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Bitopertin

investig.

Pronunciation: bye-toe-PER-tin

Bitopertin ballicule: receptor binding, kinetics and half-life diagram
Mechanism of action: Bitopertin ballicule

What it isGlycine transporter type 1 inhibitor; failed in schizophrenia, now studied in erythropoietic protoporphyria.

Why this oneRaising synaptic glycine was the leading strategy for NMDA hypofunction in schizophrenia.

What limits itThe phase 3 schizophrenia program failed, which reframed the whole glycine hypothesis. Investigational only.

Bitopertin molecular structure (skeletal formula)
Molecular structure: Bitopertin

FDA-approved for

Off-label

NO BOXED WARNINGS

Principal riskThe schizophrenia program failed in phase 3

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4
Sedation liability2 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism0 / 4

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