evocalcet 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
calcium-sensing receptors (CaSR) agonists	5307	870964-67-3

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: evocalcet orkedia KHK-7580 KHK7580 MT-4580	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. Molecular weight: 374.48 Formula: C24H26N2O2 CLOGP: 2.14 LIPINSKI: 0 HAC: 4 HDO: 2 TPSA: 52.57 ALOGS: -5.22 ROTB: 6

Molecule

Description

Molfile Inchi Smiles

Synonyms:

evocalcet
orkedia
KHK-7580
KHK7580
MT-4580

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.

Molecular weight: 374.48
Formula: C24H26N2O2
CLOGP: 2.14
LIPINSKI: 0
HAC: 4
HDO: 2
TPSA: 52.57
ALOGS: -5.22
ROTB: 6

Drug dosage:

None

ADMET properties:

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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

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Approvals:

Date	Agency	Company	Orphan
March 23, 2018	PMDA	Kyowa Hakko Kirin Co., Ltd.

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

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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	94.84	60.19	12	67	770	34956082

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FDA Adverse Event Reporting System (Geriatric)

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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	162.19	56.62	20	117	1371	79742880
Shunt occlusion	98.44	56.62	13	124	1491	79742760

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

None

Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Hypercalcemia in primary hyperparathyroidism	indication	2243000
Hypercalcemia in parathyroid carcinoma	indication	47709007
Secondary hyperparathyroidism	indication	91478007	DOID:12466

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🐶 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:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Extracellular calcium-sensing receptor	GPCR	P41180	CASR_HUMAN	AGONIST	EC50	7.03		SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE

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External reference:

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ID	Source
H43	PDB_CHEM_ID
10098	INN_ID
71242808	PUBCHEM_CID
9042	IUPHAR_LIGAND_ID
C000631688	MESH_SUPPLEMENTAL_RECORD_UI
C4519114	UMLSCUI
CHEMBL4297621	ChEMBL_ID
D11063	KEGG_DRUG
DB12388	DRUGBANK_ID
E58MLH082P	UNII

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Pharmaceutical products:

None