Trametinib, sold under the brand name Mekinist, is an anticancer medication used to treat melanoma and glioma. It works as a MEK inhibitor, blocking the MEK1 and MEK2 proteins that relay growth signals inside cancer cells. Taken orally, it received United States approval in May 2013 for patients with V600E mutated metastatic melanoma as a single agent, and European Union approval followed in June 2014. Later approvals extended its use to combination therapies and to glioma treatment through 2024.
Facts
Drug ClassMEK inhibitor, anticancer medication 1 Mechanism of ActionInhibits the MEK1 and MEK2 proteins that relay growth signals in cancer cells 1 Approved UseIndicated for the treatment of melanoma and glioma, as monotherapy or combined with dabrafenib 1 First Approved / Isolated Year Significant RiskAs monotherapy, common side effects include rash, diarrhea, tiredness, peripheral edema, nausea and acneiform dermatitis 1 Prescription Status Mechanism of Action Classification
Approval Status ATC ClassSourced to the subject's own accountL: Antineoplastic and Immunomodulating Agents 2 Route of Administration Connections
Sources
1. Trametinib (Wikipedia)
Lead section
MEK inhibitor drug with anti-cancer activity
Lead section, mechanism sentence
It inhibits MEK1 and MEK2
Medical uses section
indicated for the treatment of melanoma and glioma
Lead section, approval sentence
In May 2013, trametinib was approved as a single-agent in the United States for the treatment of people with V600E mutated metastatic melanoma
Lead section, side effects sentence
rash, diarrhea, tiredness, peripheral edema (swelling, especially of ankles and feet), nausea and acneiform dermatitis
https://en.wikipedia.org/wiki/Trametinib, lead section
nti-cancer activity. It inhibits MEK1 and MEK2. It is taken by mouth.
- Regulatory approval status
View the Source2. Anatomical Therapeutic Chemical Classification System (Wikipedia)
WikipediaFirst-level anatomical group codes, Code LQuote, First-level anatomical group codes, Code L
Antineoplastic and immunomodulating agents
3. Wikipedia
Wikipedia contributors, Wikimedia Foundation- Route of Administration: Oral
4. U.S. Food and Drug Administration (openFDA): openFDA drug labels of Trametinib by product type
U.S. Food and Drug Administration (openFDA)count by product typeQuote, count by product type
"term": "HUMAN PRESCRIPTION DRUG", "count": 1
5. ChEMBL: ChEMBL mechanism of action for Trametinib (CHEMBL2103875)
ChEMBLmechanism_of_actionQuote, mechanism_of_action
Dual specificity mitogen-activated protein kinase kinase; MEK1/2 inhibitor
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