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

General Information of Drug (ID: DMZE6Y9)

• Drug Name: TT-100 Drug Info
• Synonyms: TT-100, TriAct; Dual IGF-1/EGFR inhibitor (non-small-cell lung cancer), TriAct

Indication

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

• Cross-matching ID: TTD Drug ID: DMZE6Y9

Molecule-Related Drug Atlas

Drug(s) Targeting Insulin-like growth factor I receptor (IGF1R)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Teprotumumab	DM4L59B	Graves disease	5A02.0	Approved	[3]
Mecasermin	DM1O3BY	Growth failure	LD2F.1Y	Approved	[4]
Somatomedin-1	DMZ9FAO	Hormone deficiency	5A61.1	Approved	[5]
OSI-906	DMHKZLF	Solid tumour/cancer	2A00-2F9Z	Phase 3	[6]
Rinfabate	DML9FD4	Solid tumour/cancer	2A00-2F9Z	Phase 2/3	[7]
MM-141	DM2RJ4D	Pancreatic cancer	2C10	Phase 2	[8]
AMG 479	DM0DRAZ	Breast cancer	2C60-2C65	Phase 2	[9]
VPI-2690B	DMUQZT4	Diabetic nephropathy	GB61.Z	Phase 2	[10]
AXL-1717	DMTQ1Y3	Solid tumour/cancer	2A00-2F9Z	Phase 2	[11]
R1507	DMIUS5X	Graves ophthalmopathy	9C82.3	Phase 2	[12]

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	[13]
Lapatinib	DM3BH1Y	Breast cancer	2C60-2C65	Approved	[14]
Gefitinib	DM15F0X	Solid tumour/cancer	2A00-2F9Z	Approved	[15]
Erlotinib	DMCMBHA	Non-small-cell lung cancer	2C25.Y	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	[19]
SKI-758	DMQ8E9R	Ischemia	8B10-8B11	Approved	[20]
Epidermal growth factor	DMVONE6	Vulnerary	ND56.Z	Approved	[18]
Merimepodib	DM0HS92	Breast cancer	2C60-2C65	Approved	[21]

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	Inhibitor	[2]
Insulin-like growth factor I receptor (IGF1R)	TTHRID2	IGF1R_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 800021633)
• [2] BiPar Sciences Co-founder Reunites Management Team At TriAct Therapeutics to Advance Clinical Stage Cancer Programs. TriAct Therapeutics. Sept. 10, 2009.
• [3] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [4] IGF-1R, IGF-1 and IGF-2 expression as potential prognostic and predictive markers in colorectal-cancer. Virchows Arch. 2003 Aug;443(2):139-45.
• [5] 2005 approvals: Safety first. Nature Reviews Drug Discovery 5, 92-93 (February 2006).
• [6] Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family... Bioorg Med Chem Lett. 2010 Apr 15;20(8):2452-5.
• [7] Mecasermin rinfabate: insulin-like growth factor-I/insulin-like growth factor binding protein-3, mecaserimin rinfibate, rhIGF-I/rhIGFBP-3. Drugs R D. 2005;6(2):120-7.
• [8] 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.
• [9] Clinical pipeline report, company report or official report of Amgen (2009).
• [10] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [11] Clinical Phase I study with an Insulin-like Growth Factor-1 receptor inhibitor: experiences in patients with squamous non-small cell lung carcinoma. Acta Oncol. 2011 Apr;50(3):441-7.
• [12] Clinical pipeline report, company report or official report of Roche (2009).
• [13] Nasopharyngeal carcinoma: Current treatment options and future directions. J Nasopharyng Carcinoma, 2014, 1(16): e16.
• [14] 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.
• [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] Boehringer Ingelheim. Product Development Pipeline. June 2 2009.
• [20] 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.
• [21] Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).