Toceranib
Toceranib phosphate
Also known as: Palladia · PHA-291639 · SU-11654 · UNII59L7Y0530C · toceranibum · tocéranib · toceranib phosphate · SU11654
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 |
|---|---|---|---|---|---|
| Patnaik grade II or III, recurrent, cutaneous mast cell tumors (Label Dose) | 3.25 mg/kg PO every other day (q48h) | PO | q48h | Ongoing as tolerated | 🌎 NA |
| Patnaik grade II or III, recurrent, cutaneous mast cell tumors (Clinical Experience Dose) | 2.5-2.75 mg/kg PO every other day | PO | q48h | Ongoing as tolerated | 🌎 NA |
| Mast cell tumours and other malignancies | 2.5-3.25 mg/kg | PO | q48h or on a Monday, Wednesday, Friday basis | Ongoing based on response and toxicity | 🌍 EU |
- Patnaik grade II or III, recurrent, cutaneous mast cell tumors (Label Dose): Dose reductions of 0.5 mg/kg (to a minimum dose of 2.2 mg/kg every other day) and dose interruptions for up to two weeks may be utilized to manage adverse reactions. Do not split tablets.
- Patnaik grade II or III, recurrent, cutaneous mast cell tumors (Clinical Experience Dose): Often better tolerated than the label dose, resulting in less toxicity and fewer drug holidays. Alternatively, a Monday/Wednesday/Friday schedule may be used, especially when combined with other drugs in metronomic protocols.
- Mast cell tumours and other malignancies: Monitor closely. See Appendix for specific chemotherapy protocols.
Cats
| Indication | Dose | Route | Frequency | Duration | Region |
|---|---|---|---|---|---|
| Malignancies (Off-label) | 2.5 mg/kg (range 1.5-3.25 mg/kg) | PO | Monday, Wednesday, Friday basis (or less frequently q48h) | Ongoing based on response and toxicity | 🌍 EU |
- Malignancies (Off-label): Limited information available. Off-label use.
Doses are a clinical reference for licensed veterinary professionals. Always confirm against the current label and the individual patient.
Overview
Toceranib is a pioneering veterinary-specific oral targeted therapy, classified as a small molecule tyrosine kinase inhibitor (TKI).
Key Indications:
- FDA-approved for the treatment of Patnaik grade II or III, recurrent, cutaneous mast cell tumors (MCTs) with or without regional lymph node involvement in dogs.
Off-label / Investigational Uses:
- May be useful for treating a variety of other tumors in dogs, including sarcomas, carcinomas, melanomas, and multiple myeloma.
- Increasingly utilized as part of metronomic chemotherapy protocols (using low, continuous doses of anticancer agents to inhibit tumor angiogenesis and growth).
Clinical Pearls:
- Calcitriol may synergistically enhance the antiproliferative activity of toceranib in dogs with mast cell tumors.
- Due to its mechanism, it can cause significant vascular dysfunction; surgical interventions require careful timing around toceranib administration.
Mechanism of action
Toceranib competitively inhibits ATP binding at the intracellular kinase domain of several split kinase receptor tyrosine kinases (RTKs).
Key Targets:
- VEGFR-2 (Vascular Endothelial Growth Factor Receptor-2)
- PDGFR-β (Platelet-Derived Growth Factor Receptor-Beta)
- c-Kit (Stem Cell Growth Factor Receptor)
Pathway: Inhibition of RTKs → prevents receptor phosphorylation → blocks downstream signal transduction → exerts an antiproliferative effect on endothelial cells and induces cell cycle arrest and apoptosis in tumor cells.
Because canine mast cell tumor growth is frequently driven by activating mutations in c-Kit, toceranib directly targets the neoplastic cells while simultaneously reducing tumor angiogenesis via VEGFR-2 and PDGFR-β inhibition.
Safety & warnings
Contraindications
- Breeding, pregnant, or lactating bitches
- Dogs less than 24 months of age or weighing less than 5 kg (safe use not evaluated)
- Dogs < 2 years old
- Dogs < 5 kg
- Patients with any signs of gastrointestinal haemorrhage
- Known hypersensitivity to toceranib
Adverse effects
- Diarrhea (can be severe)
- Decreased or loss of appetite
- Weight loss
- Gastrointestinal bleeding (blood in stool, melena)
- Muscle cramping
- Neutropenia
- Hypoalbuminemia
- Thromboembolic disease (including pulmonary emboli)
- Vasculitis
- Pancreatitis
- Nasal depigmentation
- Change in coat or skin color
- Pruritus
- Diarrhoea
- Gastrointestinal haemorrhage
- Anorexia
- Vomiting
- Lethargy
- Myelosuppression
- Lameness / musculoskeletal disorders
- Dermatitis
- Anaemia
- Increased ALT activity
- Coagulation derangements (including pulmonary thromboembolism)
- Hypoalbuminaemia
- Hypertension
- Seizures (uncommon)
- Epistaxis (uncommon)
- Circulatory shock (uncommon)
- Death (uncommon)
Precautions
Surgical Warning: Because toceranib can cause vascular dysfunction leading to edema and thromboembolism, wait at least 3 days after stopping the drug before performing surgery.
Systemic Mastocytosis: When used in the presence of systemic mast cell tumors, significant mast cell degranulation may occur, leading to severe adverse effects (e.g., anaphylaxis, GI ulceration). Attempt to rule out systemic mastocytosis prior to starting therapy.
Hazardous Drug Handling: Use caution when handling this medication. Wear gloves and follow standard veterinary cytotoxic drug handling protocols.
Toxicity Mimicry: Toceranib can cause clinical signs similar to those seen with aggressive mast cell tumors; if these occur, stop the drug and re-evaluate the patient.
Drug interactions
Increased risk of gastrointestinal ulceration or perforation. Use with extreme caution; never give on the same day as toceranib to avoid exacerbating GI toxicity.
May theoretically increase toceranib plasma concentrations and toxicity. Use with caution.
Increased risk of severe gastrointestinal toxicity and ulceration.
Increased risk of severe gastrointestinal toxicity and ulceration.
Potential for additive myelosuppression and systemic toxicity. Use with caution.
Monitoring
- CBC (monitor for neutropenia and anemia)
- Hematocrit
- Serum Albumin
- Creatinine
- Serum Phosphate
- Full chemistry panels
- Clinical signs of GI toxicity (diarrhea, fresh blood in stool, melena)
- Tumor size and response to therapy
- Blood pressure (baseline and monthly)
- Urinalysis (baseline and monthly, monitor for proteinuria)
- Haematology (baseline and monthly)
- Biochemistry (baseline and monthly, monitor albumin and ALT)
- Coagulation profiles (if adverse signs occur)
- Faecal occult blood tests (if adverse signs occur)
- Weekly owner check-ins for the first 6 weeks to monitor for GI signs
Pharmacokinetics
Half-life
Absorption
Oral bioavailability in dogs is about 77%. The presence of food does not significantly impact absorption.
Distribution
Binding to canine plasma proteins is around 94%. The volume of distribution is very large (>20 L/kg).
Metabolism
Metabolized via cytochrome P450 and/or flavin monooxygenase to an N-oxide metabolite.
Elimination
Terminal elimination half-life is about 17 hours (after IV) and 31 hours (oral).
Overdose
Toceranib has a narrow margin of safety. While specific acute toxicity data is limited, overdoses are likely to cause severe gastrointestinal distress, myelosuppression, and vascular events.
Action: In the event of an acute overdose, consider immediate gut decontamination (emesis/activated charcoal) if caught early. Contact an animal poison control center for further guidance and provide aggressive supportive care.
Available products
Formulations
- Oral tablets
- 10 mg film-coated tablet
- 15 mg film-coated tablet
- 50 mg film-coated tablet
Veterinary
- Toceranib Phosphate Oral Tablets: 10 mg, 15 mg, 50 mg (Palladia)
- Palladia 10 mg film-coated tablets
- Palladia 15 mg film-coated tablets
- Palladia 50 mg film-coated tablets
Regulatory status
POM-V classification.
POM-V classification.
No regulatory data for: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
Storage & stability
Store at controlled room temperature 20-25°C (68-77°F).
Client information
Important Safety Warning: Toceranib is an anti-cancer drug. Always wear gloves when handling the tablets or cleaning up your pet's feces, urine, or vomit. Pregnant women or children should not handle this medication.
- Administration: May be given with or without food. Do not split or crush the tablets.
- Adverse Effects: Watch closely for side effects. Stop the medication immediately and contact your veterinarian if your dog develops severe diarrhea (4 or more watery stools a day), loss of appetite, vomiting, or any signs of bleeding in the stool (red blood or dark, tarry stools).
- Missed Doses: If you miss a dose, do not double up. Give the next dose at the regularly scheduled time.
- Always read the Client Information Sheet provided with your prescription.
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.