Why the study?
SPH3127 is a novel direct renin inhibitor approved for hypertension in China, but its pharmacokinetics, mass balance, and biotransformation in humans required characterization.
What are the pharmacokinetics, mass balance, and metabolism of a single oral dose of [14C]SPH3127 in healthy Chinese male subjects?
Comparison
Single 100 mg oral dose of [14C]SPH3127 (100 μCi)
Design
Isotope labeling pharmacokinetic and mass balance study
Follow-up
192 h
Key result
A single 100 mg oral dose of SPH3127 was rapidly absorbed and extensively metabolized, with a mean cumulative excreted radioactivity of 101.66% primarily through feces (57.31%) and urine (44.35%).
Authors
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Healthy volunteer PK data warrant no practice change; leaves open efficacy testing of SPH3127 in hypertension.
What are the pharmacokinetics, mass balance, and metabolism of a single oral dose of [14C]SPH3127 in healthy Chinese male subjects?
SPH3127 (sitokiren), a novel direct renin inhibitor, demonstrates rapid absorption and balanced elimination via urine and feces in healthy Chinese males.
Ma et al. (2026) studied Healthy volunteers (n=6). [14C]SPH3127 (sitokiren) was evaluated on Mean cumulative excreted radioactivity at 192 hours. A single 100 mg oral dose of SPH3127 was rapidly absorbed and extensively metabolized, with a mean cumulative excreted radioactivity of 101.66% primarily through feces (57.31%) and urine (44.35%).
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