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.