Phase I dose escalation study of telatinib, a tyrosine kinase inhibitor of vascular endothelial growth factor receptor 2 and 3, platelet-derived growth factor receptor beta, and c-Kit, in patients with advanced or metastatic solid tumors
PURPOSE: Telatinib (BAY 57-9352) is an orally available tyrosine kinase inhibitor of vascular endothelial growth factor receptor (VEGFR) -2, VEGFR-3, platelet-derived growth factor receptor-beta, and c-Kit. This phase I dose escalation study was conducted to evaluate the safety and tolerability of telatinib, with additional pharmacokinetic, pharmacodynamic, and efficacy assessments. PATIENTS AND METHODS: Patients with solid tumors refractory to standard therapies or with no standard therapy available were enrolled. Doses of continuously administered telatinib were escalated from 20 mg once daily to 1,500 mg twice daily. RESULTS: Fifty-three patients were enrolled. Most frequently observed drug-related adverse events were nausea (26.4%; grade >or= 3, 0%) and hypertension (20.8%; grade 3, 11.3%; grade 4, 0%). Two dose-limiting toxicities were observed: one poorly controlled hypertension (600 mg twice daily), and one grade 2 weight loss, anorexia, and fatigue (1,500 mg twice daily). A for
%0 Journal Article
%1 Eskens.2009
%A Eskens, F. A.
%A Steeghs, N.
%A Verweij, J.
%A Bloem, J. L.
%A Christensen, O.
%A van, Doorn L.
%A Ouwerkerk, J.
%A Jonge, M. J.
%A Nortier, J. W.
%A Kraetzschmar, J.
%A Rajagopalan, P.
%A Gelderblom, H.
%D 2009
%J J.Clin.Oncol.
%K & A Administration Adolescent Adult Aged Angiogenesis Biological Contrast Dose Dose-Response Drug Endothelial Factor Factors Fatigue Female Growth Human Humans Hypertension Imaging Inhibitors Kinase Magnetic Male Markers Maximum Media Medical Metastasis Middle Neoplasm Neoplasms Oncology Oral Outcome Pharmacokinetics Plasma Platelet-Derived Protein Proteins Proto-Oncogene Pyridazines Pyridines Receptor Receptor-2 Receptor-3 Relationship Research Resonance Safety Schedule Time Tolerated Treatment Tumor Tyrosine Vascular Young administration adverse antagonists beta blood c-kit diagnostic dosage drug effects enzymology inhibitors methods pathology protein response supply therapy toxicity use
%N 25
%P 4169-4176
%T Phase I dose escalation study of telatinib, a tyrosine kinase inhibitor of vascular endothelial growth factor receptor 2 and 3, platelet-derived growth factor receptor beta, and c-Kit, in patients with advanced or metastatic solid tumors
%U PM:19636022
%V 27
%X PURPOSE: Telatinib (BAY 57-9352) is an orally available tyrosine kinase inhibitor of vascular endothelial growth factor receptor (VEGFR) -2, VEGFR-3, platelet-derived growth factor receptor-beta, and c-Kit. This phase I dose escalation study was conducted to evaluate the safety and tolerability of telatinib, with additional pharmacokinetic, pharmacodynamic, and efficacy assessments. PATIENTS AND METHODS: Patients with solid tumors refractory to standard therapies or with no standard therapy available were enrolled. Doses of continuously administered telatinib were escalated from 20 mg once daily to 1,500 mg twice daily. RESULTS: Fifty-three patients were enrolled. Most frequently observed drug-related adverse events were nausea (26.4%; grade >or= 3, 0%) and hypertension (20.8%; grade 3, 11.3%; grade 4, 0%). Two dose-limiting toxicities were observed: one poorly controlled hypertension (600 mg twice daily), and one grade 2 weight loss, anorexia, and fatigue (1,500 mg twice daily). A for
@article{Eskens.2009,
abstract = {PURPOSE: Telatinib (BAY 57-9352) is an orally available tyrosine kinase inhibitor of vascular endothelial growth factor receptor (VEGFR) -2, VEGFR-3, platelet-derived growth factor receptor-beta, and c-Kit. This phase I dose escalation study was conducted to evaluate the safety and tolerability of telatinib, with additional pharmacokinetic, pharmacodynamic, and efficacy assessments. PATIENTS AND METHODS: Patients with solid tumors refractory to standard therapies or with no standard therapy available were enrolled. Doses of continuously administered telatinib were escalated from 20 mg once daily to 1,500 mg twice daily. RESULTS: Fifty-three patients were enrolled. Most frequently observed drug-related adverse events were nausea (26.4%; grade >or= 3, 0%) and hypertension (20.8%; grade 3, 11.3%; grade 4, 0%). Two dose-limiting toxicities were observed: one poorly controlled hypertension (600 mg twice daily), and one grade 2 weight loss, anorexia, and fatigue (1,500 mg twice daily). A for},
added-at = {2010-02-05T11:28:39.000+0100},
author = {Eskens, F. A. and Steeghs, N. and Verweij, J. and Bloem, J. L. and Christensen, O. and van, Doorn L. and Ouwerkerk, J. and Jonge, M. J. and Nortier, J. W. and Kraetzschmar, J. and Rajagopalan, P. and Gelderblom, H.},
biburl = {https://www.bibsonomy.org/bibtex/2e1e0093a21e2bfab8ccf40b5087dc8ef/kanefendt},
interhash = {0d60aac3b91a2635a1caa2a846078bbd},
intrahash = {e1e0093a21e2bfab8ccf40b5087dc8ef},
journal = {J.Clin.Oncol.},
keywords = {& A Administration Adolescent Adult Aged Angiogenesis Biological Contrast Dose Dose-Response Drug Endothelial Factor Factors Fatigue Female Growth Human Humans Hypertension Imaging Inhibitors Kinase Magnetic Male Markers Maximum Media Medical Metastasis Middle Neoplasm Neoplasms Oncology Oral Outcome Pharmacokinetics Plasma Platelet-Derived Protein Proteins Proto-Oncogene Pyridazines Pyridines Receptor Receptor-2 Receptor-3 Relationship Research Resonance Safety Schedule Time Tolerated Treatment Tumor Tyrosine Vascular Young administration adverse antagonists beta blood c-kit diagnostic dosage drug effects enzymology inhibitors methods pathology protein response supply therapy toxicity use},
number = 25,
pages = {4169-4176},
timestamp = {2010-02-05T11:28:52.000+0100},
title = {Phase I dose escalation study of telatinib, a tyrosine kinase inhibitor of vascular endothelial growth factor receptor 2 and 3, platelet-derived growth factor receptor beta, and c-Kit, in patients with advanced or metastatic solid tumors},
url = {PM:19636022},
volume = 27,
year = 2009
}