This invention relates to inhibition of αv integrins, especially αvβ3 and αvβ6 integrins, by specific antagonists, preferably non-peptidic antagonists, related compounds and compounds with comparable specificity, that downregulate fibrogenesis by inhibiting
cell migration and production of pro-fibrogenic molecules (e.g., collagens, TIMP-1) and cytokines (e.g.,
CTGF) by activated hepatic stellate cells / myofibroblasts, activated epithelia and endothelia. These antagonists alone or in combination with other agents can effectively prevent, mitigate or even reverse development of advanced
fibrosis, such as
fibrosis /
cirrhosis of the liver and
fibrosis of other organs, such as lungs, kidneys, intestine,
pancreas,
skin and arteries.