberculosis antibiotic combination efficacy | GEODE: an in silico tool that translates in vitro to in vivo predictions of tuberculosis antibiotic combination efficacy Abstract Introduction Tuberculosis (TB) remains the primary cause of death due to infectious disease in the world. TB, while treatable, requires an extended course of multiple antibiotics, taking 6–9... |
PMC5872082 | core_pubmed_pmc | Pharmacogenomic Impact of CYP2C19 Variation on Clopidogrel Therapy in Precision Cardiovascular Medicine | Pharmacogenomic Impact of CYP2C19 Variation on Clopidogrel Therapy in Precision Cardiovascular Medicine Abstract Abstract Variability in response to antiplatelet therapy can be explained in part by pharmacogenomics, particularly of the CYP450 enzyme encoded by CYP2C19 . Loss-of-function and gain-of-function variants he... |
PMC6175062 | core_pubmed_pmc | Gaining Mechanistic Insight Into Coproporphyrin I as Endogenous Biomarker for OATP1B‐Mediated Drug–Drug Interactions Using Population Pharmacokinetic Modeling and Simulation | Gaining Mechanistic Insight Into Coproporphyrin I as Endogenous Biomarker for OATP1B‐Mediated Drug–Drug Interactions Using Population Pharmacokinetic Modeling and Simulation Abstract This study evaluated coproporphyrin I (CPI) as a selective endogenous biomarker of OATP1B‐mediated drug–drug interactions (DDIs) relative... |
PMC8596879 | core_pubmed_pmc | A Target‐Mediated Drug Disposition Model to Explain Nonlinear Pharmacokinetics of the 11β‐Hydroxysteroid Dehydrogenase Type 1 Inhibitor SPI‐62 in Healthy Adults | A Target‐Mediated Drug Disposition Model to Explain Nonlinear Pharmacokinetics of the 11β‐Hydroxysteroid Dehydrogenase Type 1 Inhibitor SPI‐62 in Healthy Adults Abstract Abstract SPI‐62 is a selective and potent small‐molecule inhibitor of 11β‐hydroxysteroid dehydrogenase type 1 (HSD‐1). SPI‐62 has demonstrated substan... |
PMC3516572 | core_pubmed_pmc | MiniCD4 Microbicide Prevents HIV Infection of Human Mucosal Explants and Vaginal Transmission of SHIV 162P3 in Cynomolgus Macaques | MiniCD4 Microbicide Prevents HIV Infection of Human Mucosal Explants and Vaginal Transmission of SHIV 162P3 in Cynomolgus Macaques Abstract Abstract In complement to an effective vaccine, development of potent anti-HIV microbicides remains an important priority. We have previously shown that the miniCD4 M48U1, a functi... |
PMC5094430 | core_pubmed_pmc | Effect of tramadol on metamizol pharmacokinetics and pharmacodynamics after single and repeated administrations in arthritic rats | Effect of tramadol on metamizol pharmacokinetics and pharmacodynamics after single and repeated administrations in arthritic rats Abstract Combined administration of certain doses of opioid compounds with a non-steroidal anti-inflammatory drug can produce additive or supra-additive effects while reducing unwanted effec... |
PMC3600724 | core_pubmed_pmc | Simulations to Assess Phase II Noninferiority Trials of Different Doses of Capecitabine in Combination With Docetaxel for Metastatic Breast Cancer | Simulations to Assess Phase II Noninferiority Trials of Different Doses of Capecitabine in Combination With Docetaxel for Metastatic Breast Cancer Abstract Abstract A phase II trial in metastatic breast cancer (MBC) (NO16853) failed to show noninferiority (progression-free survival, PFS) of capecitabine 825 mg/m 2 plus... |
PMC8224687 | core_pubmed_pmc | Lipophilicity, Pharmacokinetic Properties, and Molecular Docking Study on SARS-CoV-2 Target for Betulin Triazole Derivatives with Attached 1,4-Quinone | Lipophilicity, Pharmacokinetic Properties, and Molecular Docking Study on SARS-CoV-2 Target for Betulin Triazole Derivatives with Attached 1,4-Quinone Abstract A key parameter in the design of new active compounds is lipophilicity, which influences the solubility and permeability through membranes. Lipophilicity affect... |
PMC10609681 | core_pubmed_pmc | Differential Responders to a Mixed Meal Tolerance Test Associated with Type 2 Diabetes Risk Factors and Gut Microbiota—Data from the MEDGI-Carb Randomized Controlled Trial | Differential Responders to a Mixed Meal Tolerance Test Associated with Type 2 Diabetes Risk Factors and Gut Microbiota—Data from the MEDGI-Carb Randomized Controlled Trial Abstract Abstract The global prevalence of type 2 diabetes mellitus (T2DM) has surged in recent decades, and the identification of differential glyc... |
PMC4576779 | core_pubmed_pmc | Phenotypic differences in nebivolol metabolism and bioavailability in healthy volunteers | Phenotypic differences in nebivolol metabolism and bioavailability in healthy volunteers Abstract Abstract Introduction Nebivolol, a third-generation β-blocker, is subject to extensive first-pass metabolism and produces active β-blocking hydroxylated metabolites, like 4-OH-nebivolol. It is primarily a substrate of CYP2... |
PMC8592410 | core_pubmed_pmc | PD-L1 expression on circulating tumor cells and platelets in patients with metastatic breast cancer | PD-L1 expression on circulating tumor cells and platelets in patients with metastatic breast cancer Abstract Background Immune checkpoint inhibition is effective in several cancers. Expression of programmed death-ligand 1 (PD-L1) on circulating tumor or immune effector cells could provide insights into selection of pat... |
PMC11539233 | core_pubmed_pmc | Therapeutic drug monitoring of linezolid in Chinese premature neonates: a population pharmacokinetic analysis and dosage optimization | Therapeutic drug monitoring of linezolid in Chinese premature neonates: a population pharmacokinetic analysis and dosage optimization Abstract ABSTRACT This study aimed to develop a pharmacokinetic model of linezolid in premature neonates and evaluate and optimize the administration regimen. Liquid chromatography-tande... |
PMC5340401 | core_pubmed_pmc | Favipiravir pharmacokinetics in Ebola-Infected patients of the JIKI trial reveals concentrations lower than targeted | Favipiravir pharmacokinetics in Ebola-Infected patients of the JIKI trial reveals concentrations lower than targeted Abstract Background In 2014–2015, we assessed favipiravir tolerance and efficacy in patients with Ebola virus (EBOV) disease (EVD) in Guinea (JIKI trial). Because the drug had never been used before for ... |
PMC5913882 | core_pubmed_pmc | Extrahepatic cytochrome P450s play an insignificant role in triptolide-induced toxicity | Extrahepatic cytochrome P450s play an insignificant role in triptolide-induced toxicity Abstract Abstract Background Triptolide, an active ingredient of Chinese medicine plant Tripterygium wilfordii Hook.f., has been shown to exert anti-tumor, immunosuppressive, anti-inflammatory, and anti-fertility pharmacological eff... |
PMC10322960 | core_pubmed_pmc | Pharmacokinetics and Drug–Drug Interaction of Ocedurenone (KBP-5074) in vitro and in vivo | Pharmacokinetics and Drug–Drug Interaction of Ocedurenone (KBP-5074) in vitro and in vivo Abstract Background and Objectives Ocedurenone (KBP-5074) is a novel nonsteroidal mineralocorticoid receptor antagonist that has demonstrated safety and efficacy in clinical trials in patients with uncontrolled hypertension and st... |
PMC12881942 | core_pubmed_pmc | Pharmacokinetic analysis and steady-state predictions of different preparations of metronidazole administered per rectum in adult horses | Pharmacokinetic analysis and steady-state predictions of different preparations of metronidazole administered per rectum in adult horses Abstract Abstract Background Manipulation of forms of rectally administered metronidazole to improve bioavailability in horses has not been reported. Hypothesis/Objectives Evaluate th... |
PMC12316928 | core_pubmed_pmc | Synthesis and evaluation of novel thiohydantoin derivatives for antidiabetic activity using in silico in vitro and in vivo methods | Synthesis and evaluation of novel thiohydantoin derivatives for antidiabetic activity using in silico in vitro and in vivo methods Abstract Diabetes mellitus remains a global health challenge, necessitating the development of novel therapeutic agents. In this study, a series of thiohydantoin derivatives (FP1–FP7) were ... |
PMC7229567 | core_pubmed_pmc | Comparative Pharmacokinetics of Geniposidic Acid, Genipin-1- β -Gentiobioside, Geniposide, Genipin, and Crocetin in Rats after Oral Administration of Crude Gardeniae Fructus and Its Three Processed Products Using LC-MS/MS | Comparative Pharmacokinetics of Geniposidic Acid, Genipin-1- β -Gentiobioside, Geniposide, Genipin, and Crocetin in Rats after Oral Administration of Crude Gardeniae Fructus and Its Three Processed Products Using LC-MS/MS Abstract Abstract The extract of Gardeniae Fructus (GF) with different processing methods processe... |
PMC12860500 | core_pubmed_pmc | Exploiting Pharmacokinetic/Pharmacodynamic Methods for Optimizing and Accelerating Drug Development of Innovative Anti‐Infectives | Exploiting Pharmacokinetic/Pharmacodynamic Methods for Optimizing and Accelerating Drug Development of Innovative Anti‐Infectives Abstract Bearing the increase in antimicrobial resistance as well as the emergence of novel viruses with pandemic potential in mind, it is obvious that development pathways need to be accele... |
PMC11356933 | core_pubmed_pmc | Optimization and Spectrum–Effect Analysis of Ultrasonically Extracted Antioxidant Flavonoids from Persicae Ramulus | Optimization and Spectrum–Effect Analysis of Ultrasonically Extracted Antioxidant Flavonoids from Persicae Ramulus Abstract The objectives of this study were to optimize the ultrasonic-assisted flavonoid extraction process from PR and to establish fingerprints in order to analyze the spectrum–effect relationship of ant... |
PMC12572095 | core_pubmed_pmc | Aldosterone Synthase Inhibitors for Resistant Hypertension: Pharmacological Insights – A Systematic Review | Aldosterone Synthase Inhibitors for Resistant Hypertension: Pharmacological Insights – A Systematic Review Abstract Background Resistant hypertension (RHT) is a challenging clinical condition characterized by persistently elevated blood pressure despite adherence to lifestyle modifications and the use of at least three... |
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