ELACRIDAR

Investigational

Details

Stereochemistry	ACHIRAL
Molecular Formula	C34H33N3O5
Molecular Weight	563.6429
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

COC1=C(OC)C=C2CN(CCC3=CC=C(NC(=O)C4=C5NC6=C(OC)C=CC=C6C(=O)C5=CC=C4)C=C3)CCC2=C1

InChI

InChIKey=OSFCMRGOZNQUSW-UHFFFAOYSA-N

InChI=1S/C34H33N3O5/c1-40-28-9-5-7-26-32(28)36-31-25(33(26)38)6-4-8-27(31)34(39)35-24-12-10-21(11-13-24)14-16-37-17-15-22-18-29(41-2)30(42-3)19-23(22)20-37/h4-13,18-19H,14-17,20H2,1-3H3,(H,35,39)(H,36,38)

HIDE SMILES / InChI

Description

Elacridar is an oral bioenhancer that targets multiple drug resistance in tumors. Elacridar is a strong and relatively specific inhibitor of P-gp and BCRP, two main efflux transporters. Development of elacridar is assumed to have been discontinued.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
P-glycoprotein 1 54	Inhibitor 8,297		70.0 nM [IC50]
ATP-binding cassette sub-family G member 2 16	Inhibitor 8,297		0.31 µM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Cancer 592	Primary		Phase I 428	Unknown

C_max

Value	Dose	Co-administered	Analyte	Population
185 μg/L	1000 mg 1 times / week multiple, oral	TOPOTECAN	ELACRIDAR plasma	Homo sapiens

AUC

Value	Dose	Co-administered	Analyte	Population
2629 μg × h/L	1000 mg 1 times / week multiple, oral	TOPOTECAN	ELACRIDAR plasma	Homo sapiens

Doses

Doses

Show entries

Dose	Population	Adverse events
1000 mg 1 times / week multiple, oral Highest studied dose	unhealthy, ADULT

Showing 1 to 1 of 1 entries

Previous1Next

Sourcing

Sourcing

Show entries

Vendor/Aggregator	ID	URL
001 Chemical	DY116194	https://www.001chemical.com/chem/search?q=DY116194
1PlusChem LLC	1P001IXZ	https://www.1pchem.com/search?query=1P001IXZ
1PlusChem LLC	1P00AP6W	https://www.1pchem.com/search?query=1P00AP6W
A2B Chem	AE98408	http://a2bchem.com/prod/AE98408
AChemBlock	10315	http://www.achemblock.com/catalogsearch/result/?q=10315

Showing 1 to 5 of 51 entries

Previous1 2 3 4 5…11Next

PubMed

Show entries

Title	Date	PubMed
Assessing safety and efficacy of directed P-glycoprotein inhibition to improve the pharmacokinetic properties of saquinavir coadministered with ritonavir.	2003 Feb	12538811
Human organic anion-transporting polypeptide OATP-A (SLC21A3) acts in concert with P-glycoprotein and multidrug resistance protein 2 in the vectorial transport of Saquinavir in Hep G2 cells.	2004 Jan 12	15832500
P-glycoprotein (P-gp/MDR1)-mediated efflux of sex-steroid hormones and modulation of P-gp expression in vitro.	2004 Jul	15290871
Differentiation of gut and hepatic first pass metabolism and secretion of saquinavir in ported rabbits.	2004 Jul	15004217
Multiple mechanisms are involved in the biliary excretion of acetaminophen sulfate in the rat: role of Mrp2 and Bcrp1.	2005 Aug	15860656

Showing 1 to 5 of 23 entries

Previous1 2 3 4 5Next

Patents

Sample Use Guides

In Vivo Use Guide

The starting daily dose of GF120918 was 50 mg and was to be increased in subsequent cohorts until a steady state plasma level of 100 ng/ml was reached.

Route of Administration: Oral

In Vitro Use Guide

In Caki-1 and ACHN cells, elacridar ( 2.5 μM) significantly inhibits the cell growth. The P-glycoprotein expression is found to be inhibited by 5 uM elacridar in all cell lines (786-O, ACHN, and Caki-1).

Show entries

Name

Type

Language

ELACRIDAR

Official Name

English

elacridar [INN]

Common Name

English

4-ACRIDINECARBOXAMIDE, N-(4-(2-(3,4-DIHYDRO-6,7-DIMETHOXY-2(1H)-ISOQUINOLINYL)ETHYL)PHENYL)-9,10-DIHYDRO-5-METHOXY-9-OXO-

Systematic Name

English

Elacridar [WHO-DD]

Common Name

English

LY-335979

Code

English

Showing 1 to 5 of 7 entries

Previous1 2Next

Show entries

Classification Tree

Code System

Code

Pharmacologic Substance

NCI_THESAURUS

C1744

Showing 1 to 1 of 1 entries

Previous1Next

Show entries

Code System

Code

Type

Description

CAS

143664-11-3

PRIMARY

INN

7582

PRIMARY

EVMPD

SUB06475MIG

PRIMARY

ChEMBL

CHEMBL396298

PRIMARY

SMS_ID

100000080519

PRIMARY

Showing 1 to 5 of 11 entries

Previous1 2 3Next

ACTIVE MOIETY


					N488540F94

ELACRIDAR

SALT/SOLVATE (PARENT)


					NX2BHH1A5B

ELACRIDAR HYDROCHLORIDE

SMILES

InChI

CNS Activity

Originator

Approval Year

Targets

Conditions

Cmax

AUC

Doses

Sourcing

PubMed

Patents

Sample Use Guides

C_max