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Details

Stereochemistry RACEMIC
Molecular Formula C34H38N3O7P.ClH
Molecular Weight 668.116
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of EFONIDIPINE HYDROCHLORIDE

SMILES

Cl.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=OXVTXPCIJDYQIS-UHFFFAOYSA-N
InChI=1S/C34H38N3O7P.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;/h5-17,20,31,35H,18-19,21-23H2,1-4H3;1H

HIDE SMILES / InChI
Molecular Formula C34H38N3O7P
Molecular Weight 631.6552
Charge 0
Count
Stereochemistry RACEMIC
Additional Stereochemistry No
Defined Stereocenters 0 / 1
E/Z Centers 0
Optical Activity ( + / - )
Molecular Formula ClH
Molecular Weight 36.461
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description

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

Unknown
149124
Targets

Targets

Primary TargetPharmacologyConditionPotency
Blocker
555
 13.0 nM [IC50]
Blocker
555
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8583
LANDEL

Approved Use

Unknown
Primary
Approved
8583
LANDEL

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
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

AUC

ValueDoseCo-administeredAnalytePopulation
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
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
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
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
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

Doses

DosePopulationAdverse 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

PubMed

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

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).
Substance Class Chemical
Created
by admin
on Mon Mar 31 18:35:24 GMT 2025
Edited
by admin
on Mon Mar 31 18:35:24 GMT 2025
Record UNII
3BR983K69O
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
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
Preferred Name English
EFONIDIPINE HYDROCHLORIDE
MART.   MI   WHO-DD  
Common Name English
Efonidipine hydrochloride [WHO-DD]
Common Name English
EFONIDIPINE HYDROCHLORIDE [MI]
Common Name English
3-PYRIDINECARBOXYLIC ACID, 5-(5,5-DIMETHYL-2-OXIDO-1,3,2-DIOXAPHOSPHORINAN-2-YL)-1,4-DIHYDRO-2,6-DIMETHYL-4-(3-NITROPHENYL)-, 2-(PHENYL(PHENYLMETHYL)AMINO)ETHYL ESTER, MONOHYDROCHLORIDE
Common Name English
EFONIDIPINE HYDROCHLORIDE [MART.]
Common Name English
EFONIDIPINE HCL
Common Name English
2-(N-BENZYLANILINO)ETHYL (±)-1,4-DIHYDRO-2,6-DIMETHYL-4-(M-NITROPHENYL)-5-PHOSPHONONICOTINATE, CYCLIC 2,2-DIMETHYLTRIMETHYLENE ESTER, HYDROCHLORIDE
Common Name English
3-PYRIDINECARBOXYLIC ACID, 5-(5,5-DIMETHYL-2-OXIDO-1,3,2-DIOXAPHOSPHORINAN-2-YL)-1,4-DIHYDRO-2,6-DIMETHYL-4-(3-NITROPHENYL)-, 2-(PHENYL(PHENYLMETHYL)AMINO)ETHYL ESTER, HYDROCHLORIDE (1:1)
Systematic Name English
Classification Tree Code System Code
NCI_THESAURUS C333
Created by admin on Mon Mar 31 18:35:24 GMT 2025 , Edited by admin on Mon Mar 31 18:35:24 GMT 2025
Code System Code Type Description
ChEMBL
CHEMBL2074922
Created by admin on Mon Mar 31 18:35:24 GMT 2025 , Edited by admin on Mon Mar 31 18:35:24 GMT 2025
PRIMARY
SMS_ID
100000087740
Created by admin on Mon Mar 31 18:35:24 GMT 2025 , Edited by admin on Mon Mar 31 18:35:24 GMT 2025
PRIMARY
EVMPD
SUB01862MIG
Created by admin on Mon Mar 31 18:35:24 GMT 2025 , Edited by admin on Mon Mar 31 18:35:24 GMT 2025
PRIMARY
CAS
111011-53-1
Created by admin on Mon Mar 31 18:35:24 GMT 2025 , Edited by admin on Mon Mar 31 18:35:24 GMT 2025
PRIMARY
NCI_THESAURUS
C77825
Created by admin on Mon Mar 31 18:35:24 GMT 2025 , Edited by admin on Mon Mar 31 18:35:24 GMT 2025
PRIMARY
EPA CompTox
DTXSID20911942
Created by admin on Mon Mar 31 18:35:24 GMT 2025 , Edited by admin on Mon Mar 31 18:35:24 GMT 2025
PRIMARY
PUBCHEM
119170
Created by admin on Mon Mar 31 18:35:24 GMT 2025 , Edited by admin on Mon Mar 31 18:35:24 GMT 2025
PRIMARY
DRUG BANK
DBSALT001268
Created by admin on Mon Mar 31 18:35:24 GMT 2025 , Edited by admin on Mon Mar 31 18:35:24 GMT 2025
PRIMARY
FDA UNII
3BR983K69O
Created by admin on Mon Mar 31 18:35:24 GMT 2025 , Edited by admin on Mon Mar 31 18:35:24 GMT 2025
PRIMARY
MERCK INDEX
m4841
Created by admin on Mon Mar 31 18:35:24 GMT 2025 , Edited by admin on Mon Mar 31 18:35:24 GMT 2025
PRIMARY Merck Index
Related Record Type Details
Structure of EFONIDIPINE HYDROCHLORIDE, (S)-
ENANTIOMER -> RACEMATE
Structure of EFONIDIPINE HYDROCHLORIDE, (R)-
ENANTIOMER -> RACEMATE
Structure of EFONIDIPINE
PARENT -> SALT/SOLVATE
Structure of EFONIDIPINE HYDROCHLORIDE ETHANOLATE
SOLVATE->ANHYDROUS
Related Record Type Details
Structure of EFONIDIPINE
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