The Navigation Model of Therapy: Why Awareness Changes Everything
November 16, 2025
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Brand Name :
Cotellic
(United States) [Available]Synonyms :
cobimetinib
Class :
Antineoplastics and MEK Inhibitors 
Brand Name :
Cotellic
(United States) [Available]Synonyms :
cobimetinib
Class :
Antineoplastics and MEK Inhibitors 
60
mg
Tablet
Oral
once a day
21
days
Take the dose until disease progression or unacceptable toxicity 
Safety and efficacy not established
Refer adult dosing
when both drugs are combined, there may be increase in the serum concentration of abemaciclib 
when both drugs are combined, there may be increase in the bradycardic effect of ceritinib 
It may diminish the effect when combined with phenobarbital by affecting the intestinal/hepatic enzyme CYP3A4 metabolism
It may enhance the effect when combined with grapefruit by CYP3A4 metabolism
may enhance the concentration of serum when combined with cobimetinib
may enhance the concentration of serum when combined with cobimetinib
may enhance the concentration of serum when combined with cobimetinib
may enhance the concentration of serum when combined with cobimetinib
may enhance the concentration of serum when combined with cobimetinib
It may diminish the levels when combined with efavirenz by CYP3A4 metabolism
When naficillin combines with cobimetinib, nafcillin will decrease the effect of action of cobimetinib by affecting enzyme CYP3A4 metabolism.
when both drugs are combined, there may be an increased effect of cobimetinib by affecting hepatic or intestinal enzyme cyp3a4 metabolism  
may enhance the serum concentration of CYP3A4 inhibitors
when both drugs are combined, there may be increase in the serum concentration of acalabrutin 
when both drugs are combined, there may be increase in ceritinib and arsenic trioxide both increase QTc interval
when both drugs are combined, there may be increase in both increase QTc interval 
when both drugs are combined, there may be increase in both increase QTc interval 
when both drugs are combined, there may be increase in both increase QTc interval 
when both drugs are combined, there may be increase in both increase QTc interval  arsenic trioxide 
when both drugs are combined, there may be increase in both increase QTc interval 
cobimetinib: they may diminish the serum concentration of CYP3A4 Inducers
cobimetinib: they may diminish the serum concentration of CYP3A4 Inducers
cobimetinib: they may diminish the serum concentration of CYP3A4 Inducers
cobimetinib: they may diminish the serum concentration of CYP3A4 Inducers
cobimetinib: they may diminish the serum concentration of CYP3A4 Inducers
lapatinib increases the effect of cobimetinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
CYP3A strong enhancers of the small intestine may reduce the bioavailability of cobimetinib
CYP3A4 inducers decrease the concentration of cobimetinib in serum
metronidazole/tetracycline/bismuth subsalicylateÂ
by altering the intestinal/hepatic CYP3A4 metabolism, the effects of cobimetinib will be increased by metronidazole
When cobimetinib is used together with oleandomycin, this leads to enhanced concentration serum of cobimetinib
When cobimetinib is used together with patupilone, this leads to enhanced concentration serum of cobimetinib
When cobimetinib is used together with ridaforolimus, this leads to enhanced concentration serum of cobimetinib
may decrease the serum concentration of CYP3A4 Inducers
meningococcal group B vaccineÂ
the efficacy of the vaccine may be reduced
the serum levels of cobimetinib may be increased
Extracellular signal-regulated kinase 1 (MEK1) and mitogen-activated protein kinase (MAPK) are both reversibly inhibited by cobometinib.Â
Cell proliferation is encouraged via the extracellular signal-related kinase (ERK) pathway, which is upstream regulated by MEK proteins.Â
Mutations in BRAF V600E and K cause constitutive activation of the BRAF pathway, which involves MEK1 and MEK2.Â
In an in vivo mouse implantation model, Cobimetinib also inhibited the growth increase of a wild-type BRAF tumor cell line caused by vemurafenib.Â
Adverse drug reactions: Â
Frequency defined Â
>10%  Â
Increased alkaline phosphatase (71%)  Â
Anemia (69%)  Â
Increased ALT (68%)  Â
Increased creatinine (99.6%)  Â
Increased CPK (79%)  Â
Increased AST (73%)  Â
Lymphopenia (73%)  Â
Hypophosphatemia (68%)  Â
Increased GGT (65%)  Â
Diarrhea (60%)  Â
Pyrexia (28%)  Â
Hyperkalemia (26%)  Â
Hypokalemia (25%)  Â
Hypocalcemia (24%)  Â
Photosensitivity (46%)  Â
Hypoalbuminemia (42%)  Â
Nausea (41%)  Â
Hyponatremia (38%)  Â
Vomiting (24%)  Â
Thrombocytopenia (18%)  Â
Acneiform dermatitis (16%)  Â
Hypertension (15%)  Â
Vision impaired (15%)  Â
Alopecia (15%)  Â
Stomatitis (14%)  Â
Hemorrhage (13%)  Â
Chorioretinopathy (13%)  Â
Retinal detachment (12%)  Â
Hyperkeratosis (11%)  Â
Grades 3-4  Â
Increased GGT (21%)  Â
Increased CPK (14%)  Â
Hypophosphatemia (12%)  Â
Increased ALT (11%)  Â
1-10%  Â
Chills (10%)  Â
NoneÂ
Contraindication:Â
None Â
Caution:Â
Serous retinopathy and retinal vein occlusionÂ
HepatotoxicityÂ
Severe photosensitivityÂ
CardiomyopathyÂ
HemorrhageÂ
Pregnancy warnings:    Â
Breastfeeding warnings: Â
Pregnancy Categories:      Â
Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first trimester or the later trimester.      Â
Category B: No evidence shown of risk to the fetus found in animal reproduction studies, and there are not enough studies on pregnant women      Â
Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for a result in humans must take care of potential risks in pregnant women      Â
Category D: There is adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits      Â
Category X: Drugs listed in this category outweigh risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.      Â
Category N: There is no data available for the drug under this category     Â
Â
The growth of tumor cells with a BRAF mutation, which has been linked to a variety of tumor types, can be effectively inhibited by this drug, according to preclinical research.Â
Growth-promoting signals from many receptor tyrosine kinases must be transmitted via MEK1, a threonine-tyrosine kinase and an essential part of the RAS/RAF/MEK/ERK signaling pathway that is commonly active in human malignancies.Â
In BRAF-mutant melanomas, reactivation of the MAPK pathway is a primary cause of treatment failure; reactivation of MAPK signaling causes over 80% of melanoma tumors to become resistant to BRAF inhibitors.Â
It is taken orally in tablet form with foodÂ
If a dose was missed or vomited, start dosing again with the following scheduled dose.Â
Patient information leafletÂ
Generic Name: cobimetinibÂ
Why do we use cobimetinib?Â
For the treatment of metastatic or incurable melanoma with a BRAF V600E or V600K mutation, cobometinib is recommended in combination with vemurafenib.Â
Cobimetinib is also approved for use as a single treatment for adult patients with histiocytic neoplasms.Â
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