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PMC7197763
core_pubmed_pmc
PG-path: Modeling and personalizing pharmacogenomics-based pathways
PG-path: Modeling and personalizing pharmacogenomics-based pathways Abstract Abstract A pharmacogenomics-based pathway represents a series of reactions that occur between drugs and genes in the human body after drug administration. PG-path is a pharmacogenomics-based pathway that standardizes and visualizes the compone...
PMC5421726
core_pubmed_pmc
Pharmacokinetic/Pharmacodynamic Modeling of the PDE4 Inhibitor TAK‐648 in Type 2 Diabetes: Early Translational Approaches for Human Dose Prediction
Pharmacokinetic/Pharmacodynamic Modeling of the PDE4 Inhibitor TAK‐648 in Type 2 Diabetes: Early Translational Approaches for Human Dose Prediction Abstract Abstract TAK‐648 is a PDE4 inhibitor with demonstrated preclinical antidiabetic properties. Our objective was to develop a translational pharmacokinetic/pharmacody...
PMC2825537
core_pubmed_pmc
Development and validation of a rapid method for the detection of latrunculol A in plasma
Development and validation of a rapid method for the detection of latrunculol A in plasma Abstract Abstract Latrunculol A is a recently discovered 6,7-dihydroxy analog of the potent actin inhibitor latrunculin A. Latrunculol A has exhibited greater cytotoxicity than latrunculin A against both murine and human colon tum...
PMC7239618
core_pubmed_pmc
The immunology of COVID-19: is immune modulation an option for treatment?
The immunology of COVID-19: is immune modulation an option for treatment? Abstract Summary In December, 2019, an outbreak of COVID-19 emerged in Wuhan, China and quickly spread globally. As of May 7, 2020, there were 3 672 238 confirmed infections and 254 045 deaths attributed to COVID-19. Evidence has shown that there...
PMC5298035
core_pubmed_pmc
Pharmacokinetic Evaluation of CYP3A4‐Mediated Drug‐Drug Interactions of Isavuconazole With Rifampin, Ketoconazole, Midazolam, and Ethinyl Estradiol/Norethindrone in Healthy Adults
Pharmacokinetic Evaluation of CYP3A4‐Mediated Drug‐Drug Interactions of Isavuconazole With Rifampin, Ketoconazole, Midazolam, and Ethinyl Estradiol/Norethindrone in Healthy Adults Abstract Abstract This report describes the phase 1 trials that evaluated the metabolism of the novel triazole antifungal isavuconazole by c...
PMC11947755
core_pubmed_pmc
A Phase I/IB, Open Label, Dose Finding Study to Evaluate Safety, Pharmacodynamics and Efficacy of Pembrolizumab in Combination With Vorinostat in Patients With Advanced Prostate, Renal or Urothelial Carcinoma
A Phase I/IB, Open Label, Dose Finding Study to Evaluate Safety, Pharmacodynamics and Efficacy of Pembrolizumab in Combination With Vorinostat in Patients With Advanced Prostate, Renal or Urothelial Carcinoma Abstract ABSTRACT Background Immunosuppressive factors such as regulatory T cells and myeloid‐derived suppressi...
PMC12141017
core_pubmed_pmc
Pharmacokinetic and pharmacodynamic analyses of nafamostat in ECMO patients: comparing central vein and ECMO machine samples
Pharmacokinetic and pharmacodynamic analyses of nafamostat in ECMO patients: comparing central vein and ECMO machine samples Abstract Objectives To better understand nafamostat mesylate (NM) dose requirements during extracorporeal membrane oxygenation (ECMO), this study investigated its pharmacokinetic/pharmacodynamic ...
PMC6018403
core_pubmed_pmc
A 42-Markers Pharmacokinetic Study Reveals Interactions of Berberine and Glycyrrhizic Acid in the Anti-diabetic Chinese Medicine Formula Gegen-Qinlian Decoction
A 42-Markers Pharmacokinetic Study Reveals Interactions of Berberine and Glycyrrhizic Acid in the Anti-diabetic Chinese Medicine Formula Gegen-Qinlian Decoction Abstract Abstract Herbal medicines are commonly used as compound formulas in clinical practice to achieve optimal therapeutic effects. However, the combination...
PMC11144068
core_pubmed_pmc
Investigation of Herb-Drug Interactions between Xylopia aethiopica , Its Principal Constituent Xylopic Acid, and Antidepressants
Investigation of Herb-Drug Interactions between Xylopia aethiopica , Its Principal Constituent Xylopic Acid, and Antidepressants Abstract Introduction Depression affects an estimated 350 million people worldwide and is implicated in up to 60% of suicides. Only about 60–70% of patients respond to antidepressant therapy....
PMC10410017
core_pubmed_pmc
The kinetics of isotonic and hypertonic resuscitation fluids is dependent on the sizes of the body fluid volumes
The kinetics of isotonic and hypertonic resuscitation fluids is dependent on the sizes of the body fluid volumes Abstract Abstract Background and Aims: The extracellular and intracellular fluid volumes (ECV and ICV) vary not only with age, gender, and body weight but also with the habitual intake of water. The present ...
PMC12950821
core_pubmed_pmc
Safety pharmacology and toxicology of a novel nitroimidazooxazole antitubercular agent in SD rat and Beagle dogs
Safety pharmacology and toxicology of a novel nitroimidazooxazole antitubercular agent in SD rat and Beagle dogs Abstract We developed JBD0131, a novel nitroimidazooxazole antitubercular agent, and conducted a comprehensive preclinical evaluation of its safety pharmacology, toxicology, and pharmacokinetics in SD rats a...
PMC9742878
core_pubmed_pmc
Neurotoxicity associated with colistin methanesulfonate treatment is enhanced by concomitant sevoflurane inhalation
Neurotoxicity associated with colistin methanesulfonate treatment is enhanced by concomitant sevoflurane inhalation Abstract Abstract Colistin methanesulfonate (CMS) is a cyclic polypeptide antibiotic with neurotoxic side effects. Sevoflurane (Sevo), an inhaled anesthetic, is known to enhance the non-depolarizing effec...
PMC6580366
core_pubmed_pmc
A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction
A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction Abstract The p38αMAPK is a serine/threonine protein kinase and a key node in the intracellular signaling networks that transduce and amplify stress signa...
PMC8265417
core_pubmed_pmc
Prediction of pharmacokinetic values of two various dosages of caffeine in premature neonates with apnea
Prediction of pharmacokinetic values of two various dosages of caffeine in premature neonates with apnea Abstract Abstract OBJECTIVES: Despite extensive caffeine use in preterm infants, the pharmacokinetics (PKs) data are limited because of the studies are complicated to do in these patients. This research was investig...
PMC10100687
core_pubmed_pmc
Pharmacokinetics of Bictegravir in Older Japanese People Living with HIV-1
Pharmacokinetics of Bictegravir in Older Japanese People Living with HIV-1 Abstract ABSTRACT Bictegravir (BIC) is an integrase strand transfer inhibitor widely used in the treatment of HIV-1. Although its potency and safety have been demonstrated in older patients, pharmacokinetics (PK) data remain limited in this pati...
PMC8740778
core_pubmed_pmc
Translational Pharmacokinetic–Pharmacodynamic Modeling of NaV1.7 Inhibitor MK-2075 to Inform Human Efficacious Dose
Translational Pharmacokinetic–Pharmacodynamic Modeling of NaV1.7 Inhibitor MK-2075 to Inform Human Efficacious Dose Abstract MK-2075 is a small-molecule selective inhibitor of the NaV1.7 channel investigated for the treatment of postoperative pain. A translational strategy was developed for MK-2075 to quantitatively in...
PMC12434307
core_pubmed_pmc
Synergistic antiallodynic effects of pregabalin and thioctic acid in a rat model of neuropathic pain
Synergistic antiallodynic effects of pregabalin and thioctic acid in a rat model of neuropathic pain Abstract Abstract Background Neuropathic pain is a chronic and often disabling condition that remains refractory to monotherapy because of limited efficacy and dose-limiting adverse effects. Combination therapies that e...
PMC8284440
core_pubmed_pmc
Toward New Transmission-Blocking Combination Therapies: Pharmacokinetics of 10-Amino-Artemisinins and 11-Aza-Artemisinin and Comparison with Dihydroartemisinin and Artemether
Toward New Transmission-Blocking Combination Therapies: Pharmacokinetics of 10-Amino-Artemisinins and 11-Aza-Artemisinin and Comparison with Dihydroartemisinin and Artemether Abstract ABSTRACT As artemisinin combination therapies (ACTs) are compromised by resistance, we are evaluating triple combination therapies (TACT...
PMC12025280
core_pubmed_pmc
A Clinical Comparative Study of Schnider and Eleveld Pharmacokinetic–Pharmacodynamic Models for Propofol Target-Controlled Infusion Sedation in Drug-Induced Sleep Endoscopy
A Clinical Comparative Study of Schnider and Eleveld Pharmacokinetic–Pharmacodynamic Models for Propofol Target-Controlled Infusion Sedation in Drug-Induced Sleep Endoscopy Abstract Background: Optimizing sedative techniques for drug-induced sleep endoscopy (DISE) enhances accuracy and reproducibility in tailoring trea...
PMC11128199
core_pubmed_pmc
Prophylactic efficacy of an intranasal spray with 2 synergetic antibodies neutralizing Omicron
Prophylactic efficacy of an intranasal spray with 2 synergetic antibodies neutralizing Omicron Abstract Abstract BACKGROUND As Omicron is prompted to replicate in the upper airway, neutralizing antibodies (NAbs) delivered through inhalation might inhibit early-stage infection in the respiratory tract. Thus, elucidating...
PMC6423892
core_pubmed_pmc
Treatment of pigs with endectocides as a complementary tool for combating malaria transmission by Anopheles farauti ( s.s. ) in Papua New Guinea
Treatment of pigs with endectocides as a complementary tool for combating malaria transmission by Anopheles farauti ( s.s. ) in Papua New Guinea Abstract Background Outdoor, early-biting, zoophagic behaviours by Anopheles farauti ( s.s .) can compromise the effectiveness of bed nets for malaria control. In the Western ...
PMC5446366
core_pubmed_pmc
Minocycline for the Treatment of Multidrug and Extensively Drug-Resistant A. baumannii : A Review
Minocycline for the Treatment of Multidrug and Extensively Drug-Resistant A. baumannii : A Review Abstract Acinetobacter baumannii can cause life-threatening nosocomial infections associated with high rates of morbidity and mortality. In recent years, the increasing number of infections due to extensively drug-resistan...
PMC7579265
core_pubmed_pmc
First-in-Human Study of the Safety, Tolerability, Pharmacokinetics and -Preliminary Dynamics of Neuroprotectant 2-Iminobiotin in Healthy Subjects
First-in-Human Study of the Safety, Tolerability, Pharmacokinetics and -Preliminary Dynamics of Neuroprotectant 2-Iminobiotin in Healthy Subjects Abstract Abstract Background 2-iminobiotin (2-IB) is an investigational neuroprotective agent in development for the reduction of brain cell injury after cerebral hypoxia-isc...
PMC8707461
core_pubmed_pmc
In Vitro and In Vivo Inhibition of MATE1 by Tyrosine Kinase Inhibitors
In Vitro and In Vivo Inhibition of MATE1 by Tyrosine Kinase Inhibitors Abstract The membrane transport of many cationic prescription drugs depends on facilitated transport by organic cation transporters of which several members, including OCT2 ( SLC22A2 ), are sensitive to inhibition by select tyrosine kinase inhibitor...
PMC5937083
core_pubmed_pmc
Physicochemical, Stress Degradation Evaluation and Pharmacokinetic Study of AZGH101; a New Synthesized COX2 Inhibitor after I.V. and Oral Administration in Male and Female Rats
Physicochemical, Stress Degradation Evaluation and Pharmacokinetic Study of AZGH101; a New Synthesized COX2 Inhibitor after I.V. and Oral Administration in Male and Female Rats Abstract Nonsteroidal anti-inflammatory drugs (NSAIDs) act mainly via inhibition of prostaglandins synthesis by inhibition of cyclooxygenase (C...
PMC10419826
core_pubmed_pmc
Efficacy and Safety of S1P1 Receptor Modulator Drugs for Patients with Moderate-to-Severe Ulcerative Colitis
Efficacy and Safety of S1P1 Receptor Modulator Drugs for Patients with Moderate-to-Severe Ulcerative Colitis Abstract Abstract Ulcerative colitis (UC) is a chronic inflammatory bowel disease (IBD) that negatively impacts patients’ quality of life. In the last decades, the therapeutic options available for the managemen...
PMC10509964
core_pubmed_pmc
IL-33 receptor inhibition in subjects with uncontrolled asthma: A randomized, placebo-controlled trial
IL-33 receptor inhibition in subjects with uncontrolled asthma: A randomized, placebo-controlled trial Abstract Abstract Background Most biologics for severe asthma target only type 2 immunity. Inhibition of IL-33 signaling has the potential to target type 2 and non–type 2 pathways. Objective This multicenter phase IIA...
PMC8826824
core_pubmed_pmc
In Vitro Activity of KBP-7072 against 536 Acinetobacter baumannii Complex Isolates Collected in China
In Vitro Activity of KBP-7072 against 536 Acinetobacter baumannii Complex Isolates Collected in China Abstract ABSTRACT Acinetobacter baumannii has emerged globally as a difficult-to-treat nosocomial pathogen and become resistant to carbapenems, resulting in limited treatment options. KBP-7072 is a novel semisynthetic ...
PMC5328512
core_pubmed_pmc
Pharmacokinetics of Miltefosine in Children and Adults with Cutaneous Leishmaniasis
Pharmacokinetics of Miltefosine in Children and Adults with Cutaneous Leishmaniasis Abstract ABSTRACT An open-label pharmacokinetics (PK) clinical trial was conducted to comparatively assess the PK and explore the pharmacodynamics (PD) of miltefosine in children and adults with cutaneous leishmaniasis (CL) in Colombia....
PMC11398325
core_pubmed_pmc
In vivo Imaging and Pharmacokinetics of Percutaneously Injected Ultrasound and X-ray Imageable Thermosensitive Hydrogel loaded with Doxorubicin versus Free Drug in Swine
In vivo Imaging and Pharmacokinetics of Percutaneously Injected Ultrasound and X-ray Imageable Thermosensitive Hydrogel loaded with Doxorubicin versus Free Drug in Swine Abstract Intratumoral injections often lack visibility, leading to unpredictable outcomes such as incomplete tumor coverage, off-target drug delivery ...
PMC11510156
core_pubmed_pmc
Rutin and Physalis peruviana Extract: Population Pharmacokinetics in New Zealand Rabbits
Rutin and Physalis peruviana Extract: Population Pharmacokinetics in New Zealand Rabbits Abstract Background/Objectives: An extract of calyces from Physalis peruviana with hypoglycemic activity is being considered as a potential herbal medicine. Preclinical pharmacokinetics (PK) studies of the extract in rats, focusing...
PMC5986682
core_pubmed_pmc
Delafloxacin: Place in Therapy and Review of Microbiologic, Clinical and Pharmacologic Properties
Delafloxacin: Place in Therapy and Review of Microbiologic, Clinical and Pharmacologic Properties Abstract Abstract Delafloxacin (formerly WQ-3034, ABT492, RX-3341) is a novel fluoroquinolone chemically distinct from currently marketed fluoroquinolones with the absence of a protonatable substituent conferring a weakly ...
PMC8502823
core_pubmed_pmc
A Proof of Concept of the Role of TDM-Based Clinical Pharmacological Advices in Optimizing Antimicrobial Therapy on Real-Time in Different Paediatric Settings
A Proof of Concept of the Role of TDM-Based Clinical Pharmacological Advices in Optimizing Antimicrobial Therapy on Real-Time in Different Paediatric Settings Abstract Introduction: Antimicrobial treatment is quite common among hospitalized children. The dynamic age-associated physiological variations coupled with the ...
PMC6243382
core_pubmed_pmc
A phase I study of TAS‐205 in patients with Duchenne muscular dystrophy
A phase I study of TAS‐205 in patients with Duchenne muscular dystrophy Abstract Abstract Objective Currently, the only approved standard Duchenne muscular dystrophy (DMD) treatment in Japan is oral steroids, which have various disadvantages. Previous work has suggested that hematopoietic‐type prostaglandin D synthase ...
PMC6692323
core_pubmed_pmc
Model based development of tacrolimus dosing algorithm considering CYP3A5 genotypes and mycophenolate mofetil drug interaction in stable kidney transplant recipients
Model based development of tacrolimus dosing algorithm considering CYP3A5 genotypes and mycophenolate mofetil drug interaction in stable kidney transplant recipients Abstract This study quantifies the interaction between tacrolimus (TAC) and mycophenolate mofetil (MMF) in kidney transplant recipients. Concentrations of...
PMC5678723
core_pubmed_pmc
Effects of CD49d-targeted antisense-oligonucleotide on α4 integrin expression and function of acute lymphoblastic leukemia cells: Results of in vitro and in vivo studies
Effects of CD49d-targeted antisense-oligonucleotide on α4 integrin expression and function of acute lymphoblastic leukemia cells: Results of in vitro and in vivo studies Abstract Abstract We recently demonstrated the effectiveness of blocking CD49d with anti-functional antibodies or small molecule inhibitors as a ratio...
PMC12303110
core_pubmed_pmc
Enzyme inhibitory activity of marine alkaloid aaptamines for neurodegenerative diseases: an in silico study
Enzyme inhibitory activity of marine alkaloid aaptamines for neurodegenerative diseases: an in silico study Abstract The enzyme inhibitory activities of a dataset of 28 aaptamines are performed to identify potential multifunctional drugs for neurodegenerative diseases (NDs). First, the drug-like properties and pharmaco...
PMC10610003
core_pubmed_pmc
Clinical Relevance of Drug Interactions in People Living with Human Immunodeficiency Virus on Antiretroviral Therapy—Update 2022: Systematic Review
Clinical Relevance of Drug Interactions in People Living with Human Immunodeficiency Virus on Antiretroviral Therapy—Update 2022: Systematic Review Abstract Abstract Background: The clinical outcomes of antiretroviral drugs may be modified through drug interactions; thus, it is important to update the drug interactions...
PMC10568562
core_pubmed_pmc
Results from three phase 1 trials of NNC9204-1177, a glucagon/GLP-1 receptor co-agonist: Effects on weight loss and safety in adults with overweight or obesity
Results from three phase 1 trials of NNC9204-1177, a glucagon/GLP-1 receptor co-agonist: Effects on weight loss and safety in adults with overweight or obesity Abstract Objective Glucagon/glucagon-like peptide-1 (GLP-1) receptor co-agonists may provide greater weight loss than agonists targeting the GLP-1 receptor alon...
PMC5054300
core_pubmed_pmc
Comparison of intravenous and subcutaneous exposure supporting dose selection of subcutaneous belimumab systemic lupus erythematosus Phase 3 program
Comparison of intravenous and subcutaneous exposure supporting dose selection of subcutaneous belimumab systemic lupus erythematosus Phase 3 program Abstract Background Belimumab is a recombinant, human, IgG1λ monoclonal antibody that targets B-lymphocyte stimulator. The intravenous formulation is indicated for the tre...
PMC12777504
core_pubmed_pmc
Diagnosis and management of invasive candidiasis in critically ill patients: SIAARTI multidisciplinary statement
Diagnosis and management of invasive candidiasis in critically ill patients: SIAARTI multidisciplinary statement Abstract Abstract Critically ill patients in Intensive Care Units are at high risk of developing invasive candidiasis (IC). Delay in diagnosis and suboptimal management contribute to high mortality rates, hi...
PMC8213421
core_pubmed_pmc
PBPK modeling to predict drug‐drug interactions of ivosidenib as a perpetrator in cancer patients and qualification of the Simcyp platform for CYP3A4 induction
PBPK modeling to predict drug‐drug interactions of ivosidenib as a perpetrator in cancer patients and qualification of the Simcyp platform for CYP3A4 induction Abstract Abstract Ivosidenib is a potent, targeted, orally active, small‐molecule inhibitor of mutant isocitrate dehydrogenase 1 (IDH1) that has been approved i...
PMC10107467
core_pubmed_pmc
Justification of empiric methodology to determine dexmedetomidine dose for the TREX study
Justification of empiric methodology to determine dexmedetomidine dose for the TREX study Abstract Abstract Introduction Dexmedetomidine is the sedative agent administered in combination with remifentanil and low dose of sevoflurane in the interventional arm of the ongoing TREX trial ( T rial R emifentanil DE xmedetomi...
PMC6852105
core_pubmed_pmc
Pharmacokinetics of Risankizumab in Asian Healthy Subjects and Patients With Moderate to Severe Plaque Psoriasis, Generalized Pustular Psoriasis, and Erythrodermic Psoriasis
Pharmacokinetics of Risankizumab in Asian Healthy Subjects and Patients With Moderate to Severe Plaque Psoriasis, Generalized Pustular Psoriasis, and Erythrodermic Psoriasis Abstract Abstract Risankizumab, a humanized monoclonal antibody that targets interleukin‐23 p19 subunit, was developed for the treatment of psoria...
PMC10779115
core_pubmed_pmc
Statins—From Fungi to Pharmacy
Statins—From Fungi to Pharmacy Abstract Statins have been used in the treatment of hyperlipidemia, both as monotherapy and in combination therapy. Natural fermentation processes of fungi such as Monascus spp., Penicillium spp., Aspergillus terreus , and Pleurotus ostreatus have given rise to natural statins. Compactin ...
PMC10455820
core_pubmed_pmc
Management of Coronary Artery Disease in Older Adults: Recent Advances and Gaps in Evidence
Management of Coronary Artery Disease in Older Adults: Recent Advances and Gaps in Evidence Abstract Coronary artery disease (CAD) is highly prevalent in older adults, yet its management remains challenging. Treatment choices are made complex by the frailty burden of older patients, a high prevalence of comorbidities a...
PMC8954798
core_pubmed_pmc
A Microphysiological Cell-Culturing System for Pharmacokinetic Drug Exposure and High-Resolution Imaging of Arrays of 3D Microtissues
A Microphysiological Cell-Culturing System for Pharmacokinetic Drug Exposure and High-Resolution Imaging of Arrays of 3D Microtissues Abstract Abstract Understanding the pharmacokinetic/pharmacodynamic (PK/PD)-relationship of a drug candidate is key to determine effective, yet safe treatment regimens for patients. Howe...
PMC9617324
core_pubmed_pmc
Safety, pharmacokinetics and efficacy of SCT200, an anti-EGFR monoclonal antibody in patients with wild-type KRAS/NRAS/BRAF metastatic colorectal cancer: a phase I dose-escalation and dose-expansion study
Safety, pharmacokinetics and efficacy of SCT200, an anti-EGFR monoclonal antibody in patients with wild-type KRAS/NRAS/BRAF metastatic colorectal cancer: a phase I dose-escalation and dose-expansion study Abstract Abstract Background An over-expression of the epidermal growth factor receptor (EGFR) has been observed in...
PMC9069442
core_pubmed_pmc
Anti-inflammatory activity of nicotine isolated from Brassica oleracea in rheumatoid arthritis
Anti-inflammatory activity of nicotine isolated from Brassica oleracea in rheumatoid arthritis Abstract Abstract Objectives: Rheumatoid arthritis (RA) is an autoimmune disease, associated with chronic inflammation of synoviocytes. Tumor necrosis factor α (TNF-α) plays a crucial role in the pathogenesis of RA through pr...
PMC11390765
core_pubmed_pmc
Pharmacokinetic study of capivasertib and the CYP3A4 substrate midazolam in patients with advanced solid tumors
Pharmacokinetic study of capivasertib and the CYP3A4 substrate midazolam in patients with advanced solid tumors Abstract Abstract Purpose Capivasertib, a potent, selective inhibitor of all three AKT serine/threonine kinase (AKT) isoforms, is being evaluated in phase 3 trials in advanced breast and prostate cancer. This...
PMC9804438
core_pubmed_pmc
Organic Anion Transporter Gene Variants Associated With Plasma Exposure and Long‐Term Response to Atrasentan in Patients With Diabetic Kidney Disease
Organic Anion Transporter Gene Variants Associated With Plasma Exposure and Long‐Term Response to Atrasentan in Patients With Diabetic Kidney Disease Abstract Abstract Plasma exposure of the endothelin receptor antagonist atrasentan varies between individuals and is associated with nephroprotective effects and the risk...
PMC11963608
core_pubmed_pmc
Pharmacokinetics, tolerability, and safety of TBI-223, a novel oxazolidinone, in healthy participants
Pharmacokinetics, tolerability, and safety of TBI-223, a novel oxazolidinone, in healthy participants Abstract ABSTRACT TBI-223 is an oxazolidinone antibiotic under clinical development for the treatment of tuberculosis. Preclinical data indicate potent antituberculosis activity and a potentially improved safety profil...
PMC4431469
core_pubmed_pmc
Profile of PEGylated interferon beta in the treatment of relapsing-remitting multiple sclerosis
Profile of PEGylated interferon beta in the treatment of relapsing-remitting multiple sclerosis Abstract Several treatments are currently available for relapsing-remitting multiple sclerosis. Among them, interferon (IFN) beta remains a valid treatment approach because of its good benefit/risk profile. Due to the need f...
PMC4599717
core_pubmed_pmc
Physiologically based pharmacokinetic modeling of zinc oxide nanoparticles and zinc nitrate in mice
Physiologically based pharmacokinetic modeling of zinc oxide nanoparticles and zinc nitrate in mice Abstract Abstract Zinc oxide nanoparticles (ZnO NPs) have been widely used in consumer products, therapeutic agents, and drug delivery systems. However, the fate and behavior of ZnO NPs in living organisms are not well d...
PMC9785202
core_pubmed_pmc
Changes in Disposition of Ezetimibe and Its Active Metabolites Induced by Impaired Hepatic Function: The Influence of Enzyme and Transporter Activities
Changes in Disposition of Ezetimibe and Its Active Metabolites Induced by Impaired Hepatic Function: The Influence of Enzyme and Transporter Activities Abstract Ezetimibe (EZE) is a selective cholesterol absorption inhibitor. Hepatic impairment significantly increases the systemic exposure of EZE and its main active ph...
PMC3910017
core_pubmed_pmc
The Pharmacokinetics and Pharmacokinetic/Pharmacodynamic Relationships of Evacetrapib Administered as Monotherapy or in Combination With Statins
The Pharmacokinetics and Pharmacokinetic/Pharmacodynamic Relationships of Evacetrapib Administered as Monotherapy or in Combination With Statins Abstract Abstract Evacetrapib is a novel cholesteryl ester transfer protein (CETP) inhibitor currently being evaluated in a late-stage cardiovascular outcome trial. Using popu...
PMC6017666
core_pubmed_pmc
Optimization of the Preparation Conditions of Borneol-Modified Ginkgolide Liposomes by Response Surface Methodology and Study of Their Blood Brain Barrier Permeability
Optimization of the Preparation Conditions of Borneol-Modified Ginkgolide Liposomes by Response Surface Methodology and Study of Their Blood Brain Barrier Permeability Abstract Abstract Ginkgolides (GG), containing ginkgolide A (GA), ginkgolide B (GB) and ginkgolide C (GC), are mainly prescribed for ischemic stroke and...
PMC9732110
core_pubmed_pmc
An intravenous anesthetic drug-propofol, influences the biological characteristics of malignant tumors and reshapes the tumor microenvironment: A narrative literature review
An intravenous anesthetic drug-propofol, influences the biological characteristics of malignant tumors and reshapes the tumor microenvironment: A narrative literature review Abstract Abstract Malignant tumors are the second leading cause of death worldwide. This is a public health concern that negatively impacts human ...
PMC12613722
core_pubmed_pmc
3D printing of acetaminophen suppository and its quality and pharmacokinetic evaluation
3D printing of acetaminophen suppository and its quality and pharmacokinetic evaluation Abstract Abstract Introduction Acetaminophen is a widely used antipyretic and analgesic treatment. Becuase oral administration poses a risk of acute liver failure, researchers are exploring alternative routes of administration using...
PMC11050816
core_pubmed_pmc
Pharmacokinetics and Safety of Lurbinectedin Administrated with Itraconazole in Cancer Patients: A Drug–Drug Interaction Study
Pharmacokinetics and Safety of Lurbinectedin Administrated with Itraconazole in Cancer Patients: A Drug–Drug Interaction Study Abstract This open-label, two-part, phase Ib drug–drug interaction study investigated whether the pharmacokinetic (PK) and safety profiles of lurbinectedin (LRB), a marine-derived drug, are aff...
PMC5744177
core_pubmed_pmc
Dose/Exposure‐Response Modeling to Support Dosing Recommendation for Phase III Development of Baricitinib in Patients with Rheumatoid Arthritis
Dose/Exposure‐Response Modeling to Support Dosing Recommendation for Phase III Development of Baricitinib in Patients with Rheumatoid Arthritis Abstract Baricitinib is an oral inhibitor of Janus kinases (JAKs), selective for JAK1 and 2. It demonstrated dose‐dependent efficacy in patients with moderate‐to‐severe rheumat...
PMC9381915
core_pubmed_pmc
Development of and insights from systems pharmacology models of antibody‐drug conjugates
Development of and insights from systems pharmacology models of antibody‐drug conjugates Abstract Abstract Antibody‐drug conjugates (ADCs) have gained traction in the oncology space in the past few decades, with significant progress being made in recent years. Although the use of pharmacometric modeling is well‐establi...
PMC5351319
core_pubmed_pmc
Toward Optimum Benefit‐Risk and Reduced Access Lag For Cancer Drugs in Asia: A Global Development Framework Guided by Clinical Pharmacology Principles
Toward Optimum Benefit‐Risk and Reduced Access Lag For Cancer Drugs in Asia: A Global Development Framework Guided by Clinical Pharmacology Principles Modeling PK/PD‐INFORMED DOSE SELECTION FOR THE ASIAN REGION A quantitative clinical pharmacology assessment is critical for dose selection in Asian patients. Recent scie...
PMC8964029
core_pubmed_pmc
Ritonavir-Boosted Exposure of Kinase Inhibitors: an Open Label, Cross-over Pharmacokinetic Proof-of-Concept Trial with Erlotinib
Ritonavir-Boosted Exposure of Kinase Inhibitors: an Open Label, Cross-over Pharmacokinetic Proof-of-Concept Trial with Erlotinib Abstract Background Although kinase inhibitors (KIs) are generally effective, their use has a large impact on the current health care budget. Dosing strategies to reduce treatment costs are w...
PMC11291528
core_pubmed_pmc
Mirtazapine loaded polymeric micelles for rapid release tablet: A novel formulation—In vitro and in vivo studies
Mirtazapine loaded polymeric micelles for rapid release tablet: A novel formulation—In vitro and in vivo studies Abstract Major depression is a prevalent disorder characterized by sadness, lack of interest or pleasure, interrupted sleep or food, and impaired concentration. Mirtazapine (MTZ), a tetracyclic antidepressan...
PMC9887786
core_pubmed_pmc
In vitro co-culture systems of hepatic and intestinal cells for cellular pharmacokinetic and pharmacodynamic studies of capecitabine against colorectal cancer
In vitro co-culture systems of hepatic and intestinal cells for cellular pharmacokinetic and pharmacodynamic studies of capecitabine against colorectal cancer Abstract Background As a prodrug of 5-fluorouracil (5-FU), orally administrated capecitabine (CAP) undergoes preliminary conversion into active metabolites in th...
PMC11871483
core_pubmed_pmc
Mechanistic insights into novel cyano-pyrimidine pendant chalcone derivatives as LSD1 inhibitors by docking, ADMET, MM/GBSA, and molecular dynamics simulation
Mechanistic insights into novel cyano-pyrimidine pendant chalcone derivatives as LSD1 inhibitors by docking, ADMET, MM/GBSA, and molecular dynamics simulation Abstract Cancer presents a formidable and complex foe, standing as one of the foremost contributors to disease-related fatalities across the globe. According to ...
PMC4359180
core_pubmed_pmc
Pharmacokinetic Effects of Simultaneous Administration of Single-Dose Gabapentin 500 mg and Zolpidem Tartrate 10 mg in Healthy Volunteers: A Randomized, Open-Label, Crossover Trial
Pharmacokinetic Effects of Simultaneous Administration of Single-Dose Gabapentin 500 mg and Zolpidem Tartrate 10 mg in Healthy Volunteers: A Randomized, Open-Label, Crossover Trial Abstract Objective Gabapentin is being investigated as a potential treatment for occasional disturbed sleep. This study assessed the pharma...
PMC12968080
core_pubmed_pmc
Comparative Efficacy and Pharmacokinetic Parameters of Micronized Creatine Monohydrate (KleanCREATINE™) in Active Men: A Randomized, Controlled Clinical Study
Comparative Efficacy and Pharmacokinetic Parameters of Micronized Creatine Monohydrate (KleanCREATINE™) in Active Men: A Randomized, Controlled Clinical Study Abstract Abstract Introduction This two-phase clinical study evaluated KleanCREATINE™ (micronized creatine monohydrate) for its pharmacokinetic properties, safet...
PMC2847537
core_pubmed_pmc
Efficacy, safety and pharmacokinetic of once-daily boosted saquinavir (1500/100 mg) together with 2 nucleos(t)ide reverse transcriptase inhibitors in real life: a multicentre prospective study
Efficacy, safety and pharmacokinetic of once-daily boosted saquinavir (1500/100 mg) together with 2 nucleos(t)ide reverse transcriptase inhibitors in real life: a multicentre prospective study Abstract Abstract Background Ritonavir-boosted saquinavir (SQVr) is nowadays regarded as an alternative antiretroviral drug pro...
PMC12290195
core_pubmed_pmc
Polyherbal Formulation as a Therapeutic Strategy for Lung Cancer: Phytochemical Profiling, Molecular Docking, and Pharmacological Evaluation
Polyherbal Formulation as a Therapeutic Strategy for Lung Cancer: Phytochemical Profiling, Molecular Docking, and Pharmacological Evaluation Abstract Globally, lung cancer continues to be the primary cause of both cancer incidence and death. The disease is multifaceted, influenced by numerous external factors and the i...
PMC10706748
core_pubmed_pmc
No Interference of H9 Extract on Trastuzumab Pharmacokinetics in Their Combinations
No Interference of H9 Extract on Trastuzumab Pharmacokinetics in Their Combinations Abstract Trastuzumab is used to treat breast cancer patients overexpressing human epidermal growth factor receptor 2, but resistance and toxicity limit its uses, leading to attention to trastuzumab combinations. Recently, the synergisti...
PMC7762810
core_pubmed_pmc
Brigatinib Dose Rationale in Anaplastic Lymphoma Kinase–Positive Non‐Small Cell Lung Cancer: Exposure–Response Analyses of Pivotal ALTA Study
Brigatinib Dose Rationale in Anaplastic Lymphoma Kinase–Positive Non‐Small Cell Lung Cancer: Exposure–Response Analyses of Pivotal ALTA Study Abstract Abstract Brigatinib is a kinase inhibitor indicated for patients with advanced anaplastic lymphoma kinase–positive non‐small cell lung cancer who progressed on or are in...
PMC4056810
core_pubmed_pmc
Pharmacokinetics, hemodynamic and metabolic effects of epinephrine to prevent post-operative low cardiac output syndrome in children
Pharmacokinetics, hemodynamic and metabolic effects of epinephrine to prevent post-operative low cardiac output syndrome in children Abstract Abstract Introduction The response to exogenous epinephrine (Ep) is difficult to predict given the multitude of factors involved such as broad pharmacokinetic and pharmacodynamic...
PMC9704389
core_pubmed_pmc
Non-human primates in the PKPD evaluation of biologics: Needs and options to reduce, refine, and replace. A BioSafe White Paper
Non-human primates in the PKPD evaluation of biologics: Needs and options to reduce, refine, and replace. A BioSafe White Paper Abstract ABSTRACT Monoclonal antibodies (mAbs) deliver great benefits to patients with chronic and/or severe diseases thanks to their strong specificity to the therapeutic target. As a result ...
PMC11988199
core_pubmed_pmc
Polyallylamine Hydrochloride-Modified Bovine Serum Albumin Nanoparticles Loaded with α-Solanine for Chemotherapy of Pancreatic Cancer
Polyallylamine Hydrochloride-Modified Bovine Serum Albumin Nanoparticles Loaded with α-Solanine for Chemotherapy of Pancreatic Cancer Abstract Abstract Introduction α-Solanine (α-Sol) shows promise for pancreatic cancer (PC) treatment by inhibiting PC cell proliferation, migration, and invasion. However, its clinical a...
PMC7600697
core_pubmed_pmc
Omics-Based Platforms: Current Status and Potential Use for Cholangiocarcinoma
Omics-Based Platforms: Current Status and Potential Use for Cholangiocarcinoma Abstract Abstract Cholangiocarcinoma (CCA) has been identified as a highly malignant cancer that can be transformed from epithelial cells of the bile duct, including intrahepatic, perihilar and extrahepatic. High-resolution imaging tools (ab...
PMC5823072
core_pubmed_pmc
Pharmacokinetics and tolerability of eletriptan hydrobromide in healthy Korean subjects
Pharmacokinetics and tolerability of eletriptan hydrobromide in healthy Korean subjects Abstract Background Migraine is one of the most common headache disorders that greatly affect the quality of life. Selective serotonin (5-HT) receptor agonists such as triptamine-based drugs called triptans are used for treatment of...
PMC9816378
core_pubmed_pmc
Guidance for the treatment of adult growth hormone deficiency with somapacitan, a long-acting growth hormone preparation
Guidance for the treatment of adult growth hormone deficiency with somapacitan, a long-acting growth hormone preparation Abstract Adult growth hormone deficiency (AGHD) is a rare endocrine disorder characterized by an abnormal body composition, metabolic abnormalities associated with increased cardiovascular diseases, ...
PMC8305117
core_pubmed_pmc
LP1 and LP2: Dual-Target MOPr/DOPr Ligands as Drug Candidates for Persistent Pain Relief
LP1 and LP2: Dual-Target MOPr/DOPr Ligands as Drug Candidates for Persistent Pain Relief Abstract Abstract Although persistent pain is estimated to affect about 20% of the adult population, current treatments have poor results. Polypharmacology, which is the administration of more than one drug targeting on two or more...
PMC3740141
core_pubmed_pmc
Rapid quantitative pharmacodynamic imaging by a novel method: theory, simulation testing and proof of principle
Rapid quantitative pharmacodynamic imaging by a novel method: theory, simulation testing and proof of principle Abstract Abstract Pharmacological challenge imaging has mapped, but rarely quantified, the sensitivity of a biological system to a given drug. We describe a novel method called rapid quantitative pharmacodyna...
PMC12923478
core_pubmed_pmc
A randomized, phase Ib trial of recombinant human serum albumin in cirrhotic patients with ascites
A randomized, phase Ib trial of recombinant human serum albumin in cirrhotic patients with ascites Abstract Abstract Background Recombinant human serum albumin (rHA) is a promising alternative to human serum albumin (HSA) for managing ascites in cirrhotic patients. This phase Ib study aims to assess the safety, tolerab...
PMC6283789
core_pubmed_pmc
Phase 1 Parkinson’s Disease Studies Show the Dopamine D1/D5 Agonist PF-06649751 is Safe and Well Tolerated
Phase 1 Parkinson’s Disease Studies Show the Dopamine D1/D5 Agonist PF-06649751 is Safe and Well Tolerated Abstract Introduction There is a need for new therapies in Parkinson’s disease that may help to address known limitations of current options. PF-06649751 is a novel, highly selective dopamine D1/D5 agonist targete...
PMC9925696
core_pubmed_pmc
The first-in-human phase I study of a brain-penetrant mutant IDH1 inhibitor DS-1001 in patients with recurrent or progressive IDH1-mutant gliomas
The first-in-human phase I study of a brain-penetrant mutant IDH1 inhibitor DS-1001 in patients with recurrent or progressive IDH1-mutant gliomas Abstract Abstract Background Approximately 70% of lower-grade gliomas harbor isocitrate dehydrogenase 1 (IDH1) mutations, resulting in the accumulation of oncometabolite D-2-...
PMC12824232
core_pubmed_pmc
ER degradation for ER + /HER2– advanced or metastatic breast cancer: a phase 1 trial
ER degradation for ER + /HER2– advanced or metastatic breast cancer: a phase 1 trial Abstract AC699 is a novel, orally bioavailable chimeric estrogen receptor-α (ERα) degrader that induces proteasome-dependent ERα degradation via cereblon E3 ligase recruitment. Here we report findings from a first-in-human, phase 1, do...
PMC4297374
core_pubmed_pmc
Pharmacokinetics of chewed vs. swallowed raltegravir in a patient with AIDS and MAI infection: some new conflicting data
Pharmacokinetics of chewed vs. swallowed raltegravir in a patient with AIDS and MAI infection: some new conflicting data Abstract Abstract Background While HIV, AIDS and atypical Mycobacterium infections are closely linked, the use of Integrase-Inhibitor based cART, notably raltegravir-based regimens is more widespread...
PMC12960388
core_pubmed_pmc
Pharmacokinetics and Safety of a Single Dose of Brensocatib in Participants with Hepatic Impairment and Matched Participants with Normal Hepatic Functions
Pharmacokinetics and Safety of a Single Dose of Brensocatib in Participants with Hepatic Impairment and Matched Participants with Normal Hepatic Functions Abstract Abstract Aim Brensocatib is an oral, competitive, and reversible dipeptidyl peptidase 1 (DPP1) inhibitor in development for the treatment of neutrophil-medi...
PMC10053770
core_pubmed_pmc
Assessment of the Pharmacokinetics, Disposition, and Duration of Action of the Tumour-Targeting Peptide CEND-1
Assessment of the Pharmacokinetics, Disposition, and Duration of Action of the Tumour-Targeting Peptide CEND-1 Abstract CEND-1 (iRGD) is a bifunctional cyclic peptide that can modulate the solid tumour microenvironment, enhancing the delivery and therapeutic index of co-administered anti-cancer agents. This study explo...
PMC5632828
core_pubmed_pmc
A randomised, double-blind clinical phase II trial of the efficacy, safety, tolerability and pharmacokinetics of a single dose combination treatment with artefenomel and piperaquine in adults and children with uncomplicated Plasmodium falciparum malaria
A randomised, double-blind clinical phase II trial of the efficacy, safety, tolerability and pharmacokinetics of a single dose combination treatment with artefenomel and piperaquine in adults and children with uncomplicated Plasmodium falciparum malaria Abstract Abstract Background The clinical development of a single ...
PMC6958537
core_pubmed_pmc
Setting Our Sights on Infectious Diseases
Setting Our Sights on Infectious Diseases Abstract Abstract In May 2019, the Wellcome Centre for Anti-Infectives Research ( W CAIR) at the University of Dundee, UK, held an international conference with the aim of discussing some key questions around discovering new medicines for infectious diseases and a particular fo...
PMC7061854
core_pubmed_pmc
Population Pharmacokinetics of Caspofungin and Dosing Optimization in Children With Allogeneic Hematopoietic Stem Cell Transplantation
Population Pharmacokinetics of Caspofungin and Dosing Optimization in Children With Allogeneic Hematopoietic Stem Cell Transplantation Abstract Abstract Caspofungin is the first echinocandin antifungal agent that licented for pediatric use in invasive candidiasis and aspergillosis. In this study, we evaluated the popul...
PMC5836969
core_pubmed_pmc
Optimal prandial timing of bolus insulin in diabetes management: a review
Optimal prandial timing of bolus insulin in diabetes management: a review Abstract Abstract The inability to achieve optimal diabetes glucose control in people with diabetes is multifactorial, but one contributor may be inadequate control of postprandial glucose. In patients treated with multiple daily injections of in...
PMC7541232
core_pubmed_pmc
Prolonged versus intermittent β-lactam antibiotics intravenous infusion strategy in sepsis or septic shock patients: a systematic review with meta-analysis and trial sequential analysis of randomized trials
Prolonged versus intermittent β-lactam antibiotics intravenous infusion strategy in sepsis or septic shock patients: a systematic review with meta-analysis and trial sequential analysis of randomized trials Abstract Background The prolonged β-lactam infusion strategy has emerged as the standard treatment for sepsis or ...
PMC6166767
core_pubmed_pmc
Integrated pharmacokinetic–pharmacodynamic modeling to evaluate empiric carbapenem therapy in bloodstream infections
Integrated pharmacokinetic–pharmacodynamic modeling to evaluate empiric carbapenem therapy in bloodstream infections Abstract Objectives Treatment for nosocomial bloodstream infections (BSI) caused by multidrug-resistant (MDR) Gram-negative bacteria (GNB) is challenging. Rising antimicrobial resistance, especially in e...
PMC10852043
core_pubmed_pmc
Influence of Intravenous S-Ketamine on the Pharmacokinetics of Oral Morphine in Healthy Volunteers
Influence of Intravenous S-Ketamine on the Pharmacokinetics of Oral Morphine in Healthy Volunteers Abstract Abstract BACKGROUND: Subanesthetic ketamine may reduce perioperative consumption of opioids. We studied whether intravenous S-ketamine alters the pharmacokinetics of oral morphine in healthy volunteers. METHODS: ...
PMC12664287
core_pubmed_pmc
Antiproliferative Potential of Linagliptin-Rivaroxaban Mixture in Cervical Cancer: Mechanistic Insights into Targeting Mutant MAPK, RAS kinase Signal Protein
Antiproliferative Potential of Linagliptin-Rivaroxaban Mixture in Cervical Cancer: Mechanistic Insights into Targeting Mutant MAPK, RAS kinase Signal Protein Abstract Background: Repositioning existing marketed drugs represents a viable strategy for identifying new anticancer agents. This study employed an approach tha...
PMC8245385
core_pubmed_pmc
A Phase 1 Study to Evaluate the Drug Interaction Between Islatravir (MK-8591) and Doravirine in Adults Without HIV
A Phase 1 Study to Evaluate the Drug Interaction Between Islatravir (MK-8591) and Doravirine in Adults Without HIV Abstract Background and Objectives Islatravir (MK-8591) is a novel nucleoside analogue in development for the treatment and prevention of HIV-1 infection. Doravirine is a non-nucleoside reverse transcripta...
PMC9414910
core_pubmed_pmc
Optimized 68 Ga-Labeled Urea-Based PSMA-Targeted PET Tracers for Prostate Cancer
Optimized 68 Ga-Labeled Urea-Based PSMA-Targeted PET Tracers for Prostate Cancer Abstract Prostate-specific membrane antigen (PSMA)-targeting radiopharmaceuticals have become some of the most promising tools for the diagnosis and therapy prostate cancer (PCa). The structure of existing PSMA-targeted PET tracers still n...
PMC5482694
core_pubmed_pmc
Phase I study of QLNC120, a novel EGFR and HER2 kinase inhibitor, in pre-treated patients with HER2-overexpressing advanced breast cancer
Phase I study of QLNC120, a novel EGFR and HER2 kinase inhibitor, in pre-treated patients with HER2-overexpressing advanced breast cancer Abstract Abstract This study evaluated the dose-limiting toxicities (DLT), maximum tolerated dose (MTD), pharmacokinetic profile, and preliminary antitumor activity of QLNC120, an in...
PMC12957122
core_pubmed_pmc
Bioactive flavonoids from Anacardium occidentale as promising natural inhibitors of Cryptococcus neoformans : a computational perspective on secondary metabolites against critical fungal pathogens
Bioactive flavonoids from Anacardium occidentale as promising natural inhibitors of Cryptococcus neoformans : a computational perspective on secondary metabolites against critical fungal pathogens Abstract The investigation of bioactive phytochemicals from Anacardium occidentale (cashew) nut has attracted increasing in...