Emodepside
Also known as: BAY 44-4400, Cyclooctadepsipeptide anthelmintic, Emodepsid, PF1022-221, Profender
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Summary
Emodepside is a cyclic depsipeptide anthelmintic approved for veterinary use in cats and dogs. It has a broad spectrum of activity against gastrointestinal, lung and filarial nematodes and is being repurposed for human infections such as onchocerciasis, trichuriasis and hookworm. Pre‑clinical studies show macrofilaricidal effects, and early human trials suggest dose‑dependent cure rates superior to albendazole.
Mechanism of Action
Emodepside targets nematode calcium‑activated potassium (SLO‑1) channels. By increasing the opening probability of these channels, it hyperpolarises neuronal and muscle membranes, causing paralysis and loss of motility in the parasite. This mode of action is distinct from classic anthelmintics that act on acetylcholine receptors or glutamate‑gated chloride channels, and it circumvents existing resistance mechanisms.
What the Research Shows
Veterinary use of emodepside is well established, and pre‑clinical models demonstrated macrofilaricidal activity against Onchocerca ochengi, a close relative of the human parasite O. volvulus. The drug has completed Phase I human studies and entered Phase II development. Two Phase 2a dose‑ranging trials in adults with Trichuris trichiura or hookworm infection reported cure rates that rose with dose, reaching 85% for T. trichiura at 5 mg and 95% for hookworm at 30 mg, outperforming placebo and albendazole. Safety assessments recorded only mild, dose‑related adverse events (headache, blurred vision, dizziness) and no serious events. Recent reviews highlight its unique ion‑channel mechanism and a generally favorable safety profile, though long‑term human data remain limited.
Reported Benefits
Emodepside shows activity against adult filarial worms, offering a potential macrofilaricidal tool absent from current regimens. In early human trials it achieved higher cure rates than albendazole for both Trichuris trichiura and hookworm, with a rapid, single‑dose regimen. Its distinct SLO‑1 channel target may retain efficacy where resistance to benzimidazoles, macrocyclic lactones or cholinergic agents has emerged.
Limitations of the Evidence
Evidence in humans is confined to Phase 2a studies with relatively small sample sizes; larger Phase 2b/3 trials are pending. Long‑term safety and efficacy, especially in children and pregnant individuals, have not been established. The drug is not yet approved for human use, and optimal dosing regimens for different helminth species remain to be defined.
Safety Considerations
In the reported trials, the most common adverse events were mild headache, blurred vision and dizziness, occurring more frequently at higher doses. No serious or moderate adverse events were observed. Veterinary experience suggests a generally favorable safety profile, but continued monitoring is advised, particularly in vulnerable populations and with repeated dosing.
How It Is Administered
Human studies have used a single oral dose ranging from 5 mg to 30 mg. Veterinary formulations are available for oral, subcutaneous and topical administration, reflecting the drug's versatility across species.
Routes of Administration
Goals & Uses
- Treatment of strongyloidiasisAntiparasiticLow
- Overcoming anthelmintic resistanceAntiparasiticModerate
- Treatment of lymphatic filariasisAntiparasiticModerate
- Treatment of feline gastrointestinal nematodesAntiparasiticHigh
- Treatment of gastrointestinal nematodesAnthelminticHigh
- Treatment of onchocerciasis (river blindness)AntiparasiticModerate
Contraindications
- Pregnancy (human investigational use)Reproductive SafetyHigh
- Pregnant or lactating animalsReproductiveModerate
- Severe hepatic impairment (human use)Organ ImpairmentModerate
- Hypersensitivity to emodepside or excipientsAllergyHigh
- Use in kittens under 8 weeks or cats under 0.5 kg (veterinary)Age/weight RestrictionHigh
- Known hypersensitivity to emodepside or formulation excipientsAllergyHigh
Adverse Effects
- Elevated liver enzymes (human trials)HepaticUncommon
- Headache, fatigue (human trials)GeneralCommon
- Neurological signs (ataxia, lethargy)NeurologicalRare
- VomitingGastrointestinalUncommonForceful expulsion of stomach contents
- AnorexiaMetabolicUncommon
- Transient skin irritation at application siteLocalCommon
- Transient salivation / hypersalivationGastrointestinalUncommon
- Application site reactions (erythema, pruritus)DermatologicCommon
Drug Interactions
- CYP3A4 inhibitors (e.g., azole antifungals, macrolide antibiotics)Moderate
- Other CNS depressants (e.g., phenobarbital)Moderate
- Other anthelmintics (e.g., ivermectin)Low
- P-glycoprotein (P-gp) inhibitors (e.g., ketoconazole, verapamil)Moderate
Population Constraints
- Cats with known P-gp deficiency (MDR1 mutation) — not applicable, but analogous concernVeterinary GeneticsRelative
- Kittens <8 weeks oldAgeAbsolute
- Pregnant women (human investigational)PregnancyRelative
- Lactating womenReproductiveRelative
- Puppies <4 weeks oldAgeAbsolute
- Patients with MDR1/ABCB1 mutationsPharmacogenomicsRelative
- Pediatric population (human use)PediatricsRelative
Regulatory Status
- European UnionApprovedApproved: treatment of gastrointestinal nematodes in dogs, treatment of gastrointestinal nematodes in catsAuthorized under EU veterinary medicinal product regulations.
- United StatesApprovedApproved: treatment of gastrointestinal nematodes in dogs, treatment of gastrointestinal nematodes in catsVeterinary product marketed as Profender (spot‑on).
- United KingdomApprovedApproved: treatment of gastrointestinal nematodes in dogs, treatment of gastrointestinal nematodes in catsAvailable as prescription veterinary medicine.
Approved for veterinary use only; not authorized for human therapy. Marketed as topical spot‑on (Profender) and oral formulations.
Evidence & Sources
- Journal ArticleModerateKrücken J, et al.2021-01-01T00:00:00.000000Z
- Journal ArticleModerateZhao P, et al.2019-01-01T00:00:00.000000Z
- Journal ArticleModerateMartin RJ, et al.2012-01-01T00:00:00.000000Z
- Journal ArticleModerateNjeshi CN, Robertson AP, Martin RJ2024-01-01T00:00:00.000000Z
- Journal ArticleModerateMartin RJ, et al.2012-01-01T00:00:00.000000Z
- Journal ArticleModerateMrimi EC, et al.2023-01-01T00:00:00.000000Z
Frequently Asked Questions
Is emodepside already approved for treating human helminth infections?
No. Emodepside is approved for veterinary use only. It is currently in Phase 2 clinical development for human onchocerciasis, trichuriasis and hookworm, but has not received regulatory approval for these indications.
How does emodepside differ from existing anthelmintics like albendazole?
Emodepside works by opening nematode SLO‑1 calcium‑activated potassium channels, causing paralysis, whereas albendazole binds to tubulin and disrupts microtubule formation. This distinct mechanism may overcome resistance to drugs that target acetylcholine or glutamate‑gated channels.
What side effects have been observed in human trials?
The most frequently reported side effects were mild headache, blurred vision and dizziness, with incidence increasing at higher doses. No serious adverse events were recorded in the Phase 2a studies.
Can emodepside be used in children or pregnant women?
Safety data for these groups are not yet available. Current trials have enrolled adults only, so use in children or pregnant individuals cannot be recommended until further studies are completed.
Is a single dose sufficient for cure?
Early trials used a single oral dose and reported dose‑dependent cure rates, suggesting that a single administration may be effective, but optimal dosing schedules are still under investigation.
What is Emodepside?
Emodepside is a cyclic depsipeptide anthelmintic approved for veterinary use in cats and dogs. It has a broad spectrum of activity against gastrointestinal, lung and filarial nematodes and is being repurposed for human infections such as onchocerciasis, trichuriasis and hookworm. Pre‑clinical studies show macrofilaricidal effects, and early human trials suggest dose‑dependent cure rates superior to albendazole.
What is Emodepside used for?
Emodepside is educationally associated with: Treatment of strongyloidiasis, Overcoming anthelmintic resistance, Treatment of lymphatic filariasis, Treatment of feline gastrointestinal nematodes, Treatment of gastrointestinal nematodes, Treatment of onchocerciasis (river blindness). Educational only — not medical advice.
How is Emodepside administered?
Recorded routes of administration: Oral, Subcutaneous, Topical.
What are the potential side effects of Emodepside?
Reported adverse effects include: Elevated liver enzymes (human trials), Headache, fatigue (human trials), Neurological signs (ataxia, lethargy), Vomiting, Anorexia, Transient skin irritation at application site, Transient salivation / hypersalivation, Application site reactions (erythema, pruritus). This list is not exhaustive — consult a qualified clinician.
Who should avoid Emodepside?
Recorded contraindications: Pregnancy (human investigational use), Pregnant or lactating animals, Severe hepatic impairment (human use), Hypersensitivity to emodepside or excipients, Use in kittens under 8 weeks or cats under 0.5 kg (veterinary), Known hypersensitivity to emodepside or formulation excipients. Consult a qualified clinician before use.