KPG-818 is a novel generation of small molecule modulators of the CRBN E3 ubiquitin ligase complex CRL4-CRBN and potently induces 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. In preclinical studies, KPG-818 demonstrated outstanding in vitro anti-inflammatory properties and broad spectrum of anti-proliferative activities as well as remarkable in vivo efficacy in animal models of multiple blood cancers. In the Phase I single ascending dose (SAD) clinical study recently completed in the U.S., KPG-818 was well tolerated at all tested dose levels (2-30 mg) 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). In addition, KPG-818 has recently been approved by the FDA for a Phase IIa clinical trial in patients with COVID-19 infection in the U.S.

KPG-818 is a novel generation of small molecule modulators of the CRBN E3 ubiquitin ligase complex CRL4-CRBN and potently induces 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. In preclinical studies, KPG-818 demonstrated outstanding in vitro anti-inflammatory properties and broad spectrum of anti-proliferative activities as well as remarkable in vivo efficacy in animal models of multiple blood cancers. In the Phase I single ascending dose (SAD) clinical study recently completed in the U.S., KPG-818 was well tolerated at all tested dose levels (2-30 mg) 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). In addition, KPG-818 has recently been approved by the FDA for a Phase IIa clinical trial in patients with COVID-19 infection in the U.S.

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 is currently being evaluated in 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).

KPG-818 is a novel generation of small molecule modulators of the CRBN E3 ubiquitin ligase complex CRL4-CRBN and potently induces 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. In preclinical studies, KPG-818 demonstrated outstanding in vitro anti-inflammatory properties and broad spectrum of anti-proliferative activities as well as remarkable in vivo efficacy in animal models of multiple blood cancers. In the Phase I single ascending dose (SAD) clinical study recently completed in the U.S., KPG-818 was well tolerated at all tested dose levels (2-30 mg) 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). In addition, KPG-818 has recently been approved by the FDA for a Phase IIa clinical trial in patients with COVID-19 infection in the U.S.