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KRASG12C proteins don’t quit
RAS mutations are among the most common mutations in cancer, found in approximately 25 percent of patients with cancer.1 Until recently, KRAS mutations had earned a reputation for being “undruggable”, but scientists have recently identified how to effectively target KRASG12C.2
About one-quarter of patients with non-small cell lung cancer (NSCLC) have a KRAS mutation, and G12C mutations make up about 14 percent of them. KRASG12C mutations are also found in many other difficult to treat cancers, and are historically associated with poor prognosis.2,3
“Despite advancements in the treatment of cancer, patients with a KRASG12C mutation are still in need of a targeted treatment with improved responses and sustained durability,” said Joseph Leveque, chief medical officer, Mirati Therapeutics, Inc. “KRAS mutations are found in an aggressive subset of cancers that have minimal treatment options. Although first generation KRAS inhibitors bind to and irreversibly inhibit the KRASG12C mutated protein, it is an underappreciated observation that new KRASG12C proteins regenerate every 24-48 hours. Thus, continuous drug levels and persistent inhibition of the KRASG12C mutant protein is needed to achieve maximum antitumor activity.”
Leveque continued, “It’s not enough to just turn KRAS mutants off transiently. The good news is the science is still evolving and new research may shed light on how to further optimize targeting these mutations in difficult to treat cancers.”
Despite advancements in the treatment of cancer, patients with a KRASG12C mutation are still in need of a targeted treatment with improved responses and sustained durability
Mirati launched KRAS Regeneration — a healthcare professional campaign in part to raise awareness of the KRASG12C mutation and what is needed to overcome the insidious nature of the mutation.
Visit KRASRegeneration.com to learn more.
References
- Chien, Shanley. Targeting the KRAS mutation for more effective cancer treatment. MDAnderson.org. Published February 12, 2021.
- Nassar AH, Adib E, Kwiatkowski DJ. Distribution of KRASG12C somatic mutations across race, sex, and cancer type. N Engl J Med. 2021; 384(2):185-187.
- Pakkala S, Ramalingam SS. Personalized therapy for lung cancer: Striking a moving target. JCI Insight. 2018;3(15):e120858.