Rifampin
Contraindicated
Textbook
Reduced AUC by >95%, leading to loss of efficacy.
Cannot be taken with CYP3A4 inducers.
Source: G&G 14e · p368
Drug reference
lumateperone
second-generation antipsychotic · Antipsychotic
second-generation antipsychoticAntipsychotic
CDSCO approved
EXCRETION
—
not curated
INTERACTIONS
12 major
incl. contraindicated
PREGNANCY
C
FDA category + note
Top interactionssee all 12 →
- RifampinContraindicatedTextbookG&G 14e · p368
- AlfentanilSevereDatabaseDDInter
- AminoglutethimideSevereDatabaseDDInter
- AmobarbitalSevereDatabaseDDInter
Mechanism
Lumateperone is a 5HT2a and D2 antagonist. Its antidepressant mechanisms include a combination of 5HT2A antagonism and D1 activation.
Indications
Schizophreniabipolar depression (monotherapy and adjunct)
Dosing
- Adult
- 42 mg (oral). Must be given with 350 kcal food to facilitate absorption. Administration with evening meal improves tolerability.
Pharmacokinetics
Peak effect
1–2 h
Bioavailability
4.4%
Metabolism
CYP3A4 is the primary pathway. UGT1A4 is involved in phase 2 metabolism. Lumateperone is not a Pgp or BCRP substrate.
Contraindications
- Cannot be taken with CYP3A4 inducers
- cannot be used with CYP3A4 inhibitors or UGT inhibitors
- use in elderly dementia patients (increased mortality risk)
Side effects
Common
Very low risk for anticholinergic side effectsvery low risk for sedationvery low risk for weight gainvery low risk for hypotensionvery low risk of EPSsvery low risk of metabolic and endocrine adverse effects
Serious
- Neuroleptic malignant syndrome
- increased mortality in elderly dementia patients
Pregnancy & lactation
Pregnancy
C
Lactation
Not specified
Drug interactions
Alfentanil
Severe
Database
Drug interaction classified as: synergy
Source: DDInter
Aminoglutethimide
Severe
Database
Drug interaction classified as: metabolism
Source: DDInter
Amobarbital
Severe
Database
Drug interaction classified as: metabolism
Source: DDInter
Amprenavir
Severe
Database
Drug interaction classified as: metabolism
Source: DDInter
Apalutamide
Severe
Database
Drug interaction classified as: metabolism
Source: DDInter
Aprepitant
Severe
Database
Drug interaction classified as: metabolism
Source: DDInter
Armodafinil
Severe
Database
Drug interaction classified as: metabolism
Source: DDInter
Atazanavir
Severe
Database
Drug interaction classified as: metabolism
Source: DDInter
Benzhydrocodone
Severe
Database
Drug interaction classified as: synergy
Source: DDInter
Berotralstat
Severe
Database
Drug interaction classified as: metabolism
Source: DDInter
Bexarotene
Severe
Database
Drug interaction classified as: metabolism
Source: DDInter
Related guidelines
Other second-generation antipsychotic drugs
Ask House about lumateperone
Continue into a citation-backed clinical answer with the drug context already attached.
Sources: Goodman & Gilman 14e·Verified: 2026-05-10 · House clinical team