ISSN 2398-2942      

Toceranib phosphate

icanis

Synonym(s): Palladia


Introduction

Name

  • Toceranib phosphate.

Class of drug

  • A tyrosine kinase (TK) inhibitor.

Description

Chemical name

  • (Z)-5-[(5-Fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-N-(2-pyrrolidin-1-ylethyl)-1H-pyrrole-3-carboxamide phosphate.

Molecular formula

  • C22H25FN4O2H3O4P

Molecular weight

  • 494.46

Storage requirements

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

Uses

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Indications

  • Indicated for the Patnaik Grade II or III, recurrent, cutaneous mast cell tumors Skin: mastocytoma with or without regional lymph node involvement in dogs. The presence of the KIT mutation is more common in high grade mast cell tumors, and mast cell tumors with the KIT mutation tend to be more responsive to Palladia.
  • Preliminary studies have also demonstrated promising responses in anal sac adenocarcinomas, gastrointestinal stromal cell tumors (GIST), thyroid carcinomas, malignant melanomas and nasal adenocarcinomas.
  • Preliminary studies in cats suggest a dose of 2.5 mg/kg three days per week may be beneficial in the treatment of mast cell tumors.

Administration

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Pharmacokinetics

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Precautions

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Interactions

with other drugs

  • NSAID drugs should be used with caution in conjunction with Palladia due to an increased risk of gastrointestinal ulceration or perforation and should not be given on the same day as Palladia.
  • Corticosteroids used concurrently with Palladia should also not be given on the same day as Palladia.
    Current recommendation is that chemotherapy for mast cell tumors including vincristine and lomustine should be administered prior to starting palladia.

Adverse Reactions

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Further Reading

Publications

Refereed papers

  • Recent references from PubMed and VetMedResource.
  • London C A et al (2009) Multi-center, placebo-controlled, double-blind, randomized study of oral toceranib phosphate (SU11654), a receptor tyrosine kinase inhibitor, for the treatment of dogs with recurrent (either local or distant) mast cell tumor following surgical excision. Clin Cancer Res 15 (11), 3645-3647 PubMed.

Other sources of information

  • London C A (2009) Tyrosine kinase inhibitor (TKI) therapy in companion animals: a practical approach. ACVIM Proceedings, Montreal, Quebec.
  • www.zoetisus.com
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