Kangpu Biopharmaceuticals Successfully Completed Phase I Study of Novel CRL4-CRBN Modulator KPG-818 in the U.S.

On October 11, 2019 Kangpu Biopharmaceuticals reported that it has successfully completed a first-in-human phase I single ascending dose (SAD) clinical study of KPG-818 conducted in the United States (Press release, Kangpu Biopharmaceuticals, OCT 11, 2019, View Source [SID1234540934]).

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This randomized, double-blind, placebo-controlled study evaluated the safety, tolerability and pharmacokinetics (PK) of KPG-818 in healthy male and female participants following oral administration. A total of 40 subjects were randomized to receive active drug or placebo in a double-blind fashion (8 subjects in each dose cohort, 6 subjects randomized to receive active drug and 2 subjects randomized to receive placebo). Five dose levels (2, 5, 10, 20 and 30 mg) were investigated.

In the completed phase I study, there were no safety or tolerability concerns. No serious adverse events (SAE) were reported at any dose level studied. No stopping criteria were met. KPG-818 was well tolerated at all tested dose levels. KPG-818 also demonstrated a favorable pharmacokinetic profile supporting once-daily oral dosing. The phase I results also revealed that dosing under fed conditions does not have significant influence on the exposure of KPG-818 as compared to fasted conditions.

The study results will assist Kangpu Biopharmaceuticals in identifying appropriate doses of KPG-818 that can be administered in subsequent clinical trials in patients with systemic lupus erythematosus (SLE) or hematological malignancies.

About KPG-818

KPG-818 is a novel small molecule modulator of the CRBN E3 ubiquitin ligase complex CRL4-CRBN. In preclinical studies, KPG-818 demonstrated outstanding in vitro anti-inflammatory and anti-proliferative properties as well as remarkable in vivo efficacy in myeloma and lymphoma animal models. KPG-818 is currently being developed by Kangpu Biopharmaceuticals for the treatment of SLE and hematological malignancies.