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

General Information of Drug (ID: DMWZ2TU)

• Drug Name: CO-1686 Drug Info
• Synonyms: 1374640-70-6; AVL-301; CO1686; UNII-72AH61702G; CNX-419; CO-1686 (AVL-301); Rociletinib(AVL-301,CNX-419,CO-1686); 72AH61702G; N-(3-((2-((4-(4-acetylpiperazin-1-yl)-2-methoxyphenyl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)phenyl)acrylamide; CO 1686; Rociletinib (CO-1686, AVL-301); Rociletinib [USAN:INN]; Tube721; Rociletinib (USAN/INN); Rociletinib (CO-1686); SCHEMBL4177736; GTPL7966; CHEMBL3545308; EX-A228; MolPort-035-395-816; C27H28F3N7O3; HMS3653G08; BDBM149404; BCP07085; AOB87314; ZINC98043800; s7284

Indication

Disease Entry	ICD 11	Status	REF
Lung cancer	2C25.0	Phase 3	[1]
Non-small-cell lung cancer	2C25.Y	Phase 3	[2] , [3] , [4]

• Cross-matching ID:
  PubChem CID: 57335384
  CAS Number: CAS 1374640-70-6
  TTD Drug ID: DMWZ2TU

Molecule-Related Drug Atlas

Drug(s) Targeting Epidermal growth factor receptor (EGFR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Sorafenib	DMS8IFC	Hepatocellular carcinoma	2C12.02	Approved	[6]
Lapatinib	DM3BH1Y	Breast cancer	2C60-2C65	Approved	[7]
Gefitinib	DM15F0X	Solid tumour/cancer	2A00-2F9Z	Approved	[8]
Erlotinib	DMCMBHA	Non-small-cell lung cancer	2C25.Y	Approved	[9]
Vandetanib	DMRICNP	Solid tumour/cancer	2A00-2F9Z	Approved	[10]
Dacomitinib	DMOH8VY	Non-small-cell lung cancer	2C25.Y	Approved	[11]
BIBW 2992	DMTKD7Q	Non-small-cell lung cancer	2C25.Y	Approved	[12]
SKI-758	DMQ8E9R	Ischemia	8B10-8B11	Approved	[13]
Epidermal growth factor	DMVONE6	Vulnerary	ND56.Z	Approved	[11]
Merimepodib	DM0HS92	Breast cancer	2C60-2C65	Approved	[14]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Epidermal growth factor receptor (EGFR)	TTGKNB4	EGFR_HUMAN	Modulator	[5]

References

• [1] ClinicalTrials.gov (NCT02322281) TIGER-3: Open Label, Multicenter Study of Rociletinib (CO-1686) Mono Therapy Versus Single-agent Cytotoxic Chemotherapy in Patients With Mutant EGFR NSCLC Who Have Failed at Least One Previous EGFR-Directed TKI and Platinum-doublet Chemotherapy
• [2] 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. (Ligand id: 7966).
• [3] ClinicalTrials.gov (NCT02322281) TIGER-3: Open Label, Multicenter Study of Rociletinib (CO-1686) Mono Therapy Versus Single-agent Cytotoxic Chemotherapy in Patients With Mutant EGFR NSCLC Who Have Failed at Least One Previous EGFR-Directed TKI and Platinum-doublet Chemotherapy. U.S. National Institutes of Health.
• [4] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [5] Rociletinib in EGFR-mutated non-small-cell lung cancer. N Engl J Med. 2015 Apr 30;372(18):1700-9.
• [6] Nasopharyngeal carcinoma: Current treatment options and future directions. J Nasopharyng Carcinoma, 2014, 1(16): e16.
• [7] Triple negative breast cancer--current status and prospective targeted treatment based on HER1 (EGFR), TOP2A and C-MYC gene assessment. Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub. 2009 Mar;153(1):13-7.
• [8] Gefitinib ('Iressa', ZD1839) and new epidermal growth factor receptor inhibitors. Br J Cancer. 2004 Feb 9;90(3):566-72.
• [9] Quantitative prediction of fold resistance for inhibitors of EGFR. Biochemistry. 2009 Sep 8;48(35):8435-48.
• [10] 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.
• [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: 1797).
• [12] Boehringer Ingelheim. Product Development Pipeline. June 2 2009.
• [13] Synthesis and Src kinase inhibitory activity of a series of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-7-furyl-3-quinolinecarbonitriles. J Med Chem. 2006 Dec 28;49(26):7868-76.
• [14] Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).