| 01 |
CI-1040 (PD184352) |
Phase 2 |
Allosteric, non-ATP competitive inhibitor (MEK1/2) |
Breast cancer, lung cancer, colon cancer and tumours of the pancreas |
Pfizer |
106, 107
|
| 02 |
Mirdametinib (PD-0325901) |
Phase 2 |
ATP competitive inhibitor (MEK1/2) |
Colonic neoplasms, breast neoplasm carcinoma, melanoma skin cancer and NSCLC |
Pfizer |
106, 108
|
| 03 |
AZD-8330 |
Phase 2 |
Non-ATP competitive inhibitor (MEK1/2) |
Advanced solid tumors |
AstraZeneca |
109, 110
|
| 04 |
TAK-733 |
Phase 1 |
Non-ATP competitive inhibitor (MEK1/2) |
Advanced non-hematologic cancers and metastatic advanced melanoma |
Millennium/Takeda |
82, 111
|
| 05 |
GDC-0623 |
Phase 1 |
Allosteric, non-ATP competitive inhibitor (MEK1/2) |
Solid metastatic tumors |
Genentech |
112, 113
|
| 06 |
Refametinib (RDEA-119, BYA-869766) |
Phase 2 |
Allosteric, non-ATP competitive inhibitor (MEK1/2) |
Hepatocellular and colorectal cancer, and melanoma |
Ardea Biosciences/Bayer |
45, 114
|
| 07 |
Pimasertib (AS703026 or MSC1936369B) |
Phase 2 |
Non-ATP competitive inhibitor (MEK1/2) |
Colorectal cancer and multiple myeloma |
Merck and Co. |
45, 115
|
| 08 |
RO4987655 (CH4987655) |
Phase 1 |
Non-ATP competitive inhibitor (MEK1/2) |
Neoplasms |
Hoffman-La Roche |
94, 107
|
| 09 |
RO5126766 (Avutometinib) |
Phase 1 |
ATP competitive inhibitor (MEK1/2) |
Neoplasms |
Hoffman-La Roche |
94, 107
|
| 10 |
EBI-1051 |
Phase 3 |
Non-ATP competitive inhibitor (MEK1/2) |
Melanoma, and thyroid and colorectal cancer |
Shanghai Hengrui Pharmaceutical Co. Ltd. |
116, 117
|
| 11 |
DPS-2 |
Phase 1 |
Non-ATP competitive inhibitor (MEK1/2) |
Colon cancer and melanoma |
De Novo Pharmaceuticals |
99, 118
|
| 12 |
KZ-001 |
Preclinical trials |
Non-ATP competitive inhibitor (MEK1/2) |
Melanoma, and colon and non-small cell lung cancer |
Innovent Biologics |
100, 110
|
| 13 |
BI-847325 |
Phase 1 trials (discontinued) |
ATP-competitive inhibitor (MEK1/2) |
Anaplastic thyroid carcinoma |
Boehringer Ingelheim |
119, 120
|
| 14 |
URML3881 |
Phase 2 |
Allosteric, non-ATP competitive inhibitor (MEK1/2) |
Epithelial ovarian cancer |
University of Rochester Medical Center (URMC) and Array BioPharma |
102
|
| 15 |
WX-554 |
Phase 2 |
ATP-competitive inhibitor (MEK1/2) |
Advanced solid tumor |
Wilex AG, Germany |
103, 121
|
| 16 |
KZ-02 |
Phase 2 |
Allosteric, non-ATP competitive inhibitor (MEK1/2) |
Colorectal cancer |
Kineta |
71
|
