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)

+ [18]

Target

cGMP-PDE

Mechanism

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

Therapeutic Areas

Cardiovascular DiseasesSkin and Musculoskeletal Diseases

Active Indication

Pressure 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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5,999

Literatures (Medical) associated with Bucladesine Sodium

01 Jan 2025·Molecular and Cellular Endocrinology

FSH increases lipid droplet content by regulating the expression of genes related to lipid storage in Rat Sertoli cells

Article

Author: Riera, Maria Fernanda ; Meroni, Silvina Beatriz ; Centola, Cecilia Lucia ; Dasso, Marina Ercilia ; Galardo, Maria Noel

Sertoli cells (SCs) are essential for appropriate spermatogenesis. From a metabolic standpoint, they catabolize glucose and provide germ cells with lactate, which is their main energy source. SCs also oxidize fatty acids (FAs), which are stored as triacylglycerides (TAGs) within lipid droplets (LDs), to fulfill their own energy requirements. On the other hand, it has been demonstrated that FSH regulates some of SCs functions, but little is known about its effect on lipid metabolism. In the present study, we aimed to analyze FSH-mediated regulation of (1) lipid storage in LDs and (2) the expression of genes involved in FAs activation and TAG synthesis and storage in SCs. SCs obtained from 20-day-old rats were cultured for different incubation periods with FSH (100 ng/ml). It was observed that FSH increased LD content and TAG levels in SCs. There were also increments in the expression of Plin1, Fabp5, Acsl1, Acsl4, Gpat3, and Dgat1, which suggests that these proteins may mediate the increase in TAGs and LDs elicited by FSH. Regarding the signaling involved in FSH actions, it was observed that dbcAMP increased LD, and H89, a PKA inhibitor, inhibited FSH stimulus. Also, dbcAMP increased Plin2, Fabp5, Acsl1, Acsl4, and Dgat1 mRNA levels, confirming a role of the cAMP/PKA pathway in the regulation of lipid storage in SCs. Altogether, these results suggest that FSH, via the cAMP/PKA pathway, regulates lipid storage in SCs ensuring the availability of substrates to satisfy their energy requirements.

01 Dec 2024·Biotechnology Letters

Enhanced hypoxanthine utilization for cAMP salvage synthesis efficiently by Arthrobacter sp. CCTCC 2013431 via xanthine oxidase inhibition

Article

Author: Li, Chang ; Zhang, Zhonghua ; Li, Zhigang ; Tan, Hai ; Chen, Baofeng ; Li, Linbo

When hypoxanthine was utilized as the activator for the salvage pathway in cAMP synthesis, xanthine oxidase would generate in quantity leading to low hypoxanthine conversion ratios and cell viability. To enhance cAMP salvage synthesis, fermentations with citrate/luteolin and hypoxanthine coupling added were conducted in a 7 L bioreactor and then multiple physiological indicators of fermentation with luteolin addition were assayed. Due to hypoxanthine feeding, cAMP productivity reached 0.066 g/(L·h) with 43.5% higher than control, however, cAMP synthesis, cell growth and glucose uptake all ceased at 50 h which was shortened by 22 h in comparison to control. The addition of citrate resulted in the cessation of fermentation at 61 h, on the contrary, owing to luteolin addition, cAMP fermentation performance was enhanced significantly during the whole fermentation period (72 h) with higher hypoxanthine conversion ratios and cAMP contents when compared with citrate and only hypoxanthine added batches. Multiple physiological indicators revealed that luteolin inhibited xanthine oxidase activity reducing hypoxanthine decomposition and ROS generation. ATP/AMP, NADH/NAD⁺ and NADPH/NADP⁺ were significantly increased especially at the late phase. Moreover, HPRT, PUP expression contents and corresponding gene transcription levels were also elevated. Luteolin could inhibit xanthine oxidase activity and further decrease hypoxanthine decomposition and ROS generation leading to higher hypoxanthine conversion and less cell damage for cAMP salvage synthesis efficiently.

01 Dec 2024·Journal of Controlled Release

Tissue nano-transfection of antimicrobial genes drives bacterial biofilm killing in wounds and is potentially mediated by extracellular vesicles

Article

Author: Rincon-Benavides, Maria Angelica ; Vasquez-Martinez, Carlos A ; Kordowski, Mia ; Cuellar-Gaviria, Tatiana Z ; Nguyen, Kim Truc ; Halipci Topsakal, Hatice Nur ; Deng, Binbin ; Higuita-Castro, Natalia ; Reategui, Eduardo ; Rima, Xilal Y ; Wozniak, Daniel ; Jaramillo-Garrido, Shara ; Rana, Pranav S J B ; Gallego-Perez, Daniel ; Salazar-Puerta, Ana Isabel ; McComb, David W ; Dathathreya, Kavya ; Combita-Heredia, Orlando

The emergence of bacteria that are resistant to antibiotics is on track to become a major global health crisis. Therefore, there is an urgent need for new treatment options. Here, we studied the implementation of tissue-nanotransfection (TNT) to treat Staphylococcus aureus-infected wounds by delivering gene cargos that boost the levels of naturally produced antimicrobial peptides. The Cathelicidin Antimicrobial Peptide gene (CAMP), which produces the antimicrobial peptide LL-37, was used as model gene cargo. In vitro evaluation showed successful transfection and an increase in the transcription and translation of CAMP-coding plasmid in mouse primary epithelial cells. Moreover, we found that the extracellular vesicles (EVs) derived from the transfected cells (in vitro and in vivo) carried significantly higher concentrations of CAMP transcripts and LL-37 peptide compared to control EVs, possibly mediating the trafficking of the antimicrobial contents to other neighboring cells. The TNT platform was then used in vivo on an excisional wound model in mice to nanotransfect the CAMP-coding plasmid on the edge of infected wounds. After 4 days of daily treatment, we observed a significant decrease in the bacterial load in the CAMP-treated group compared to the sham group. Moreover, histological analysis and bacterial load quantification also revealed that TNT of CAMP on S. aureus-infected wounds was effective in treating biofilm progression by reducing the bacterial load. Lastly, we observed a significant increase in macrophage recruitment to the infected tissue, a robust increase in vascularization, as well as and an increased expression of IL10 and Fli1. Our results demonstrate that TNT-based delivery of gene cargos coding for antimicrobial compounds to the wound is a promising approach for combating biofilm infections in wounds.

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
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	ajbfvibyjn(hgsulclnov) = sziiolhqna tknbucsqyn (ttiuiwlwwh )	-	01 May 2004
				Dibutyryl-cAMP	hqpbeegeei(shfmdzhcnh) = zuptrynfbi rrkoajvhjr (zgygbjtfad )