Last reviewed 2026-04-23 · How we verify

TKI

TKI inhibits tyrosine kinases to block cancer cell proliferation and survival.

TKI inhibits tyrosine kinases to block cancer cell proliferation and survival. Used for Chronic myeloid leukemia, Non-small cell lung cancer, Gastrointestinal stromal tumor.

At a glance

Mechanism of action

TKIs work by selectively inhibiting specific tyrosine kinases, which are enzymes involved in the activation of proteins that promote cell growth and survival. By blocking these enzymes, TKIs can prevent cancer cells from growing and dividing, ultimately leading to cell death.

Approved indications

• Chronic myeloid leukemia
• Non-small cell lung cancer
• Gastrointestinal stromal tumor

Common side effects

• Dermatologic reactions
• Fatigue
• Hypertension

Key clinical trials

• TILs Plus Third-Generation EGFR-TKI Therapy for TKI-Resistant NSCLC (EARLY_PHASE1)
• Immunotherapy With Nivolumab and Ipilimumab Followed by Nivolumab or Nivolumab With Cabozantinib for Patients With Advanced Kidney Cancer, The PDIGREE Study (PHASE3)
• Testing the Use of Steroids and Tyrosine Kinase Inhibitors With Blinatumomab or Chemotherapy for Newly Diagnosed BCR-ABL-Positive Acute Lymphoblastic Leukemia in Adults (PHASE3)
• CHOICE:Decision Factor of EGFR-TKI in Chinese IV NSCLC
• Asciminib & Standard-of-Care Integration in Maintenance Therapy for POST Allogeneic Stem Cell Transplant (Allo-HSCT) of Patient With Ph+ B-ALL or Blastic Transformed CML (PHASE2)
• Chemotherapy With Targeted-Immunotherapy for Newly Diagnosed Ph+ ALL (NA)
• Regorafenib in Patients With Refractory Primary Bone Tumors (PHASE1, PHASE2)
• A Phase 1/2 Study of TRI-611 in ALK-Positive NSCLC (PHASE1, PHASE2)

Primary sources

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