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) |
|
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 |
|
gDAC-S |
Degrader-Antibody Conjugate |
Solid Tumors |
|
gDAC-H |
Degrader-Antibody Conjugate |
Hematological Malignancies |
|
gDAC-A |
Degrader-Antibody Conjugate |
Auto-immune Diseases |
|
Oncology Auto-immune Diseases
KPG-818
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
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
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.