Sotorasib is an oral small molecule targeted inhibitor that specifically inhibits GTPase activity and blocks abnormal activation of the RAS signaling pathway by covalently binding to the switch pocket of KRAS G12C mutant protein.

1、 Drug name

1. Common name: Sotorasib

2. Product Name: LUMAKRAS ™

2、 Indications

Used to treat adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) confirmed by FDA approved testing to have KRASG12C mutations, and who have received at least one previous systemic treatment. This indication was granted accelerated approval based on overall response rate (ORR) and duration of response (DOR).

3、 Specifications and characteristics

1. Specification: 120mg per piece

2. Appearance: Tablets.

4、 Main components

Active ingredient: Sotolabib (molecular formula C30H30F2N6O3). Auxiliary materials include microcrystalline cellulose, lactose monohydrate, cross-linked carboxymethyl cellulose sodium, magnesium stearate, etc.

5、 Usage and dosage

1. Recommended dose: 960mg (8 tablets) orally once daily until disease progression or intolerable toxicity occurs.

2. Usage: Swallow the whole tablet, it can be taken with food or on an empty stomach. If dispersed, the tablets can be added to 120mL of non carbonated room temperature water and stirred until dispersed before drinking immediately, and consumed within 2 hours.

3. Omission treatment: If the missed dose exceeds 6 hours, the dose will be skipped and the medication will be taken according to the original plan the next day, and cannot be supplemented.

4. Vomiting treatment: Vomiting after taking medication does not require supplementation, and the original dose should be continued the next day.

6、 Dose adjustment

1. Hepatotoxicity or adverse reactions: Suspend, reduce dosage (first to 480mg/day, second to 240mg/day) or permanently discontinue medication based on severity.

2. Interstitial lung disease (ILD): Suspected ILD requires immediate discontinuation of medication, and permanent discontinuation upon diagnosis.

7、 Medication precautions

1. Dietary impact: A high-fat diet may increase drug exposure by 25%, but there is no need for deliberate adjustment.

2. Gastric acid regulator: Avoid combination with proton pump inhibitors (PPIs) or H2 receptor antagonists. When combined, an interval of 4 hours (antacids) or 10 hours (H2 antagonists) is required.

3. Drug interactions: Avoid co administration with strong CYP3A4 inducers, CYP3A4 substrates, or P-gp substrates as they may affect efficacy or increase toxicity.

8、 Medication for special populations

1. Pregnant woman: No human data available, animal experiments have not shown teratogenicity, but risks need to be weighed.

2. Breastfeeding period: Avoid breastfeeding during treatment and within one week after the last dose.

3. Elderly: No need to adjust dosage.

9、 Adverse reactions

1. Common (≥ 20%) symptoms include diarrhea, musculoskeletal pain, nausea, fatigue, hepatotoxicity, and cough. Laboratory abnormalities include decreased lymphocytes, decreased hemoglobin, elevated transaminase, etc.

2. Serious adverse reactions include pneumonia (8%), hepatotoxicity (3.4%), etc.

10、 Contraindications

There are no clear contraindications.

11、 Drug interactions

1. Strong CYP3A4 inducer: Reduce the concentration of sotaloxib and avoid combination therapy.

2. CYP3A4/P-gp substrates: It may be necessary to adjust the dosage of combination therapy (such as digoxin).

12、 Storage method

Store at room temperature of 20 ° C to 25 ° C (68 ° F to 77 ° F), with short-term fluctuations of 15 ° C to 30 ° C (59 ° F to 86 ° F) allowed.

Sotorasibinformation