Cobimetinib Brand Name– Cotellic
What is Cobimetinib
Cobimetinib fumarate is a selective mitogen-activated protein kinase (MEK) inhibitor. It is indicated in combination with vemurafenib for the treatment of unresectable or metastatic melanoma in patients with a BRAF V600E or V600K mutation.
At a median follow-up of 7.3 months (range, 0.5 to 16.5 months), the median investigator-assessed progression-free survival time was significantly improved with cobimetinib plus vemurafenib compared with placebo plus vemurafenib (9.9 months vs. 6.2 months; hazard ratio = 0.51; 95% CI, 0.39 to 0.68) in patients with previously untreated unresectable locally advanced or metastatic BRAF V600 mutation–positive melanoma in a multinational, randomized, double-blind, phase III trial (n = 495; the CoBRIM trial).
Cobimetinib (Cotellic) received priority review from the FDA in November 2015.
Indications
- malignant melanoma
For the treatment of malignant melanoma
NOTE: Cobimetinib was designated by the FDA as an orphan drug for the treatment of stage IIb, IIc, III, and IV melanoma in patients with a BRAFV600 mutation.
Side Effects
- acneiform rash
- acneiform rash
- alopecia
- anemia
- anemia
- bleeding
- bleeding
- blurred vision
- cardiomyopathy
- chills
- diarrhea
- diarrhea
- ecchymosis
- elevated hepatic enzymes
- elevated hepatic enzymes
- epistaxis
- erythema
- fever
- fever
- GI bleeding
- heart failure
- hematemesis
- hematoma
- hematuria
- hemoptysis
- hyperbilirubinemia
- hyperkalemia
- hyperkalemia
- hyperkeratosis
- hypertension
- hypertension
- hypoalbuminemia
- hypoalbuminemia
- hypocalcemia
- hypocalcemia
- hypokalemia
- hypokalemia
- hyponatremia
- hyponatremia
- hypophosphatemia
- hypophosphatemia
- intracranial bleeding
- lymphopenia
- lymphopenia
- macular edema
- melena
- menorrhagia
- nausea
- nausea
- new primary malignancy
- ocular hemorrhage
- oral ulceration
- photosensitivity
- photosensitivity
- pneumonitis
- purpura
- rash
- renal failure (unspecified)
- retinal detachment
- retinal detachment
- retinal hemorrhage
- retinopathy
- rhabdomyolysis
- skin cancer
- stomatitis
- stomatitis
- thrombocytopenia
- vaginal bleeding
- visual impairment
- visual impairment
- vomiting
- vomiting
Monitoring Parameters
- CBC with differential
- creatine phosphokinase (CPK)
- ECG
- ejection fraction
- LFTs
- ophthalmologic exam
- serum creatinine/BUN
- serum electrolytes
- skin cancer screening exam
Contraindications
- anticoagulant therapy
- bleeding
- breast-feeding
- cardiac disease
- cardiomyopathy
- contraception requirements
- geriatric
- GI bleeding
- heart failure
- hepatic disease
- hepatotoxicity
- infertility
- intracranial bleeding
- new primary malignancy
- ocular disease
- pregnancy
- reproductive risk
- retinal detachment
- rhabdomyolysis
- serious rash
- sunlight (UV) exposure
- thrombocytopenia
- ventricular dysfunction
- visual disturbance
Interactions
- Acetaminophen; Butalbital
- Acetaminophen; Butalbital; Caffeine
- Acetaminophen; Butalbital; Caffeine; Codeine
- Aldesleukin, IL-2
- Alogliptin; Pioglitazone
- Amiodarone
- Amobarbital
- Amoxicillin; Clarithromycin; Lansoprazole
- Amoxicillin; Clarithromycin; Omeprazole
- Apalutamide
- Aprepitant, Fosaprepitant
- Armodafinil
- Aspirin, ASA; Butalbital; Caffeine
- Aspirin, ASA; Butalbital; Caffeine; Codeine
- Atazanavir
- Atazanavir; Cobicistat
- Atropine; Hyoscyamine; Phenobarbital; Scopolamine
- Belladonna Alkaloids; Ergotamine; Phenobarbital
- Bexarotene
- Boceprevir
- Bosentan
- Brigatinib
- Butabarbital
- Cabozantinib
- Carvedilol
- Cenobamate
- Ceritinib
- Chloramphenicol
- Chloroquine
- Cimetidine
- Ciprofloxacin
- Clarithromycin
- Cobicistat
- Cocaine
- Conivaptan
- Crizotinib
- Cyclosporine
- Dabrafenib
- Daclatasvir
- Danazol
- Darunavir
- Darunavir; Cobicistat
- Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
- Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
- Deferasirox
- Delavirdine
- Dexamethasone
- Dextromethorphan; Quinidine
- Diltiazem
- Dronedarone
- Drospirenone; Ethinyl Estradiol
- Drospirenone; Ethinyl Estradiol; Levomefolate
- Duvelisib
- Efavirenz
- Efavirenz; Emtricitabine; Tenofovir
- Efavirenz; Lamivudine; Tenofovir Disoproxil Fumarate
- Elagolix
- Elagolix; Estradiol; Norethindrone acetate
- Elbasvir; Grazoprevir
- Eliglustat
- Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
- Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
- Enalapril; Felodipine
- Encorafenib
- Enzalutamide
- Erythromycin
- Erythromycin; Sulfisoxazole
- Eslicarbazepine
- Ethinyl Estradiol
- Ethinyl Estradiol; Desogestrel
- Ethinyl Estradiol; Ethynodiol Diacetate
- Ethinyl Estradiol; Etonogestrel
- Ethinyl Estradiol; Levonorgestrel
- Ethinyl Estradiol; Levonorgestrel; Ferrous bisglycinate
- Ethinyl Estradiol; Levonorgestrel; Folic Acid; Levomefolate
- Ethinyl Estradiol; Norelgestromin
- Ethinyl Estradiol; Norethindrone
- Ethinyl Estradiol; Norethindrone Acetate
- Ethinyl Estradiol; Norethindrone Acetate; Ferrous fumarate
- Ethinyl Estradiol; Norethindrone; Ferrous fumarate
- Ethinyl Estradiol; Norgestimate
- Ethinyl Estradiol; Norgestrel
- Etravirine
- Fedratinib
- Felbamate
- Felodipine
- Flibanserin
- Fluconazole
- Fluoxetine
- Fluoxetine; Olanzapine
- Flutamide
- Fluvoxamine
- Fosamprenavir
- Fosphenytoin
- Fostamatinib
- Glecaprevir; Pibrentasvir
- Glimepiride; Pioglitazone
- grapefruit juice
- Idelalisib
- Iloperidone
- Imatinib
- Indinavir
- Isavuconazonium
- Isoniazid, INH; Pyrazinamide, PZA; Rifampin
- Isoniazid, INH; Rifampin
- Istradefylline
- Itraconazole
- Ivosidenib
- Ketoconazole
- Lapatinib
- Ledipasvir; Sofosbuvir
- Lefamulin
- Letermovir
- Lopinavir; Ritonavir
- Lorlatinib
- Mefloquine
- Mephobarbital
- Metformin; Pioglitazone
- Mifepristone
- Mitotane
- Modafinil
- Nafcillin
- Nefazodone
- Nelfinavir
- Netupitant, Fosnetupitant; Palonosetron
- Nevirapine
- Nicardipine
- Nilotinib
- Octreotide
- Ombitasvir; Paritaprevir; Ritonavir
- Omeprazole; Amoxicillin; Rifabutin
- Oritavancin
- Osimertinib
- Pazopanib
- Pentobarbital
- Perampanel
- Pexidartinib
- Phenobarbital
- Phentermine; Topiramate
- Phenytoin
- Pioglitazone
- Pirfenidone
- Porfimer
- Posaconazole
- Primidone
- Propafenone
- Quinidine
- Quinine
- Ranolazine
- Ribociclib
- Ribociclib; Letrozole
- Rifabutin
- Rifampin
- Rifaximin
- Ritonavir
- Rivaroxaban
- Rolapitant
- Sapropterin
- Saquinavir
- Secobarbital
- Segesterone Acetate; Ethinyl Estradiol
- Simeprevir
- Sofosbuvir; Velpatasvir; Voxilaprevir
- Sorafenib
- St. John’s Wort, Hypericum perforatum
- Tacrolimus
- Telithromycin
- Telotristat Ethyl
- Temsirolimus
- Testosterone
- Ticagrelor
- Tipranavir
- Topiramate
- Trandolapril; Verapamil
- Tucatinib
- Ulipristal
- Valproic Acid, Divalproex Sodium
- Vemurafenib
- Verapamil
- Verteporfin
- Voriconazole
- Zafirlukast
- Zonisamide
