Last reviewed 2026-06-03 · How we verify

Lumateperone high dose

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

Lumateperone high dose is a 5-HT7 receptor antagonist / PDE10 inhibitor Small molecule drug developed by Intra-Cellular Therapies, Inc.. It is currently in Phase 3 development for Schizophrenia (phase 3), Bipolar depression (phase 3).

Lumateperone is a serotonin 5-HT7 receptor antagonist and phosphodiesterase 10 (PDE10) inhibitor that modulates dopamine and glutamate signaling in the brain.

Lumateperone is a small molecule serotonin 2a (5-HT2a) receptor antagonist used to treat conditions such as schizophrenia and irritability associated with autism spectrum disorder. It is administered in high and low doses as part of clinical trials.

Likelihood of approval

55.3% vs 58.3% industry baseline

If approved by FDA: likely 2028–2030

Steps remaining: NDA/BLA submission

Confidence: High

Why this estimate

Baseline phase 3 → approval rate +58.3pp
Industry-wide phase 3 drugs reach approval ~58.3% of the time (BIO/Informa 2023 industry benchmark across all therapeutic areas).
CNS / neurology attrition -3.0pp
CNS drugs have historically high Phase 3 failure rates (notably in Alzheimer disease + major depression).

Predicted approval windows by jurisdiction (conditional on FDA approval)

Regulator	Country	Likely year	Lag vs FDA
FDA	US	2028–2030	—
EMA	EU	2029–2031	+0.7 yr
MHRA	GB	2029–2031	+0.7 yr
Health Canada	CA	2029–2032	+0.9 yr
TGA	AU	2029–2032	+1.2 yr
PMDA	JP	2029–2032	+1.5 yr
NMPA	CN	2030–2033	+2.3 yr
MFDS	KR	2029–2032	+1.4 yr
CDSCO	IN	2029–2033	+1.8 yr
ANVISA	BR	2030–2033	+2.3 yr

Hover any row for the lag rationale. Lag estimates are reduced when the drug has FDA Breakthrough or EMA PRIME designation (sponsors file globally in parallel).

Estimate based on the BIO/Informa industry phase transition rates plus per-drug modifiers for therapeutic area, sponsor type, FDA designations, mechanism, and trial design. Per-jurisdiction lags from Tufts CSDD international approval studies. Not investment, clinical or regulatory advice. Methodology: /methodology#likelihood.

At a glance

Generic name	Lumateperone high dose
Sponsor	Intra-Cellular Therapies, Inc.
Drug class	5-HT7 receptor antagonist / PDE10 inhibitor
Target	5-HT7 receptor, PDE10
Modality	Small molecule
Therapeutic area	Psychiatry / Neurology
Phase	Phase 3

Mechanism of action

Lumateperone works through dual mechanisms: antagonism of 5-HT7 receptors and inhibition of PDE10, which together reduce excessive glutamate signaling and normalize dopamine neurotransmission. This combination is thought to address both positive and negative symptoms of psychosis while potentially improving cognitive function. The high-dose formulation is being evaluated to optimize therapeutic efficacy in treatment-resistant conditions.

Approved indications

Schizophrenia (phase 3)
Bipolar depression (phase 3)

Common side effects

Nausea
Headache
Somnolence
Akathisia
Weight gain

Key clinical trials

Primary sources

Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.

Source	Used for
ClinicalTrials.gov	Trial enrolment, design, endpoints, results

Competitive intelligence

For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:

Lumateperone high dose CI brief — competitive landscape report
Lumateperone high dose updates RSS · CI watch RSS
Intra-Cellular Therapies, Inc. portfolio CI

Frequently asked questions about Lumateperone high dose

What is Lumateperone high dose?

Lumateperone high dose is a 5-HT7 receptor antagonist / PDE10 inhibitor drug developed by Intra-Cellular Therapies, Inc., indicated for Schizophrenia (phase 3), Bipolar depression (phase 3).

How does Lumateperone high dose work?

Lumateperone is a serotonin 5-HT7 receptor antagonist and phosphodiesterase 10 (PDE10) inhibitor that modulates dopamine and glutamate signaling in the brain.

What is Lumateperone high dose used for?

Lumateperone high dose is indicated for Schizophrenia (phase 3), Bipolar depression (phase 3).

Who makes Lumateperone high dose?

Lumateperone high dose is developed by Intra-Cellular Therapies, Inc. (see full Intra-Cellular Therapies, Inc. pipeline at /company/intra-cellular-therapies-inc).

What drug class is Lumateperone high dose in?

Lumateperone high dose belongs to the 5-HT7 receptor antagonist / PDE10 inhibitor class. See all 5-HT7 receptor antagonist / PDE10 inhibitor drugs at /class/5-ht7-receptor-antagonist-pde10-inhibitor.

What development phase is Lumateperone high dose in?

Lumateperone high dose is in Phase 3.

What are the side effects of Lumateperone high dose?

Common side effects of Lumateperone high dose include Nausea, Headache, Somnolence, Akathisia, Weight gain.

What does Lumateperone high dose target?

Lumateperone high dose targets 5-HT7 receptor, PDE10 and is a 5-HT7 receptor antagonist / PDE10 inhibitor.

Drug class: All 5-HT7 receptor antagonist / PDE10 inhibitor drugs
Target: All drugs targeting 5-HT7 receptor, PDE10
Manufacturer: Intra-Cellular Therapies, Inc. — full pipeline
Therapeutic area: All drugs in Psychiatry / Neurology
Indication: Drugs for Schizophrenia (phase 3)
Indication: Drugs for Bipolar depression (phase 3)

Primary sources · FDA · ClinicalTrials.gov · EMA · SEC EDGAR · ChEMBL · Wikidata · full sourcing