Telatinib (BAY 57-9352) is an orally available, small-molecule inhibitor of vascular endothelial growth factor receptors 2 and 3 (VEGFR-2/-3) and platelet-derived growth factor receptor beta tyrosine kinases. In this multicentre phase I dose escalation study, 71 patients with refractory solid tumours were enroled into 14 days on/7 days off (noncontinuous dosing) or continuous dosing groups to receive telatinib two times daily (BID). Hypertension (23%) and diarrhoea (7%) were the most frequent study drug-related adverse events of CTC grade 3. The maximum-tolerated dose was not reached up to a dose of 1500 mg BID continuous dosing. Telatinib was rapidly absorbed with median t(max) of 3 hours or less. Geometric mean C(max) and AUC(0-12) increased in a less than dose-proportional manner and plateaued in the 900-1500 mg BID dose range. Two renal cell carcinoma patients reached a partial response. Tumour blood flow measured by contrast-enhanced magnetic resonance imaging and sVEGFR-2 plasma
%0 Journal Article
%1 Strumberg.2008
%A Strumberg, D.
%A Schultheis, B.
%A Adamietz, I. A.
%A Christensen, O.
%A Buechert, M.
%A Kraetzschmar, J.
%A Rajagopalan, P.
%A Ludwig, M.
%A Frost, A.
%A Steinbild, S.
%A Scheulen, M. E.
%A Mross, K.
%D 2008
%J Br.J.Cancer
%K & 80 Adult Aged Agents Angiogenesis Antineoplastic Carcinoma Dose Female Growth Humans Hypertension Imaging Inhibitors Magnetic Male Maximum Medical Middle Neoplasms Oncology Plasma Pyridazines Pyridines RANGE Resonance Tolerated Tyrosine administration and blood dosage drug over response therapy
%N 10
%P 1579-1585
%T Phase I dose escalation study of telatinib (BAY 57-9352) in patients with advanced solid tumours
%U PM:19002179
%V 99
%X Telatinib (BAY 57-9352) is an orally available, small-molecule inhibitor of vascular endothelial growth factor receptors 2 and 3 (VEGFR-2/-3) and platelet-derived growth factor receptor beta tyrosine kinases. In this multicentre phase I dose escalation study, 71 patients with refractory solid tumours were enroled into 14 days on/7 days off (noncontinuous dosing) or continuous dosing groups to receive telatinib two times daily (BID). Hypertension (23%) and diarrhoea (7%) were the most frequent study drug-related adverse events of CTC grade 3. The maximum-tolerated dose was not reached up to a dose of 1500 mg BID continuous dosing. Telatinib was rapidly absorbed with median t(max) of 3 hours or less. Geometric mean C(max) and AUC(0-12) increased in a less than dose-proportional manner and plateaued in the 900-1500 mg BID dose range. Two renal cell carcinoma patients reached a partial response. Tumour blood flow measured by contrast-enhanced magnetic resonance imaging and sVEGFR-2 plasma
@article{Strumberg.2008,
abstract = {Telatinib (BAY 57-9352) is an orally available, small-molecule inhibitor of vascular endothelial growth factor receptors 2 and 3 (VEGFR-2/-3) and platelet-derived growth factor receptor beta tyrosine kinases. In this multicentre phase I dose escalation study, 71 patients with refractory solid tumours were enroled into 14 days on/7 days off (noncontinuous dosing) or continuous dosing groups to receive telatinib two times daily (BID). Hypertension (23%) and diarrhoea (7%) were the most frequent study drug-related adverse events of CTC grade 3. The maximum-tolerated dose was not reached up to a dose of 1500 mg BID continuous dosing. Telatinib was rapidly absorbed with median t(max) of 3 hours or less. Geometric mean C(max) and AUC(0-12) increased in a less than dose-proportional manner and plateaued in the 900-1500 mg BID dose range. Two renal cell carcinoma patients reached a partial response. Tumour blood flow measured by contrast-enhanced magnetic resonance imaging and sVEGFR-2 plasma },
added-at = {2010-02-05T11:28:39.000+0100},
author = {Strumberg, D. and Schultheis, B. and Adamietz, I. A. and Christensen, O. and Buechert, M. and Kraetzschmar, J. and Rajagopalan, P. and Ludwig, M. and Frost, A. and Steinbild, S. and Scheulen, M. E. and Mross, K.},
biburl = {https://www.bibsonomy.org/bibtex/28f5964e30624735de6cd198fda68f485/kanefendt},
interhash = {5c0728a20e9baeef80c1bc9eb733ed61},
intrahash = {8f5964e30624735de6cd198fda68f485},
journal = {Br.J.Cancer},
keywords = {& 80 Adult Aged Agents Angiogenesis Antineoplastic Carcinoma Dose Female Growth Humans Hypertension Imaging Inhibitors Magnetic Male Maximum Medical Middle Neoplasms Oncology Plasma Pyridazines Pyridines RANGE Resonance Tolerated Tyrosine administration and blood dosage drug over response therapy},
number = 10,
pages = {1579-1585},
timestamp = {2010-02-05T11:28:50.000+0100},
title = {Phase I dose escalation study of telatinib (BAY 57-9352) in patients with advanced solid tumours},
url = {PM:19002179},
volume = 99,
year = 2008
}