Nilotinib (Tasigna)
Targeted Therapy · Approved since 2007
Description
Nilotinib is a second-generation BCR-ABL tyrosine kinase inhibitor primarily approved for chronic myeloid leukemia that has been evaluated in colorectal cancer as a repurposed therapy. In CRC, nilotinib has been combined with standard treatments like paclitaxel for peritoneal carcinomatosis and with cetuximab in patients with solid tumors. The drug's potential anti-tumor activity in CRC relates to its ability to inhibit multiple kinases beyond BCR-ABL that may play roles in colorectal tumor growth and metastasis.
Mechanism of Action
Nilotinib selectively inhibits the BCR-ABL tyrosine kinase by binding to the ATP-binding site, preventing phosphorylation of downstream substrates involved in cell proliferation. The drug also inhibits other kinases including PDGFR, KIT, and DDR1, which may contribute to its activity against solid tumors like colorectal cancer by disrupting angiogenesis and tumor cell survival pathways.
Molecular Targets
Side Effects
Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.
Clinical Trials
Quick Info
| Brand Name | Tasigna |
| Category | Targeted Therapy |
 Status | Off-label |
 EMA Status | EMA Approved |
 Spain Access | Hospital use off-label in CRC |
| Administration | Oral |
| Year Approved | 2007 |
| Clinical Trials | 3 |
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Medical Disclaimer
This information is for educational purposes only and should not replace professional medical advice. Always consult your healthcare team before making treatment decisions.