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

General Information of DTT (ID: TTFZYTO)

• DTT Name: C-C chemokine receptor type 2 (CCR2) DTT Info
• UniProt ID: CCR2_HUMAN
• Gene Name: CCR2

Molecule-Related Drug & Molecule List

11 Clinical Trial Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
AZD-2423	DMF34UY	Chronic obstructive pulmonary disease	CA22	Phase 2	[1]
BMS-813160	DMKY638	Diabetic nephropathy	GB61.Z	Phase 2	[2], [3]
CCX-140	DMJ9XCO	Diabetic nephropathy	GB61.Z	Phase 2	[4]
CCX872	DMPVAUT	Pancreatic tumour	2C10	Phase 2	[5]
Cenicriviroc	DM4V8WF	Human immunodeficiency virus infection	1C62	Phase 2	[6]
MK-0812	DMRT8K4	Multiple sclerosis	8A40	Phase 2	[7]
MLN1202	DM24SOL	Metastatic cancer	2D50-2E2Z	Phase 2	[8]
Aminoguanidine	DMJQDUC	Diabetic retinopathy	9B71.0	Phase 1	[9]
CNTX-6970	DMCOJM7	Inflammatory pain	MG30.42	Phase 1	[10]
OPL-CCL2-LPM	DM3HOUX	Arthritis	FA20	Phase 1	[11]
TAK-202	DMVYEFZ	Melanoma	2C30	Phase 1	[12], [13]

5 Discontinued Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
CCX915	DMHMST3	Multiple sclerosis	8A40	Discontinued in Phase 1	[14]
INCB8696	DM8PTUC	Multiple sclerosis	8A40	Discontinued in Phase 1	[15]
AZD-6942	DMZ90OV	Rheumatoid arthritis	FA20	Terminated	[17]
INCB3344	DMW39DV	Arteriosclerosis	BD40	Terminated	[18]
SB-282241	DMZLKCF	Inflammation	1A00-CA43.1	Terminated	[17]

2 Preclinical Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
MCP-1	DMYEFKH	Rheumatoid arthritis	FA20	Preclinical	[8]
RS-504393	DMB9IPR	Chronic obstructive pulmonary disease	CA22	Preclinical	[16], [8]

13 Investigative Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(R)-3-(1'-Adamantanecarbonyl)amino-caprolactam	DMRZDM0	Discovery agent	N.A.	Investigative	[19]
(S)-3-(1'-Adamantanecarbonyl)amino-caprolactam	DMS5IHX	Discovery agent	N.A.	Investigative	[19]
(S)-3-(2',2'-Dimethyl-propionyl)amino-caprolactam	DMANICH	Discovery agent	N.A.	Investigative	[19]
BMS-A	DMI796T	Inflammation	1A00-CA43.1	Investigative	[20]
GSK-1344386B	DMHBUG5	Arteriosclerosis	BD40	Investigative	[20]
INCB-10820	DMZCHSD	Inflammation	1A00-CA43.1	Investigative	[20]
NSC-651016	DMWY39L	Discovery agent	N.A.	Investigative	[21]
RAP-103	DM961JG	Neuropathic pain	8E43.0	Investigative	[20]
RAP-310	DMP2DMB	Alzheimer disease	8A20	Investigative	[20]
RS-102895	DMF71B3	Discovery agent	N.A.	Investigative	[22]
RS-136270	DMEHN2L	Discovery agent	N.A.	Investigative	[22]
Teijin-lead_cmp_5	DMSMLRB	Discovery agent	N.A.	Investigative	[23]
viral macrophage inflammatory protein-II	DMAXOPS	Discovery agent	N.A.	Investigative	[24]

References

• [1] CA patent application no. 841416, Method of selecting therapeutic indications.
• [2] A dual CCR2/CCR5 chemokine antagonist, BMS-813160. Expert Opin Ther Pat. 2011 Dec;21(12):1919-24.
• [3] Methods for improving thymic recovery and preventing and treating graft versus host disease using ccr2 and ccr5 antagonists
• [4] Present and future in the treatment of diabetic kidney disease. J Diabetes Res. 2015;2015:801348.
• [5] Therapeutic use of a clinical stage CCR2 inhibitor, CCX872, in obesity-associated steatohepatitis. The Lancet Volume 383, Supplement 1, 26 February 2014, Pages S78.
• [6] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [7] Assessment of chemokine receptor function on monocytes in whole blood: In vitro and ex vivo evaluations of a CCR2 antagonist. J Immunol Methods. 2010 Jan 31;352(1-2):101-10.
• [8] Emerging drugs for the treatment of chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2006 May;11(2):275-91.
• [9] Incyte Announces Second Quarter 2005 Financial Results; Reports Positive Phase IIb Results for Reverset in Treatment-Experienced HIV Patients. Incyte Corporation. 2005.
• [10] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [11] Selective CCR2-targeted macrophage depletion ameliorates experimental mesangioproliferative glomerulonephritis. Clin Exp Immunol. 2009 February; 155(2): 295-303.
• [12] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [13] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [14] Marketed and experimental medicines for the treatment of multiple sclerosis. The Association of the British Pharmaceutical Industry. 2009.
• [15] Incyte. Product Development Pipeline.
• [16] Beneficial or detrimental effects of carotenoids contained in food: cell culture models. Mini Rev Med Chem. 2007 Nov;7(11):1120-8.
• [17] Patent EP2727944 A1.
• [18] Discovery of ((1S,3R)-1-isopropyl-3-((3S,4S)-3-methoxy-tetrahydro-2H-pyran-4-ylamino)cyclopentyl)(4-(5-(trifluoromethyl)pyridazin-3-yl)piperazin-1-yl)methanone, PF-4254196, a CCR2 antagonist with an improved cardiovascular profile. Bioorg Med Chem Lett. 2011 May 1;21(9):2626-30.
• [19] Highly potent, orally available anti-inflammatory broad-spectrum chemokine inhibitors. J Med Chem. 2009 Jun 11;52(11):3591-5.
• [20] 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: 59).
• [21] Inhibition of in vitro and in vivo HIV replication by a distamycin analogue that interferes with chemokine receptor function: a candidate for chemo... J Med Chem. 1998 Jun 18;41(13):2184-93.
• [22] Identification of the binding site for a novel class of CCR2b chemokine receptor antagonists: binding to a common chemokine receptor motif within t... J Biol Chem. 2000 Aug 18;275(33):25562-71.
• [23] CCR2: characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach. J Med Chem. 2003 Sep 11;46(19):4070-86.
• [24] A broad-spectrum chemokine antagonist encoded by Kaposi's sarcoma-associated herpesvirus. Science. 1997 Sep 12;277(5332):1656-9.