EFONIDIPINE

Possibly Marketed Outside US

Details

Stereochemistry	RACEMIC
Molecular Formula	C34H38N3O7P
Molecular Weight	631.6552
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

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=NSVFSAJIGAJDMR-UHFFFAOYSA-N

InChI=1S/C34H38N3O7P/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

HIDE SMILES / InChI

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

Targets

Primary Target	Pharmacology	Condition	Potency
Voltage-gated T-type calcium channel 19	Blocker 555		13.0 nM [IC50]
Voltage-gated L-type calcium channel 95	Blocker 555

Conditions

Condition	Modality	Targets	Highest Phase	Product
Hypertension 575	Primary		Approved 8,583	LANDEL
Angina pectoris 110	Primary		Approved 8,583	LANDEL

C_max

Value	Dose	Analyte	Population
1.7 ng/mL	10 mg single, oral	EFONIDIPINE plasma	Homo sapiens
11.7 ng/mL	20 mg single, oral	EFONIDIPINE plasma	Homo sapiens
17.9 ng/mL	40 mg single, oral	EFONIDIPINE plasma	Homo sapiens
10.8 ng/mL	20 mg single, oral	EFONIDIPINE plasma	Homo sapiens
12.9 ng/mL	20 mg single, oral	EFONIDIPINE plasma	Homo sapiens
19.7 ng/mL	30 mg single, oral	EFONIDIPINE plasma	Homo sapiens
26.1 ng/mL	30 mg single, oral	EFONIDIPINE plasma	Homo sapiens

AUC

Value	Dose	Analyte	Population
4.1 ng × h/mL	10 mg single, oral	EFONIDIPINE plasma	Homo sapiens
25.4 ng × h/mL	20 mg single, oral	EFONIDIPINE plasma	Homo sapiens
57.6 ng × h/mL	40 mg single, oral	EFONIDIPINE plasma	Homo sapiens
34.7 ng × h/mL	20 mg single, oral	EFONIDIPINE plasma	Homo sapiens
31.5 ng × h/mL	20 mg single, oral	EFONIDIPINE plasma	Homo sapiens
61.7 ng × h/mL	30 mg single, oral	EFONIDIPINE plasma	Homo sapiens
68.8 ng × h/mL	30 mg single, oral	EFONIDIPINE plasma	Homo sapiens

T_1/2

Value	Dose	Analyte	Population
2.9 h	10 mg single, oral	EFONIDIPINE plasma	Homo sapiens
1.4 h	20 mg single, oral	EFONIDIPINE plasma	Homo sapiens
2.2 h	40 mg single, oral	EFONIDIPINE plasma	Homo sapiens
2 h	20 mg single, oral	EFONIDIPINE plasma	Homo sapiens
2.1 h	20 mg single, oral	EFONIDIPINE plasma	Homo sapiens
1.8 h	30 mg single, oral	EFONIDIPINE plasma	Homo sapiens
1.7 h	30 mg single, oral	EFONIDIPINE plasma	Homo sapiens

F_unbound

Value	Dose	Co-administered	Analyte	Population
0.2%			EFONIDIPINE serum	Homo sapiens

Doses

Doses

Show entries

Dose	Population	Adverse events
40 mg 1 times / day multiple, oral Recommended	unhealthy, ADULT

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PubMed

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).

Show entries

Name

Type

Language

(±)-EFONIDIPINE

Preferred Name

English

EFONIDIPINE

Official Name

English

Efonidipine [WHO-DD]

Common Name

English

efonidipine [INN]

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

Systematic Name

English

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Classification Tree

Code System

Code

Cation Channel Blocker

NCI_THESAURUS

C333

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Show entries

Code System

Code

Type

Description

EPA CompTox

DTXSID9043988

PRIMARY

EVMPD

SUB06471MIG

PRIMARY

MERCK INDEX

m4841

PRIMARY

Merck Index

CHEBI

135859

PRIMARY

NCI_THESAURUS

C73026

PRIMARY

Showing 1 to 5 of 15 entries

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ACTIVE MOIETY


					40ZTP2T37Q

EFONIDIPINE

SALT/SOLVATE (PARENT)


					84HJ0Q6TMN

EFONIDIPINE HYDROCHLORIDE ETHANOLATE

SALT/SOLVATE (PARENT)


					3BR983K69O

EFONIDIPINE HYDROCHLORIDE

SMILES

InChI

Description<div class="info-popup-container"><div><span class="pop-sub-key ">Sources:&nbsp;</span><span class="pop-sub-val"><span class="ext-link"><a target="_self" href="http://www.ncbi.nlm.nih.gov/pubmed/12070536">http://www.ncbi.nlm.nih.gov/pubmed/12070536</a></span></span></div></div>

Originator

Approval Year

Targets

Conditions

Cmax

AUC

T1/2

Funbound

Doses

PubMed

Sample Use Guides

Description

C_max

T_1/2

F_unbound