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Article
Cobalt intoxication: mitochondrial features and condition
Cobalt intoxication is a rare complication of joint arthroplasty with a metal-on-metal prothesis or metal implants after broken ceramic implants. Patients with metal components should be monitored closely for ...
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Article
Open AccessPhase Ib dose-escalation study of the hypoxia-modifier Myo-inositol trispyrophosphate in patients with hepatopancreatobiliary tumors
Hypoxia is prominent in solid tumors and a recognized driver of malignancy. Thus far, targeting tumor hypoxia has remained unsuccessful. Myo-inositol trispyrophosphate (ITPP) is a re-oxygenating compound witho...
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Article
Activation of D1 receptors affects human reactivity and flexibility to valued cues
Reward-predicting cues motivate goal-directed behavior, but in unstable environments humans must also be able to flexibly update cue-reward associations. While the capacity of reward cues to trigger motivation...
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Article
Open AccessPrediction of exposure-driven myelotoxicity of continuous infusion 5-fluorouracil by a semi-physiological pharmacokinetic–pharmacodynamic model in gastrointestinal cancer patients
To describe 5-fluorouracil (5FU) pharmacokinetics, myelotoxicity and respective covariates using a simultaneous nonlinear mixed effect modelling approach.
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Article
Severe reduction in tacrolimus concentrations with concomitant metamizole (dipyrone) therapy in transplant patients
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Article
Do clinical and laboratory parameters predict thiopurine metabolism and clinical outcome in patients with inflammatory bowel diseases?
The thiopurines azathioprine and 6-mercaptopurine are frequently used for remission maintenance in patients with inflammatory bowel diseases. However, there are therapy failures, and it is unclear whether clin...
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Article
Open AccessDevelopment of OXY111A, a novel hypoxia-modifier as a potential antitumor agent in patients with hepato-pancreato-biliary neoplasms - Protocol of a first Ib/IIa clinical trial
Solid tumors, such as hepato-pancreato-biliary cancer, develop tumor hypoxia with tumor growth. Despite advances in surgery, a majority of these patients are in an unresectable condition. At this stage standar...
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Article
Open AccessAssessment of CYP1A2 enzyme activity in relation to type-2 diabetes and habitual caffeine intake
Coffee consumption is a known inducer of cytochrome P450 1A2 (CYP1A2) enzyme activity. We recently observed that a group of type-2 diabetes patients consumed more caffeine (coffee) on a daily basis than non-ty...
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Article
Open AccessNo major effects of vitamin D3 (1,25 dihydroxyvitamin D3) on absorption and pharmacokinetics of folic acid and fexofenadine in healthy volunteers
In Caco-2 cells, folate uptake via the proton-coupled folate transporter (PCFT) increases significantly by a 3-day treatment with 1,25-dihydroxyvitamin D3 (1,25(OH)2D3). Additionally, mRNA content and protein exp...
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Article
Impact of variable CYP genotypes on breast cancer relapse in patients undergoing adjuvant tamoxifen therapy
Tamoxifen is frequently used for the treatment of hormone receptor positive breast cancer (BC). Mainly CYP2D6 is responsible for the transformation to therapeutically active metabolites, but CYP2C19, CYP2C9 a...
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Article
Low allopurinol doses are sufficient to optimize azathioprine therapy in inflammatory bowel disease patients with inadequate thiopurine metabolite concentrations
Recent studies in patients with inflammatory bowel diseases (IBD) on thiopurine therapy suggest that too low 6-thioguanine nucleotide concentrations (6-TGN) and too high methylmercaptopurine nucleotide concent...
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Article
Effect of ritonavir on the pharmacokinetics of the benzimidazoles albendazole and mebendazole: an interaction study in healthy volunteers
Benzimidazoles are often used concomitantly with protease inhibitors in patients with helminthic disease and HIV infection. Low bioavailability and extensive first-pass metabolism make benzimidazoles prone to ...
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Article
Phenoty** of N-acetyltransferase type 2 and xanthine oxidase with caffeine: when should urine samples be collected?
Individual activities of N-acetyltransferase 2 (NAT2) and of xanthine oxidase (XO) can be assessed using ratios of urinary caffeine metabolites. We investigated how ratios changed over time and which urine collec...
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Article
Mesalazine pharmacokinetics and NAT2 phenotype
Mesalazine undergoes extensive metabolism by N-acetylation. While there is some evidence for an involvement of N-acetyltransferase (NAT) type 1, a potential role of NAT type 2 (NAT2) in vivo has not been tested.
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Article
Assessment of urinary mephenytoin metrics to phenotype for CYP2C19 and CYP2B6 activity
(S)-Mephenytoin is selectively metabolised to (S)-4′-hydroxymephenytoin by CYP2C19. The urinary excretion of 4′-hydroxymephenytoin reflects the activity of individual enzymes. We evaluated fractioned urinary c...
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Article
Population Pharmacokinetics of the BEACOPP Polychemotherapy Regimen in Hodgkin’s Lymphoma and its Effect on Myelotoxicity
The BEACOPP (bleomycin, etoposide, doxorubicin, cyclophosphamide, vincristine, procarbazine and prednisone) chemotherapy regimen for the treatment of advanced Hodgkin’s lymphoma has a superior outcome, but its...
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Article
Pharmacokinetics of piritramide in newborns, infants and young children in intensive care units
Piritramide is indicated for treatment of postoperative pain and analgosedation in the intensive care unit (ICU) setting. In an open prospective study the pharmacokinetics of piritramide were investigated in f...
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Article
Clinical Pharmacokinetics of Trospium Chloride
Trospium chloride, a quaternary amine with anticholinergic properties, is used for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency and urinary frequency. The pharmacokin...
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Article
Cytochrome P 450 2C9 phenoty** using low-dose tolbutamide
The hypoglycaemic drug tolbutamide is used for assessment of CYP2C9 activity in vivo. However, therapeutically active doses of 500 mg bear the risk of hypoglycaemia, and a tolbutamide-derived parameter based o...
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Article
Phenoty** of N-acetyltransferase type 2 by caffeine from uncontrolled dietary exposure
The standard approach for phenoty** of the human arylamine N-acetyltransferase 2 (NAT2) uses urinary caffeine metabolite ratios after a caffeine test dose taken in after methylxanthine abstinence. We tested whe...
