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

General Information of Drug (ID: DM0LXBW)

• Drug Name: RG-7256 Drug Info
• Synonyms: B-raf inhibitor (melanoma), Roche/Plexxikon

Indication

Disease Entry	ICD 11	Status	REF
Melanoma	2C30	Discontinued in Phase 1	[1]

• Cross-matching ID: TTD Drug ID: DM0LXBW

Molecule-Related Drug Atlas

Drug(s) Targeting Serine/threonine-protein kinase B-raf (BRAF)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Dabrafenib	DMX6OE3	Melanoma	2C30	Approved	[3]
Vemurafenib	DM62UG5	Melanoma	2C30	Approved	[4]
LGX818	DMNQXV8	Melanoma	2C30	Approved	[5]
PLX8394	DMRTD7I	Solid tumour/cancer	2A00-2F9Z	Phase 2	[6]
CEP-32496	DMAO04B	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[7]
BGB-283	DMVYTG7	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[8]
ARQ 736	DMP9ZT1	Solid tumour/cancer	2A00-2F9Z	Phase 1	[9]
RO-5212054	DML4C3Q	Solid tumour/cancer	2A00-2F9Z	Phase 1	[10]
ASN003	DMJCX6D	Solid tumour/cancer	2A00-2F9Z	Phase 1	[11]
BMS-908662	DM3K8VM	Solid tumour/cancer	2A00-2F9Z	Phase 1	[12]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Serine/threonine-protein kinase B-raf (BRAF)	TTWCGQT	BRAF_HUMAN	Inhibitor	[2]

References

• [1] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800022593)
• [2] First-in-Man Dose-Escalation Study of the Selective BRAF Inhibitor RG7256 in Patients with BRAF V600-Mutated Advanced Solid Tumors. Target Oncol. 2016 Apr;11(2):149-56.
• [3] Clinical pipeline report, company report or official report of GlaxoSmithKline (2011).
• [4] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [5] Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
• [6] Identification of PLX4032-resistance mechanisms and implications for novel RAF inhibitors. Pigment Cell Melanoma Res. 2014 Mar;27(2):253-62.
• [7] Clinical pipeline report, company report or official report of Ambit Biosciences.
• [8] BGB-283, a Novel RAF Kinase and EGFR Inhibitor, Displays Potent Antitumor Activity in BRAF-Mutated Colorectal Cancers. Mol Cancer Ther. 2015 Oct;14(10):2187-97.
• [9] National Cancer Institute Drug Dictionary (drug id 688029).
• [10] National Cancer Institute Drug Dictionary (drug id 680347).
• [11] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [12] Clinical pipeline report, company report or official report of Exelixis (2011).