Mobutinib is an oral epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. By selectively binding and inhibiting receptors with EGFR exon 20 insertion mutations, abnormal signaling pathways are blocked, tumor cell proliferation and growth are inhibited, and anti-tumor effects are exerted, providing a new treatment option for non-small cell lung cancer patients carrying this mutation.

1、 Drug name

1. Product Name: EXKIVITY

2. Common name: Mobocetinib

2、 Indications

Mobutinib is suitable for the treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC) adult patients with epidermal growth factor receptor (EGFR) exon 20 insertion mutations, who have experienced disease progression after platinum based chemotherapy and whose mutations have been confirmed through FDA approved testing methods.

3、 Specifications and characteristics

Specification: 40mg capsules.

Characteristic: Oral capsule formulation.

4、 Main components

1. Active ingredient: Mobocetinib

2. Accessories: The capsule shell contains gelatin and titanium dioxide, and the printing ink contains cordyceps, dehydrated alcohol, isopropanol, butanol, propylene glycol, concentrated ammonia solution, black iron oxide, potassium hydroxide, and purified water.

5、 Usage and dosage

1. Recommended dosage: 160mg once daily, orally, can be taken with food or separately.

2. Administration method: Swallow the whole capsule, do not open, chew or dissolve the contents of the capsule.

6、 Dose adjustment

1. Adjust the dosage according to the severity of adverse reactions, reducing it to 120mg once daily for the first dose and 80mg once daily for the second dose.

2. For QTc interval prolongation, decide whether to suspend medication, reduce dosage, or permanently discontinue medication based on the severity.

3. For moderate CYP3A inhibitors, if co administration is unavoidable, the dose of Mobotinib should be reduced by about 50% and restored to its original dose after 3-5 half lives of discontinuation of the inhibitor.

7、 Medication precautions

1. Before and after meals: Mobotinib should be taken with or without food, but at a fixed daily time.

2. Missed dose: If missed for more than 6 hours, skip the dose and take the next dose according to the original plan the next day.

3. Vomiting: If vomiting occurs after taking medication, there is no need for additional supplementation. The next dose should be taken according to the original plan the next day.

8、 Medication for special populations

1. Pregnant women: Mobutinib may be harmful to the fetus and should not be used in pregnant women.

2. Breastfeeding women should not breastfeed during the treatment period or within one week after discontinuing medication.

3. Reproductive potential women and men: It is recommended that women with reproductive potential use effective non hormonal contraceptive measures during treatment and within one month after discontinuation of medication; It is recommended that female partners of male patients use effective contraceptive measures during treatment and within one week after discontinuation of medication.

4. Children: The safety and efficacy of Mobutinib in children have not been established.

5. Elderly: There is no significant difference in overall effectiveness among patients aged 65 and above, but the incidence of grade 3 and above adverse reactions and severe adverse reactions is higher in patients aged 65 and above.

6. Liver and kidney dysfunction: Patients with mild to moderate liver and kidney dysfunction do not need to adjust the dosage, and the recommended dosage for patients with severe liver and kidney dysfunction has not yet been determined.

9、 Adverse reactions

1. Common adverse reactions (>20%): diarrhea, rash, nausea, stomatitis, vomiting, decreased appetite, paronychia, fatigue, dry skin, and musculoskeletal pain.

2. Common (≥ 2%) grade 3 or 4 laboratory abnormalities: decreased lymphocytes, increased amylase, increased lipase, decreased potassium, decreased hemoglobin, increased creatinine, and decreased magnesium.

3. Serious adverse reactions: including QTc interval prolongation with apical torsion transition ventricular tachycardia, interstitial lung disease (ILD)/pneumonia, cardiac toxicity, diarrhea, etc.

10、 Contraindications

Mobutinib has no absolute contraindications.

11、 Drug interactions

1. CYP3A inhibitors: Avoid co administration with potent or moderate CYP3A inhibitors. If unavoidable, reduce dosage and strengthen QTc monitoring.

2. CYP3A inducers: Avoid co administration with potent or moderate CYP3A inducers as it may reduce the efficacy of Mobotinib.

3. Medications that prolong QTc: Avoid co administration with other drugs known to prolong QTc intervals to increase the risk of cardiac events.

12、 Storage method

Stored at 20 ° C to 25 ° C (68 ° F to 77 ° F), with a permissible temperature fluctuation range of 15 ° C to 30 ° C (59 ° F to 86 ° F).

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