Chinese pharma company Kangpu Biopharmaceuticals said that it has wrapped up the first-in-human phase 1 clinical trial of CRL4-CRBN modulator KPG-818 in the US.

KPG-818 is being developed for the treatment of systemic lupus erythematosus (SLE) or hematological malignancies.

The single ascending dose (SAD) randomized, double-blind, placebo-controlled study assessed the safety, tolerability, and pharmacokinetics of KPG-818 in healthy male and female participants after oral administration of the investigational drug.

A total of 40 participants were randomly grouped to get placebo or the active drug in double-blind fashion. Five dose levels – 2, 5, 10, 20 and 30mg of KPG-818 were studied in the phase 1 clinical trial.

Kangpu Biopharmaceuticals said that there were no safety or tolerability concerns in the completed phase 1 study. No serious adverse incidents were observed at any studied dose level.

KPG-818 was well tolerated at all tested dose levels and also demonstrated a favorable pharmacokinetic profile that supports once-daily oral dosing.

The results also showed that dosing under fed conditions does not have any major influence on the exposure of KPG-818 as compared to fasted conditions.

Kangpu Biopharmaceuticals, with the study results, can find out the appropriate doses of KPG-818 that can be administrated in the upcoming clinical trials of the drug in patients with systemic lupus erythematosus or hematological malignancies.

KPG-818 is a small molecule modulator of CRL4-CRBN, CRBN E3 ubiquitin ligase complex. It is said to have shown outstanding in vitro anti-inflammatory and anti-proliferative properties and remarkable in vivo efficacy in myeloma and lymphoma animal models in preclinical studies.

Kangpu Biopharmaceuticals is a clinical-stage pharma company in Shangai. The Chinese pharma company is engaged in the discovery and development of small molecules for the treatments of solid tumors, hematological malignancies, auto-immune diseases, and inflammatory disorders through novel-generation solutions like targeted protein ubiquitination and degradation.

Kangpu Biopharmaceuticals has developed a drug combination technology called X-Synergy platform for the treatment of castration-resistant prostate cancer (CRPC/mCRPC).

  China, hematological malignancies, Kangpu Biopharmaceuticals, KPG-818, Shanghai, systemic lupus erythematosus, USA