Olverembatinib Explained
| Legal Status: | Investigational |
| Synonyms: | GZD-824; GZD824 |
| Cas Number: | 1257628-77-5 |
| Pubchem: | 51038269 |
| Unii: | KV1M7Q3CBP |
| Drugbank: | DB16185 |
| Chembl: | 2316582 |
| Chemspiderid: | 29395146 |
| Iuphar Ligand: | 10630 |
| Iupac Name: | 4-Methyl-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-3-[2-(1''H''-pyrazolo[3,4-''b'']pyridin-5-yl)ethynyl]benzamide |
| C: | 29 |
| H: | 27 |
| F: | 3 |
| N: | 6 |
| O: | 1 |
| Stdinchi: | 1S/C29H27F3N6O/c1-19-3-5-22(14-21(19)6-4-20-13-24-17-34-36-27(24)33-16-20)28(39)35-25-8-7-23(26(15-25)29(30,31)32)18-38-11-9-37(2)10-12-38/h3,5,7-8,13-17H,9-12,18H2,1-2H3,(H,35,39)(H,33,34,36) |
| Stdinchikey: | TZKBVRDEOITLRB-UHFFFAOYSA-N |
| Smiles: | CC1=C(C=C(C=C1)C(=O)NC2=CC(=C(C=C2)CN3CCN(CC3)C)C(F)(F)F)C#CC4=CC5=C(NN=C5)N=C4 |
Olverembatinib is a BCR-ABL1 tyrosine kinase inhibitor developed by Ascentage Pharma. In 2021, it was approved in China "for the treatment of adult patients with TKI-resistant chronic-phase CML (CML-CP) or accelerated-phase CML (CML-AP) harbouring the T315I mutation".[1] [2] [3]
Notes and References
- Dhillon . Sohita . Olverembatinib: First Approval . Drugs . March 2022 . 82 . 4 . 469–475 . 10.1007/s40265-022-01680-9. 35195876 . 247027755 .
- Jiang . Qian . Li . Zongru . Qin . Yazhen . Li . Weiming . Xu . Na . Liu . Bingcheng . Zhang . Yanli . Meng . Li . Zhu . Huanling . Du . Xin . Chen . Suning . Liang . Yang . Hu . Yu . Liu . Xiaoli . Song . Yongping . Men . Lichuang . Chen . Zi . Niu . Qian . Wang . Hengbang . Lu . Ming . Yang . Dajun . Zhai . Yifan . Huang . Xiaojun . Olverembatinib (HQP1351), a well-tolerated and effective tyrosine kinase inhibitor for patients with T315I-mutated chronic myeloid leukemia: results of an open-label, multicenter phase 1/2 trial . Journal of Hematology & Oncology . 18 August 2022 . 15 . 1 . 113 . 10.1186/s13045-022-01334-z . 35982483 . 9389804 . free .
- Jiang . Qian . Huang . Xiaojun . Chen . Zi . Niu . Qian . Shi . Dayu . Li . Zongru . Hou . Yue . Hu . Yu . Li . Weiming . Liu . Xiaoli . Xu . Na . Song . Yongping . Zhang . Yanli . Meng . Li . Hong . Zhenya . Liu . Bingcheng . Zeng . Shan . Men . Lichuang . Li . Yan . Chen . Suning . Xue . Mengxing . Zhu . Huanling . Li . He . Du . Xin . Lou . Jin . Zhang . Xiaohan . Liang . Yang . Dai . Yujun . Lu . Ming . Wang . Hengbang . Ji . Jiao . Yue . Changai . Yang . Dajun . Zhai . Yifan . Novel BCR-ABL1 Tyrosine Kinase Inhibitor (TKI) HQP1351 (Olverembatinib) Is Efficacious and Well Tolerated in Patients with T315I-Mutated Chronic Myeloid Leukemia (CML): Results of Pivotal (Phase II) Trials . Blood . 5 November 2020 . 136 . Supplement 1 . 50–51 . 10.1182/blood-2020-142142. 228875477 .
