Synonyms: GRN-163 | GRN163 | Rytelo®
imetelstat is an approved drug (FDA (2024))
Compound class:
Nucleic acid
Comment: Imetelstat is a lipid (palmitoyl) conjugated thio-phosphoramidate oligonucleotide-based telomerase (TERT) inhibitor [1]. It binds competitively to the RNA template region of the enzyme and blocks its catalytic action and its interaction with telomeres [3]. It was developed for the treatment of myeloid hematologic malignancies.
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References |
1. Asai A, Oshima Y, Yamamoto Y, Uochi TA, Kusaka H, Akinaga S, Yamashita Y, Pongracz K, Pruzan R, Wunder E et al.. (2003)
A novel telomerase template antagonist (GRN163) as a potential anticancer agent. Cancer Res, 63 (14): 3931-9. [PMID:12873987] |
2. Keam SJ. (2024)
Imetelstat: First Approval. Drugs, 84 (9): 1149-1155. [PMID:39162963] |
3. Lennox AL, Huang F, Behrs MK, González-Sales M, Bhise N, Wan Y, Sun L, Berry T, Feller F, Morcos PN. (2024)
Imetelstat, a novel, first-in-class telomerase inhibitor: Mechanism of action, clinical, and translational science. Clin Transl Sci, 17 (11): e70076. [PMID:39555853] |