Erlotinib: preclinical investigations.

M Hidalgo - Oncology (Williston Park, NY), 2003 - europepmc.org
Erlotinib (Tarceva) is an orally available selective small-molecule inhibitor of HER1/EGFR
tyrosine kinase with a 50% inhibitory concentration of 2 nM for purified tyrosine kinase. This …

Preclinical studies with erlotinib (Tarceva)

RW Akita, MX Sliwkowski - Seminars in oncology, 2003 - Elsevier
Erlotinib HCl (Tarceva; Genentech, Inc, South San Francisco, CA) is an orally available,
highly selective, reversible inhibitor of epidermal growth factor receptor (HER1/EGFR) …

Targeting HER1/EGFR in cancer therapy: experience with erlotinib

G Giaccone - Future Oncology, 2005 - Taylor & Francis
Research into the role of the human epidermal receptor growth factor receptor 1/epidermal
growth factor receptor (HER1/EGFR) in tumorigenesis has generated a new class of …

Clinical experience with the HER1/EGFR tyrosine kinase inhibitor erlotinib.

A Sandler - Oncology (Williston Park, NY), 2003 - europepmc.org
In phase I trials in healthy volunteers and patients with refractory cancers, erlotinib (Tarceva)
was well tolerated and showed activity against non-small-cell lung cancer and other tumors …

Erlotinib (Tarceva): an update on the clinical trial program

RS Herbst - Seminars in oncology, 2003 - Elsevier
Erlotinib HCI (Tarceva; Genentech, Inc, South San Francisco, CA) is an orally available,
quinazoline-based agent that competes with adenosine triphosphate for binding with the …

Erlotinib directly inhibits HER2 kinase activation and downstream signaling events in intact cells lacking epidermal growth factor receptor expression

G Schaefer, L Shao, K Totpal, RW Akita - Cancer research, 2007 - AACR
Erlotinib (Tarceva), is an orally available, reversible inhibitor of epidermal growth factor
receptor (EGFR; HER1) that exhibits inhibitory activity on purified HER2 kinase at much …

Antitumor activity of erlotinib (OSI-774, Tarceva) alone or in combination in human non-small cell lung cancer tumor xenograft models

B Higgins, K Kolinsky, M Smith, G Beck… - Anti-cancer …, 2004 - journals.lww.com
Our objective was the preclinical assessment of the pharmacokinetics, monotherapy and
combined antitumor activity of the epidermal growth factor receptor (HER1/EGFR) tyrosine …

Erlotinib in cancer treatment

MA Bareschino, C Schettino, T Troiani, E Martinelli… - Annals of oncology, 2007 - Elsevier
The epidermal growth factor receptor (EGFR) is a transmembrane tyrosine kinase (TK)
receptor that is frequently expressed in many epithelial tumors. The signaling pathways of …

Erlotinib (Tarceva®): a promising drug targeting epidermal growth factor receptor tyrosine kinase

AM Bulgaru, S Mani, S Goel… - Expert review of …, 2003 - Taylor & Francis
Overexpression of the epidermal growth factor receptor (EGFR) is correlated with a poor
prognosis in several human malignancies. In addition, cancers overexpressing EGFR …

Enhanced sensitivity to the HER1/epidermal growth factor receptor tyrosine kinase inhibitor erlotinib hydrochloride in chemotherapy-resistant tumor cell lines

Q Dai, YH Ling, M Lia, YY Zou, G Kroog, KK Iwata… - Clinical Cancer …, 2005 - AACR
Abstract Purpose: Erlotinib (Tarceva, OSI-774) is a potent and specific inhibitor of the
HER1/epidermal growth factor receptor (EGFR) tyrosine kinase. In phase II clinical studies …