Drug intelligence / Profile preview

imetelstat + lenalidomide

Development stage
Unknown
Lead developer
Geron
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

Imetelstat + lenalidomide is an investigational combination of two small molecule drugs: **imetelstat**, a first-in-class, intravenously administered telomerase inhibitor (brand name Rytelo), and **lenalidomide**, an oral immunomodulatory agent (brand name Revlimid). - **Imetelstat** acts by inhibiting telomerase, an enzyme that maintains telomere length, leading to decreased proliferation and apoptosis of malignant hematopoietic progenitor cells. It is primarily approved for transfusion-dependent anemia in adults with low- to intermediate-1 risk myelodysplastic syndromes (MDS) with inadequate response to erythropoiesis-stimulating agents[3][4][7]. - **Lenalidomide** is an immunomodulator that inhibits the proliferation of abnormal hematopoietic cells, alters cytokine production, and stimulates immune responses. It is approved and widely used for multiple myeloma, del(5q) MDS, and other hematologic malignancies. The combination has been evaluated in clinical research, including open-label studies in multiple myeloma, where imetelstat was investigated as monotherapy or in combination with lenalidomide maintenance therapy, primarily to assess safety, pharmacokinetics, and antitumor activity[3]. There is no evidence of regulatory approval for the combination, and its use is investigational.

02

Targets

Telomerase (Human telomerase)IKZF3 (Zinc finger protein Aiolos)IKZF1 (Ikaros family zinc finger protein 1)CRBN (Cereblon)

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