GSK2793660

GSK2793660 is an oral, irreversible inhibitor of cathepsin C (CTSC), a lysosomal cysteine protease essential for the activation of several serine proteases including neutrophil elastase (NE), cathepsin G, and proteinase 3. By inhibiting CTSC, GSK2793660 was hypothesized to provide an alternative route to NE inhibition. The drug demonstrated potent and selective inhibition of CTSC in preclinical studies and Phase I clinical trials in healthy volunteers. However, only modest reductions were observed in downstream serine proteases' activity. Notably, repeated dosing led to palmar–plantar epidermal desquamation in most subjects—suggesting a role for CTSC or its targets in skin integrity. Developed by GlaxoSmithKline (now known as GSK), the compound was investigated primarily for bronchiectasis but development has been discontinued[1][3][4][5].

Other names

2H-pyran-4-carboxamide 4-amino-N-((1S,2E)-4-(2,3-dihydro-1H-indol-1-yl)but-2-enyl)-5-methyl-, hydrochloride