Induction of remission in patients with acute promyelocytic leukemia (APL), French American British (FAB) classification M3 (including the M3 variant) characterized by t(15;17) translocation and/or PML/RARα gene presence.
藥理
Tretinoin appears to bind one or more nuclear receptors and decreases proliferation and induces differentiation of APL cells; initially produces maturation of primitive promyelocytes and repopulates the marrow and peripheral blood with normal hematopoietic cells to achieve complete remission.
藥動學
Absorption: well absorbed; Protein binding: >95%, predominantly to albumin. Metabolism: hepatic via CYP; primary metabolite: 4-oxo-all-trans-retinoic acid; displays autometabolism. Terminal elimination half-life:: parent drug: 0.5-2 hours. Time to peak: 1-2 hours. Excretion: Urine (63%), feces (30%).
禁忌症
Hypersensitivity to retinoids, pregnancy, lactation.
Acute promyelocytic leukaemia 45 mg/m2 /day in 2 divided doses, continue treatment until 30 days after complete remission or 90 days of treatment given, whichever occurs 1st.