Delving into the Latest Updates on Mepacrine hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

2-methoxy-6-chloro-9-diethylaminopentylaminoacridine, 3-chloro-7-methoxy-9-(1-methyl-4-diethylaminobutylamino)acridine, 6-chloro-9-((4-(diethylamino)-1-methylbutyl)amino)-2-methoxyacridine

+ [15]

Target

NF-κB x p53 x sPLA2

Action

inhibitors, modulators

Mechanism

NF-κB inhibitors(Nuclear factor NF-kappa-B complex inhibitors), p53 modulators(Tumor protein p53 modulators), sPLA2 inhibitors(Secretory phospholipase A2 inhibitors)

Therapeutic Areas

Immune System DiseasesInfectious DiseasesDigestive System Disorders+ [2]

Active Indication

GiardiasisLeishmaniasisMalaria+ [1]

Inactive Indication

Advanced Renal Cell CarcinomaCastration-Resistant Prostatic CancerCreutzfeldt-Jakob Disease, Sporadic+ [5]

Originator Organization

Bayer AG

Active Organization

Bayer AG

The Third Affiliated Hospital, Sun Yat-Sen University

Inactive Organization

Cleveland BioLabs, Inc.

Incuron LLC

National Cancer Institute

+ [1]

Drug Highest PhaseApproved

First Approval Date

(01 Jan 1932),

GiardiasisLeishmaniasisMalaria+ [1]

RegulationOrphan Drug (United States)

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Structure/Sequence

Molecular FormulaC23H36Cl3N3O3

InChIKeyRZFNKJVCPDLQQA-UHFFFAOYSA-N

CAS Registry6151-30-0

View All Structures (2)

Breast cancer, a leading cause of cancer-related mortality in women, is characterized by genomic instability and aberrant gene expression, often influenced by noncanonical nucleic acid structures such as G-quadruplexes (G4s). These structures, commonly found in the promoter regions and 5'-untranslated RNA sequences of several oncogenes, play crucial roles in regulating transcription and translation. Stabilizing these G4 structures offers a promising therapeutic strategy for targeting key oncogenic pathways. In this study, we employed a drug repurposing approach to identify FDA-approved drugs capable of binding and stabilizing G4s in breast cancer-related genes. Using ligand-based virtual screening and biophysical methods, we identified several promising compounds, such as azelastine, belotecan, and irinotecan, as effective G4 binders, with significant antiproliferative effects in breast cancer cell lines. Notably, belotecan and irinotecan exhibited a synergistic mechanism, combining G4 stabilization with their established topoisomerase I inhibition activity to enhance cytotoxicity in cancer cells. Our findings support the therapeutic potential of G4 stabilization in breast cancer, validate drug repurposing as an efficient strategy to identify G4-targeting drugs, and highlight how combining G4 stabilization with other established drug activities may improve anticancer efficacy.

01 Mar 2025·Life Sciences

Corrigendum on “Hepatoprotective and neuroprotective effects of quinacrine against bile duct ligation-induced hepatic encephalopathy in rats: Role of bone morphogenetic proteins signaling” [Life Sci. 359 (2024) 123229]

Author: El-Naga, Reem N ; Esmail, Manar M ; Azab, Samar S ; Michel, Haidy E ; Hanna, Diana M F ; Saeed, Noha M

05 Feb 2025·The American Journal of Tropical Medicine and Hygiene

Splenic Modulation of Plasmodium vivax Relapses and Hypnozoite Activation during the Second World War?

Article

Author: Shanks, G. Dennis

ABSTRACT.Despite their colonial experience with tropical medicine, Allied (United States, United Kingdom, Australia, and India) Armies in the Indo-Pacific region were surprised by the large number of Plasmodium vivax infections in their soldiers during the Second World War. Even after the institution of effective chemoprophylaxis with quinacrine, multiple cycles of clinical relapses often occurred when months of medication was discontinued. Nearly monthly symptomatic relapses (>10) were not unusual and resulted in important manpower losses after each campaign. Retrospective consideration suggests that small splenic size was associated with the risk of recurrent clinical episodes of vivax malaria. Potential non–mutually exclusive explanations for frequent relapses of vivax malaria in soldiers are reviewed. These include decreased retention of parasitized red blood cells by small spleens through greater filtration stringency preventing relapses from becoming clinically patent; small spleen size being a marker of lower innate and/or acquired immunity, modulating the risk of clinically patent recurrences; or small spleen size increasing the number of relapses through decreased removal of triggers of hypnozoite activation. Apparent splenic modulation of vivax malaria relapses suggests a complex interaction between the parasite and host that might be amenable to manipulation to facilitate malaria elimination.

100 Deals associated with Mepacrine hydrochloride

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External Link

KEGG	Wiki	ATC	Drug Bank
-	Mepacrine hydrochloride	P01AX05	DB01103

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Giardiasis	-	Bayer AG	01 Jan 1932
Leishmaniasis	-	Bayer AG	01 Jan 1932
Malaria	-	Bayer AG	01 Jan 1932
Systemic Lupus Erythematosus	-	Bayer AG	01 Jan 1932

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Advanced Renal Cell Carcinoma	Phase 2	United States	Cleveland BioLabs, Inc.	01 Nov 2007
Systemic Lupus Erythematosus	Preclinical	China	The Third Affiliated Hospital, Sun Yat-Sen University	25 Oct 2013
Castration-Resistant Prostatic Cancer	Preclinical	-	Cleveland BioLabs, Inc.	01 Dec 2006
Metastatic Prostate Carcinoma	Preclinical	-	Cleveland BioLabs, Inc.	01 Dec 2006
Prostatic Cancer	Preclinical	United States	Incuron LLC	16 Nov 2006
Creutzfeldt-Jakob Disease, Sporadic	Preclinical	United States	National Institute on Aging	01 Apr 2005
Liver Cancer	Preclinical	Russia	Incuron LLC	-
Malignant ascites	Preclinical	Russia	Incuron LLC	-
Non-Small Cell Lung Cancer	Preclinical	United States	National Cancer Institute	-

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT01844076 (CTgov)	Phase 1/2	Adenocarcinoma of large intestine \| Advanced Colorectal Adenocarcinoma	19	Quinacrine+Capecitabine (Phase I Level -2)	whrczdgmja(totupocszw) = ihfozrletw nxetauxshk (rjrvizjqvr, ujasubwtha - msmnxpgmbc) View more	-	25 Mar 2021
				Quinacrine+Capecitabine (Phase I Level -1)	whrczdgmja(totupocszw) = kyiexuulib nxetauxshk (rjrvizjqvr, tkhjtniwip - evlpakjxtq) View more
NCT01844076 (ASCO2019)	Phase 1	Metastatic colon cancer	10	Quinacrine plus Capecitabine	(vmynrxfvnc) = lzrhkhffmo kfcwkhtcto (crtrqsokay ) View more	-	26 May 2019
NCT00183092 (CTgov)	Phase 2	Creutzfeldt-Jakob Disease, Sporadic	69	Placebo (Placebo)	jmdhaetqae(bplhoaacco) = gcyexxjwjl qnshwekczy (eigpcduqon, nzzaznuttc - oowwddzbqb) View more	-	29 May 2014
				Quinacrine (Quinacrine)	jmdhaetqae(bplhoaacco) = ojcicukwwt qnshwekczy (eigpcduqon, dxlexrodbe - ynnvwhvejt) View more
AACR2013	Not Applicable	Glioma	-	Cediranib	jaiiqdvjeh(ditxaoxlkx) = Quin may also stimulate autophagic flux, consistent with its reported inhibition of PI3K/Akt/mTOR signaling aynotplkmc (aewgcauffm ) View more	-	15 Apr 2013
				Quinacrine
NCT00417274 (CTgov)	Phase 2	Castration-Resistant Prostatic Cancer \| Metastatic Prostate Carcinoma	31	Quinacrine	deevvpltfn(ekhaimrjrx) = epronshmti pqjznvmvdx (amtjfkkrhd, kcnzgcgbdx - tlxbhhlrma) View more	-	11 Apr 2013