Biotransformation and disposition characteristics of HSK7653 , a novel long‐acting dipeptidyl peptidase‐4 inhibitor for the treatment of type 2 diabetes
Authors' conclusion
HSK7653 was well absorbed, slightly metabolized and slowly excreted in humans. The high plasma exposure and long t1/2 of HSK7653 may contribute to its long-lasting efficacy as a long-acting dipeptidyl peptidase-4 inhibitor.
Study context
- Population
- Healthy male Chinese participants
- Participants
- 6 participants
- Outcome
- Metabolism and disposition (PK, blood-to-plasma ratio, mass balance, metabolism) of HSK7653
Methodological detailssingle oral dose, [14C]-radiolabelled
- Single oral dose
- [14C]-radiolabelled
Main finding
As reported in the abstract
Pharmacokinetics, mass balance and metabolism of HSK7653
- Time to maximum concentration
- 1.25 h
- t1/2 of drug-related components
- 111 h
- Unchanged HSK7653 share of total plasma radioactivity
- more than 97%
- Blood-to-plasma ratio (no tendency to distribute into blood cells)
- 0.573-0.845
- Dose excreted at 504 h postdose
- up to 95.9%
- Excreted in urine
- 79.8%
- Excreted in faeces
- 16.1%
- Radioactivity in excreta as unchanged HSK7653
- 75.5% dose
- Metabolites detected in urine and faeces
- 9
- Most abundant metabolite M6-2 (dioxidation product), % of dose in urine
- 4.73%
- Most abundant metabolite M6-2 (dioxidation product), % of dose in faeces
- 2.63%
Original publication
Biotransformation and disposition characteristics of HSK7653 , a novel long‐acting dipeptidyl peptidase‐4 inhibitor for the treatment of type 2 diabetes. Diabetes Obes Metab. Published 22 April 2024. doi:10.
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