EFONIDIPINE HYDROCHLORIDE ETHANOLATE

Details

Stereochemistry	RACEMIC
Molecular Formula	C34H38N3O7P.C2H6O.ClH
Molecular Weight	714.185
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure of EFONIDIPINE HYDROCHLORIDE ETHANOLATE

Structure Search

SMILES

Cl.CCO.CC1=C(C(C2=CC(=CC=C2)[N+]([O-])=O)C(=C(C)N1)P3(=O)OCC(C)(C)CO3)C(=O)OCCN(CC4=CC=CC=C4)C5=CC=CC=C5

InChI

InChIKey=IKBJGZQVVVXCEQ-UHFFFAOYSA-N

InChI=1S/C34H38N3O7P.C2H6O.ClH/c1-24-30(33(38)42-19-18-36(28-15-9-6-10-16-28)21-26-12-7-5-8-13-26)31(27-14-11-17-29(20-27)37(39)40)32(25(2)35-24)45(41)43-22-34(3,4)23-44-45;1-2-3;/h5-17,20,31,35H,18-19,21-23H2,1-4H3;3H,2H2,1H3;1H

HIDE SMILES / InChI

Description
Sources: http://www.ncbi.nlm.nih.gov/pubmed/12070536

Efonidipine is a 1,4-dihydropyridine derivative for the treatment of hypertension and angina. Efonidipine exerts its antihypertensive and antianginal effects through blocking L- and T-type calcium channels.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Voltage-gated T-type calcium channel 19 Target ID: CHEMBL2362995 Sources: http://www.ncbi.nlm.nih.gov/pubmed/12070536	Blocker 555		13.0 nM [IC50]
Voltage-gated L-type calcium channel 95 Target ID: CHEMBL2095229 Sources: http://www.ncbi.nlm.nih.gov/pubmed/12070536	Blocker 555

Conditions

Condition	Modality	Targets	Highest Phase	Product
Hypertension 575 Sources: http://www.ncbi.nlm.nih.gov/pubmed/21088755	Primary		Approved 8583	LANDEL Approved Use Unknown
Angina pectoris 110 Sources: http://www.ncbi.nlm.nih.gov/pubmed/21088755	Primary		Approved 8583	LANDEL Approved Use Unknown

C_max

Value	Dose	Analyte	Population
1.7 ng/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/3/380077_2149034F1020_3_1F.pdf#page=22	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	EFONIDIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
11.7 ng/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/3/380077_2149034F1020_3_1F.pdf#page=22	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	EFONIDIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
17.9 ng/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/3/380077_2149034F1020_3_1F.pdf#page=22	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	EFONIDIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
10.8 ng/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/3/380077_2149034F1020_3_1F.pdf#page=23	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	EFONIDIPINE plasma	Homo sapiens population: UNKNOWN age: ADULT sex: FEMALE / MALE food status: UNKNOWN
12.9 ng/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/3/380077_2149034F1020_3_1F.pdf#page=23	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	EFONIDIPINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
19.7 ng/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/3/380077_2149034F1020_3_1F.pdf#page=23	30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered:	EFONIDIPINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
26.1 ng/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/3/380077_2149034F1020_3_1F.pdf#page=23	30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered:	EFONIDIPINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
4.1 ng × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/3/380077_2149034F1020_3_1F.pdf#page=22	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	EFONIDIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
25.4 ng × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/3/380077_2149034F1020_3_1F.pdf#page=22	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	EFONIDIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
57.6 ng × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/3/380077_2149034F1020_3_1F.pdf#page=22	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	EFONIDIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
34.7 ng × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/3/380077_2149034F1020_3_1F.pdf#page=23	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	EFONIDIPINE plasma	Homo sapiens population: UNKNOWN age: ADULT sex: FEMALE / MALE food status: UNKNOWN
31.5 ng × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/3/380077_2149034F1020_3_1F.pdf#page=23	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	EFONIDIPINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
61.7 ng × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/3/380077_2149034F1020_3_1F.pdf#page=23	30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered:	EFONIDIPINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
68.8 ng × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/3/380077_2149034F1020_3_1F.pdf#page=23	30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered:	EFONIDIPINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

T_1/2

Value	Dose	Analyte	Population
2.9 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/3/380077_2149034F1020_3_1F.pdf#page=22	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	EFONIDIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1.4 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/3/380077_2149034F1020_3_1F.pdf#page=22	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	EFONIDIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2.2 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/3/380077_2149034F1020_3_1F.pdf#page=22	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	EFONIDIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/3/380077_2149034F1020_3_1F.pdf#page=23	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	EFONIDIPINE plasma	Homo sapiens population: UNKNOWN age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2.1 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/3/380077_2149034F1020_3_1F.pdf#page=23	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	EFONIDIPINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.8 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/3/380077_2149034F1020_3_1F.pdf#page=23	30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered:	EFONIDIPINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.7 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/3/380077_2149034F1020_3_1F.pdf#page=23	30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered:	EFONIDIPINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
0.2% DRUG LABEL https://www.info.pmda.go.jp/go/interview/3/380077_2149034F1020_3_1F.pdf#page=25			EFONIDIPINE serum	Homo sapiens

Doses

Dose	Population	Adverse events
40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/24944418/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/24944418/	Sources: https://pubmed.ncbi.nlm.nih.gov/24944418/

PubMed

Title	Date	PubMed
Efonidipine hydrochloride: a dual blocker of L- and T-type ca(2+) channels.	2002 Winter	12070536

Sample Use Guides

In Vivo Use Guide

40 mg once daily for 12 weeks

Route of Administration: Oral

In Vitro Use Guide

Effects of efonidipine on isolated myocardial and aortic preparations was studied. The drug produced concentration-dependent negative chronotropic effects on isolated guinea-pig atrial preparations.The potency was 3.08 x 10(-8)M (EC30).

Name

Type

Language

EFONIDIPINE HYDROCHLORIDE ETHANOLATE

Common Name

English

LANDEL

Preferred Name

English

NZ-105

Code

English

EFONIDIPINE HYDROCHLORIDE ETHANOLATE [MI]

Common Name

English

(±)-EFONIDIPINE HYDROCHLORIDE ETHANOLATE

Common Name

English

3-PYRIDINECARBOXYLIC ACID, 5-(5,5-DIMETHYL-1,3,2-DIOXAPHOSPHORINAN-2-YL)-1,4-DIHYDRO-2,6-DIMETHYL-4-(3-NITROPHENYL)-, 2-(PHENYL(PHENYLMETHYL)AMINO)ETHYL ESTER, P-OXIDE, MONOHYDROCHLORIDE, COMPD. WITH ETHANOL (1:1)

Common Name

English

Efonidipine hydrochloride ethanolate [WHO-DD]

Common Name

English

EFONIDIPINE HYDROCHLORIDE ETHANOLATE [JAN]

Common Name

English

Code System Code Type Description

SMS_ID

100000085033