Table 1.
MEK inhibitors in clinical trials
| MEK Inhibitors | Target | Clinical trial | Common toxicities | Tumors | References |
|---|---|---|---|---|---|
|
Trametinib (GSK1120212) |
MEK1/2 |
III |
Rash, diarrhea, retinopathy |
Melanoma, colorectal cancer |
[67] |
|
Pimasertib (AST03026) |
MEK1/2 |
I |
Nausea, rash, visual disturbance, asthenia |
Colorectal, multiple myeloma |
[74] |
|
Selumetinib (AZD6244) |
MEK1 |
II |
Nausea, rash, xerostomia |
Melanoma, NSCLC |
[76-85] |
|
PD-0325901 |
MEK1/2 |
I |
Rash, fatigue, blurry vision, diarrhea |
Melanoma, NSCLC |
[89-91] |
|
Refametinib (RDEA119) |
MEK1/2 |
II |
Rash |
Hepatocellular cancer, melanoma, colorectal cancer |
[94,95] |
|
TAK733 |
MEK1/2 |
I |
Not available |
Melanoma, NSCLC, colorectal, breast cancer |
[96,97] |
|
MEK162 |
MEK1/2 |
I/II |
Rash, dermatitis, CPK elevation |
N-Ras melanoma, NSCLC, pancreatic cancer |
[100] |
|
RO5126766 |
Raf/MEK1/2 |
I |
Rash, diarrhea, CPK elevation |
Melanoma |
[101] |
|
WX-554 |
MEK1/2 |
II |
Not available |
Advanced solid tumors |
[102] |
|
RO4987655 |
MEK1 |
I |
Rash, GI disorders |
Melanoma |
[104] |
|
GDC-0973 |
MEK1 |
I |
Rash, nausea, dysguesia, elevated CK |
Melanoma, Pancreatic cancer, endometrial cancer |
[108] |
| AZD8330 | MEK1/2 | I | Mental status change, rash, nausea | Advanced solid tumors | [110] |