Development of LHRH antagonists suitable for oral administration via the VB12 uptake system

G. J. Russell-Jones*, S. W. Westwood, B. McInerney, P. G. Farnworth, J. K. Findlay, H. G. Burger

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

1 Citation (Scopus)


Preliminary research has shown that it is possible to make two analogues of ANTIDE, ANTIDE-1 and ANTIDE-3 that have activities similar to ANTIDE in the rat pituitary cell assay. Direct conjugation of these analogues to VB12 dramatically reduced the bio-activity of either analogue. Conjugation of either ANTIDE-1 or ANTIDE-3 to VB12 via extended spacers regenerated their in vitro activity, however their in vivo activity was still greatly diminished. Conjugation of either analogue to VB12 via thiol cleavable spacers gave rise to analogues with similar in vitro and in vivo bio-activity to ANTIDE.

Original languageEnglish
Pages (from-to)35-36
Number of pages2
JournalProceedings of the Controlled Release Society
Issue number21
Publication statusPublished - 12 Dec 1994
Externally publishedYes


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