Table 1 MEK inhibitors in clinical trials

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]