Kinase Inhibitor

A drug that blocks the activity of one or more protein kinases, enzymes that transfer phosphate groups from ATP to substrate proteins. Kinase inhibitors are classified as Type I (ATP-competitive, active conformation), Type II (inactive conformation), Type III (allosteric), or Type IV (substrate-competitive). They represent one of the most successful drug classes in oncology.

Beispiele

• Imatinib — BCR-ABL inhibitor (chronic myeloid leukemia)
• Osimertinib — EGFR T790M inhibitor (NSCLC)
• Tofacitinib — JAK1/JAK3 inhibitor (rheumatoid arthritis)