Details of the Drug-Related molecule(s) Interaction Atlas

General Information of DTT (ID: TTROQ37)

• DTT Name: MAPK/ERK kinase kinase (MAP3K) DTT Info
• Gene Name: MAP3K

Molecule-Related Drug & Molecule List

2 Approved Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
ARRY-162	DM1P6FR	Melanoma	2C30	Approved	[1]
Trametinib	DM2JGQ3	Melanoma	2C30	Approved	[2]

11 Clinical Trial Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BAY 86-9766	DMPW5SB	Solid tumour/cancer	2A00-2F9Z	Phase 3	[3]
Selumetinib	DMC7W6R	Neurofibromatosis type 1	LD2D.10	Phase 3	[4]
E6201	DMOSL9P	Psoriasis vulgaris	EA90	Phase 2	[5]
MSC1936369B	DMH1DYU	Colorectal cancer	2B91.Z	Phase 2	[6]
PD-0325901	DM27D4J	Breast cancer	2C60-2C65	Phase 2	[1]
RO-5126766	DM3U9BY	Non-small-cell lung cancer	2C25	Phase 2	[7]
WX-554	DMRABOS	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[1]
ARRY-300	DMMPTCK	Solid tumour/cancer	2A00-2F9Z	Phase 1	[8]
BI-847325	DMY4B6J	Solid tumour/cancer	2A00-2F9Z	Phase 1	[9]
RG7304	DMGFAVQ	Solid tumour/cancer	2A00-2F9Z	Phase 1	[10]
TAK-733	DMC4RNA	Solid tumour/cancer	2A00-2F9Z	Phase 1	[1]

3 Discontinued Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
AZD8330	DMUKNQ5	Solid tumour/cancer	2A00-2F9Z	Discontinued in Phase 1	[1]
RG-7167	DMGLRK0	Solid tumour/cancer	2A00-2F9Z	Discontinued in Phase 1	[11]
RO-4987655	DMMF0OP	Solid tumour/cancer	2A00-2F9Z	Discontinued in Phase 1	[1]

6 Investigative Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
CIP-137401	DMZ2WS9	Solid tumour/cancer	2A00-2F9Z	Investigative	[11]
G-573	DMC54UG	Solid tumour/cancer	2A00-2F9Z	Investigative	[11]
MEK inhibitor I	DMYJI90	Discovery agent	N.A.	Investigative	[12]
NSC-686549	DM0164B	Discovery agent	N.A.	Investigative	[13]
RO-4920506	DMD9SCI	Solid tumour/cancer	2A00-2F9Z	Investigative	[11]
SL-327	DMYJV4I	Discovery agent	N.A.	Investigative	[13]

References

• [1] MEK and the inhibitors: from bench to bedside. J Hematol Oncol. 2013; 6: 27.
• [2] Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.
• [3] RDEA119/BAY 869766: a potent, selective, allosteric inhibitor of MEK1/2 for the treatment of cancer.Cancer Res.2009 Sep 1;69(17):6839-47.
• [4] Intrinsic resistance to selumetinib, a selective inhibitor of MEK1/2, by cAMP-dependent protein kinase A activation in human lung and colorectal cancer cells.Br J Cancer.2012 May 8;106(10):1648-59.
• [5] E6201, a novel kinase inhibitor of mitogen-activated protein kinase/extracellular signal-regulated kinase kinase-1 and mitogen-activated protein kinase/extracellular signal-regulated kinase kinase kinase-1: in vivo effects on cutaneous inflammatory responses by topical administration. J Pharmacol Exp Ther. 2010 Oct;335(1):23-31.
• [6] Antitumor activity of pimasertib, a selective MEK 1/2 inhibitor, in combination with PI3K/mTOR inhibitors or with multi-targeted kinase inhibitors in pimasertib-resistant human lung and colorectal cancer cells. Int J Cancer. 2013 Nov;133(9):2089-101.
• [7] The dual RAF/MEK inhibitor CH5126766/RO5126766 may be a potential therapy for RAS-mutated tumor cells.PLoS One.2014 Nov 25;9(11):e113217.
• [8] MEK and the inhibitors: from bench to bedside. J Hematol Oncol. 2013 Apr 12;6:27.
• [9] doi: 10.1158/1535-7163.TARG-13-B281
• [10] Clinical pipeline report, company report or official report of Roche.
• [11] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2063).
• [12] Beyond U0126. Dianion chemistry leading to the rapid synthesis of a series of potent MEK inhibitors. Bioorg Med Chem Lett. 2004 Mar 22;14(6):1483-6.
• [13] A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. Proc Natl Acad Sci U S A. 2007 Dec 18;104(51):20523-8.