Drug intelligence / Profile preview

APG-2575 + lenalidomide + dexamethasone

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

Overview

APG-2575 + lenalidomide + dexamethasone is a combination therapy under clinical investigation for the treatment of relapsed or refractory multiple myeloma. - **APG-2575 (lisaftoclax)** is an oral, small molecule inhibitor targeting BCL-2, a protein that prevents apoptosis in cancer cells, thus promoting programmed cell death in BCL-2 dependent hematologic malignancies. - **Lenalidomide** is an oral immunomodulatory drug (IMiD) that inhibits proliferation of myeloma cells, supports immune surveillance by stimulating T and NK cells, and impedes blood vessel formation that supplies the myeloma. - **Dexamethasone** is a synthetic corticosteroid used to reduce inflammation and suppress immune responses in the treatment of hematologic malignancies[1][3][5]. The combination exploits the complementary mechanisms of BCL-2 inhibition, immune modulation, and anti-inflammatory activity to overcome resistance to standard therapies in relapsed/refractory multiple myeloma[1][3][5].

02

Targets

BCL-2 (BCL-2 family)GR (Glucocorticoid receptor)RELA (Nuclear Factor Kappa B Subunit p65)CD28 (Cluster of Differentiation 28)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)CRBN (Cereblon)

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