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MedKoo Cat#: 319768 | Name: Lusutrombopag
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Lusutrombopag, also known as S-888711, is an orally bioavailable, small molecule thrombopoietin (TPO) receptor agonist being developed by Shionogi for chronic liver disease (CLD) patients with thrombocytopenia prior to elective invasive surgery. Lusutrombopag acts selectively on the human TPO receptor and activates signal transduction pathways that promote the proliferation and differentiation of bone marrow cells into megakaryocytes, thereby increasing platelet levels. In September 2015, lusutrombopag received its first global approval in Japan for the improvement of CLD-associated thrombocytopenia in patients scheduled to undergo elective invasive procedures.

Chemical Structure

Lusutrombopag
Lusutrombopag
CAS#1110766-97-6

Theoretical Analysis

MedKoo Cat#: 319768

Name: Lusutrombopag

CAS#: 1110766-97-6

Chemical Formula: C29H32Cl2N2O5S

Exact Mass: 590.1409

Molecular Weight: 591.54

Elemental Analysis: C, 58.88; H, 5.45; Cl, 11.99; N, 4.74; O, 13.52; S, 5.42

Price and Availability

Size Price Availability Quantity
50mg USD 750.00 2 Weeks
100mg USD 1,250.00 2 Weeks
200mg USD 1,950.00 2 Weeks
500mg USD 3,950.00 2 Weeks
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Related CAS #
No Data
Synonym
S-888711; S 888711; S888711; Lusutrombopag, brand name: Mulpleta.
IUPAC/Chemical Name
(2E)-3-(2,6-Dichloro-4-((4-(3-((1S)-1-(hexyloxy)ethyl)-2-methoxyphenyl)-1,3-thiazol-2-yl)carbamoyl)phenyl)-2-methylprop-2-enoic acid
InChi Key
NOZIJMHMKORZBA-KJCUYJGMSA-N
InChi Code
InChI=1S/C29H32Cl2N2O5S/c1-5-6-7-8-12-38-18(3)20-10-9-11-21(26(20)37-4)25-16-39-29(32-25)33-27(34)19-14-23(30)22(24(31)15-19)13-17(2)28(35)36/h9-11,13-16,18H,5-8,12H2,1-4H3,(H,35,36)(H,32,33,34)/b17-13+/t18-/m0/s1
SMILES Code
O=C(O)/C(C)=C/C1=C(Cl)C=C(C(NC2=NC(C3=CC=CC([C@@H](OCCCCCC)C)=C3OC)=CS2)=O)C=C1Cl
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
>2 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
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Lusutrombopag is an orally bioavailable thrombopoietin (TPO) receptor agonist, used for treatment of chronic liver disease.
In vitro activity:
To investigate the proliferative activity and efficacy of megakaryocytic colony formation via human TPOR, lusutrombopag was applied to cultured human c-Mpl-expressing Ba/F3 (Ba/F3-hMpl) cells and human bone marrow-derived CD34-positive cells, respectively. Lusutrombopag caused a robust increase in Ba/F3-hMpl cells by activating pathways in a manner similar to that of thrombopoietin and induced colony-forming units-megakaryocyte and polyploid megakaryocytes in human CD34-positive cells. Reference: Exp Hematol. 2018 Mar;59:30-39.e2. https://pubmed.ncbi.nlm.nih.gov/29274361/
In vivo activity:
In TPOR-Ki/Shi mice, lusutrombopag significantly increased circulating platelets in a dose-dependent manner during 21-day repeated oral administration. Histopathological study of the TPOR-Ki/Shi mice on day 22 also revealed a significant increase in megakaryocytes in the bone marrow. These results indicate that lusutrombopag acts on human TPOR to upregulate differentiation and proliferation of megakaryocytic cells, leading to platelet production. Reference: Exp Hematol. 2018 Mar;59:30-39.e2. https://pubmed.ncbi.nlm.nih.gov/29274361/
Solvent mg/mL mM
Solubility
DMSO 54.3 91.85
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 591.54 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.

Recalculate based on batch purity %
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
Formulation protocol:
1. Yoshida H, Yamada H, Nogami W, Dohi K, Kurino-Yamada T, Sugiyama K, Takahashi K, Gahara Y, Kitaura M, Hasegawa M, Oshima I, Kuwabara K. Development of a new knock-in mouse model and evaluation of pharmacological activities of lusutrombopag, a novel, nonpeptidyl small-molecule agonist of the human thrombopoietin receptor c-Mpl. Exp Hematol. 2018 Mar;59:30-39.e2. doi: 10.1016/j.exphem.2017.12.005. Epub 2017 Dec 20. PMID: 29274361.
In vitro protocol:
1. Yoshida H, Yamada H, Nogami W, Dohi K, Kurino-Yamada T, Sugiyama K, Takahashi K, Gahara Y, Kitaura M, Hasegawa M, Oshima I, Kuwabara K. Development of a new knock-in mouse model and evaluation of pharmacological activities of lusutrombopag, a novel, nonpeptidyl small-molecule agonist of the human thrombopoietin receptor c-Mpl. Exp Hematol. 2018 Mar;59:30-39.e2. doi: 10.1016/j.exphem.2017.12.005. Epub 2017 Dec 20. PMID: 29274361.
In vivo protocol:
1. Yoshida H, Yamada H, Nogami W, Dohi K, Kurino-Yamada T, Sugiyama K, Takahashi K, Gahara Y, Kitaura M, Hasegawa M, Oshima I, Kuwabara K. Development of a new knock-in mouse model and evaluation of pharmacological activities of lusutrombopag, a novel, nonpeptidyl small-molecule agonist of the human thrombopoietin receptor c-Mpl. Exp Hematol. 2018 Mar;59:30-39.e2. doi: 10.1016/j.exphem.2017.12.005. Epub 2017 Dec 20. PMID: 29274361.
1: Tsuji Y, Kawaratani H, Ishida K, Kaya D, Kubo T, Fujinaga Y, Sawada Y, Takaya H, Shimozato N, Kaji K, Namisaki T, Moriya K, Akahane T, Yoshiji H. Effectiveness of Lusutrombopag in Patients with Mild to Moderate Thrombocytopenia. Dig Dis. 2019 Oct 25:1-6. doi: 10.1159/000504044. [Epub ahead of print] PubMed PMID: 31655803. 2: Shirley M, McCafferty EH, Blair HA. Lusutrombopag: A Review in Thrombocytopenia in Patients with Chronic Liver Disease Prior to a Scheduled Procedure. Drugs. 2019 Oct;79(15):1689-1695. doi: 10.1007/s40265-019-01197-8. Review. PubMed PMID: 31529283. 3: Katsube T, Wajima T, Fukuhara T, Kano T. Effects of Food and Calcium Carbonate on the Pharmacokinetics of Lusutrombopag, a Novel Thrombopoietin Receptor Agonist. Clin Ther. 2019 Sep;41(9):1747-1754.e2. doi: 10.1016/j.clinthera.2019.06.004. Epub 2019 Jul 11. PubMed PMID: 31303281. 4: 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. PubMed PMID: 31296323. 5: Sasaki R, Shiino C, Imawari M, Bentley R, Cai B, Yoshida M, Afdhal N. Safety and effectiveness of lusutrombopag in Japanese chronic liver disease patients with thrombocytopenia undergoing invasive procedures: Interim results of a postmarketing surveillance. Hepatol Res. 2019 Oct;49(10):1169-1181. doi: 10.1111/hepr.13392. Epub 2019 Jul 22. PubMed PMID: 31228221. 6: Katsube T, Shimizu R, Fukuhara T, Kano T, Wajima T. Pharmacokinetic/Pharmacodynamic Modelling and Simulation of Lusutrombopag, a Novel Thrombopoietin Receptor Agonist, for the Treatment of Thrombocytopenia in Patients with Chronic Liver Disease Undergoing Invasive Procedures. Clin Pharmacokinet. 2019 Nov;58(11):1469-1482. doi: 10.1007/s40262-019-00770-4. PubMed PMID: 31055790; PubMed Central PMCID: PMC6856258. 7: Takada H, Kurosaki M, Nakanishi H, Takahashi Y, Itakura J, Tsuchiya K, Yasui Y, Tamaki N, Takaura K, Komiyama Y, Higuchi M, Kubota Y, Wang W, Okada M, Shimizu T, Watakabe K, Enomoto N, Izumi N. Real-life experience of lusutrombopag for cirrhotic patients with low platelet counts being prepared for invasive procedures. PLoS One. 2019 Feb 15;14(2):e0211122. doi: 10.1371/journal.pone.0211122. eCollection 2019. PubMed PMID: 30768601; PubMed Central PMCID: PMC6377090. 8: Peck-Radosavljevic M, Simon K, Iacobellis A, Hassanein T, Kayali Z, Tran A, Makara M, Ben Ari Z, Braun M, Mitrut P, Yang SS, Akdogan M, Pirisi M, Duggal A, Ochiai T, Motomiya T, Kano T, Nagata T, Afdhal N. 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. PubMed PMID: 30762895; PubMed Central PMCID: PMC6849531. 9: Ishikawa T, Okoshi M, Tomiyoshi K, Kojima Y, Horigome R, Imai M, Nozawa Y, Iwanaga A, Sano T, Honma T, Yoshida T. Efficacy and safety of repeated use of lusutrombopag prior to radiofrequency ablation in patients with recurrent hepatocellular carcinoma and thrombocytopenia. Hepatol Res. 2019 May;49(5):590-593. doi: 10.1111/hepr.13305. Epub 2019 Feb 6. PubMed PMID: 30602063; PubMed Central PMCID: PMC6849762. 10: Uojima H, Arase Y, Itokawa N, Atsukawa M, Satoh T, Miyazaki K, Hidaka H, Sung JH, Kako M, Tsuruya K, Kagawa T, Iwakiri K, Horie R, Koizumi W. Relationship between response to lusutrombopag and splenic volume. World J Gastroenterol. 2018 Dec 14;24(46):5271-5279. doi: 10.3748/wjg.v24.i46.5271. PubMed PMID: 30581275; PubMed Central PMCID: PMC6295839. 11: Hidaka H, Kurosaki M, Tanaka H, Kudo M, Abiru S, Igura T, Ishikawa T, Seike M, Katsube T, Ochiai T, Kimura K, Fukuhara T, Kano T, Nagata T, Tanaka K, Kurokawa M, Yamamoto K, Osaki Y, Izumi N, Imawari M. Lusutrombopag Reduces Need for Platelet Transfusion in Patients With Thrombocytopenia Undergoing Invasive Procedures. Clin Gastroenterol Hepatol. 2019 May;17(6):1192-1200. doi: 10.1016/j.cgh.2018.11.047. Epub 2018 Nov 28. PubMed PMID: 30502505. 12: Katano T, Sanada Y, Okada N, Mizuta K. Lusutrombopag as pretreatment for liver biopsy following liver transplantation. Pediatr Int. 2018 Nov;60(11):1033-1034. doi: 10.1111/ped.13698. Epub 2018 Oct 30. PubMed PMID: 30375132. 13: Tateishi R, Seike M, Kudo M, Tamai H, Kawazoe S, Katsube T, Ochiai T, Fukuhara T, Kano T, Tanaka K, Kurokawa M, Yamamoto K, Osaki Y, Izumi N, Imawari M. A randomized controlled trial of lusutrombopag in Japanese patients with chronic liver disease undergoing radiofrequency ablation. J Gastroenterol. 2019 Feb;54(2):171-181. doi: 10.1007/s00535-018-1499-2. Epub 2018 Aug 13. PubMed PMID: 30105510; PubMed Central PMCID: PMC6349796. 14: Yoshida H, Yamada H, Nogami W, Dohi K, Kurino-Yamada T, Sugiyama K, Takahashi K, Gahara Y, Kitaura M, Hasegawa M, Oshima I, Kuwabara K. Development of a new knock-in mouse model and evaluation of pharmacological activities of lusutrombopag, a novel, nonpeptidyl small-molecule agonist of the human thrombopoietin receptor c-Mpl. Exp Hematol. 2018 Mar;59:30-39.e2. doi: 10.1016/j.exphem.2017.12.005. Epub 2017 Dec 20. PubMed PMID: 29274361. 15: Fujita M, Abe K, Hayashi M, Okai K, Takahashi A, Ohira H. Two cases of liver cirrhosis treated with lusutrombopag before partial splenic embolization. Fukushima J Med Sci. 2017 Dec 19;63(3):165-171. doi: 10.5387/fms.2017-07. Epub 2017 Nov 15. PubMed PMID: 29142151; PubMed Central PMCID: PMC5792501. 16: Kotani S, Kohge N, Tsukano K, Ogawa S, Yamanouchi S, Kusunoki R, Aimi M, Miyaoka Y, Fujishiro H. Avoidance of platelet transfusion with readministration of lusutrombopag before radiofrequency ablation in hepatocellular carcinoma:a case report. Nihon Shokakibyo Gakkai Zasshi. 2017;114(10):1853-1859. doi: 10.11405/nisshoshi.114.1853. Japanese. PubMed PMID: 28978885. 17: Sato S, Miyake T, Kataoka M, Isoda K, Yazaki T, Tobita H, Ishimura N, Kinoshita Y. Efficacy of Repeated Lusutrombopag Administration for Thrombocytopenia in a Patient Scheduled for Invasive Hepatocellular Carcinoma Treatment. Intern Med. 2017 Nov 1;56(21):2887-2890. doi: 10.2169/internalmedicine.8791-16. Epub 2017 Sep 25. PubMed PMID: 28943563; PubMed Central PMCID: PMC5709632. 18: Sakamaki A, Watanabe T, Abe S, Kamimura K, Tsuchiya A, Takamura M, Kawai H, Yamagiwa S, Terai S. Lusutrombopag increases hematocytes in a compensated liver cirrhosis patient. Clin J Gastroenterol. 2017 Jun;10(3):261-264. doi: 10.1007/s12328-017-0735-2. Epub 2017 Mar 21. PubMed PMID: 28324272; PubMed Central PMCID: PMC5429890. 19: Katsube T, Ishibashi T, Kano T, Wajima T. 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. PubMed PMID: 27209291. 20: Kim ES. Lusutrombopag: First Global Approval. Drugs. 2016 Jan;76(1):155-8. doi: 10.1007/s40265-015-0525-4. PubMed PMID: 26666417.