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evocalcet 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| calcium-sensing receptors (CaSR) agonists | 5307 | 870964-67-3 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Evocalcet is a new type of oral calcimimetics agent. The drug suppresses parathyroid hormone secretion by acting on the calcium receptors on parathyroid gland cells.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 2.50 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BA (Bioavailability) | 0.63 % | Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,DYRK1B,EGFR,EIF2AK3,ERBB2,GRK2,ITK,MAP2K6,MAP3K7,MAPK10,MAPK14,MAPK7,MAPKAPK2,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PIM2,PRKDC,STK33,SYK,TEK,TGFBR1,ZAP70 | 32 | |||
| kinase-selectivity-class | AXL,EIF2AK3,GRK2 | 3 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| March 23, 2018 | PMDA | Kyowa Hakko Kirin Co., Ltd. |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Shunt stenosis | 68.43 | 52.99 | 8 | 88 | 551 | 90627800 |
| Shunt occlusion | 56.62 | 52.99 | 7 | 89 | 768 | 90627583 |
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Shunt stenosis | 87.72 | 57.55 | 12 | 156 | 765 | 42620402 |
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Shunt stenosis | 149.50 | 52.93 | 20 | 316 | 1396 | 110587567 |
| Shunt occlusion | 96.67 | 52.93 | 14 | 322 | 1723 | 110587240 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | H05BX06 | SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS CALCIUM HOMEOSTASIS ANTI-PARATHYROID AGENTS Other anti-parathyroid agents |
Related Drugs by ATC class:
H05BX Other anti-parathyroid agents 5 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Hypercalcemia in primary hyperparathyroidism | indication | 2243000 | |
| Hypercalcemia in parathyroid carcinoma | indication | 47709007 | |
| Secondary hyperparathyroidism | indication | 91478007 | DOID:12466 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 4.32 | acidic |
| pKa2 | 8.08 | Basic |
| pKa3 | 4.84 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Extracellular calcium-sensing receptor | GPCR | AGONIST | EC50 | 7.03 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE |
External reference:
| ID | Source |
|---|---|
| E58MLH082P | UNII |
| C4519114 | UMLSCUI |
| CHEBI:757091 | CHEBI |
| H43 | PDB_CHEM_ID |
| CHEMBL4297621 | ChEMBL_ID |
| 71242808 | PUBCHEM_CID |
| DB12388 | DRUGBANK_ID |
| D11063 | KEGG_DRUG |
| 10098 | INN_ID |
| C000631688 | MESH_SUPPLEMENTAL_RECORD_UI |
| 9042 | IUPHAR_LIGAND_ID |
| 020073 | NDDF |
| E58MLH082P | INXIGHT DRUGS |
Pharmaceutical products:
None