KRAS Inhibitors

KRAS mutations are among the most common mutations in cancer, found in approximately 25 percent of patients. Until recently, KRAS mutations had earned a reputation for being “undruggable,” but scientists have identified how to effectively target KRAS^G12C.

KRAS mutations are among the most common mutations in cancer, found in approximately 25 percent of patients. Until recently, KRAS mutations had earned a reputation for being “undruggable,” but scientists have identified how to effectively target KRAS^G12C.

Scientific Rationale

KRAS acts as an on/off switch for cell growth. When functioning normally, it regulates cellular growth. When it is mutated, cells grow and spread out of control. These cells often develop into some of the deadliest cancers.^1,3

The KRAS mutation:

One of the first discovered oncogenes²

Identified more than 30 years ago^1,2

The most commonly mutated cancer-causing gene^2,4

Cancers stemming from RAS mutations account for nearly a quarter of all human cancers and contribute to 1 million deaths per year worldwide.^5,6

Mutations in KRAS are the most common, accounting for 85 percent of all RAS mutations.⁵

Unmet Need

Targeted treatment options have been approved for many mutations that cause cancer—except KRAS. KRAS mutations rarely co-occur with other, more treatable cancer-causing mutations.³ There are hundreds of thousands of patients with a KRAS mutation who are currently without a targeted treatment option. Patients with these mutations typically have a poor prognosis and resistance to standard of care treatment options.² Patients with this mutation still face an unmet medical need.

KRAS^G12C by the numbers:

KRAS^G12C is estimated to impact >70,000 patients in the U.S. and Europe^7,8

Occurs in 14% of non-small cell lung cancer patients with approximately

44,000
patients

in the U.S. and Europe^7,9

Occurs in 3-4% of colorectal cancer patients with approximately

20,000
patients

in the U.S. and Europe⁷

Occurs in 2% of pancreatic cancer patients with approximately

4,000
patients

in the U.S. and Europe^7,10

KRAS^G12D by the numbers:

KRAS^G12D is estimated to impact 180,000 patients in the U.S. and Europe^7,8

Occurs in 36% of pancreatic cancer patients with approximately

70,000
patients

in the U.S. and Europe^7,10

Occurs in 12% of colorectal cancer patients with approximately

80,000
patients

in the U.S. and Europe⁷

Occurs in 6% of endometrial cancer patients with approximately

15,000
patients

in the U.S. and Europe⁷

Occurs in 4% of NSCLC adenocarcinoma patients with approximately

13,000
patients

in the U.S. and Europe^7,9