Miltefosine
Hexadecylphosphocholine
Also known as: Milteforan · Impavido · Miltex · D-18506 · HDPC · hexadecilfosfocolina · hexadecylphosphocholine · miltefosiini · miltefosina · miltéfosine · miltefosinum
Reviewed by the VetSheet Veterinary TeamUpdated Apr 5, 2026Evidence-based veterinary reference
Doses are a clinical reference for licensed veterinary professionals. Always confirm against the current label and the individual patient.
Dosing by species
🌎 NA — North America🌍 EU — Europe
Dogs
| Indication | Dose | Route | Frequency | Duration | Region |
|---|---|---|---|---|---|
| Canine leishmaniasis | 2 mg/kg PO | PO | once a day | 28 days | 🌎 NA |
| Canine leishmaniasis (alternative treatment to meglumine antimoniate) | 2 mg/kg PO | PO | once daily | 28 days | 🌎 NA |
| Leishmaniosis | 2 mg/kg | PO | q24h | 28 days | 🌍 EU |
- Canine leishmaniasis: Poured onto food, with a full or partial meal.
- Canine leishmaniasis (alternative treatment to meglumine antimoniate): Use with allopurinol (10 mg/kg PO q12h, orally for at least 6 months).
- Leishmaniosis: It is particularly important that the full course is completed and given with allopurinol. Pour on feed to reduce digestive side effects.
Doses are a clinical reference for licensed veterinary professionals. Always confirm against the current label and the individual patient.
Overview
Miltefosine is an oral antileishmanial agent primarily used in veterinary medicine to treat canine leishmaniasis (CanL), a severe systemic disease caused by the intracellular protozoan Leishmania infantum.
- Originally developed as an antineoplastic (anti-cancer) drug.
- Clinical Pearl: While it significantly reduces the parasitic load and improves clinical signs, it rarely achieves complete parasitological cure. Remission is the primary therapeutic goal.
- Efficacy is markedly improved when used in combination with allopurinol.
- It is an orphan drug in human medicine and is not commercially available as a veterinary-labeled product in the USA, though it is widely used in endemic regions (e.g., Europe).
Mechanism of action
Miltefosine is an alkylphosphocholine (phospholipid derivative). Its exact mechanism against Leishmania is multifactorial:
- Inhibits macrophage penetration: Interacts with glycosomes and glycosylphosphatidyl-inositol (GPI) anchors that are essential for the parasite's intracellular survival.
- Enzyme inhibition: Inhibits phospholipase → disrupts parasite membrane signal transduction and lipid metabolism.
- Apoptosis induction: Triggers apoptosis-like cell death in the parasite by disrupting lipid rafts in the cell membrane.
- Additionally, miltefosine exhibits mild antineoplastic, immunomodulatory, and antiviral properties.
Safety & warnings
Contraindications
- Hypersensitivity to miltefosine
- Pregnant animals
- Lactating animals
- Breeding animals
- Pregnancy
- Lactation
Adverse effects
- Vomiting (most common)
- Diarrhea
- Inappetence
- Potential nephrotoxicity
- Potential hepatotoxicity
- Vomiting (moderate, transient)
- Diarrhoea (moderate, transient)
Precautions
Resistance Warning: Do not underdose, as subtherapeutic levels significantly increase the risk of developing drug-resistant Leishmania strains.
- Use with extreme caution in patients with severe hepatic dysfunction.
- While leishmaniasis itself causes kidney and liver damage, miltefosine has a lower risk of severe renal tubular damage compared to meglumine antimoniate, though monitoring is still required.
Monitoring
- Baseline and periodic renal function
- Hepatic enzymes
- Adverse effects (especially vomiting)
- Patient weight
- Clinical signs of leishmaniosis
- Gastrointestinal signs (vomiting, diarrhoea)
Pharmacokinetics
Half-life
Absorption
High oral bioavailability of 94% in dogs. Peak plasma levels occur around 5 hours post-dose.
Distribution
Widely distributed throughout major organs, including the brain. Intravascularly, it is approximately equally distributed in the plasma and erythrocytes.
Metabolism
Not extensively metabolized; primarily acts unchanged.
Elimination
Mainly eliminated via the feces, with approximately 10% of a dose eliminated unchanged. Renal elimination appears negligible.
Overdose
Overdoses are likely to cause severe gastrointestinal signs (vomiting, diarrhea, anorexia). In cases of massive overdose, there is a potential for hepatic, renal, and retinal toxicity.
There is no specific antidote for miltefosine overdose; treatment should consist of prompt gastrointestinal decontamination (if recent and patient is asymptomatic) followed by aggressive supportive care (IV fluids, antiemetics, hepatoprotectants).
Available products
Formulations
- Capsules
- Oral solution: 20 mg/ml
Veterinary
- Miltefosine Oral Solution: 20 mg/mL in 30 mL, 50 mL & 90 mL vials (Milteforan)
- Milteforan 20 mg/ml oral solution
Human-labeled
- Miltefosine capsules: 10 mg, 50 mg (Impavido)
Regulatory status
Authorized for veterinary use in specific countries such as Spain and Germany.
A Special Treatment Authorization (STA) is required to obtain this product in the UK.
No regulatory data for: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
Storage & stability
This veterinary medicinal product does not require any special storage conditions. Avoid freezing the solution.
Client information
CRITICAL SAFETY WARNING: This medication is known to cause birth defects. Pregnant women or women trying to conceive MUST NOT handle this drug.
- Administration: Always give this medication poured onto food (with a full or partial meal). This significantly reduces the chance of stomach upset and vomiting.
- Handling Precautions: Wear disposable gloves when administering the liquid, as it can cause skin reactions. Do not shake the vial (to avoid foaming).
- Pet Interaction: Do not allow treated dogs to lick people immediately after they have taken the medication.
- Side Effects: Vomiting is very common. If your dog experiences severe vomiting, loss of appetite, or diarrhea, contact your veterinarian for advice (they may prescribe an anti-nausea medication).
VetSheet drug reference is intended for licensed veterinary professionals as a clinical decision-support aid, not a substitute for professional judgement or the manufacturer’s current label.