molecules of the month


potent, selective, oral gamma-secretase modulator

PD effect on A-beta in model, well-tol. in 2 species

from optimization of prior ligand

ACS Med. Chem. Lett., May 1, 2020

Roche, Basel, CH

1 min read

RO7185876 is a gamma-secretase modulator (GSM) intended for treatment of Alzheimer’s disease. GSMs, which act by stabilizing the enzyme/substrate complex to promote generation of shorter peptides rather than inhibiting enzyme activity, and hence are anticipated to be less toxic than gamma-secretase inhibitors (GSI’s) which were abandoned due to serious safety liabilities. This compound competed two-week toxicology studies in two species (including one non-rodent), supporting its potential advancement to GLP tox. studies.

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