Imetelstat or GRN163L is a drug that blocks telomerase, and is already in clinical trials as a potential treatment for breast and lung cancer.Imetelstat is a short chain oligonucleotide that binds with high affinity and specificity to the catalytic site of telomerase, resulting in competitive inhibition of enzyme activity or cell death. Imetelstat demonstrated anti-tumor effects in a wide range of preclinical models of hematological and solid tumors. There are six ongoing phase I studies patients with solid tumors, chronic lymphoproliferative disease, multiple myeloma, lung and breast cancers, as a single agent or in combination with standard treatments.
Calin O. Marian, Steve K. Cho, Brian M. Mcellin, Elizabeth A. Maher, Kimmo J. Hatanpaa, Christopher J. Madden, Bruce E. Mickey, Woodring E. Wright, Jerry W. Shay, and Robert M. BachooThe Telomerase Antagonist, Imetelstat, Efficiently Targets Glioblastoma Tumor-Initiating Cells Leading to Decreased Proliferation and Tumor Growth
Clin Cancer Res January 1, 2010 16:154-163; Published OnlineFirst January 4, 2010; doi:10.1158/1078-0432.CCR-09-2850
Small Molecules in Oncology Imetelstat (GRN163L) – Telomerase-Based Cancer Therapy
Springer Berlin Heidelberg