Related Experiment Video
Updated: Feb 15, 2026

Manual Restraint and Common Compound Administration Routes in Mice and Rats
Published on: September 26, 2012
Pharmacokinetics, tissue distribution, and excretion of FGF-21 following subcutaneous administration in rats
Yufei He1, Yazhuo Li2, Zihong Wei2
1Shenyang Pharmaceutical University, Shenyang, China.
Abstract:
As one of the fibroblast growth factor (FGF) superfamily, FGF-21 has been extensively investigated for its functions and roles since its discovery. It has been demonstrated to be one of the key regulators for glucose and lipid metabolism, and exhibits beneficial effects on cardiovascular disease. However, studies focusing on its pharmacokinetic behavior in vivo as a novel therapeutic agent have not been reported. In the present study, rapid and sensitive analytical approaches including radioactivity assay and assay after precipitation/separation by high performance liquid chromatography (HPLC) were established to determine the content of FGF-21 tagged with 125 I in plasma, tissue, and excrement. The results indicated that FGF-21 were quickly absorbed into systematic circulation and slowly eliminated; Cmax and exposure increased in a dose-dependent manner, exhibiting a typical linear pharmacokinetic pattern. Tissue distribution also confirmed that the kidney is the primary organ for FGF-21 to be distributed, even though radioactivity of FGF-21 was recovered in all tissues examined. In addition, the results also supported that urinary excretion was the critical route for FGF-21 to be eliminated. The study fully clarifies the pharmacokinetic behavior of FGF-21 and can provide valuable information and support further safety and toxicology development.
Insights
Fibroblast growth factor 21 (FGF-21) shows linear pharmacokinetics, with rapid absorption and slow elimination. The kidney is the primary distribution organ, and urinary excretion is the main elimination route.
Area of Science:
- Biochemistry
- Pharmacology
- Endocrinology
Background:
- Fibroblast growth factor 21 (FGF-21) is a key regulator of glucose and lipid metabolism.
- FGF-21 demonstrates potential therapeutic benefits for cardiovascular disease.
- Pharmacokinetic data for FGF-21 in vivo is currently lacking.
Purpose of the Study:
- To establish analytical methods for quantifying FGF-21.
- To elucidate the in vivo pharmacokinetic profile of FGF-21.
- To provide data for future safety and toxicology studies.
Main Methods:
- Development of radioactivity assay and HPLC-based methods.
- Quantification of 125I-labeled FGF-21 in plasma, tissues, and excrement.
- Analysis of absorption, distribution, metabolism, and excretion (ADME) properties.
Main Results:
- FGF-21 exhibited rapid systemic absorption and slow elimination.
- Pharmacokinetics followed a linear, dose-dependent pattern (Cmax and exposure).
- The kidney was the primary tissue for FGF-21 distribution; urinary excretion was the main elimination route.
Conclusions:
- The study successfully characterized the in vivo pharmacokinetic behavior of FGF-21.
- Findings indicate linear pharmacokinetics and highlight the kidney's role in distribution and urine in elimination.
- This research provides crucial data supporting the development of FGF-21 as a therapeutic agent.
Related Concept Videos
Pharmacokinetics in Pediatric Patients: Drug Excretion
Pharmacokinetics in Geriatric Patients: Effect of Age on Drug Excretion
Pharmacokinetics in Obese Patients: Drug Metabolism and Excretion
Pharmacokinetics in Pediatric Patients: Drug Distribution
Pharmacokinetics in Geriatric Patients: Effect of Age on Drug Distribution
Pharmacokinetics in Obese Patients: Drug Absorption and Distribution

