Imatinib

Category: pharmacological

Aliases: Gleevec, STI571

Pharmacological Mechanism

First-in-class targeted-cancer drug — competitive ATP-site inhibitor of BCR-ABL tyrosine kinase (chronic myeloid leukemia) plus c-Kit (GIST) and PDGFR. Transformed CML from a fatal disease into a chronic condition. CYP3A4 substrate + moderate inhibitor.

Half-Life (t½)

PO: 18h

Dosing Guidelines

• PO: Typical 400mg (Range: 100 - 800 mg)

Target Organ Systems

• digestive
• immune-hematologic