emodepside (BAY 44-4400) / Bayer - LARVOL DELTA

Effects of emodepside on single-channel properties of Onchocerca volvulus SLO-1A (BK) potassium channels. (PubMed, Parasit Vectors) - "This study successfully expressed Ovo-SLO-1A in HEK293 cells, measured the conductance of the main open-state, and detected the presence of subconductance states and flickering openings. The increased amplitudes of the single-channel currents, open burst times, and open probabilities provides insights into the complex kinetics by which emodepside increases Slo-1K currents and illustrates the dynamic actions of emodepside on Ovo-SLO-1A."

Journal • Infectious Disease • Ophthalmology

EMOTI: Efficacy and Safety of a Single Dose of Emodepside Compared to a Single Dose of Albendazole in Adolescents and Adults Infected With Trichuris Incognita (clinicaltrials.gov) - P2 | N=100 | Not yet recruiting | Sponsor: Jennifer Keiser

New P2 trial • Infectious Disease

Antiparasitic agent emodepside exerts cytotoxicity in human corneal stromal cells by blocking the interaction between mini-chromosome maintenance 6 protein (MCM6) and chromatin licensing and DNA replication factor 1 (CDT1). (PubMed, Toxicology) - "Moreover, emodepside-induced cell cycle arrest in HCS cells leads to dose-dependent apoptosis and proliferation inhibition with the IC50 value being 32.3μM.  In conclusion, this study not only provides new insights into the mechanism of emodepside-induced vision blur but also offers a valuable molecular tool for the research of MCM6-CDT1 interaction."

Journal • CDT1 • MCM6

21 - New Drugs for Treatment of Filarial Infections (ASTMH 2025) - "The drugs presented during the symposium (Corallopyronin A, Oxfendazole, Emodepside, Moxidectin and a re-purposed antibiotic, fusidic acid) are in various stages of development, from transition between preclinical development and Phase I to Phase II or Phase III clinical trials. An initial clinical trial using Moxidectin in combination with Albendazole alone or with Albendazole and Diethylcarbamazine for treatment of lymphatic filariasis has been carried out to evaluate the efficacy of the different combinations. Moxidectin, with its confirmed efficacy for the treatment of onchocerciasis has been used for the first time for mass drug administration in Ghana.#Vaccinology#ChildHealth#InfectiousDisease#Prevention#NewDrugs#ClinicalTrials"

Infectious Disease

TREMO-Pemba: Efficacy and Safety of Emodepside in Participants With Soil-transmitted Helminth Infections (clinicaltrials.gov) - P3 | N=315 | Not yet recruiting | Sponsor: Swiss Tropical & Public Health Institute | Trial completion date: Nov 2025 ➔ Apr 2026 | Initiation date: May 2025 ➔ Oct 2025 | Trial primary completion date: Sep 2025 ➔ Feb 2026

Trial completion date • Trial initiation date • Trial primary completion date • Infectious Disease

TREMO-Siargao: Efficacy and Safety of Emodepside in Participants With Soil-transmitted Helminth Infections (clinicaltrials.gov) - P3 | N=315 | Not yet recruiting | Sponsor: Swiss Tropical & Public Health Institute | Trial completion date: Feb 2026 ➔ Sep 2026 | Initiation date: Aug 2025 ➔ Jan 2026 | Trial primary completion date: Dec 2025 ➔ Jun 2026

Trial completion date • Trial initiation date • Trial primary completion date • Infectious Disease

Positive allosteric modulation of emodepside sensitive Brugia malayi SLO-1F and Onchocerca volvulus SLO-1A potassium channels by GoSlo-SR-5-69. (PubMed, PLoS Pathog) - "In contrast, GoSlo-SR-5-69 binds at the RCK1 pocket. This study reveals for the first time, allosteric modulation of filarial nematode SLO-1 K channels by a mammalian BK channel activator and highlights its ability to increase emodepside potency on the B. malayi SLO-1 K channel."

Journal • Infectious Disease

Effects of Emodepside on Single-Channel Properties of Onchocerca volvulus SLO-1A (BK) Potassium Channels. (PubMed, Res Sq) - " This study successfully expressed Ovo -SLO-1A in HEK 293 cells, measured the conductance of the main open-state and detected the presence of sub-conductance states, and flickering openings. The increased amplitudes of the single-channel currents, open-burst times and open probabilities provide insights into how emodepside increases Slo-1K currents and illustrate dynamic actions of emodepside on Ovo -SLO-1A."

Journal • Infectious Disease • Ophthalmology

Emodepside for strongyloidiasis: insights from parasite genetics. (PubMed, Lancet Infect Dis) - No abstract available

Journal

Emodepside for strongyloidiasis: insights from parasite genetics - Authors' reply. (PubMed, Lancet Infect Dis) - No abstract available

Journal

Discovery of the new active ingredient tigolaner, an allosteric modulator of the GABA-gated chloride channel for use as a spot-on ectoparasiticide in animal health. (PubMed, Bioorg Med Chem Lett) - "Felpreva® employs this active ingredient for ectoparasite control together with the endoparasiticides emodepside and praziquantel. Some synthetic pathways for tigolaner and its analogs are also described. This publication also outlines the efficacy of tigolaner against various parasites, making it a key compound of the Felpreva® product."

Journal

Differential Emodepside Efficacy in Drug-Resistant and Drug-Susceptible Ancylostoma caninum Highlights Variability in Potassium Channel Activity. (PubMed, Trop Med Infect Dis) - "The addition of penitrem A reversed the enhanced emodepside sensitivity in BCR, implicating elevated basal expression of SLO-1 channels as a potential factor. These findings suggest that emodepside, via its action on SLO-1, may offer a promising therapeutic avenue to combat multidrug-resistant hookworm infections."

Journal • Infectious Disease

Eucoleus boehmi in dogs: Anthelmintic treatment challenges and impact on olfactory capacity. (PubMed, Vet Parasitol) - "The treatment protocols included moxidectin/imidacloprid (MI) and pyrantel pamoate/febantel/praziquantel (PFP), separately and combined, as well as emodepside/praziquantel (EP) alone. In general, lower FEC were associated with better performance in the olfactory assessment. Further studies are needed to evaluate additional anthelmintics' efficacy, and to further understand the effect of E. boehmi on a dog's olfactory capacity."

Journal

Efficacy and safety of ascending doses of emodepside in comparison with ivermectin in adults infected with Strongyloides stercoralis in Laos: a phase 2a, dose-ranging, randomised, parallel-group, placebo-controlled, single-blind clinical trial. (PubMed, Lancet Infect Dis) - P2 | "At all doses tested, emodepside was efficacious and well tolerated in individuals infected with S stercoralis. The broad-spectrum weight-independent dose and robust safety profile positions emodepside as a promising new candidate for strongyloidiasis treatment."

Journal • P2a data • Infectious Disease

Untangling "dissolved" drug species from various formulations of a poorly soluble drug: Sampling methods, mechanistic insights, and IVIVC. (PubMed, J Pharm Sci) - "In vitro two-stage dissolution tests, that simulate the transfer from gastric to intestinal phases, using four different formulations at two dose strengths of the poorly water-soluble and weakly basic drug emodepside were performed...Microdialysis and nanofiltration reflected human oral bioavailability best, followed by conventional filtration and bench-top centrifugation, while 2nd derivative UV spectroscopy showed the poorest correlation. Analysis of molecularly dissolved drug thus appears to better predict formulation behavior in vivo."

Journal

Implementation of real-time PCR assays for diagnosing intestinal protozoa infections. (PubMed, Parasitol Res) - "The study highlights the utility of qPCR in providing species-level differentiation and improving the speed and cost-effectiveness of testing. The high prevalence of protozoa in this region underscores the need for continued monitoring and control efforts, though emodepside was not effective against protozoa infections."

Journal • Infectious Disease

Topical and oral emodepside formulations for last-line treatment of multianthelmintic drug-resistant hookworms when given orally to dogs are not bioequivalent. (PubMed, Am J Vet Res) - "Poor absorption following topical administration suggests it may be unsuitable for treating multianthelmintic drug-resistant hookworm infections. These findings highlight potential emodepside toxicity risks with extralabel use of the FDA-approved topical feline product and help inform safe off-label use in dogs."

Journal • Infectious Disease

Performance of real-time polymerase chain reaction and Kato-Katz for diagnosing soil-transmitted helminth infections and evaluating treatment efficacy of emodepside in randomized controlled trials. (PubMed, PLoS Negl Trop Dis) - "Our study confirmed that qPCR is a sensitive diagnostic method for diagnosing STH infections compared to Kato-Katz and serves as a valuable tool for determining treatment efficacy in clinical trials. Furthermore, qPCR confirmed the better treatment efficacy of emodepside compared to albendazole, despite indicating lower cure rates than Kato-Katz."

Clinical • Journal • Polymerase Chain Reaction • Infectious Disease

TREMO-Siargao: Efficacy and Safety of Emodepside in Participants With Soil-transmitted Helminth Infections (clinicaltrials.gov) - P3 | N=315 | Not yet recruiting | Sponsor: Swiss Tropical & Public Health Institute

New P3 trial • Infectious Disease

Emodepside: the anthelmintic's mode of action and toxicity. (PubMed, Front Parasitol) - "Although emodepside demonstrates a favorable safety profile, continued monitoring of its toxicity is crucial, particularly in vulnerable populations. This mini-review serves as a concise resource for researchers and clinicians interested in anthelmintic therapy."

Journal • Review • Infectious Disease • Ophthalmology

Potential of emodepside for vector-borne disease control. (PubMed, Malar J) - "Emodepside was not lethal to An. dirus at human-relevant concentrations and had no effect on Ae. aegypti survival. Thus, mass distribution of emodepside does not appear to be a potential tool for vector-borne disease control. Emodepside induced mortality in An. dirus does suggest that the SLO-1 channel could be a potential target for novel vector control and may warrant further investigation."

Journal

TREMO-Pemba: Efficacy and Safety of Emodepside in Participants With Soil-transmitted Helminth Infections (clinicaltrials.gov) - P3 | N=315 | Not yet recruiting | Sponsor: Swiss Tropical & Public Health Institute

New P3 trial • Infectious Disease

Elimination goals for onchocerciasis can be progressed faster by incorporating treatment with repurposed drugs that target various stages of filarial worms (ASTMH 2024) - "We demonstrated that, 1) Nelfinavir (anti-HIV drug that targets aspartic proteases) significantly inhibited motility of Brugia pahangi female worms in vitro and reduced survival of adult worms as well as their fecundity in vivo; 2) Niclosamide and Rottlerin (autophagy inducing drugs) significantly reduced Wolbachia levels in vitro and in vivo , as well as embryogenesis and fecundity in treated female B. pahangi worms in vivo; and 3) Emodepside (repurposed macrofilaricide under clinical development), when used as a prophylactic drug, inhibits molting and motility of O. volvulus and B. pahangi early stages of the parasite in vitro with IC 50 s in the nanomolar range. Our findings indicate that a major programmatic shift that incorporates integrated control strategies, aimed at reducing both the overall adult worm burden and transmission, is needed to achieve the 2030 WHO elimination of transmission goals for onchocerciasis."

Human Immunodeficiency Virus • Infectious Disease

Efficacy and Safety of Emodepside in Adults Infected With Strongyloidiasis Stercoralis (clinicaltrials.gov) - P2 | N=202 | Completed | Sponsor: Swiss Tropical & Public Health Institute | Active, not recruiting ➔ Completed

Trial completion • Infectious Disease

Development of alternative treatments for filarial diseases (ASTMH 2024) - "Successful repurposed drugs include benzimidazoles, ivermectin and moxidectin. The Drugs for Neglected Diseases initiative (DNDi) is investigating emodepside (with Bayer AG) and ABBV-4083 (with the Anti-Wolbachia (AWOL) consortium and AbbVie), along with multiple partners...Recent studies show its strong activity against Trichuris trichiura and hookworm infections in humans. Here, we present emodepside results for Onchocerca volvulus , recent failures, and considerations for patient access to new medicines."

Late-breaking abstract • Infectious Disease • Ophthalmology