Synta Pharmaceuticals Corp. (NASDAQ: SNTA), a biopharmaceutical company
focused on discovering, developing, and commercializing small molecule
drugs to treat severe medical conditions, today announced that
preclinical results presented at the AACR-IASLC (American Academy of
Cancer Research – International Association for the Study of Lung
Cancer) Joint Conference based on work done at Synta and at the
Dana-Farber Cancer Institute in Boston showed that STA-9090, a potent,
synthetic inhibitor of heat shock protein 90 (Hsp90), demonstrated
potent activity against 100% of all non-small cell lung cancer cell
lines tested, including those with EGFR, HER2 or KRAS mutations
including the EGFR T790 mutation that is present in roughly 50% of cases
of erlotinib or gefitinib resistance.
“Taken together, the in vitro and in vivo results
presented at this conference demonstrate the potency, broad activity,
and safety profile of STA-9090, both as a single agent and in
combination with taxanes in NSCLC”
Synta is currently enrolling patients in a Phase 2 single-arm,
open-label, single-agent study of STA-9090 in patients with stage IIIB
or IV non-small cell lung cancer, with patient cohorts defined by the
genetic profile of their tumors.
STA-9090 potently inhibited cell proliferation in 24 out of 24 human
NSCLC lines tested irrespective of EGFR, HER2 or KRAS mutational status. In
vivo, STA-9090 stopped tumor growth in both Tarceva® (erlotinib)-sensitive
and Tarceva-resistant NSCLC xenograft models. In addition, in a HER2
positive adenosquamous lung cancer study, 3 out of 4 animals treated
with STA-9090 experienced partial responses as measured by MRI.
Analysis of protein expression showed that STA-9090 causes substantial
down-regulation of client proteins relevant to lung cancer growth and
proliferation including AKT, EGFR, MET, HER2, CDK4, and RAF1.