Delving into the Latest Updates on Diethylcarbamazine Citrate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Diethylcarbamazine, Diethylcarbamazine citrate (JP17/USP), RP-3799

+ [5]

Target

COX-1

Action

inhibitors

Mechanism

COX-1 inhibitors(Cyclooxygenase-1 inhibitors)

Therapeutic Areas

Infectious DiseasesOther Diseases

Active Indication

Filariasis

Inactive Indication

Elephantiasis, Filarial

Originator Organization

Lederle Laboratories

Active Organization

Mitsubishi Tanabe Pharma Corp.

Inactive Organization

Lederle LaboratoriesLederle Cyanamid Canada Inc

License Organization-

Drug Highest PhaseApproved

First Approval Date

United States (13 Nov 1950),

Elephantiasis, Filarial

Regulation-

Login to view timeline

Structure/Sequence

Molecular FormulaC16H29N3O8

InChIKeyPGNKBEARDDELNB-UHFFFAOYSA-N

CAS Registry1642-54-2

Lymphatic filariasis caused by Wuchereria bancrofti causes hydroceles and lymphedema in millions of individuals worldwide. Annual mass drug administration of ivermectin plus albendazole (IA) temporarily clears microfilariae from the blood of infected individuals and is used in Africa to reduce W bancrofti transmission. This study aimed to investigate whether moxidectin combination therapies are superior to ivermectin combination therapies for clearance of W bancrofti microfilaremia.

METHODS:

In this open-label, parallel assignment, masked-observer, randomised, superiority clinical trial in Côte d'Ivoire, we used gender-stratified, block randomisation to sequentially assign adults with bancroftian filariasis (1:1:1:1) to receive annual ivermectin plus albendazole (IA; standard of care) or one of three single-dose regimens: moxidectin plus albendazole (MoxA), ivermectin plus diethylcarbamazine (DEC) plus albendazole (IDA), or moxidectin plus DEC plus albendazole (MoxDA). This trial was conducted at the Filariasis Research Center in Agboville, located at the Centre Hôspitalier Regional, d'Agboville, Côte d'Ivoire. Men and non-pregnant, non-breastfeeding women aged 18-70 years in good general health and with screening microfilaria loads of at least 40 per mL (≥3 microfilariae on 60μL nocturnal thick blood smear) were eligible for enrolment; those found to have at least 40 microfilariae per mL by 1 mL blood filtration at enrolment were eligible for inclusion in the primary, modified intention-to-treat, efficacy analysis. Medicines were administered by an unmasked pharmacist; all other team members were masked to treatment assignment. Primary outcomes were complete microfilaria clearance at 12 months (MoxA vs IA) or 24 months (MoxDA vs IDA) post-treatment. This trial is registered at ClinicalTrials.gov (NCT04410406) and is complete.

FINDINGS:

Enrolment occurred from Aug 20, 2020 to July 31, 2021. 190 individuals were predicted to have nocturnal blood microfilariae counts of at least 40 microfilariae per mL, of whom 26 were excluded and 164 were randomly assigned to an intervention (41 to the IA group, 40 to the MoxA group, 41 to the IDA group, and 42 to the MoxDA group). 113 participants met the pre-specified efficacy analysis criteria and completed follow-up. The proportion of participants who were amicrofilaraemic at 12 months was eight of 25 (32% [95% CI 15-54]) among IA recipients versus 18 of 19 (95% [95% CI 74-100]) among MoxA recipients (adjusted risk ratio [RR] 2·79 [95% CI 1·59-4·90]; p=0·0004). The proportion of amicrofilaraemic participants at 24 months was 20 of 22 (91% [95% CI 71-99]) for IDA versus 21 of 23 (91% [72-99]) for MoxDA (adjusted RR 0·98 [95% CI 0·83-1·15]; p=0·78). Most MoxA recipients (14 of 16 [88%; 95% CI 62-98]) remained amicrofilaraemic at 24 months.

INTERPRETATION:

In this study, single-dose MoxA was superior to IA for W bancrofti microfilaria clearance at 12 months and provided prolonged microfilaria clearance for most participants. These results suggest that MoxA could be a powerful tool to accelerate the elimination of lymphatic filariasis in Africa.

FUNDING:

The Bill & Melinda Gates Foundation.

TRANSLATION:

For the French translation of the abstract see Supplementary Materials section.

01 Apr 2025·CURRENT TOPICS IN MEDICINAL CHEMISTRY

An Overview on Antifilarial Efficacy of Heterocyclic Motifs Encompassing Synthetic Strategies, SAR, and Commercialized Medications

Article

Author: Tahlan, Sumit ; Singh, Sucheta ; Pandey, Kailash C

Filariasis is one of the oldest, most dangerous, debilitating, disfiguring diseases and often ignores tropical disorders. It presents with a range of clinical symptoms, a low death rate, and a high morbidity rate, which contributes to social discrimination. This condition has major effects on people's socioeconomic circumstances. This illness is carried by mosquitoes that have spread malaria. Lymphatic filariasis, caused by Wuchereria bancrofti, Brugia malayi, and Brugia timori, is a crippling illness with serious social and economic consequences. The infection persisted despite therapy with conventional antifilarial medications such as diethylcarbamazine (DEC), albendazole, and ivermectin, which are mostly microfilaricides. Current treatments (ivermectin, diethylcarbamazine, and albendazole) have limited effectiveness against adult parasites and produce side effects; therefore, innovative antifilarial medications are urgently required. Hence, macrofilaricides, embryostatic agents, and improved microfilaricides are required. The following article discusses the typical synthetic methodologies established for antifilarial activity as well as their marketed pharmaceuticals, which will help researchers, medicinal chemists, and pharmaceutical scientists to develop new and effective antifilarial therapies. This review can help to identify new lead compounds and optimize existing commercial medications to improve their therapeutic efficacy. The majority of the studies addressed in this review concern the forms of filariasis, parasite life cycle, symptoms, medications used to treat filariasis, synthetic schemes, SAR, and results from the reported research.

30 Mar 2025·RAPID COMMUNICATIONS IN MASS SPECTROMETRY

Metabolomic Analysis of Patients With Patent Foramen Ovale and Migraine Using Liquid Chromatography‐Mass Spectrometry Technology

Article

Author: Li, Xiu‐fen ; Nizhamuding, Dilimulati ; Ye, Hai‐tao ; Xie, Yang ; Gong, Peng‐fei ; Tuerxun, Paerhati ; Yang, Yan

ABSTRACT:

Objective:

This study aims to examine the changes in metabolic profiles in patients with patent foramen ovale (PFO) and migraine, as well as in patients with isolated migraine, before and after surgical intervention using metabolomics.

Methods:

Patients were categorized into four groups: the simple migraine (SM) group, the PFO with migraine preoperative group (PRE), the PFO with migraine postoperative Day 3 group (POST_3d), and the PFO with migraine postoperative Day 30 group (POST_30d). Untargeted metabolomics using liquid chromatography–mass spectrometry (LC‐MS) were employed to identify differential metabolites across these groups. Differential metabolites were identified, their clinical diagnostic value was assessed, and a correlation analysis was conducted to examine changes in metabolic pathways before and after surgery.

Results:

The expression levels of metabolites such as linoleic acid, quinolinic acid, homophenylalanine, and amphetamine showed significant changes in patients with PFO and migraine following surgery. Notably, linoleic acid demonstrated strong diagnostic potential for this patient population. Trend analysis revealed that the levels of 3‐phenylpropionic acid and caffeine decreased on postoperative Day 3 and subsequently increased by postoperative Day 30, whereas gallic acid continuously declined. Compared to the PRE group, differential metabolites in the SM group were primarily associated with α‐linolenic acid metabolism, niacin and nicotinamide metabolism, sphingolipid signaling, and tyrosine metabolism. In contrast, differential metabolites in the POST_3d group were predominantly enriched in phenylalanine metabolism, niacin and nicotinamide metabolism, protein digestion and absorption, and caffeine metabolism.

Conclusion:

Linoleic acid may serve as a potential biomarker, and the activation of inflammation and oxidative stress‐related pathways could contribute significantly to the development of complicated migraine in patients with PFO.

1

News (Medical) associated with Diethylcarbamazine Citrate

12 Nov 2024

·www.globenewswire.com

Timor-Leste eliminates lymphatic filariasis as a public health problem

DECATUR, Ga., Nov. 12, 2024 (GLOBE NEWSWIRE) -- The Mectizan Donation Program applauds Timor-Leste for eliminating lymphatic filariasis (LF) as a public health problem, a remarkable achievement that was recently validated by the World Health Organization (WHO). Timor-Leste is the fifth country in Southeast Asia to achieve this milestone and the first country in the region to do so by co-administering Mectizan, albendazole and diethylcarbamazine (DEC). Since 2017, Merck (known as MSD outside of the U.S. and Canada), GSK and Eisai have been partnering to donate Mectizan, albendazole, and DEC, respectively, to accelerate the elimination of LF in eligible countries where river blindness is not endemic based on a recommendation of triple drug therapy from WHO. LF, commonly known as elephantiasis, is a debilitating disease caused by a parasite transmitted by mosquitoes. Long-term, chronic infection can cause damage to the lymphatic system, as well as severe and irreversible swelling to the limbs, breasts and/or genitals. These symptoms can cause extreme discomfort, disability and social stigmatization. “We are delighted to learn of Timor-Leste’s success in eliminating LF as a public health problem,” said Allison Goldberg, president, Merck Foundation. “This achievement is a testament to the strength and determination of the Timor-Leste people and the power of public-private partnerships, including the Mectizan Donation Program.”Thomas Breuer, Chief Global Health Officer at GSK, stated, “We congratulate Timor-Leste for this remarkable achievement. The elimination of lymphatic filariasis as a public health problem in Timor-Leste is demonstrative of the power of effective partnerships and the unwavering commitment of the global NTD community.” Mectizan Donation Program director Dr. Yao Sodahlon, an expert in tropical diseases who played a vital role in the elimination of LF in Togo, stated, “We celebrate the government of Timor-Leste, the endemic communities who helped distribute the medicines with high coverage demonstrating effectiveness of triple drug therapy, and the partners who made elimination of LF in Timor-Leste possible. This success demonstrates that elimination of LF can be achieved through the donations of these essential medicines, the commitment of the government and people of the endemic countries, and the global partnership working to end LF.” About the Mectizan Donation Program The Mectizan Donation Program (MDP) was established in 1987 to provide medical, technical, and administrative oversight of the donation of Mectizan by Merck for the treatment of onchocerciasis, also known as river blindness. In 1998, MDP expanded its mandate to include oversight of the donation of albendazole by GSK for the elimination of lymphatic filariasis in onchocerciasis co-endemic areas. Contacts MDP:Joni Lawrence Deputy Director Mectizan Donation Program jlawrence@taskforce.org Yao SodahlonDirectorMectizan Donation Programysodahlon@taskforce.org

100 Deals associated with Diethylcarbamazine Citrate

Login to view more data

External Link

KEGG	Wiki	ATC	Drug Bank
D00803	Diethylcarbamazine Citrate	P02CB02	DB00711

R&D Status

10 top approved records.

Login

to view more data

Indication	Country/Location	Organization	Date
Filariasis	Japan	Mitsubishi Tanabe Pharma Corp.	01 Feb 1951
Elephantiasis, Filarial	United States	Lederle Laboratories	13 Nov 1950

Login to view more data

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03177993 (Pubmed \| Clin Infect Dis)	Not Applicable	Elephantiasis, Filarial	3,816	Ivermectin, diethylcarbamazine, and albendazole	dwjbyevfsu(rhewzgozxh) = hepuasvymb faevjdcoep (cqtqcjjvhl, 43.6 - 78.2)	-	17 Mar 2021
				Diethylcarbamazine and albendazole	dwjbyevfsu(rhewzgozxh) = ttphxkhdmj faevjdcoep (cqtqcjjvhl, 57.2 - 79.1)
NCT02974049 (Pubmed \| Clin Infect Dis)	Not Applicable	Elephantiasis, Filarial	95	Single dose of IDA (ivermectin plus diethylcarbamazine plus albendazole)	fihtsovvqx(mqiscuxzer) = qncytqmxwo akzumxuxrc (loyulqeoxh, 56 - 85) View more	Positive	23 Oct 2019
				Three annual doses of IA (ivermectin plus albendazole)	fihtsovvqx(mqiscuxzer) = uhlliqaama akzumxuxrc (loyulqeoxh, 14 - 42) View more
NCT01111305 (CTgov)	Phase 2	Loiasis \| Eosinophilia	31	Reslizumab+Diethylcarbamazine (Reslizumab + DEC)	pdbehfaopw(wbhwhweudg) = vsfdavpykd qvkerpmkec (jlnnkzivmj, wlbtendgae - wxivobnxku) View more	-	01 Jun 2017
				Placebo+Diethylcarbamazine (Placebo + DEC)	pdbehfaopw(wbhwhweudg) = shxnwauchk qvkerpmkec (jlnnkzivmj, rojsrfcxog - nxlbgkmrwv) View more
NCT01593722 (CTgov)	Phase 4	Loiasis	155	Diethylcarbamazine (Diethylcarbamazine)	oesfyoezoh(kyjfjzxbpo) = mwteaqzoxm wscirlwhpi (vglkurnrsc, gqpouwbuim - dhratzvfjl) View more	-	09 Nov 2016
				Ivermectin (Ivermectin)	oesfyoezoh(kyjfjzxbpo) = tvarwykdbj wscirlwhpi (vglkurnrsc, trvvcvpwfg - cmigjyrbry) View more
NCT00511004 (CTgov)	Phase 2	Elephantiasis, Filarial	40	Albendazole+Diethylcarbamazine (Diethylcarbamazine/Albendazole -STD)	ykeqkarcts(brgqikitnl) = rbjimltrfs tctudtjwaf (srdtlonlhf, uctchbkumx - joehuydqtf)	-	31 Aug 2015
				Albendazole+Diethylcarbamazine (Diethylcarbamazine/Albendazole- HD1)	ykeqkarcts(brgqikitnl) = ntqyjquhje tctudtjwaf (srdtlonlhf, jijukcxowc - behlqsvxsy)