KRAS Inhibitors

Cancer-causing KRAS mutations have evaded drug discovery and development efforts for over 30 years,2,4 but our novel approach is bringing us one step closer to providing an effective treatment for these patients.

Cancer-causing KRAS mutations have evaded drug discovery and development efforts for over 30 years,2,4 but our novel approach is bringing us one step closer to providing an effective treatment for these patients.

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.3

The KRAS mutation:

One of the first discovered oncogenes2,4
Identified more than 30 years ago2,4
The most commonly mutated oncogene2,4

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

Mutations in KRAS are the most common, accounting for 85% 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 These patients represent an extraordinary unmet need.

KRASG12C by the numbers:

KRASG12C is estimated to impact >70,000 patients in the U.S. and Europe6,7

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

44,000
patients6,8

Occurs in 3-4% of colorectal cancer patients

20,000
patients6

Occurs in 2% of pancreatic cancer patients

4,000
patients6

KRASG12D by the numbers:

KRASG12D is estimated to impact 180,000 patients in the U.S. and Europe6,7

Occurs in 36% of pancreatic cancer patients

70,000
patients6

Occurs in 12% of colorectal cancer patients

80,000
patients6

Occurs in 6% of endometrial cancer patients

15,000
patients6

Occurs in 4% of NSCLC adenocarcinoma patients

13,000
patients6,8

Adagrasib (MRTX849)
Adagrasib (MRTX849)

Mirati is developing adagrasib, an investigational, highly selective, potent and optimized KRASG12C inhibitor.

MRTX1133
MRTX1133

Mirati is developing an investigational, highly selective and potent small molecule inhibitor of KRASG12D, called MRTX1133.