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imetelstat + momelotinib
- Development stage
- Preclinical
- Lead developer
- Geron
- Modality
- Small Molecules, 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 Interfering RNA (siRNA) → Small RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics
- Administration
- Intravenous, Oral
01
Overview
A combination of **imetelstat**, a first-in-class direct competitive inhibitor of telomerase, and **momelotinib**, an oral Janus kinase (JAK) 1/2 inhibitor, investigated for the treatment of myelofibrosis (MF). Imetelstat targets telomerase (reverse transcriptase), disrupting malignant hematopoietic stem cell function by limiting proliferation and survival, thus exhibiting disease-modifying potential. Momelotinib blocks JAK1 and JAK2 signaling, reducing pro-inflammatory cytokine production and improving anemia through effects on hepcidin and iron homeostasis. Both drugs are being developed to address the unmet needs in MF, particularly for disease modification and symptom improvement. The combination has not been widely studied together in formal trials as of the current date, but both agents have been used in MF populations, typically individually or in combinations with other JAK inhibitors.
- Other names
- imetelstat + momelotinib
02
Targets
TYK2 (Tyrosine kinase 2)JAK2 (Janus kinase 2)PKD (Protein kinase D family)TBK1 (TANK binding kinase 1)ROCK2 (Rho-associated coiled-coil containing protein kinase 2)JAK1 (Janus kinase 1)JNK (Mitogen-activated protein kinase kinase kinase family)CDK2 (Cyclin-dependent kinase 2)ACVR1 (Activin receptor type I)FLT3-ITD (Fms-like tyrosine kinase 3 with internal tandem duplication)TERT (Telomerase)
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