索托拉西布，（Sotorasib）120mg
1. Composition:
Sotorasib is a targeted anti-cancer drug designed for the KRAS G12C mutation. The KRAS gene is one of the most common oncogenes in humans, and the mutated version KRAS G12C is a major driver of various cancers, especially non-small cell lung cancer (NSCLC) and certain types of colorectal cancer. Sotorasib specifically targets the KRAS G12C protein, inhibiting the growth and spread of cancer cells.
2. Indications:
- Anti-Cancer Activity: Sotorasib selectively kills cancer cells carrying the KRAS G12C mutation, showing significant efficacy particularly in patients with non-small cell lung cancer (NSCLC).
- Non-Small Cell Lung Cancer (NSCLC): Sotorasib is FDA-approved for the treatment of locally advanced or metastatic NSCLC with a KRAS G12C mutation, especially in patients who have failed at least one prior systemic therapy.
- Other KRAS G12C-Mutated Cancers: Although mainly used for NSCLC, Sotorasib has also shown potential in other KRAS G12C-mutated cancers, such as colorectal and pancreatic cancer.
3. Administration:
- Oral: Sotorasib is taken orally in tablet form, typically at a recommended dose of 960 mg once daily. It should be taken as directed by a physician and, if possible, at the same time each day. The drug can be taken with or without food.
- Treatment Cycle: The treatment cycle should be determined based on the patient’s tumor response, drug tolerance, and adverse reactions. Typically, treatment continues for several weeks or longer, with the exact duration decided by the doctor based on the patient’s condition.
4. Research & Development History:
- Development Background: Sotorasib is the world’s first approved drug targeting the KRAS G12C mutation, developed by Amgen. KRAS gene mutations have long been considered "undruggable" due to the smooth surface of the KRAS protein lacking obvious binding sites. However, after decades of effort, scientists finally developed molecular inhibitors that specifically target the KRAS G12C mutation. Sotorasib represents a major breakthrough in this field.
- Approval and Market Release**: Sotorasib was approved by the U.S. FDA in 2021 for the treatment of NSCLC with the KRAS G12C mutation, marking a milestone in KRAS-targeted therapy.
5. Mechanism of Action:
The KRAS G12C mutation causes continuous activation of the KRAS protein, promoting tumor cell growth and proliferation. Sotorasib irreversibly binds to the active site of the KRAS G12C protein, inhibiting its signal transduction function, thus blocking downstream cell proliferation pathways. This process effectively suppresses the growth of cancer cells dependent on KRAS G12C.
6. Summary:
Sotorasib is the world’s first targeted anti-cancer drug for the KRAS G12C mutation, demonstrating significant efficacy, particularly in the treatment of non-small cell lung cancer. By irreversibly binding to the KRAS G12C protein, Sotorasib effectively inhibits tumor cell growth and proliferation. Although its side effects are relatively mild, liver function monitoring and pulmonary toxicity are key considerations during its use.
