Delving into the Latest Updates on Pimagedine with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Aminate base, Aminoguanidine, Aminoguanidine hydrochloride

+ [9]

Target

AGE

Mechanism

AGE inhibitors(renin binding protein inhibitors)

Therapeutic Areas

Cardiovascular DiseasesEndocrinology and Metabolic DiseaseEye Diseases+ [2]

Active Indication-

Inactive Indication

Coronary DiseaseDiabetes ComplicationsDiabetic Nephropathies+ [2]

Originator Organization

Astellas Pharma, Inc.

Active Organization-

Inactive Organization

Synvista Therapeutics, Inc.

Astellas Pharma, Inc.Gamida SA

Drug Highest PhaseDiscontinuedPhase 3

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaCH6N4

InChIKeyHAMNKKUPIHEESI-UHFFFAOYSA-N

CAS Registry79-17-4

Diabetic retinopathy is the leading cause of blindness in the developed world. The causes of the disease are poorly understood. One of the earliest changes that occur in the retinas of diabetic patients, well before overt retinopathy is observed, is a reduction in light-evoked increases in blood flow in retinal vessels. The loss of this vascular response may lead to retinal hypoxia and it has been suggested that hypoxia could be a principal cause of diabetic retinopathy.
The long-term goals of this project are to determine whether decreased blood flow in diabetic patients and the resulting retinal hypoxia contributes to the development of diabetic retinopathy and whether restoration of normal blood flow in diabetic patients slows or prevents the development of retinopathy.

Start Date01 Jul 2016

Sponsor / Collaborator

University of Minnesota

NCT00184990

/ CompletedPhase 1IIT

Effect of Selective iNOS Inhibition During Human Endotoxemia

Sepsis or endotoxemia is manifested by hypotension, resistance to vasopressors, myocardial depression,and altered organ blood flow distribution. The mechanisms underlying the cardiovascular dysfunction during sepsis are complex; however, they are partially mediated by an uncontrolled production of NO by inducible NO synthase (iNOS).Control subjects received 2 ng/kg E. coli endotoxin, whereas the active intervention group received endotoxin in the presence of selective iNOS-inhibitor aminoguanidine. Hemodynamics, vascular responses to norepinephrine, acetylcholine and sodium nitroprusside, as well as circulating cytokines and other mediators of inflammation were measured. We tested the hypothesis that inhibition of NO-synthesis prevented the LPS-mediated insensitivity to noradrenalin and endothelial-dependent vasorelaxation. Furthermore, we tested whether NO participates in occurrence of the endotoxin tolerance in humans by using the iNOS inhibitor aminoguanidine on healthy volunteers with endotoxemia. At 0; 2 and 4 hours after the LPS challenge whole blood was stimulated with five TLR agonists in vitro and pro- and anti-inflammatory cytokines were measured.

Start Date01 Jan 2005

Sponsor / Collaborator

Radboud University Medical Center

NCT00180635

/ CompletedNot ApplicableIIT

A Double Blind, Crossover Placebo-controlled Study to Evaluate the Effect of L-arginine and Aminoguanidine on Bronchial and Alveolar Nitric Oxide and Nitric Oxide Metabolites

The primary aim of this study is to investigate the effects of oral and inhaled administration of L-arginine and of inhaled aminoguanidine on bronchial and alveolar exhaled NO and NO metabolites in exhaled breath condensate, induced sputum, nasal lavage and mouth wash fluid in healthy non-smokers, current smokers and patients with COPD.

Start Date01 Oct 2003

Sponsor / Collaborator

Imperial College London

100 Clinical Results associated with Pimagedine

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100 Translational Medicine associated with Pimagedine

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100 Patents (Medical) associated with Pimagedine

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4,669

Literatures (Medical) associated with Pimagedine

01 Feb 2025·JOURNAL OF HAZARDOUS MATERIALS

Naked-eye and fluorescence resonance energy transfer based ratiometric fluorescent probe for rapid, sensitive and selective detection of hydrazine and its applications in imaging of environmental samples and living systems

Article

Author: Sai, Zhipeng ; Li, Zhiyuan ; Yang, Zhijun ; Pei, Feng ; Ni, Tianjun ; Zhang, Pengcheng ; Chang, Kaiwen ; Ge, Chunpo ; Wang, Xiaoyu

Hydrazine, a compound recognized for its carcinogenic and genotoxic properties, presents a significant threat to human health via environmental exposure and drug metabolism. The detection of hydrazine is essential for safeguarding human health. However, a tool capable of accurately detecting hydrazine across diverse sample types, such as soil, water sources, and plant specimens contaminated by hydrazine leakage, as well as cells and live mice containing endogenously generated hydrazine from drug metabolism, is still lacking. In this study, we have designed and synthesized a ratiometric fluorescent probe utilizing the fluorescence resonance energy transfer mechanism. Upon exposure to hydrazine, the probe exhibits an increased fluorescence ratio (F_485 nm/F_650 nm) accompanied by a color change from orange to light blue-green. The fluorescence sensing mechanism has been validated through high resolution mass spectrometer and density functional theory. This probe demonstrates significant potential for practical applications in detecting hydrazine within water and soil samples, as well as for imaging exogenous and drug-metabolized endogenous hydrazine in cellular and murine models.

01 Feb 2025·BIORESOURCE TECHNOLOGY

Hydrazine promoted nitrite reduction in partial-denitrification by enhancing organic-substrate uptake and electron transport

Article

Author: Dai, Ben ; He, Junxia ; Wang, Zhenyu ; Zhou, Jingzhou ; Rittmann, Bruce E ; Wang, Zuobin ; Xia, Siqing ; Yang, Yifeng

Partial denitrification coupled with anammox is a promising approach for sustainable nitrogen removal from wastewater. However, this coupling can be influenced by hydrazine (N₂H₄) released by anammox bacteria. This study aimed to reveal how N₂H₄ regulates partial denitrification. Short-term batch experiments showed that 0.5 to 10 mg N/L of N₂H₄ promoted nitrite (NO₂^-) accumulation, likely by inhibiting the electron transfer from cyt c to nitrite reductase. However, long-term exposure to N₂H₄ (0.5 and 1 mg N/L) shifted the microbial community and increased NO₂^- reduction. This exposure enriched the genera OLB8, Thauera, and f_Rhodocyclaceae, and increased the abundance of genes involved in EPS formation, substrate transport and electron transport. The long-term outcome was more NO₂^- reduction to N₂ and more substrate (COD) oxidation. While N₂H₄ benefits NO₂^- accumulation in short-term, the mechanism is not sustainable, highlighting the importance of minimizing N₂H₄ release for successful in such coupled nitrogen removal systems.

01 Feb 2025·BIORESOURCE TECHNOLOGY

Revealing the combined effect of hydroxylamine and hydrazine on nitrogen removal performance of completely autotrophic nitrogen removal over nitrite (CANON) process

Article

Author: Zhang, Qian-Qian ; Zhou, Jia-Min ; Wang, Ying ; Sun, Ying-Jun ; Ma, Xin ; Jin, Ren-Cun ; Chen, Ying ; Zhang, Xin-Rui ; Liu, Xin-Tao

This study explored capabilities of completely autotrophic nitrogen removal over nitrite (CANON) process under co-regulation of hydroxylamine (NH₂OH) and hydrazine (N₂H₄). Results indicated that granular (R₁) and flocculated (R₂) sludge CANON systems were started-up respectively on day 14 and day 17 by co-introduction of 0.50 + 1.00 mg/L and 1.00 + 5.00 mg/L NH₂OH and N₂H₄, with ammonia removal efficiency (ARE) of 53.75 % ± 8.30 % and 54.17 % ± 7.40 %, respectively. Furthermore, the relative abundance of Nitrosomonas, Nitrospira, Candidatus_Nitrotoga and Nitrobacter reduced after NH₂OH and N₂H₄ was supplied into R₁ and R₂ for 30 days, thereby inhibiting ammonia-oxidizing bacteria (AOB) and nitrite-oxidizing bacteria (NOB) activity. Nevertheless, the relative abundance of Candidatus_Kuenenia and Candidatus_Jettenia recovered once NH₂OH and N₂H₄ were absent, produced reversible inhibitory on anaerobic ammonia-oxidation bacteria (AnAOB) activity. Results will demystify the nitrogen elimination performance and mechanism of the CANON process from a novel viewpoint.

100 Deals associated with Pimagedine

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External Link

KEGG	Wiki	ATC	Drug Bank
D05479	Pimagedine	-	DB05383

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Diabetic Nephropathies	Phase 3	US	-	-
Diabetic Nephropathies	Phase 3	CA	-	-
Diabetic Nephropathies	Phase 3	-	Astellas Pharma, Inc.	-
Diabetic Nephropathies	Phase 3	-	Synvista Therapeutics, Inc.	-
Diabetic Retinopathy	Phase 3	-	Astellas Pharma, Inc.	-
Diabetic Retinopathy	Phase 3	-	Synvista Therapeutics, Inc.	-
Diabetes Complications	Phase 2	IL	Gamida SA	-
Coronary Disease	Preclinical	US	-	-
Graft Rejection	Preclinical	US	-	-

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


SFN2001	Not Applicable	-	-	Aminoguanidine	zlroiaxndr(ixbqyvangh) = zqykdpcogz kgznewxzpl (lluapxibwz, 3)	-	14 Nov 2001
				L-NAME	zlroiaxndr(ixbqyvangh) = dqqeqpplnx kgznewxzpl (lluapxibwz, 7)