Delving into the Latest Updates on Sarpogrelate Hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Sarpogrelate, Sarpogrelate hydrochloride (JP17)

+ [5]

Target

5-HT2A receptor

Mechanism

5-HT2A receptor antagonists(Serotonin 2a (5-HT2a) receptor antagonists)

Therapeutic Areas

Cardiovascular Diseases

Active Indication

Arterial Occlusive Diseases

Inactive Indication

Brain InfarctionPeripheral arterial occlusive disease

Originator Organization

Mitsubishi Tanabe Pharma Corp.

Active Organization

Mitsubishi Tanabe Pharma Corp.

Inactive Organization

Alvogen Korea Co., Ltd.

Drug Highest PhaseApproved

First Approval Date

JP (02 Jul 1993),

Arterial Occlusive Diseases

Regulation-

Login to view timeline

Structure

Molecular FormulaC24H32ClNO6

InChIKeyPOQBIDFFYCYHOB-UHFFFAOYSA-N

CAS Registry135159-51-2

View All Structures (2)

A Randomized, Open-label, Investigator-initiated, Pilot Clinical Trial Comparing the Improvement for Ankle Brachial Index and Safety of Sarpogrelate and Clopidogrel in Stroke Patients Accompanying Lower Extremity Vascular Atherosclerosis With Decrease of Ankle Brachial Index and Intermittent Claudication.

The clinical trial aims to confirm the improvement effect of the ankle brachial index and the safety of sarpogrelate administration compared to clopidogrel in stroke patients with decreased ankle brachial arterial pressure index and intermittent claudication of lower limb vascular atherosclerosis. Subjects are assigned to one of the two combinations through random allocation.
Intervention group: Aspirin 100mg + sarpogrelate 300mg dosing group, Control group: Aspirin 100mg + clopidogrel 75mg dosing group. This clinical trial is a prospective open study and will be conducted in compliance with the usual diagnosis and treatment process, and in particular, all trial subjects will be tested and treated appropriately in accordance with the standard treatment guidelines for ischemic stroke during the clinical trial period.

Start Date16 May 2024

Sponsor / Collaborator

Ewha Womans University

NCT05730621 / RecruitingPhase 4

A Study to Compare the Effects of Sarpogrelate Sustained Release /Aspirin Combination Therapy Versus Aspirin on Blood Viscosity in the Patients With Peripheral Arterial Disease and Coronary Artery Disease; A Prospective, Randomized, Parallel, Open-Label, Single-center, Phase IV Clinical Trial

This study is to compare the effects of sarpogrelate sustained release /aspirin combination therapy versus aspirin on blood viscosity in the patients with peripheral arterial disease and coronary artery disease

Start Date11 Jan 2023

Sponsor / Collaborator

Yuhan Corp.

KCT0006237 / Not yet recruitingPhase 4IIT

A Phase 4, Randomized, Open, Phase 4 Study to Evaluate the Efficacy of Sarpogrelate versus Cilostazol in patients with type2 diabetes with thickened carotid artery

Start Date15 Jun 2021

Sponsor / Collaborator

THE CATHOLIC UNIVERSITY OF KOREA, INCHEON ST. MARYS HOSPITAL

100 Clinical Results associated with Sarpogrelate Hydrochloride

Login to view more data

100 Translational Medicine associated with Sarpogrelate Hydrochloride

Login to view more data

100 Patents (Medical) associated with Sarpogrelate Hydrochloride

Login to view more data

284

Literatures (Medical) associated with Sarpogrelate Hydrochloride

22 Oct 2024·Current Vascular Pharmacology

Efficacy and Safety of Sarpogrelate on Symptom Improvement in Patients with Peripheral Arterial Disease (PAD) and/or Being at Risk of PAD: A Single Arm, Multi-Centered, Open-Label Trial

Article

Author: Jeon, Ung ; Lee, Kyong Hoon ; Min, Kyung Wan ; Won, Jong Chul ; Park, Jae Hyoung ; Song, Tae-Jin ; Jeong, Ho-Seung ; Lim, Soo ; Kim, Hee-Tae ; Park, Keun Yong

Aims:To assess the efficacy and safety of sarpogrelate (300 mg) for symptom improvement in patients having peripheral arterial disease (PAD) and/or being at risk of PAD in clinical practice using the Peripheral Artery Questionnaire (PAQ).Background:Symptomatic changes with antiplatelets in patients with PAD are limited.Objective:To determine the effect and safety of sarpogrelate on the PAQ at 24 weeks from baseline.Method:A total of 1003 patients having PAD and/or being at risk of PAD from 17 tertiary hospitals in South Korea who were treated with sarpogrelate, were enrolled in this study. PAQs were collected at baseline and at 12 and 24 weeks, together with physical examination and vital signs measurements. Lifestyle pattern was also investigated.Results:The average PAQ Summary Score in the efficacy evaluation analysis group significantly improved from 62.9 ± 23.7 at baseline to 68.9 ± 21.7 at 24 weeks (P<0.0001). Physical limitation items significantly improved from 69.5 ± 30.0 at baseline to 72.9 ± 28.3 after 24 weeks (P=0.0011). Symptom stability also significantly improved from 52.1 ± 21.6 at baseline to 63.6 ± 22.9 after 24 weeks (P<0.0001). Symptoms, treatment satisfaction, quality of life, and social limitation domains all improved after treatment. A total of 201 patients reported adverse events (20.0%), not directly associated with treatment.Conclusion:Treatment with 300 mg (orally) of sarpogrelate demonstrated statistically significant improvements in all domains and for the summary score of the PAQ at 24 weeks, it gave good results in terms of safety. Sarpogrelate may be helpful in reducing symptoms related to PAD.

01 Jul 2024·Biomedicine & Pharmacotherapy

Chronic sarpogrelate treatment improves renal sympathetic hyperactivity in experimental diabetes

Article

Author: Martín, María Luisa ; Morán, Asunción ; Fernández-González, Juan Francisco ; García-Pedraza, José Ángel ; García-Domingo, Mónica ; Terol-Úbeda, Anaïs Clara

Diabetes and derived complications, especially diabetic nephropathy and neuropathy annually cause great morbimortality worldwide. 5-hydroxytryptamine (5-HT) acts as a modulator of renal sympathetic input and vascular tone. In this line, 5-HT₂ receptor blockade has been linked with reduced incidence and progression of diabetic microvascular alterations. In this work, we aimed to determine, in diabetic rats, whether 5-HT₂ blockade ameliorates renal function and to characterize the serotonergic modulatory action on renal sympathetic neurotransmission. Diabetes was induced in male Wistar rats by alloxan administration (150 mg/kg, s.c.), and sarpogrelate (30 mg/kg·day, p.o.; 5-HT₂ antagonist) was administered for 14 days (DM-S). Normoglycemic and diabetic (DM) animals were maintained as aged-matched controls. At 28th day, DM-S animals were anesthetized and prepared for the in situ autoperfusion of the kidney. Renal vasoconstrictor responses were induced electrically or by i.a. noradrenaline (NA) administration. The role of 5-HT and selective 5-HT agonist/antagonist were studied on these renal vasopressor responses. Sarpogrelate treatment decreased renal sympathetic-induced vasopressor responses, reduced renal hypertrophy and kidney damage markers increased in DM. Intraarterial 5-HT inhibited the sympathetic-induced renal vasoconstrictions, effect reproduced by 5-CT, AS-19, L-694,247 and LY 344864 (5-HT_1/5/7, 5-HT₇, 5-HT_1D and 5-HT_1F receptor agonists, respectively). Blocking 5-HT_1D/1F/7 receptors completely abolished the 5-CT sympatho-inhibition. NA vasoconstrictions were not altered by any of the 5-HT agonists tested. Thus, in experimental diabetes, chronic sarpogrelate treatment reduces renal damage markers, kidney hypertrophy and renal sympathetic hyperactivity and modifies serotonergic modulation of renal sympathetic neurotransmission, causing a sympatho-inhibition by prejunctional 5-HT_1D/1F and 5-HT₇ activation.

01 Mar 2023·Molecular Immunology

Myocardial ischemia-reperfusion injury is probably due to the excessive production of mitochondrial ROS caused by the activation of 5-HT degradation system mediated by PAF receptor

Article

Author: Guan, Jing ; Xu, Fan ; Fu, Jihua ; Jin, Jiaqi ; Zhang, Yuxin

AIMPreviously, we revealed a crucial role of 5-HT degradation system (5DS), consisting of 5-HT2A receptor (5-HT2AR), 5-HT synthases and monoamine oxidase A (MAO-A), in ischemia-reperfusion (IR)-caused organ injury. Whereas, platelet activating factor receptor (PAFR) also mediates myocardial ischemia-reperfusion injury (MIRI). Here, we try to clarify the relationship between 5DS and PAFR in mediating MIRI.METHODSH9c2 cell injury and rat MIRI were caused by hypoxia/reoxygenation (H/R) or PAF, and by ligating the left anterior descending coronary artery then untying, respectively. 5-HT_2AR and PAFR antagonists [sarpogrelate hydrochloride (SH) and BN52021], MAO-A, AKT, mTOR and 5-HT synthase inhibitors (clorgyline, perifosine, rapamycin and carbidopa), and gene-silencing PKCε were used in experiments RESULTS: The mitochondrial ROS production, respiratory chain damage, inflammation, apoptosis and myocardial infarction were significantly prevented by BN52021, SH and clorgyline in H/R and PAF-treated cells and in IR myocardium. BN52021 also significantly suppressed the upregulation of PAFR, 5-HT_2AR, 5-HT synthases and MAO-A expression (mRNA and protein), and Gα_q and PKCε (in plasmalemma) expression induced by H/R, PAF or IR; the effects of SH were similar to that of BN52021 except for no affecting the expression of PAFR and 5-HT_2AR. Gene-silencing PKCε suppressed H/R and PAF-induced upregulation of 5-HT synthases and MAO-A expression in cells; perifosine and rapamycin had not such effects; however, clorgyline suppressed H/R and PAF-induced phosphorylation of AKT and mTOR.CONCLUSIONMIRI is probably due to PAFR-mediated 5-HT_2AR activation, which further activates PKCε-mediated 5-HT synthesis and degradation, leading to mitochondrial ROS production.

100 Deals associated with Sarpogrelate Hydrochloride

Login to view more data

External Link

KEGG	Wiki	ATC	Drug Bank
D01624	Sarpogrelate Hydrochloride	B01A	DB12163

R&D Status

Approved

10 top approved records.

Login

to view more data

Indication	Country/Location	Organization	Date
Arterial Occlusive Diseases	JP	Mitsubishi Tanabe Pharma Corp.	02 Jul 1993

Developing

10 top R&D records.

Login

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Peripheral arterial occlusive disease	Preclinical	-	Alvogen Korea Co., Ltd.	01 Oct 2012
Brain Infarction	Preclinical	-	Mitsubishi Tanabe Pharma Corp.	01 Jan 2001

Login to view more data

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT01165567 (Pubmed \| Eur Spine J)	Phase 4	Contrast agents	-	Sarpogrelate	ygalvvvaod(talomvwcyd) = bkulpwtasg cocjnyvzel (yoqtnfjkpw ) View more	Negative	21 Oct 2019
				Sarpogrelate (Control)	ygalvvvaod(talomvwcyd) = tphaeogexd cocjnyvzel (yoqtnfjkpw ) View more
NCT02607436 (EASD2016)	Phase 4	Diabetes Mellitus, Type 2 \| Coronary Artery Disease	-	Sarpogrelate 300 mg/day plus aspirin 100 mg/day	kdgcjweawz(lrtusgofdu) = scilzsnbjt cumzmvffyd (zlshomvsze, 57.5) View more	Positive	14 Sep 2016
				Aspirin 100 mg/day	jmkqpiwncf(gimzcfuxjg) = inxyicfdgy drriexnzlp (cdkrtyxoom, 13.6) View more
NCT00129805 (S-ACCESS, Pubmed \| Cochrane Database Syst Rev)	Phase 3	Brain Infarction	1,510	Sarpogrelate (100 mg TID)	adeqqixoim(dmupffkocq) = zsirbkhyie awzilxdgov (ddnkxzrpvj ) View more	Negative	01 Jun 2008
				Aspirin (81 mg/d)	adeqqixoim(dmupffkocq) = fiisjwjcwn awzilxdgov (ddnkxzrpvj ) View more