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

General Information of Drug (ID: DMPC4EK)

• Drug Name: EP-217609 Drug Info
• Synonyms: Neutralizable NAPAP analog (thrombosis), Endotis; Neutralizable NAPAP analog (thrombosis), Organon; Fondaparinux analog + thrombin inhibitor (thrombosis), Endotis; Neutralizable Factor IIa/Factor X dual inhibitor (thrombosis), Endotis; Neutralizable Factor IIa/Factor X dual inhibitor (thrombosis), Organon

Indication

Disease Entry	ICD 11	Status	REF
Thrombosis	DB61-GB90	Phase 2	[1]

• Cross-matching ID:
  PubChem CID: 11686894
  CAS Number: CAS 894494-99-6
  TTD Drug ID: DMPC4EK

Molecule-Related Drug Atlas

Drug(s) Targeting Coagulation factor Xa (F10)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Apixaban	DM89JLN	Thrombosis	DB61-GB90	Approved	[3]
Rivaroxaban	DMQMBZ1	Deep vein thrombosis	BD71	Approved	[4]
DU-176b	DMCIJBH	Atrial fibrillation	BC81.3	Approved	[5]
Emicizumab	DM0AQ83	Factor VIII deficiency	3B10	Approved	[6]
BETRIXABAN	DM2C4RF	Venous thromboembolism	BD72	Approved	[7]
Lmw heparin	DMJPD06	Coagulation defect	3B10.0	Approved	[8]
Nadroparin calcium	DMBNKST	Coagulation defect	3B10.0	Approved	[9]
Fondaparinux sodium	DMWS3FH	Deep vein thrombosis	BD71	Approved	[10]
Danaparoid	DM6CLBN	Deep venous clot	BD71	Approved	[11]
Coagulation Factor IX	DM8HBJI	Haemophilia B	3B11.0	Approved	[12]

Drug(s) Targeting Coagulation factor IIa (F2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Argatroban	DMFI46A	Thrombosis	DB61-GB90	Approved	[13]
Pyridoxal Phosphate	DMO2K0J	Malnutrition	5B50-5B71	Approved	[14]
Bivalirudin	DMECRX1	Thrombocytopenia	3B64	Approved	[15]
Ximelegatran	DMU8ANS	Myocardial infarction	BA41-BA43	Approved	[16]
Dabigatran	DMDI6R4	Stroke	8B20	Approved	[17]
Desirudin Recombinant	DM2BTFN	Coagulation defect	3B10.0	Approved	[18]
Human prothrombin complex concentrate	DMPHVQ1	Bleeding disorder	GA20-GA21	Approved	[19]
Lepirudin	DM1I3D5	Thrombocytopenia	3B64	Approved	[20]
Anisindione	DM2C48U	Coagulation defect	3B10.0	Approved	[21]
ATryn antithrombin	DM79Y2T	Multiple sclerosis	8A40	Approved	[22]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Coagulation factor IIa (F2)	TT6L509	THRB_HUMAN	Modulator	[2]
Coagulation factor Xa (F10)	TTCIHJA	FA10_HUMAN	Modulator	[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 800033781)
• [2] Specificity and selectivity profile of EP217609: a new neutralizable dual-action anticoagulant that targets thrombin and factor Xa.Blood.2012 Mar 8;119(10):2187-95.
• [3] Pfizer. Product Development Pipeline. March 31 2009.
• [4] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [5] 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: 2359).
• [6] 2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85.
• [7] Company report (Portola)
• [8] Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77.
• [9] Serum zinc concentrations: contamination from laboratory equipment. JPEN J Parenter Enteral Nutr. 1979 May-Jun;3(3):179-81.
• [10] Biochemistry and clinical pharmacology of new anticoagulant agents. Pathophysiol Haemost Thromb. 2002 Sep-Dec;32(5-6):218-24.
• [11] Effect of factor X inhibition on coagulation activation and cytokine induction in human systemic inflammation. J Infect Dis. 2002 Nov 1;186(9):1270-6.
• [12] Haemophilia B: Christmas disease. Expert Opin Pharmacother. 2005 Aug;6(9):1517-24.
• [13] Studies on the different modes of action of the anticoagulant protease inhibitors DX-9065a and Argatroban. I. Effects on thrombin generation. J Biol Chem. 2002 Dec 27;277(52):50439-44.
• [14] New antithrombotic drugs (excluding plasminogen activators. Arch Mal Coeur Vaiss. 2001 Nov;94(11 Suppl):1225-32.
• [15] New anticoagulants. Am Heart J. 2001 Aug;142(2 Suppl):S3-8.
• [16] Emerging drugs in peripheral arterial disease. Expert Opin Emerg Drugs. 2006 Mar;11(1):75-90.
• [17] Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.
• [18] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [19] 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: 2362).
• [20] Recombinant hirudin (lepirudin) as anticoagulant in intensive care patients treated with continuous hemodialysis. Kidney Int Suppl. 1999 Nov;(72):S46-50.
• [21] Anticoagulation with anisindione in a patient with a warfarin-induced skin eruption. Pharmacotherapy. 2003 Apr;23(4):533-6.
• [22] Antithrombin III Utilization in a Large Teaching Hospital. P T. 2013 December; 38(12): 764-767, 779.