Asenapine

Atypical Antipsychotic — NERVOUS SYSTEM

Key facts

Asenapine is an ofp drug in the Atypical Antipsychotic class catalogued in DrugCentral. It was first approved by the FDA in 2009. DrugCentral lists 30 molecular targets, including HTR2C, HTR2B and HTR2A. Recorded indications include Bipolar affective disorder, current episode manic, Mixed bipolar I disorder and Schizophrenia.

• Approval status: ofp (first approved 2009 by the FDA).
• Drug class: Atypical Antipsychotic.
• Molecular targets: HTR2C, HTR2B, HTR2A and HTR7 (30 listed in DrugCentral).
• Indications: Bipolar affective disorder, current episode manic, Mixed bipolar I disorder and Schizophrenia.
• ATC code: N05AH05 (Diazepines, oxazepines, thiazepines and oxepines).
• Molecular formula: C17H16ClNO; molecular weight 285.77 g/mol.

Indications & contraindications

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

Indications (3)

• Bipolar affective disorder, current episode manic
• Mixed bipolar I disorder
• Schizophrenia

Off-label uses (1)

• Depression Treatment Adjunct

Contraindications (35)

• Agranulocytosis
• Alzheimer's disease
• At risk for aspiration
• Bradycardia
• Cerebrovascular accident
• Cerebrovascular disease
• Congenital long QT syndrome
• Dehydration
• Diabetes mellitus
• Dysphagia
• Esophageal dysmotility
• Hepatic failure
• Hyperglycemia
• Hyperprolactinemia
• Hypokalemia
• Hypomagnesemia
• Hypovolemia
• Impaired cognition
• Leukopenia
• Lowered convulsive threshold
• Myocardial infarction
• Myocardial ischemia
• Neuroleptic malignant syndrome
• Neutropenic disorder
• Obesity
• Orthostatic hypotension
• Prolonged QT interval
• Seizure disorder
• Senile dementia with psychosis
• Suicidal thoughts
• + 5 more

Mechanism & targets

• Established pharmacologic class: Atypical Antipsychotic

Molecular targets (30)

Target	Gene	Action	Activity
5-hydroxytryptamine receptor 2C	HTR2C	unknown	Ki 9.93
5-hydroxytryptamine receptor 2B	HTR2B	unknown	Ki 9.80
5-hydroxytryptamine receptor 2A	HTR2A	antagonist	Ki 9.61
5-hydroxytryptamine receptor 7	HTR7	unknown	Ki 9.47
5-hydroxytryptamine receptor 6	HTR6	unknown	Ki 9.22
D(3) dopamine receptor	DRD3	unknown	Ki 9.06
Histamine H1 receptor	HRH1	unknown	Ki 9.00
Alpha-1A adrenergic receptor	ADRA1A	unknown	Ki 8.92
D(2) dopamine receptor	DRD2	antagonist	Ki 8.75
Alpha-2B adrenergic receptor	ADRA2B	unknown	Ki 8.73
D(4) dopamine receptor	DRD4	unknown	Ki 8.71
D(1A) dopamine receptor	DRD1	unknown	Ki 8.70
5-hydroxytryptamine receptor 5A	HTR5A	unknown	Ki 8.60
Alpha-1B adrenergic receptor	ADRA1B	unknown	Ki 8.41
5-hydroxytryptamine receptor 1D	HTR1D	agonist	Ki 8.40
5-hydroxytryptamine receptor 1B	HTR1B	unknown	Ki 8.40
Histamine H2 receptor	HRH2	unknown	IC50 8.21
Alpha-2A adrenergic receptor	ADRA2A	unknown	Ki 8.19
5-hydroxytryptamine receptor 1E	HTR1E	agonist	Ki 8.00
5-hydroxytryptamine receptor 1A	HTR1A	unknown	Ki 7.97

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
2009-08-13	FDA	—	FOREST LABS INC

ATC classification

ATC code	Therapeutic hierarchy
N05AH05	NERVOUS SYSTEM › PSYCHOLEPTICS › ANTIPSYCHOTICS › Diazepines, oxazepines, thiazepines and oxepines

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
Anosognosia	1722.1
Blood prolactin abnormal	1695.2
Disturbance in social behaviour	1589.0
Sexual dysfunction	1420.2
Sedation	1386.8
Dystonia	1380.7
Suicide attempt	1340.3
Metabolic disorder	1323.4
Personality change	1218.8
Dyskinesia	1088.3
Akathisia	1063.9
Hypoaesthesia oral	742.9

Chemical structure

• Molecular formula: C₁₇H₁₆ClNO
• Molecular weight: 285.77 g/mol
• CAS number: 65576-45-6
• InChIKey: VSWBSWWIRNCQIJ-UHFFFAOYSA-N
• PubChem CID: 163091

CN1CC2C(C1)C1=C(OC3=C2C=CC=C3)C=CC(Cl)=C1

Frequently asked questions

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

What is Asenapine used for?

DrugCentral lists the following indications for Asenapine: Bipolar affective disorder, current episode manic, Mixed bipolar I disorder and Schizophrenia.

How does Asenapine work?

Its molecular targets in DrugCentral include HTR2C, HTR2B, HTR2A (antagonist) and HTR7.

When was Asenapine first approved?

Asenapine was first approved by the FDA in 2009.

What drug class does Asenapine belong to?

Asenapine is in the Atypical Antipsychotic class.

What is the chemical formula of Asenapine?

Asenapine has the molecular formula C17H16ClNO and a molecular weight of 285.77 g/mol.

Sources

• DrugCentral drug card 4115 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL3187365 — compound record and bioactivity
• PubChem CID 163091 — chemical identifiers
• DrugBank DB06216 — drug record
• FDA UNII JKZ19V908O — substance identity
• DailyMed: FDA labels for Asenapine — current prescribing information (label search)
• UniProt P28335 (HTR2C) — target protein
• UniProt P41595 (HTR2B) — target protein
• UniProt P28223 (HTR2A) — target protein
• UniProt P34969 (HTR7) — target protein
• UniProt P50406 (HTR6) — target protein
• UniProt P35462 (DRD3) — 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.