Revision as of 23:53, 27 June 2018

Mechanism of action

From the NCI Drug Dictionary: An orally available inhibitor of mitogen-activated protein kinase kinase 1 and 2 (MEK1/2) with potential antineoplastic activity. Binimetinib, noncompetitive with ATP, binds to and inhibits the activity of MEK1/2.

Diseases for which it is used

History of changes in FDA indication

6/27/2018: Initial FDA approval in combination with Encorafenib (Braftovi) "for patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation, as detected by an FDA-approved test."

Also known as

Code names: ARRY-162, ARRY-438162, MEK162
Brand name: Mektovi

@@ Line 2: / Line 2: @@
 From the [http://www.cancer.gov/publications/dictionaries/cancer-drug?cdrid=653635 NCI Drug Dictionary]: An orally available inhibitor of mitogen-activated protein kinase kinase 1 and 2 (MEK1/2) with potential antineoplastic activity. Binimetinib, noncompetitive with ATP, binds to and inhibits the activity of MEK1/2.
-=Preliminary data=
+=Diseases for which it is used=
+*[[Melanoma,_BRAF-mutated|BRAF-mutant melanoma]]
+*[[Melanoma,_NRAS-mutated|NRAS-mutant melanoma]]
-==[[Melanoma]]==
+=History of changes in FDA indication=
-# Ascierto PA, Schadendorf D, Berking C, Agarwala SS, van Herpen CM, Queirolo P, Blank CU, Hauschild A, Beck JT, St-Pierre A, Niazi F, Wandel S, Peters M, Zubel A, Dummer R. MEK162 for patients with advanced melanoma harbouring NRAS or Val600 BRAF mutations: a non-randomised, open-label phase 2 study. Lancet Oncol. 2013 Mar;14(3):249-56. Epub 2013 Feb 13. [http://www.sciencedirect.com/science/article/pii/S147020451370024X link to SD article] [https://www.ncbi.nlm.nih.gov/pubmed/23414587 PubMed]
+*6/27/2018: Initial FDA approval in combination with [[Encorafenib (Braftovi)]] "for patients with unresectable or metastatic [[Melanoma,_BRAF-mutated|melanoma with a BRAF V600E or V600K mutation]], as detected by an FDA-approved test."
-# Dummer R, Schadendorf D, Ascierto PA, Arance A, Dutriaux C, Di Giacomo AM, Rutkowski P, Del Vecchio M, Gutzmer R, Mandala M, Thomas L, Demidov L, Garbe C, Hogg D, Liszkay G, Queirolo P, Wasserman E, Ford J, Weill M, Sirulnik LA, Jehl V, Bozón V, Long GV, Flaherty K. Binimetinib versus dacarbazine in patients with advanced NRAS-mutant melanoma (NEMO): a multicentre, open-label, randomised, phase 3 trial. Lancet Oncol. 2017 Apr;18(4):435-445. Epub 2017 Mar 8. [https://www.thelancet.com/journals/lanonc/article/PIIS1470-2045(17)30180-8/fulltext link to original article] [https://www.ncbi.nlm.nih.gov/pubmed/28284557 PubMed]
-* '''COLUMBUS:''' Dummer R, Ascierto PA, Gogas HJ, Arance A, Mandala M, Liszkay G, Garbe C, Schadendorf D, Krajsova I, Gutzmer R, Chiarion-Sileni V, Dutriaux C, de Groot JWB, Yamazaki N, Loquai C, Moutouh-de Parseval LA, Pickard MD, Sandor V, Robert C, Flaherty KT. Encorafenib plus binimetinib versus vemurafenib or encorafenib in patients with BRAF-mutant melanoma (COLUMBUS): a multicentre, open-label, randomised phase 3 trial. Lancet Oncol. 2018 Mar 21. [Epub ahead of print] [https://www.thelancet.com/journals/lanonc/article/PIIS1470-2045(18)30142-6/fulltext link to original article] '''contains protocol''' [https://www.ncbi.nlm.nih.gov/pubmed/29573941 PubMed]
 =Also known as=
 *'''Code names:''' ARRY-162, ARRY-438162, MEK162
+*'''Brand name:''' Mektovi
 [[Category:Drugs]]
@@ Line 21: / Line 22: @@
 [[Category:Melanoma medications]]
-[[Category:Investigational]]
+[[Category:Drugs FDA approved in 2018]]

Difference between revisions of "Binimetinib (Mektovi)"

Revision as of 23:53, 27 June 2018

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Mechanism of action

Diseases for which it is used

History of changes in FDA indication

Also known as

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