Cobimetinib (COTELLIC)

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Indication

Melanoma, advanced or metastatic with BRAF V600E or BRAF V600K mutation

Dose

Melanoma, advanced or metastatic with BRAF V600E or BRAF V600K mutation

Oral: 60 mg once daily on days 1 to 21 out of every 28 days until disease progression or unacceptable toxicity.
Given in combination with vemurafenib

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Supplied

Available as 20 mg film-coated tablet. Tablets contain lactose. Tablets should NOT be crushed or broken. Store at room temperature.

Pharmacological Category

Mitogen-activated Extracellular Kinase (MEK) Inhibitor

Administration

Take with or without food

Missed Dose

If a dose is missed, patients should be instructed to take it as soon as they can if it is within 12 hours of the missed dose. If it is over 12 hours since the missed dose, patients should skip the missed dose and resume with the next scheduled dose.

Adverse Effects

Common: Serous retinopathy, Diarrhea, Nausea, Fatigue, ALT increase, AST increase, Creatinine phosphokinase increase, Photosensitivity reaction, Rash.

Less Common: Retinal vein occlusion, Left ejection fraction decrease, Secondary malignancies, Rhabdomyolysis.

The adverse effects listed above are not exhaustive. Please refer to the relevant product monograph for full details.

Monitoring Parameters

Baseline before treatment: CBC & differential, creatinine, electrolytes, CPK levels, MUGA scan or echocardiogram, liver function tests, blood pressure.

During treatment: CBC & differential, creatinine, electrolytes, CPK levels, MUGA scan or echocardiogram (at least every 3 months or as clinically indicated), liver function tests, blood pressure.

Drug Interactions

Avoid grapefruit, grapefruit juice, Seville oranges, or Seville orange juice.
This drug can impact or be impacted by metabolic enzymes for absorption and excretion. Many drugs can also affect or be affected by these enzymes, so please consult with pharmacy to assess for interactions.
Current drug interaction databases should be consulted for more information.

Clinical Pearls

Avoid in pregnancy and lactation.
Creatine phosphokinase (CPK) elevations and rhabdomyolysis have been associated with cobimetinib and may require treatment interruption, dose reduction, or discontinuation.

References

BC Cancer. BC Cancer Drug Manual. Cobimetinib. Vancouver, British Columbia: BC Cancer Agency. Available at: http://www.bccancer.bc.ca/drug-database-site/Drug%20Index/Cobimetinib_monograph_1Sep2017.pdf. Developed September 1, 2017. Accessed January 22, 2024.

Lexicomp. Cobimetinib Monograph. In: Lexi-Drugs. Hudson, Ohio: Lexi-Comp, Inc. Available at: https://online-lexi-com.qe2a-proxy.mun.ca/lco/action/doc/retrieve/docid/patch_f/5925392?cesid=2k8maFLqIGc&searchUrl=%2Flco%2Faction%2Fsearch%3Fq%3Dcobimetinib%26t%3Dname%26acs%3Dfalse%26acq%3Dcobimetinib. Updated January 24, 2024. Accessed January 28, 2024.

Cancer Care Ontario. Cobimetinib Monograph. Drug Formulary. Toronto, Ontario: Cancer Care Ontario. Available at: https://www.cancercareontario.ca/en/drugformulary/drugs/monograph/44436. Updated July 2023. Accessed January 22, 2024.Hoffmann-La Roche Ltd. COTELLIC® Product monograph. Mississauga, Ontario. Updated March 24, 2023.