Cobitinib (Cotellic) ®) It is a multi kinase inhibitor that selectively inhibits the activity of MEK1 and MEK2 kinases, blocks the RAS/RAF/MEK/ERK signaling pathway, and thus inhibits the proliferation and survival of tumor cells.

1、 Drug name

Cobimetinib, also known as COTELLIC.

2、 Indications

Used to treat unresectable or metastatic melanoma with BRAFV600E or V600K mutation positivity, it should be used in combination with vemurafenib. Not applicable to patients with wild-type BRAF melanoma.

3、 Specifications and characteristics

1. Specification: 20mg film coated tablets, each containing 22mg of cabozantinib fumarate (equivalent to 20mg of cabozantinib free base).

2. Appearance: White round tablet.

4、 Main components

1. Active ingredient: Cobitinib fumarate salt.

2. Accessories: Microcrystalline cellulose, lactose monohydrate, cross-linked carboxymethyl cellulose sodium, magnesium stearate (core); Polyvinyl alcohol, titanium dioxide, polyethylene glycol 3350, talc powder (coating).

5、 Usage and dosage

1. Usage: Oral administration, once daily, 60mg each time (3 tablets 20mg), taken continuously for 21 days and stopped for 7 days (28 days per cycle).

2. Dosage: Can be taken with food or on an empty stomach. If missed or vomited, there is no need to take it again. Continue taking the next dose according to the original plan.

6、 Dose adjustment

1. First reduction: 40mg once daily; Secondary reduction: 20mg once daily; If it is still intolerable, the medication will be permanently discontinued.

2. Combination use of CYP3A inhibitors: avoid strong/moderate CYP3A inhibitors; If combination therapy is necessary (≤ 14 days), the dose should be reduced to 20mg, and the original dose should be restored after discontinuation.

7、 Medication precautions

1. Diet: No special requirements.

2. Missed dose/vomiting: skip this dose and take the next dose as planned.

3. Other:

Avoid direct sunlight and use sunscreen with SPF ≥ 30.

Monitor liver function, left ventricular ejection fraction (LVEF), creatine phosphokinase (CPK), and visual acuity changes during medication.

8、 Medication for special populations

1. Pregnant women: Prohibited, may cause fetal malformation. Women of childbearing age need to use contraception for 2 weeks after discontinuing the medication.

2. Breastfeeding period: Breastfeeding is prohibited within 2 weeks after discontinuation of medication.

3. Liver/kidney dysfunction: No dose adjustment is required for mild to moderate cases, and there is no clear recommendation for severe cases.

4. Children/elderly: Safety has not been established.

9、 Adverse reactions

1. Common (≥ 20%): Diarrhea, photosensitivity, nausea, fever, vomiting.

2. Serious adverse reactions:

3. Newly developed skin/non skin malignant tumors (such as squamous cell carcinoma).

4. Bleeding (such as cerebral hemorrhage), cardiomyopathy, severe rash, retinopathy, hepatotoxicity, rhabdomyolysis.

10、 Contraindications

There are no absolute contraindications, but it is contraindicated for those who are allergic to the ingredients.

11、 Drug interactions

1. CYP3A inhibitors (such as itraconazole): significantly increase the blood concentration of cabozantinib and avoid combination therapy.

2. CYP3A inducers (such as rifampicin): reduce the efficacy of cabozantinib and avoid combination therapy.

12、 Storage method

Store at room temperature below 30 ° C (86 ° F) and keep dry.

Cobimetinibinformation