Drug intelligence / Profile preview

Lu AF90103

Development stage
Phase 1
Lead developer
Lundbeck
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

Lu AF90103 (also known as compound 42e) is a methyl ester prodrug of compound 42d, developed to penetrate the blood-brain barrier. Compound 42d acts as a partial agonist at the GluN1/GluN2B complex of the NMDA receptor, with approximately 24% efficacy and an EC50 value of 78 nM. Lu AF90103 was designed to provide rapid and sustained antidepressant effects by targeting NMDA receptors, specifically aiming for fast-onset antidepressant activity without the psychotomimetic side effects associated with ketamine. The drug was developed by H. Lundbeck A/S and reached phase I clinical trials for depression but has since been discontinued[1][2][3][7].

Other names
42e
02

Targets

GluR (Glutamate receptors)

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