Cotellic (Cobimetinib Fumarate)
What is Cotellic (Cobimetinib Fumarate)?
Cotellic is an antineoplastic protein kinase inhibitor medication used for the treatment of metastatic melanoma, a type of skin cancer that is unable to be removed from the body with surgery and that has spread to other areas of the patient’s body. It is typically prescribed alongside the use of Zelboraf (vemurafenib).
This medication is only used for patients whose melanoma has been tested and come back positive for the specific genetic marker BRAF V600E or V600K.
How is Cotellic Used?
Cotellic is available as a tablet that should be taken orally, either with or without food, once daily for a duration of 21 days. The patient will then stop taking the medication for seven days and begin another round of 21-day treatment with Cotellic as instructed by their physician. Specific directions regarding the duration of treatment and method of taking Cotellic will be provided by the patient’s doctor.
This medication should be taken at the same time each day without any missed doses for maximum efficacy. It should be taken exactly as instructed to provide the best possible treatment of the patient’s melanoma while avoiding increasing the risk of side effects associated with Cotellic.
Cotellic should be stored at room temperature and should not be exposed to moisture or light.
Keep this medication out of the reach of children at all times.
Cotellic may be absorbed through a person’s lungs and skin. Pregnant individuals or those who are trying to become pregnant should avoid handling Cotellic or breathing in any dust from Cotellic tablets.
Cotellic is prescribed for the treatment of the type of skin cancer known as melanoma.
How Does Cotellic Work?
Cotellic is a kinase inhibitor that functions by inhibiting the growth and spread of mutated cells with abnormal MEK markers. Zelboraf, which is used alongside Cotellic, targets those cells associated with abnormal BRAF markers. Together, they effectively attack melanoma cells that are tied into both of these proteins, as treating only one of these types of cells would be ineffective.
The proteins MEK and BRAF are associated with cell growth. When there are abnormalities in these two proteins, such as in the case of cancer, the pairing of Cotellic and Zelboraf has proven to be effective at inhibiting the two proteins when mutated and reducing the growth and spread of cancer cells.
Cotellic comes as a 20 mg tablet that is taken once per day in a dosage of 60 mg (three tablets) at once.
This medication should be taken exactly as directed by the patient’s prescribing physician. In special circumstances, a patient’s doctor may give them a modified dosing schedule.
If a patient has consumed too much Cotellic, they should contact their local Poison Control Center or seek out emergency medical attention. Patients that have consumed an excessive amount of this medication may experience severe side effects as a result.
Cotellic has been associated with a variety of side effects ranging from common and mild symptoms to ones that require medical intervention.
The most common side effects of taking Cotellic are as follows:
- abdominal pain
- abnormal lab test results
- cold sores
- dry mouth
- low sodium levels
- mouth sores
- sunlight sensitivity (i.e., easy sunburning)
Some of the following side effects may also occur. If these side effects develop while taking Cotellic, patients should stop using the medication and contact their doctor immediately:
- bleeding gums
- blood clotting problems
- dark-colored urine
- easy bleeding
- easy bruising
- high blood sugar levels (or any associated symptoms)
- increased blood pressure
- infection symptoms
- liver-related issues
- appetite loss
- clay-colored stool
- dark urine
- upper stomach pain
- yellowing of the eyes or skin (jaundice)
- muscle weakness or tenderness
- new development of skin cancer
- partial vision loss
- seeing “halos” when looking at lights
- severe skin-related reactions
- spreading rash with peeling and blistering
- wrinkled or thickened skin
- symptoms of heart trouble
- chest pain
- rapid heart rate
- shortness of breath
- swelling in the ankles or feet
- symptoms of internal bleeding
- bloody stools
- coughing up blood
- pink or red urine
- tarry stools
- vomiting (especially if it looks like coffee grounds)
- symptoms of low sodium
- coordination difficulties
- severe fatigue and weakness
- slurring of speech
- unusual muscle pain
- vision changes
If you experience any of the following symptoms of an allergic reaction, call 911 or seek out emergency medical assistance immediately:
- breathing difficulties
- swelling of the throat, tongue, lips, or face
Warnings & Precautions
Cotellic is known to cause changes in a patient’s blood as well as organ function. Please discuss any preexisting medical conditions, medications, or herbal supplements with your physician before being prescribed this medication.
New Skin Cancers and Skin Changes
Using Cotellic in combination with Zelboraf has been linked to the development of new types of skin cancers during treatment, such as keratoacanthoma, basal cell carcinoma, and cutaneous squamous cell carcinoma. There have also been reported incidents of the development of new lesions of melanoma while using these medications. Any changes to a patient’s skin should be reported to their doctor immediately, and patients should typically have their skin monitored bi-monthly while using Cotellic for treatment. Color or size changes of moles, bumps or sores that bleed or do not heal, and new warts are among the potential risks of using these medications, and these changes should be reported immediately to a patient’s prescribing physician.
Patients taking blood-thinning medications or that have medical conditions that reduce the body’s ability to clot blood should inform their doctor before using Cotellic. Cotellic is capable of increasing a patient’s risk of having uncontrollable bleeding, and the dosage of the medication may need to be adjusted to accommodate any preexisting blood-related disorders or medications.
Patients taking Cotellic for treatment are at risk of developing anemia, a condition characterized by low levels of red blood cells within the body. Individuals being treated with this medication will have their blood cell numbers monitored regularly but should report any of the following symptoms to their doctor if experienced: pale skin, lightheadedness or dizziness, fatigue or unusual tiredness, or shortness of breath.
High Blood Pressure
Cotellic has been found to increase a patient’s blood pressure during treatment. Individuals taking Cotellic should be monitored by their doctor for the duration of treatment to manage any hypertension that may occur. Patients with preexisting high blood pressure should discuss this with their doctor before beginning treatment with Cotellic to ensure that they receive the appropriate dosage to both treat their melanoma as well as avoid negative impacts on their current blood pressure levels.
Cotellic is associated with an increased risk of sensitivity to sunlight, resulting in higher risks of developing sunburn if outdoors or otherwise exposed to direct sunlight. Patients taking this medication should avoid being in sunlight as much as they can during treatment with Cotellic and should wear protective lip balm and sunscreen if outdoors. Those taking Cotellic who have had sun exposure and develop skin peeling or a rash should contact their prescribing physician immediately.
Patients with a history of decreased liver function are at an increased risk of having Cotellic build up in their systems, resulting in an increased risk of adverse side effects as well. This medication may also contribute to decreasing a patient’s liver function, so any symptoms associated with liver impairment that develop while taking this medication should be immediately reported to the patient’s prescribing physician.
Cotellic may contribute to the worsening of a patient’s preexisting heart disease. Patients with conditions such as arrhythmia, angina, or congestive heart failure may need to be monitored during treatment with Cotellic or be prescribed an adjusted dosage of this medication to ensure patient safety. If you experience heart-related symptoms such as chest pain, shortness of breath, swollen ankles, or a rapid heart rate while taking Cotellic, contact your doctor or seek emergency medical assistance immediately.
Using Cotellic for treatment has been linked to the development of muscle damage in some patients. Individuals taking this medication who experience fever, malaise, urine discoloration, weakness, tenderness, muscle pain, or cramps should report these symptoms to their prescribing physician as soon as possible.
Patients taking Cotellic who experience changes in their vision should contact their doctor immediately. This medication can worsen the risk of blockages developing within the blood vessels of the eyes and may also contribute to fluid buildup in the back of a patient’s eyes.
Pregnancy and Breastfeeding
Cotellic is harmful to unborn and developing infants, so the use of this medication during pregnancy is not advised. However, if this medication is deemed necessary for a pregnant patient, that individual should be sure to address all potential risks as well as the benefits of this medication before beginning treatment with Cotellic. It is strongly advised that patients taking Cotellic use multiple forms of birth control if pregnancy is possible for the patient using this medication. Patients who become pregnant while taking Cotellic should immediately contact their physician. Those who are trying to conceive after taking Cotellic for treatment should wait at least three months after their last dose of Cotellic before attempting to become pregnant.
It has not been determined whether Cotellic can be passed through breastmilk, so there is a chance that taking this medication while breastfeeding may cause side effects to develop in the breastfed infant. Patients wanting or attempting to breastfeed while using this medication should consult with their doctor about the risks of doing so.
Patients above the age of 60 years old that may need to use Cotellic are at an increased risk of side effects. In some cases, it may be suitable for the dosage to be lowered to accommodate the risks associated with this age group being affected by the medication and prevent serious adverse events from occurring.
Additional Medical Conditions
If you have any of the following medical conditions, exercise caution when taking Cotellic and discuss your medical history with your doctor before beginning this medication:
- any conditions requiring blood thinners
- bleeding disorders
- clotting disorders
- eye problems
- heart disease
- kidney disease
- liver disease
- muscle issues
- preexisting skin conditions
Speak to your doctor about any medications or herbal supplements you are currently taking before beginning treatment with Cotellic. Discuss any concerns you may have with your doctor or a trusted pharmacist.
Drugs Known to Interact with Cotellic
The following medications are known to interact with Cotellic:
- “-azole” antifungal medications
- HIV non-nucleoside reverse transcriptase inhibitors
- HIV protease inhibitors
- macrolide antibiotic medications
- protein kinase inhibitors
- seizure medications
If you are taking any of the above medications, please discuss this with your physician before beginning treatment with Cotellic.
Other Substances That Should Not Be Used with Cotellic
The following additional substances should never be used alongside Cotellic:
- grapefruit juice
- John’s wort
For patients who are unable to take Cotellic or experiencing significant adverse side effects, alternative medications may be used to treat the type of melanoma for which this medication is commonly prescribed:
- Braftovi (encorafenib)
- Imylgic (talimogene laherparepvec)
- Intron A (recombinant interferon alfa-2b)
- Keytruda (pembrolizumab)
- Kimmtrak (tebentafusp-tebn)
- Mekinist (trametinib dimethyl sulfoxide)
- Mektovi (binimetinib)
- Opdivo (nivolumab)
- Opdualag (nivolumab and relatlimab-rmbw)
- PEG-Intron/Sylatron (peginterferon alfa-2b)
- Proleukin (aldesleukin)
- Tafinlar (dabrafenib mesylate)
- Yervoy (ipilimumab)