Delving into the Latest Updates on NO-Ursodeoxycholic Acid with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

,no-udca, NO-ursodiol

+ [2]

Target

caspase 3 x caspase 8 x caspase 9

Mechanism

caspase 3 inhibitors(Caspase-3 inhibitors), caspase 8 inhibitors(Caspase-8 inhibitors), caspase 9 inhibitors(Caspase-9 inhibitors)

Therapeutic Areas

Digestive System Disorders

Active Indication-

Inactive Indication

Hypertension, Portal

Originator Organization

Nicox SA

Active Organization-

Inactive Organization

Nicox SAForest Laboratories, Inc.

Drug Highest PhaseDiscontinuedPhase 2

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC38H55NO10

InChIKeyWTAVOESJEWSDJC-DNVPPMEBSA-N

CAS Registry301828-26-2

This is an observational, retrospective cohort study of patients with primary biliary cholangitis (PBC) who failed ursodeoxycholic acid (UDCA) treatment, using a real-world data source, the Komodo Health United States (US) claims database. The study is designed to evaluate the effectiveness of obeticholic acid (OCA). All patients who meet diagnostic criteria for PBC in the database between 01 Jun 2015 and 31 Dec 2021 and who meet all eligibility criteria will be considered for this study.

Start Date28 Mar 2022

Sponsor / Collaborator

Intercept Pharmaceuticals, Inc.

[+2]

NCT03512821

/ CompletedPhase 1

A Single-dose, Comparative Bioavailability Study of Two Formulations of Ursodiol 500mg Tablets Under Fed Conditions

single-dose, comparative bioavailability study of two formulations of ursodiol 500mg tablets under fed conditions

Start Date01 Oct 2017

Sponsor / Collaborator

Daewoong Pharmaceutical Co., Ltd.

NCT03512808

/ CompletedPhase 1

A Single-dose, Comparative Bioavailability Study of Two Formulations of Ursodiol 500mg Tablets Under Fasting Conditions

A single-dose, comparative bioavailability study of two formulations of ursodiol 500mg tablets under fasting conditions

Start Date01 Jun 2017

Sponsor / Collaborator

Daewoong Pharmaceutical Co., Ltd.

100 Clinical Results associated with NO-Ursodeoxycholic Acid

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100 Translational Medicine associated with NO-Ursodeoxycholic Acid

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100 Patents (Medical) associated with NO-Ursodeoxycholic Acid

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20

Literatures (Medical) associated with NO-Ursodeoxycholic Acid

01 Jun 2024·Colloids and Surfaces B: Biointerfaces

Ursodeoxycholic acid loaded dual-modified graphene oxide nanocomposite alleviates cholestatic liver injury through inhibiting hepatocyte apoptosis

Article

Author: Liu, Jing ; Zhang, Mingman ; Li, Tao ; Lu, Binghui ; Yang, Zhangyou ; Yang, Xinrui ; Li, Rong ; Yang, Luxun ; Chen, Si ; Yin, Yaru ; Zhou, Wanyi

Ursodeoxycholic acid (UDCA) is the preferred treatment for various types of cholestasis, however, its effectiveness is limited because of its insolubility in water. We used polyethylene glycol (PEG) and cationic polymer polyethylenimine (PEI) to double-modify graphite oxide (PPG) as a drug delivery system. UDCA was successfully loaded onto PPG through intermolecular interactions to form UDCA-PPG nanoparticles. UDCA-PPG nanoparticles not only improve the solubility and dispersibility of UDCA, but also have good biocompatibility and stability, which significantly improve the delivery rate of UDCA. The results indicated that UDCA-PPG significantly reduced ROS levels, promoted cell proliferation, protected mitochondrial membrane potential, reduced DNA damage and reduced apoptosis in the DCA-induced cell model. In a mouse cholestasis model established by bile duct ligation (BDL), UDCA-PPG improved liver necrosis, fibrosis, and mitochondrial damage and reduced serum ALT and AST levels, which were superior to those in the UDCA-treated group. UDCA-PPG reduced the expression of the apoptosis-related proteins, Caspase-3 and Bax, increased the expression of Bcl-2, and reduced the expression of the oxidative stress-related proteins, NQO and HO-1, as well as the autophagy-related proteins LC3, p62 and p-p62. Therefore, UDCA-PPG can enhance the therapeutic effect of UDCA in cholestasis, by significantly improving drug dispersibility and stability, extending circulation time in vivo, promoting absorption, decreasing ROS levels, enhancing autophagy flow and inhibiting apoptosis via the Bcl-2/Bax signaling pathway.

25 Jan 2022·Gastroenterology Report

Co-administration of ursodeoxycholic acid with rosuvastatin/ezetimibe in a non-alcoholic fatty liver disease model

Article

Author: Lee, Da Hyun ; Seo, Sang Hyun ; Kim, Do Young ; Bae, Soo Han ; Cho, Kyung Joo ; Ahn, Sang Hoon ; Kim, Seung Up ; Park, Hye Jung ; Lee, Hye Won ; Kim, Beom Kyung ; Lee, Yu Seol ; Park, Jun Yong

AbstractBackgroundUrsodeoxycholic acid (UDCA), statins, and ezetimibe (EZE) have demonstrated beneficial effects against non-alcoholic fatty liver disease (NAFLD). We investigated the efficacy of the combination of UDCA and the mix of rosuvastatin (RSV)/EZE in the treatment of NAFLD.MethodsNAFLD mouse models were developed by injecting thioacetamide, fasting, and high-carbohydrate refeeding, high-fat diet, and choline-deficient L-amino acid-defined high-fat diet (CDAHFD). Low-dose UDCA (L-UDCA; 15 mg/kg) or high-dose UDCA (H-UDCA; 30 mg/kg) was administered with RSV/EZE. We also employed an in vitro model of NAFLD developed using palmitic acid-treated Hepa1c1c7 cells.ResultsCo-administration of RSV/EZE with UDCA significantly decreased the collagen accumulation, serum alanine aminotransferase (ALT) levels, and mRNA levels of fibrosis-related markers than those observed in the vehicle group in thioacetamide-treated mice (all P < 0.01). In addition, in the group fasted and refed with a high-carbohydrate diet, UDCA/RSV/EZE treatment decreased the number of apoptotic cells and serum ALT levels compared with those observed in the vehicle group (all P < 0.05). Subsequently, H-UDCA/RSV/EZE treatment decreased the number of ballooned hepatocytes and stearoyl-CoA desaturase 1 (SCD-1) mRNA levels (P = 0.027) in the liver of high-fat diet-fed mice compared with those observed in the vehicle group. In the CDAHFD-fed mouse model, UDCA/RSV/EZE significantly attenuated collagen accumulation and fibrosis-related markers compared to those observed in the vehicle group (all P < 0.05). In addition, UDCA/RSV/EZE treatment significantly restored cell survival and decreased the protein levels of apoptosis-related markers compared to RSV/EZE treatment in palmitic acid-treated Hepa1c1c7 cells (all P < 0.05).ConclusionCombination therapy involving UDCA and RSV/EZE may be a novel strategy for potent inhibition of NAFLD progression.

01 Sep 2019·Chemical and Pharmaceutical BulletinQ4 · MEDICINE

Preparation of Amorphous Composite Particles of Drugs with Ursodeoxycholic Acid as Preclinical Formulations

Q4 · MEDICINE

Article

Author: Yoshida, Miyabi ; Uchiyama, Hiromasa ; Yoshimoto, Aika ; Tozuka, Yuichi ; Tanida, Satoshi ; Kadota, Kazunori

We studied the possibility of using ursodeoxycholic acid (UDCA) as an excipient to create an amorphous composite that can be administered to animals in preclinical studies of experimental drugs. Three UDCA-based amorphous samples composed of nifedipine (NIF), indomethacin (IND), and naproxen (NAP) were found by screening. The UDCA-based formulations were adjudged amorphous by solid-state analysis using X-ray powder diffraction and differential scanning calorimetry. In addition, amorphous samples of NIF-UDCA, IND-UDCA, and NAP-UDCA did not crystallize while in 1% methyl cellulose (MC) solution for 120 min, although an amorphous solid dispersion of NIF-poly(vinylpyrrolidone) (PVP) crystallized rapidly. The low hygroscopicity of UDCA helps NIF maintain an amorphous state in 1% MC solution. The UDCA-based amorphous composites can be administered as suspended formulations to animals in preclinical studies.

100 Deals associated with NO-Ursodeoxycholic Acid

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External Link

KEGG	Wiki	ATC	Drug Bank
-	NO-Ursodeoxycholic Acid	-	DB16026

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Hypertension, Portal	Phase 2	ES	Forest Laboratories, Inc.	01 Nov 2005

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


PANURSO STUDY (UEGW2021)	Not Applicable	-	422	UDCA	rjweoocxrr(cgvfluihjj) = bxpvywcjyj jwsrveovan (wtrgcxjrtn, 660 - 790) View more	Positive	02 Oct 2021
				No UDCA	rjweoocxrr(cgvfluihjj) = wclgpzzkot jwsrveovan (wtrgcxjrtn, 525 - 664)
EHA2017	Not Applicable	Thrombotic Microangiopathies	671	Ursodeoxycholic acid	nwhuhtqmol(jpwvsykmmb) = fliwtxmzig ejdgnwowcg (ktfzlbiudr, 5.9 - 14.3)	-	18 May 2017
				Non-ursodeoxycholic acid	nwhuhtqmol(jpwvsykmmb) = zotliiddeb ejdgnwowcg (ktfzlbiudr, 11.7 - 18.1)