Trial reportBritish journal of clinical pharmacology2009
Effects of ketoconazole and carbamazepine on lapatinib pharmacokinetics in healthy subjects.
Trial report in British journal of clinical pharmacology, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers, 1 of them a synthesis that pooled it.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
27 citing papers in PubMed, 1 synthesis or guideline pooled it, 61 citations in OpenAlex.
- Management of epilepsy in brain tumors.Neurological sciences : official journal of the Italian Neurological Society and of the Italian Society of Clinical Neurophysiology · 2019Guideline
- Effects of low-fat and high-fat meals on steady-state pharmacokinetics of lapatinib in patients with advanced solid tumours.Investigational new drugs · 2014Trial
- Investigating the Impact of Calcium Channel Blockers on the Pharmacokinetics of Lapatinib: Possible Role of Cytochrome P450 Enzymes and P-glycoprotein Efflux Transporters.European journal of drug metabolism and pharmacokinetics · 2026Article
- Comparative pharmacokinetics of tyrosine kinase inhibitor, lapatinib, in dogs and cats following single oral administration.The Journal of veterinary medical science · 2024Article
- Prediction of Pharmacokinetic Drug-Drug Interactions Involving Anlotinib as a Victim by Using Physiologically Based Pharmacokinetic Modeling.Drug design, development and therapy · 2024Article
- Factors affecting high-grade hepatotoxicity of tyrosine kinase inhibitors in cancer patients: a multi-center observational study.European journal of clinical pharmacology · 2020Observational
- Lung cancer cells survive epidermal growth factor receptor tyrosine kinase inhibitor exposure through upregulation of cholesterol synthesis.FASEB bioAdvances · 2020Article
- Pivotal Considerations for Optimal Deployment of Healthy Volunteers in Oncology Drug Development.Clinical and translational science · 2020Review
- Structural Perspectives of the CYP3A Family and Their Small Molecule Modulators in Drug Metabolism.Liver research (Beijing, China) · 2019Article
- Oral oncolytic and antiretroviral therapy administration: dose adjustments, drug interactions, and other considerations for clinical use.Drugs in context · 2019Review
- A Model for Predicting the Interindividual Variability of Drug-Drug Interactions.The AAPS journal · 2017Article
- Seizures and cancer: drug interactions of anticonvulsants with chemotherapeutic agents, tyrosine kinase inhibitors and glucocorticoids.Neuro-oncology practice · 2016Review
- Cytochrome P450 3A4 and CYP3A5-Catalyzed Bioactivation of Lapatinib.Drug metabolism and disposition: the biological fate of chemicals · 2016Article
- Drug-Drug Interaction Potentials of Tyrosine Kinase Inhibitors via Inhibition of UDP-Glucuronosyltransferases.Scientific reports · 2015Article
- Mechanism-based inactivation of CYP450 enzymes: a case study of lapatinib.Drug metabolism reviews · 2015Review
- Metabolism-related pharmacokinetic drug-drug interactions with tyrosine kinase inhibitors: current understanding, challenges and recommendations.British journal of clinical pharmacology · 2015Review
- Phase I dose-escalation study of 5-day intermittent oral lapatinib therapy in patients with human epidermal growth factor receptor 2-overexpressing breast cancer.Journal of clinical oncology : official journal of the American Society of Clinical Oncology · 2014Article
- Physiologically based pharmacokinetic model of lapatinib developed in mice and scaled to humans.Journal of pharmacokinetics and pharmacodynamics · 2013Article
- Tyrosine kinase inhibitors and drug interactions: a review with practical recommendations.Clinical & translational oncology : official publication of the Federation of Spanish Oncology Societies and of the National Cancer Institute of Mexico · 2012Review
- Lapatinib for advanced or metastatic breast cancer.The oncologist · 2012Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
6 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
aimsTo characterize the impact of potent CYP3A4 inhibition and induction on lapatinib pharmacokinetics.
methodsTwo studies were conducted in healthy subjects. One study examined the effect of ketoconazole 200 mg b.i.d. for 7 days on a single 100-mg dose of lapatinib in 22 healthy subjects. The other study examined the effect of carbamazepine titrated up to 200 mg b.i.d. over 20 days on a single 250-mg dose of lapatinib in 24 healthy subjects.
resultsKetoconazole altered lapatinib AUC, C(max) and half-life, with geometric mean [95% confidence interval (CI)] increases of 3.57-fold (3.07, 4.15), 2.14-fold (1.74, 2.64) and 1.66-fold (1.50, 1.84), respectively, but had no effect on absorption rate. Carbamazepine altered lapatinib AUC, C(max) and absorption rate, with geometric mean (95% CI) decreases of 72% (68, 77), 59% (49, 66) and 28% (4, 46), respectively, but had no effect on half-life.
conclusionsSystemic exposure to lapatinib was significantly altered by potent inhibition and induction of CYP3A4. Dose adjustments may be required when lapatinib is administered with orally administered drugs that potently alter the activity of this enzyme.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.