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托塞拉尼

Toceranib

Toceranib phosphate

酪氨酸激酶抑制劑 / 抗腫瘤藥PO狗貓

別名: Palladia · PHA-291639 · SU-11654 · UNII59L7Y0530C · toceranibum · tocéranib · toceranib phosphate · SU11654

由 VetSheet 獸醫團隊審訂更新於 2026年4月5日本內容以實證獸醫文獻為本

3.25 mg/kg PO every other day (q48h)PO· q48h· Ongoing as tolerated
— 🐕

劑量為持牌獸醫專業人員的臨床參考。請務必對照最新藥品說明書及個別病患確認。

各物種劑量

🌎 NA — North America🌍 EU — Europe

狗

適應症劑量途徑頻次療程地區
Patnaik grade II or III, recurrent, cutaneous mast cell tumors (Label Dose)3.25 mg/kg PO every other day (q48h)POq48hOngoing 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 dayPOq48hOngoing as tolerated🌎 NA
Mast cell tumours and other malignancies2.5-3.25 mg/kgPOq48h or on a Monday, Wednesday, Friday basisOngoing 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.

貓

適應症劑量途徑頻次療程地區
Malignancies (Off-label)2.5 mg/kg (range 1.5-3.25 mg/kg)POMonday, Wednesday, Friday basis (or less frequently q48h)Ongoing based on response and toxicity🌍 EU
  • Malignancies (Off-label): Limited information available. Off-label use.

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概覽

托塞拉尼（Toceranib）是一種專為獸醫開發的口服標靶治療藥物，屬於小分子酪氨酸激酶抑制劑（TKI）。

​主要適應症：​

  • 獲 FDA 批准用於治療犬隻的第二或第三級復發性皮膚​肥大細胞瘤（MCTs）​（伴隨或不伴隨局部淋巴結侵犯）。

​仿單標示外 / 研究中用途：​

  • 可能有助於治療犬隻的多種其他腫瘤，包括肉瘤、癌、黑色素瘤和多發性骨髓瘤。
  • 越來越常被納入​節拍性化學療法（Metronomic chemotherapy）​方案中（使用低劑量、持續給藥的抗癌藥物來抑制腫瘤血管生成與生長）。

作用機制

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.

安全性與警告

禁忌症

  • 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

不良反應

  • 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)

注意事項

​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.

藥物相互作用

NSAIDs (e.g., piroxicam, carprofen)

Increased risk of gastrointestinal ulceration or perforation. Use with extreme caution; never give on the same day as toceranib to avoid exacerbating GI toxicity.

CYP3A4 Inhibitors (e.g., ketoconazole, fluconazole, itraconazole, clarithromycin, verapamil, grapefruit juice)

May theoretically increase toceranib plasma concentrations and toxicity. Use with caution.

CorticosteroidsMajor

Increased risk of severe gastrointestinal toxicity and ulceration.

NSAIDsMajor

Increased risk of severe gastrointestinal toxicity and ulceration.

Other chemotherapeutic agentsModerate

Potential for additive myelosuppression and systemic toxicity. Use with caution.

監測

  • 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

藥物動力學

半衰期

狗17 hours (IV), 31 hours (PO)

吸收

Oral bioavailability in dogs is about 77%. The presence of food does not significantly impact absorption.

分佈

Binding to canine plasma proteins is around 94%. The volume of distribution is very large (>20 L/kg).

代謝

Metabolized via cytochrome P450 and/or flavin monooxygenase to an N-oxide metabolite.

排除

Terminal elimination half-life is about 17 hours (after IV) and 31 hours (oral).

過量

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.

可用產品

劑型

  • Oral tablets
  • 10 mg film-coated tablet
  • 15 mg film-coated tablet
  • 50 mg film-coated tablet

獸醫用

  • 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

各地核准狀態

European Union✓ 已核准處方藥EMA
🐕 Dogs

POM-V classification.

United Kingdom✓ 已核准處方藥VMD
🐕 Dogs

POM-V classification.

暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU

儲存與穩定性

Store at controlled room temperature 20-25°C (68-77°F).

飼主須知

​重要安全警告：​ 托塞拉尼是一種抗癌藥物。在處理藥錠或清理寵物的糞便、尿液或嘔吐物時，​請務必戴上手套​。孕婦或兒童不應接觸此藥物。

  • ​給藥方式：​ 可與食物一起或空腹餵食。​絕對不可剝半或壓碎藥錠。​
  • ​副作用：​ 請密切觀察副作用。如果您的狗狗出現嚴重腹瀉（每天4次或以上的稀便）、食慾不振、嘔吐，或糞便中有任何出血跡象（鮮血或黑色柏油狀糞便），請​立即停藥並聯絡您的獸醫師​。
  • ​漏藥處理：​ 若忘記給藥，請勿給予雙倍劑量。請在下一次預定時間給予正常劑量即可。
  • 請務必閱讀處方附帶的寵物主人用藥資訊表。

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