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

General Information of DTT (ID: TTCBFJO)

• DTT Name: Insulin receptor (INSR) DTT Info
• UniProt ID: INSR_HUMAN
• Gene Name: INSR

Molecule-Related Drug & Molecule List

9 Approved Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Human neutral insulin	DMA5OBU	Diabetic complication	5A2Y	Approved	[1]
Insulin Lyspro recombinant	DM5XHVR	Diabetic complication	5A2Y	Approved	[1]
Insulin recombinant	DMYVP5G	Diabetic complication	5A2Y	Approved	[1]
Insulin, porcine	DMO95XI	Diabetic complication	5A2Y	Approved	[2]
Insulin-glulisine	DMQI0FU	Diabetic complication	5A2Y	Approved	[3]
Insulin-lispro	DM4O90W	Diabetic complication	5A2Y	Approved	[4]
Meglitinides	DM1OFHN	Type-2 diabetes	5A11	Approved	[5]
Metformin arginine-hemisuccinimide	DMTPAM3	Type-2 diabetes	5A11	Approved	[6]
Ryzodeq	DMOFP18	Type-2 diabetes	5A11	Approved	[7]

18 Clinical Trial Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
NN5401	DM0QV27	Diabetic complication	5A2Y	Phase 3	[7]
Metformin glycinate	DMFE0P1	Type-2 diabetes	5A11	Phase 2/3	[8]
DM-71	DMMSIG7	Type-2 diabetes	5A11	Phase 2	[7]
DM-99	DM1HG3U	Alzheimer disease	8A20	Phase 2	[7]
EGS-21	DMN1SWB	Crohn disease	DD70	Phase 2	[9]
Mitoglitazone	DMIRPSA	Alzheimer disease	8A20	Phase 2	[10]
MSDC-0602	DMGUI51	Type-2 diabetes	5A11	Phase 2	[11]
NP-01	DMP1W9Z	Type-2 diabetes	5A11	Phase 2	[7]
S-707106	DM3GRKY	Type-2 diabetes	5A11	Phase 2	[7]
TAK-379	DMEYKRN	Type-2 diabetes	5A11	Phase 2	[7]
Tesofensine	DM1KGS7	Pain	MG30-MG3Z	Phase 2	[12]
VVP-808	DM6BKG2	Type-2 diabetes	5A11	Phase 2	[7]
AEW-541	DMQF982	Multiple myeloma	2A83	Phase 1	[13]
AGT-182	DML79KE	Hunter syndrome	5C56.31	Phase 1	[7]
Insulin oral sublingual	DMMR7CH	Type-1 diabetes	5A10	Phase 1	[7]
Insulin transdermal	DM93QP2	Type-1/2 diabetes	5A10-5A11	Phase 1	[14]
ISF-402	DMKO7EA	Type-2 diabetes	5A11	Phase 1	[15]
NN-1218	DMDGCHR	Diabetic complication	5A2Y	Phase 1	[16]

6 Discontinued Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
AKP-020	DM6IPWN	Type-2 diabetes	5A11	Discontinued in Phase 2	[17]
DM-83	DMIP3EC	Type-2 diabetes	5A11	Discontinued in Phase 2	[7]
EML-336	DMML2PX	Type-2 diabetes	5A11	Discontinued in Phase 2	[7]
KW-2450	DM7QGSX	Breast cancer	2C60-2C65	Discontinued in Phase 1/2	[18]
CLX-0900	DMYPRS9	Hyperlipidaemia	5C80	Terminated	[19]
TER-16998	DMQIYZR	Diabetic complication	5A2Y	Terminated	[7]

14 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	[20]
4-((naphthalen-2-ylamino)methyl)benzene-1,2-diol	DM52Y3Q	Discovery agent	N.A.	Investigative	[20]
AD10-1025	DMYLA29	Hypercholesterolaemia	5C80.0	Investigative	[7]
DC-9703	DM62IBX	Non-insulin dependent diabetes	5A11	Investigative	[7]
FPT-038	DM0T2LQ	Non-insulin dependent diabetes	5A11	Investigative	[7]
GSK-1838705A	DM4HLK3	Discovery agent	N.A.	Investigative	[21]
L-betagamma-meATP	DMTNQCE	Discovery agent	N.A.	Investigative	[22]
NVP-TAE684	DMFZXI2	Lymphoma	2A80-2A86	Investigative	[23]
PMID24900237C15	DM6TFPY	Discovery agent	N.A.	Investigative	[24]
Quick-acting insulin	DM9YWG8	Diabetic complication	5A2Y	Investigative	[7]
RHIIP	DMWP09B	Diabetic complication	5A2Y	Investigative	[25]
VVP-100X	DMEZAND	Non-insulin dependent diabetes	5A11	Investigative	[7]
XMetD	DMHWTCY	Hypoglycemia	5A41	Investigative	[7]
XMetS	DM6JKL7	Non-insulin dependent diabetes	5A11	Investigative	[7]

References

• [1] Knockouts model the 100 best-selling drugs--will they model the next 100 Nat Rev Drug Discov. 2003 Jan;2(1):38-51.
• [2] Acidic residues on the N-terminus of proinsulin C-Peptide are important for the folding of insulin precursor. J Biochem. 2002 Jun;131(6):855-9.
• [3] Insulin glulisine: a review of its use in the management of diabetes mellitus. Drugs. 2009;69(8):1035-57.
• [4] Hope for insulin mimetic oral antidiabetic drugs. Eur J Endocrinol. 1999 Dec;141(6):561-2.
• [5] New drugs for type 2 diabetes mellitus: what is their place in therapy Drugs. 2008;68(15):2131-62.
• [6] Metformin (Glucophage) inhibits tyrosine phosphatase activity to stimulate the insulin receptor tyrosine kinase. Biochem Pharmacol. 2004 Jun 1;67(11):2081-91.
• [7] 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: 1800).
• [8] Effect of Metformin Glycinate on Glycated Hemoglobin A1c Concentration and Insulin Sensitivity in Drug-Naive Adult Patients with Type 2 Diabetes Mellitus. Diabetes Technol Ther. 2012 December; 14(12): 1140-1144.
• [9] Ceramides and glucosylceramides are independent antagonists of insulin signaling. J Biol Chem. 2014 Jan 10;289(2):723-34.
• [10] An evaluation of MSDC-0160, a prototype mTOT modulating insulin sensitizer, in patients with mild Alzheimer's disease. Curr Alzheimer Res. 2014;11(6):564-73.
• [11] Insulin resistance and metabolic derangements in obese mice are ameliorated by a novel peroxisome proliferator-activated receptor gamma-sparing thiazolidinedione. J Biol Chem. 2012 Jul 6;287(28):23537-48.
• [12] The novel triple monoamine reuptake inhibitor tesofensine induces sustained weight loss and improves glycemic control in the diet-induced obese rat: comparison to sibutramine and rimonabant. Eur J Pharmacol. 2010 Jun 25;636(1-3):88-95.
• [13] Inhibition of the insulin-like growth factor-1 receptor (IGF1R) tyrosine kinase as a novel cancer therapy approach. J Med Chem. 2009 Aug 27;52(16):4981-5004.
• [14] Transdermal drug delivery of insulin with ultradeformable carriers. Clin Pharmacokinet. 2003;42(5):461-74.
• [15] Ability of GHTD-amide and analogs to enhance insulin activity through zinc chelation and dispersal of insulin oligomers. Peptides. 2009 Jun;30(6):1088-97.
• [16] Ultrafast-Acting Insulins: State of the Art. J Diabetes Sci Technol. 2012 July; 6(4): 728-742.
• [17] Effect of vanadium on insulin and leptin in Zucker diabetic fatty rats. Mol Cell Biochem. 2001 Feb;218(1-2):93-6.
• [18] Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
• [19] CLX-0901 (Calyx Therapeutics). Curr Opin Investig Drugs. 2001 May;2(5):650-3.
• [20] 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.
• [21] GSK1838705A inhibits the insulin-like growth factor-1 receptor and anaplastic lymphoma kinase and shows antitumor activity in experimental models of human cancers. Mol Cancer Ther. 2009 Oct;8(10):2811-20.
• [22] How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
• [23] Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. Proc Natl Acad Sci U S A. 2007 Jan 2;104(1):270-5.
• [24] Discovery of a potent inhibitor of anaplastic lymphoma kinase with in vivo antitumor activity. ACS Med Chem Lett. 2010 Sep 1;1(9):493-8.
• [25] PROMAXX inhaled insulin: safe and efficacious administration with a commercially available dry powder inhaler. Diabetes Obes Metab. 2009 May;11(5):455-9.