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GS-1148569
- Development stage
- Preclinical
- Lead developer
- Gilead Sciences
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
GS-1148569 is a small molecule antagonist of the lysophosphatidic acid receptor 1 (LPAR1) developed by Gilead Sciences. LPAR1 activation is implicated in tissue fibrosis, promoting epithelial cell injury and myofibroblast proliferation. In preclinical models of diabetic kidney disease (DKD), including rat adenine-induced tubulointerstitial injury and mouse db/db eNos -/- glomerulosclerosis, GS-1148569 has demonstrated the ability to reduce tubulointerstitial fibrosis, decrease global glomerular sclerosis, and preserve kidney function. It also blocks LPA-induced myocardin-related transcription factor A (MRTFA) nuclear translocation and profibrotic gene expression in kidney fibroblasts, mesangial cells, and tubular epithelial cells.
02
Targets
LPAR1 (Lysophosphatidic acid receptor 1)
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