Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C34H33N3O5.ClH |
| Molecular Weight | 600.104 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.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=IQOJZZHRYSSFJM-UHFFFAOYSA-N
InChI=1S/C34H33N3O5.ClH/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);1H
DescriptionCurator's Comment: description was created based on several sources, including:
http://www.drugbank.ca/drugs/DB04881
Curator's Comment: description was created based on several sources, including:
http://www.drugbank.ca/drugs/DB04881
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.
Originator
Approval Year
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
185 μg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17545533 |
1000 mg 1 times / week multiple, oral dose: 1000 mg route of administration: Oral experiment type: MULTIPLE co-administered: TOPOTECAN |
ELACRIDAR plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
2629 μg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/17545533 |
1000 mg 1 times / week multiple, oral dose: 1000 mg route of administration: Oral experiment type: MULTIPLE co-administered: TOPOTECAN |
ELACRIDAR plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
Doses
| Dose | Population | Adverse events |
|---|---|---|
1000 mg 1 times / week multiple, oral Highest studied dose Dose: 1000 mg, 1 times / week Route: oral Route: multiple Dose: 1000 mg, 1 times / week Co-administed with:: topotecan(1000 mg of elacridar on days 1 and 8 1 h before or simultaneously with 2.0 mg oral topotecan) Sources: Page: p.3279 |
unhealthy, ADULT n = 4 Health Status: unhealthy Condition: cancer Age Group: ADULT Sex: M+F Food Status: FED Population Size: 4 Sources: Page: p.3279 |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Assessing safety and efficacy of directed P-glycoprotein inhibition to improve the pharmacokinetic properties of saquinavir coadministered with ritonavir. | 2003 Feb |
|
| 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 |
|
| P-glycoprotein (P-gp/MDR1)-mediated efflux of sex-steroid hormones and modulation of P-gp expression in vitro. | 2004 Jul |
|
| Differentiation of gut and hepatic first pass metabolism and secretion of saquinavir in ported rabbits. | 2004 Jul |
|
| Multiple mechanisms are involved in the biliary excretion of acetaminophen sulfate in the rat: role of Mrp2 and Bcrp1. | 2005 Aug |
|
| Flavonoid structure-activity studies identify 6-prenylchrysin and tectochrysin as potent and specific inhibitors of breast cancer resistance protein ABCG2. | 2005 Jun 1 |
|
| Comparison of drug efflux transport kinetics in various blood-brain barrier models. | 2006 Jun |
|
| Expression and transport activity of breast cancer resistance protein (Bcrp/Abcg2) in dually perfused rat placenta and HRP-1 cell line. | 2006 Oct |
|
| The effect of low pH on breast cancer resistance protein (ABCG2)-mediated transport of methotrexate, 7-hydroxymethotrexate, methotrexate diglutamate, folic acid, mitoxantrone, topotecan, and resveratrol in in vitro drug transport models. | 2007 Jan |
|
| Abcg2/Bcrp1 mediates the polarized transport of antiretroviral nucleosides abacavir and zidovudine. | 2007 Jul |
|
| P-glycoprotein-mediated active efflux of the anti-HIV1 nucleoside abacavir limits cellular accumulation and brain distribution. | 2007 Nov |
|
| Mechanisms underlying saturable intestinal absorption of metformin. | 2008 Aug |
|
| Investigation of the role of breast cancer resistance protein (Bcrp/Abcg2) on pharmacokinetics and central nervous system penetration of abacavir and zidovudine in the mouse. | 2008 Aug |
|
| N-(4-[2-(1,2,3,4-tetrahydro-6,7-dimethoxy-2-isoquinolinyl)ethyl]-phenyl)-9,10-dihydro-5-methoxy-9-oxo-4-acridine carboxamide (GF120918) as a chemical ATP-binding cassette transporter family G member 2 (Abcg2) knockout model to study nitrofurantoin transfer into milk. | 2008 Dec |
|
| P-glycoprotein restricts the penetration of oseltamivir across the blood-brain barrier. | 2008 Feb |
|
| Kinetic identification of membrane transporters that assist P-glycoprotein-mediated transport of digoxin and loperamide through a confluent monolayer of MDCKII-hMDR1 cells. | 2008 Feb |
|
| Multidrug resistance-associated protein 2 is primarily responsible for the biliary excretion of fexofenadine in mice. | 2008 Jan |
|
| Small P-gp modulating molecules: SAR studies on tetrahydroisoquinoline derivatives. | 2008 Jan 1 |
|
| Role of P-glycoprotein and the intestine in the excretion of DPC 333 [(2R)-2-{(3R)-3-amino-3-[4-(2-methylquinolin-4-ylmethoxy)phenyl]-2-oxopyrrolidin-1-yl}-N-hydroxy-4-methylpentanamide] in rodents. | 2008 Jun |
|
| Effect of the ABCB1 modulators elacridar and tariquidar on the distribution of paclitaxel in nude mice. | 2008 May |
|
| Apparent differences in mechanisms of harmol sulfate biliary excretion in mice and rats. | 2008 Nov |
|
| Development and characterisation of a new model of rat trophoblasts. | 2009 Feb |
|
| Cross-functioning between the extraneuronal monoamine transporter and multidrug resistance protein 1 in the uptake of adrenaline and export of 5-(glutathion-S-yl)adrenaline in rat cardiomyocytes. | 2009 Jan |
|
| Substrate-dependent breast cancer resistance protein (Bcrp1/Abcg2)-mediated interactions: consideration of multiple binding sites in in vitro assay design. | 2009 Mar |
|
| Multiple efflux pumps are involved in the transepithelial transport of colchicine: combined effect of p-glycoprotein and multidrug resistance-associated protein 2 leads to decreased intestinal absorption throughout the entire small intestine. | 2009 Oct |
|
| Functional characterization of mouse organic anion transporting peptide 1a4 in the uptake and efflux of drugs across the blood-brain barrier. | 2010 Jan |
|
| Hepatobiliary disposition of 3alpha,6alpha,7alpha,12alpha-tetrahydroxy-cholanoyl taurine: a substrate for multiple canalicular transporters. | 2010 Oct |
|
| In vitro investigation of the hepatobiliary disposition mechanisms of the antifungal agent micafungin in humans and rats. | 2010 Oct |
|
| In situ intestinal perfusion in knockout mice demonstrates inhibition of intestinal p-glycoprotein by ritonavir causing increased darunavir absorption. | 2010 Sep |
|
| Role of P-glycoprotein and breast cancer resistance protein-1 in the brain penetration and brain pharmacodynamic activity of the novel phosphatidylinositol 3-kinase inhibitor GDC-0941. | 2010 Sep |
|
| Oral and inhaled corticosteroids: differences in P-glycoprotein (ABCB1) mediated efflux. | 2012 May 1 |
|
| Early identification of clinically relevant drug interactions with the human bile salt export pump (BSEP/ABCB11). | 2013 Dec |
Patents
Sample Use Guides
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
| Name | Type | Language | ||
|---|---|---|---|---|
|
Official Name | English | ||
|
Code | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Systematic Name | English | ||
|
Common Name | English | ||
|
Common Name | English |
| Classification Tree | Code System | Code | ||
|---|---|---|---|---|
|
NCI_THESAURUS |
C1744
Created by
admin on Fri Dec 15 15:38:12 GMT 2023 , Edited by admin on Fri Dec 15 15:38:12 GMT 2023
|
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
170320
Created by
admin on Fri Dec 15 15:38:12 GMT 2023 , Edited by admin on Fri Dec 15 15:38:12 GMT 2023
|
PRIMARY | |||
|
C72752
Created by
admin on Fri Dec 15 15:38:12 GMT 2023 , Edited by admin on Fri Dec 15 15:38:12 GMT 2023
|
PRIMARY | |||
|
CHEMBL396298
Created by
admin on Fri Dec 15 15:38:12 GMT 2023 , Edited by admin on Fri Dec 15 15:38:12 GMT 2023
|
PRIMARY | |||
|
HH-43
Created by
admin on Fri Dec 15 15:38:12 GMT 2023 , Edited by admin on Fri Dec 15 15:38:12 GMT 2023
|
PRIMARY | |||
|
DBSALT000816
Created by
admin on Fri Dec 15 15:38:12 GMT 2023 , Edited by admin on Fri Dec 15 15:38:12 GMT 2023
|
PRIMARY | |||
|
143851-98-3
Created by
admin on Fri Dec 15 15:38:12 GMT 2023 , Edited by admin on Fri Dec 15 15:38:12 GMT 2023
|
PRIMARY | |||
|
DTXSID30932123
Created by
admin on Fri Dec 15 15:38:12 GMT 2023 , Edited by admin on Fri Dec 15 15:38:12 GMT 2023
|
PRIMARY | |||
|
NX2BHH1A5B
Created by
admin on Fri Dec 15 15:38:12 GMT 2023 , Edited by admin on Fri Dec 15 15:38:12 GMT 2023
|
PRIMARY |
ACTIVE MOIETY
SUBSTANCE RECORD
