Drug intelligence / Profile preview

kpg-121 + apalutamide

Development stage
Unknown
Lead developer
Kangpu Biopharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

KPG-121 + apalutamide is a **combination therapy** consisting of KPG-121, a novel lenalidomide analogue and cereblon modulator, together with apalutamide, an androgen receptor antagonist. KPG-121 binds to the CRL4-Cereblon E3 ligase complex, promoting the rapid ubiquitination and degradation of casein kinase 1α (CK1α), as well as the transcription factors Aiolos (IKZF3) and Ikaros (IKZF1), resulting in immunomodulatory, anti-proliferative, and anti-angiogenic effects. Apalutamide antagonizes androgen receptor signaling, thereby inhibiting growth and survival of prostate cancer cells. This combination is being investigated primarily in **metastatic castration-resistant prostate cancer (mCRPC)**, with preclinical data showing enhanced anti-tumor activity when combining KPG-121 with apalutamide versus either agent alone. The developer of KPG-121 is Kangpu Biopharmaceuticals[1][2][3][5][8].

Brand names
Erleada (for apalutamide)
Other names
lenalidomide analogue + apalutamide
02

Targets

CK1α (Casein kinase I alpha)IKZF1 (Ikaros family zinc finger protein 1)AR (Adrenergic receptors)CRBN (Cereblon)IKZF3 (Zinc finger protein Aiolos)

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