Last update 01 Nov 2024

TXA2 synthase

Last update 01 Nov 2024

Basic Info

Synonyms

CYP5, CYP5A1, Cytochrome P450 5A1

+ [12]

Introduction

Catalyzes the conversion of prostaglandin H2 (PGH2) to thromboxane A2 (TXA2), a potent inducer of blood vessel constriction and platelet aggregation (PubMed:8436233, PubMed:11297515, PubMed:9873013, PubMed:11097184, PubMed:24009185, PubMed:22735388). Cleaves also PGH2 to 12-hydroxy-heptadecatrienoicacid (12-HHT) and malondialdehyde, which is known to act as a mediator of DNA damage. 12-HHT and malondialdehyde are formed stoichiometrically in the same amounts as TXA2 (PubMed:11297515, PubMed:9873013, PubMed:22735388). Additionally, displays dehydratase activity, toward (15S)-hydroperoxy-(5Z,8Z,11Z,13E)-eicosatetraenoate (15(S)-HPETE) producing 15-KETE and 15-HETE (PubMed:17459323).

Drugs associated with TXA2 synthase

Ozagrel Trometamol

Target

TXA2 synthase

Mechanism

TXA2 synthase inhibitors

Active Org.

Wuhan Hengxinyuan Pharmaceutical Co., Ltd.

Originator Org.

Wuhan Hengxinyuan Pharmaceutical Co., Ltd.

Active Indication

Platelet Aggregation, Spontaneous [+1]

Inactive Indication

Thrombosis

Drug Highest PhaseApproved

First Approval Ctry. / Loc.

First Approval Date12 Aug 2021

Ozagrel Hydrochloride Hydrate

Target

TXA2 synthase

Mechanism

TXA2 synthase inhibitors

Active Org.

Kissei Pharmaceutical Co., Ltd.

Originator Org.

Ono Pharmaceutical Co., Ltd.

Active Indication

Asthma

Inactive Indication-

Drug Highest PhaseApproved

First Approval Ctry. / Loc.

First Approval Date27 Mar 1992

Ozagrel Sodium

Target

TXA2 synthase

Mechanism

TXA2 synthase inhibitors

Active Org.

Maruishi Pharmaceutical Co., Ltd. [+1]

Originator Org.

Maruishi Pharmaceutical Co., Ltd.

Active Indication

Cerebrovascular Disorders [+2]

Inactive Indication

Sjogren's Syndrome

Drug Highest PhaseApproved

First Approval Ctry. / Loc.

First Approval Date20 Jan 1988

Clinical Trials associated with TXA2 synthase

CTR20231309 / RecruitingPhase 3

吡拉格雷钠注射液治疗急性缺血性脑卒中的多中心、随机、双盲、安慰剂平行对照Ⅲ期临床试验

[Translation] A multicenter, randomized, double-blind, placebo-controlled phase III clinical trial of piragrel sodium injection in the treatment of acute ischemic stroke

评价吡拉格雷钠注射液治疗发病在48 h以内的急性缺血性脑卒中患者的有效性和安全性

[Translation]

To evaluate the efficacy and safety of piragrel sodium injection in the treatment of patients with acute ischemic stroke within 48 hours of onset

Start Date04 Aug 2023

Sponsor / Collaborator

Hefei medical and Pharmaceutical Co., Ltd.

[+1]

CTR20213158 / CompletedPhase 1

健康受试者单次和多次口服HY-021068片的安全性、耐受性与药代、药效动力学及食物对HY-021068片的药代、药效动力学影响的I期临床研究

[Translation] A phase I clinical study on the safety, tolerability, pharmacokinetics, and pharmacodynamics of HY-021068 tablets after single and multiple oral administration in healthy subjects, and the effects of food on the pharmacokinetics and pharmacodynamics of HY-021068 tablets

评价中国健康受试者单多次口服HY-021068片后的安全性与耐受性，评价HY-021068在健康受试者中单多次给药后HY-021068的药代动力学（PK）和药效动力学（PD）特征，评估食物对HY-021068的药代动力学（PK）和药效动力学（PD）的影响

[Translation]

To evaluate the safety and tolerability of HY-021068 tablets after single or multiple oral administration in healthy Chinese subjects, to evaluate the pharmacokinetic (PK) and pharmacodynamic (PD) characteristics of HY-021068 after single or multiple administration in healthy subjects, and to assess the effect of food on the pharmacokinetics (PK) and pharmacodynamics (PD) of HY-021068

Start Date15 Nov 2021

Sponsor / Collaborator

Hefei medical and Pharmaceutical Co., Ltd.

[+2]

ChiCTR2100053162 / RecruitingPhase 1IIT

Phase I clinical study on the safety, tolerability, and pharmacokinetics and pharmacodynamics of single and multiple oral administration of HY-021068 tablets in healthy subjects and the effects of food on the pharmacokinetics and pharmacodynamics of HY-021068 tablets

Start Date01 Nov 2021

Sponsor / Collaborator

The Third Xiangya Hospital of Central South University

100 Clinical Results associated with TXA2 synthase

100 Translational Medicine associated with TXA2 synthase

0 Patents (Medical) associated with TXA2 synthase

1,049

Literatures (Medical) associated with TXA2 synthase

01 Oct 2024·Journal of Chromatography B

A proteomics-based study of the mechanism of oxymatrine to ameliorate hepatic fibrosis in mice

Article

Author: Liu, Enqi ; Li, Weihua ; Wu, Jing ; Jin, Xueqin

OBJECTIVEThis study investigated the protective effect of oxymatrine (OMT) on carbon tetrachloride (CCl₄)-induced hepatic fibrosis in mice and explored its possible targets and signaling pathways.METHODSMale BALB/c mice were randomly divided into blank control, model, positive drug (silymarin), and OMT administration groups, respectively, with 10 mice in each group. Hepatic fibrosis was induced in mice using CCl₄ and the corresponding drug intervention was given. After the final administration, ultrasonography tests, blood tests, and analysis of liver differential proteins using tandem mass tag labeling and liquid chromatography-mass spectrometry were performed.RESULTSOMT intervention ameliorated CCl₄-induced hepatic fibrosis in mice, significantly reduced serum alanine aminotransferase and aspartate aminotransferase levels, down-regulated the expression of fibrosis factors, such as type IV collagen IV, laminin, type III procollagen III, and alpha-smooth muscle actin, and improved liver function. The results of the proteomic analysis showed that the intervention of OMT significantly down-regulated 130 out of 440 up-regulated proteins and up-regulated 70 out of 294 down-regulated proteins, primarily involving the transient receptor potential (TRP) signaling pathway, the peroxisome proliferator-activated receptors (PPAR) signaling pathway, and the metabolic pathway of arachidonic acid. The main differential proteins involved were Cyp2c37, SCP-2, and Tbxas1. In addition, OMT intervention significantly reversed the expression of sterol carrier protein-2 (SCP2) and upregulated the expression of peroxisome proliferator-activated receptor gamma, Cyp2c37, and transient receptor potential cation channel subfamily V member 1 proteins.CONCLUSIONOMT inhibited the proliferative capacity of hepatic stellate cells, induced apoptotic properties, and suppressed the development of fibrosis by elevating Cyp2c37/TRP signaling axis activity and upregulating PPAR pathway activity by inhibiting SCP2.

01 Oct 2024·Clinical and Translational Science

Thai pharmacogenomics database −2 (TPGxD‐2) sequel to TPGxD‐1, analyzing genetic variants in 26 non‐VIPGx genes within the Thai population

Article

Author: Thongchompoo, Nartthawee ; Charoenyingwattana, Angkana ; Own‐eium, Paravee ; Vathesatogkit, Prin ; Sura, Thanyachai ; Chantratita, Wasun ; Teerakulkittipong, Nuttinee ; Klumsathian, Sommon ; Sritara, Piyamitr ; Thabthimthong, Wiphaporn ; Sukasem, Chonlaphat ; John, Shobana ; Eu‐ahsunthornwattana, Jakris ; Dejsuphong, Donniphat

AbstractNext‐generation sequencing (NGS) has transformed pharmacogenomics (PGx), enabling thorough profiling of pharmacogenes using computational methods and advancing personalized medicine. The Thai Pharmacogenomic Database‐2 (TPGxD‐2) analyzed 948 whole genome sequences, primarily from the Electricity Generating Authority of Thailand (EGAT) cohort. This study is an extension of the previous Thai Pharmacogenomic Database (TPGxD‐1) and specifically focused on 26 non‐very important pharmacogenes (VIPGx) genes. Variant calling was conducted using Sentieon (version 201808.08) following GATK's best workflow practices. We then annotated variant call format (VCF) files using Golden Helix VarSeq 2.5.0. Star allele analysis was performed with Stargazer v2.0.2, which called star alleles for 22 of 26 non‐VIPGx genes. The variant analysis revealed a total of 14,529 variants in 26 non‐VIPGx genes, with TBXAS1 had the highest number of variants (27%). Among the 14,529 variants, 2328 were novel (without rsID), with 87 identified as clinically relevant. We also found 56 known PGx variants among the known variants (n = 12,201), with UGT2B7 (19.64%), CYP1B1 (8.9%), SLCO2B1 (8.9%), and POR (8.9%) being the most common. We reported a high frequency of intermediate metabolizers (IMs) in CYP2F1 (34.6%) and CYP4A11 (8.6%), and a high frequency of decreased functional alleles in POR (53.9%) and SLCO1B3 (34.9%) genes. This study enhances our understanding of pharmacogenomic profiling of 26 non‐VIPGx genes of notable clinical importance in the Thai population. However, further validation with additional computational and reference genotyping methods is necessary, and novel alleles identified in this study should undergo further orthogonal validation.

01 Oct 2024·Radiology case reports

Middle-aged women with hematodiaphyseal dysplasia: Ghosal syndrome: Case report.

Article

Author: Sivasubramanian, Barath Prashanth ; Khader, Abul Hasan Shadali Abdul ; Venkata, Vikram Samala ; Ravikumar, Diviya Bharathi ; Qadeer, Husna ; Thungala, Shreya ; Panchal, Viraj ; Srinivasan, Gopinath

Ghosal hematodiaphyseal dysplasia (GHDD) is a rare autosomal recessive disorder characterized by increased bone density involving diaphyses of long bones and defective hematopoiesis. It is due to biallelic variants in the TBXAS1 (OMIM*274180) gene, which encodes for thromboxane synthase. We present a rare case of a middle-aged woman who presented with chronic anemia and bone pain. About 31-year-old Southeast Asian female with a history of persistent iron deficiency anemia (6.1 gm/dL) presents with bilateral knee pain for 4 years. Autoimmune panel turned out to be negative. CT scan of the lower limbs showed multilamellated endosteal thickening specifically involving diaphyses with severe narrowing of medullary canal. PET CT scan revealed tubular remodeling, intramedullary ground glass matrix, and mild cortical thickening with increased FDG uptake in diaphyseal regions of femur and tibia. Bone marrow biopsy of left tibia revealed fibrocellular marrow with dyserythropoiesis. Considering the slow progression of illness over 4 years and radiological evidence suggestive of bone remodeling with severe narrowing of medullary canal as the cause of anemia, the patient underwent molecular analysis for GHDD. Results revealed homozygous p.Arg412Gln (exon 11) in TBXAS1 gene. Considering the effect of NSAIDs on cyclooxygenase and its downstream metabolites, oral Aspirin 150 mg/day was initiated. Hemoglobin improved to 11 gm/dL at 3-month follow-up visit. The complexity of reaching a diagnosis of GHDD underscores the importance of maintaining a high clinical suspicion and thorough analysis of radiological evidence. The treatment for GHDD involves aspirin, a readily available drug.

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TXA2 synthase

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