telomerase-inhibitor-ix

Overview

Telomerase Inhibitor IX is an experimental small-molecule inhibitor of TERT (telomerase reverse transcriptase). It has been evaluated preclinically in acral lentiginous melanoma (ALM) cell lines with TERT copy-number gains or promoter mutations.

Evidence in the corpus

  • 2.5 µM Telomerase Inhibitor IX for 72 h produced ≥75% loss of viability in two primary ALM cell lines (SMC-09 with TERT copy-number gain; SU2C-001-002 with homozygous TERT promoter mutation Chr5:1,295,113:G>A) versus only ~12% loss in normal melanocyte controls (NHM-002); TERT mRNA dropped ≥25% in ALM lines and was undetectable in the normal control; proposed as a putative therapeutic strategy for ALM given limited targeted treatment options PMID:28373299.

Resistance mechanisms

  • Not reported in corpus.

Cancer types (linked)

  • MEL (acral lentiginous melanoma subtype)

Sources

  • PMID:28373299 — ALM genomic study (n=34); Telomerase Inhibitor IX selectively cytotoxic to TERT-altered ALM cell lines at 2.5 µM (≥75% viability loss vs ~12% in normal melanocytes).

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