Drug intelligence / Profile preview

lisaftoclax + palbociclib

Development stage
Unknown
Lead developer
Ascentage Pharma
Modality
Small Molecules
Administration
Oral
01

Overview

Lisaftoclax + palbociclib is an investigational combination therapy under clinical evaluation for the treatment of estrogen receptor-positive, human epidermal growth factor receptor 2-negative (ER+/HER2-) metastatic breast cancer. Lisaftoclax (APG-2575) is a novel, potent, selective small-molecule inhibitor of B-cell lymphoma 2 (BCL-2), designed to induce apoptosis in cancer cells that overexpress BCL-2 proteins. Palbociclib is a well-established oral small-molecule inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), which blocks cell cycle progression from G1 to S phase, thereby inhibiting tumor cell proliferation. Preclinical studies have shown complementary effects when these agents are combined, supporting their use together in patients whose disease has progressed or relapsed after prior CDK4/6 inhibitor therapy. The combination is being evaluated in global multicenter phase Ib/II trials for safety and efficacy[1][2].

Brand names
Ibrance
Other names
lisaftoclax and palbociclibAPG-2575 and palbociclibAPG2575 and palbociclibAPG 2575 and palbociclib
02

Targets

BCL-2 (BCL-2 family)CDK6 (Cyclin-dependent kinase 6)CDK4 (Cyclin-dependent kinase 4)

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