Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TT2O84V)

• DTT Name: Thromboxane A2 receptor (TBXA2R)
• Synonyms: TXA2-R; TXA2 receptor; Prostanoid TP receptor
• Gene Name: TBXA2R
• DTT Type: Successful target; [1]
• BioChemical Class: GPCR rhodopsin
• UniProt ID: TA2R_HUMAN
• TTD ID: T76198
• Sequence:
  MWPNGSSLGPCFRPTNITLEERRLIASPWFAASFCVVGLASNLLALSVLAGARQGGSHTR
  SSFLTFLCGLVLTDFLGLLVTGTIVVSQHAALFEWHAVDPGCRLCRFMGVVMIFFGLSPL
  LLGAAMASERYLGITRPFSRPAVASQRRAWATVGLVWAAALALGLLPLLGVGRYTVQYPG
  SWCFLTLGAESGDVAFGLLFSMLGGLSVGLSFLLNTVSVATLCHVYHGQEAAQQRPRDSE
  VEMMAQLLGIMVVASVCWLPLLVFIAQTVLRNPPAMSPAGQLSRTTEKELLIYLRVATWN
  QILDPWVYILFRRAVLRRLQPRLSTRPRSLSLQPQLTQRSGLQ
• Function: The activity of this receptor is mediated by a G-protein that activates a phosphatidylinositol-calcium second messenger system. In the kidney, the binding of TXA2 to glomerular TP receptors causes intense vasoconstriction. Activates phospholipase C. Isoform 1 activates adenylyl cyclase. Isoform 2 inhibits adenylyl cyclase. Receptor for thromboxane A2 (TXA2), a potent stimulator of platelet aggregation.
• KEGG Pathway:
  Calcium signaling pathway (hsa04020)
  Neuroactive ligand-receptor interaction (hsa04080)
  Platelet activation (hsa04611)
• Reactome Pathway:
  G alpha (q) signalling events (R-HSA-416476)
  G alpha (12/13) signalling events (R-HSA-416482)
  Thromboxane signalling through TP receptor (R-HSA-428930)
  Prostanoid ligand receptors (R-HSA-391908)

Molecular Interaction Atlas (MIA) of This DTT

3 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Alprostadil	DMWH7NQ	Aorta coarctation		Approved	[2]
Ridogrel	DMWH9CN	Acute myocardial infarction	BA41	Approved	[1]
LAROPIPRANT	DM5FABJ	Coronary heart disease	BA80.Z	Phase 4	[3]

11 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Ramatroban	DMB8UQ3	Perennial allergic rhinitis	CA08.03	Phase 2/3	[4]
FK-070	DMJSD5W	Angina pectoris	BA40	Phase 2	[5]
Ifetroban	DMEV39E	Aspirin-induced asthma	CA23.20	Phase 2	[6]
Ifetroban sodium	DMZP84Y	Thrombosis	DB61-GB90	Phase 2	[7]
KP-496	DMCO8UZ	Asthma	CA23	Phase 2	[8]
TAK-128	DMHPEFS	Diabetic neuropathy	8C0Z	Phase 2	[9]
BIBV 308	DMUBMN5	Peripheral vascular disease	BD4Z	Phase 1	[7]
DT-TX-30	DM1FX09	Angina pectoris	BA40	Phase 1	[10]
G-619	DM3H6YC	Thrombosis	DB61-GB90	Phase 1	[11]
YM-57158	DMS31YW	Allergic rhinitis	CA08.0	Phase 1	[12]
PGF2alpha	DM4XAU7	Solid tumour/cancer	2A00-2F9Z	Clinical trial	[13]

18 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Domitroban	DM3OUWC	Thrombosis	DB61-GB90	Discontinued in Preregistration	[14]
DALTROBAN	DMNQIKV	N. A.	N. A.	Discontinued in Phase 3	[15]
Seratrodast	DMPNTDL	Allergic asthma	CA23.0	Discontinued in Phase 3	[16]
Terutroban sodium	DMYF1DN	Thrombosis	DB61-GB90	Discontinued in Phase 3	[17]
ICI-192605	DMY8X6Q	Thrombosis	DB61-GB90	Discontinued in Phase 2	[18]
Linotroban	DM32JL5	Thrombosis	DB61-GB90	Discontinued in Phase 2	[19]
SQ-30741	DMTC4VY	Thrombosis	DB61-GB90	Discontinued in Phase 2	[20]
Z-335	DM2438J	Thrombosis	DB61-GB90	Discontinued in Phase 2	[21]
CGS-22652	DMF05DL	Angina pectoris	BA40	Discontinued in Phase 1	[22]
KT2-962	DMBH5G3	Thrombosis	DB61-GB90	Discontinued in Phase 1	[23]
KW-3635	DMG068H	Thrombosis	DB61-GB90	Discontinued in Phase 1	[24]
L-657925	DMOTY3G	N. A.	N. A.	Terminated	[25]
ON-579	DMTS6HB	Asthma	CA23	Terminated	[26]
SQ-33961	DMZBQ4I	Thrombosis	DB61-GB90	Terminated	[27]
Sulotroban	DM4SVIR	Asthma	CA23	Terminated	[28]
UP-116-77	DMEIR7F	Thrombosis	DB61-GB90	Terminated	[29]
Vapiprost	DMJLV03	Cardiovascular disease	BA00-BE2Z	Terminated	[30]
ZT-386	DM193WR	Asthma	CA23	Terminated	[31]

27 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
10,10-difluoro TXA2	DML745Y	Discovery agent	N.A.	Investigative	[32]
AGN 191976	DMTPV4Y	Discovery agent	N.A.	Investigative	[33]
AGN192093	DMISJXB	Discovery agent	N.A.	Investigative	[33]
AH23848	DM4S1Y6	Discovery agent	N.A.	Investigative	[13]
BM-573	DMD2H7L	Discovery agent	N.A.	Investigative	[34]
butaprost (free acid form)	DM5MZHP	Discovery agent	N.A.	Investigative	[13]
carbacyclin	DMMBQYE	Discovery agent	N.A.	Investigative	[13]
carbocyclic thromboxane A2	DMGKSVF	Discovery agent	N.A.	Investigative	[35]
cloprostenol	DMH01JV	Discovery agent	N.A.	Investigative	[13]
EP 171	DM7YION	Discovery agent	N.A.	Investigative	[36]
fluprostenol	DM9Q2PG	Discovery agent	N.A.	Investigative	[13]
I-BOP	DMJAPML	Discovery agent	N.A.	Investigative	[37]
I-SAP	DMJ2FQA	Discovery agent	N.A.	Investigative	[38]
M&B 28767	DMJQG82	Discovery agent	N.A.	Investigative	[13]
ONO-3708	DM84IW9	Discovery agent	N.A.	Investigative	[39]
ONO-8809	DM5BMA9	Thrombosis	DB61-GB90	Investigative	[40]
PGH2	DMZFVGC	Discovery agent	N.A.	Investigative	[35]
S 18204	DM2FC5V	Discovery agent	N.A.	Investigative	[41]
SQ 26655	DMRP42B	Discovery agent	N.A.	Investigative	[42]
SQ-29548	DM9G3UD	Discovery agent	N.A.	Investigative	[13]
STA2	DMIYJ2M	Discovery agent	N.A.	Investigative	[37]
U-44069	DM0DMNS	Discovery agent	N.A.	Investigative	[43]
U46619	DM13FX4	Discovery agent	N.A.	Investigative	[13]
[125I]BOP	DMV6I7H	Discovery agent	N.A.	Investigative	[44]
[125I]PTA-OH	DMROKJP	Discovery agent	N.A.	Investigative	[45]
[125I]SAP	DM1DXHG	Discovery agent	N.A.	Investigative	[38]
[125I]SQ-29548	DM0GKMA	Discovery agent	N.A.	Investigative	[46]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Asthma	CA23	Nasal and bronchial airway	2.78E-04	-0.11	-0.31

References

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