Imetelstat

ATC Code L01XX80

Imetelstat

Definition

A synthetic lipid-conjugated, 13-mer oligonucleotide N3'-P5'-thio-phosphoramidate with potential antineoplastic activity. Complementary to the template region of telomerase (hTR) RNA, imetelstat acts as a competitive enzyme inhibitor that binds and blocks the active site of the enzyme (a telomerase template antagonist), a mechanism of action which differs from that for the antisense oligonucleotide-mediated inhibition of telomerase activity through telomerase mRNA binding. Inhibition of telomerase activity in tumor cells by imetelstat results in telomere shortening, which leads to cell cycle arrest or apoptosis.

Also known as DNA, d(3'-amino-3'-deoxy-P-thio)(T-A-G-G-G-T-T-A-G-A-C-A-A), 5'-[O-[2-hydroxy-3- [(1-oxohexadecyl)amino]propyl] hydrogen phosphorothioate], GRN 163L, GRN-163L, IMETELSTAT — per NCIT

Also identified as