VetSheet

トセラニブ

Toceranib

Toceranib phosphate

チロシンキナーゼ阻害薬 / 抗悪性腫瘍薬PO犬猫

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

VetSheet 獣医チームが監修更新日 2026年4月5日エビデンスに基づく獣医学リファレンス

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

用量は獣医専門家向けの臨床参考資料です。必ず最新の医薬品情報および個別症例に基づいて確認してください。

動物種別用量

🌎 NA — North America🌍 EU — Europe

犬

適応用量経路頻度期間地域
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.

猫

適応用量経路頻度期間地域
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.

用量は獣医専門家向けの臨床参考資料です。必ず最新の医薬品情報および個別症例に基づいて確認してください。

診察中ですか？VetSheet の AI が薬剤・用量・投与期間を構造化された診察記録に直接記入します。VetSheet の仕組みを見る

概要

トセラニブは、獣医療専用に開発された経口分子標的薬であり、小分子チロシンキナーゼ阻害薬（TKI）に分類されます。

​主な適応症:​

  • 犬のグレードIIまたはIIIの再発性皮膚​肥満細胞腫（MCT）​（所属リンパ節病変の有無を問わない）の治療薬としてFDAに承認されています。

​適応外 / 研究中の用途:​

  • 肉腫、癌腫、黒色腫、多発性骨髄腫など、犬の様々な腫瘍の治療に有用である可能性があります。
  • 腫瘍の血管新生と増殖を抑制するための​メトロノミック化学療法​（低用量の抗がん剤を持続的に投与する療法）の一部として利用されることが増えています。

作用機序

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・警告

禁忌

  • 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

有害事象

  • 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.

医薬品相互作用

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.

監視

  • 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

薬物動態

半減期

犬17 hours (IV), 31 hours (PO)

吸収

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

分布

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.

消失

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

過剰投与

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.

製品

製剤

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

動物用医薬品

  • 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

規制ステータス

European Union✓ 承認済み処方箋医薬品EMA
🐕 Dogs

POM-V classification.

United Kingdom✓ 承認済み処方箋医薬品VMD
🐕 Dogs

POM-V classification.

規制データなし: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU

保管・安定性

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

飼主向け情報

​重要な安全上の警告:​ トセラニブは抗がん剤です。錠剤を取り扱う際や、ペットの便、尿、吐き戻しを片付ける際は、​必ず手袋を着用してください​。妊娠中の女性や子供はこの薬に触れないでください。

  • ​投与方法:​ 食事の有無にかかわらず投与できます。​錠剤を割ったり砕いたりしないでください。​
  • ​副作用:​ 副作用に注意してください。犬に重度な下痢（1日に4回以上の水様便）、食欲不振、嘔吐、または便への出血の兆候（鮮血または黒色タール便）が見られた場合は、​直ちに投薬を中止し、獣医師に連絡してください​。
  • ​飲み忘れ:​ 投与を忘れた場合でも、2回分を一度に与えないでください。次の予定時刻に通常の用量を与えてください。
  • 処方箋に付属している飼い主向け情報シートを必ずお読みください。

VetSheet医薬品リファレンスは獣医専門家の臨床意思決定支援を目的としており、専門的判断または製造業者の最新医薬品情報の代替にはなりません。