Target
Information |
Name | Dual specificity mitogen-activated protein kinase kinase |
Type of target | Clinical trial target |
Synonyms | ERK activator kinase |
MAP kinase kinase |
MAPKK |
MEK |
Disease | Cancer, unspecific [ICD9: 140-229 ICD10: C00-C96] | [1] |
Heart failure [ICD9: 428 ICD10: I50] | [1] |
Immunodeficiency [ICD9: 279.3 ICD10: D84.9] | [1] |
Inflammation | [1] |
Proliferative diseases | [1] |
Psoriasis [ICD9: 696 ICD10: L40] | [1] |
Restenosis | [1] |
Stroke [ICD9: 434.91 ICD10: I61-I63] | [1] |
Drug(s) | RG7421+RG7204 |  | Phase III | Metastatic melanoma BRAF mutation positive | |
ARRY-162 |  | Phase II | Malignant melanoma (BRAFV600E or NRAS mutations) (see also solid tumors) | |
AZD6244 |  | Phase II | Non Small Cell Lung Cancer/Melanoma | [2] |
BAY 86-9766 |  | Phase II | First-line liver cancer | |
E6201 |  | Phase II | Psoriasis | |
GSK1120212 |  | Phase II | Solid Tumors and Lymphoma | [3] |
MEK-Inhibitor |  | Phase II | Cancer | |
MEK162 |  | Phase II | Melanoma | |
BAY 86-9766 |  | Phase I/II | First-line pancreatic cancer | |
GDC-0973 |  | Phase Ib | Solid tumours | [4] |
ARRY-162 |  | Phase I | Late-stage solid tumors (see also skin) | |
ARRY-300 |  | Phase I | Cancer | |
AZD8330 |  | Phase I | Solid tumours | [2] |
Anti-Mek |  | Phase I | Cancer | [5] |
GDC-0623 |  | Phase I | Solid tumours | [6] |
MSC2015103B |  | Phase I | Solid Tumors | |
RG7167 |  | Phase I | Solid Tumors | |
RG7167 |  | Phase I | Solid tumors | |
RG7304 |  | Phase I | Solid tumors | |
RG7420 |  | Phase I | Solid tumors | |
SAR245408/MSC1936369B combination therapy |  | Phase I | Solid Tumors | |
SAR245409/MSC1936369B combination therapy |  | Phase I | Solid Tumors | |
TAK-733 |  | Phase I | Solid Tumors | |
TAK-733 |  | Phase I | Solid tumors | |
PD-0325901 |  | Terminated in Phase I | Solid tumours | [7] |
PD-0325901 |  | Terminated in Phase II | NSCLC, melanoma, breast, colon cancer | [7] |
Related US Patent | 6,310,060 |
6,440,966 |
6,455,582 |
6,469,004 |
6,506,798 |
6,638,945 |
Target Validation | Click to Find Target Validation Information. |
Inhibitor | AZD6244 |  | [2] |
AZD8330 |  | [2] |
Anti-Mek |  | [5] |
GDC-0623 |  | [6] |
GDC-0973 |  | [4] |
GSK1120212 |  | [3] |
PD-0325901 |  | [7] |
U-0126 |  | [8] |
Cross References |
3D Structure
Related Literature
On-Line
Medical Dictionary |
Ref 1 | Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. To Reference |
Ref 2 | AstraZeneca. Product Development Pipeline. January 29 2009. To Reference |
Ref 3 | GSK. Product Development Pipeline. February 2009. To Reference |
Ref 4 | 2011 Pipeline of Genentech. To Reference |
Ref 5 | Roche. Product Development Pipeline. July 29 2009. To Reference |
Ref 6 | 2011 Pipeline of Genentech. To Reference |
Ref 7 | A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22. To Reference |
Ref 8 | Biochem J. 2000 Oct 1;351(Pt 1):95-105.Specificity and mechanism of action of some commonly used protein kinase inhibitors. To Reference |