Orelabrutinib

Catalog No: 25116

CAS Number: 1655504-04-3

Purity: 98% Min.

Orelabrutinib, also known as ICP-022, is a potent, orally active, and irreversible Bruton's tyrosine kinase (BTK) inhibitor, being developed by InnoCare Pharma, for the treatment of chronic lymphocytic leukaemia.

For research use only. We do not sell to patients.

Chemical Information

Name	Orelabrutinib
Iupac Chemical Name	2-(4-phenoxyphenyl)-6-[1-(prop-2-enoyl)piperidin- 4-yl]pyridine-3-carboxamide
Synonyms	Orelabrutinib; ICP-022; ICP022; ICP 022;
Molecular Formula	C26H25N3O3
Molecular Weight	427.50
Smile	O=C(C1=CC=C(C2CCN(C(C=C)=O)CC2)N=C1C3=CC=C(OC4=CC=CC=C4)C=C3)N
InChiKey	MZPVEMOYADUARK-UHFFFAOYSA-N
InChi	InChI=1S/C26H25N3O3/c1-2-24(30)29-16-14-18(15-17-29)23-13-12-22(26(27)31)25(28-23)19-8-10-21(11-9-19)32-20-6-4-3-5-7-20/h2-13,18H,1,14-17H2,(H2,27,31)
CAS Number	1655504-04-3
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Formulation	Off-white solid
Purity	98% Min.
Storage	Dry, dark and at 0 - 4℃ for short term (days to weeks) or -20℃ for long term (months to years).
Solubility	Soluble in DMSO
Handling
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.
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Targets
Mechanism
Cell study
Animal study
Clinical study

1: Gao YH, Duan MH, Li J, Zhang L. Successful treatment of relapsed idiopathic multicentric Castleman disease-idiopathic plasmacytic lymphadenopathy with orelabrutinib monotherapy: A case report. Br J Haematol. 2024 Jun 10. doi: 10.1111/bjh.19596. Epub ahead of print. PMID: 38859582.

2: Xu M, Xu Y, Yuan L, Shang D, Chen R, Liu S, Li Y, Liu A, Liu R, Wang Q, Ding T, Xie Q, Hao CM. Case report: BTK inhibitors is effective in type II mixed cryoglobulinemia with wild-type MyD88. Front Immunol. 2024 May 3;15:1390958. doi: 10.3389/fimmu.2024.1390958. PMID: 38765016; PMCID: PMC11099222.

3: Schaff L, Nayak L, Grommes C. Bruton's tyrosine kinase (BTK) inhibitors for the treatment of primary central nervous system lymphoma (PCNSL): current progress and latest advances. Leuk Lymphoma. 2024 Jul;65(7):882-894. doi: 10.1080/10428194.2024.2333985. Epub 2024 Apr 10. PMID: 38597202.

4: Yan S, Zhou H, Huang R, Wang F, Mei H, Lin L, Guo J, Zhou X, Li Z, Liu Y, Li S, Zhou W, Hou Y, Hou M. A phase 2 trial of orelabrutinib showing promising efficacy and safety in patients with persistent or chronic primary immune thrombocytopenia. Am J Hematol. 2024 Jul;99(7):1392-1395. doi: 10.1002/ajh.27303. Epub 2024 Mar 28. PMID: 38546375.

5: Deng T, Zhang S, Xiao M, Gu J, Huang L, Zhou X. A single-centre, real-world study of BTK inhibitors for the initial treatment of MYD88mut /CD79Bmut diffuse large B-cell lymphoma. Cancer Med. 2024 Feb;13(4):e7005. doi: 10.1002/cam4.7005. PMID: 38457222; PMCID: PMC10923040.

6: Wu C, Chen S, Wu Z, Xue J, Zhang W, Wang S, Xindong Zhao, Wu S. Chidamide and orelabrutinib synergistically induce cell cycle arrest and apoptosis in diffuse large B-cell lymphoma by regulating the PI3K/AKT/mTOR pathway. J Cancer Res Clin Oncol. 2024 Feb 21;150(2):98. doi: 10.1007/s00432-024-05615-7. PMID: 38381215; PMCID: PMC10881688.

7: Guo XL, Zhao ZY, Guo XF, Zuo YB, Li JA, Nie ZY, Ren JH. Effectiveness and safety of orelabrutinib with rituximab and lenalidomide in low KPS score and elderly patients with newly diagnosed primary central nervous system lymphoma-a single-center retrospective study. Neurol Sci. 2024 Jun;45(6):2931-2934. doi: 10.1007/s10072-024-07348-4. Epub 2024 Feb 7. PMID: 38326666.

8: Xie Y, Qu S, Liao LS, Zheng ZH, Lin Y, Chen WM, Chen BY. [Evaluation of the Short-Term Efficacy and Safety of Orelabrutinib Combined with High-Dose Methotrexate in the First-line Treatment of Elderly Patients with High Risk Primary Central Nervous System Lymphoma]. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2023 Dec;31(6):1714-1719. Chinese. doi: 10.19746/j.cnki.issn.1009-2137.2023.06.017. PMID: 38071050.

9: Liu H, Ding K, Zhang W, Xing L, Wang Y, Wang H, Song J, Li L, Fu R. A pilot study of orelabrutinib treatment in three cases of refractory/relapsed autoimmune haemolytic anaemia/Evans syndrome. Br J Haematol. 2024 Mar;204(3):1082-1085. doi: 10.1111/bjh.19146. Epub 2023 Nov 6. PMID: 37932927.

10: Li Y, Li Y, Zeng R, He Y, Liang L, Ou L, Su C, Zhou H, Xiao L. High-dose methotrexate, thiotepa, orelabrutinib combined with or without rituximab in primary or secondary central nervous system diffuse large B-cell lymphoma: a single-center retrospective analysis. J Cancer. 2023 Sep 25;14(17):3182-3190. doi: 10.7150/jca.85756. PMID: 37928429; PMCID: PMC10622989.

11: Wei R, Wu Y, Jiang S, Zhang A, Zhang L, Liu L, Wang Y, Zhang M, Mei H, Liu F, Xia L, Cui G, Fang J. Efficacy and safety of Orelabrutinib-based regimens in diffuse large B-cell lymphoma: a single-center retrospective analysis. Clin Exp Med. 2023 Dec;23(8):4609-4621. doi: 10.1007/s10238-023-01231-w. Epub 2023 Nov 4. PMID: 37925380; PMCID: PMC10725366.

12: Huang F, Ruan Y, He X, Lian H, Yang J. Clinicopathologic and mutational profiles of primary breast diffuse large B cell lymphoma in a male patient: case report and literature review. World J Surg Oncol. 2023 Oct 26;21(1):342. doi: 10.1186/s12957-023-03234-z. Erratum in: World J Surg Oncol. 2023 Dec 12;21(1):382. doi: 10.1186/s12957-023-03259-4. PMID: 37884941; PMCID: PMC10601260.

13: Song Y, Wu SJ, Shen Z, Zhao D, Chan TSY, Huang H, Qiu L, Li J, Tan TD, Zhu J, Song Y, Huang WH, Zhao W, Liu HSY, Xu W, Chen N, Ma J, Chang CS, Tse EWC. Chinese expert consensus on Bruton tyrosine kinase inhibitors in the treatment of B-cell malignancies. Exp Hematol Oncol. 2023 Oct 16;12(1):92. doi: 10.1186/s40164-023-00448-5. PMID: 37845755; PMCID: PMC10578030.

14: Shang Y, Zhao H, Li D. Effect and Safety of Orelabrutinib and Lenalidomide Plus R-mini CDOP in Relapsed/Refractory Aggressive B-cell Non-Hodgkin Lymphoma. Turk J Haematol. 2023 Dec 5;40(4):284-285. doi: 10.4274/tjh.galenos.2023.2023.0263. Epub 2023 Sep 1. PMID: 37656047; PMCID: PMC10701323.

15: Deng L, Li Z, Zhang H, Huang H, Hu J, Liu L, Liu T, Jin J, Zhu Z, Li W, Huang Z, Huang W, Zhou K, Yang H, Zhang M, Ding K, Zhou H, Hu Y, Shuang Y, Cao J, Gao S, Li D, Sun Z, Zhang Q, Yi S, Ji C, Zhang L, Hou C, Du Y, Wang W, Zhao R, Song Y, Zhu J. Orelabrutinib for the treatment of relapsed or refractory marginal zone lymphoma: A phase 2, multicenter, open-label study. Am J Hematol. 2023 Nov;98(11):1742-1750. doi: 10.1002/ajh.27064. Epub 2023 Aug 30. PMID: 37647123.

16: Zhou Y, Wang X, Lin X, Wang J, Yan X, Wen Y. Sustained response following BTK inhibitors based treatment in HIV-related primary central nervous system lymphoma: case report. AIDS Res Ther. 2023 Aug 29;20(1):63. doi: 10.1186/s12981-023-00554-8. PMID: 37644480; PMCID: PMC10466696.

17: Robak P, Witkowska M, Wolska-Washer A, Robak T. The preclinical discovery and development of orelabrutinib as a novel treatment option for B-cell lymphoid malignancies. Expert Opin Drug Discov. 2023 Jul-Dec;18(10):1065-1076. doi: 10.1080/17460441.2023.2236547. Epub 2023 Jul 13. PMID: 37438969.

18: Song Y, Zhou K, Yang S, Hu J, Zou D, Gao S, Pan L, Wang T, Yang H, Zhang H, Zhou D, Ji J, Xu W, Feng R, Jin J, Lv F, Huang H, Fan X, Xu S, Zhu J. Indirect comparisons of efficacy of zanubrutinib versus orelabrutinib in patients with relapsed or refractory chronic lymphocytic leukemia/small lymphocytic lymphoma or relapsed or refractory mantle cell lymphoma. Invest New Drugs. 2023 Aug;41(4):606-616. doi: 10.1007/s10637-023-01376-1. Epub 2023 Jul 8. PMID: 37420136; PMCID: PMC10447591.

19: Qiao L, Liu Q, Huang C. Orelabrutinib versus ibrutinib for patients with refractory/relapsed primary central nervous system lymphoma: An efficacy and safety analysis. Medicine (Baltimore). 2023 Jul 7;102(27):e33880. doi: 10.1097/MD.0000000000033880. PMID: 37417642; PMCID: PMC10328710.

20: Zhao Y, Guo YJ, Chen XL, Yang YL, Ma H, Wang YQ, Sun LN. Determination of Orelabrutinib in Human Plasma Using LC-MS/MS. Ther Drug Monit. 2023 Oct 1;45(5):599-605. doi: 10.1097/FTD.0000000000001106. Epub 2023 May 5. PMID: 37199420.

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25116 - Orelabrutinib | CAS 1655504-04-3

Orelabrutinib

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