PIPELINE
Scientific Approach
XL184
XL147
XL765
XL518
XL228
XL139
XL413
XL888
XL880
XL281
XL652
XL550
FXR

 

XL019

Development Status

A phase 1 trial in patients with myelofibrosis is ongoing.

Indications

Hematological Malignancies

Principal Targets

Cell proliferation, differentiation, migration, and survival: JAK2

  • Activating mutations of JAK2 occur frequently in a variety of myeloproliferative disorders including:
    • Polycythemia vera
    • Essential thrombocytosis
    • Idiopathic myelofibrosis
  • JAK2 signaling is upregulated in several types of lymphoma and a number of solid tumors.

XL019 Targets

Preclinical Data

XL019 is a selective inhibitor of JAK2, a cytoplasmic tyrosine kinase. JAK2 is activated by cytokine and growth factor receptors, and phosphorylates members of the STAT family of inducible transcription factors. Activation of the JAK/STAT pathway promotes cell growth and survival, and is a common feature of human tumors. JAK2 is activated by mutation in the majority of patients with polycythemia vera, myelofibrosis, and essential thrombocythemia, and appears to drive the inappropriate proliferation of blood cells in these conditions. XL019 is a potent and selective JAK2 inhibitor with favorable pharmacodynamic properties.

Information on Clinical Trials

Information about ongoing clinical trials of Exelixis' investigational product candidates is available at ClinicalTrials.gov, a service of the U.S. National Institutes of Health. General information about clinical trials and issues related to participating in clinical trials also is available at ClinicalTrials.gov.

Related Publications

For publication information related to this compound, please see the Related Publications page.