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

General Information of Drug (ID: DM3U9BY)

• Drug Name: RO-5126766 Drug Info
• Synonyms: VS-6766; CH-5126766; Dual Raf/MEK protein kinase inhibitor (cancer), Roche

Indication

Disease Entry	ICD 11	Status	REF
Non-small cell lung cancer	2C25	Phase 2	[1]
Ovarian cancer	2C73	Phase 2	[1]
Solid tumour/cancer	2A00-2F9Z	Phase 1	[2]

• Cross-matching ID:
  PubChem CID: 16719221
  ChEBI ID: CHEBI:78825
  CAS Number: CAS 946128-88-7
  TTD Drug ID: DM3U9BY

Molecule-Related Drug Atlas

Drug(s) Targeting MAPK/ERK kinase kinase (MAP3K)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Arry-162	DM1P6FR	Melanoma	2C30	Approved	[4]
Trametinib	DM2JGQ3	Melanoma	2C30	Approved	[5]
Bay 86-9766	DMPW5SB	Solid tumour/cancer	2A00-2F9Z	Phase 3	[6]
Selumetinib	DMC7W6R	Melanoma	2C30	Phase 3	[7]
MSC1936369B	DMH1DYU	Colorectal cancer	2B91.Z	Phase 2	[8]
E6201	DMOSL9P	Psoriasis vulgaris	EA90	Phase 2	[9]
PD-0325901	DM27D4J	Breast cancer	2C60-2C65	Phase 2	[4]
WX-554	DMRABOS	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[4]
RG7304	DMGFAVQ	Solid tumour/cancer	2A00-2F9Z	Phase 1	[10]
BI-847325	DMY4B6J	Solid tumour/cancer	2A00-2F9Z	Phase 1	[11]

Drug(s) Targeting Serine/threonine-protein kinase Raf (RAF)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
MLN2480	DMBR8NF	Solid tumour/cancer	2A00-2F9Z	Phase 2	[12]
LY3009120	DM6PFCN	Solid tumour/cancer	2A00-2F9Z	Phase 1	[13]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
MAPK/ERK kinase kinase (MAP3K)	TTROQ37	NOUNIPROTAC	Modulator	[3]
Serine/threonine-protein kinase Raf (RAF)	TTQ9K3Y	ARAF_HUMAN; BRAF_HUMAN; RAF1_HUMAN	Modulator	[3]

References

• [1] ClinicalTrials.gov (NCT04625270) A Study of VS-6766 v. VS-6766 + Defactinib in Recurrent Low-Grade Serous Ovarian Cancer With and Without a KRAS Mutation. U.S. National Institutes of Health.
• [2] ClinicalTrials.gov (NCT02407509) Phase I Trial of RO5126766. U.S. National Institutes of Health.
• [3] 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.
• [4] MEK and the inhibitors: from bench to bedside. J Hematol Oncol. 2013; 6: 27.
• [5] Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.
• [6] 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.
• [7] 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.
• [8] 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.
• [9] 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.
• [10] Clinical pipeline report, company report or official report of Roche.
• [11] doi: 10.1158/1535-7163.TARG-13-B281
• [12] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [13] Company report (eli lily)