Drug intelligence / Profile preview

pacritinib + momelotinib

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

pacritinib + momelotinib is a theoretical combination of two oral small‑molecule Janus kinase (JAK) inhibitors being individually used and studied for the treatment of myelofibrosis, particularly in patients with anemia and/or thrombocytopenia. Pacritinib is a selective inhibitor of JAK2, fms-related receptor tyrosine kinase 3 (FLT3), and interleukin-1 receptor–associated kinase 1 (IRAK1), with additional inhibition of the ACVR1 pathway, and is approved in the United States for patients with myelofibrosis and severe thrombocytopenia.[1][3] Momelotinib is an oral inhibitor of JAK1, JAK2, and ACVR1 that has demonstrated improvements in splenomegaly, constitutional symptoms, and anemia, including transfusion independence, in phase 3 trials in myelofibrosis.[1][5][8] While these two agents have been compared indirectly and in real‑world analyses for safety, anemia benefit, and survival, there are no clinical data or an approved product combining pacritinib and momelotinib into a single co‑formulated therapy; thus, this represents a conceptual drug combination rather than a defined pharmaceutical product.[1][2][4][9][11][12]

02

Targets

ACVR1 (Activin receptor type I)FLT3 (Fms related receptor tyrosine kinase 3)IRAK1 (Interleukin-1 receptor-associated kinase 1)JAK1 (Janus kinase 1)JAK2 (Janus kinase 2)

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