Delving into the Latest Updates on Auranofin with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

(1-Thio-beta-D-glucopyranosato)(triethylphosphine)gold 2,3,4,6-tetraacetate, 2,3,4,6-Tetra-O-acetyl-1-thio-beta-D-glucopyranosato-S (triethylphosphine)gold, Auranofin (JP17/USAN/INN)

+ [7]

Target

IKK complex

Mechanism

IKK complex inhibitors(IκB kinase complex inhibitors)

Therapeutic Areas

Immune System DiseasesSkin and Musculoskeletal Diseases

Active Indication

Rheumatoid Arthritis

Inactive Indication-

Originator Organization

Sebela Ireland Ltd.

Active Organization

Sebela Ireland Ltd.

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

US (24 May 1985),

Rheumatoid Arthritis

RegulationOrphan Drug (US)

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Structure

Molecular FormulaC20H34AuO9PS

InChIKeyFHXOLDDEPGFZFF-XTZHGVARSA-N

CAS Registry34031-32-8

This is a phase IIa, randomized, placebo-controlled, single-blinded superiority treatment study in males and non-pregnant females, 18 to 65 years of age who are in good health. This study is designed to compare placebo to once daily doses of 6mg auranofin for adults with amebiasis or giardiasis. A sample size of 68 subjects enrolled with amebiasis (34 per arm) and 68 with giardiasis (34 per arm); Power based on 60 subjects with amebiasis and 60 with giardiasis completing the study.Eligible subjects will be randomly assigned to a treatment group with auranofin (6 mg orally once daily for 5 days for giardiasis or 7 days for amebiasis) compared to a placebo group receiving similar but not identical placebo capsules. Projected duration of subject participation will be approximately 30 days of face to face visits, including the pre-enrollment screening period of up to 4 days. It is anticipated that it will take approximately 3.5 years to finish the study. Primary objectives are: 1) to compare the proportion of subjects with stools positive by rapid Enzyme Immunoassay (EIA) and positive antigen detection EIA for E. histolytica at enrollment with resolution of diarrhea (less than 3 loose stools/24 hrs) by Day 7 for E. histolytica infections. 2) to compare the proportion of subjects with stools positive by rapid EIA and positive antigen detection EIA for Giardia at enrollment with resolution of diarrhea (less than 3 loose stools/24 hrs) by Day 5 for Giardia infections.

Start Date06 Nov 2016

Sponsor / Collaborator

National Institute of Allergy & Infectious Diseases

100 Clinical Results associated with Auranofin

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100 Translational Medicine associated with Auranofin

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100 Patents (Medical) associated with Auranofin

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1,381

Literatures (Medical) associated with Auranofin

01 Mar 2025·Biomaterials

Hypoxia-responsive micelles deprive cofactor of stearoyl-CoA desaturase-1 and sensitize ferroptotic ovarian cancer therapy

Article

Author: Luo, Jiajia ; Li, Xin ; Zhao, Ning ; Zhao, Yanjun ; Meng, Xuan ; Shang, Yaqi ; Lu, Xiaoying ; Wang, Zheng ; Lv, Xiaoying

Ferroptosis has been recognized as a promising therapeutic strategy for cancer due to its unique mechanism of action. However, the upregulation of stearoyl-CoA desaturase 1 (SCD1) in ovarian cancer leads to resistance to ferroptotic therapy. Zinc ion (Zn²⁺) serves as the cofactor of SCD1. It was hypothesized that selective deprivation of Zn²⁺ from SCD1 could sensitize ferroptotic ovarian cancer therapy. Here, we report a hypoxia-responsive polymer micelle for enhanced ferroptosis of ovarian cancer cells. A SCD1 inhibitor, PluriSIn 1 (Plu), and a ferroptosis inducer, Auranofin (Aur), were co-encapsulated in nitroimidazole-bearing micelles. Under the hypoxic tumor microenvironment, the conversion of nitroimidazole to aminoimidazole triggered the cargo release and induced the depletion of antioxidant molecules (e.g., glutathione, thioredoxin, and NADPH). Meanwhile, because of the strong coordination between aminoimidazole and Zn²⁺ compared to that of histidine and Zn²⁺, such conversion can deprive the metal cofactor of SCD1, hence sensitizing the action of Plu and Aur. The proof-of-concept was demonstrated in cell and animal models with minimal systemic toxicity. The current work integrates ferroptosis induction with SCD1 inhibition in a hypoxia-responsive vehicle, offering a promising strategy for addressing the ferroptosis resistance and opening novel avenues for managing the difficult-to-treat ovarian cancer.

01 Jan 2025·Journal of Inorganic Biochemistry

In the search for new gold metalloantibiotics: In vitro evaluation of Au(III) (C^S)-cyclometallated complexes

Article

Author: Rodríguez-Solla, Humberto ; Soto, Sara M ; Pérez-Ramos, Paula ; Gabasa, Yaiza ; Soto, Sara M. ; Soengas, Raquel G. ; Cornielle, Enmanuel ; Soengas, Raquel G

A series of (C^S)-cyclometallated Au(III) cationic complexes of general formula [Au(dppta)(dtc)]⁺, [Au(dppta)(azmtd)]⁺ and [Au(dppta)(azc)Cl]⁺ (dppta = N,N-diisopropyl-P,P-diphenylphosphinothioic amide-κ²C,S; dtc = dithiocarbamate-κ²S,S'; azc = azolium-2-dithiocarboxylate-κ¹S; azmdt = azol(in)ium-2-(methoxy)methanedithiol-κ²S,S') were synthetized and tested against a panel of bacterial strains belonging to different Gram-positive and Gram-negative species of the ESKAPE group of pathogens. Among the tested compounds, complex 4c had the higher Therapeutic Index (TI) against multidrug resistant strains of S. aureus, S. epidermidis and A. baumannii, showing a more favourable cytotoxicity profile than the reference gold metalloantibiotic Auranofin. © 2024 xxxxxxxx. Hosting by Elsevier B.V. All rights reserved.

01 Dec 2024·International Journal for Parasitology: Drugs and Drug Resistance

Evaluating the amoeba thioredoxin reductase selenoprotein as potential drug target for treatment of Acanthamoeba infections

Article

Author: Andor, Attila ; Martín-Pérez, Tania ; Loufouma-Mbouaka, Alvie ; Leitsch, David ; Walochnik, Julia ; Arnér, Elias S J ; Pérez-Serrano, Jorge ; Arnér, Elias S.J. ; Loufouma Mbouaka, Alvie

The genus Acanthamoeba comprises facultative pathogens, causing Acanthamoeba keratitis (AK) and granulomatous amoebic encephalitis (GAE). In both diseases, treatment options are limited, and drug development is challenging. This study aimed to investigate the role of the large thioredoxin reductase selenoprotein of Acanthamoeba (AcTrxR-L) as a potential drug target assessing the effects of the thioredoxin reductase inhibitors auranofin, TRi-1, and TRi-2 on AcTrxR-L activity and on the viability of Acanthamoeba trophozoites. Recombinant expression and purification of AcTrxR-L as a selenoprotein allowed assessments of its enzymatic activity, with reduction of various substrates, including different thioredoxin isoforms. Auranofin demonstrated potent inhibition towards AcTrxR-L, followed by TRi-1, and TRi-2 exhibiting lower effectiveness. The inhibitors showed variable activity against trophozoites in culture, with TRi-1 and TRi-2 resulting in strongly impaired trophozoite viability. Cytotoxicity tests with human corneal epithelial cells revealed lower susceptibility to all compounds compared to Acanthamoeba trophozoites, underscoring their potential as future amoebicidal agents. Altogether, this study highlights the druggability of AcTrxR-L and suggests it to be a promising drug target for the treatment of Acanthamoeba infections. Further research is warranted to elucidate the role of AcTrxR-L in Acanthamoeba pathogenesis and to develop effective therapeutic strategies targeting this redox enzyme.

100 Deals associated with Auranofin

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External Link

KEGG	Wiki	ATC	Drug Bank
D00237	Auranofin	M01CB03	DB00995

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Rheumatoid Arthritis	US	Sebela Ireland Ltd.	24 May 1985

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02736968 (CTgov)	Phase 2	Dysentery, Amebic \| Giardiasis	93	auranofin (Symptomatic Giardia- Auranofin)	ibkpkkcozz(yufflslmnm) = owmlycmkaa xyzckrajtp (jtnvgzbtta, rasjmohwkb - hnfgynibtq) View more	-	26 Jan 2023
				placebo (Symptomatic Giardia- Placebo)	ibkpkkcozz(yufflslmnm) = vfxsyvkwcw xyzckrajtp (jtnvgzbtta, dusddfvjqw - agtvnvbmyn) View more
NCT03456700 (CTgov)	Phase 2	Ovarian Serous Tumor \| Recurrent ovarian cancer	22	Laboratory Biomarker Analysis+Sirolimus+Auranofin	jiugtszhge(nlwetvrcnh) = jclfttvcnd jmrxotorqa (bskfmjxppc, vscbaiwwoj - gubjmqfhmd) View more	-	02 Jul 2020
NCT02961829 (Pubmed \| J Microbiol Immunol Infect) Manual	Not Applicable	HIV Infections	30	Antiretroviral therapy +auranofin	(vermtfqjkm) = No major adverse events were detected ynyabxisyv (cdnbqpbllu )	Positive	01 Nov 2019
				Antiretroviral therapy +dolutegravir+maraviroc
NCT02063698 (CTgov)	Phase 2	Pain \| Pain Disorder	30	questionnaire administration+auranofin (Arm I (Auranofin))	mshpofgkwn(nypohsjsdg): P-Value = 1.0; P-Value = 0.45; P-Value = 0.38; P-Value = 0.12; P-Value = 0.70; P-Value = 1.0; P-Value = 0.44 View more	-	23 Apr 2019
				placebo (Arm II (Placebo))
AACR2017	Not Applicable	Breast Cancer	-	Mesupron	fuhgatdvsv(bsuejetlns) = combined mesupron and auranofin treatment significantly suppressed mitochondrial antiapoptotic proteins including Bcl-2 and Bcl-xL qdapchetbu (mfdwwjtrce ) View more	Positive	01 Jul 2017
				Auranofin
NCT02089048 (Pubmed \| Antimicrob Agents Chemother)	Phase 1	Amebiasis	15	Auranofin 6 mg	(lhwobwqxhu) = Treatment-associated adverse events were reported by 47% of the subjects, but all were mild and resolved without treatment udcvgoijna (jaahazmkfw )	-	01 Jan 2017
ASCO2012	Not Applicable	Chronic Lymphocytic Leukemia	-	Auranofin	dsbjeszhsd(ecaatbjxhw) = cqhqgkjamp wloxsewmlt (rbkhnccwla ) View more	-	20 May 2012