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更新于：2025-12-04

Toceranib

托西尼布

更新于：2025-12-04

概要

基本信息

药物类型

小分子化药

别名

PHA-291639、SU 11654、SU-11654

靶点

c-Kit

作用方式

抑制剂

作用机制

c-Kit抑制剂(干细胞生长因子受体抑制剂)

治疗领域

肿瘤

在研适应症

肿瘤

非在研适应症-

原研机构

Sugen, Inc.

在研机构

Sugen, Inc.

非在研机构-

权益机构-

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

结构/序列

分子式C22H28FN4O6P

InChIKeyAOORBROPMMRREB-HBPAQXCTSA-N

CAS号874819-74-6

关联

100 项与托西尼布相关的临床结果

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100 项与托西尼布相关的转化医学

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100 项与托西尼布相关的专利（医药）

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168

项与托西尼布相关的文献（医药）

2025-11-01·VETERINARY RADIOLOGY & ULTRASOUND

A Single Institution Retrospective Comparison of Two Radiotherapy Protocols for the Palliative Treatment of Canine Nasal Carcinoma

Article

作者: Preston, Annette ; Hayes, Alison ; Wong, Hannah ; Dobson, Jane

ABSTRACT:

Optimal radiation protocols for canine nasal carcinoma are not established. Co‐morbidities, access, and owner compliance can influence scheduling. Between 2015 and 2022, two radiotherapy protocols were used in the palliative treatment of canine nasal carcinoma at a single institution. Group A comprised 17 cases receiving 40 Gy in ten 4 Gy fractions delivered Monday, Wednesday, and Friday. Epistaxis was present in 11/17 (65%) cases. Median survival time (MST) was 298 days (95% CI: 163.54–432.45); progression‐free survival was 173 days (95% CI: 117.87–228.12). Group B comprised 24 cases receiving 36 Gy in six 6 Gy fractions delivered Monday and Friday. Epistaxis was present in 20/24 (83%) cases. MST was 375 days (95% CI: 240.73–509.27); progression‐free survival was 243 days (95% CI: 138.42–347.58). Dogs with Adams Stage 1 disease had the longest median overall (593 days) and progression‐free survival (609 days). Four cases each received additional radiation treatment and/or toceranib at relapse. Palliative radiation therapy achieved control of clinical signs in the majority of cases, with an overall response rate of 100% (Group A) and 96% (Group B). In a multivariate Cox regression model with backwards elimination, when cases were stratified for tumor stage, neither the presence of epistaxis nor treatment (6 vs. 10 fractions) was independently associated with significant improvements in survival. Epistaxis at presentation did not appear to influence survival. These results indicate that palliative radiation therapy is highly effective in controlling clinical signs associated with nasal carcinoma. Increasing fractionation may have a limited effect on survival outcome or toxicity in the palliative setting.

2025-11-01·VETERINARY SURGERY

Pancreaticoduodenectomy with choledochoduodenostomy and pancreaticojejunostomy in a cat with bile and pancreatic duct obstruction secondary to a recurrent carcinoid

Article

作者: Kazuyuki Suzuki DVM ; Takeshi Hayakawa DVM ; Yuma Tomo DVM, PhD ; Kumiko Ishigaki DVM, PhD ; Kazushi Asano DVM, PhD, Charter DJCVS

Abstract:

Objective:

To describe the surgical procedure for pancreaticoduodenectomy with choledochoduodenostomy and pancreaticojejunostomy for carcinoids of the common bile duct (CBD) in a cat and to report its outcomes.

Study design:

Case report.

Animal:

A 6‐year‐old neutered male Munchkin cat.

Methods:

A small tissue plug causing CBD obstruction was surgically removed from a cat. The obstructive plug was diagnosed histopathologically as carcinoid. Nine months after initial surgery, the cat developed anorexia and vomiting. Diagnostic imaging revealed dilation of both the CBD and pancreatic duct, and the cat underwent a second surgery 11 months after the initial procedure. En bloc resection of the pancreatic body and duodenum, including the site of the CBD obstruction, was performed. Following the duodenal reconstruction with end‐to‐end anastomosis, the biliary system was rebuilt with end‐to‐side anastomosis, connecting the CBD's resected end to the duodenum. Pancreatojejunostomy of the distal end of the left pancreatic lobe and jejunum was performed to reconstruct the pancreatic duct.

Results:

No postoperative complications such as bile leakage, pancreatic fluid leakage, or pancreatitis were observed. Toceranib therapy was initiated postoperatively. The cat showed good general condition 524 days after the second surgery and exhibited favorable progress at the time of writing.

Conclusion:

This is the first report of a successful reconstructive surgery with choledochoduodenostomy and pancreatojejunostomy after en bloc resection of the pancreatic body and proximal duodenum in a cat with recurrent carcinoid‐induced ductal obstruction. Pancreatic body duodenectomy may be a viable and effective option for managing pancreatic duct obstruction in cats.

2025-09-03·NEW ZEALAND VETERINARY JOURNAL

Toceranib phosphate for treatment of hypercalcaemia of malignancy in two dogs with metastatic anal sac apocrine gland adenocarcinoma

Article

作者: Brockley, L ; Morey, J

CASE HISTORY:

Two dogs, a 10-year-old male Siberian Husky cross and an 11-year-old male Cocker Spaniel were referred to a specialist veterinary hospital in Melbourne, Australia, for treatment of metastatic anal sac apocrine gland adenocarcinoma (ASAGAC) and concurrent hypercalcaemia (concentration of ionised calcium in serum > 1.5 mmol/L) of malignancy.

CLINICAL FINDINGS:

Case 1 had a left anal sac mass approximately 5.5 cm in diameter, enlarged sub-lumbar lymph nodes palpable on rectal examination and a concentration of ionised calcium in serum of 2.45 (reference range 1.2-1.32) mmol/L. Soft tissue opacities suspicious for metastatic pulmonary nodules were observed on thoracic radiographs. CT of Case 2 revealed bilateral anal gland masses (left: 4.7 × 3.2 cm; right: 2.8 × 2.1 cm) and a large, ill-defined, intrapelvic mass (7.0 × 6.0 cm) encompassing the medial iliac and internal iliac lymph nodes and intimately associated with the aortic blood vessels. Cytology of fine-needle aspirates of the anal gland masses of both dogs was consistent with ASAGAC. The owners of both dogs declined surgical intervention and medical management with toceranib phosphate was initiated in the gross disease setting.

TREATMENT AND OUTCOME:

Toceranib was initially administered at a dose of 2.5 mg/kg orally every other day in both dogs. Due to side effects from this medication, including hypocalcaemia, the dosing schedule was adjusted to Monday, Wednesday, and Friday with a dose range of 2.25-2.5 mg/kg. Both dogs remained alive, Case 1 after 519 days and Case 2 after 477 days, and were normocalcaemic at the time of writing. Both dogs experienced resolution of hypercalcaemia of malignancy while being treated with toceranib alone: hypercalcaemia was controlled for a total of 12 months in Case 1 and 15 months in Case 2. During treatment the anal sac mass of Case 1 remained approximately 5 cm in diameter and the sub-lumbar lymph node remained subjectively stable though no objective measurements were taken. Case 2's anal sac masses and intrapelvic lymph node mass subjectively reduced in size based on palpation.

CLINICAL RELEVANCE:

This case series highlights two instances where toceranib monotherapy effectively managed hypercalcaemia of malignancy secondary to metastatic ASAGAC. Despite the presence of extensive macroscopic neoplastic disease, both dogs achieved durable control of hypercalcaemia with toceranib treatment.Abbreviations: ASAGAC: Anal sac apocrine gland adenocarcinoma; cRECIST: Canine response evaluation criteria in solid tumours; HHM: Humoral hypercalcaemia of malignancy; OST: Overall survival time; PFS: Progression-free survival; PTH: Parathyroid hormone; PTHrP: Parathyroid-related hormone peptide; RTK: Receptor tyrosine kinase; TKI: Tyrosine kinase inhibitor.

项与托西尼布相关的新闻（医药）

2025-10-30

·简书

宠物药品展会上有哪些值得关注的新品和趋势？

宠物药品展会上有哪些值得关注的新品和趋势？一、1. 新型靶向治疗药物崭露头角近年来，随着宠物医疗技术的不断进步，靶向治疗在宠物肿瘤、免疫系统疾病等复杂病症中的应用逐渐成熟。2023年全球宠物医药市场规模已突破350亿美元，预计到2028年将增长至近500亿美元（数据来源：Grand View Research）。在这一背景下，多家国际制药企业推出了针对犬猫特定基因突变或蛋白表达异常的靶向药物。例如，美国Zoetis公司展出的新型口服抗肿瘤药Toceranib Phosphate（商品名Palladia）已在国内部分高端宠物医院投入使用，用于治疗犬肥大细胞瘤，其临床缓解率可达67%以上。此外，德国勃林格殷格翰推出的单克隆抗体类药物也在控制猫慢性肾病相关的炎症反应中展现出良好疗效。这类药物通过精准干预病理通路，显著提升了治疗效率并减少了副作用，成为本次展会最受关注的技术方向之一。二、2. 生物制剂与免疫调节产品加速发展生物制剂正逐步改变传统宠物用药格局。相较于化学合成药物，生物制剂具有更高的特异性和更低的毒性风险。展会上，多款重组蛋白、疫苗增强剂及细胞疗法产品集中亮相。其中，加拿大MedGene Labs发布的新型犬用狂犬病口服疫苗引发广泛关注，该疫苗采用腺病毒载体技术，可实现非注射接种，极大提升了接种依从性。同时，日本卫材动物健康展出的IL-4/IL-13双靶点抑制剂——Cadirocatinab，在治疗猫过敏性皮炎的III期临床试验中显示出8周内瘙痒评分下降逾50%的效果。这些产品的共同特点是基于对宠物免疫机制的深入研究，推动了从“症状控制”向“病因干预”的转变。值得注意的是，国内企业如瑞普生物也发布了自主开发的干扰素α喷雾剂，适用于犬猫疱疹病毒和杯状病毒感染的辅助治疗，标志着我国在生物兽药领域的自主研发能力正在快速提升。三、3. 智能给药系统与数字化健康管理融合智能化设备与药品的结合成为本届展会的一大亮点。传统宠物用药常面临剂量不准、依从性差等问题，而智能给药系统的出现有效缓解了这些痛点。瑞士诺华动物健康展示的“SmartDose”胶囊系统，可通过蓝牙连接手机APP，自动记录投药时间与剂量，并在错过用药时发出提醒。更进一步，该系统还能根据体重变化动态调整推荐用量。与此同时，美国Elanco推出的透皮凝胶递送平台TransDerm™，使难以口服的老年猫也能便捷接受甲状腺药物治疗。配合配套的皮肤传感器，可实时监测血药浓度波动。这类技术不仅提升了治疗安全性，也为远程诊疗提供了数据支持。多个参展商表示，未来三年内将有超过15款集成AI算法的宠物用药管理设备进入市场，涵盖从处方分发到疗效评估的全流程。四、4. 天然成分与功能性补充剂持续升温消费者对宠物食品安全性的关注度不断提升，推动天然来源药品和营养补充剂需求激增。据Allied Market Research统计，2023年全球宠物营养补充剂市场已达98亿美元，年复合增长率稳定在8.3%。展会上，含有姜黄素、Omega-3脂肪酸、益生菌复合物的产品占据显著展位。美国VetriScience推出的“Joint Support Gold”添加了非变性II型胶原蛋白，临床数据显示连续使用12周后，患有关节炎的犬只活动能力改善率达74%。另一款由法国Virbac研发的口腔益生菌含片，能在宠物口腔定植有益菌群，抑制牙龈卟啉单胞菌繁殖，减少牙结石形成。值得注意的是，越来越多产品开始提供第三方检测报告，标注重金属残留、微生物限度等指标，增强透明度。此外，CBD油类产品虽仍受限于部分国家法规，但在欧美市场已有合法化趋势，主要用于缓解宠物焦虑与慢性疼痛，相关产品均明确标注THC含量低于0.3%，符合联邦标准。

疫苗细胞疗法免疫疗法临床3期

100 项与托西尼布相关的药物交易

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