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ITI-007 (Lumateperone)

Intra-Cellular Therapies, Inc. · Phase 3 active Small molecule

Lumateperone is a serotonin 5-HT7 receptor antagonist and phosphodiesterase 1 inhibitor that modulates intracellular signaling pathways implicated in psychosis and mood disorders.

Lumateperone is a serotonin 5-HT7 receptor antagonist and phosphodiesterase 1 inhibitor that modulates intracellular signaling pathways implicated in psychosis and mood disorders. Used for Schizophrenia (acute and maintenance treatment), Bipolar disorder (in development).

At a glance

Generic nameITI-007 (Lumateperone)
SponsorIntra-Cellular Therapies, Inc.
Drug classSerotonin 5-HT7 receptor antagonist / Phosphodiesterase 1 inhibitor
Target5-HT7 receptor, PDE1
ModalitySmall molecule
Therapeutic areaPsychiatry / Neurology
PhasePhase 3

Mechanism of action

ITI-007 works through a dual mechanism: it antagonizes 5-HT7 receptors and inhibits phosphodiesterase 1 (PDE1), leading to modulation of intracellular cAMP signaling. This mechanism is proposed to address both positive and negative symptoms of schizophrenia while potentially reducing extrapyramidal side effects associated with dopamine antagonism, as it does not directly block dopamine D2 receptors at therapeutic doses.

Approved indications

Common side effects

Key clinical trials

Primary sources

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SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results

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