TTD Target ID: TTDC00164

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

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Professor in Department of Pharmacy
National University of Singapore, Singapore

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