EVOCALCET

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 Search

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

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/29724589 | https://www.kyowa-kirin.com/news_releases/2018/pdf/e20180522_01.pdf | https://www.ncbi.nlm.nih.gov/pubmed/29614098

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.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Extracellular calcium-sensing receptor 1 Target ID: P41180 Gene ID: 846.0 Gene Symbol: CASR Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/29724589	Agonist 2678		93.0 nM [EC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Secondary hyperparathyroidism 9 Sources: https://www.kyowa-kirin.com/news_releases/2018/pdf/e20180522_01.pdf	Primary		Approved 8429	ORKEDIA Approved Use Secondary hyperparathyroidism in patients on maintenance dialysis. Launch Date 2018

PubMed

Title	Date	PubMed
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	29614098
Long-Term Efficacy and Safety of Evocalcet in Japanese Patients with Secondary Hyperparathyroidism Receiving Hemodialysis.	2019 Apr 23	31015494

Patents

Sample Use Guides

In Vivo Use Guide

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 `Sat Dec 16 10:53:25 GMT 2023` Edited by `admin` on `Sat Dec 16 10:53:25 GMT 2023`
Record UNII	E58MLH082P
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

EVOCALCET

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