Drug intelligence / Profile preview

imetelstat + bortezomib + dexamethasone

Development stage
Phase 1
Lead developer
Geron
Modality
Small Interfering RNA (siRNA) → Small RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, MicroRNA (miRNA) → Small RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Antisense Oligonucleotides (ASOs) → Long RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Antisense DNA → DNA Therapeutics → Nucleic Acid Therapeutics, Small Molecules
Administration
Intravenous, Subcutaneous, Oral
01

Overview

**imetelstat + bortezomib + dexamethasone** is an investigational combination regimen for the treatment of hematologic malignancies. - **Imetelstat** is a telomerase inhibitor that binds to the RNA template of telomerase (TERC), leading to direct and selective inhibition of telomerase activity, which can result in cell death in certain malignant cells. - **Bortezomib** is a reversible proteasome inhibitor that disrupts the 26S proteasome, leading to cellular apoptosis, particularly in myeloma and some lymphoma cells. - **Dexamethasone** is a synthetic glucocorticoid with anti-inflammatory and immunosuppressive effects, frequently used in hematological cancer regimens to promote cell death and manage side effects. The combination is designed to leverage distinct yet potentially complementary anti-myeloma mechanisms. While bortezomib plus dexamethasone is a well-established standard of care for multiple myeloma, the addition of imetelstat is being explored for its novel mechanism targeting telomerase, which may help overcome resistance or enhance antitumor activity. The regimen remains investigational for most indications and is undergoing early-phase clinical evaluation primarily in multiple myeloma and other related malignancies.

02

Targets

GR (Glucocorticoid receptor)Telomerase (Human telomerase)PSMB5 (Proteasome subunit beta Type-5)TERT (Telomerase)

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