| Width | 260px |
|---|---|
| Cas number | 2180923-05-9 |
| Pubchem | 137355972 |
| Drugbank | DB18054 |
| Chemspiderid | 103835872 |
| Unii | OSL3FEZ1IF |
| Synonyms | APG-2575 |
| Iupac name | 4-[4-[[8-(4-chlorophenyl)spiro[3.5]non-7-en-7-yl]methyl]piperazin-1-yl]-N-[4-[[(2S)-1,4-dioxan-2-yl]methylamino]-3-nitrophenyl]sulfonyl-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide |
| C | 45 |
| H | 48 |
| Cl | 1 |
| N | 7 |
| O | 8 |
| S | 1 |
| Smiles | C1CC2(C1)CCC(=C(C2)C3=CC=C(C=C3)Cl)CN4CCN(CC4)C5=CC(=C(C=C5)C(=O)NS(=O)(=O)C6=CC(=C(C=C6)NC[C@H]7COCCO7)[N+](=O)[O-])OC8=CN=C9C(=C8)C=CN9 |
| Stdinchi | InChI=1S/C45H48ClN7O8S/c46-33-4-2-30(3-5-33)39-25-45(12-1-13-45)14-10-32(39)28-51-16-18-52(19-17-51)34-6-8-38(42(23-34)61-35-22-31-11-15-47-43(31)49-26-35)44(54)50-62(57,58)37-7-9-40(41(24-37)53(55)56)48-27-36-29-59-20-21-60-36/h2-9,11,15,22-24,26,36,48H,1,10,12-14,16-21,25,27-29H2,(H,47,49)(H,50,54)/t36-/m0/s1 |
| Stdinchikey | FNBXDBIYRAPDPI-BHVANESWSA-N |
Lisaftoclax is an investigational new drug being developed by Ascentage Pharma for the treatment of hematological malignancies, particularly chronic lymphocytic leukemia (CLL) and small lymphocytic lymphoma (SLL). It is a selective inhibitor of the B-cell lymphoma 2 (BCL-2) protein, designed to restore the normal process of programmed cell death (apoptosis) in cancer cells.[1][2][3] As of 2024, lisaftoclax is undergoing multiple Phase 3 clinical trials, including studies in combination with BTK inhibitors for relapsed/refractory CLL/SLL.[2][4]
In July 2025, lisaftoclax was approved in China for the treatment of CLL or SLL in adult patients who had received at least one prior systemic therapy.[5]
References
- ^ Deng J, Paulus A, Fang DD, Manna A, Wang G, Wang H, Zhu S, Chen J, Min P, Yin Y, Dutta N, Halder N, Ciccio G, Copland JA, Miller J, Han B, Bai L, Liu L, Wang M, McEachern D, Przybranowski S, Yang CY, Stuckey JA, Wu D, Li C, Ryan J, Letai A, Ailawadhi S, Yang D, Wang S, Chanan-Khan A, Zhai Y (December 2022). "Lisaftoclax (APG-2575) Is a Novel BCL-2 Inhibitor with Robust Antitumor Activity in Preclinical Models of Hematologic Malignancy". Clinical Cancer Research. 28 (24): 5455–5468. doi:10.1158/1078-0432.CCR-21-4037. PMID 36048524
- ^ "FDA Grants Clearance for Phase 3 Study of Lisaftoclax in Previously Treated CLL/SLL". OncLive. 7 August 2023. Retrieved 2024-11-23.
- ^ "Ascentage Pharma Announces New Drug Application for Lisaftoclax". PR Newswire. Retrieved 2024-11-23.
- ^ "FDA Clears Phase 3 Trial of Lisaftoclax in CLL/SLL". Targeted Oncology. 8 August 2023. Retrieved 2024-11-23.
- ^ Syed YY (2025). "Lisaftoclax: First Approval". Drugs. 85 (12): 1635–1642. doi:10.1007/s40265-025-02251-4. PMID 41060518