eltrombopag (AKR-501, Promacta)
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Indications
- thrombocytopenia (investigational)
- ITP, chronic liver disease, chemotherapy-induced
- FDA approved for patients who have failed at least one standard therapy for ITP
- adjunctive treatment for aplastic anemia
Contraindications
- not indicated for the treatment of thrombocytopenia in patients with chronic liver disease[4]
Dosage
- 20-75 mg PO QD
- dosing should be amined at increasing platelet count to a level that reduces the risk of bleeding, not normalizing platelet count[4]
Monitor
- serum AST & serum ALT & serum bilirubin at baseline, every 2 weeks during dosage adjustment & monthly when dose is stable[6]
Adverse effects
- none noted[2]
- hepatotoxicity[4][5]
- bone marrow toxicity[5]
- nausea, vomiting, & minor transaminase increases[3]
- portal vein thrombosis[4]
Mechanism of action
- thrombopoietin receptor agonist
- 20-40% of patients respond[2][4]
- most responders achieve platelet counts of > 50,000/uL within 15 days,
- thrombocytopenia relapses after cessation of treatment
Notes
- patients, pharmacies, & prescribers must be registered with Promacta CARES[5]
- noninstitutional retail pharmacies are not eligible to dispense Promacta
More general terms
References
- ↑ Jenkins JM et al, Phase 1 clinical study of eltrombopag, an oral nonpepeptide thrombopoietin receptor agonist. Blood 2007, 109:4739 PMID: https://www.ncbi.nlm.nih.gov/pubmed/17327409
- ↑ 2.0 2.1 2.2 Bussel JB et al, Eltrombopag for the treatment of chronic idiopathic thrombocytopenic purpura. N Engl J Med 2007, 357:2237 PMID: https://www.ncbi.nlm.nih.gov/pubmed/18046028
McHutchison JG et al, Eltrombopag for thrombocytopenia in patients with cirrhosis associated with hepatitis C. N Engl J Med 2007, 357::2227 PMID: https://www.ncbi.nlm.nih.gov/pubmed/18046027 - ↑ 3.0 3.1 Bussel JB et al. Effect of eltrombopag on platelet counts and bleeding during treatment of chronic idiopathic thrombocytopenic purpura: A randomised, double-blind, placebo-controlled trial. Lancet 2009 Feb 21; 373:641. PMID: https://www.ncbi.nlm.nih.gov/pubmed/19231632
- ↑ 4.0 4.1 4.2 4.3 4.4 4.5 FDA Medwatch Promacta (eltrombopag): Portal Venous System Thromboses in Study of Patients With Chronic Liver Disease http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm211796.htm
- ↑ 5.0 5.1 5.2 5.3 Promacta CARES http://www.promacta.com (877) 9-PROMACTA
- ↑ 6.0 6.1 Prescriber's Letter 17(7): 2010 Recommended Lab Monitoring for Common Medications Liver Function Test Scheduling Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=260704&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ Saleh MN et al. Safety and efficacy of eltrombopag for treatment of chronic immune thrombocytopenia (ITP): Results of the long-term, open-label EXTEND study. Blood 2012 Nov 20 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/23169778 <Internet> http://www.bloodjournal.org/cgi/doi/10.1182/blood-2012-04-425512
- ↑ Townsley DM, Scheinberg P, Winkler T et al Eltrombopag Added to Standard Immunosuppression for Aplastic Anemia. N Engl J Med 2017; 376:1540-1550. April 20, 2017 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/28423296 <Internet> http://www.nejm.org/doi/full/10.1056/NEJMoa1613878