Lusutrombopag

Lusutrombopag is an orally bioavailable, small molecule TPO receptor agonist that interacts with the transmembrane domain of human TPO receptors expressed on megakaryocytes to induce the proliferation and differentiation of megakaryocytic progenitor cells from hematopoietic stem cells and megakaryocyte maturation.

• MULPLETA is indicated for the treatment of thrombocytopenia in adult patients with chronic liver disease who are scheduled to undergo a procedure. MULPLETA is a thrombopoietin receptor agonist indicated for the treatment of thrombocytopenia in adult patients with chronic liver disease who are scheduled to undergo a procedure.

• None. None.contraindicated

Begin MULPLETA dosing 8-14 days prior to a scheduled procedure. ( 2.1 ) Patients should undergo their procedure 2-8 days after the last dose. ( 2.1 ) Recommended Dosage: 3 mg orally once daily with or without food for 7 days. ( 2.1 ) 2.1 Recommended Dosage Begin MULPLETA dosing 8-14 days prior to a scheduled procedure. Patients should undergo their procedure 2-8 days after the last dose. The recommended dosage of MULPLETA is 3 mg taken orally once daily with or without food for 7 days. In the case of a missed dose of MULPLETA, patients should take the missed dose as soon as possible on the same day and return to the normal schedule the following day. MULPLETA has been investigated only as a single 7-day once daily dosing regimen in clinical trials in patients with chronic liver disease [see Clinical Studies (14) ] . MULPLETA should not be administered to patients with chronic liver disease in an attempt to normalize platelet counts. 2.2 Monitoring Obtain a platelet count prior to initiation of MULPLETA therapy and not more than 2 days before the procedure.

Thrombotic/Thromboembolic Complications: MULPLETA is a thrombopoietin (TPO) receptor agonist, and TPO receptor agonists have been associated with thrombotic and thromboembolic complications in patients with chronic liver disease. Monitor platelet counts and for thromboembolic events and institute treatment promptly. ( 5.1 ) 5.1 Thrombotic/Thromboembolic Complications MULPLETA is a thrombopoietin (TPO) receptor agonist, and TPO receptor agonists have been associated with thrombotic and thromboembolic complications in patients with chronic liver disease. Portal vein thrombosis has been reported in patients with chronic liver disease treated with TPO receptor agonists. Portal vein thrombosis was reported in 1% (2 of 171) of MULPLETA-treated patients and 1% (2 of 170) of placebo-treated patients in 3 randomized, double-blind trials and was identified post-procedure in protocol-specified imaging. The thromboses were not associated with a marked increase in platelet count. Consider the potential increased thrombotic risk when administering MULPLETA to patients with known risk factors for thromboembolism, including genetic pro-thrombotic conditions (Factor V Leiden, Prothrombin 20210A, Antithrombin deficiency, or Protein C or S deficiency). In patients with ongoing or prior thrombosis or absence of hepatopetal blood flow, MULPLETA should only be used if the potential benefit to the patient justifies the potential risk. MULPLETA should not be administered to patients with chronic liver disease in an attempt to normalize platelet counts.

The following serious adverse reactions are discussed in detail in other sections of the labeling: Thrombotic/Thromboembolic Complications [see Warnings and Precautions (5.1) ] The most common adverse reaction (≥3%): headache. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Eddingpharm (U. S.) Inc. at 1-888-465-2125 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The safety of MULPLETA was evaluated in 3 randomized, double-blind, placebo-controlled trials, L-PLUS 1, L-PLUS 2, and M0626, in which patients with chronic liver disease and thrombocytopenia were treated with MULPLETA (N=171) or placebo (N=170) at a dose of 3 mg daily for up to 7 days prior to a scheduled procedure. The majority of patients were males (59%), and median age was 61 years (range 19-88). The racial and ethnic distribution was White (50%), Asian (47%), Black (<1%), and Other (3%). The most common adverse reactions (those occurring in at least 3%) in the MULPLETA-treated group across the pooled data from the three trials are summarized in table 1. Table 1. Adverse Reactions with a Frequency ≥3% in Patients Treated with MULPLETA (Pooled Data (L-PLUS 1, L-PLUS 2, and M0626)) Adverse Reaction Includes treatment-emergent adverse reactions occurring at a rate higher than placebo.

Lactation: Breastfeeding is not recommended during treatment. ( 8.2 ) 8.1 Pregnancy Risk Summary There are no available data on MULPLETA in pregnant women to inform the drug-associated risk. In animal reproduction studies, oral administration of lusutrombopag to pregnant rats during organogenesis and the lactation period resulted in adverse developmental outcomes. These findings were observed at exposures based on AUC that were substantially higher than the AUC observed in patients (approximately 89 times) at the recommended clinical dose of 3 mg once daily . Advise pregnant women of the potential risk to a fetus (see Data ) . The background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the general population in the United States, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Data Animal Data In an embryo-fetal development study in rats, lusutrombopag was orally administered during organogenesis at doses of 4, 12.5, 40, and 80 mg/kg/day. Low body weight and a decrease in the number of ossified sternebrae were noted in fetuses at 80 mg/kg/day (approximately 251 times the AUC observed in patients at the recommended clinical dose of 3 mg once daily).

Metabolism

Lusutrombopag demonstrated dose-proportional pharmacokinetics after single doses ranging from 1 mg (0.33 times the lowest approved dosage) to 50 mg (16.7 times the highest recommended dosage). Healthy subjects administered 3 mg of lusutrombopag had a geometric mean (%CV) maximal concentration (C max ) of 111 (20.4) ng/mL and area under the time-concentration curve extrapolated to infinity (AUC 0-inf ) of 2931 (23.4) ng.hr/mL.

No antidote for MULPLETA overdose is known. In the event of overdose, platelet count may increase excessively and result in thrombotic or thromboembolic complications. Closely monitor the patient and platelet count. Treat thrombotic complications in accordance with standard of care. Hemodialysis is not expected to enhance the elimination of MULPLETA because lusutrombopag is highly bound to protein in plasma [see Clinical Pharmacology (12.3) ] .

• Jul 31, 2018NDANDA210923Vancocin Italia

1. 1Death37.7%
2. 2Drug Ineffective37.7%
3. 3Nausea37.7%
4. 4Ascites25.1%
5. 5Diarrhoea25.1%
6. 6Headache25.1%
7. 7Hospitalisation25.1%
8. 8Mesenteric Vein Thrombosis25.1%
9. 9Pain25.1%
10. 10Pancytopenia25.1%
11. 11Portal Vein Thrombosis25.1%
12. 12Pulmonary Embolism25.1%
13. 13Shock Haemorrhagic25.1%
14. 14Acute Hepatic Failure12.6%
15. 15Arterial Injury12.6%

The 8 most recently updated of 8 ClinicalTrials.gov registrations naming Lusutrombopag as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Efficacy and Safety of Lusutrombopag After Allogeneic Hematopoietic Stem Cell Transplantation
  Recruiting · Interventional · 45 enrolled · The General Hospital of Western Theater Command
  NCT07483385updated 2026-03-25
• Lusutrombopag in the Treatment of Immune Thrombocytopenia (ITP)
  Completed · Phase 2 · Interventional · 17 enrolled · Institute of Hematology & Blood Diseases Hospital, China
  NCT06287567updated 2025-12-19
• Lusutrombopag Combined With Recombinant Human Thrombopoietin for the Treatment of Thrombocytopenia in Patients With Chronic Liver Disease Destined to Undergo Elective Invasive Surgery
  Recruiting · Phase 2 · Interventional · 60 enrolled · Anhui Provincial Hospital
  NCT06673498updated 2024-11-05
• A Prospective Study on the Treatment of Recurrent/Refractory/Intolerable NSAA With Lusutrombopag
  Unknown · Phase 4 · Interventional · 40 enrolled · Peking Union Medical College Hospital
  NCT06426043updated 2024-05-23
• Efficacy of Avatrombopag in Thrombocytopenic Patients With Chronic Liver Disease Undergoing an Elective Procedure
  Unknown · Phase 4 · Interventional · 476 enrolled · Chinese PLA General Hospital
  NCT04915287updated 2022-11-15
• A Study to Investigate the Efficacy and Safety of Lusutrombopag (S-888711) Tablets Administered to Adults With Immune Thrombocytopenia (ITP)
  Terminated · Phase 2 · Interventional · 20 enrolled · Shionogi
  NCT01054443updated 2021-03-18
• An Open-label Safety Study of Lusutrombopag (S-888711) in Adults With Chronic Immune Thrombocytopenia (ITP)
  Terminated · Phase 2 · Interventional · 19 enrolled · Shionogi
  NCT01129024updated 2021-02-26
• Safety and Efficacy Study of Lusutrombopag for Thrombocytopenia in Patients With Chronic Liver Disease Undergoing Elective Invasive Procedures
  Completed · Phase 3 · Interventional · 215 enrolled · Shionogi
  NCT02389621updated 2018-10-30

Frequently asked questions

How does Lusutrombopag work?

Lusutrombopag is an orally bioavailable, small molecule TPO receptor agonist that interacts with the transmembrane domain of human TPO receptors expressed on megakaryocytes to induce the proliferation and differentiation of megakaryocytic progenitor cells from hematopoietic stem cells and megakaryocyte maturation.

What is Lusutrombopag used for?

According to FDA labeling, Lusutrombopag carries indications including: MULPLETA is indicated for the treatment of thrombocytopenia in adult patients with chronic liver disease who are scheduled to undergo a procedure. MULPLETA is a thrombopoietin receptor agonist indicated for the treatment of thrombocytopenia in adult patients with chronic liver disease who are scheduled to undergo a procedure.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Lusutrombopag?

Lusutrombopag is classified as Other systemic hemostatics, Thrombopoietin Receptor Agonists, Increased Megakaryocte Cell Production, Increased Megakaryocyte Maturation, Increased Platelet Production.

What are the brand names for Lusutrombopag?

Lusutrombopag is marketed under brand names including Mulpleta.

What are the contraindications for Lusutrombopag?

Lusutrombopag labeling lists contraindications including: None. None.. Always consult the full prescribing information and a clinician.