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Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
BIO-5192 is a highly selective and potent (KD of <10 pM) inhibitor of integrin alpha 4 beta 1. The high affinity
for integrin alpha 4 beta 1 results from an extremely slow dissociation rate of
the inhibitor from the integrin/inhibitor complex, with a dissociation
half-life of >12 h for both the unactivated and
activated integrin. Preclinical trials in multiple sclerosis in USA were underway, but no recent development of BIO-5192 or its pegylated form has been reported; it appears that development has been discontinued.