Delving into the Latest Updates on Meglumine Antimoniate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Glucantim, Meglumine antimonate

+ [1]

Target-

Mechanism-

Therapeutic Areas

Infectious DiseasesSkin and Musculoskeletal DiseasesOther Diseases

Active Indication

Leishmaniasis

Inactive Indication-

Originator Organization

Sanofi

Active Organization

Sanofi

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC7H18NO8Sb

InChIKeyJLGCKKAHTCRITP-SESJOKTNSA-O

CAS Registry133-51-7

View All Structures (2)

This study aims to identify the most sensitive colorimetric test for assessing intracellular drug susceptibility of Leishmania tropica to conventional antileishmanial drugs. To this end, the efficacy of four colorimetric methods-MTT, XTT, MTS, and WST-8-was compared using reference L. tropica promastigotes. The intracellular drug susceptibility was further evaluated using the test with the widest absorbance range on isolates from Türkiye CL patients: two responsive to a single course of meglumine antimoniate (MA) and two that showed no clinical improvement after two treatments. CL isolates were identified via real-time PCR targeting the ITS1 region. Promastigote suspensions at standardized densities (0.08 × 10⁶ to 10 × 10⁶ promastigotes/well) were prepared in both RPMI (phenol red-containing) and RPMIØRP (phenol red-free) media, then analyzed with ELISA-based MTT, XTT, MTS, and WST-8 to identify the method with the broadest specific absorbance range. Intracellular drug susceptibility of CL isolates was subsequently assessed in a macrophage/amastigote model by infecting THP-1 macrophages with promastigotes from both reference and patient isolates, followed by treatment with MA, sodium stibogluconate (SSG), miltefosine (MTF), pentamidine (PMD), and amphotericin B (AmB). Promastigotes obtained from parasite rescue and transformation assays were analyzed using the most sensitive colorimetric method to determine IC₅₀ values. Species identification confirmed all four CL isolates as L. tropica, and the XTT assay provided the widest absorbance range in RPMIØRP media. IC₅₀ values for both treatment-responsive and unresponsive isolates were similar to those of the reference isolate, showing susceptibility to all tested drugs without statistically significant differences. Expanding the isolate set is necessary to further evaluate the predictive value of Sb^V (pentavalent antimonials) susceptibility for treatment outcomes. The identification of XTT as the most sensitive method for intracellular antileishmanial susceptibility testing is expected to aid in standardizing laboratory models and provide valuable insights for researchers and clinicians managing treatment-unresponsive CL cases.

01 Feb 2025·Molecular and Biochemical Parasitology

Glucantime and quercetin electrospun nanofiber membranes: Fabrication and their evaluation as dressing for cutaneous leishmaniasis

Article

Author: Alemzadeh, Effat ; Abdollahpour-Alitappeh, Meghdad ; Mahi-Birjand, Motahareh ; Karamian, Mehdi ; Alemzadeh, Esmat ; Eshaghi, Soudabeh ; Abedi, Ali

Cutaneous leishmaniasis is considered as one of the most concerns of the World Health Organization (WHO). The main objective of this study was to use polycaprolactone (PCL) nanofiber scaffolds in order to provide a topical drug delivery system capable of delivering glucantime (glu) and quercetin (qur) to cutaneous leishmaniasis wounds. First, PCL/glu/qur, PCL/glu, and PCL/qur nanofibers were prepared by an electrospinning method followed by characterization through scanning electron microscopy (SEM) and fourier transform infrared spectroscopy (FTIR). Subsequently, we investigated the release of the drugs from nano-scaffolds and anti-promastigote effects. Lastly, the effect of nanobandage was evaluated on 20 female inbred BALB/c mice infected with the parasite. The nanofibers were bead-free and uniform with an average diameter of 224 ± 25 nm and showed a sustained release. Results from in vivo experiments showed that the number of amastigotes and macrophages infected with the parasite and the infiltration of inflammatory cells in mice treated with PCL/qur and PCL/glu/qur nanofibers significantly decreased as compared with those treated with the PCL/glu and PCL nanofibers. Collectively, PCL/glu/qur and PCL/qur nanofibers have promising therapeutic effects in cutaneous leishmaniasis wound healing.

04 Dec 2024·The American Journal of Tropical Medicine and Hygiene

Effectiveness of Antileishmanial Treatments in Three Endemic Areas of Colombia: A Community-Based Cohort Study

Article

Author: Castillo, Ruth Mabel ; Gutiérrez, Yeison ; Castaño Grajales, Patricia ; Alexander, Neal ; Del Castillo, Alejandra María ; Cossio, Alexandra ; Castro, María del Mar

ABSTRACT.The effectiveness of treatment of cutaneous leishmaniasis (CL) in rural settings remains underexplored. This study assessed the effectiveness of standard antileishmanial treatments using a community-based approach supported by mobile health (mHealth) in three rural areas of Colombia. From January 2018 to September 2021, we assessed treatment outcomes, adherence, and adverse drug reactions in CL patients, with the support of the Guaral+ST app. Treatment decisions were made by providers at health facilities at each site in accordance with national guidelines, whereas treatment follow-up and presumptive case identification were made by trained community leaders and health agents at the community level. In total, 231 participants received antileishmanial treatment (63 received miltefosine, 110 meglumine antimoniate, and 58 pentamidine). Disease presentation was mild (median number of lesions = 1, interquartile range [IQR]: 1–2) and of short duration (1.5 months, IQR: 1–3). The strategy yielded information on the therapeutic outcomes in 81% of study participants. Effectiveness, measured as the proportion of cure at 90 to 180 days, was 86.3% (95% CI: 73.3–93.48) for miltefosine; 77.6% (67.5–85.3) for meglumine antimoniate, and 73.1% (59.0–83.6) for pentamidine. The effectiveness of pentamidine in children ≤10 years old was 79.4% (61.6–90.3). This is one of the few reports of effectiveness of pentamidine in children with prospective data collection in the Americas. Adverse drug reactions occurred in 32% of patients, most frequently with meglumine antimoniate. Our findings demonstrate that standard antileishmanial treatments are effective in rural areas where the disease is endemic and that mHealth has a pivotal role in improving patient follow-up and data collection on therapeutic outcomes.

100 Deals associated with Meglumine Antimoniate

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External Link

KEGG	Wiki	ATC	Drug Bank
-	Meglumine Antimoniate	P01CB01	DB13732

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Leishmaniasis	-	Sanofi	-

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


WCD2023	Not Applicable	Leishmaniasis, Cutaneous	32	Sbv + G-CSF	afcdoitkvn(idlmysbenu) = blaqhzbong pxafndycmk (mknpveotzc )	Positive	03 Jul 2023
				Sbv + Placebo	afcdoitkvn(idlmysbenu) = bvjgykblfh pxafndycmk (mknpveotzc )
NCT03023111 (Pubmed \| Int J Infect Dis)	Phase 3	Leishmaniasis, Cutaneous	150	Topical GM-CSF + Miltefosine	oqwthktnep(lufzzxobqi) = One patient (group MA) stopped treatment after presenting with fever, exanthema, and severe arthralgia qaxpkeozbi (snklbanqtp ) View more	-	01 Feb 2021
				Placebo + Miltefosine
NCT01462500 \| NCT00487253 \| NCT01464242 (Pubmed \| PLoS Negl Trop Dis)	Not Applicable	Leishmaniasis, Cutaneous	-	miltefosine	sctwqviiim(jtqttkqjxf) = qltmbmdgfr vwqhcaqkbn (vjakakiird, 3.59 - 14.26)	-	01 Apr 2017
				meglumine antimoniate	sctwqviiim(jtqttkqjxf) = getizgjqnp vwqhcaqkbn (vjakakiird, 14.48 - 29.58)
NCT00487253 (Pubmed \| J Infect Dis)	Phase 3	Leishmaniasis, Cutaneous	116	Miltefosine	(qwuihuebok) = yavrbvyklj qesrzbohgw (bnnfyzlgfg, 5.7% - 28.7%)	Positive	15 Feb 2012
				Meglumine antimoniate	(qwuihuebok) = mqayuttngt qesrzbohgw (bnnfyzlgfg, 16.9% - 45.2%)