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

General Information of Drug (ID: DMGFAVQ)

• Drug Name: RG7304 Drug Info

Indication

Disease Entry	ICD 11	Status	REF
Solid tumour/cancer	2A00-2F9Z	Phase 1	[1]

• Cross-matching ID:
  PubChem CID: 74890577
  TTD Drug ID: DMGFAVQ

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	[3]
Trametinib	DM2JGQ3	Melanoma	2C30	Approved	[4]
Bay 86-9766	DMPW5SB	Solid tumour/cancer	2A00-2F9Z	Phase 3	[5]
Selumetinib	DMC7W6R	Melanoma	2C30	Phase 3	[6]
MSC1936369B	DMH1DYU	Colorectal cancer	2B91.Z	Phase 2	[7]
RO-5126766	DM3U9BY	Non-small cell lung cancer	2C25	Phase 2	[8]
E6201	DMOSL9P	Psoriasis vulgaris	EA90	Phase 2	[9]
PD-0325901	DM27D4J	Breast cancer	2C60-2C65	Phase 2	[3]
WX-554	DMRABOS	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[3]
BI-847325	DMY4B6J	Solid tumour/cancer	2A00-2F9Z	Phase 1	[10]

Drug(s) Targeting Raf messenger RNA (Raf mRNA)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
MLN2480	DMBR8NF	Solid tumour/cancer	2A00-2F9Z	Phase 2	[11]
SPN-803	DM8O2AQ	Parkinson disease	8A00.0	Phase 1	[11]
LXH254	DMQE9PS	Non-small-cell lung cancer	2C25.Y	Phase 1	[12]
ICo-007	DM79W8K	Diabetic macular edema	9B71.02	Phase 1	[13]
LErafAON	DMNHPOT	Solid tumour/cancer	2A00-2F9Z	Phase 1	[14]
DEBROMOHYMENIALDISINE	DMDLER8	Discovery agent	N.A.	Investigative	[15]
ZM-336372	DMD5JYQ	Discovery agent	N.A.	Investigative	[16]
6-[(E)-2-(4-Fluoro-phenyl)-vinyl]-9H-purine	DMDNG8F	Discovery agent	N.A.	Investigative	[17]
PLX-ORI3	DMZG1L5	Solid tumour/cancer	2A00-2F9Z	Investigative	[11]
6-Benzylsulfanyl-9H-purine	DMI7FNZ	Discovery agent	N.A.	Investigative	[17]

Drug(s) Targeting Microtubule-associated protein (MAP)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Demecolcine	DMCZQGK	Solid tumour/cancer	2A00-2F9Z	Approved	[18]
Costunolide	DMU6OB4	Discovery agent	N.A.	Investigative	[19]

Drug(s) Targeting A-Raf messenger RNA (ARAF mRNA)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
ISIS 9065	DMH50RX	Discovery agent	N.A.	Investigative	[20]
ISIS 9063	DM8E5RO	Discovery agent	N.A.	Investigative	[20]
ISIS 10228	DMESKQX	Discovery agent	N.A.	Investigative	[21]
ISIS 9064	DMBMTGP	Discovery agent	N.A.	Investigative	[20]
ISIS 9061	DMFAL2E	Discovery agent	N.A.	Investigative	[20]
ISIS 9071	DMWY2XB	Discovery agent	N.A.	Investigative	[20]
ISIS 9060	DMZL7SW	Discovery agent	N.A.	Investigative	[20]
ISIS 9070	DMU0HQF	Discovery agent	N.A.	Investigative	[20]
ISIS 9069	DM5C86M	Discovery agent	N.A.	Investigative	[20]
ISIS 9067	DML8HCZ	Discovery agent	N.A.	Investigative	[20]

Drug(s) Targeting B-Raf messenger RNA (BRAF mRNA)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
MLN2480	DMBR8NF	Solid tumour/cancer	2A00-2F9Z	Phase 2	[22]
SPN-803	DM8O2AQ	Parkinson disease	8A00.0	Phase 1	[22]
PLX-4720	DMBK9AM	Cutaneous melanoma	2C30	Phase 1	[23]
L-779450	DM51B74	Discovery agent	N.A.	Investigative	[24]
ZM-336372	DMD5JYQ	Discovery agent	N.A.	Investigative	[16]
PLX-ORI3	DMZG1L5	Solid tumour/cancer	2A00-2F9Z	Investigative	[22]
2-(Phenylamino)-6-(3-acetamidophenyl)pyrazine	DMPUARE	Discovery agent	N.A.	Investigative	[25]
ISIS 13741	DMC7Q38	Discovery agent	N.A.	Investigative	[26]
ISIS 14144	DMWIKD5	Discovery agent	N.A.	Investigative	[26]
PMID26061392C2	DMHZOIU	Discovery agent	N.A.	Investigative	[27]

Drug(s) Targeting ERK activator kinase (MEK)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Arry-162	DM1P6FR	Melanoma	2C30	Approved	[28]
HL-085	DMJDVCW	Melanoma	2C30	Phase 1/2	[29]
GDC-0623	DMDY08K	Solid tumour/cancer	2A00-2F9Z	Phase 1	[30]
BI 3011441	DMFJGUL	Solid tumour/cancer	2A00-2F9Z	Phase 1	[31]
Pyridinone compound 1	DM2GR5Q	N. A.	N. A.	Patented	[32]
Quinazolines and azaquinazoline derivative 1	DME24BI	N. A.	N. A.	Patented	[32]
PMID28594589-Compound-TABLE3C2	DMVYG0U	N. A.	N. A.	Patented	[32]
Benzoheterocyclic compound 1	DM3K25J	N. A.	N. A.	Patented	[32]
Benzoimidazole derivative 1	DMUJFCK	N. A.	N. A.	Patented	[32]
PMID28594589-Compound-TABLE3C12	DMPK7IU	N. A.	N. A.	Patented	[32]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
A-Raf messenger RNA (ARAF mRNA)	TT5TURO	ARAF_HUMAN	Inhibitor	[2]
B-Raf messenger RNA (BRAF mRNA)	TT0EOB8	BRAF_HUMAN	Inhibitor	[2]
ERK activator kinase (MEK)	TTZCRP3	NOUNIPROTAC	Modulator	[2]
MAPK/ERK kinase kinase (MAP3K)	TTROQ37	NOUNIPROTAC	Inhibitor	[2]
Microtubule-associated protein (MAP)	TT1EDJZ	MAP1A_HUMAN; MAP1B_HUMAN	Modulator	[2]
Raf messenger RNA (Raf mRNA)	TTAN5W2	RAF1_HUMAN	Modulator	[2]

References

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• [10] doi: 10.1158/1535-7163.TARG-13-B281
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• [14] Combination with liposome-entrapped, ends-modified raf antisense oligonucleotide (LErafAON) improves the anti-tumor efficacies of cisplatin, epirubicin, mitoxantrone, docetaxel and gemcitabine. Anticancer Drugs. 2004 Mar;15(3):243-53.
• [15] Aldisine alkaloids from the Philippine sponge Stylissa massa are potent inhibitors of mitogen-activated protein kinase kinase-1 (MEK-1). J Med Chem. 2002 Jan 17;45(2):529-32.
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• [22] 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: 1943).
• [23] Comprehensive analysis of kinase inhibitor selectivity. Nat Biotechnol. 2011 Oct 30;29(11):1046-51.
• [24] The identification of potent and selective imidazole-based inhibitors of B-Raf kinase. Bioorg Med Chem Lett. 2006 Jan 15;16(2):378-81.
• [25] Novel inhibitors of B-RAF based on a disubstituted pyrazine scaffold. Generation of a nanomolar lead. J Med Chem. 2006 Jan 12;49(1):407-16.
• [26] US patent application no. 5,981,731, Antisense oligonucleotide modulation of B-raf gene expression.
• [27] Photoactivatable Prodrugs of Antimelanoma Agent Vemurafenib. ACS Chem Biol. 2015 Sep 18;10(9):2099-107.
• [28] 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
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• [31] Clinical pipeline report, company report or official report of Boehringer Ingelheim.
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