Kangpu Biopharmaceuticals’ R&D program is exclusively focused on the discovery and development of novel and effective therapies that address significant unmet medical needs worldwide.
| PROGRAM | MOA | INDICATION | PRECLINICAL | IND | PHASE I | PHASE II |
|---|---|---|---|---|---|---|
| KPG-818 | CRL4-CRBN Modulator | Systemic Lupus Erythematosus (SLE) | ||||
| Inflammatory Bowel Disease (lBD) | ||||||
| Behcet's Disease (BD) | ||||||
| Multiple Myeloma (MM) | ||||||
| Non-Hodgkin Lymphoma (NHL) | ||||||
| KPG-121 | CRL4-CRBN Modulator | Metastatic Castration-Resistant Prostate Cancer (mCRPc) | ||||
| KP-09S | CRL4-CRBN Modulator | Hematological Malignancies | ||||
| DAC-1 | Molecular Glue-Antibody Dual-targeting |
Solid Tumors | ||||
| DAC-2 | Molecular Glue-Antibody Dual-targeting |
Hematological Malignancies | ||||
| DAC-3 | Molecular Glue-Antibody Dual-targeting |
Autoimmune Diseases | ||||
KPG-818 is a small molecule immunomodulator of Cereblon (CRBN) E3 ubiquitin ligase complex CRL4-CRBN, designed and developed by Kangpu Biopharmaceuticals. It provides a potent induction of the ubiquitination and degradation of Aiolos (IKZF3) and Ikaros (IKZF1). KPG-818 demonstrated outstanding in vitro anti-inflammatory properties, a broad spectrum of anti-proliferative activities, and remarkable in vivo efficacy in multiple blood cancer animal models. In the first-in-human Phase Ia single ascending dose (SAD) clinical study, and the Phase Ib/IIa clinical studies in SLE patients (NCT04643067) completed in the US, KPG-818 was well tolerated and demonstrated a favorable pharmacokinetic profile as well as promising efficacy. A bridge study (CTR20241116) for the treatment of SLE has been initiated in China. Meanwhile, KPG-818 is currently being developed in a Phase I/II study for the treatment of patients with hematological malignancies in the U.S. (NCT04283097).
KPG-121 is a modulator of the Cereblon (CRBN) E3 ubiquitin ligase complex CRL4-CRBN targeting rapid ubiquitination and degradation of casein kinase 1A1 (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 U.S. (NCT03569280). KPG-121 was well tolerated and demonstrated a favorable pharmacokinetic profile as well as promising efficacy.
KP-09S belongs to a novel class of molecular glues targeting the CRBN E3 ubiquitin ligase complex CRL4-CRBN with great potential for the treatment of relapsed/refractory hematological malignancies.
