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Cobimetinib can enhance the anti-tumor effect against BRAFV600 mutation-positive melanoma when used in combination with vemurafenib, or as a single agent for the treatment of histiocytic tumors.
1. Common name: Cobimetini
2. Trade name: COTELLIC
3. English name: Cobimetini b
1. Cobimetinib is a kinase inhibitor, combined with vemurafenib, for the treatment of patients with unresectable or metastatic melanoma confirmed by FDA-approved testing methods to have BRAF V600E or V600K mutations.
2. Restricted use: Cobimetinib is not suitable for the treatment of patients with wild-type BRAF melanoma.
1. Specifications: 20 mg/tablet.
2. Characteristics: White round film-coated tablets.
IV. Main ingredients
1. Active ingredient: Cobimetinib fumarate. Each 20 mg tablet contains 22 mg of cobimetinib fumarate, equivalent to 20 mg of cobimetinib free base.
2. Inactive ingredients: The tablet core contains microcrystalline cellulose, lactose monohydrate, croscarmellose sodium and magnesium stearate. The coating contains polyvinyl alcohol, titanium dioxide, polyethylene glycol 3350 and talc.
1. Recommended dosage: Take 60 mg orally once a day (i.e. three 20 mg tablets) for the first 21 days of each 28-day treatment cycle until disease progression or unacceptable toxicity occurs.
2. How to take: Can be taken with food or on an empty stomach.
3. Missing a dose or vomiting: If you miss a dose or vomit after taking the medicine, you should resume taking the medicine at the next scheduled time without making up the dose.
1. Dose reduction steps: Reduce the first dose to 40 mg once a day; reduce the second dose to 20 mg once a day; if 20 mg once a day is intolerable, discontinue use permanently.
2. Adjustment for adverse reactions: The dose needs to be suspended, reduced or permanently discontinued according to the severity of adverse reactions. The specific adjustment plan has detailed provisions for adverse reactions of different systems (such as bleeding, cardiomyopathy, severe skin reactions, serous retinopathy, hepatotoxicity, rhabdomyolysis, photosensitivity reactions, etc.).
3. Adjustments due to drug interactions: Simultaneous use with strong or moderate CYP3A inhibitors should be avoided. If patients taking cobimetinib 60 mg inevitably require short-term (≤14 days) concomitant use of a moderate CYP3A inhibitor, the cobimetinib dose should be reduced to 20 mg. After discontinuing the inhibitor, resume the original dose. For patients whose dose has been reduced, an alternative drug that is a strong or moderate CYP3A inhibitor should be used.
1. Medication time: Take once a day, preferably at a fixed time, before or after meals.
2. Treatment of missed doses: Skip the missed dose and take the next dose at the next regular time. Do not take a double dose to make up for a missed dose.
3. Vomiting treatment: If vomiting occurs after taking the medicine, there is no need to take a supplementary dose, just take the next dose as planned.
4. Monitoring requirements: During treatment, skin examination, heart function (LVEF) assessment, eye examination, liver function, serum creatine phosphokinase (CPK) and creatinine need to be monitored regularly.
1. Pregnant women: Based on the mechanism of action and animal studies, it may cause fetal harm. Pregnant women should be informed of the potential risk to the fetus.
2. Breastfeeding women: It is recommended not to breastfeed during treatment and within 2 weeks after the last dose.
3. Women and men of childbearing potential: Women should take effective contraceptive measures during treatment and for at least 2 weeks after the last dose. Based on animal data, cobimetinib may decrease female and male fertility.
4. Pediatric patients: Safety and effectiveness have not been established.
5. Elderly patients:Clinical studies have not included a sufficient number of patients aged 65 and above to determine whether their responses are different.
6. Patients with liver damage: Patients with mild liver damage do not need to adjust the dosage. The pharmacokinetics in patients with moderate to severe hepatic impairment have not been studied and caution is warranted.
7. Patients with renal impairment: No dosage adjustment is required for patients with mild to moderate renal impairment. Recommended dosages for patients with severe renal impairment have not been established.
1. The most common adverse reactions (≥20%) include: Diarrhea, photosensitivity reaction, nausea, fever, and vomiting.
2. Common (≥5%) grade 3-4 laboratory abnormalities include: Elevated GGT, elevated CPK, hypophosphatemia, elevated ALT, lymphopenia, elevated AST, elevated alkaline phosphatase, and hyponatremia.
3. Serious adverse reactions include: New primary malignant tumors (cutaneous and non-cutaneous), hemorrhage, cardiomyopathy, severe skin reactions, serous retinopathy and retinal vein occlusion, hepatotoxicity, rhabdomyolysis, severe photosensitivity reactions, etc.
There are currently no obvious contraindications.
1. Combination with strong or moderate CYP3A inhibitors (such as itraconazole) should be avoided, as it will significantly increase the plasma concentration of cobimetinib.
2. Combination with strong or moderate CYP3A inducers (such as carbamazepine, rifampicin, St. John's wort) should be avoided, as it will significantly reduce the plasma concentration of cobimetinib and affect its efficacy.
Store at room temperature, below 30°C (86°F).