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migoprotafib
- Development stage
- Discontinued
- Lead developer
- Relay Therapeutics
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Migoprotafib (GDC-1971) is an orally available, potent, and selective small-molecule inhibitor of the protein tyrosine phosphatase SHP2 (PTPN11). It binds to an allosteric site on SHP2, stabilizing the enzyme in a closed, inactive conformation. By inhibiting SHP2 activity, migoprotafib blocks RAS/MAPK signal transduction downstream of growth factor receptor activation and inhibits the MAPK/ERK signaling pathway. This mechanism results in antitumor activity by suppressing cellular proliferation in models with receptor tyrosine kinase (RTK), SHP2, or KRAS mutations. Migoprotafib is being developed for use as a single agent and in combination with KRAS inhibitors such as divarasib (GDC‑6036) for the treatment of solid tumors driven by KRAS G12C mutations.
- Brand names
- migoprotafib
- Other names
- migoprotafib
02
Targets
PTPN11 (Tyrosine-protein phosphatase non-receptor type 11)
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