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Trametinib information


Trametinib
Clinical data
Trade namesMekinist, Spexotras
Other namesGSK1120212
AHFS/Drugs.comMonograph
MedlinePlusa613040
License data
  • US DailyMed: Trametinib
Routes of
administration
By mouth
ATC code
  • L01EE01 (WHO)
Legal status
Legal status
  • AU: S4 (Prescription only)[1]
  • CA: ℞-only[2][3]
  • US: ℞-only[4]
  • EU: Rx-only[5][6][7]
Identifiers
IUPAC name
  • N-(3-{3-Cyclopropyl-5-[(2-fluoro-4-iodophenyl)amino]-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydropyrido[4,3-d]pyrimidin-1(2H)-yl}phenyl)acetamide
CAS Number
  • 871700-17-3
PubChem CID
  • 11707110
DrugBank
  • DB08911
ChemSpider
  • 9881833
UNII
  • 33E86K87QN
KEGG
  • D10175
ChEBI
  • CHEBI:75998
ChEMBL
  • ChEMBL2103875
CompTox Dashboard (EPA)
  • DTXSID901007381 Edit this at Wikidata
ECHA InfoCard100.158.135 Edit this at Wikidata
Chemical and physical data
FormulaC26H23FIN5O4
Molar mass615.404 g·mol−1
3D model (JSmol)
  • Interactive image
SMILES
  • Ic1ccc(c(F)c1)N\C3=C\2/C(=O)N(C(=O)N(C/2=C(\C(=O)N3C)C)c4cccc(NC(=O)C)c4)C5CC5
InChI
  • InChI=1S/C26H23FIN5O4/c1-13-22-21(23(31(3)24(13)35)30-20-10-7-15(28)11-19(20)27)25(36)33(17-8-9-17)26(37)32(22)18-6-4-5-16(12-18)29-14(2)34/h4-7,10-12,17,30H,8-9H2,1-3H3,(H,29,34)
  • Key:LIRYPHYGHXZJBZ-UHFFFAOYSA-N

Trametinib, sold under the brand name Mekinist among others, is an anticancer medication used for the treatment of melanoma[4][5] and glioma.[6][7] It is a MEK inhibitor drug with anti-cancer activity.[8] It inhibits MEK1 and MEK2.[8] It is taken by mouth.[4][5]

The most common side effects include rash, diarrhea, tiredness, peripheral edema (swelling, especially of ankles and feet), nausea and acneiform dermatitis (acne-like inflammation of the skin).[5] When taken in combination with dabrafenib the most common side effects include fever, tiredness, nausea, chills, headache, diarrhea, vomiting, joint pain and rash.[5]

In May 2013, trametinib was approved as a single-agent by the US Food and Drug Administration for the treatment of people with V600E mutated metastatic melanoma.[9][10] It was approved for medical use in the European Union in June 2014.[5]

  1. ^ "Prescription medicines: registration of new chemical entities in Australia, 2014". Therapeutic Goods Administration (TGA). 21 June 2022. Archived from the original on 10 April 2023. Retrieved 10 April 2023.
  2. ^ "Product monograph brand safety updates". Health Canada. February 2024. Retrieved 24 March 2024.
  3. ^ "Regulatory Decision Summary for Mekinist". Drug and Health Products Portal. 24 July 2023. Retrieved 2 April 2024.
  4. ^ a b c "Mekinist- trametinib tablet, film coated". DailyMed. 22 June 2022. Archived from the original on 26 November 2022. Retrieved 3 January 2023.
  5. ^ a b c d e f "Mekinist EPAR". European Medicines Agency. 17 September 2018. Archived from the original on 9 August 2021. Retrieved 27 February 2023. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  6. ^ a b "Spexotras Product information". Union Register of medicinal products. 8 January 2024. Retrieved 14 January 2024.
  7. ^ a b "Spexotras EPAR". European Medicines Agency. 9 November 2023. Retrieved 14 January 2024.
  8. ^ a b "Trametinib". NCI Drug Dictionary. U.S. Department of Health and Human Services, National Institutes of Health, National Cancer Institute. Archived from the original on 3 January 2023. Retrieved 28 February 2023. Public Domain This article incorporates text from this source, which is in the public domain.
  9. ^ "Drug Approval Package: Mekinist (trametinib) Tablets NDA #204114". U.S. Food and Drug Administration (FDA). 8 July 2013. Archived from the original on 27 October 2022. Retrieved 27 February 2023.
  10. ^ "GSK melanoma drugs add to tally of U.S. drug approvals". Reuters. 30 May 2013. Archived from the original on 24 September 2015. Retrieved 5 July 2021.

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rash, joint pain, fever and tiredness. When taken in combination with trametinib, the most common side effects include fever, tiredness, nausea, chills...

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evaluated as a combination treatment against solid tumors together with trametinib in a clinical trial sponsored by the National Cancer Institute. In this...

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include uveal melanoma (failed), and differentiated thyroid carcinoma. Trametinib (GSK1120212), FDA-approved to treat BRAF-mutated melanoma. Also studied...

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BRAF inhibitors, such as vemurafenib and dabrafenib; and a MEK inhibitor trametinib. Important prognosis factors for nodular melanoma include: Thickness Ulceration...

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BRAF inhibitors, such as vemurafenib and dabrafenib; and a MEK inhibitor trametinib. When arising in the nailbed of a digit, the evidence suggests that digit-sparing...

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Rosuvastatin Crestor 1.37 in hemodialysis patients Lisinopril Prinivil and others 1.38 Ivacaftor Kalydeco 2.2–2.9 Trametinib Mekinist 6.0 at 2 mg once daily...

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metastatic melanoma that harbors BRAF V600E mutation MEK inhibitors (trametinib, MEK162) are used in experiments, often in combination with BRAF inhibitors...

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BRAF inhibitors, such as vemurafenib and dabrafenib; and a MEK inhibitor trametinib. In February 2024, the Food and Drug Administration approved the first...

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trial results compared vemurafenib with the combination of dabrafenib and trametinib for metastatic melanoma. Vemurafenib was approved in the United States...

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Elranatamab

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Momelotinib Pacritinib Ruxolitinib MAP2K Binimetinib Cobimetinib Selumetinib Trametinib EML4-ALK Crizotinib Entrectinib Lorlatinib Bruton's Acalabrutinib Ibrutinib...

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Anaplastic thyroid cancer

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thyroid cancer harboring such mutations. The combination of dabrafenib and trametinib has shown significant increases in overall survival and has been approved...

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ALK inhibitors with MEK inhibitors: brigatinib+binimetinib, ceritinib+trametinib, and alectinib+cobimetinib. Results for the last two are expected around...

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ATC code L01

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