EGFR and WZ4002

I can’t tell you how excited I am about what researchers recently discovered at Dana Farber Cancer Center.

Currently non-small cell lung cancer patients taking Tarceva (erlotnib) who have a response to the drug can expect an average response time of only 9 months. Pasi A. Jänne, MD, PhD of Dana Farber and Brigham and Women’s Hospital (BWH) has discovered a new medication, WX4002, that could eventually be used once the Erlotnib no longer works. And in fact, the new drug is expected to have fewer side effects.

“Dana-Farber investigators hypothesized that current agents lose their potency because they don’t bind as tightly or fully to the EGFR T790M protein as they ideally should. To improve the fit, researchers led by chemical biologist Nathanael Gray, PhD, prepared a group of inhibitors with a different structural scaffold, known as a pyrimidine core, which, it was thought, would mesh more thoroughly. They lab-tested the agents in NSCLC cells with EGFR T90M and found several that were up to 100 times more potent than quinazolines in restricting cell growth. As an unexpected bonus, these compounds were nearly 100 times less powerful at slowing the growth of cells with normal EGFR, suggesting they would be less likely to produce side effects than current drugs. The agent which performed the best is the pyrimidine WZ4002.”  – MORE

Let’s pray that they can develop this drug, get it approved by the FDA and get it to market quickly so that those patients currently on Tarceva can continue to survive.

Read the full article here.