ReviewExpert opinion on drug metabolism & toxicology2010
Metabolism considerations for kinase inhibitors in cancer treatment.
Review in Expert opinion on drug metabolism & toxicology, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 47 papers, 2 of them syntheses 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
47 citing papers in PubMed, 2 syntheses or guidelines pooled it, 107 citations in OpenAlex.
- CYP3A4*22 Genotype-Guided Dosing of Kinase Inhibitors in Cancer Patients.Clinical pharmacokinetics · 2023Pooled it
- Safe handling of oral antineoplastic medications: Focus on targeted therapeutics in the home setting.Journal of oncology pharmacy practice : official publication of the International Society of Oncology Pharmacy Practitioners · 2017Pooled it
- Drug-drug interactions in targeted cancer therapies: a focus on tyrosine kinase inhibitors.Expert review of clinical pharmacology · 2025Review
- Variable response of germline activating PDGFRB variants to receptor tyrosine kinase inhibitors: implications for treatment.European journal of human genetics : EJHG · 2025Article
- Impact of variation in CYP3A and CYP2C8 on tucatinib metabolic clearance in human liver microsomes.Drug metabolism and disposition: the biological fate of chemicals · 2025Article
- Cellular and molecular aspects of drug resistance in cancers.Daru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences · 2024Review
- Targeting the EphA2 pathway: could it be the way for bone sarcomas?Cell communication and signaling : CCS · 2024Review
- Multiparametric MRI for characterization of the tumour microenvironment.Nature reviews. Clinical oncology · 2024Review
- Physiologically based pharmacokinetic modeling of imatinib and N-desmethyl imatinib for drug-drug interaction predictions.CPT: pharmacometrics & systems pharmacology · 2024Article
- Kinase Inhibitors FDA Approved 2018-2023: Drug Targets, Metabolic Pathways, and Drug-Induced Toxicities.Drug metabolism and disposition: the biological fate of chemicals · 2024Review
- Targeted therapy for head and neck cancer: signaling pathways and clinical studies.Signal transduction and targeted therapy · 2023Review
- Inhibition of Abelson Tyrosine-Protein Kinase 2 Suppresses the Development of Alcohol-Associated Liver Disease by Decreasing PPARgamma Expression.Cellular and molecular gastroenterology and hepatology · 2023Article
- In silico design of EGFRHeliyon · 2022Article
- The Role of CYP3A in Health and Disease.Biomedicines · 2022Review
- Cytochromes P450 2C8 and 3A Catalyze the Metabolic Activation of the Tyrosine Kinase Inhibitor Masitinib.Chemical research in toxicology · 2022Article
- Article
- Transport and metabolism of tyrosine kinase inhibitors associated with chronic myeloid leukemia therapy: a review.Molecular and cellular biochemistry · 2022Review
- Prediction of drug-drug interaction potential mediated by transporters between dasatinib and metformin, pravastatin, and rosuvastatin using physiologically based pharmacokinetic modeling.Cancer chemotherapy and pharmacology · 2022Article
- β-Dystroglycan Restoration and Pathology Progression in the DystrophicBiomolecules · 2021Article
- Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
2 authors at 1 institution in 1 country.
Funding
Abstract
importance of the fieldA concerted effort by the pharmaceutical industry over the last decade has led to the successful clinical development of protein kinase inhibitors as effective targeted therapies for certain cancers. AREAS COVERED IN THIS REVIEW: This review details eight small molecule kinase inhibitors that have been approved for the treatment of cancer in either the US or Europe as of March 2010: imatinib, sorafenib, gefitinib, erlotinib, dasatinib, lapatinib, sunitinib and nilotinib. These eight compounds vary from the relatively specific inhibitor lapatinib to the more promiscuous kinase inhibitors dasatinib and sunitinib. WHAT THE READER WILL GAIN: A brief discussion on the biology of each inhibitor, selectivity over other kinases and toxicity is provided. A more detailed discussion on the metabolism, drug transporters, drug-drug interactions and possible roles of metabolism in compound toxicity is provided for each compound. TAKE HOME MESSAGE: The majority of the currently approved kinase inhibitors is heavily influenced by drug transporters and significantly affected by CYP3A4 inhibitors/inducers. At least three, gefitinib, erlotinib and dasatinib, are metabolized to form reactive metabolites capable of covalently-binding biomolecules.
Indexed as
Identifiers
What OpenQuestion holds
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.