KPG-818 is a novel generation of small molecule modulators of CRBN E3 ubiquitin ligase complex CRL4-CRBN. It provides a potent induction of the ubiquitination and degradation of Aiolos (IKZF3) and Ikaros (IKZF1), two members of the Ikaros family of zinc-finger transcription factors critical in B-cell development. KPG-818 demonstrated outstanding in vitro anti-inflammatory properties and a broad spectrum of anti-proliferative activities as well as remarkable in vivo efficacy in animal models of multiple blood cancers. In the first-in-human Phase Ia single ascending dose (SAD) clinical study and the Phase Ib clinical study in SLE patients completed in the US, KPG-818 was well tolerated at all tested dose levels and demonstrated a favorable pharmacokinetic profile. KPG-818 is currently being developed in a Phase I study for the treatment of patients with hematological malignancies and a Phase Ib/IIa study for the treatment of patients with Systemic Lupus Erythematosus (SLE) in the United States (NCT04283097 and NCT04643067).

KPG-121 is a novel modulator of the Cerebron (CRBN) E3 ubiquitin ligase complex CRL4^CRBN targeting rapid ubiquitination and degradation of casein kinase 1A1 (CK1α) and transcription factors Aiolos and Ikaros. 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. KPG-121 has finished a Phase I study in the US for the treatment of patients with metastatic and non-metastatic castration-resistant prostate cancer in combination with Enzalutamide, Abiraterone Acetate, or Apalutamide (NCT03569280).

This compound belongs to a novel class of small molecules targeting the CRBN E3 ubiquitin ligase complex CRL4^CRBN with the potential to address the unmet medical needs in hematological malignancies relapsed or refractory to current SOC treatments.

KPG-419 is a next-generation of the CRBN E3 ubiquitin ligase complex CRL4^CRBN modulator enabling efficient down-regulation of transcription factors Aiolos and Ikaros. The compound possesses excellent anti-angiogenesis activity in the HUVEC model.

KPG-419 is being developed by Kangpu Biopharmaceuticals for the treatment of cancer.

KP-0696S represents a class of novel chemical entities designed to tune substrate specificity of the CRBN E3 ubiquitin ligase complex CRL4^CRBN with the aim of treating solid tumors.

KPG-712 is a small molecule PDE4 inhibitor with strong target binding affinity. PDE4 is a type-4 phosphodiesterase that hydrolyzes cAMP in immune cells. PDE4 inhibitors block the hydrolyzation of phosphodiesterase 4 on cyclic adenosine monophosphate and have the potential to treat diseases by reversing certain signals in the immune system that cause disease flares.

 KPG-712 is currently being developed by Kangpu Biopharmaceuticals for the treatment of inflammatory and auto-immune disorders.