Lisaftoclax

Lisaftoclax
Clinical data
Other names	APG-2575
Identifiers
	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;
CAS Number	2180923-05-9;
PubChem CID	137355972;
UNII	OSL3FEZ1IF;
Chemical and physical data
Formula	C45H48ClN7O8S
Molar mass	882.43 g·mol−1
3D model (JSmol)	Interactive image;
	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;
	InChI InChI=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; Key: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]

References

^ Deng J, Paulus A, Fang DD, Manna A, Wang G, Wang H, et al. (December 2022). "Lisaftoclax (APG-2575) Is a Novel BCL-2 Inhibitor with Robust Antitumor Activity in Preclinical Models of Hematologic Malignancy". Clinical Cancer Research : an Official Journal of the American Association for Cancer Research. 28 (24): 5455–5468. doi:10.1158/1078-0432.CCR-21-4037. PMID 36048524.
^ ^a ^b "FDA Grants Clearance for Phase 3 Study of Lisaftoclax in Previously Treated CLL/SLL". OncLive. 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. Retrieved 2024-11-23.

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