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Drug intelligence / Profile preview
itacitinib + ibrutinib
- Development stage
- Phase 2
- Lead developer
- Incyte
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Itacitinib + ibrutinib is an investigational combination of two oral small molecule inhibitors: itacitinib, a selective Janus kinase 1 (JAK1) inhibitor, and ibrutinib, an irreversible inhibitor of Bruton's tyrosine kinase (BTK) and interleukin-2–inducible kinase (ITK)[2][4][5][6]. - **Itacitinib** selectively inhibits JAK1, reducing signaling through pathways such as the JAK-STAT cascade, important in inflammation and growth of certain cancers, supporting anti-proliferative and anti-inflammatory effects[5]. - **Ibrutinib** covalently inhibits BTK, a key mediator of B-cell receptor signaling, preventing B-cell growth and survival; it also irreversibly inhibits ITK, modulating T-helper cell activity, and impacts downstream pathways including PLC-γ, ERK1/2, PI3K, and NF-κB[2][4][6]. This combination aims to provide enhanced anti-cancer efficacy by dual targeting of B-cell and inflammatory pathways, relying on synergistic suppression of malignant cell growth and immune modulation. Both drugs are orally administered and developed for various hematologic and solid tumors.
- Other names
- itacitinib + ibrutinib
02
Targets
BTK (Bruton tyrosine kinase)ERBB2 (Erb-b2 receptor tyrosine kinase 2)ITK (Interleukin 2-inducible T-cell kinase)JAK1 (Janus kinase 1)JAK3 (Janus kinase 3)
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