WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 200127
CAS#: 570406-98-3 (free base)
Description: Avatrombopag, also known as AKR-501, YM477, AS 1670542 or E5501, is a novel orally-active thrombopoietin (TPO) receptor agonist. AKR-501 specifically targeted the TPO receptor and stimulated megakaryocytopoiesis throughout the development and maturation of megakaryocytes just as rhTPO did. AKR-501 may be useful in the treatment of patients with thrombocytopenia. Avatrombopag was first approved in 2018.
MedKoo Cat#: 200127
Name: Avatrombopag free base
CAS#: 570406-98-3 (free base)
Chemical Formula: C29H34Cl2N6O3S2
Exact Mass: 648.15109
Molecular Weight: 649.65
Elemental Analysis: C, 53.61; H, 5.28; Cl, 10.91; N, 12.94; O, 7.39; S, 9.87
Synonym: AKR501; AKR 501; AKR-501; YM477; YM-477; YM 477; AS 1670542; AS1670542; AS-1670542; E5501; E-5501; E 5501; Avatrombopag;
IUPAC/Chemical Name: (1-(3-chloro-5-((4-(4-chloro-2-thienyl)-5-(4-cyclohexylpiperazin-1-yl)thiazol-2-yl)carbamoyl)-2-pyridyl)piperidine-4-carboxylic acid)
InChi Key: OFZJKCQENFPZBH-UHFFFAOYSA-N
InChi Code: InChI=1S/C29H34Cl2N6O3S2/c30-20-15-23(41-17-20)24-27(37-12-10-35(11-13-37)21-4-2-1-3-5-21)42-29(33-24)34-26(38)19-14-22(31)25(32-16-19)36-8-6-18(7-9-36)28(39)40/h14-18,21H,1-13H2,(H,39,40)(H,33,34,38)
SMILES Code: O=C(C1CCN(C2=NC=C(C(NC3=NC(C4=CC(Cl)=CS4)=C(N5CCN(C6CCCCC6)CC5)S3)=O)C=C2Cl)CC1)O
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >5 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 649.65 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
1: Mladsi D, Barnett C, Aggarwal K, Vredenburg M, Dieterich D, Kim R. Cost- Effectiveness of Avatrombopag for the Treatment of Thrombocytopenia in Patients with Chronic Liver Disease. Clinicoecon Outcomes Res. 2020 Sep 14;12:515-526. doi: 10.2147/CEOR.S262772. PMID: 32982341; PMCID: PMC7500829.
2: Lim MY, Gilreath JA. Periprocedural use of avatrombopag for neurosurgical interventions: a strategy to avoid platelet utilization. Blood Adv. 2020 Sep 22;4(18):4438-4441. doi: 10.1182/bloodadvances.2020003045. PMID: 32936905; PMCID: PMC7509863.
3: Khemichian S, Terrault NA. Thrombopoietin Receptor Agonists in Patients with Chronic Liver Disease. Semin Thromb Hemost. 2020 Sep;46(6):682-692. doi: 10.1055/s-0040-1715451. Epub 2020 Aug 20. PMID: 32820479.
4: Dieterich DT, Bernstein D, Flamm S, Pockros PJ, Reau N. Review article: a treatment algorithm for patients with chronic liver disease and severe thrombocytopenia undergoing elective medical procedures in the United States. Aliment Pharmacol Ther. 2020 Aug 19. doi: 10.1111/apt.16044. Epub ahead of print. PMID: 32813292.
5: Nilles KM, Flamm SL. Thrombocytopenia in Chronic Liver Disease: New Management Strategies. Clin Liver Dis. 2020 Aug;24(3):437-451. doi: 10.1016/j.cld.2020.04.009. Epub 2020 May 31. PMID: 32620282.
6: Birocchi S, Podda GM, Manzoni M, Casazza G, Cattaneo M. Thrombopoietin receptor agonists for the treatment of primary immune thrombocytopenia: a meta- analysis and systematic review. Platelets. 2020 Apr 12:1-11. doi: 10.1080/09537104.2020.1745168. Epub ahead of print. PMID: 32281449.
7: Saab S, Bernstein D, Hassanein T, Kugelmas M, Kwo P. Treatment Options for Thrombocytopenia in Patients With Chronic Liver Disease Undergoing a Scheduled Procedure. J Clin Gastroenterol. 2020 Jul;54(6):503-511. doi: 10.1097/MCG.0000000000001338. PMID: 32195771.
8: Poordad F, Terrault NA, Alkhouri N, Tian W, Allen LF, Rabinovitz M. Avatrombopag, an Alternate Treatment Option to Reduce Platelet Transfusions in Patients with Thrombocytopenia and Chronic Liver Disease-Integrated Analyses of 2 Phase 3 Studies. Int J Hepatol. 2020 Jan 25;2020:5421632. doi: 10.1155/2020/5421632. PMID: 32047671; PMCID: PMC7003278.
9: Nilles KM, Caldwell SH, Flamm SL. Thrombocytopenia and Procedural Prophylaxis in the Era of Thrombopoietin Receptor Agonists. Hepatol Commun. 2019 Sep 4;3(11):1423-1434. doi: 10.1002/hep4.1423. PMID: 31701067; PMCID: PMC6824078.
10: Abdela J. Current Advance in Thrombopoietin Receptor Agonists in the Management of Thrombocytopenia Associated With Chronic Liver Disease: Focus on Avatrombopag. Clin Med Insights Blood Disord. 2019 Oct 21;12:1179545X19875105. doi: 10.1177/1179545X19875105. Erratum in: Clin Med Insights Blood Disord. 2020 Jan 6;13:1179545X19900859. PMID: 31673229; PMCID: PMC6804364.
11: Hussar DA. New Drugs 2019, part 4. Nursing. 2019 Nov;49(11):34-43. doi: 10.1097/01.NURSE.0000585892.82614.f4. PMID: 31651773.
12: Cheloff AZ, Al-Samkari H. Avatrombopag for the treatment of immune thrombocytopenia and thrombocytopenia of chronic liver disease. J Blood Med. 2019 Sep 5;10:313-321. doi: 10.2147/JBM.S191790. PMID: 31565009; PMCID: PMC6733339.
13: Witkowski M, Witkowska M, Robak T. Autoimmune thrombocytopenia: Current treatment options in adults with a focus on novel drugs. Eur J Haematol. 2019 Dec;103(6):531-541. doi: 10.1111/ejh.13319. Epub 2019 Sep 18. PMID: 31449692.
14: Li C, Li X, Huang F, Yang J, Wu A, Wang L, Qin D, Zou W, Wu J. Efficacy and Safety of Avatrombopag in Patients With Thrombocytopenia: A Systematic Review and Meta-Analysis of Randomized Controlled Trials. Front Pharmacol. 2019 Jul 26;10:829. doi: 10.3389/fphar.2019.00829. PMID: 31402863; PMCID: PMC6677019.
15: Miller JB, Figueroa EJ, Haug RM, Shah NL. Thrombocytopenia in Chronic Liver Disease and the Role of Thrombopoietin Agonists. Gastroenterol Hepatol (N Y). 2019 Jun;15(6):326-332. PMID: 31391802; PMCID: PMC6676354.
16: Xu H, Cai R. Avatrombopag for the treatment of thrombocytopenia in patients with chronic liver disease. Expert Rev Clin Pharmacol. 2019 Sep;12(9):859-865. doi: 10.1080/17512433.2019.1649137. Epub 2019 Aug 5. PMID: 31352834.
17: Hussar DA, Kludjian GA. Prucalopride succinate, Fostamatinib disodium hexahydrate, Avatrombopag maleate, and Lusutrombopag. J Am Pharm Assoc (2003). 2019 Jul-Aug;59(4):601-604. doi: 10.1016/j.japh.2019.05.013. PMID: 31296323.
18: Dou X, Yang R. Current and emerging treatments for immune thrombocytopenia. Expert Rev Hematol. 2019 Sep;12(9):723-732. doi: 10.1080/17474086.2019.1636644. Epub 2019 Jul 4. PMID: 31237783.
19: Clemons Bankston P, Al-Horani RA. New Small Molecule Drugs for Thrombocytopenia: Chemical, Pharmacological, and Therapeutic Use Considerations. Int J Mol Sci. 2019 Jun 20;20(12):3013. doi: 10.3390/ijms20123013. PMID: 31226783; PMCID: PMC6628068.
20: Saab S, Brown RS Jr. Management of Thrombocytopenia in Patients with Chronic Liver Disease. Dig Dis Sci. 2019 Oct;64(10):2757-2768. doi: 10.1007/s10620-019-05615-5. Epub 2019 Apr 22. PMID: 31011942.
AKR-501, a novel, small-molecule thrombopoietin mimetic being investigated for the treatment of thrombocytopenia. AkaRx is now a wholly-owned subsidiary of Eisai Inc. and Eisai has the exclusive worldwide rights to develop, market and manufacture AKR-501. AKR-501 is an investigational thrombopoietin receptor agonist that, based on preclinical studies, increases platelet production by stimulating megakaryocytic proliferation and differentiation. Eisai is currently conducting Phase II clinical trials of AKR-501 in the United States as a potential treatment for idiopathic thrombocytopenic purpura (ITP) and thrombocytopenia associated with liver diseases (TLD), and has confirmed proof of concept in the clinical studies for ITP. In addition, Eisai will explore the compound's potential as a treatment for chemotherapy-induced thrombocytopenia (CIT).