Drug intelligence / Profile preview

KPG-121 + enzalutamide

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

Overview

KPG-121 + enzalutamide is an investigational **oral combination therapy** evaluated for treatment of **non-metastatic and metastatic castration-resistant prostate cancer (CRPC)**. KPG-121 is a novel small molecule and a next-generation **lenalidomide analogue** developed for potent immunomodulatory and anti-proliferative effects; it binds **CRL4-Cereblon (CRBN)**, yielding rapid degradation of **casein kinase 1α (CK1α)** and the transcription factors **Aiolos (IKZF3)** and **Ikaros (IKZF1)**, resulting in enhanced immunomodulation and anti-tumor activity. Enzalutamide is a well-established **androgen receptor antagonist** that blocks androgen receptor signaling, a key driver of prostate cancer growth. The combination has shown preclinical and early clinical synergy, with increased anti-tumor efficacy compared to monotherapy, and is under investigation particularly for **castration-resistant prostate cancer**[2][3][4].

Other names
KPG-121 plus enzalutamideKPG121 plus enzalutamideKPG 121 plus enzalutamideKPG-121 combined with enzalutamideKPG121 combined with enzalutamideKPG 121 combined with enzalutamide
02

Targets

CRBN (Cereblon)AR (Adrenergic receptors)CK1α (Casein kinase I alpha)

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