Platelet‐derived endothelial cell growth factor Pharmacokinetics, organ distribution and degradation after intravenous administration in rats

FEBS Letters

Usuki, Kensuke²  Heldin, Carl-Henrik²  Waltenberger, Johannes²  Fellström, Bengt¹  Funa, Keiko² 

[1] Department of Internal Medicine, University Hospital, S-75124 Uppsala, Sweden;Ludwig Institute for Cancer Research, Uppsala Branch, University Hospital, S-75124 Uppsala, Sweden

关键词: Angiogenesis;    Platelet-derived endothelial cell growth factor;    Re-endothelialization of blood vessel;    Pharmacokinetics;    Thymidine phosphorylase;    Chemotherapy;   

DOI  :  10.1016/0014-5793(92)81428-O

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

Platelet-derived endothelial cell growth factor (PD-ECGF) stimulates chemotaxis of endothelial cells in vitro and has angiogenic activity in vivo. Recently PD-ECGF was shown to have thymidine phosphorylase activity. In order to study possible therapeutic applications of PD-ECGF we used a rat model to determine its pharmacokinetics and tissue distribution after intravenous injection. [¹²⁵I]PD-ECGF disappeared from the plasma in a biphasic manner, with estimated distribution and elimination half-lives of 17 min and 7 h, respectively. PD-ECGF was metabolized in the liver, excreted via the bile, and not accumulated in any organ system. The stability and long half-life in the circulation, together with the specificity for endothelial cells, suggest that PD-ECGF may be useful as a therapeutic agent to stimulate re-endothelialization in vivo, or, in view of its thymidine phosphorylase activity, in chemotherapy, by decreasing the pool of available thymidine.

【 授权许可】

Unknown