ラロトレクチニブ

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Warning

• 危険有害性情報

  H302：飲み込むと有害

  H317：アレルギー性皮膚反応を起こすおそれ

• 注意書き

  P280：保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。

ラロトレクチニブ 化学特性,用途語,生産方法

• 効能

  抗悪性腫瘍薬

• 説明

  LOXO-101 is an inhibitor of the tropomyosin-related kinases TrkA, TrkB, and TrkC (IC₅₀s = 2-20 nM). It is selective for TrkA, -B, and -C over a panel of 226 kinases at 1 μM. LOXO-101 inhibits the growth of CUTO-3.29, KM12, and MO-91 patient-derived cancer cell lines (IC₅₀s = <100, <10, and <10 nM, respectively). In vivo, LOXO-101 (60 and 200 mg/kg) reduces tumor growth in a KM12 mouse xenograft model.

• 説明

  Larotrectinib, also known as LOXO-101 and ARRY-470, is a small molecule that was designed to block the ATP-binding site of the TRKA, TRKB, and TRKC, serving as a highly specific and potent inhibitor of all of the three tropomyosin kinase receptors.

• 使用

  Larotrectinib is a TRK Inhibitor (Tyrosine kinase inhibitor).

• 臨床応用

  The US Food and Drug Administration (FDA) granted accelerated approval to larotrectinib (Vitrakvi?) on November 26th, 2018, as a treatment for adult and pediatric patients with solid tumors that have NTRK gene fusions without a known acquired resistance mutation, are metastatic or where surgical resection is likely to result in severe morbidity, and have no satisfactory alternative treatments or that have progressed following treatment on. In the approval statement by FDA, a complete response rate of 22% and partial response rate of 53% were cited.

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