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]

License Organization

Incuron LLC

Cleveland BioLabs, Inc.

Drug Highest PhaseApproved

First Approval Date

(01 Jan 1932),

GiardiasisLeishmaniasisMalaria+ [1]

RegulationOrphan Drug (United States)

Login to view timeline

Structure/Sequence

Molecular FormulaC23H36Cl3N3O3

InChIKeyRZFNKJVCPDLQQA-UHFFFAOYSA-N

CAS Registry6151-30-0

View All Structures (2)

INTRODUCTIONGynecologic cancers, in order of prevalence, include uterine, ovarian, cervical, vaginal, and vulvar cancers. In 2024, there will be more than 116,000 new cases of gynecologic cancers and 33,800 disease-related deaths. Therefore, a concerted effort has been made to better understand the underlying pathophysiological processes and identify novel theranostic approaches.PURPOSEComprehensively examine the current peer-reviewed literature surrounding Nectin-4 and its implication in the identification and treatment of gynecologic cancers.METHODSPubMed and Google search with relevant keywords for articles published in the last 15 years.RESULTSNectin-4 as a cell adhesion molecule (CAM) promotes cell growth through intra-tumoral angiogenesis, strengthens cell-cell bonds, and creates a tight spheroid structure, which is more chemotherapy resistant. In high-grade serous ovarian cancer (HGSOC), Nectin-4 is strongly associated with the presence of peritoneal metastases and worse prognoses. When compared to CA-125, a common tumor marker for ovarian cancer, Nectin-4 showed higher specificity and sensitivity for predictive value of tumorigenesis. Regarding cervical cancer, inhibition of Nectin-4 by nanoformulated Quinacrine inhibits both cancer stem cell proliferation and DNA damage. Nectin-4 as a tumor marker can discriminate endometrial cancer from healthy adjacent tissue with a specificity of 95.4 % and sensitivity of 82.81 %. Lastly, there is scarce evidence of Nectin-4 and fallopian tube, vaginal, or vulvar cancer but given ovarian cancer cells may originate from the fallopian tube, there is plausibility of using Nectin-4 to detect fallopian and/or ovarian cancer earlier.CONCLUSIONOverall, Nectin-4 as a promoter of cancer cell growth and metastasis supports the emphasis in current peer-reviewed literature as an effective theranostic biomarker.

01 Apr 2025·Cellular Oncology

Retraction Note: TRAIL enhances quinacrine-mediated apoptosis in breast cancer cells through induction of autophagy via modulation of p21 and DR5 interactions

Article

Author: Nayak, Deepika ; Das, Sarita ; Narayan, Satya ; Siddharth, Sumit ; Nayak, Anmada ; Kundu, Chanakya Nath

01 Mar 2025·European Journal of Medicinal Chemistry

Repurposing FDA-approved drugs to target G-quadruplexes in breast cancer

Article

Author: Marzano, Simona ; Randazzo, Antonio ; Landolfi, Laura ; Catalanotti, Bruno ; Malfitano, Anna Maria ; Pagano, Bruno ; Moraca, Federica ; Castellano, Giuliano ; Napolitano, Fabiana ; Arciuolo, Valentina ; Di Porzio, Anna ; D'Aria, Federica ; Amato, Jussara

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.

100 Deals associated with Mepacrine hydrochloride

Login to view more data

External Link

KEGG	Wiki	ATC	Drug Bank
-	Mepacrine hydrochloride	P01AX05	DB01103

R&D Status

Approved

10 top approved records.

Login

to view more data

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.

Login

to view more data

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	Discovery	-	Cleveland BioLabs, Inc.	01 Dec 2006
Metastatic Prostate Carcinoma	Discovery	-	Cleveland BioLabs, Inc.	01 Dec 2006
Prostatic Cancer	Discovery	United States	Incuron LLC	16 Nov 2006
Creutzfeldt-Jakob Disease, Sporadic	Discovery	United States	National Institute on Aging	01 Apr 2005
Liver Cancer	Discovery	Russia	Incuron LLC	-
Malignant ascites	Discovery	Russia	Incuron LLC	-
Non-Small Cell Lung Cancer	Discovery	United States	National Cancer Institute	-

Login to view more data

Clinical Result

Indication

Phase

Evaluation

View All Results

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)	fdkesumrgp(wisqhtofsr) = rcywxjwhtg yzjeialrbw (fjxabhcgzy, bpotfqqhpv - kvwejghzan) View more	-	25 Mar 2021
				Quinacrine+Capecitabine (Phase I Level -1)	fdkesumrgp(wisqhtofsr) = orlqdszceg yzjeialrbw (fjxabhcgzy, wfsvzqcdcc - qutgadnaak) View more
NCT01844076 (ASCO2019)	Phase 1	Metastatic colon cancer	10	Quinacrine plus Capecitabine	(wyjrmvlmlb) = mkbgzbzcnd mukmwnuwsn (pvrxhrlnvu ) View more	-	26 May 2019
NCT00183092 (CTgov)	Phase 2	Creutzfeldt-Jakob Disease, Sporadic	69	Placebo (Placebo)	ktrvmrrhsn(xcjhvrngdo) = baiggdeqiq zpurmfcjma (fxpzxonlde, ddyhxhckcr - sxiwvlbbez) View more	-	29 May 2014
				Quinacrine (Quinacrine)	ktrvmrrhsn(xcjhvrngdo) = uhucvdnwjf zpurmfcjma (fxpzxonlde, unkgvucgre - cpapmtdczq) View more
AACR2013	Not Applicable	Glioma	-	Cediranib	jtllrrcvxa(lijzzuydah) = Quin may also stimulate autophagic flux, consistent with its reported inhibition of PI3K/Akt/mTOR signaling qtvhcgdlvd (pfcohoeldc ) View more	-	15 Apr 2013
				Quinacrine
NCT00417274 (CTgov)	Phase 2	Castration-Resistant Prostatic Cancer \| Metastatic Prostate Carcinoma	31	Quinacrine	yidnaucqdz(aknfdzpecz) = jmrneqhlkw yellbtrtwh (gxobggerlp, rnkrcvjqif - pdgmkibmbb) View more	-	11 Apr 2013