Drug intelligence / Profile preview

pacritinib + rifampin

Development stage
Unknown
Lead developer
Sobi
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Pacritinib is an oral small molecule kinase inhibitor used to treat adults with intermediate or high-risk primary or secondary myelofibrosis (including post-polycythemia vera and post-essential thrombocythemia) who have low platelet counts. It selectively inhibits Janus kinase 2 (JAK2), FMS-like tyrosine kinase 3 (FLT3), interleukin-1 receptor-associated kinase 1 (IRAK1), and colony-stimulating factor 1 receptor (CSF1R). Pacritinib does not inhibit JAK1 at clinically relevant concentrations. Its mechanism of action involves blocking abnormal signaling pathways that drive excessive inflammation and proliferation in the bone marrow[4][5][6][7]. Rifampin is a broad-spectrum antibiotic primarily used to treat tuberculosis and other bacterial infections. It works by binding to the beta-subunit of bacterial DNA-dependent RNA polymerase, thereby inhibiting RNA synthesis essential for bacterial survival[8].

Brand names
VonjoRifadinRimactane
Other names
pacritinibrifampicin
02

Targets

JAK2 (Janus kinase 2)rpoB (DNA-directed RNA polymerase subunit beta)CSF1R (Macrophage colony-stimulating factor receptor)CYP3A4 (Cytochrome P450 3A4)IRAK1 (Interleukin-1 receptor-associated kinase 1)FLT3 (Fms related receptor tyrosine kinase 3)

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