Toceranib
Toceranib is a small-molecule receptor tyrosine kinase inhibitor used in veterinary oncology. Its established canine indication is recurrent cutaneous mast cell tumor, with additional extra-label applications in selected other malignancies. It acts through both tumor-cell signaling and tumor-associated vascular pathways, making response dependent on the biological targets present in the tumor.
Group
Receptor tyrosine kinase inhibitor
Mechanism of Action
Toceranib inhibits several receptor tyrosine kinases, including KIT, VEGFR and PDGFR. Inhibition of susceptible KIT signaling can reduce mast-cell tumor proliferation and survival. Effects on VEGF- and PDGF-dependent pathways inhibit aspects of angiogenesis and supporting vascular function. These combined actions can limit tumor growth or stabilize disease, with response varying by tumor type and target dependence.
Dose Rates
Dogs
| Use / stage | Dose | Route | Schedule | Instructions |
|---|---|---|---|---|
| Mast cell tumor | 3.25 mg/kg | PO | Every 48 h | Reported label amount; use whole tablets. |
| Mast cell tumor | 2.2 mg/kg | PO | Every 48 h | Minimum effective amount cited in monograph; individualize. |
| Intermittent oncology treatment | Reference only | PO | 2.5-2.75 mg/kg orally three days weekly, for example Monday/Wednesday/Friday. A weekly calendar schedule cannot be replaced by a uniform 48-hour interval. | |
| Mast cell tumor lower-dose alternative | 2.5–2.75 mg/kg | PO | Every 48 h | Often better tolerated than 3.25 mg/kg. Whole tablets only; modify or interrupt for adverse effects. |
Cats
| Use / stage | Dose | Route | Schedule | Instructions |
|---|---|---|---|---|
| Reported oncology treatment | 2.5–2.75 mg/kg | PO | Every 48 h | Alternative to three-times-weekly reported schedule; feline efficacy depends on tumor. |
| Intermittent oncology treatment | Reference only | PO | 2.5-2.75 mg/kg orally three times weekly; weekly calendar spacing is not a fixed hour interval. |
Indications
- Treatment of recurrent canine cutaneous mast cell tumors, including the labeled Patnaik grade II or III setting with or without regional lymph-node involvement.
- Specialist extra-label treatment of selected canine gastrointestinal stromal tumors.
- Specialist treatment of selected canine carcinomas, including some apocrine anal-sac or thyroid carcinomas, with variable and less-established efficacy.
Contraindications
- Pregnancy
- Daily dosing has excessive adverse events.
Interactions
- Interaction information is limited; concurrent treatment requires individualized oncology assessment.
Adverse effects
- Diarrhea, anorexia, weight loss, lameness, GI bleeding, hypertension and proteinuria risk.
Toxicity
Toceranib has a narrow safety margin. Prompt exposure assessment and individualized GI, hematologic and hemodynamic support are needed after overdose.
Preparations
| Preparation | Form | Strength | Route |
|---|---|---|---|
| Palladia 10 mg film-coated tablet Do not split film-coated tablets. Whole tablets only. | Tablet | 10 mg / tablet | PO |
| Palladia 15 mg film-coated tablet Do not split film-coated tablets. Whole tablets only. | Tablet | 15 mg / tablet | PO |
| Palladia 50 mg film-coated tablet Do not split film-coated tablets. Whole tablets only. | Tablet | 50 mg / tablet | PO |
Monitoring and Administration
Monitor gastrointestinal signs, weight, blood pressure, proteinuria and thyroid values when indicated. Interrupt for adverse reactions and restart lower after recovery; reported regimen describes interruption up to 2 weeks.
Handle as a cytotoxic medicine and keep film-coated tablets intact. Compounded formulations have shown substandard strengths.
Use gloves when handling toceranib and do not crush or split coated tablets; avoid exposure to contaminated waste.