Anticancer efficacy of the irreversible EGFr tyrosine kinase inhibitor PD 0169414 against human tumor xenografts
| Autor: | William L. Elliott, Steven E. Rose, Patrick W. Vincent, Sandra J. Patmore, Veronika Sherwood, David W. Fry, Hairong Zhou, Wilber R. Leopold, Billy J. Roberts, Alex J. Bridges, Donald J. Dykes |
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| Rok vydání: | 2000 |
| Předmět: |
Cancer Research
medicine.drug_class Transplantation Heterologous Mice Nude Antineoplastic Agents Mice SCID Toxicology Drug Administration Schedule Tyrosine-kinase inhibitor Mice Epidermal growth factor In vivo Tumor Cells Cultured Carcinoma medicine Animals Humans Pharmacology (medical) Enzyme Inhibitors Phosphorylation Receptor Pharmacology Mice Inbred ICR biology Drug Administration Routes Receptor Protein-Tyrosine Kinases 3T3 Cells Infusion Pumps Implantable Neoplasms Experimental medicine.disease ErbB Receptors Treatment Outcome Liver Oncology Epidermoid carcinoma Enzyme inhibitor Area Under Curve Quinazolines biology.protein Cancer research Tyrosine kinase Neoplasm Transplantation |
| Zdroj: | Cancer Chemotherapy and Pharmacology. 45:231-238 |
| ISSN: | 1432-0843 0344-5704 |
| Popis: | Purpose: The involvement of the EGF receptor (EGFr) family of receptors in cancers suggests that a selective inhibitor of the tyrosine kinase activity of the EGFr family could have a therapeutic effect. PD 0169414, an anilinoquinazoline, is a potent irreversible inhibitor of the EGFr family tyrosine kinase activity with IC50 values of 0.42 nM against the isolated EGF receptor, and 4.7 nM and 22 nM against EGF- and heregulin-mediated receptor phosphorylation in A431 and MDA-MB-453 cells, respectively. Methods and Results: Oral administration of 260 mg/kg per day PD 0169414 for 15 days to animals bearing advanced-stage A431 epidermoid carcinoma produced a 28.2-day delay in tumor growth and resulted in three complete and three partial tumor regressions in six animals. Toxicity at this dose level was limited to |
| Databáze: | OpenAIRE |
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