Medical Information

Sotorasib, as a KRASG12C mutation specific inhibitor, has shown significant efficacy in the treatment of non-small cell lung cancer and colorectal cancer, delaying disease progression and improving progression free survival. Its effectiveness is mainly reflected in targeted inhibition of mutant proteins, indication coverage, and combination therapy regimens.

Targeted therapy effect

Sotolabib specifically inhibits GTPase activity by covalently binding to the switch pocket of KRASG12C mutant protein, effectively blocking abnormal activation of the RAS signaling pathway. This mechanism gives it a highly selective inhibitory effect on tumors carrying the mutation.

2 Indications and Efficacy

(1) Non small cell lung cancer

As a second-line monotherapy for KRASG12C mutant NSCLC, clinical trials have shown that it can significantly prolong the progression free survival of patients, with an objective response rate of 32% and a median response duration of 11.1 months.

(2) Colorectal cancer

In 2025, the FDA approved the combination therapy with pembrolizumab for the treatment of metastatic colorectal cancer, which increased the disease control rate to 85.7% and significantly improved the efficacy compared to monotherapy.

3 Pharmacokinetic characteristics

The oral bioavailability of the drug is good, with a median peak time of 1 hour and a steady-state concentration of 22 days. Food has little impact, and patients with mild to moderate liver and kidney function damage do not need to adjust the dosage, ensuring the stability of the treatment effect.

4. Durability of therapeutic effects

The half-life of the drug is 5 hours, mainly excreted through feces (74%). Clinical data shows that its anti-tumor effect can last for a long time, and some patients can achieve long-term disease control.

5. Medication cycle of sotaloxib

(1) Basic medication principle: Sotolabib, as a targeted therapy drug, needs to be taken for a long time to continuously inhibit tumor growth. Clinical advice is to take it orally at a fixed time every day until the disease worsens or serious adverse reactions occur.

(1) Evaluation of treatment effectiveness: Regular monitoring of tumor markers and imaging changes is required during medication. If the disease is stable or relieved, continue with the original plan; If there is progress, the treatment strategy needs to be adjusted.

6 key factors affecting medication duration

(1) Adverse reaction management: permanent discontinuation of medication is required in cases of grade 3-4 hepatotoxicity, interstitial lung disease, etc; Other levels 3-4 toxicity may be restored to medication after dose adjustment.

(2) Individual differences: Although elderly people do not need to adjust their dosage, their liver and kidney function needs to be monitored more frequently, which may affect the feasibility of long-term medication.

(3) Drug expiration date: The expiration date of sotaloxib is 24 months. Long term use should pay attention to the storage conditions and expiration date of the drug.