Data (unaudited) from cohort 1 (100mg), cohort 2 (200mg) and cohort 3
(300mg) were presented today and the key findings by investigators include:
-- Preliminary clinical activity observed in most subjects, including:
- Reduction in spleen size of 33 to 100% in five of six patients
- Reduction in erythropoietin-independent colony formation of up to
39% and up to 100% in two patients evaluated
-- Relief of constitutional symptoms, including pruritus, fatigue, back
pain and abdominal fullness
-- Reduction in the number of cells with the JAK2 V617F mutation (allele
-- Correlation between XL019 exposure and decreases in phosphorylation of
STAT, a marker for JAK activity.
-- XL019 was generally well tolerated.
- Adverse events included Grade 1 nausea, headaches, equilibrium
imbalance, dizziness, chest discomfort, visual disturbances, fatigue
- Grade 2 AEs of lightheadedness and decreased sensation in soles and
one serious adverse event of confusion in a patient with baseline
history of dementia were also observed.
-- No evidence of myelosuppression
The maximum tolerated dose has not been reached. The phase 1 dose escalating clinical trial continues.
About JAK2 and XL019
JAK kinases are activated by cytokines and growth factor receptors and
phosphorylate members of the STAT family of inducible transcription
factors. JAK2 plays a pivotal role in the cellular response to growth
factors that drive blood cell expansion, including erythrop
|SOURCE Exelixis, Inc.|
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