Table 1.

Approval and status of MEK inhibitors in active clinical development

Drug	Developer or owner	Target	In vitro IC50 for MEK (nM)	Tumor	Approval/development status
Trametinib (GSK1120212, JTP-74057)	NOVARTIS	MEK1/2	0.7 (MEK1), 0.9 (MEK2) [24]	Melanoma, NSCLC, thyroid cancer	Approved by US FDA (05/2013)
Binimetinib (MEK162, ARRY-438162)	ARRAY BIOPHARMA INC	MEK1/2	12 [28]	Melanoma	Approved by US FDA (06/2018)
Selumetinib (AZD6244, ARRY-142886)	ASTRAZENECA	MEK1/2	14 [23]	Neurofibroma	Approved by US FDA (4/2020)
Cobimetinib (GDC-0973, XL518)	GENENTECH INC	MEK1/2	5 [29]	Melanoma	Approved by US FDA (11/2015)
Pimasertib (AS703026, MSC1936369B)	Merck KGaA	MEK1/2	30 [30]	Melanoma, ovarian cancer, pancreatic adenocarcinoma, solid tumor	I/II
Mirdametinib (PD-0325901)	Spring Works Therapeutics	MEK1/2	0.1–1000 [31]	Neurofibroma, solid tumor	I/II
Refametinib (BAY 86–9766, RDEA119)	Bayer AG	MEK1/2	19 (MEK1), 47 (MEK2) [32]	Biliary tract cancer, hepatocellular cancer, solid tumor	I/II
E6201	Eisai Co Ltd./Strategia Theraputics	MEK1/FLT3	NA	Melanoma with brain metastases, solid tumor	I
GDC-0623 (RG 7421)	Genentech, Inc.	MEK1	0.13 [33, 34]	Solid tumor	I
CH5126766(RO5126766)	Chugai Pharmaceutical Co., Roche	MEK/BRAF/CRAF	160/190/56 [35]	KRAS-mutant NSCLC, solid tumor	I
HL-085	Shanghai Kechow Pharma, Inc.	MEK1/2	1.9–10 [27]	Melanoma, NSCLC, solid tumor	I/II
SHR7390	HENGRUI MEDICINE	MEK1/2	NA	Breast neoplasm, solid tumor	I/II
TQ-B3234	CHIATAI TIANQING	MEK1/2	NA	Solid tumor	I
CS-3006	CSTONE PHARMACEUTICALS	MEK1/2	NA	Solid tumor	I
FCN-159	FOSUN PHARMA	MEK1/2	NA	NRAS-aberrant (Ia) and NRAS-mutant (Ib) melanoma	I