토세라닙
Toceranib
Toceranib phosphate
다른 이름: Palladia · PHA-291639 · SU-11654 · UNII59L7Y0530C · toceranibum · tocéranib · toceranib phosphate · SU11654
VetSheet 수의사 팀 검수업데이트 2026년 4월 5일근거 기반 수의학 참고자료
용량은 수의사 전문가를 위한 임상 참고자료입니다. 반드시 최신 약물 정보 및 개별 환자에 따라 확인하시기 바랍니다.
동물 종별 용량
🌎 NA — North America🌍 EU — Europe
개
| 적응증 | 용량 | 경로 | 빈도 | 기간 | 지역 |
|---|---|---|---|---|---|
| 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.
고양이
| 적응증 | 용량 | 경로 | 빈도 | 기간 | 지역 |
|---|---|---|---|---|---|
| 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.
용량은 수의사 전문가를 위한 임상 참고자료입니다. 반드시 최신 약물 정보 및 개별 환자에 따라 확인하시기 바랍니다.
개요
토세라닙은 수의학 전용으로 개발된 경구용 표적 치료제로, 소분자 티로신 키나제 억제제(TKI)로 분류됩니다.
주요 적응증:
- 국소 림프절 침범 여부와 관계없이 반려견의 2등급 또는 3등급 재발성 피부 비만세포종(MCT) 치료제로 FDA 승인을 받았습니다.
오프라벨 / 연구 중인 용도:
- 육종, 암종, 흑색종 및 다발성 골수종을 포함한 반려견의 다양한 종양 치료에 유용할 수 있습니다.
- 종양 혈관 신생 및 성장을 억제하기 위한 메트로노믹 화학요법(저용량의 항암제를 지속적으로 투여하는 요법) 프로토콜의 일부로 점점 더 많이 활용되고 있습니다.
작용 기전
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.
안전성·주의사항
금기사항
- 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
부작용
- 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)
주의
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.
약물 상호작용
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.
모니터링
- 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
약동학
반감기
흡수
Oral bioavailability in dogs is about 77%. The presence of food does not significantly impact absorption.
분포
Binding to canine plasma proteins is around 94%. The volume of distribution is very large (>20 L/kg).
대사
Metabolized via cytochrome P450 and/or flavin monooxygenase to an N-oxide metabolite.
배설
Terminal elimination half-life is about 17 hours (after IV) and 31 hours (oral).
과다투여
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.
제품
제형
- Oral tablets
- 10 mg film-coated tablet
- 15 mg film-coated tablet
- 50 mg film-coated tablet
동물용의약품
- 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
규제 현황
POM-V classification.
POM-V classification.
규제 데이터 없음: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
보관·안정성
Store at controlled room temperature 20-25°C (68-77°F).
보호자 정보
중요 안전 경고: 토세라닙은 항암제입니다. 알약을 만지거나 반려동물의 대변, 소변, 구토물을 치울 때는 반드시 장갑을 착용하십시오. 임산부나 어린이는 이 약을 만져서는 안 됩니다.
- 투여 방법: 식사와 관계없이 투여할 수 있습니다. 알약을 쪼개거나 부수지 마십시오.
- 부작용: 부작용이 나타나는지 주의 깊게 관찰하십시오. 반려견에게 심한 설사(하루 4회 이상의 물설사), 식욕 부진, 구토 또는 대변에 출혈 징후(선홍색 피 또는 검고 끈적한 대변)가 나타나면 즉시 투여를 중단하고 수의사에게 연락하십시오.
- 투여를 잊은 경우: 투여를 잊은 경우 두 배의 용량을 주지 마십시오. 다음 예정된 시간에 정상 용량을 투여하십시오.
- 처방전과 함께 제공되는 보호자 안내서를 반드시 읽어보십시오.
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