Dosing & Uses
Myelofibrosis
Pending FDA approval for treating and reducing key hallmarks of myelofibrosis (eg, anemia, splenomegaly)
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Pharmacology
Mechanism of Action
Inhibits signals along 3 pathways – Janus kinase (JAK) 1, JAK2, and activin A receptor type 1 (ACVR1)
Competes with JAK1/2 for ATP binding, which may result in inhibition of JAK1/2 activation, inhibition of the JAK-STAT signaling pathway, and therefore, induction of apoptosis and a reduction of tumor cell proliferation in JAK1/2-expressing tumor cells
JAK2 is the most common mutated gene in bcr-abl-negative myeloproliferative disorder
ACVR1 is a protein which in humans is encoded by the ACVR1 gene; also known as ALK-2 (activin receptor-like kinase-2); transduces signals of bone morphogenetic protein (BMP)
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Images
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Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.
