Difference between revisions of "Imetelstat (Rytelo)"
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===[[Myelofibrosis]]=== | ===[[Myelofibrosis]]=== | ||
<!-- # '''Abstract:''' Kebede Begna, Rebecca R. Laborde, Mrinal M Patnaik, Terra L Lasho, Darci Zblewski, Christy Finke, Lauren Schimek, Betsy R. LaPlant, Curtis A. Hanson, Monic J. Stuart, Animesh Pardanani. Imetelstat, a Telomerase Inhibitor, Induces Morphologic and Molecular Remissions In Myelofibrosis and Reversal Of Bone Marrow Fibrosis. Blood Nov 2013,122(21)662 [http://www.bloodjournal.org/content/122/21/662 link to original abstract] --> | <!-- # '''Abstract:''' Kebede Begna, Rebecca R. Laborde, Mrinal M Patnaik, Terra L Lasho, Darci Zblewski, Christy Finke, Lauren Schimek, Betsy R. LaPlant, Curtis A. Hanson, Monic J. Stuart, Animesh Pardanani. Imetelstat, a Telomerase Inhibitor, Induces Morphologic and Molecular Remissions In Myelofibrosis and Reversal Of Bone Marrow Fibrosis. Blood Nov 2013,122(21)662 [http://www.bloodjournal.org/content/122/21/662 link to original abstract] --> | ||
| − | # Tefferi A, Lasho TL, Begna KH, Patnaik MM, Zblewski DL, Finke CM, Laborde RR, Wassie E, Schimek L, Hanson CA, Gangat N, Wang X, Pardanani A. A Pilot Study of the Telomerase Inhibitor Imetelstat for Myelofibrosis. N Engl J Med. 2015 Sep 3;373(10):908-19. [https://www.nejm.org/doi/full/10.1056/NEJMoa1310523 link to original article] [https:// | + | # Tefferi A, Lasho TL, Begna KH, Patnaik MM, Zblewski DL, Finke CM, Laborde RR, Wassie E, Schimek L, Hanson CA, Gangat N, Wang X, Pardanani A. A Pilot Study of the Telomerase Inhibitor Imetelstat for Myelofibrosis. N Engl J Med. 2015 Sep 3;373(10):908-19. [https://www.nejm.org/doi/full/10.1056/NEJMoa1310523 link to original article] [https://pubmed.ncbi.nlm.nih.gov/26332545 PubMed] |
===[[Essential thrombocythemia]]=== | ===[[Essential thrombocythemia]]=== | ||
| − | # Baerlocher GM, Oppliger Leibundgut E, Ottmann OG, Spitzer G, Odenike O, McDevitt MA, Röth A, Daskalakis M, Burington B, Stuart M, Snyder DS. Telomerase Inhibitor Imetelstat in Patients with Essential Thrombocythemia. N Engl J Med. 2015 Sep 3;373(10):920-8. [https://www.nejm.org/doi/full/10.1056/NEJMoa1503479 link to original article] [https:// | + | # Baerlocher GM, Oppliger Leibundgut E, Ottmann OG, Spitzer G, Odenike O, McDevitt MA, Röth A, Daskalakis M, Burington B, Stuart M, Snyder DS. Telomerase Inhibitor Imetelstat in Patients with Essential Thrombocythemia. N Engl J Med. 2015 Sep 3;373(10):920-8. [https://www.nejm.org/doi/full/10.1056/NEJMoa1503479 link to original article] [https://pubmed.ncbi.nlm.nih.gov/26332546 PubMed] |
[[Category:Drugs]] | [[Category:Drugs]] | ||
Revision as of 02:24, 25 February 2020
Mechanism of action
From NCI Drug Dictionary: The sodium salt of imetelstat, a synthetic lipid-conjugated, 13-mer oligonucleotide N3' P5'-thio-phosphoramidate with potential antineoplastic activity. Complementary to the template region of telomerase RNA (hTR), 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. Link to company website
Preliminary data
Myelofibrosis
- Tefferi A, Lasho TL, Begna KH, Patnaik MM, Zblewski DL, Finke CM, Laborde RR, Wassie E, Schimek L, Hanson CA, Gangat N, Wang X, Pardanani A. A Pilot Study of the Telomerase Inhibitor Imetelstat for Myelofibrosis. N Engl J Med. 2015 Sep 3;373(10):908-19. link to original article PubMed
Essential thrombocythemia
- Baerlocher GM, Oppliger Leibundgut E, Ottmann OG, Spitzer G, Odenike O, McDevitt MA, Röth A, Daskalakis M, Burington B, Stuart M, Snyder DS. Telomerase Inhibitor Imetelstat in Patients with Essential Thrombocythemia. N Engl J Med. 2015 Sep 3;373(10):920-8. link to original article PubMed