fezolinetant 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| neurokinin NK3 and dual NK3-NK1 receptor antagonists | 5729 | 1629229-37-3 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Fezolinetant is a neurokinin 3 (NK3) receptor antagonist that blocks neurokinin B (NKB) binding on the kisspeptin/neurokinin B/dynorphin (KNDy) neuron to modulate neuronal activity in the thermoregulatory center. Fezolinetant has high affinity for the NK3 receptor (Ki value of 19.9 to 22.1 nmol/L), which is more than 450-fold higher than binding affinity to NK1 or NK2 receptors.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| May 12, 2023 | FDA | ASTELLAS |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | G02CX06 | GENITO URINARY SYSTEM AND SEX HORMONES OTHER GYNECOLOGICALS OTHER GYNECOLOGICALS Other gynecologicals |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Vasomotor symptoms due to menopause | indication | 123756000 | |
| Cirrhosis of liver | contraindication | 19943007 | DOID:5082 |
| End stage renal disease | contraindication | 46177005 | DOID:784 |
| Renal impairment | contraindication | 236423003 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
None
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| 45MG | VEOZAH | ASTELLAS | N216578 | May 12, 2023 | RX | TABLET | ORAL | 10836768 | March 28, 2034 | TREATMENT OF MODERATE TO SEVERE VASOMOTOR SYMPTOMS DUE WITH MENOPAUSE |
| 45MG | VEOZAH | ASTELLAS | N216578 | May 12, 2023 | RX | TABLET | ORAL | 9422299 | March 28, 2034 | TREATMENT OF MODERATE TO SEVERE VASOMETER SYMPTOMS DUE TO MENOPAUSE |
| 45MG | VEOZAH | ASTELLAS | N216578 | May 12, 2023 | RX | TABLET | ORAL | 9987274 | March 28, 2034 | TREATMENT OF MODERATE TO SEVERE VASOMETER SYMPTOMS DUE TO MENOPAUSE |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 45MG | VEOZAH | ASTELLAS | N216578 | May 12, 2023 | RX | TABLET | ORAL | May 12, 2028 | NEW CHEMICAL ENTITY |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Neuromedin-K receptor | GPCR | ANTAGONIST | Ki | 7.60 | SCIENTIFIC LITERATURE | DRUG LABEL |
External reference:
| ID | Source |
|---|---|
| CHEMBL3608680 | ChEMBL_ID |
| C000608808 | MESH_SUPPLEMENTAL_RECORD_UI |
| 10422 | IUPHAR_LIGAND_ID |
| DB15669 | DRUGBANK_ID |
| 019428 | NDDF |
| 4042266 | VANDF |
| C4547455 | UMLSCUI |
| 10205 | INN_ID |
| 117604931 | PUBCHEM_CID |
| 2637134 | RXNORM |
| D11976 | KEGG_DRUG |
| 83VNE45KXX | UNII |
| 367097 | MMSL |
| 41521 | MMSL |
| d10045 | MMSL |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| VEOZAH | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0469-2460 | TABLET, FILM COATED | 45 mg | ORAL | NDA | 27 sections |
| VEOZAH | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0469-2660 | TABLET, FILM COATED | 45 mg | ORAL | NDA | 27 sections |
| VEOZAH | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0469-2760 | TABLET, FILM COATED | 45 mg | ORAL | NDA | 27 sections |