Table 1 Approval and status of MEK inhibitors in active clinical development
From: MEK inhibitors for the treatment of non-small cell lung cancer
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 | 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 |