Chemical Compounds to Block a Specific KRAS Cancer Gene

This patent describes new chemical compounds designed to stop a specific mutated protein called KRAS G12C, which is often found in various cancers, potentially offering new ways to treat the disease.

What it covers

This patent describes new chemical compounds, generally referred to as Formula (I), and their pharmaceutically acceptable salts. These compounds are designed to stop or 'inhibit' the activity of a specific mutated protein called KRAS G12C. By blocking this protein, the compounds are intended to act as therapeutic agents to treat various types of cancer. The patent also covers pharmaceutical compositions containing these compounds and methods for using them in the therapy and prophylaxis of cancer. For example, a patient with lung cancer driven by the KRAS G12C mutation could receive a drug based on these compounds to slow or stop tumor growth. Without the specific claims, the precise chemical structures and their exact scope of protection are not detailed.

What it doesn't cover

• —Does not cover inhibitors for other specific KRAS mutations, such as KRAS G12D or KRAS G12V.
• —Does not cover cancer treatments that target different proteins or biological pathways unrelated to KRAS G12C.
• —Does not cover non-chemical methods of inhibiting KRAS G12C, such as gene editing or RNA interference.
• —Does not cover compounds that do not fall under the general chemical description of Formula (I) as implied by the abstract.
• —Does not cover treating cancers where the KRAS G12C mutation is not present.

The clever bit

The clever bit is identifying specific chemical structures (Formula I) that can selectively bind to and inhibit the KRAS G12C mutant protein. This is a significant challenge because KRAS is a small protein with a smooth surface, making it difficult for drugs to attach effectively. The compounds described here achieve this precise targeting.

Why it matters

The KRAS G12C mutation is a common driver in several difficult-to-treat cancers, including lung, colorectal, and pancreatic cancers. For decades, KRAS was considered 'undruggable,' meaning scientists struggled to find ways to block its activity with medicines. This patent contributes to the development of specific chemical compounds that can overcome this challenge, offering a new class of targeted therapies for patients with these specific mutations.

Real-world examples

• 1.Sotorasib (Lumakras)
• 2.Adagrasib (Krazati)
• 3.Targeted lung cancer therapies
• 4.Targeted colorectal cancer therapies