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

General Information of Drug (ID: DMDG8Q3)

• Drug Name: Varlitinib Drug Info
• Synonyms: VARLITINIB; 845272-21-1; ARRY-334543; ARRY334543; ARRY 334543; ARRY-543; UNII-846Y8197W1; ASLAN-001; 846Y8197W1; (R)-N4-(3-chloro-4-(thiazol-2-ylmethoxy)phenyl)-N6-(4-methyl-4,5-dihydrooxazol-2-yl)quinazoline-4,6-diamine; Varlitinib [USAN:INN]; Varlitinib (ARRY334543); Varlitinib free base; Varlitinib (USAN/INN); MLS006011274; GTPL7645; SCHEMBL1384578; CHEMBL2103842; SYN1192; MolPort-028-720-424; EX-A1005; 4-N-[3-chloro-4-(1,3-thiazol-2-ylmethoxy)phenyl]-6-N-[(4R)-4-methyl-4,5-dihydro-1,3-oxazol-2-yl]quinazoline-4,6-diamine

Indication

Disease Entry	ICD 11	Status	REF
Metastatic biliary tract neoplasms	2C14-2C17	Phase 2/3	[1]
Breast cancer	2C60-2C65	Phase 1/2	[2]

• Cross-matching ID:
  PubChem CID: 42642648
  CAS Number: CAS 845272-21-1
  TTD Drug ID: DMDG8Q3

Molecule-Related Drug Atlas

Drug(s) Targeting Erbb2 tyrosine kinase receptor (HER2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Lapatinib	DM3BH1Y	Breast cancer	2C60-2C65	Approved	[4]
Dacomitinib	DMOH8VY	Non-small-cell lung cancer	2C25.Y	Approved	[5]
BIBW 2992	DMTKD7Q	Non-small-cell lung cancer	2C25.Y	Approved	[6]
Merimepodib	DM0HS92	Breast cancer	2C60-2C65	Approved	[7]
NERATINIB MALEATE	DMEDU7B	HER2/NEU overexpressing breast cancer	2C60-2C65	Approved	[8]
Margetuximab	DMKEY6S	HER2-positive breast cancer	2C60-2C65	Approved	[9]
Trastuzumab	DMZQOUX	Breast cancer	2C60-2C65	Approved	[10]
Tucatinib	DMBESUA	HER2-positive breast cancer	2C60-2C65	Approved	[11]
Pertuzumab	DMHJV0X	Adrenal gland neoplasm		Approved	[12]
Masoprocol	DMMVNZ0	Prostate cancer	2C82.0	Approved	[13]

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

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Sorafenib	DMS8IFC	Adenocarcinoma	2D40	Approved	[14]
Lapatinib	DM3BH1Y	Breast cancer	2C60-2C65	Approved	[4]
Gefitinib	DM15F0X	Colon adenocarcinoma		Approved	[15]
Erlotinib	DMCMBHA	Adrenal gland neoplasm		Approved	[16]
Vandetanib	DMRICNP	Solid tumour/cancer	2A00-2F9Z	Approved	[17]
Dacomitinib	DMOH8VY	Non-small-cell lung cancer	2C25.Y	Approved	[18]
BIBW 2992	DMTKD7Q	Non-small-cell lung cancer	2C25.Y	Approved	[6]
SKI-758	DMQ8E9R	Ischemia	8B10-8B11	Approved	[19]
Epidermal growth factor	DMVONE6	Vulnerary	ND56.Z	Approved	[18]
Merimepodib	DM0HS92	Breast cancer	2C60-2C65	Approved	[7]

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	[3]
Erbb2 tyrosine kinase receptor (HER2)	TT6EO5L	ERBB2_HUMAN	Modulator	[3]

References

• [1] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [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: 7645).
• [3] Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
• [4] 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.
• [5] 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: 7422).
• [6] Boehringer Ingelheim. Product Development Pipeline. June 2 2009.
• [7] Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
• [8] 2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85.
• [9] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [10] Her2/neu is not a commonly expressed therapeutic target in melanoma -- a large cohort tissue microarray study. Melanoma Res. 2004 Jun;14(3):207-10.
• [11] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [12] Clinical pipeline report, company report or official report of Roche (2009).
• [13] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [14] Nasopharyngeal carcinoma: Current treatment options and future directions. J Nasopharyng Carcinoma, 2014, 1(16): e16.
• [15] Gefitinib ('Iressa', ZD1839) and new epidermal growth factor receptor inhibitors. Br J Cancer. 2004 Feb 9;90(3):566-72.
• [16] Quantitative prediction of fold resistance for inhibitors of EGFR. Biochemistry. 2009 Sep 8;48(35):8435-48.
• [17] 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.
• [18] 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).
• [19] 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.