FDA Approved Ph 2/3 Study of KPG-121 + Abiraterone combination as 1L Treatment for metastatic CRPC
“Discovered by Kangpu Biopharmaceuticals, KPG-121 is a modulator of the Cereblon (CRBN) E3 ubiquitin ligase complex CRL4CRBN targeting rapid ubiquitination and degradation of casein kinase 1α (CK1α) and transcription factors Aiolos (IKZF3) and Ikaros (IKZF1). KPG-121 promotes anti-proliferation and anti-angiogenesis activities and enhances immunomodulatory properties. KPG-121 significantly improves anti-tumor efficacies when combined with androgen-receptor antagonists including enzalutamide, abiraterone acetate, apalutamide, or darolutamide in xenograft models when compared to the androgen-receptor antagonist therapy alone. A Phase I study to evaluate the safety, pharmacokinetics, and efficacy of KPG-121 when combined with enzalutamide, abiraterone, or apalutamide for the treatment of patients with metastatic or non-metastatic castration-resistant prostate cancer was completed in the US (NCT03569280). KPG-121 was generally well tolerated and demonstrated a favorable pharmacokinetic profile as well as promising efficacy.”
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