Delving into the Latest Updates on Bucladesine Sodium with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

3',5'-cyclic AMP dibutyrate, Bucladesine, Bucladesine sodium (JAN)

+ [17]

Target

cGMP-PDE

Mechanism

cGMP-PDE inhibitors(3',5'-cyclic phosphodiesterase inhibitors)

Therapeutic Areas

Cardiovascular DiseasesSkin and Musculoskeletal Diseases

Active Indication

Pressure UlcerSkin UlcerVentricular Dysfunction

Inactive Indication-

Originator Organization

Alfresa Pharma Corp.

Active Organization

Alfresa Pharma Corp.Nipro Pharma Corp.

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

JP (24 Jul 1984),

Ventricular Dysfunction

Regulation-

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Structure

Molecular FormulaC18H24N5NaO8P

InChIKeyWAOODRHZYQRSDS-JBVYASIDSA-N

CAS Registry16980-89-5

View All Structures (2)

主要研究目的：考察单次静脉泵入300mg受试制剂注射用二丁酰环磷腺苷钠和参比制剂注射用二丁酰环磷腺苷钠在中国成年健康受试者体内的药代动力学特征，初步评估两种制剂的生物等效性。次要研究目的：评价单次静脉泵入300mg受试制剂和参比制剂在中国成年健康受试者中的安全性。

[Translation]

Main study objectives: To investigate the pharmacokinetic characteristics of a single intravenous infusion of 300 mg of the test preparation sodium dibutyryladenosine cyclophosphate for injection and the reference preparation sodium dibutyryladenosine cyclophosphate for injection in healthy adult Chinese subjects, and to preliminarily evaluate the bioequivalence of the two preparations. Secondary study objectives: To evaluate the safety of a single intravenous infusion of 300 mg of the test preparation and the reference preparation in healthy adult Chinese subjects.

Start Date-

Sponsor / Collaborator

Hunan Er-Kang Pharmaceutical Co., Ltd.

JPRN-jRCT2041210065 / RecruitingPhase 1/2IIT

A Phase I/II Multi-Institutional Study of Bucladesine in Patients with Severe Methylmalonic Acidemia - McAMP

Start Date10 Mar 2022

Sponsor / Collaborator-

100 Clinical Results associated with Bucladesine Sodium

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100 Translational Medicine associated with Bucladesine Sodium

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100 Patents (Medical) associated with Bucladesine Sodium

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5,996

Literatures (Medical) associated with Bucladesine Sodium

01 Sep 2024·Genomics

Screening of novel disease genes of sepsis-induced myocardial Disfunction by RNA sequencing and bioinformatics analysis

Article

Author: Xiao, Zixi ; Wu, Zehong ; Zhang, Weizhi ; Li, Dongping ; Zhou, Haojie ; Yao, Hanyi ; Gao, Xingjian ; Liu, Shufang ; Yi, Zhangqing

BACKGROUNDThere is still a lack of effective treatment for sepsis-induced myocardial dysfunction (SIMD), while the pathogenesis of SIMD still remains largely unexplained.METHODSRNA sequencing results (GSE267388 and GSE79962) were used for cross-species integrative analysis. Bioinformatic analyses were used to delve into function, tissue- and cell- specificity, and interactions of genes. External datasets and qRT-PCR experiments were used for validation. L1000 FWD was used to predict targeted drugs, and 3D structure files were used for molecular docking.RESULTSBased on bioinformatic analyses, ten differentially expressed genes were selected as genes of interest, seven of which were verified to be significantly differential expression. Bucladesine was considered as a potential targeted drug for SIMD, which banded to seven target proteins primarily by forming hydrogen bonds.CONCLUSIONIt was considered that Cebpd, Timp1, Pnp, Osmr, Tgm2, Cp, and Asb2 were novel disease genes, while bucladesine was a potential therapeutic drug, of SIMD.

01 Sep 2024·Reproductive Biology

Overexpression of USP22 ameliorates LPS-induced endometrial stromal cells inflammation and modulates cells decidualization by inhibiting ferroptosis

Article

Author: Zhang, Guoli ; Xu, Xinghua ; Xing, Xiuye ; Yi, Fangjie

Endometritis and the failure of decidualization of the endometrium are important factors contributing to the increased incidence of abortion. USP22 is associated with various inflammatory diseases and has been shown to be involved in endometrial decidualization in mice. This study aims to investigate whether USP22 is involved in the regulation of inflammatory response and decidualization in human endometrial stromal cells (hESCs). In this study, lipopolysaccharide (LPS) was used to induce inflammation in hESCs, and MPA combined with cAMP was used to induce decidualization of hESCs. USP22 overexpression vector was constructed to study the role of USP22 in endometritis. The results showed that the USP22 protein and mRNA levels were decreased in LPS-induced hESCs. LPS induction increased the levels of TNF-α, IL-1β, and IL-6, as well as the expression of iNOS and COX2 proteins in hESCs. In the LPS group, the levels of F-actin, PRL, IGFBP1, SLC7A11, and GPX4 proteins decreased, while the levels of lipid peroxidation and total iron content increased. Additionally, the levels of ACSL4 and TFR1 proteins were up-regulated. Overexpression of USP22 reversed LPS-induced cellular inflammation, attenuated decidualization, and inhibited ferroptosis. However, the use of ferroptosis inducers diminished the regulatory effects of USP22 on inflammatory responses and decidualization. In summary, these suggested that USP22 reduces the LPS-induced inflammatory response and regulates the decidualization of hESCs, and possibly involving ferroptosis.

07 Aug 2024·Journal of the American Chemical Society

Regioselective Homolytic C²–H Borylation of Unprotected Adenosine and Adenine Derivatives via Minisci Reaction

Article

Author: Jiang, Yujie ; Zhou, Dazhi ; Que, Yingchuan ; Li, Zhiming ; Chen, Gang ; Zhou, Yutong ; Li, Yangyan ; Yang, Hui ; Butt, Madiha

A Minisci-type borylation of unprotected adenosine, adenine nucleotide, and adenosine analogues was successfully achieved through photocatalysis or thermal activation. Despite the challenges posed by the presence of two potential reactive sites (C² and C⁸) in the purine motif, the unique nucleophilic amine-ligated boryl radicals effortlessly achieved excellent C² site selectivity and simultaneously avoided the formation of multifunctionalized products. This protocol proved effective for the late-stage borylation of some important biomolecules as well as a few antiviral and antitumor drug molecules, such as AMP, cAMP, Vidarabine, Cordycepin, Tenofovir, Adefovir, GS-441524, etc. Theoretical calculations shed light on the site selectivity, revealing that the free energy barriers for the C²-Minisci addition are further lowered through the chelation of additive Mg²⁺ to N³ and furyl oxygen. This phenomenon has been confirmed by an IGMH analysis. Preliminary antitumor evaluation, derivation of the C²-borylated adenosine to other analogues with high-value functionalities, along with the CuAAC click reactions, suggest the potential application of this methodology in drug molecular optimization studies and chemical biology.

100 Deals associated with Bucladesine Sodium

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External Link

KEGG	Wiki	ATC	Drug Bank
D01238	Bucladesine Sodium	C01CE04	DB13242

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Pressure Ulcer	JP	Nipro Pharma Corp.	19 Jan 1993
Skin Ulcer	JP	Nipro Pharma Corp.	19 Jan 1993
Ventricular Dysfunction	JP	Alfresa Pharma Corp.	24 Jul 1984

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ASGCT2004	Not Applicable	Mouth Neoplasms	-	Ganciclovir	vazychtvzd(ltkqhganxx) = qgwnjthonf utmxzditur (phhveudlpt )	-	01 May 2004
				Dibutyryl-cAMP	smldevpjnp(qrltoiqzno) = ytesvxvhdp krbzvqtsjl (gxayqylwgg )