The most common adverse events (AEs) attributed to either vemurafenib or GDC-0973 in the 70 patients treated to date were: non-acneiform rash (52.9%; 7.1% Grade 3 or 4), diarrhea (51.4%; 5.7%), photosensitivity/sunburn (31.4%; 0%), fatigue (30.0%; 1.4%), and nausea (28.6%; 1.4%). Selected AEs attributed to either vemurafenib or GDC-0973 were: creatinine phosphokinase elevation (20.0%; 4.3%), liver function test elevation (20.0%; 4.3%), arthralgia (12.9%; 1.4%), serous choreoretinopathy (4.3%; 0%), and cutaneous squamous cell carcinoma (1.4%; 1.4%).
Temporary interruptions in vemurafenib, GDC-0973, or the combination of both agents were reported in 24.3%, 21.4%, and 8.6% of patients, respectively. One patient receiving the combination discontinued vemurafenib permanently because of QT interval prolongation. No patients receiving the combination of vemurafenib and GDC-0973 discontinued treatment due to an adverse event.
All 24 BRAFi-naïve patients evaluable for tumor responses had a decrease in tumor size from baseline, however, further follow-up is required to determine the confirmed objective response rate.
About GDC-0973 (XL518)GDC-0973 is a potent, highly selective inhibitor of MEK, a serine/threonine kinase that is a component of the RAS/RAF/MEK/ERK pathway. This pathway mediates signaling downstream of growth factor receptors, and is prominently activated in a wide variety of human tumors. In preclinical studies, oral dosing of GDC-0973 resulted in potent and sustained inhibition of MEK in RAS or BRAF mutant tumor models. GDC-0973 is being developed by Genentech, a member of the Roche Group under a collaboration agreement with Exelixis. About Collaboration Exelixis discovered GDC-0973 (XL518) internally and advanced the compound to investigational new drug (IND) status. In late 2006, Exelixis entered into a worldwide co-development agreement with Genentech, under which Exelixis received initial upfront and milestone payments for signing the agreement and submitting the IND. Exelixis was responsible for development of GDC-0973 through the end of Phase I, at which point Genentech exercised its option to further develop the compound.
Select the service that is right for you!COMPARE ALL SERVICES
Jim Cramer and Stephanie Link actively manage a real portfolio and reveal their money management tactics while giving advanced notice before every trade.
- $2.5+ million portfolio
- Large-cap and dividend focus
- Intraday trade alerts from Cramer
- Weekly roundups
Access the tool that DOMINATES the Russell 2000 and the S&P 500.
- Buy, hold, or sell recommendations for over 4,300 stocks
- Unlimited research reports on your favorite stocks
- A custom stock screener
- Upgrade/downgrade alerts
Jim Cramer's protege, David Peltier, identifies the best of breed dividend stocks that will pay a reliable AND significant income stream.
- Diversified model portfolio of dividend stocks
- Alerts when market news affect the portfolio
- Bi-weekly updates with exact steps to take - BUY, HOLD, SELL
All of Real Money, plus 15 more of Wall Street's sharpest minds delivering actionable trading ideas, a comprehensive look at the market, and fundamental and technical analysis.
- Real Money + Doug Kass + 15 more Wall Street Pros
- Intraday commentary & news
- Ultra-actionable trading ideas
Our options trading pros provide daily market commentary and over 100 monthly option trading ideas and strategies to help you become a well-seasoned trader.
- 100+ monthly options trading ideas
- Actionable options commentary & news
- Real-time trading community
- Options TV