Aprepitant

Substance P/Neurokinin-1 Receptor Antagonist — ALIMENTARY TRACT AND METABOLISM

Key facts

Aprepitant is an ofp drug in the Substance P/Neurokinin-1 Receptor Antagonist class catalogued in DrugCentral. It was first approved by the FDA in 2003. Its mechanism of action is classified as Cytochrome P450 2C9 Inducers, Cytochrome P450 3A4 Inducers and Cytochrome P450 3A4 Inhibitors. DrugCentral lists 4 molecular targets, including TACR1, TACR1 and CYP3A4. Recorded indications include Chemotherapy-induced nausea and vomiting and Prevention of Post-Operative Nausea and Vomiting.

• Approval status: ofp (first approved 2003 by the FDA).
• Drug class: Substance P/Neurokinin-1 Receptor Antagonist.
• Mechanism of action: Cytochrome P450 2C9 Inducers; Cytochrome P450 3A4 Inducers; Cytochrome P450 3A4 Inhibitors.
• Molecular targets: TACR1, TACR1, CYP3A4 and TACR3 (4 listed in DrugCentral).
• Indications: Chemotherapy-induced nausea and vomiting and Prevention of Post-Operative Nausea and Vomiting.
• ATC code: A04AD12 (Other antiemetics).
• Molecular formula: C23H21F7N4O3; molecular weight 534.43 g/mol.

Indications & contraindications

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

Indications (2)

• Chemotherapy-induced nausea and vomiting
• Prevention of Post-Operative Nausea and Vomiting

Contraindications (1)

• Hepatic failure

Mechanism & targets

• Mechanism of action (MoA): Cytochrome P450 2C9 Inducers; Cytochrome P450 3A4 Inducers; Cytochrome P450 3A4 Inhibitors; Neurokinin 1 Antagonists
• Established pharmacologic class: Substance P/Neurokinin-1 Receptor Antagonist

Molecular targets (4)

Target	Gene	Action	Activity
Substance-P receptor	TACR1	antagonist	Ki 10.70
Substance-P receptor	TACR1	unknown	IC50 10.05
Cytochrome P450 3A4	CYP3A4	unknown	IC50 7.70
Neuromedin-K receptor	TACR3	unknown	Ki 6.34

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
2003-03-27	FDA	—	MERCK

ATC classification

ATC code	Therapeutic hierarchy
A04AD12	ALIMENTARY TRACT AND METABOLISM › ANTIEMETICS AND ANTINAUSEANTS › ANTIEMETICS AND ANTINAUSEANTS › Other antiemetics

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
Sleep disorder due to general medical condition, insomnia type	596.1
Folliculitis	530.8
Drug ineffective	528.2
Febrile neutropenia	501.9
Muscle injury	481.6
Helicobacter infection	453.7
Stomatitis	446.0
Impaired healing	440.8
Ill-defined disorder	434.7
Irritable bowel syndrome	427.2
Duodenal ulcer perforation	425.8
Gastrointestinal disorder	360.5

Chemical structure

• Molecular formula: C₂₃H₂₁F₇N₄O₃
• Molecular weight: 534.43 g/mol
• CAS number: —
• InChIKey: ATALOFNDEOCMKK-OITMNORJSA-N
• PubChem CID: 135413536

C[C@@H](O[C@H]1OCCN(CC2=NNC(=O)N2)[C@H]1C1=CC=C(F)C=C1)C1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F

Frequently asked questions

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

What is Aprepitant used for?

DrugCentral lists the following indications for Aprepitant: Chemotherapy-induced nausea and vomiting and Prevention of Post-Operative Nausea and Vomiting.

How does Aprepitant work?

Aprepitant is classified as Cytochrome P450 2C9 Inducers, Cytochrome P450 3A4 Inducers and Cytochrome P450 3A4 Inhibitors; its molecular targets in DrugCentral include TACR1 (antagonist), TACR1, CYP3A4 and TACR3.

When was Aprepitant first approved?

Aprepitant was first approved by the FDA in 2003.

What drug class does Aprepitant belong to?

Aprepitant is in the Substance P/Neurokinin-1 Receptor Antagonist class.

What is the chemical formula of Aprepitant?

Aprepitant has the molecular formula C23H21F7N4O3 and a molecular weight of 534.43 g/mol.

Sources

• DrugCentral drug card 230 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1201782 — compound record and bioactivity
• PubChem CID 135413536 — chemical identifiers
• DrugBank DB00673 — drug record
• FDA UNII 1NF15YR6UY — substance identity
• DailyMed: FDA labels for Aprepitant — current prescribing information (label search)
• UniProt P25103 (TACR1) — target protein
• UniProt P08684 (CYP3A4) — target protein
• UniProt P29371 (TACR3) — 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.