Lumateperone

Atypical Antipsychotic — NERVOUS SYSTEM

Key facts

Lumateperone is an onp drug in the Atypical Antipsychotic class catalogued in DrugCentral. It was first approved by the FDA in 2019. DrugCentral lists 10 molecular targets, including HTR2A, ADRA1B and Drd2. Recorded indications include Schizophrenia.

• Approval status: onp (first approved 2019 by the FDA).
• Drug class: Atypical Antipsychotic.
• Molecular targets: HTR2A, ADRA1B, Drd2 and DRD2 (10 listed in DrugCentral).
• Indications: Schizophrenia.
• ATC code: N05AD10 (Butyrophenone derivatives).
• Molecular formula: C24H28FN3O; molecular weight 393.51 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (1)

• Schizophrenia

Mechanism & targets

• Established pharmacologic class: Atypical Antipsychotic

Molecular targets (10)

Target	Gene	Action	Activity
5-hydroxytryptamine receptor 2A	HTR2A	antagonist	Ki 9.26
Alpha-1B adrenergic receptor	ADRA1B	unknown	Ki 7.51
D(2) dopamine receptor	Drd2	unknown	Ki 7.50
D(2) dopamine receptor	DRD2	antagonist	Ki 7.49
Sodium-dependent serotonin transporter	SLC6A4	unknown	Ki 7.48
D(1A) dopamine receptor	DRD1	antagonist	Ki 7.38
Alpha-1A adrenergic receptor	ADRA1A	unknown	Ki 7.14
D(4) dopamine receptor	DRD4	unknown	Ki 6.97
5-hydroxytryptamine receptor 2C	HTR2C	unknown	Ki 6.76
5-hydroxytryptamine receptor 1A	HTR1A	unknown	Ki 5.83

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
2019-12-20	FDA	—	INTRA-CELLULAR

ATC classification

ATC code	Therapeutic hierarchy
N05AD10	NERVOUS SYSTEM › PSYCHOLEPTICS › ANTIPSYCHOTICS › Butyrophenone derivatives

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Mania	711.9
Dizziness	572.1
Tardive dyskinesia	540.2
Sedation	486.1
Akathisia	467.2
Burning sensation	374.4
Somnolence	298.7
Suicidal ideation	243.4
Skin burning sensation	219.3
Headache	208.0
Nausea	195.1
Unevaluable event	156.4

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Lumateperone is on its molecule page.

• Molecular formula: C₂₄H₂₈FN₃O
• Molecular weight: 393.51 g/mol
• CAS number: 313368-91-1
• InChIKey: HOIIHACBCFLJET-SFTDATJTSA-N
• PubChem CID: 21302490

CN1CCN2[C@H]3CCN(CCCC(=O)C4=CC=C(F)C=C4)C[C@H]3C3=C2C1=CC=C3

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Lumateperone used for?

DrugCentral lists the following indications for Lumateperone: Schizophrenia.

How does Lumateperone work?

Its molecular targets in DrugCentral include HTR2A (antagonist), ADRA1B, Drd2 and DRD2 (antagonist).

When was Lumateperone first approved?

Lumateperone was first approved by the FDA in 2019.

What drug class does Lumateperone belong to?

Lumateperone is in the Atypical Antipsychotic class.

What is the chemical formula of Lumateperone?

Lumateperone has the molecular formula C24H28FN3O and a molecular weight of 393.51 g/mol.

Sources

• DrugCentral drug card 5358 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL3233142 — compound record and bioactivity
• PubChem CID 21302490 — chemical identifiers
• DrugBank DB06077 — drug record
• FDA UNII 70BSQ12069 — substance identity
• DailyMed: FDA labels for Lumateperone — current prescribing information (label search)
• UniProt P28223 (HTR2A) — target protein
• UniProt P35368 (ADRA1B) — target protein
• UniProt P14416 (DRD2) — target protein
• UniProt P31645 (SLC6A4) — target protein
• UniProt P21728 (DRD1) — target protein
• UniProt P35348 (ADRA1A) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.