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Lusutrombopag

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Chemical Structure| 1110766-97-6 同义名 : 鲁索曲波帕 ;S-888711;Mulpleta;Lusutrombopag, brand name: Mulpleta.
CAS号 : 1110766-97-6
货号 : A215820
分子式 : C29H32Cl2N2O5S
纯度 : 99%+
分子量 : 591.546
MDL号 : MFCD28502075
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(59.17 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Thrombopoietin (TPO) plays an important role in regulating thrombopoiesis and is a proven therapeutic target to stimulate production of platelets. Lusutrombopag, a small-molecule, TPO receptor agonist, was evaluated as a treatment to raise platelet counts (PCs) in patients with thrombocytopenia and CLD (chronic liver disease) undergoing invasive procedures. Adults with CLD and baseline PCs < 50 × 109/L were randomized to receive once‐daily lusutrombopag 3 mg or placebo ≤ 7 days before an invasive procedure scheduled 2‐7 days after the last dose. 64.8% (70/108) of patients in the lusutrombopag group versus 29.0% (31/107) in the placebo group met the primary endpoint (P < 0.0001; difference of proportion 95% confidence interval [CI], 36.7 [24.9, 48.5]). The median duration of PCs ≥ 50 × 109/L was 19.2 days with lusutrombopag (without platelet transfusion) compared with 0.0 in the placebo group (with platelet transfusion) (P = 0.0001). Those date indicated that lusutrombopag was superior to placebo for reducing the need for platelet transfusions and achieved durable PC response in patients with thrombocytopenia and CLD undergoing invasive procedures [3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.69mL

0.34mL

0.17mL

8.45mL

1.69mL

0.85mL

16.90mL

3.38mL

1.69mL
参考文献

[1]Katsube T, Ishibashi T, et al. Population Pharmacokinetic and Pharmacodynamic Modeling of Lusutrombopag, a Newly Developed Oral Thrombopoietin Receptor Agonist, in Healthy Subjects. Clin Pharmacokinet. 2016 Nov;55(11):1423-1433.

[2]Kim ES. Lusutrombopag: First Global Approval. Drugs. 2016 Jan;76(1):155-8.

[3]Peck-Radosavljevic M. Lusutrombopag for the Treatment of Thrombocytopenia in Patients With Chronic Liver Disease Undergoing Invasive Procedures (L-PLUS 2). Hepatology. 2019 Oct;70(4):1336-1348. doi: 10.1002/hep.30561. Epub 2019 Mar 15.