-
用途
ダサチニブ（dasatinib）は、BCR-ABLをはじめとした複数のチロシンキナーゼを標的とした、分子標的治療薬であるチロシンキナーゼ阻害薬(Tyrosine-Kinase Inhibitor：TKI)としてブリストル?マイヤーズ スクイブ社により開発された抗悪性腫瘍剤（抗がん剤）である。慢性骨髄性白血病 (CML)、および既存の治療に抵抗性または不耐容のフィラデルフィア染色体陽性急性リンパ性白血病 (Ph+ALL) の治療に用いられる。
-
効能
抗悪性腫瘍薬, チロシンキナーゼ阻害薬
-
説明
Dasatinib, developed and marketed by Bristol Myers, is the first approved oral tyrosine kinase inhibitor which binds to multiple conformations of ABL kinase for the treatment of two leukemia indications: chronic myeloid leukemia (CML) and Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL). Dasatinib is a highly potent, ATPcompetitive ATPcompetitive kinase inhibitor which, at nanomolar concentrations, inhibits BCR-ABL, SRC family, c-KIT, EPHA2 and PDGFR-B.
-
化学的特性
Pale-Yellow Solid
-
一般的な説明
Dasatinib is available in 20-, 50-, and 70-mg tablets fororal administration in the treatment of CML and ALL thatare Ph1 positive. Although dasatinib is more potent thanimatinib, bioavailability is much lower with values rangingbetween 14% to 34%. The agent is extensively metabolizedwith as many as 29 metabolites seen as result of oxidationby primarily CYP3A4 and phase II conjugation.The agent may act as an inhibitor of CYP3A4 andCYP2C8. Metabolism does give an active metabolite, but this accounts for only 5% of the total and is not believed tobe important for the overall activity of the agent. Dasatinibis 95% protein bound with a terminal half-life of 3 to5 hours. The majority of the drug and metabolites are eliminatedin the feces. The most common side effects are skinrash, nausea, diarrhea, and fatigue. Serious side effects includemyelosuppression appearing as neutropenia andthrombocytopenia, bleeding of the brain and GI tract, andfluid retention.
