ZJCK-6-72: Pharmacokinetics and Safety Data for a Novel Alzheimer's Drug Candidate

ZJCK-6-72, a novel DYRK1A inhibitor, demonstrated an oral bioavailability of 78.03% and a brain-to-plasma ratio up to 4.63 in rats. The study, authored by Zhenshu Li and shared under a CC-BY-4.0 license on figshare in 2026, includes in vitro and in vivo ADMET profiling. It reports an acute toxicity LD50 of 233.9 mg/kg and identifies CYP1A2 and CYP2C19 as primary metabolic pathways.

Use Cases

• Modeling brain exposure for CNS-targeted drugs based on reported brain-to-plasma ratios and unbound partition coefficients.
• Assessing drug-drug interaction potential based on the described CYP1A2 and CYP2C19 inhibition data.
• Evaluating safety margins for novel therapeutics using the reported acute toxicity LD50 value.
• Benchmarking oral bioavailability and tissue distribution parameters for preclinical drug candidates.

Strengths

• Report includes specific, quantitative pharmacokinetic results such as 78.03% oral bioavailability and a brain-to-plasma ratio of 1.92 to 4.63.
• Provides concrete safety data including an acute toxicity LD50 of 233.9 mg/kg and enzyme inhibition IC50 values.
• Data is shared under a permissive CC-BY-4.0 license, allowing for broad reuse.

Limitations

• The dataset is a 291.2 KB DOCX file, suggesting it is likely a textual report or summary rather than raw, structured experimental data.
• Row count and column-level documentation are absent, limiting direct analysis of underlying data points.
• Data is from a single, non-peer-reviewed source on figshare; methodological details are summarized rather than exhaustively documented.

Provenance

Source

figshare

Collection Method

In vitro and in vivo ADMET profiling conducted as part of a pharmacological study.

Freshness

Last updated 2026-05-01 05:24:30.