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

General Information of Drug (ID: DMHOF7T)

• Drug Name: MEHD-7945A Drug Info
• Synonyms: RG-7597; EGFR/HER3 dual monoclonal antibody, Genentech

Indication

Disease Entry	ICD 11	Status	REF
Colorectal cancer	2B91.Z	Phase 2	[1]
Solid tumour/cancer	2A00-2F9Z	Phase 2	[2]

• Cross-matching ID: TTD Drug ID: DMHOF7T

Molecule-Related Drug Atlas

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

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Sorafenib	DMS8IFC	Adenocarcinoma	2D40	Approved	[5]
Lapatinib	DM3BH1Y	Breast cancer	2C60-2C65	Approved	[6]
Gefitinib	DM15F0X	Colon adenocarcinoma		Approved	[7]
Erlotinib	DMCMBHA	Adrenal gland neoplasm		Approved	[8]
Vandetanib	DMRICNP	Solid tumour/cancer	2A00-2F9Z	Approved	[9]
Dacomitinib	DMOH8VY	Non-small-cell lung cancer	2C25.Y	Approved	[10]
BIBW 2992	DMTKD7Q	Non-small-cell lung cancer	2C25.Y	Approved	[11]
SKI-758	DMQ8E9R	Ischemia	8B10-8B11	Approved	[12]
Epidermal growth factor	DMVONE6	Vulnerary	ND56.Z	Approved	[10]
Merimepodib	DM0HS92	Breast cancer	2C60-2C65	Approved	[13]

Drug(s) Targeting Erbb3 tyrosine kinase receptor (Erbb-3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
MM-141	DM2RJ4D	Pancreatic cancer	2C10	Phase 2	[14]
Seribantumab	DMYT470	Colorectal cancer	2B91.Z	Phase 2	[15]
CDX-3379	DM5GKYD	Squamous cell carcinoma	2B60-2D01	Phase 2	[15]
MM-121	DMDJRU1	Breast cancer	2C60-2C65	Phase 2	[16]
Elisidepsin	DMB38KH	Psoriasis vulgaris	EA90	Phase 2	[17]
Zenocutuzumab	DM1FLHH	Pancreatic cancer	2C10	Phase 2	[18]
Sym013	DMZM6I2	Epithelial ovarian cancer	2B5D	Phase 1/2	[19]
Zenocutuzomab	DMMQGPE	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[20]
LJM716	DMGTB5N	Breast cancer	2C60-2C65	Phase 1/2	[21]
AMG888/U3-1287	DMEF4L5	Non-small-cell lung cancer	2C25.Y	Phase 1/2	[22]

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]
Erbb3 tyrosine kinase receptor (Erbb-3)	TTDC8N2	ERBB3_HUMAN	Modulator	[4]

References

• [1] ClinicalTrials.gov (NCT01577173) A Study of MEHD7945A Versus Cetuximab in Patients With Recurrent/Metastatic Squamous Cell Carcinoma of The Head And Neck
• [2] ClinicalTrials.gov (NCT01652482) A Study of MEHD7945A + FOLFIRI Versus Cetuximab + FOLFIRI in Second Line in Patients With KRAS Wild-Type Metastatic Colorectal Cancer. U.S. National Institutes of Health.
• [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] Company report (Biooncology)
• [5] Nasopharyngeal carcinoma: Current treatment options and future directions. J Nasopharyng Carcinoma, 2014, 1(16): e16.
• [6] 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.
• [7] Gefitinib ('Iressa', ZD1839) and new epidermal growth factor receptor inhibitors. Br J Cancer. 2004 Feb 9;90(3):566-72.
• [8] Quantitative prediction of fold resistance for inhibitors of EGFR. Biochemistry. 2009 Sep 8;48(35):8435-48.
• [9] 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.
• [10] 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).
• [11] Boehringer Ingelheim. Product Development Pipeline. June 2 2009.
• [12] 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.
• [13] Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
• [14] MM-141, an IGF-IR- and ErbB3-directed bispecific antibody, overcomes network adaptations that limit activity of IGF-IR inhibitors. Mol Cancer Ther. 2014 Feb;13(2):410-25.
• [15] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [16] Company report (Merrimack)
• [17] Molecular pharmacodynamics of PM02734 (elisidepsin) as single agent and in combination with erlotinib; synergistic activity in human non-small cell lung cancer cell lines and xenograft models. Eur J Cancer. 2009 Jul;45(10):1855-64.
• [18] Zenocutuzumab, a HER2xHER3 Bispecific Antibody, Is Effective Therapy for Tumors Driven by NRG1 Gene Rearrangements. Cancer Discov. 2022 May 2;12(5):1233-1247.
• [19] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [20] Clinical pipeline report, company report or official report of Merus.
• [21] An antibody that locks HER3 in the inactive conformation inhibits tumor growth driven by HER2 or neuregulin. Cancer Res. 2013 Oct 1;73(19):6024-35.
• [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: 1798).