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Brepocitinib is an oral TYK2/JAK1 inhibitor indicated for dermatomyositis in adults, acting through inhibition of cytokine-induced STAT phosphorylation to reduce immune-mediated muscle and skin inflammation. It inhibits TYK2- and JAK1-mediated cytokine signaling, blocking phosphorylation of signal transducers and activators of transcription (STATs) that regulate immune cell function.
- Mechanism
- Curator reviewed · 4 references
Brepocitinib is a Janus kinase (JAK) and tyrosine kinase 2 (TYK2) inhibitor. In a cell-free isolated enzyme assay, brepocitinib showed greater inhibitory potency at TYK2 and JAK1 than at JAK2 and JAK3. JAKs are cytoplasmic tyrosine kinases that mediate signal transduction from cytokine receptors, phosphorylating and activating signal transducers and activators of transcription (STATs), which in turn modulate intracellular activity including gene expression. In human cellular assays, brepocitinib inhibited TYK2- and JAK1-mediated cytokine-induced STAT phosphorylation, including signaling through TYK2/JAK1, TYK2/JAK2, JAK1/JAK3, and TYK2/JAK1/JAK2 pairings.
- Primary indication
- Brepocitinib is indicated for the treatment of dermatomyositis in adult patients.Curator reviewed · 1 structured indication
- Formula / weight
- C18H21F2N7O · 389.411 g/mol (avg)
- Code names
- PF-06700841
Resolves to
BUWBRTXGQRBBHG-MJBXVCDLSA-NSMILESCN1C=C(NC2=NC=CC(=N2)N2C[C@@H]3CC[C@H](C2)N3C(=O)[C@@H]2CC2(F)F)C=N1What you can answer from here — as of September 23, 2026
Which drugs share a target with Brepocitinib, and which of those have an active Phase 3 trial?