Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTCIHJA)

• DTT Name: Coagulation factor Xa (F10)
• Synonyms: Fxa; Factor Xa; F10; Activated coagulation factor X
• Gene Name: F10
• DTT Type: Successful target; [1]
• Related Disease:
  Blood-forming organ disease [ICD-11: 3C0Z]
  Christmas disease [ICD-11: 3B11]
  Coagulation defect [ICD-11: 3B10]
  Coronary thrombosis [ICD-11: BA43]
  Deep vein thrombosis [ICD-11: BD71]
  Supraventricular tachyarrhythmia [ICD-11: BC81]
  Thrombosis [ICD-11: DB61-GB90]
  Venous thromboembolism [ICD-11: BD72]
• BioChemical Class: Peptidase
• UniProt ID: FA10_HUMAN
• TTD ID: T84631
• EC Number: EC 3.4.21.6
• Sequence:
  MGRPLHLVLLSASLAGLLLLGESLFIRREQANNILARVTRANSFLEEMKKGHLERECMEE
  TCSYEEAREVFEDSDKTNEFWNKYKDGDQCETSPCQNQGKCKDGLGEYTCTCLEGFEGKN
  CELFTRKLCSLDNGDCDQFCHEEQNSVVCSCARGYTLADNGKACIPTGPYPCGKQTLERR
  KRSVAQATSSSGEAPDSITWKPYDAADLDPTENPFDLLDFNQTQPERGDNNLTRIVGGQE
  CKDGECPWQALLINEENEGFCGGTILSEFYILTAAHCLYQAKRFKVRVGDRNTEQEEGGE
  AVHEVEVVIKHNRFTKETYDFDIAVLRLKTPITFRMNVAPACLPERDWAESTLMTQKTGI
  VSGFGRTHEKGRQSTRLKMLEVPYVDRNSCKLSSSFIITQNMFCAGYDTKQEDACQGDSG
  GPHVTRFKDTYFVTGIVSWGEGCARKGKYGIYTKVTAFLKWIDRSMKTRGLPKAKSHAPE
  VITSSPLK
• Function: Factor Xa is avitamin K-dependent glycoprotein that converts prothrombin to thrombin in the presence of factor Va, calcium and phospholipid during blood clotting.
• Reactome Pathway:
  Intrinsic Pathway of Fibrin Clot Formation (R-HSA-140837)
  Common Pathway of Fibrin Clot Formation (R-HSA-140875)
  Gamma-carboxylation of protein precursors (R-HSA-159740)
  Transport of gamma-carboxylated protein precursors from the endoplasmic reticulum to the Golgi apparatus (R-HSA-159763)
  Removal of aminoterminal propeptides from gamma-carboxylated proteins (R-HSA-159782)
  Extrinsic Pathway of Fibrin Clot Formation (R-HSA-140834)
• BioCyc Pathway: MetaCyc:HS05000-MON

Molecular Interaction Atlas (MIA) of This DTT

11 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Apixaban	DM89JLN	Thrombosis	DB61-GB90	Approved	[1], [2]
Betrixaban	DM2C4RF	Venous thromboembolism	BD72	Approved	[3]
Certoparin sodium	DMUR94J	Deep vein thrombosis	BD71	Approved	[4], [5], [6]
Coagulation Factor IX	DM8HBJI	Haemophilia B	3B11.0	Approved	[7]
Danaparoid	DM6CLBN	Deep venous clot	BD71	Approved	[8]
DU-176B	DMCIJBH	Atrial fibrillation	BC81.3	Approved	[9]
Emicizumab	DM0AQ83	Factor VIII deficiency	3B10	Approved	[10]
Fondaparinux sodium	DMWS3FH	Venous thrombosis	BA43	Approved	[11], [12]
Lmw heparin	DMJPD06	Coagulation defect	3B10.0	Approved	[4], [13]
Nadroparin calcium	DMBNKST	Coagulation defect	3B10.0	Approved	[14], [4]
Rivaroxaban	DMQMBZ1	Deep vein thrombosis	BD71	Approved	[15]

15 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Human coagulation factor X	DMYA6TR	Renal cell carcinoma	2C90	BLA submitted	[16], [17]
Melagatran	DM4W8RE	N. A.	N. A.	Phase 3	[18]
PRT4445	DMVU8RW	Bleeding disorder	GA20-GA21	Phase 3	[16], [17]
SSR-126517E	DMT71EX	Thrombosis	DB61-GB90	Phase 3	[16], [17]
SR-123781A	DM5WQ2U	Venous thrombosis	BA43	Phase 2/3	[19]
Antistasin	DMDKRS3	Attention deficit hyperactivity disorder	6A05.Z	Phase 2	[20]
EP-217609	DMPC4EK	Thrombosis	DB61-GB90	Phase 2	[21]
GW-813893	DMH0C8J	Thrombosis	DB61-GB90	Phase 2	[16], [17]
LY-517717	DM8OG0J	Thrombosis	DB61-GB90	Phase 2	[16], [17]
BI-11634	DMKQHE5	Thrombosis	DB61-GB90	Phase 1	[16], [17]
BIBT986	DMP70FI	Thrombosis	DB61-GB90	Phase 1	[22]
EP-42675	DMKR3GD	Thrombosis	DB61-GB90	Phase 1	[23]
GCC-4401	DMHMZC7	Thrombosis	DB61-GB90	Phase 1	[16], [17]
R-1663	DM64U1Y	Coagulation defect	3B10.0	Phase 1	[16], [17]
SSR-128428	DMOJA7N	Thrombosis	DB61-GB90	Phase 1	[24]

19 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Darexaban maleate	DMC40SD	Acute coronary syndrome	BA41	Discontinued in Phase 3	[25]
Idraparinux	DM3SKAC	Thrombosis	DB61-GB90	Discontinued in Phase 3	[26]
Otamixaban	DMGOPMK	Angina pectoris	BA40	Discontinued in Phase 3	[26]
Valspodar	DMXRU9M	Acute myeloid leukaemia	2A60	Discontinued in Phase 3	[27], [20]
Octopamine	DMLQVTJ	Thrombosis	DB61-GB90	Discontinued in Phase 2a	[28], [29]
DX-9065	DMEQLC4	Coagulation defect	3B10.0	Discontinued in Phase 2	[16], [17]
DX-9065a	DMIXUMZ	Angina pectoris	BA40	Discontinued in Phase 2	[30]
PD-348292	DMMYNKH	Thrombosis	DB61-GB90	Discontinued in Phase 2	[1], [31]
R-68151	DM2NTJY	Psoriasis vulgaris	EA90	Discontinued in Phase 2	[32]
TAK-442	DMG4RFO	Thrombosis	DB61-GB90	Discontinued in Phase 2	[33]
AVE-3247	DMMPBZF	Thrombosis	DB61-GB90	Discontinued in Phase 1	[16], [17]
DPC 423	DMR6INY	Thrombosis	DB61-GB90	Discontinued in Phase 1	[34]
EMD-503982	DMQH8L2	Thrombosis	DB61-GB90	Discontinued in Phase 1	[16], [17]
JTV-803	DMXUH6W	Thrombosis	DB61-GB90	Discontinued in Phase 1	[16], [17]
YM-75466	DMDJ2O5	Thrombosis	DB61-GB90	Discontinued in Phase 1	[16], [17]
ZD-4927	DMQDNU1	Thrombosis	DB61-GB90	Discontinued in Phase 1	[16], [17]
Draculin	DMX4KIT	Thrombosis	DB61-GB90	Terminated	[36]
Hirufaxin	DM784QJ	Thrombosis	DB61-GB90	Terminated	[16], [17]
Ym60828	DM7VGOC	N. A.	N. A.	Terminated	[20]

2 Preclinical Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
CS-3030	DMK230A	Thrombosis	DB61-GB90	Preclinical	[16], [17]
Trimidox	DMY8GDA	Solid tumour/cancer	2A00-2F9Z	Preclinical	[35]

35 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
1,2,3,4,6-penta-O-galloyl-beta-D-glucose	DMTK650	Discovery agent	N.A.	Investigative	[37]
3-chlorophenyl 2-oxo-2H-chromene-3-carboxylate	DMZ0F7E	Discovery agent	N.A.	Investigative	[38]
4-(4-Benzyloxy-3-methoxy-benzylamino)-benzamidine	DME3PUT	Discovery agent	N.A.	Investigative	[39]
5-desgalloylstachyurin	DM6TM1L	Discovery agent	N.A.	Investigative	[37]
Beta-Hydroxy Aspartic Acid	DMO8LPZ	Discovery agent	N.A.	Investigative	[40]
BMS-269223	DMZLE0U	Discovery agent	N.A.	Investigative	[41]
BMS-344577	DM9WRUG	Discovery agent	N.A.	Investigative	[41]
BMS-740808	DMQ24TI	Discovery agent	N.A.	Investigative	[42]
CASUARIIN	DM5E21C	Discovery agent	N.A.	Investigative	[37]
CI-1031	DMTKVDZ	Discovery agent	N.A.	Investigative	[43], [44]
D-Pro-Phe-Arg chloromethyl ketone	DMRJQ8X	Discovery agent	N.A.	Investigative	[45]
DT-831j	DM3TMUK	Thrombosis	DB61-GB90	Investigative	[16], [17]
EP-37	DMHN82B	Cerebrovascular ischaemia	8B1Z	Investigative	[16], [17]
Gamma-Carboxy-Glutamic Acid	DMZMCT0	Discovery agent	N.A.	Investigative	[46]
GC-2107	DM46HAS	Thrombosis	DB61-GB90	Investigative	[16], [17]
Lefaxin	DM0CEY3	Discovery agent	N.A.	Investigative	[20]
M55113	DMM5X8Z	Discovery agent	N.A.	Investigative	[47]
Molecule 11	DMZ6H1X	Discovery agent	N.A.	Investigative	[48]
Pedunculagin	DMKLRCX	Discovery agent	N.A.	Investigative	[37]
PhSO2-Gly-(Me-Gly)-Arg-(2-thiazole)	DMN0D14	Discovery agent	N.A.	Investigative	[49]
PRT-064445	DMOVE31	Bleeding disorder	GA20-GA21	Investigative	[16], [17]
RAZAXABAN	DMPML15	Discovery agent	N.A.	Investigative	[42]
Recombinant coagulation factors	DMFAST4	Hemophilia	3B10.0	Investigative	[16], [17]
Recombinant Factor X	DMX6LV3	Hemophilia	3B10.0	Investigative	[16], [17]
SC-83157	DM96ATK	Discovery agent	N.A.	Investigative	[50]
SF303	DMH36A9	Discovery agent	N.A.	Investigative	[34]
SK509	DM73SC6	Discovery agent	N.A.	Investigative	[34]
SK549	DMK1OP2	Discovery agent	N.A.	Investigative	[51]
SK554	DMUTBZ8	Discovery agent	N.A.	Investigative	[20]
SN429	DMP4IJ6	Thrombosis	DB61-GB90	Investigative	[50]
Tellimagrandin II	DM60HU5	Discovery agent	N.A.	Investigative	[37]
YM-96765	DMPU5TC	Discovery agent	N.A.	Investigative	[52]
ZK-810388	DMNOWAQ	Discovery agent	N.A.	Investigative	[53]
ZK-813039	DMIC4HJ	Discovery agent	N.A.	Investigative	[53]
ZK-814048	DMCBV5F	Discovery agent	N.A.	Investigative	[53]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Renal cancer	2C82	Kidney	4.84E-02	-0.28	-0.9

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