A phase I/IIA pharmacokinetic (PK) and serial skin and tumor pharmacodynamic (PD) study of the EGFR irreversible tyrosine kinase inhibitor EKB-569 in combination with 5-fluorouracil (5FU), leucovorin (LV) and irinotecan (CPT-11) (FOLFIRI regimen) in patients (pts) with advanced colorectal cancer (ACC)

Casado, Esther; Folprecht, Gunnar; Paz-Ares, L.; Rojo, F.; Köhne, Claus‐Henning; Cortés-Funes, H.; Vauthier, J. M.; Zacharchuk, Charles; Baselga, J.; Tabernero, Josep

doi:10.1200/jco.2004.22.90140.3543

Cited by 16 publications

(6 citation statements)

References 0 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…53 A similar 38 percent response rate was seen in 39 evaluable first-line patients with advanced CRC treated with EKB-569 in combination with FOLFIRI. 54 PD158780 is a multitargeted reversible TKI that inhibits the entire ErbB family of receptor tyrosine kinases. It is currently undergoing early clinical testing with limited information available in CRC.…”

Section: Other Tkismentioning

confidence: 99%

EGFR-Targeted Therapies in Colorectal Cancer

Overman¹,

Hoff²

2007

Diseases of the Colon &Amp; Rectum

View full text Add to dashboard Cite

The management of colorectal cancer relies heavily on the combination of the pyrimidine analog antimetabolite 5-fluorouracil with the platinum-based drug oxaliplatin or the topoisomerase inhibitor irinotecan. Optimization of dosing and scheduling of these agents to improve response and survival continues to evolve. Meanwhile, the rational targeting of molecular signaling pathways that are involved in the etiology of malignancies is currently one of the most promising strategies in novel anticancer drug development. New classes of drugs that target the epidermal growth factor receptor are among the most clinically advanced molecular-targeted therapies and have shown efficacy in colorectal cancer. The current status of epidermal growth factor receptor-targeted therapeutic agents is reviewed, with emphasis on their role in the management of colorectal cancer.

show abstract

Section: Other Tkismentioning

confidence: 99%

EGFR-Targeted Therapies in Colorectal Cancer

Overman¹,

Hoff²

2007

Diseases of the Colon &Amp; Rectum

View full text Add to dashboard Cite

show abstract

“…The activity of the irreversible TKI, EKB-569, has been evaluated in the first-line setting in combination with front-line chemotherapy (FOLFOX4 and FOLFIRI) in two Phase I/II studies [81,82]. The efficacy results of these two studies did not show any meaningful clinical activity for these two combinations when compared with the results of chemotherapy alone.…”

Section: Egfr Tyrosine Kinase Inhibitorsmentioning

confidence: 97%

“…Tejpar (Phase I/II) First line EKB-569 plus FOLFOX4 11 36 [81] Casado (Phase I/IIA) First line EKB-569 plus FOLFIRI 39 38 [82] FOLFIRI: Biweekly irinotecan plus infusional 5-fluorouracil plus leucovorin; FOLFOX4: Biweekly oxaliplatin plus infusional 5-fluorouracil plus leucovorin; N/A: Not avaliable.…”

Section: Ekb-569mentioning

confidence: 99%

New approaches in systemic treatment of advanced colorectal cancer: the molecular targets era

Capdevila

Méndez²,

Macarulla

et al. 2007

Expert Review of Anticancer Therapy

View full text Add to dashboard Cite

The prognosis of advanced colorectal cancer remains poor in spite of the advances obtained in recent years with new therapeutic agents, new approaches in surgical procedures and new diagnostic methods. New treatments directed to molecular targets have emerged and are being developed to improve these results, but there is a need to optimize and define the best use of these new approaches. In this review, the authors examine the most important trials with monoclonal antibodies and tyrosine kinase inhibitors in the treatment of advanced colorectal cancer.

show abstract

“…Clinical trials with these two agents are ongoing, with the most recent reports on Phase I/IIA studies of EKB-569 in combination with conventional chemotherapy in patients with previously untreated advanced colorectal cancer. Two abstracts have indicated good tolerability and evidence of antitumour activity and EGFR inhibition in tumours [123,124].…”

Section: Irreversible Inhibitorsmentioning

confidence: 98%

Cancer therapies targeted to the epidermal growth factor receptor and its family members

Kane¹

2006

Expert Opinion on Therapeutic Patents

View full text Add to dashboard Cite

This review will provide an overview of therapeutic strategies that are targeted to the epidermal growth factor receptor (EGFR) network of signal transduction, with a focus on EGFR itself and the closely related Her-2/neu/ erbB2 (erbB2) receptor. EGFR is the founding member of the erbB family of receptor tyrosine kinases, type I membrane spanning proteins that bind a variety of peptide growth factor ligands and initiate signal transduction along multiple downstream pathways towards proliferation, survival and angiogenesis. EGFR and erbB2 are validated targets for anticancer therapy and several such targeted therapeutic agents are already approved for use in patients. These include monoclonal antibodies directed to the extracellular domains of one or more erbB receptor and small molecule inhibitors of their intracellular tyrosine kinase domains. The advantages and disadvantages of these agents, as well as new and emerging agents in this class of targeted therapeutics, will be discussed. Recent progress towards understanding the molecular and pharmacodynamic causes of treatment failure or success will also be addressed. Finally, the therapeutic potential of targeted combinations, those directed at multiple facets of erbB-family signalling and those targeted to erbB and non-erbB receptor systems, will be reviewed.

show abstract

Cited by 16 publications

References 0 publications

EGFR-Targeted Therapies in Colorectal Cancer

EGFR-Targeted Therapies in Colorectal Cancer

New approaches in systemic treatment of advanced colorectal cancer: the molecular targets era

Cancer therapies targeted to the epidermal growth factor receptor and its family members

Contact Info

Product

Resources

About