AZD2171, under development by AstraZeneca International, is an oral tyrosine kinase inhibitor of all of the VEGF receptors (VEGFR1, VEGFR2, VEGFR3), as well as KIT and (less potently) PDGFRA and PDGFRB. Vascular endothelial growth factor (VEGF) is a stimulus of angiogenesis (growth of new blood vessels), which is required to support solid tumor growth. VEGFR binds to transmembrane receptor Flt-1 (VEGF-1) and KDR (VEGF-2), resulting in subsequent propagation of intracellular signaling and angiogenesis. With the exception of growth of the long bones during growth and cyclical changes in the female reproductive tissues, angiogenesis does not occur in healthy adults. Chronic inhibition of this process may therefore be tolerated and provide a means for achieving selective therapeutic intervention through prevention of tumor progression.
For a slide show (in pdf format) about AZD2171 at the manufacturer's website, click this link and then skip to page 10 of the presentation.
There is a Phase II international clinical trial of AZD2171 presently recruiting patients. The purpose of the trial is to evaluate the biological activity of AZD2171 as measured by FDG-PET response in patients with metastatic GIST resistant or intolerant to imatinib (Gleevec).
Trial Locations and Contact information
Research Site, London, United Kingdom; Recruiting
Research Site, Manchester, United Kingdom; Not yet recruiting
Trial Contact Information:
AstraZeneca Cancer Support Network 1-866-992-9276
To view information about the Phase II clinical trial for use of AZD2171 for GIST, click clinicaltrials.gov
For a PubMed search on AZD2171, click here.
Papers about AZD2171 presented at American Society of Clinical Oncology: link here
Click here for free access via PubMed to the paper "AZD2171: a highly potent, orally bioavailable, vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor for the treatment of cancer. "