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

General Information of Drug (ID: DMPML15)

• Drug Name: RAZAXABAN Drug Info
• Synonyms: Razaxaban Hydrochloride; UNII-7CLJ1MEZ8V; BMS-561389; 7CLJ1MEZ8V; 405940-76-3; DPC 906; Razaxaban Hydrochloride [USAN]; Razaxaban hydrochloride (USAN); CHEMBL558198; DPC-906; BMS 561389; Razaxaban HCl; AC1L4BWY; SCHEMBL6885838; DTXSID10193598; Razaxaban hydrochloride, > D04029; 1H-Pyrazole-5-carboxamide, 1-(3-amino-1,2-benzisoxazol-5-yl)-N-(4-(2-((dimethylamino)methyl)-1H-imidazol-1-yl)-2-fluorophenyl)-3-(trifluoromethyl)-, monohydrochloride

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

• Cross-matching ID:
  PubChem CID: 204102
  CAS Number: CAS 218298-21-6
  TTD Drug ID: DMPML15

Molecule-Related Drug Atlas

Drug(s) Targeting Coagulation factor Va (F5)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Drotrecogin alfa	DM59JCN	Cerebrovascular ischaemia	8B1Z	Approved	[4]
Phenylmercury	DMJTC2B	Discovery agent	N.A.	Investigative	[5]

Drug(s) Targeting Coagulation factor IX (F9)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Emicizumab	DM0AQ83	Factor VIII deficiency	3B10	Approved	[6]
Recombinant Factor IX	DMY7ESM	Bleeding disorder	GA20-GA21	Approved	[7]
CSL-654	DMZJGVL	Factor IX deficiency	3B11	Phase 3	[8]
RG6013	DMER75Y	Haemophilia A	3B10.0	Phase 3	[9]
AMT-061	DMSO02K	Haemophilia B	3B11.0	Phase 3	[10]
Fidanacogene elaparvovec	DMFZ81T	Haemophilia B	3B11.0	Phase 3	[11]
Mim8	DMX33ZR	Haemophilia A	3B10.0	Phase 3	[12]
TTP889	DMCQARM	Blood forming organ disorder	JB64.1	Phase 2	[13]
AMT-060	DM7RNKM	Factor IX deficiency	3B11	Phase 1/2	[14]
SB-FIX	DMUP52Y	Haemophilia B	3B11.0	Phase 1/2	[15]

Drug(s) Targeting Coagulation factor Xa (F10)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Apixaban	DM89JLN	Thrombosis	DB61-GB90	Approved	[16]
Rivaroxaban	DMQMBZ1	Deep vein thrombosis	BD71	Approved	[17]
DU-176b	DMCIJBH	Atrial fibrillation	BC81.3	Approved	[18]
Emicizumab	DM0AQ83	Factor VIII deficiency	3B10	Approved	[6]
BETRIXABAN	DM2C4RF	Venous thromboembolism	BD72	Approved	[19]
Lmw heparin	DMJPD06	Coagulation defect	3B10.0	Approved	[20]
Nadroparin calcium	DMBNKST	Coagulation defect	3B10.0	Approved	[21]
Fondaparinux sodium	DMWS3FH	Deep vein thrombosis	BD71	Approved	[22]
Danaparoid	DM6CLBN	Deep venous clot	BD71	Approved	[23]
Coagulation Factor IX	DM8HBJI	Haemophilia B	3B11.0	Approved	[24]

Drug(s) Targeting Coagulation factor IIa (F2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Argatroban	DMFI46A	Thrombosis	DB61-GB90	Approved	[25]
Pyridoxal Phosphate	DMO2K0J	Malnutrition	5B50-5B71	Approved	[26]
Bivalirudin	DMECRX1	Thrombocytopenia	3B64	Approved	[27]
Ximelegatran	DMU8ANS	Myocardial infarction	BA41-BA43	Approved	[28]
Dabigatran	DMDI6R4	Stroke	8B20	Approved	[29]
Desirudin Recombinant	DM2BTFN	Coagulation defect	3B10.0	Approved	[30]
Human prothrombin complex concentrate	DMPHVQ1	Bleeding disorder	GA20-GA21	Approved	[31]
Lepirudin	DM1I3D5	Thrombocytopenia	3B64	Approved	[32]
Anisindione	DM2C48U	Coagulation defect	3B10.0	Approved	[33]
ATryn antithrombin	DM79Y2T	Multiple sclerosis	8A40	Approved	[34]

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	Inhibitor	[1]
Coagulation factor IX (F9)	TTFEZ5Q	FA9_HUMAN	Inhibitor	[2]
Coagulation factor Va (F5)	TT1O264	FA5_HUMAN	Inhibitor	[2]
Coagulation factor Xa (F10)	TTCIHJA	FA10_HUMAN	Inhibitor	[3]

References

• [1] Phenyltriazolinones as potent factor Xa inhibitors. Bioorg Med Chem Lett. 2010 Feb 15;20(4):1373-7.
• [2] Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1795-8.
• [3] Discovery of 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide (apixaban, BMS... J Med Chem. 2007 Nov 1;50(22):5339-56.
• [4] Protein C in critical illness. Am J Health Syst Pharm. 2009 Jun 15;66(12):1089-96.
• [5] How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
• [6] 2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85.
• [7] BAX326 (RIXUBIS): a novel recombinant factor IX for the control and prevention of bleeding episodes in adults and children with hemophilia B. Ther Adv Hematol. 2014 Oct;5(5):168-80.
• [8] Safety and pharmacokinetics of a novel recombinant fusion protein linking coagulation factor IX with albumin (rIX-FP) in hemophilia B patients. Blood. 2012 September 20; 120(12): 2405-2411.
• [9] Anti-factor IXa/X bispecific antibody (ACE910): hemostatic potency against ongoing bleeds in a hemophilia A model and the possibility of routine supplementation. J Thromb Haemost. 2014 Feb;12(2):206-13.
• [10] Clinical pipeline report, company report or official report of uniQure.
• [11] Factor IX assay discrepancies in the setting of liver gene therapy using a hyperfunctional variant factor IX-Padua. J Thromb Haemost. 2021 May;19(5):1212-1218.
• [12] ClinicalTrials.gov (NCT05878938) Open-label Safety Study in Adults and Adolescents With Haemophilia A With and Without FVIII Inhibitors Switching Directly From Emicizumab Prophylaxis to NNC0365-3769 (Mim8) Prophylaxis. U.S.National Institutes of Health.
• [13] Partial factor IXa inhibition with TTP889 for prevention of venous thromboembolism: an exploratory study. J Thromb Haemost. 2008 Mar;6(3):457-63.
• [14] Phase I/II clinical trial of AMT-060 for treating hemophilia B. uniQure N.V.
• [15] ClinicalTrials.gov (NCT02695160) Ascending Dose Study of Genome Editing by Zinc Finger Nuclease Therapeutic SB-FIX in Subjects With Severe Hemophilia B. U.S. National Institutes of Health.
• [16] Pfizer. Product Development Pipeline. March 31 2009.
• [17] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [18] 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).
• [19] Company report (Portola)
• [20] Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77.
• [21] Serum zinc concentrations: contamination from laboratory equipment. JPEN J Parenter Enteral Nutr. 1979 May-Jun;3(3):179-81.
• [22] Biochemistry and clinical pharmacology of new anticoagulant agents. Pathophysiol Haemost Thromb. 2002 Sep-Dec;32(5-6):218-24.
• [23] 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.
• [24] Haemophilia B: Christmas disease. Expert Opin Pharmacother. 2005 Aug;6(9):1517-24.
• [25] 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.
• [26] New antithrombotic drugs (excluding plasminogen activators. Arch Mal Coeur Vaiss. 2001 Nov;94(11 Suppl):1225-32.
• [27] New anticoagulants. Am Heart J. 2001 Aug;142(2 Suppl):S3-8.
• [28] Emerging drugs in peripheral arterial disease. Expert Opin Emerg Drugs. 2006 Mar;11(1):75-90.
• [29] Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.
• [30] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [31] 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).
• [32] Recombinant hirudin (lepirudin) as anticoagulant in intensive care patients treated with continuous hemodialysis. Kidney Int Suppl. 1999 Nov;(72):S46-50.
• [33] Anticoagulation with anisindione in a patient with a warfarin-induced skin eruption. Pharmacotherapy. 2003 Apr;23(4):533-6.
• [34] Antithrombin III Utilization in a Large Teaching Hospital. P T. 2013 December; 38(12): 764-767, 779.