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

General Information of Drug (ID: DMKY638)

• Drug Name: BMS-813160 Drug Info
• Synonyms: BMS-585059; CCR2/CCR5 chemokine antagonist (immune disorders, cardiovascular disorders), BMS; CCR2/CCR5 dual antagonist (cardiovascular disease), Bristol-Myers Squibb; CCR2/CCR5 dual antagonist (immunology), Bristol-Myers Squibb

Indication

Disease Entry	ICD 11	Status	REF
Diabetic nephropathy	GB61.Z	Phase 2	[1]
Solid tumour/cancer	2A00-2F9Z	Phase 1	[2]

• Cross-matching ID:
  PubChem CID: 51039119
  CAS Number: CAS 1286279-29-5
  TTD Drug ID: DMKY638

Molecule-Related Drug Atlas

Drug(s) Targeting C-C chemokine receptor type 5 (CCR5)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Maraviroc	DMTL94F	Human immunodeficiency virus infection	1C62	Approved	[4]
Vicriviroc	DMMTW9K	Human immunodeficiency virus infection	1C62	Phase 3	[5]
PRO-140	DMD1FTP	Human immunodeficiency virus infection	1C62	Phase 3	[6]
E-913	DMUHS5Q	Human immunodeficiency virus infection	1C62	Phase 3	[7]
PRO 140	DMCGK6X	Human immunodeficiency virus-1 infection	1C62	Phase 2/3	[8]
INCB9471	DMMWC6F	Infectious disease	1A00-CA43.1	Phase 2a	[7]
Cenicriviroc	DM4V8WF	Human immunodeficiency virus infection	1C62	Phase 2	[9]
SB-728-T	DMRWE5D	Human immunodeficiency virus infection	1C62	Phase 2	[10]
PF-232798	DM8T6KQ	Human immunodeficiency virus infection	1C62	Phase 2	[11]
GSK-706769	DMPLKAH	Human immunodeficiency virus infection	1C62	Phase 2	[12]

Drug(s) Targeting C-C chemokine receptor type 2 (CCR2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Cenicriviroc	DM4V8WF	Human immunodeficiency virus infection	1C62	Phase 2	[13]
MLN1202	DM24SOL	Metastatic cancer	2D50-2E2Z	Phase 2	[14]
CCX-140	DMJ9XCO	Diabetic nephropathy	GB61.Z	Phase 2	[15]
AZD-2423	DMF34UY	Chronic obstructive pulmonary disease	CA22	Phase 2	[16]
CCX872	DMPVAUT	Pancreatic tumour	2C10	Phase 2	[17]
MK-0812	DMRT8K4	Multiple sclerosis	8A40	Phase 2	[18]
Aminoguanidine	DMJQDUC	Diabetic retinopathy	9B71.0	Phase 1	[19]
TAK-202	DMVYEFZ	Melanoma	2C30	Phase 1	[2]
OPL-CCL2-LPM	DM3HOUX	Arthritis	FA20	Phase 1	[20]
CNTX-6970	DMCOJM7	Inflammatory pain	MG30.42	Phase 1	[21]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
C-C chemokine receptor type 2 (CCR2)	TTFZYTO	CCR2_HUMAN	Modulator	[3]
C-C chemokine receptor type 5 (CCR5)	TT2CEJG	CCR5_HUMAN	Modulator	[3]

References

• [1] ClinicalTrials.gov (NCT01752985) Study to Evaluate the Effects of BMS-813160 on Protein Loss in the Urine of Subjects With Type 2 Diabetes and Diabetic Kidney Disease. U.S. National Institutes of Health.
• [2] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [3] A dual CCR2/CCR5 chemokine antagonist, BMS-813160. Expert Opin Ther Pat. 2011 Dec;21(12):1919-24.
• [4] Rapamycin enhances aplaviroc anti-HIV activity: implications for the clinical development of novel CCR5 antagonists. Antiviral Res. 2009 Jul;83(1):86-9.
• [5] HIV entry: new insights and implications for patient management. Curr Opin Infect Dis. 2009 Feb;22(1):35-42.
• [6] Agonist-induced internalization of CC chemokine receptor 5 as a mechanism to inhibit HIV replication. J Pharmacol Exp Ther. 2011 Jun;337(3):655-62.
• [7] Species selectivity of small-molecular antagonists for the CCR5 chemokine receptor. Int Immunopharmacol. 2007 Dec 5;7(12):1528-34.
• [8] The return of PRO 140, a CCR5-directed mAb. Curr Opin HIV AIDS. 2018 Jul;13(4):346-353.
• [9] The dual CCR5 and CCR2 inhibitor cenicriviroc does not redistribute HIV into extracellular space: implications for plasma viral load and intracellular DNA decline. J Antimicrob Chemother. 2015 Mar;70(3):750-6.
• [10] Gene Editing of CCR5 in Autologous CD4 T Cells of Persons Infected with HIV. N Engl J Med. 2014 March 6; 370(10): 901-910.
• [11] An imidazopiperidine series of CCR5 antagonists for the treatment of HIV: the discovery of N-{(1S)-1-(3-fluorophenyl)-3-[(3-endo)-3-(5-isobutyryl-2-methyl-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridin-1-yl)-8-azabicyclo[3.2.1]oct-8-yl]propyl}acetamide (PF-232798). J Med Chem. 2011 Jan 13;54(1):67-77.
• [12] Tapping into combination pills for HIV. Nat Rev Drug Discov. 2009 Jun;8(6):439-40.
• [13] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [14] Emerging drugs for the treatment of chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2006 May;11(2):275-91.
• [15] Present and future in the treatment of diabetic kidney disease. J Diabetes Res. 2015;2015:801348.
• [16] CA patent application no. 841416, Method of selecting therapeutic indications.
• [17] Therapeutic use of a clinical stage CCR2 inhibitor, CCX872, in obesity-associated steatohepatitis. The Lancet Volume 383, Supplement 1, 26 February 2014, Pages S78.
• [18] 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.
• [19] Incyte Announces Second Quarter 2005 Financial Results; Reports Positive Phase IIb Results for Reverset in Treatment-Experienced HIV Patients. Incyte Corporation. 2005.
• [20] Selective CCR2-targeted macrophage depletion ameliorates experimental mesangioproliferative glomerulonephritis. Clin Exp Immunol. 2009 February; 155(2): 295-303.
• [21] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)