Sunitinib

From Dog

Sunitinib is a protein kinase inhibitor which interacts with an amino acid residue within the ATP binding pocket[1].

It is recommended for treatment of gastrointestinal stromal tumors and used as a second-line therapy for advance GISTs after imatinib resistance and/or tolerance[2].

Sunitinib potentially inhibits double mutation of the ATP binding pocket which is not possible with imatinib, but has little activity against double mutation in the activation loop, making it more potent against imatinib-resistant ATP binding pocket mutation but inferior potency against the activation loop.

The usual starting dose in dogs is 1 mg/kg per day for four weeks followed by a two-week rest period.

References

  1. Patil DT & Rubin BP. Gastrointestinal stromal tumor: advances in diagnosis and management. Archives of Pathology and Laboratory Medicine 135(10):1298–1310
  2. Gramza AW et al (2009) Resistance to tyrosine kinase inhibitors in gastrointestinal stromal tumors. Clinical Cancer Research 15(24):7510–7518