Several classes of ASBT inhibitors were synthesized and evaluated in both in vitro assays and animal models.  To minimize the potential side effects caused by systematic drug circulation, efforts were made to identify gastrointestinally (GI)-restricted ASBT inhibitors for the treatment of type 2 diabetes. A panel of parameters, including potency, selectivity, permeability, solubility, stability, and fecal drug recovery were used in the optimization and selection process.   One of the GI-restricted ASBT inhibitors, GSK2330672, was identified as a highly potent, non-absorbable ASBT inhibitor with excellent drug development properties.

Synthesis and evaluation of non-absorbable ASBT inhibitors for the treatment of type 2 diabetes

246th National Meeting (2013)

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