Cotellic
Cotellic (cobimetinib) is a targeted therapy that’s used to treat two different cancers in adults: histiocytic neoplasms and melanoma (a type of skin cancer). For histiocytic neoplasms, this medication is used by itself. But for melanoma, Cotellic (cobimetinib) is taken with another anticancer medication to treat people with a certain mutation called a BRAF mutation. Cotellic (cobimetinib) is convenient to take because it’s a tablet that you take by mouth. But it can cause side effects such as diarrhea, rash, and bleeding.
What is Cotellic (cobimetinib)?
What is Cotellic (cobimetinib) used for?
Melanoma with certain BRAF mutations that has spread (metastatic) or can’t be removed by surgery, used together with Zelboraf (vemurafenib)
How Cotellic (cobimetinib) works
Cotellic (cobimetinib) is a kinase inhibitor known as a MEK inhibitor. MEK is a protein in the body that’s important for cell growth. Cotellic (cobimetinib) works by blocking the MEK protein. When the medication blocks MEK, cancer cells can’t grow and spread as well.
For people with melanoma with a BRAF mutation, Cotellic (cobimetinib) is taken with Zelboraf (vemurafenib). The BRAF protein also helps cells grow, and cells can grow too quickly when there’s a BRAF mutation. By blocking two different proteins, Cotellic (cobimetinib) and vemurafenib (Zelboraf) work together to stop the growth and spread of cancer better.
Drug Facts
What are the side effects of Cotellic (cobimetinib)?
Common Side Effects
- Higher creatinine levels in blood (100%)
- Higher liver enzymes in blood (up to 73%)
- Higher creatine phosphokinase (CPK) levels in blood (79%)
- Other blood test abnormalities (up to 69%)
- Diarrhea (60%)
- Skin that’s sensitive to the sun (46%)
- Nausea (41%)
- Fever (28%)
- Vomiting (24%)
Other Side Effects
- Higher blood pressure
- Bleeding
- Vision changes
- Mouth pain or mouth sores
- Chills
- Rash
Serious Side Effects
- Bleeding: blood in urine, blood in stool, vaginal bleeding, sudden and severe headache
- Serious eye problems: sudden and severe eye pain, sudden vision loss
- Serious muscle problems: severe muscle pain or stiffness, dark red or brown urine, sudden muscle weakness
Source: DailyMed
The following side effects have also been reported
Side effects that you should report to your care team as soon as possible:
- Allergic reactions—skin rash, itching, hives, swelling of the face, lips, tongue, or throat
- Bleeding—bloody or black, tar-like stools, vomiting blood or brown material that looks like coffee grounds, red or dark brown urine, small red or purple spots on skin, unusual bruising or bleeding
- Blurry vision, vision loss, seeing wavy or bent objects or blind spots with dark, light, or flashing spots
- Heart failure—shortness of breath, swelling of the ankles, feet, or hands, sudden weight gain, unusual weakness or fatigue
- Liver injury—right upper belly pain, loss of appetite, nausea, light-colored stool, dark yellow or brown urine, yellowing skin or eyes, unusual weakness or fatigue
- Muscle injury—unusual weakness or fatigue, muscle pain, dark yellow or brown urine, decrease in amount of urine
- Sensitivity to light
Side effects that usually do not require medical attention (report to your care team if they continue or are bothersome):
Pros and cons of Cotellic (cobimetinib)
Pros
Taken by mouth, so it’s a good option for people who don’t like needles
Works in a more specific, targeted way than traditional chemotherapy
Recommended option for treating BRAF-mutated melanoma and for treating histiocytic neoplasms
Cons
Must take with a second medication if treating melanoma, so less convenient
Requires regular blood tests to monitor for side effects
Often causes diarrhea and skin sensitivity or rash
Pharmacist tips for Cotellic (cobimetinib)
You can take Cotellic (cobimetinib) with or without food.
If you miss a dose of Cotellic (cobimetinib), skip the missed dose and wait to take the next scheduled dose.
If you have diarrhea while you’re taking Cotellic (cobimetinib), make sure you drink plenty of fluids. Avoid sugary sports drinks, though, because they can make diarrhea worse. Your provider might recommend over-the-counter diarrhea medications, like loperamide (Imodium A-D), to help.
Some Cotellic (cobimetinib) side effects, such as anemia and changes in electrolyte levels in your blood, can only be found through blood testing. Your provider will order regular lab tests while you’re taking Cotellic (cobimetinib). These lab tests are important to make sure the medication is still safe for you to keep taking it.
Don't breastfeed while you're taking Cotellic (cobimetinib). We don’t know whether Cotellic (cobimetinib) is found in breast milk and whether it affects breastfed babies. But because of the possible risks to a baby, it’s best to avoid nursing if you’re taking Cotellic (cobimetinib) and for 2 weeks after the last dose.
Ask your provider about the best way to handle and throw away Cotellic (cobimetinib) safely. Anticancer medications can be harmful to people who handle or come in contact with them. Store Cotellic (cobimetinib) in a safe place away from children and pets.
Frequently asked questions about Cotellic (cobimetinib)
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What are the risks and warnings for Cotellic (cobimetinib)?
Cotellic (cobimetinib) can cause some serious health issues. This risk may be even higher for certain groups. If this worries you, talk to your doctor or pharmacist about other options.
New cancers
Some people taking Cotellic (cobimetinib) together with Zelboraf (vemurafenib) developed a new cancer. In studies, these cancers included different kinds of skin cancer (squamous cell carcinoma, basal cell carcinoma, and melanoma). Zelboraf (vemurafenib) itself might also cause growth of other cancer types. Because people with melanoma who take Cotellic (cobimetinib) must also take Zelboraf (vemurafenib), there might be a risk for other cancer types as well. Your provider will monitor you for new signs and symptoms of cancer, especially skin cancers, while you’re taking Cotellic (cobimetinib).
Bleeding
Cotellic (cobimetinib), taken with or without Zelboraf (vemurafenib), can cause bleeding. This includes bleeding in the gut, blood in the urine, vaginal bleeding, and rarely, bleeding in the brain. If you have any unusual signs or symptoms of bleeding, tell your provider right away. If it’s mild, your provider might pause Cotellic (cobimetinib) and you might be able to restart it later at a lower dose. But sometimes the medication must be permanently stopped.
Heart problems
Some people taking Cotellic (cobimetinib) developed a heart condition where their heart doesn’t pump as well. Some people with this condition might not feel anything. But others might have symptoms like tiredness, trouble breathing, and swelling in the legs. Your provider will monitor how well your heart is pumping through imaging called an echocardiogram (echo). You’ll usually need imaging scans of your heart before you start Cotellic (cobimetinib) and every 3 months while you’re taking it. If the scans show that your heart isn’t pumping as well as it should or if you experience related symptoms while you’re taking Cotellic (cobimetinib), you might need to pause or stop the medication.
Serious skin problems
Cotellic (cobimetinib) might cause skin issues, like dry skin, itchy skin, swelling around hair follicles (folliculitis), or rash. Most cases are mild, but there are some reports of severe rash that require hospitalization. If you have a new rash or skin problem, tell your provider. Based on how serious it is, you might need to pause or stop the medication.
Serious eye problems
Treatment with Cotellic (cobimetinib) can cause several different kinds of eye problems. The most commonly reported problem is a buildup of fluid in the back of the eye (serous retinopathy). Sometimes, retinal detachment has also occurred. Rarely, some people had blood clots in eye veins. Your provider might refer you to an ophthalmologist while you’re taking Cotellic (cobimetinib). Tell your provider if you have any vision changes while taking Cotellic (cobimetinib).
Liver problems
Some people taking Cotellic (cobimetinib) have had blood test results showing high levels of liver enzymes in their blood, which can suggest liver problems. Your provider will monitor your liver health on a regular basis (usually every month). If your liver enzyme levels go up, you might need to pause or stop Cotellic (cobimetinib) while your provider looks into it. Most people don’t feel any noticeable symptoms when this happens, so it’s important to keep up with your lab work regularly. If you have stomach pain, yellowish skin, or yellow around the whites of your eyes, call your provider right away since these can be symptoms of liver damage.
Muscle problems
Treatment with Cotellic (cobimetinib) can raise the level of creatine phosphokinase (CPK) in your blood. This can suggest that you have muscle damage. You’ll need to get blood work done periodically during treatment so your provider can keep track of your CPK levels. But let your provider know if you have muscle pain or very dark reddish-brown urine, as this can be a sign of a rare muscle condition called rhabdomyolysis. Your provider might pause or stop Cotellic (cobimetinib) depending on how severe your symptoms are.
Severe sun sensitivity
People taking Cotellic (cobimetinib) with Zelboraf (vemurafenib) can develop photosensitivity, or skin that’s very sensitive to sunlight. In studies, some people developed sun sensitivity around 2 months after starting treatment, but it can also appear within days or even after several months of treatment. You should avoid sun exposure when possible. If you’re outdoors, wear sunscreen with an SPF of at least 30 and clothes that protect your skin. Let your provider know if you experience a sunburn or painful skin while taking Cotellic (cobimetinib).
Harm to unborn baby
Based on animal studies, Cotellic (cobimetinib) might harm an unborn baby or raise the risk for miscarriage (pregnancy loss). Because of this risk, people who can become pregnant should use birth control while taking Cotellic (cobimetinib) and for at least 2 weeks after the last dose. Let your provider know if you become pregnant during treatment.
Cotellic (cobimetinib) dosage forms
Typical dosing for Cotellic (cobimetinib)
The usual dose is 60 mg by mouth once a day for 3 weeks. Then, you’ll take 1 week off from the medication. This is considered one treatment cycle. Repeat the treatment cycle (3 weeks of treatment, followed by 1 week off) for as long as you’re taking the medication.
What are alternatives to Cotellic (cobimetinib)?
Melanoma with certain BRAF mutations that has spread (metastatic) or can’t be removed by surgery, used together with Zelboraf (vemurafenib)
Melanoma with certain BRAF mutations that has spread (metastatic) or can’t be removed by surgery; used with Braftovi (encorafenib)
Metastatic non-small cell lung cancer (NSCLC) with certain BRAF mutations; used with Braftovi (encorafenib)
Melanoma with certain BRAF mutations
Metastatic non-small cell lung cancer (NSCLC) with a certain BRAF mutation, used with Tafinlar (dabrafenib)
Metastatic anaplastic thyroid cancer (ATC) with a certain BRAF mutation, used with Tafinlar (dabrafenib)
Solid tumors with a certain BRAF mutation that have spread or can’t be removed by surgery, used with Tafinlar (dabrafenib)
Low-grade glioma (LGG) with a certain BRAF mutation, used with Tafinlar (dabrafenib)
What is the latest news about Cotellic (cobimetinib)?
Cotellic (cobimetinib) images
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References
Best studies we foundAkinleye, A., et al. (2013). MEK and the inhibitors: From bench to bedside. Journal of Hematology & Oncology.
American Academy of Dermatology Association. (n.d.). Acne-like breakouts could be folliculitis.
American Cancer Society. (2019). Targeted therapy safety.
American Cancer Society. (2021). Mouth sores and pain.
American Cancer Society. (2022). Gene changes and cancer.
Bakri, S. J., et al. (n.d.). Central serous chorioretinopathy. American Society of Retina Specialists.
Genentech, Inc. (2023). Cotellic- cobimetinib tablet, film coated [package insert]. DailyMed.
Go, R. S., et al. (2021). Histiocytic neoplasms, version 2.2021, NCCN clinical practice guidelines in oncology. Journal of the National Comprehensive Cancer Network.
Marranci, A., et al. (2017). The landscape of BRAF transcript and protein variants in human cancer. Molecular Cancer.
MedlinePlus. (2023). Creatine kinase.
National Cancer Institute. (n.d.). BRAF V600 mutation.
National Cancer Institute. (n.d.). Histiocytic neoplasm.
National Cancer Institute. (n.d.). MEK inhibitor.
National Cancer Institute. (2022). Targeted therapy to treat cancer.
National Center for Complementary and Integrative Health. (2020). St. John’s wort.
National Comprehensive Cancer Network. (2023). Melanoma.
Russo, I., et al. (2018). Cutaneous side effects of targeted therapy and immunotherapy for advanced melanoma. Scientifica.
Skin Cancer Foundation. (2022). Basal cell carcinoma overview.
Skin Cancer Foundation. (2023). Squamous cell carcinoma overview.
Stjepanovic, N., et al. (2016). Ocular toxicities of MEK inhibitors and other targeted therapies. Annals of Oncology.
Welsh, S. J., et al. (2015). Management of BRAF and MEK inhibitor toxicities in patients with metastatic melanoma. Therapeutic Advances in Medical Oncology.
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