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

General Information of DTT (ID: TTHRID2)

• DTT Name: Insulin-like growth factor I receptor (IGF1R) DTT Info
• Gene Name: IGF1R

Molecule-Related Drug & Molecule List

3 Approved Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Mecasermin	DM1O3BY	Growth failure	LD2F.1Y	Approved	[1]
Somatomedin-1	DMZ9FAO	Hormone deficiency	5A61.1	Approved	[2]
Teprotumumab	DM4L59B	Graves disease	5A02.0	Approved	[3]

16 Clinical Trial Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
OSI-906	DMHKZLF	Solid tumour/cancer	2A00-2F9Z	Phase 3	[4]
Rinfabate	DML9FD4	Solid tumour/cancer	2A00-2F9Z	Phase 2/3	[5]
AMG 479	DM0DRAZ	Breast cancer	2C60-2C65	Phase 2	[6]
AXL-1717	DMTQ1Y3	Solid tumour/cancer	2A00-2F9Z	Phase 2	[7]
Cixutumumab	DMNRYPF	Liver cancer	2C12	Phase 2	[8]
MM-141	DM2RJ4D	Pancreatic cancer	2C10	Phase 2	[9]
R1507	DMIUS5X	Graves ophthalmopathy	9C82.3	Phase 2	[10]
TT-100	DMZE6Y9	Non-small-cell lung cancer	2C25.Y	Phase 2	[11]
VPI-2690B	DMUQZT4	Diabetic nephropathy	GB61.Z	Phase 2	[12]
AEW-541	DMQF982	Multiple myeloma	2A83	Phase 1	[13]
BIIB 022	DMZ1V0E	Hepatocellular carcinoma	2C12.02	Phase 1	[14]
Cyclolignan picropodophyllin	DMI6EUB	Colorectal cancer	2B91.Z	Phase 1	[15]
FPI-1434	DMI9A1Z	Solid tumour/cancer	2A00-2F9Z	Phase 1	[16]
HF-0299	DMDZQ23	Pain	MG30-MG3Z	Phase 1	[17]
RG-7010	DMMWS3O	Motor neurone disease	8B60	Phase 1	[18]
SAR446159	DMWAO33	Parkinson disease	8A00.0	Phase 1	[19]

3 Discontinued Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
AVE-1642	DMUQ6IL	Breast cancer	2C60-2C65	Discontinued in Phase 2	[20]
KW-2450	DM7QGSX	Breast cancer	2C60-2C65	Discontinued in Phase 1/2	[21]
Figitumumab	DMC3DVB	Malignant adrenal gland cancer	2D11	Discontinued in Phase 1	[22]

2 Preclinical Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BMS-695735	DMQG39T	Solid tumour/cancer	2A00-2F9Z	Preclinical	[23]
EGFR/IGFR tandem adnectin	DMZ3YP6	Solid tumour/cancer	2A00-2F9Z	Preclinical	[24]

8 Investigative Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
4-((1H-indazol-6-ylamino)methyl)benzene-1,2-diol	DMLV59R	Discovery agent	N.A.	Investigative	[25]
4-((naphthalen-2-ylamino)methyl)benzene-1,2-diol	DM52Y3Q	Discovery agent	N.A.	Investigative	[25]
Alpha-D-Mannose	DMF5DLW	Discovery agent	N.A.	Investigative	[26]
AMP-PNP	DMTOK1D	Discovery agent	N.A.	Investigative	[27]
BMS-536924	DMXJB4N	Discovery agent	N.A.	Investigative	[28]
Fucose	DMAHMSV	N. A.	N. A.	Investigative	[26]
JB-1	DM38L1B	Multiple myeloma	2A83	Investigative	[29]
NVP-ADW742	DMXL3CD	Multiple myeloma	2A83	Investigative	[29]

References

• [1] 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.
• [2] 2005 approvals: Safety first. Nature Reviews Drug Discovery 5, 92-93 (February 2006).
• [3] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [4] 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.
• [5] 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.
• [6] Clinical pipeline report, company report or official report of Amgen (2009).
• [7] 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.
• [8] Doxorubicin plus the IGF-1R antibody cixutumumab in soft tissue sarcoma: a phase I study using the TITE-CRM model. Ann Oncol. 2015 Jul;26(7):1459-64.
• [9] 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.
• [10] Clinical pipeline report, company report or official report of Roche (2009).
• [11] BiPar Sciences Co-founder Reunites Management Team At TriAct Therapeutics to Advance Clinical Stage Cancer Programs. TriAct Therapeutics. Sept. 10, 2009.
• [12] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [13] 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.
• [14] A phase 1, open-label, dose-escalation study of BIIB022 (anti-IGF-1R monoclonal antibody) in subjects with relapsed or refractory solid tumors. Invest New Drugs. 2014 Jun;32(3):518-25.
• [15] The cyclolignan picropodophyllin attenuates intimal hyperplasia after rat carotid balloon injury by blocking insulin-like growth factor-1 receptor signaling. J Vasc Surg. 2007 Jul;46(1):108-15.
• [16] Clinical pipeline report, company report or official report of Fusion Pharmaceuticals.
• [17] A primary adrenal steroid, 11beta-hydroxyandrostenedione, has an osteotropic effect and little androgenic activity. J Steroid Biochem Mol Biol. 2000 Nov 15;74(4):203-11.
• [18] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031207)
• [19] Clinical pipeline report, company report or official report of Sanofi
• [20] Insulin-like growth factor-1 receptor inhibition induces a resistance mechanism via the epidermal growth factor receptor/HER3/AKT signaling pathway: rational basis for cotargeting insulin-like growthfactor-1 receptor and epidermal growth factor receptor in hepatocellular carcinoma. Clin Cancer Res. 2009 Sep 1;15(17):5445-56.
• [21] Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
• [22] Pfizer. Product Development Pipeline. March 31 2009.
• [23] Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)py... J Med Chem. 2008 Oct 9;51(19):5897-900.
• [24] Clinical pipeline report, company report or official report of Bristol-Myers Squibb.
• [25] ATP non-competitive IGF-1 receptor kinase inhibitors as lead anti-neoplastic and anti-papilloma agents. Eur J Pharmacol. 2007 May 7;562(1-2):1-11.
• [26] How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
• [27] The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
• [28] SAR of PXR transactivation in benzimidazole-based IGF-1R kinase inhibitors. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1744-8.
• [29] Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127.