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Drug intelligence / Profile preview
pelabresib + ruxolitinib
- Development stage
- Phase 3
- Lead developer
- Novartis
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Pelabresib + ruxolitinib is a combination therapy currently evaluated for the treatment of myelofibrosis in patients who have not previously received a JAK inhibitor. Pelabresib is an oral, small molecule inhibitor of bromodomain and extraterminal domain (BET) proteins, targeting epigenetic regulation of genes involved in inflammation and fibrosis. Ruxolitinib is an oral, small molecule inhibitor of Janus kinase 1 and 2 (JAK1, JAK2), blocking pro-inflammatory signaling pathways. The dual inhibition demonstrated additive benefits in clinical trials, significantly increasing spleen volume reduction, improving symptom scores, and potentially modifying disease biology by reducing pro-inflammatory cytokine levels and improving bone marrow morphology compared with ruxolitinib alone[1][2][3][4][5][6].
- Brand names
- Jakafi (ruxolitinib)
- Other names
- pelabresib plus ruxolitinibBET inhibitor plus JAK inhibitor
02
Targets
BET (BET family proteins)JAK1 (Janus kinase 1)JAK2 (Janus kinase 2)BRD (Bromodomain-containing protein family)
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