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Details

Stereochemistry ABSOLUTE
Molecular Formula C24H26N2O2
Molecular Weight 374.4754
Optical Activity UNSPECIFIED
Defined Stereocenters 2 / 2
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of EVOCALCET

SMILES

C[C@@H](N[C@H]1CCN(C1)C2=CC=C(CC(O)=O)C=C2)C3=CC=CC4=C3C=CC=C4

InChI

InChIKey=RZNUIYPHQFXBAN-XLIONFOSSA-N
InChI=1S/C24H26N2O2/c1-17(22-8-4-6-19-5-2-3-7-23(19)22)25-20-13-14-26(16-20)21-11-9-18(10-12-21)15-24(27)28/h2-12,17,20,25H,13-16H2,1H3,(H,27,28)/t17-,20+/m1/s1

HIDE SMILES / InChI

Molecular Formula C24H26N2O2
Molecular Weight 374.4754
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 2 / 2
E/Z Centers 0
Optical Activity UNSPECIFIED

Evocalcet (MT-4580, KHK7580) is an allosteric calcium-sensing receptor agonist. Evocalcet directly acts on calcium receptors on parathyroid cells to suppress synthesis and secretion of parathyroid hormone (PTH), and it consequently decreases serum PTH and serum calcium. ORKEDIA® TABLETS (generic name: evocalcet, code name: KHK7580) has been listed on the National Health Insurance (NHI) Drug Price List and launched for the treatment of secondary hyperparathyroidism in patients on maintenance dialysis in Japan.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Target ID: P41180
Gene ID: 846.0
Gene Symbol: CASR
Target Organism: Homo sapiens (Human)
93.0 nM [EC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
ORKEDIA

Approved Use

Secondary hyperparathyroidism in patients on maintenance dialysis.

Launch Date

1.52167685E12
PubMed

PubMed

TitleDatePubMed
A novel calcimimetic agent, evocalcet (MT-4580/KHK7580), suppresses the parathyroid cell function with little effect on the gastrointestinal tract or CYP isozymes in vivo and in vitro.
2018
Discovery of evocalcet, a next-generation calcium-sensing receptor agonist for the treatment of hyperparathyroidism.
2018 Jun 15
Long-Term Efficacy and Safety of Evocalcet in Japanese Patients with Secondary Hyperparathyroidism Receiving Hemodialysis.
2019 Apr 23
Patents

Sample Use Guides

In general, for adults, start by taking 1 tablet (1 mg of the active ingredient) at a time, once daily, then the dosage may be adjusted between 1 to 8 tablets (1 to 8 mg) by observing PTH and serum calcium level. Depending on your condition, the dosage may start from 2 tablets (2 mg) at a time, once daily. The maximum daily dose is limited to 12 tablets (12 mg). Dose should be increased by 1 tablet (1 mg) at a time, at intervals of at least two weeks. Strictly follow the instructions.
Route of Administration: Oral
Substance Class Chemical
Created
by admin
on Thu Jul 06 16:28:17 UTC 2023
Edited
by admin
on Thu Jul 06 16:28:17 UTC 2023
Record UNII
E58MLH082P
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
EVOCALCET
INN   WHO-DD  
INN  
Official Name English
Evocalcet [WHO-DD]
Common Name English
BENZENEACETIC ACID, 4-((3S)-3-(((1R)-1-(1-NAPHTHALENYL)ETHYL)AMINO)-1-PYRROLIDINYL)-
Systematic Name English
MT-4580
Code English
KHK7580
Code English
EVOCALCET [JAN]
Common Name English
evocalcet [INN]
Common Name English
KHK-7580
Code English
EVOCALCET [MI]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C2136
Created by admin on Thu Jul 06 16:28:17 UTC 2023 , Edited by admin on Thu Jul 06 16:28:17 UTC 2023
Code System Code Type Description
INN
10098
Created by admin on Thu Jul 06 16:28:17 UTC 2023 , Edited by admin on Thu Jul 06 16:28:17 UTC 2023
PRIMARY
WIKIPEDIA
Evocalcet
Created by admin on Thu Jul 06 16:28:17 UTC 2023 , Edited by admin on Thu Jul 06 16:28:17 UTC 2023
PRIMARY
CAS
870964-67-3
Created by admin on Thu Jul 06 16:28:17 UTC 2023 , Edited by admin on Thu Jul 06 16:28:17 UTC 2023
PRIMARY
DRUG BANK
DB12388
Created by admin on Thu Jul 06 16:28:17 UTC 2023 , Edited by admin on Thu Jul 06 16:28:17 UTC 2023
PRIMARY
PUBCHEM
71242808
Created by admin on Thu Jul 06 16:28:17 UTC 2023 , Edited by admin on Thu Jul 06 16:28:17 UTC 2023
PRIMARY
NCI_THESAURUS
C153105
Created by admin on Thu Jul 06 16:28:17 UTC 2023 , Edited by admin on Thu Jul 06 16:28:17 UTC 2023
PRIMARY
SMS_ID
100000177789
Created by admin on Thu Jul 06 16:28:17 UTC 2023 , Edited by admin on Thu Jul 06 16:28:17 UTC 2023
PRIMARY
FDA UNII
E58MLH082P
Created by admin on Thu Jul 06 16:28:17 UTC 2023 , Edited by admin on Thu Jul 06 16:28:17 UTC 2023
PRIMARY
DRUG CENTRAL
5307
Created by admin on Thu Jul 06 16:28:17 UTC 2023 , Edited by admin on Thu Jul 06 16:28:17 UTC 2023
PRIMARY
MERCK INDEX
M12096
Created by admin on Thu Jul 06 16:28:17 UTC 2023 , Edited by admin on Thu Jul 06 16:28:17 UTC 2023
PRIMARY
EPA CompTox
DTXSID101132784
Created by admin on Thu Jul 06 16:28:17 UTC 2023 , Edited by admin on Thu Jul 06 16:28:17 UTC 2023
PRIMARY
Related Record Type Details
TARGET -> AGONIST
Related Record Type Details
ACTIVE MOIETY