2,919 results match your criteria Clinical pharmacokinetics[Journal]


Optimal Sampling Strategies for Therapeutic Drug Monitoring of First-Line Tuberculosis Drugs in Patients with Tuberculosis.

Clin Pharmacokinet 2019 Apr 17. Epub 2019 Apr 17.

Department of Clinical Pharmacy and Pharmacology, University Medical Center Groningen, University of Groningen, PO Box 30.001, 9700 RB, Groningen, The Netherlands.

Background: The 24-h area under the concentration-time curve (AUC)/minimal inhibitory concentration ratio is the best predictive pharmacokinetic/pharmacodynamic (PK/PD) parameter of the efficacy of first-line anti-tuberculosis (TB) drugs. An optimal sampling strategy (OSS) is useful for accurately estimating AUC; however, OSS has not been developed in the fed state or in the early phase of treatment for first-line anti-TB drugs.

Methods: An OSS for the prediction of AUC of isoniazid, rifampicin, ethambutol and pyrazinamide was developed for TB patients starting treatment. Read More

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http://dx.doi.org/10.1007/s40262-019-00763-3DOI Listing

Population Pharmacokinetics/Pharmacodynamics of Ticagrelor in Children with Sickle Cell Disease.

Clin Pharmacokinet 2019 Apr 11. Epub 2019 Apr 11.

Quantitative Clinical Pharmacology, Early Clinical Development, IMED Biotech Unit, AstraZeneca, Gothenburg, Sweden.

Background And Objective: Ticagrelor, a reversible P2Y platelet inhibitor, is under investigation as a sickle cell disease (SCD) therapy in children. HESTIA1 (NCT02214121) was the first ticagrelor study generating pharmacokinetic (PK), pharmacodynamic (PD, P2Y reactivity units [PRU]), and safety data in 45 pediatric SCD patients. Population PK and PK/PD relationships for ticagrelor were quantified using a PK approach. Read More

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http://dx.doi.org/10.1007/s40262-019-00758-0DOI Listing
April 2019
7 Reads

Optimizing Estimated Glomerular Filtration Rate to Support Adult to Pediatric Pharmacokinetic Bridging Studies in Patients with Cystic Fibrosis.

Clin Pharmacokinet 2019 Apr 10. Epub 2019 Apr 10.

Department of Clinical Pharmacy, College of Pharmacy, University of Michigan, 428 Church Street, Ann Arbor, MI, 48109, USA.

Background: The estimated glomerular filtration rate (eGFR) is often used to model drug clearance (CL) and scale doses across age and body size. Over their lifetime, patients with cystic fibrosis (CF) receive repeated courses of tobramycin, an antibiotic with eGFR-dependent CL, for the treatment of pulmonary exacerbations. Tobramycin population pharmacokinetic (PK) modeling can be used to decipher the best approach to define eGFR for pediatric bridging studies. Read More

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http://dx.doi.org/10.1007/s40262-019-00761-5DOI Listing
April 2019
1 Read

Physicochemical Properties, Biotransformation, and Transport Pathways of Established and Newly Approved Medications: A Systematic Review of the Top 200 Most Prescribed Drugs vs. the FDA-Approved Drugs Between 2005 and 2016.

Clin Pharmacokinet 2019 Apr 10. Epub 2019 Apr 10.

Clinical Pharmacokinetics Research Laboratory, Department of Biomedical and Pharmaceutical Sciences, College of Pharmacy, University of Rhode Island, Office 495 A, 7 Greenhouse Road, Kingston, RI, 02881, USA.

Background: Enzyme-mediated biotransformation of pharmacological agents is a crucial step in xenobiotic detoxification and drug disposition. Herein, we investigated the metabolism and physicochemical properties of the top 200 most prescribed drugs (established) as well as drugs approved by the US Food and Drug Administration (FDA) between 2005 and 2016 (newly approved).

Objective: Our objective was to capture the changing trends in the routes of administration, physicochemical properties, and prodrug medications, as well as the contributions of drug-metabolizing enzymes and transporters to drug clearance. Read More

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http://dx.doi.org/10.1007/s40262-019-00750-8DOI Listing
April 2019
1 Read

Assessment of Drug-Drug Interactions between Taspoglutide, a Glucagon-Like Peptide-1 Agonist, and Drugs Commonly Used in Type 2 Diabetes Mellitus: Results of Five Phase I Trials.

Clin Pharmacokinet 2019 Apr 9. Epub 2019 Apr 9.

Department of Clinical Pharmacology, Roche Pharmaceutical Research and Early Development, Roche Innovation Center Basel, F. Hoffmann-La Roche AG, Grenzacherstrasse 124, Basel, CH-4070, Switzerland.

Background And Objective: Taspoglutide, a glucagon-like peptide-1 agonist, like native glucagon-like peptide-1, delays gastric emptying time and prolongs intestinal transit time, which may alter the pharmacokinetics of concomitantly administered oral drugs. The effect of taspoglutide on the pharmacokinetics of five oral drugs commonly used in patients with type 2 diabetes mellitus was assessed in healthy subjects.

Methods: Five clinical pharmacology studies evaluated the potential drug-drug interaction between multiple subcutaneous taspoglutide doses and a single dose of lisinopril, warfarin, and simvastatin and multiple doses of digoxin and an oral contraceptive containing ethinylestradiol and levonorgestrel. Read More

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http://dx.doi.org/10.1007/s40262-019-00757-1DOI Listing

Population Pharmacokinetic and Pharmacodynamic Analysis of GLPG1690, an Autotaxin Inhibitor, in Healthy Volunteers and Patients with Idiopathic Pulmonary Fibrosis.

Clin Pharmacokinet 2019 Apr 6. Epub 2019 Apr 6.

Galapagos SASU, 102 avenue Gaston Roussel, 93230, Romainville, France.

Background And Objectives: GLPG1690 is an autotaxin inhibitor in development for the treatment of idiopathic pulmonary fibrosis. Several publications suggested a role of autotaxin in the control of disease-affected lung function and of lysophosphatidic acid in lung remodeling processes. The aim of the current article was to describe the exposure-response relationship of GLPG1690 and further develop a rational basis to support dose selection for clinical trials in patients with idiopathic pulmonary fibrosis. Read More

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http://link.springer.com/10.1007/s40262-019-00755-3
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http://dx.doi.org/10.1007/s40262-019-00755-3DOI Listing
April 2019
4 Reads

Pharmacokinetics of the BCL-2 Inhibitor Venetoclax in Subjects with Hepatic Impairment.

Clin Pharmacokinet 2019 Apr 5. Epub 2019 Apr 5.

AbbVie Inc., 1 North Waukegan Road, North Chicago, IL, 60064, USA.

Introduction: Venetoclax is a selective B cell lymphoma-2 inhibitor. It is approved for treatment of chronic lymphocytic leukemia and is being investigated for other hematological malignancies. Venetoclax is predominantly eliminated by the liver; therefore, there is a need to investigate the effect of hepatic insufficiency on venetoclax pharmacokinetics. Read More

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http://dx.doi.org/10.1007/s40262-019-00746-4DOI Listing
April 2019
4 Reads

Levothyrox New and Old Formulations: Are they Switchable for Millions of Patients?

Clin Pharmacokinet 2019 Apr 4. Epub 2019 Apr 4.

INTHERES, Université de Toulouse, INRA, ENVT, Toulouse, France.

In France, more than 2.5 million patients are currently treated with levothyroxine, mainly as the marketed product Levothyrox. In March 2017, at the request of French authorities, a new formulation of Levothyrox was licensed, with the objective of avoiding stability deficiencies of the old formulation. Read More

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http://dx.doi.org/10.1007/s40262-019-00747-3DOI Listing
April 2019
2 Reads

Effect of Oral Semaglutide on the Pharmacokinetics of Lisinopril, Warfarin, Digoxin, and Metformin in Healthy Subjects.

Clin Pharmacokinet 2019 Apr 4. Epub 2019 Apr 4.

Novo Nordisk A/S, Vandtårnsvej 108-110, 2860, Søborg, Denmark.

Background: Oral semaglutide is a tablet co-formulation of the human glucagon-like peptide-1 (GLP-1) analog semaglutide with the absorption enhancer sodium N-(8-[2-hydroxybenzoyl] amino) caprylate (SNAC). The absorption of coadministered oral drugs may be altered due to enhancement by SNAC, potential gastric emptying delay by semaglutide, or other mechanisms. Two one-sequence crossover trials investigated the effect of oral semaglutide on the pharmacokinetics of lisinopril, warfarin, digoxin, and metformin. Read More

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http://dx.doi.org/10.1007/s40262-019-00756-2DOI Listing
April 2019
2 Reads

Assessment of Antiepileptic Drug Concentrations in HIV-Infected versus HIV-Negative Patients: A Retrospective Analysis.

Clin Pharmacokinet 2019 Apr 4. Epub 2019 Apr 4.

Gestione Ambulatoriale Politerapie (GAP) Outpatient Clinic, ASST Fatebenefratelli Sacco, Milan, Italy.

Introduction: A higher rate of subtherapeutic psychotropic drug concentrations was recently found in HIV-infected versus HIV-negative patients. In this study, we sought to investigate if this trend could also apply to antiepileptic drugs.

Methods: Overall, 700 HIV-infected patients were screened during the first 2 years after the introduction of our outpatient polytherapy management service (Gestione Ambulatoriale Politerapie [GAP]) in the search for subjects with antiepileptic drug trough concentration assessments. Read More

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http://link.springer.com/10.1007/s40262-019-00752-6
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http://dx.doi.org/10.1007/s40262-019-00752-6DOI Listing
April 2019
2 Reads

Population Pharmacokinetics of Upadacitinib Using the Immediate-Release and Extended-Release Formulations in Healthy Subjects and Subjects with Rheumatoid Arthritis: Analyses of Phase I-III Clinical Trials.

Clin Pharmacokinet 2019 Apr 3. Epub 2019 Apr 3.

Clinical Pharmacology and Pharmacometrics, AbbVie Inc, 1 North Waukegan Road, Bldg. AP31-3, North Chicago, IL, 60064, USA.

Background And Objectives: Upadacitinib is a selective Janus kinase (JAK) 1 inhibitor being developed as an orally administered treatment for patients with moderate to severe rheumatoid arthritis (RA) and other autoimmune disorders. These analyses characterized the population pharmacokinetics of upadacitinib across phase I-III clinical trials using data for immediate-release (IR) and extended-release (ER) formulations.

Methods: Pharmacokinetic data from 4170 subjects taking IR doses of 1-48 mg and ER doses of 7. Read More

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http://dx.doi.org/10.1007/s40262-019-00739-3DOI Listing
April 2019
1 Read

Population-Pharmacokinetic Modeling of Tildrakizumab (MK-3222), an Anti-Interleukin-23-p19 Monoclonal Antibody, in Healthy Volunteers and Subjects with Psoriasis.

Clin Pharmacokinet 2019 Mar 26. Epub 2019 Mar 26.

Certara USA, Inc., Princeton, NJ, USA.

Background: Tildrakizumab is an anti-interleukin-23p19 monoclonal antibody recently approved for the treatment of chronic plaque psoriasis.

Methods: This analysis characterizes the population pharmacokinetics of subcutaneous tildrakizumab and identifies covariates influencing exposure in 2098 healthy volunteers and subjects with psoriasis. Tested covariates included body weight, formulation type, sex, age, race, serum albumin, creatinine clearance, Japanese origin, prior treatment with a biologic agent, subject status (subjects with psoriasis vs. Read More

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http://link.springer.com/10.1007/s40262-019-00743-7
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http://dx.doi.org/10.1007/s40262-019-00743-7DOI Listing
March 2019
7 Reads

Pharmacokinetics and Safety of Olaparib in Patients with Advanced Solid Tumours and Renal Impairment.

Clin Pharmacokinet 2019 Mar 16. Epub 2019 Mar 16.

Hôpital Saint André, Bordeaux University Hospital, Bordeaux, France.

Background: Olaparib, a potent oral poly(ADP-ribose) polymerase inhibitor, is partially renally cleared. We investigated the pharmacokinetics and safety of olaparib in patients with mild or moderate renal impairment to provide dosing recommendations.

Methods: This phase I open-label study assessed the pharmacokinetics, safety and tolerability of single-dose, oral 300-mg olaparib tablets in adults (aged 18-75 years) with solid tumours. Read More

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http://dx.doi.org/10.1007/s40262-019-00754-4DOI Listing

Clinical Pharmacokinetic and Pharmacodynamic Considerations in the (Modern) Treatment of Melanoma.

Clin Pharmacokinet 2019 Mar 13. Epub 2019 Mar 13.

School of Pharmacy and Medical Sciences, University of South Australia, Adelaide, SA, Australia.

Targeted therapies, based on identification of common oncogenic mutations such as BRAF V600E/K and monoclonal antibody immunotherapies, have transformed the treatment of melanoma. Dual mitogen-activated protein kinase (MAPK) pathway inhibition of BRAF V600E/K and MEK 1/2 kinases with BRAF-MEK inhibitors using dabrafenib-trametinib, vemurafenib-cobimetinib and encorafenib-binimetinib is now the standard of care for BRAF V600E/K tumours. Monoclonal antibodies, such as pembrolizumab and nivolumab, against programmed cell death protein (PD-1) on T cells, as well as ipilimumab against cytotoxic T lymphocyte antigen-4 (CTLA-4), enable restoration of suppressed T-cell antitumour response, and have also shown improved clinical benefit compared with traditional chemotherapy. Read More

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http://link.springer.com/10.1007/s40262-019-00753-5
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http://dx.doi.org/10.1007/s40262-019-00753-5DOI Listing
March 2019
9 Reads

Population Pharmacokinetic Modeling of Benralizumab in Adult and Adolescent Patients with Asthma.

Clin Pharmacokinet 2019 Mar 11. Epub 2019 Mar 11.

MedImmune LLC, One MedImmune Way, Gaithersburg, MD, 20878, USA.

Introduction: Benralizumab, an interleukin-5 receptor alpha-directed cytolytic anti-eosinophil monoclonal antibody, was recently approved as add-on maintenance treatment for patients aged 12 years and older with uncontrolled asthma with eosinophilic inflammation.

Methods: Pharmacokinetic (PK) data from nine clinical trials for patients with asthma were pooled and analyzed to further characterize the PK of benralizumab and evaluate demographic covariate effects.

Results: Population modeling results demonstrated that the PK of benralizumab were dose-proportional across a wide dosage range and were adequately described by a two-compartment model with first-order absorption from the subcutaneous dosing site and a first-order elimination pathway from the central compartment. Read More

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http://dx.doi.org/10.1007/s40262-019-00738-4DOI Listing
March 2019
5.053 Impact Factor

Revisiting the Pharmacology of Unfractionated Heparin.

Clin Pharmacokinet 2019 Mar 9. Epub 2019 Mar 9.

School of Pharmacy, University of Otago, Dunedin, New Zealand.

Unfractionated heparin (UFH) is a commonly used anticoagulant therapy for the acute treatment and prevention of thrombosis. Its short duration of action, reversibility of effect by protamine sulfate, and extensive clinical experience are some of the advantages that support its use. However, the choice of dose and dosing regimen of UFH remains challenging for several reasons. Read More

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http://dx.doi.org/10.1007/s40262-019-00751-7DOI Listing

Physiologically Based Pharmacokinetic Modeling for Trimethoprim and Sulfamethoxazole in Children.

Clin Pharmacokinet 2019 Mar 6. Epub 2019 Mar 6.

Department of Pediatrics, Duke University Medical Center, Durham, NC, USA.

Objective: The aims of this study were to (1) determine whether opportunistically collected data can be used to develop physiologically based pharmacokinetic (PBPK) models in pediatric patients; and (2) characterize age-related maturational changes in drug disposition for the renally eliminated and hepatically metabolized antibiotic trimethoprim (TMP)-sulfamethoxazole (SMX).

Methods: We developed separate population PBPK models for TMP and SMX in children after oral administration of the combined TMP-SMX product and used sparse and opportunistically collected plasma concentration samples to validate our pediatric model. We evaluated predictability of the pediatric PBPK model based on the number of observed pediatric data out of the 90% prediction interval. Read More

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http://link.springer.com/10.1007/s40262-018-00733-1
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http://dx.doi.org/10.1007/s40262-018-00733-1DOI Listing
March 2019
1 Read

Microdosed Cocktail of Three Oral Factor Xa Inhibitors to Evaluate Drug-Drug Interactions with Potential Perpetrator Drugs.

Clin Pharmacokinet 2019 Mar 4. Epub 2019 Mar 4.

Department of Clinical Pharmacology and Pharmacoepidemiology, University Hospital Heidelberg, Im Neuenheimer Feld 410, 69120, Heidelberg, Germany.

Objectives: The aim of this study was to prove the suitability of simultaneously administered microdoses of the factor Xa inhibitors (FXaIs) rivaroxaban, apixaban and edoxaban (100 µg in total). To evaluate drug-drug interactions, the impact of ketoconazole, a known strong inhibitor of cytochrome P450 3A4 and P-glycoprotein, was studied.

Methods: In a crossover clinical trial, 18 healthy volunteers were randomized to the two treatments using microdoses of rivaroxaban, apixaban and edoxaban alone and when coadministered with ketoconazole. Read More

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http://dx.doi.org/10.1007/s40262-019-00749-1DOI Listing
March 2019
2 Reads

Clinical Pharmacokinetics and Pharmacodynamics of Immune Checkpoint Inhibitors.

Clin Pharmacokinet 2019 Feb 28. Epub 2019 Feb 28.

Division of Systems Biomedicine and Pharmacology, Leiden Academic Centre for Drug Research, Leiden University, Einsteinweg 55, 2333 CC, Leiden, The Netherlands.

Immune checkpoint inhibitors (ICIs) have demonstrated significant clinical impact in improving overall survival of several malignancies associated with poor outcomes; however, only 20-40% of patients will show long-lasting survival. Further clarification of factors related to treatment response can support improvements in clinical outcome and guide the development of novel immune checkpoint therapies. In this article, we have provided an overview of the pharmacokinetic (PK) aspects related to current ICIs, which include target-mediated drug disposition and time-varying drug clearance. Read More

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http://link.springer.com/10.1007/s40262-019-00748-2
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http://dx.doi.org/10.1007/s40262-019-00748-2DOI Listing
February 2019
15 Reads
5.053 Impact Factor

Differences in Warfarin Pharmacodynamics and Predictors of Response Among Three Racial Populations.

Clin Pharmacokinet 2019 Feb 28. Epub 2019 Feb 28.

Department of Biopharmaceutics, Meiji Pharmaceutical University, Noshio 2-522-1, Kiyose, Tokyo, 204-8588, Japan.

Background: Population differences in warfarin dosing requirement have been reported; however, unlike the pharmacokinetics (PK) of warfarin, the quantitative influences of pharmacodynamic (PD) factors on the anticoagulation response to warfarin in different ethnic populations are totally unknown.

Methods: Using population PK/PD analysis, we attempted to identify predictors of S-warfarin clearance [CL(S)] and half maximal effective concentration (EC) to quantify racial differences in both PK and PD parameters, and to assess the contribution of these parameters to the international normalized ratio (INR) and over-anticoagulation response (INR ≥ 4) in a cohort of 309 White, Asian and African American patients.

Results: Similar to our previous findings, the median CL(S) was 30% lower in African American patients than Asian and White patients (169 vs. Read More

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http://link.springer.com/10.1007/s40262-019-00745-5
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http://dx.doi.org/10.1007/s40262-019-00745-5DOI Listing
February 2019
4 Reads

The Population Pharmacokinetics of High-Dose Methotrexate in Infants with Acute Lymphoblastic Leukemia Highlight the Need for Bedside Individualized Dose Adjustment: A Report from the Children's Oncology Group.

Clin Pharmacokinet 2019 Feb 27. Epub 2019 Feb 27.

Division of Pharmacotherapy and Experimental Therapeutics, UNC Eshelman School of Pharmacy, The University of North Carolina at Chapel Hill, CB #7569, Chapel Hill, NC, 27599-7569, USA.

Background: Infants with acute lymphoblastic leukemia (ALL) treated with high-dose methotrexate may have reduced methotrexate clearance (CL) due to renal immaturity, which may predispose them to toxicity.

Objective: The aim of this study was to develop a population pharmacokinetic (PK) model of methotrexate in infants with ALL.

Methods: A total of 672 methotrexate plasma concentrations were obtained from 71 infants enrolled in the Children's Oncology Group (COG) Clinical Trial P9407. Read More

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http://dx.doi.org/10.1007/s40262-018-00734-0DOI Listing
February 2019
4 Reads

Impact of Ethnicity-Specific Hepatic Microsomal Scaling Factor, Liver Weight, and Cytochrome P450 (CYP) 1A2 Content on Physiologically Based Prediction of CYP1A2-Mediated Pharmacokinetics in Young and Elderly Chinese Adults.

Clin Pharmacokinet 2019 Feb 15. Epub 2019 Feb 15.

Department of Pharmaceutics, College of Pharmacy, University of Florida, 1345 Center Drive, P3-27, Gainesville, FL, 32610-0494, USA.

Background: The vast majority of physiological and biological data required for physiologically based predictions are primarily available in Caucasians rather than other ethnic populations, which leads to a lack of confidence in the application of physiologically based pharmacokinetic (PBPK) modeling for ethnicity-specific prediction of pharmacokinetics in the Chinese population.

Objectives: In this study we recalibrate the system parameters of Chinese-specific PBPK modeling and explore for the first time the relative importance of ethnicity-specific microsomal protein per gram of liver (MPPGL), liver weight, and cytochrome P450 (CYP) 1A2 abundance to the projection of drug disposition mediated by CYP1A2 in young and elderly Chinese adults.

Methods: Chinese MPPGL levels and associated variability were parameterized and incorporated for the first time into ethnicity-specific PBPK models for the Chinese adults. Read More

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http://link.springer.com/10.1007/s40262-019-00737-5
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http://dx.doi.org/10.1007/s40262-019-00737-5DOI Listing
February 2019
9 Reads

Pharmacology, Pharmacokinetics and Pharmacodynamics of Eculizumab, and Possibilities for an Individualized Approach to Eculizumab.

Clin Pharmacokinet 2019 Feb 13. Epub 2019 Feb 13.

Department of Pharmacy, Radboud University Medical Center, Nijmegen, The Netherlands.

Eculizumab is the first drug approved for the treatment of complement-mediated diseases, and current dosage schedules result in large interindividual drug concentrations. This review provides insight into the pharmacokinetic and pharmacodynamic properties of eculizumab, both for reported on-label (paroxysmal nocturnal hemoglobinuria, atypical hemolytic uremic syndrome, generalized myasthenia gravis) and off-label (hematopoietic stem cell transplantation-associated thrombotic microangiopathy) indications. Furthermore, we discuss the potential of therapeutic drug monitoring to individualize treatment and reduce costs. Read More

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http://link.springer.com/10.1007/s40262-019-00742-8
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http://dx.doi.org/10.1007/s40262-019-00742-8DOI Listing
February 2019
5 Reads

Physiologically Based Pharmacokinetic Modelling for First-In-Human Predictions: An Updated Model Building Strategy Illustrated with Challenging Industry Case Studies.

Clin Pharmacokinet 2019 Feb 7. Epub 2019 Feb 7.

Pharmaceutical Sciences, Roche Pharma Research and Early Development, Roche Innovation Centre Basel, Basel, Switzerland.

Physiologically based pharmacokinetic modelling is well established in the pharmaceutical industry and is accepted by regulatory agencies for the prediction of drug-drug interactions. However, physiologically based pharmacokinetic modelling is valuable to address a much wider range of pharmaceutical applications, and new regulatory impact is expected as its full power is leveraged. As one example, physiologically based pharmacokinetic modelling is already routinely used during drug discovery for in-vitro to in-vivo translation and pharmacokinetic modelling in preclinical species, and this leads to the application of verified models for first-in-human pharmacokinetic predictions. Read More

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http://dx.doi.org/10.1007/s40262-019-00741-9DOI Listing
February 2019

Voriconazole: A Review of Population Pharmacokinetic Analyses.

Clin Pharmacokinet 2019 Jan 28. Epub 2019 Jan 28.

Department of Clinical Pharmacology, Translational Medicine Research Center, Affiliated Hangzhou First People's Hospital, Zhejiang University School of Medicine, No. 261 Huansha Road, Hangzhou, 310006, China.

Numerous population pharmacokinetic studies on voriconazole have been conducted in recent years. This review aimed to comprehensively summarize the population pharmacokinetic models for voriconazole and to determine which covariates have been identified and which remain to be explored. We searched the PubMed and EMBASE databases from inception to March 2018 for population pharmacokinetic analyses of voriconazole using the nonlinear mixed-effect method. Read More

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http://dx.doi.org/10.1007/s40262-019-00735-7DOI Listing
January 2019
1 Read
5.053 Impact Factor

Physiologically Based Pharmacokinetic Modelling of Hyperforin to Predict Drug Interactions with St John's Wort.

Clin Pharmacokinet 2019 Jan 24. Epub 2019 Jan 24.

The University of Sydney, Sydney Pharmacy School, Pharmacy and Bank Building (A15), Camperdown, NSW, 2006, Australia.

Background And Objectives: Herb-drug interactions with St John's wort (SJW) have been widely studied in numerous clinical studies. The objective of this study was to develop and evaluate a physiologically based pharmacokinetic (PBPK) model for hyperforin (the constituent of SJW responsible for interactions), which has the potential to provide unique insights into SJW interactions and allow prediction of the likely extent of interactions with SJW compared to published interaction reports.

Methods: A PBPK model of hyperforin accounting for the induction of cytochrome P450 (CYP) 3A, CYP2C9 and CYP2C19 was developed in the Simcyp Simulator (version 17) and verified using published, clinically observed pharmacokinetic data. Read More

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http://dx.doi.org/10.1007/s40262-019-00736-6DOI Listing
January 2019

Personalized Tuberculosis Treatment Through Model-Informed Dosing of Rifampicin.

Clin Pharmacokinet 2019 Jan 23. Epub 2019 Jan 23.

Department of Pharmacy, Radboud Institute for Health Sciences, Radboud University Medical Center, Nijmegen, The Netherlands.

Background And Objective: This study proposes a model-informed approach for therapeutic drug monitoring (TDM) of rifampicin to improve tuberculosis (TB) treatment.

Methods: Two datasets from pulmonary TB patients were used: a pharmacokinetic study (34 patients, 373 samples), and TDM data (96 patients, 391 samples) collected at Radboud University Medical Center, The Netherlands. Nine suitable population pharmacokinetic models of rifampicin were identified in the literature and evaluated on the datasets. Read More

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http://dx.doi.org/10.1007/s40262-018-00732-2DOI Listing
January 2019

Vancomycin Pharmacokinetics Throughout Life: Results from a Pooled Population Analysis and Evaluation of Current Dosing Recommendations.

Clin Pharmacokinet 2019 Jan 17. Epub 2019 Jan 17.

Department of Anesthesiology, University Medical Center Groningen, University of Groningen, P.O. Box 30001, 9700 RB, Groningen, The Netherlands.

Background And Objectives: Uncertainty exists regarding the optimal dosing regimen for vancomycin in different patient populations, leading to a plethora of subgroup-specific pharmacokinetic models and derived dosing regimens. We aimed to investigate whether a single model for vancomycin could be developed based on a broad dataset covering the extremes of patient characteristics. Furthermore, as a benchmark for current dosing recommendations, we evaluated and optimised the expected vancomycin exposure throughout life and for specific patient subgroups. Read More

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http://dx.doi.org/10.1007/s40262-018-0727-5DOI Listing
January 2019
3 Reads

Updated Clinical Pharmacokinetics and Pharmacodynamics of Oxycodone.

Clin Pharmacokinet 2019 Jan 17. Epub 2019 Jan 17.

Anaesthesiology and Intensive Care, Kuopio University Hospital, PO Box 100, 70029 KYS, Kuopio, Finland.

Global oxycodone consumption has increased sharply during the last two decades, and, in 2008, oxycodone consumption surpassed that of morphine. As oxycodone was synthesized in 1916 and taken to clinical use a year later, it has not undergone the same approval process required by today's standards. Most of the basic oxycodone pharmacokinetic (PK) data are from the 1990s and from academic research; however, a lot of additional data have been published over the last 10 years. Read More

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http://dx.doi.org/10.1007/s40262-018-00731-3DOI Listing
January 2019
4 Reads

Developmental Pharmacokinetics and Age-Appropriate Dosing Design of Milrinone in Neonates and Infants with Acute Kidney Injury Following Cardiac Surgery.

Clin Pharmacokinet 2019 Jan 3. Epub 2019 Jan 3.

Division of Clinical Pharmacology, Cincinnati Children's Hospital Medical Center, 3333 Burnet Avenue, MLC6018, Cincinnati, OH, 45229-3039, USA.

Background And Objective: Milrinone is used for the prevention of low cardiac output syndrome in pediatric patients after cardiac surgery. Milrinone is mainly eliminated by the kidneys; however, there is limited information on milrinone pharmacokinetics in infants who have acute kidney injury (AKI). The aim of this study was to develop a milrinone population pharmacokinetic model in neonates and infants with or without AKI. Read More

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http://link.springer.com/10.1007/s40262-018-0729-3
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http://dx.doi.org/10.1007/s40262-018-0729-3DOI Listing
January 2019
3 Reads

Lack of Effect of 12-Week Treatment with Risankizumab on the Pharmacokinetics of Cytochrome P450 Probe Substrates in Patients with Moderate to Severe Chronic Plaque Psoriasis.

Clin Pharmacokinet 2018 Dec 21. Epub 2018 Dec 21.

Clinical Pharmacology and Pharmacometrics, AbbVie Inc., 1 North Waukegan Road, North Chicago, IL, 60064, USA.

Objective: The objective of this study was to characterize the effects of risankizumab on the in vivo activity of cytochrome P450 (CYP) 1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A in psoriasis patients using a cocktail approach.

Methods: Patients with moderate to severe chronic plaque psoriasis (n = 21) received single oral doses of sensitive probe substrates for CYP1A2 (caffeine 100 mg), CYP2C9 (warfarin 10 mg), CYP2C19 (omeprazole 20 mg), CYP2D6 (metoprolol 50 mg), and CYP3A (midazolam 2 mg) on day 1, followed by 12 weeks of subcutaneous risankizumab treatment of 150 mg once every 4 weeks from day 8 to day 92, and again the same cocktail of substrates on day 98. Serial blood samples were collected for determination of the CYP probe drugs and metabolites with and without risankizumab. Read More

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http://dx.doi.org/10.1007/s40262-018-0730-xDOI Listing
December 2018
6 Reads

Safety and Pharmacokinetics of Single and Multiple Ascending Doses of the Novel Oral Human GLP-1 Analogue, Oral Semaglutide, in Healthy Subjects and Subjects with Type 2 Diabetes.

Clin Pharmacokinet 2018 Dec 18. Epub 2018 Dec 18.

Novo Nordisk A/S, Vandtårnsvej 114, 2860, Søborg, Denmark.

Background: Oral semaglutide is a novel tablet containing the human glucagon-like peptide-1 (GLP‑1) analogue semaglutide, co-formulated with the absorption enhancer sodium N-(8-[2-hydroxybenzoyl] amino) caprylate (SNAC). The safety and pharmacokinetics of oral semaglutide were investigated in two randomised, double-blind, placebo-controlled trials.

Methods: In a single-dose, first-in-human trial, 135 healthy males received oral semaglutide (2-20 mg semaglutide co-formulated with 150-600 mg SNAC) or placebo with SNAC. Read More

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http://dx.doi.org/10.1007/s40262-018-0728-4DOI Listing
December 2018
4 Reads

Correction to: Clinical Pharmacokinetics and Dose Recommendations for Posaconazole in Infants and Children.

Clin Pharmacokinet 2019 Jan;58(1):141

Infection, Inflammation, Immunity Section, Room 661, UCL Great Ormond Street Institute of Child Health, University College London, London, WC1N 1EH, UK.

However, the Original article has been updated with the Open Access under Commercial License. Read More

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http://dx.doi.org/10.1007/s40262-018-0722-xDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6325978PMC
January 2019
4 Reads

Correction to: Pharmacokinetic-Pharmacodynamic Modeling in Pediatric Drug Development, and the Importance of Standardized Scaling of Clearance.

Clin Pharmacokinet 2019 Jan;58(1):139

Infection, Inflammation and Rheumatology Section, UCL Great Ormond Street Institute of Child Heath, University College London, London, UK.

The article Pharmacokinetic-Pharmacodynamic Modeling in Pediatric Drug Development, and the Importance of Standardized Scaling of Clearance Written by Eva Germovsek,Charlotte I. S. Barker, Mike Sharland, Joseph F. Read More

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http://dx.doi.org/10.1007/s40262-018-0723-9DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6325981PMC
January 2019
1 Read

Population Pharmacokinetics of the BTK Inhibitor Acalabrutinib and its Active Metabolite in Healthy Volunteers and Patients with B-Cell Malignancies.

Clin Pharmacokinet 2019 May;58(5):659-672

Quantitative Clinical Pharmacology, Early Clinical Development, IMED Biotech Unit, AstraZeneca, Boston, MA, USA.

Introduction: Bruton tyrosine kinase (BTK) is a key component of B-cell receptor signalling, critical for cell proliferation. Acalabrutinib, a selective, covalent BTK inhibitor, recently received an accelerated approval in relapsed/refractory mantle cell lymphoma. This analysis characterized the population pharmacokinetics (PK) of acalabrutinib and its metabolite ACP-5862. Read More

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http://dx.doi.org/10.1007/s40262-018-0725-7DOI Listing
May 2019
6 Reads

Pharmacokinetic and Pharmacodynamic Modeling to Optimize the Dose of Vestronidase Alfa, an Enzyme Replacement Therapy for Treatment of Patients with Mucopolysaccharidosis Type VII: Results from Three Trials.

Clin Pharmacokinet 2019 May;58(5):673-683

Ultragenyx Pharmaceutical Inc., 60 Leveroni Court, Novato, CA, 94949, USA.

Introduction: Mucopolysaccharidosis type VII (MPS VII, Sly Syndrome) is a progressive, debilitating, ultra-rare lysosomal storage disorder caused by the deficiency of β-glucuronidase (GUS), an enzyme required for breakdown of glycosaminoglycans (GAGs). Vestronidase alfa, a recombinant human GUS, is an enzyme replacement therapy approved in the US and EU for the treatment of MPS VII.

Methods: The pharmacokinetics (PK) and pharmacodynamics (PD) of vestronidase alfa were evaluated in 23 adult and pediatric subjects with MPS VII enrolled in phase I-III clinical trials to optimize the clinical dosing regimen of vestronidase alfa. Read More

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http://dx.doi.org/10.1007/s40262-018-0721-yDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6451706PMC
May 2019
16 Reads

Pharmacogenetics of Membrane Transporters of Tacrolimus in Solid Organ Transplantation.

Clin Pharmacokinet 2019 May;58(5):593-613

Department of Clinical and Biological Pharmacology and Pharmacovigilance, Pharmacoepidemiology and Drug Information Centre, Rennes University Hospital, Rennes, France.

Membrane transporters play an essential role in the pharmacokinetics of drugs as they mediate exchanges between biological compartments. Tacrolimus is characterized by wide interpatient variability in terms of its pharmacokinetics that may in part be due to genetic factors. The pharmacogenetics of drug transporters is therefore a promising area to explore in the clinical pharmacology of tacrolimus. Read More

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http://dx.doi.org/10.1007/s40262-018-0717-7DOI Listing
May 2019
29 Reads

A Systematic Review on the Effect of HIV Infection on the Pharmacokinetics of First-Line Tuberculosis Drugs.

Clin Pharmacokinet 2018 Nov 8. Epub 2018 Nov 8.

Department of Clinical Pharmacy and Pharmacology, University of Groningen, University Medical Center Groningen, PO Box 30.001, 9700 RB, Groningen, The Netherlands.

Introduction: Contrasting findings have been published regarding the effect of human immunodeficiency virus (HIV) on tuberculosis (TB) drug pharmacokinetics (PK).

Objectives: The aim of this systematic review was to investigate the effect of HIV infection on the PK of the first-line TB drugs (FLDs) rifampicin, isoniazid, pyrazinamide and ethambutol by assessing all published literature.

Methods: Searches were performed in MEDLINE (through PubMed) and EMBASE to find original studies evaluating the effect of HIV infection on the PK of FLDs. Read More

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http://link.springer.com/10.1007/s40262-018-0716-8
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http://dx.doi.org/10.1007/s40262-018-0716-8DOI Listing
November 2018
14 Reads

Interactions Between Antiepileptic and Antibiotic Drugs: A Systematic Review and Meta-Analysis with Dosing Implications.

Clin Pharmacokinet 2018 Nov 7. Epub 2018 Nov 7.

Unit of Clinical Pharmacology, Department of Biomedical and Clinical Sciences L. Sacco, "Luigi Sacco" University Hospital, Università di Milano, Via GB Grassi 74, 20157, Milan, Italy.

Introduction: Qualitative studies on drug-drug interactions (DDIs) between anticonvulsants and antibiotics report pharmacokinetic changes that may increase the clinical risks in terms of adverse drug reactions (ADRs) and efficacy. However, no studies have provided a systematic and quantitative analysis of anticonvulsant-antibiotic pharmacokinetic DDIs. To provide such indications, we systematically and critically reviewed the literature on anticonvulsant-antibiotic DDIs in terms of quantitative pharmacokinetic changes and related ADRs. Read More

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http://dx.doi.org/10.1007/s40262-018-0720-zDOI Listing
November 2018
23 Reads

Clinical Pharmacology of Fast-Acting Insulin Aspart Versus Insulin Aspart Measured as Free or Total Insulin Aspart and the Relation to Anti-Insulin Aspart Antibody Levels in Subjects with Type 1 Diabetes Mellitus.

Clin Pharmacokinet 2019 May;58(5):639-649

Profil, Hellersbergstrasse 9, 41460, Neuss, Germany.

Background: Fast-acting insulin aspart (faster aspart) is an ultra-fast-acting formulation of insulin aspart (IAsp). This post hoc analysis investigated the pharmacokinetics of faster aspart versus IAsp, measured as free or total IAsp, and the relationship between anti-IAsp antibodies and the pharmacokinetics/pharmacodynamics of faster aspart and IAsp.

Methods: Free and total IAsp concentrations and anti-IAsp antibodies were determined in adults with type 1 diabetes mellitus receiving subcutaneous faster aspart and/or IAsp in four single-dose clinical pharmacology trials (n = 175) and a 26-week phase IIIa trial (n = 1040). Read More

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http://dx.doi.org/10.1007/s40262-018-0718-6DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6451708PMC
May 2019
21 Reads

Impact of CYP3A4*22 on Pazopanib Pharmacokinetics in Cancer Patients.

Clin Pharmacokinet 2019 May;58(5):651-658

Department of Medical Oncology, Erasmus MC Cancer Institute, Josephine Nefkens Building, Room Be-424, PO Box 5201, 3008 AE, Rotterdam, The Netherlands.

Background And Objective: As pazopanib plasma trough concentrations are correlated with treatment outcome, we explored whether single nucleotide polymorphisms in the elimination pathway of pazopanib affect systemic pazopanib concentrations.

Methods: The decreased function alleles CYP3A4 15389 C > T (*22), ABCB1 3435 C >T, ABCG2 421 C >A, and ABCG2 34G >A were analyzed within a recently developed population-pharmacokinetic model.

Results: Incorporation of CYP3A4*22 in the model resulted in a 35% lower clearance for variant carriers (0. Read More

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http://link.springer.com/10.1007/s40262-018-0719-5
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http://dx.doi.org/10.1007/s40262-018-0719-5DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6451710PMC
May 2019
13 Reads

Bridging Olaparib Capsule and Tablet Formulations Using Population Pharmacokinetic Meta-analysis in Oncology Patients.

Clin Pharmacokinet 2019 May;58(5):615-625

Quantitative Clinical Pharmacology, Early Clinical Development, IMED Biotech Unit, AstraZeneca, 35 Gatehouse Drive, Boston, MA, 02451, USA.

Background: Olaparib is a first-in-class potent oral poly(ADP-ribose) polymerase inhibitor.

Objectives: The aims of this analysis were to establish an integrated population pharmacokinetic (PK) model of olaparib in patients with solid tumors and to bridge the PK of olaparib between capsule and tablet formulations.

Methods: The population PK model was developed using plasma concentration data from 659 patients in 11 phase I, II, and III studies of olaparib tablets/capsules monotherapy. Read More

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http://link.springer.com/10.1007/s40262-018-0714-x
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http://dx.doi.org/10.1007/s40262-018-0714-xDOI Listing
May 2019
34 Reads

Population Pharmacokinetics of Fludarabine in Children and Adults during Conditioning Prior to Allogeneic Hematopoietic Cell Transplantation.

Clin Pharmacokinet 2019 May;58(5):627-637

Department of Pharmacy and Pharmacology, Antoni van Leeuwenhoek Hospital/Netherlands Cancer Institute, Amsterdam, The Netherlands.

Background: Fludarabine is often used as an important drug in reduced toxicity conditioning regimens prior to hematopoietic cell transplantation (HCT). As no definitive pharmacokinetic (PK) basis for HCT dosing for the wide age and weight range in HCT is available, linear body surface area (BSA)-based dosing is still used.

Objective: We sought to describe the population PK of fludarabine in HCT recipients of all ages. Read More

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http://dx.doi.org/10.1007/s40262-018-0715-9DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6451721PMC
May 2019
5 Reads

Cardiovascular Risk Management and Hepatitis C: Combining Drugs.

Clin Pharmacokinet 2019 May;58(5):565-592

Department of Pharmacy, Radboud university medical center, Geert Grooteplein Zuid 10, 6525 GA, Nijmegen, The Netherlands.

Direct-acting antivirals (DAAs) are known victims (substrate) and perpetrators (cause) of drug-drug interactions (DDIs). These DAAs are used for the treatment of hepatitis C virus (HCV) infections and are highly effective drugs. Drugs used for cardiovascular risk management are frequently used by HCV-infected patients, whom also are treated with DAAs. Read More

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http://dx.doi.org/10.1007/s40262-018-0710-1DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6451722PMC
May 2019
4 Reads

Pharmacokinetics of Hydroxychloroquine in Pregnancies with Rheumatic Diseases.

Clin Pharmacokinet 2019 Apr;58(4):525-533

Duke Clinical Research Institute, Duke University School of Medicine, Durham, NC, USA.

Background: Hydroxychloroquine is an oral drug prescribed to pregnant women with rheumatic disease to reduce disease activity and prevent flares. Physiologic changes during pregnancy may substantially alter drug pharmacokinetics. However, the effect of pregnancy on hydroxychloroquine disposition and the potential need for dose adjustment remains virtually unknown. Read More

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http://link.springer.com/10.1007/s40262-018-0712-z
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http://dx.doi.org/10.1007/s40262-018-0712-zDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6397666PMC
April 2019
26 Reads

Comprehensive Measurements of Intrauterine and Postnatal Exposure to Lamotrigine.

Clin Pharmacokinet 2019 Apr;58(4):535-543

Department of Psychiatry, Psychotherapy and Psychosomatics, RWTH Aachen University, 52074, Aachen, Germany.

Objective: The aim of this study was to measure and investigate correlations of lamotrigine concentrations in maternal as well as umbilical cord blood, amniotic fluid, and breast milk to account for the distribution of the drug.

Methods: Concentrations of lamotrigine were measured in 19 mother-infant pairs at the time of delivery. To account for the penetration ratio into amniotic fluid, cord blood and breast milk, the concentration of lamotrigine in the particular environment was divided by the concentration in maternal serum. Read More

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http://dx.doi.org/10.1007/s40262-018-0713-yDOI Listing
April 2019
2 Reads

A Generic Model for Quantitative Prediction of Interactions Mediated by Efflux Transporters and Cytochromes: Application to P-Glycoprotein and Cytochrome 3A4.

Clin Pharmacokinet 2019 Apr;58(4):503-523

Pharmacie, Groupement Hospitalier Nord, Hospices Civils de Lyon, Lyon, France.

Background And Objective: The In Vivo Mechanistic Static Model (IMSM) is a powerful method used to predict the magnitude of drug-drug interactions (DDIs) mediated by cytochromes. The objective of this study was to extend the IMSM paradigm to DDIs mediated by efflux transporters and cytochromes.

Methods: First, a generic model for this kind of interaction was devised. Read More

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http://link.springer.com/10.1007/s40262-018-0711-0
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http://dx.doi.org/10.1007/s40262-018-0711-0DOI Listing
April 2019
12 Reads

Monitoring of Tobramycin Exposure: What is the Best Estimation Method and Sampling Time for Clinical Practice?

Clin Pharmacokinet 2019 Mar;58(3):389-399

School of Pharmacy, Pharmacy Australia Centre of Excellence, University of Queensland, 20 Cornwall Street, Woolloongabba, Brisbane, QLD, 4102, Australia.

Objectives: The objective of this article is to investigate the influence of blood sampling times on tobramycin exposure estimation and clinical decisions and to determine the best sampling times for two estimation methods used for therapeutic drug monitoring.

Methods: Adult patients with cystic fibrosis, treated with once-daily intravenous tobramycin, were intensively sampled over one 24-h dosing interval to determine true exposure (AUC). The AUCs were then estimated using both log-linear regression and Bayesian forecasting methods for 21 different sampling time combinations. Read More

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http://link.springer.com/10.1007/s40262-018-0707-9
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http://dx.doi.org/10.1007/s40262-018-0707-9DOI Listing
March 2019
16 Reads

Repository Describing an Aging Population to Inform Physiologically Based Pharmacokinetic Models Considering Anatomical, Physiological, and Biological Age-Dependent Changes.

Clin Pharmacokinet 2019 Apr;58(4):483-501

Division of Infectious Diseases and Hospital Epidemiology, Departments of Medicine and Clinical Research, University Hospital Basel, Basel, Switzerland.

Background: Aging is characterized by anatomical, physiological, and biological changes that can impact drug kinetics. The elderly are often excluded from clinical trials and knowledge about drug kinetics and drug-drug interaction magnitudes is sparse. Physiologically based pharmacokinetic modeling can overcome this clinical limitation but detailed descriptions of the population characteristics are essential to adequately inform models. Read More

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http://dx.doi.org/10.1007/s40262-018-0709-7DOI Listing
April 2019
4 Reads