Toceranib
Toceranib phosphate
También conocido como: Palladia · PHA-291639 · SU-11654 · UNII59L7Y0530C · toceranibum · tocéranib · toceranib phosphate · SU11654
Revisado por el equipo veterinario de VetSheetActualizado 5 abr 2026Referencia veterinaria basada en la evidencia
Las dosis son una referencia clínica para profesionales veterinarios autorizados. Confirme siempre con el prospecto actual y cada paciente individual.
Dosis por especie
🌎 NA — North America🌍 EU — Europe
Perros
| Indicación | Dosis | Vía | Frecuencia | Duración | Región |
|---|---|---|---|---|---|
| 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.
Gatos
| Indicación | Dosis | Vía | Frecuencia | Duración | Región |
|---|---|---|---|---|---|
| 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.
Las dosis son una referencia clínica para profesionales veterinarios autorizados. Confirme siempre con el prospecto actual y cada paciente individual.
Resumen
El toceranib es una terapia dirigida oral pionera específica para uso veterinario, clasificada como un inhibidor de la tirosina quinasa (TKI) de molécula pequeña.
Indicaciones principales:
- Aprobado por la FDA para el tratamiento de mastocitomas (MCTs) cutáneos de grado II o III de Patnaik, recurrentes, con o sin afectación de los ganglios linfáticos regionales en perros.
Usos fuera de etiqueta / en investigación:
- Puede ser útil para tratar una variedad de otros tumores en perros, incluyendo sarcomas, carcinomas, melanomas y mieloma múltiple.
- Se utiliza cada vez más como parte de protocolos de quimioterapia metronómica (uso de dosis bajas y continuas de agentes anticancerígenos para inhibir la angiogénesis y el crecimiento tumoral).
Perlas clínicas:
- El calcitriol puede potenciar sinérgicamente la actividad antiproliferativa del toceranib en perros con mastocitomas.
- Debido a su mecanismo, puede causar una disfunción vascular significativa; las intervenciones quirúrgicas requieren una programación cuidadosa en relación con la administración de toceranib.
Mecanismo de acción
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.
Seguridad y advertencias
Contraindicaciones
- 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
Efectos adversos
- 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)
Precauciones
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.
Interacciones farmacológicas
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.
Monitorización
- 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
Farmacocinética
Vida media
Absorción
Oral bioavailability in dogs is about 77%. The presence of food does not significantly impact absorption.
Distribución
Binding to canine plasma proteins is around 94%. The volume of distribution is very large (>20 L/kg).
Metabolismo
Metabolized via cytochrome P450 and/or flavin monooxygenase to an N-oxide metabolite.
Eliminación
Terminal elimination half-life is about 17 hours (after IV) and 31 hours (oral).
Sobredosis
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.
Productos disponibles
Formulaciones
- Oral tablets
- 10 mg film-coated tablet
- 15 mg film-coated tablet
- 50 mg film-coated tablet
Veterinario
- 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
Estado regulador
POM-V classification.
POM-V classification.
Sin datos reguladores para: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
Almacenamiento y estabilidad
Store at controlled room temperature 20-25°C (68-77°F).
Información para el cliente
Advertencia de seguridad importante: El toceranib es un medicamento contra el cáncer. Use siempre guantes al manipular las tabletas o al limpiar las heces, la orina o el vómito de su mascota. Las mujeres embarazadas o los niños no deben manipular este medicamento.
- Administración: Puede administrarse con o sin alimentos. No parta ni triture las tabletas.
- Efectos adversos: Observe de cerca si aparecen efectos secundarios. Suspenda la medicación inmediatamente y contacte a su veterinario si su perro desarrolla diarrea grave (4 o más deposiciones líquidas al día), pérdida de apetito, vómitos o cualquier signo de sangre en las heces (sangre roja o heces oscuras y alquitranadas).
- Dosis omitidas: Si olvida una dosis, no duplique la siguiente. Administre la siguiente dosis en el horario programado regularmente.
- Lea siempre la Hoja de Información para el Cliente proporcionada con su receta.
La referencia de medicamentos de VetSheet está destinada a profesionales veterinarios autorizados como ayuda para la toma de decisiones clínicas, no como sustituto del criterio profesional ni del prospecto actual del fabricante.