Fosaprepitant

Substance P/Neurokinin-1 Receptor Antagonist

Key facts

Fosaprepitant 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 Neurokinin 1 Antagonists. DrugCentral lists 1 molecular target, including TACR1. Recorded indications include Chemotherapy-induced nausea and vomiting.

• Approval status: ofp (first approved 2003 by the FDA).
• Drug class: Substance P/Neurokinin-1 Receptor Antagonist.
• Mechanism of action: Neurokinin 1 Antagonists.
• Molecular targets: TACR1 (1 listed in DrugCentral).
• Indications: Chemotherapy-induced nausea and vomiting.
• Molecular formula: C23H22F7N4O6P; molecular weight 614.41 g/mol.

Indications & contraindications

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

Indications (1)

• Chemotherapy-induced nausea and vomiting

Contraindications (1)

• Hepatic failure

Mechanism & targets

• Mechanism of action (MoA): Neurokinin 1 Antagonists
• Established pharmacologic class: Substance P/Neurokinin-1 Receptor Antagonist

Molecular targets (1)

Target	Gene	Action	Activity
Substance-P receptor	TACR1	antagonist	IC50 8.92

Regulatory approvals (1)

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

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
Febrile neutropenia	493.4
Drug ineffective	459.8
Sleep disorder due to general medical condition, insomnia type	369.4
Folliculitis	303.3
Ill-defined disorder	284.0
Stomatitis	276.0
Duodenal ulcer perforation	265.8
Muscle injury	261.8
Impaired healing	261.4
Porphyria acute	257.6
Fall	239.2
Helicobacter infection	239.1

Chemical structure

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

• Molecular formula: C₂₃H₂₂F₇N₄O₆P
• Molecular weight: 614.41 g/mol
• CAS number: —
• InChIKey: BARDROPHSZEBKC-OITMNORJSA-N
• PubChem CID: 135413538

C[C@@H](O[C@H]1OCCN(CC2=NN(C(=O)N2)P(O)(O)=O)[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 Fosaprepitant used for?

DrugCentral lists the following indications for Fosaprepitant: Chemotherapy-induced nausea and vomiting.

How does Fosaprepitant work?

Fosaprepitant is classified as Neurokinin 1 Antagonists; its molecular targets in DrugCentral include TACR1 (antagonist).

When was Fosaprepitant first approved?

Fosaprepitant was first approved by the FDA in 2003.

What drug class does Fosaprepitant belong to?

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

What is the chemical formula of Fosaprepitant?

Fosaprepitant has the molecular formula C23H22F7N4O6P and a molecular weight of 614.41 g/mol.

Sources

• DrugCentral drug card 4470 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1199324 — compound record and bioactivity
• PubChem CID 135413538 — chemical identifiers
• DrugBank DB06717 — drug record
• FDA UNII 6L8OF9XRDC — substance identity
• DailyMed: FDA labels for Fosaprepitant — current prescribing information (label search)
• UniProt P25103 (TACR1) — 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.