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].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT02389621	Chronic Liver Disease ... more >> Thrombocytopenia Collapse <<	Phase 3	Completed	-	-
  NCT01129024	Immune Thrombocytopenia	Phase 2	Completed	-	United States, California ... more >> Investigator Anaheim, California, United States, 92801 Investigator Los Angeles, California, United States, 90272 United States, District of Columbia Investigator Washington, District of Columbia, United States, 20007 United States, Florida Investigator Boynton Beach, Florida, United States, 33426 Investigator Jacksonville, Florida, United States, 32207 United States, Georgia Investigator Atlanta, Georgia, United States, 30341 Investigator Riverdale, Georgia, United States, 30274 United States, Louisiana Investigator Metairie, Louisiana, United States, 70006 United States, Maryland Investigator Bethesda, Maryland, United States, 20817 United States, Massachusetts Investigator Boston, Massachusetts, United States, 02114 United States, Missouri Investigator Jefferson City, Missouri, United States, 65109 Investigator Kansas City, Missouri, United States, 64131 United States, New Jersey Investigator New Brunswick, New Jersey, United States, 08903 United States, New York Investigator New York, New York, United States, 10021 Investigator New York, New York, United States, 10029 United States, Ohio Investigator Cleveland, Ohio, United States, 44106 United States, Texas Investigator San Antonio, Texas, United States, 78229 United States, Utah Investigator Salt Lake City, Utah, United States, 84132 United States, Washington Investigator Seattle, Washington, United States, 98109 Collapse <<
  NCT02389621	-	-	Completed	-	-

• 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.