Fezolinetant

Neurokinin 3 Receptor Antagonist — GENITO URINARY SYSTEM AND SEX HORMONES

Key facts

Fezolinetant is an onp drug in the Neurokinin 3 Receptor Antagonist class catalogued in DrugCentral. It was first approved by the FDA in 2023. Its mechanism of action is classified as Neurokinin 3 Receptor Antagonists. DrugCentral lists 2 molecular targets, including TACR3 and KCNH2. Recorded indications include Vasomotor symptoms due to menopause.

• Approval status: onp (first approved 2023 by the FDA).
• Drug class: Neurokinin 3 Receptor Antagonist.
• Mechanism of action: Neurokinin 3 Receptor Antagonists.
• Molecular targets: TACR3 and KCNH2 (2 listed in DrugCentral).
• Indications: Vasomotor symptoms due to menopause.
• ATC code: G02CX06 (Other gynecologicals).
• Molecular formula: C16H15FN6OS; molecular weight 358.40 g/mol.

Indications & contraindications

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

Indications (1)

• Vasomotor symptoms due to menopause

Contraindications (3)

• Cirrhosis of liver
• End stage renal disease
• Renal impairment

Mechanism & targets

• Mechanism of action (MoA): Neurokinin 3 Receptor Antagonists
• Established pharmacologic class: Neurokinin 3 Receptor Antagonist

Molecular targets (2)

Target	Gene	Action	Activity
Neuromedin-K receptor	TACR3	antagonist	Ki 7.60
Potassium voltage-gated channel subfamily H member 2	KCNH2	unknown	IC50 4.16

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
2023-05-12	FDA	—	ASTELLAS

ATC classification

ATC code	Therapeutic hierarchy
G02CX06	GENITO URINARY SYSTEM AND SEX HORMONES › OTHER GYNECOLOGICALS › OTHER GYNECOLOGICALS › Other gynecologicals

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
Alanine aminotransferase increased	464.0
Aspartate aminotransferase increased	315.2
Hepatic enzyme increased	236.7
Liver function test increased	174.2
Gamma-glutamyltransferase increased	104.7
Drug ineffective	82.3
Transaminases increased	62.7
Blood alkaline phosphatase increased	56.7
Hot flush	56.3

Chemical structure

• Molecular formula: C₁₆H₁₅FN₆OS
• Molecular weight: 358.40 g/mol
• CAS number: 1629229-37-3
• InChIKey: PPSNFPASKFYPMN-SECBINFHSA-N
• PubChem CID: 117604931

C[C@@H]1C2=NN=C(N2CCN1C(=O)C3=CC=C(C=C3)F)C4=NC(=NS4)C

Frequently asked questions

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

What is Fezolinetant used for?

DrugCentral lists the following indications for Fezolinetant: Vasomotor symptoms due to menopause.

How does Fezolinetant work?

Fezolinetant is classified as Neurokinin 3 Receptor Antagonists; its molecular targets in DrugCentral include TACR3 (antagonist) and KCNH2.

When was Fezolinetant first approved?

Fezolinetant was first approved by the FDA in 2023.

What drug class does Fezolinetant belong to?

Fezolinetant is in the Neurokinin 3 Receptor Antagonist class.

What is the chemical formula of Fezolinetant?

Fezolinetant has the molecular formula C16H15FN6OS and a molecular weight of 358.40 g/mol.

Sources

• DrugCentral drug card 5729 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL3608680 — compound record and bioactivity
• PubChem CID 117604931 — chemical identifiers
• DrugBank DB15669 — drug record
• FDA UNII 83VNE45KXX — substance identity
• DailyMed: FDA labels for Fezolinetant — current prescribing information (label search)
• UniProt P29371 (TACR3) — target protein
• UniProt Q12809 (KCNH2) — 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.