Page last updated: 2024-12-10

biricodar

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

biricodar: a non-macrocyclic ligand for FKBP12; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID3037617
CHEMBL ID350775
CHEBI ID135847
SCHEMBL ID154547
MeSH IDM0276514

Synonyms (28)

Synonym
incel
vx-710
biricodar
CHEBI:135847
CHEMBL350775 ,
vx 710
(s)-1-[2-oxo-2-(3,4,5-trimethoxy-phenyl)-acetyl]-piperidine-2-carboxylic acid 4-pyridin-3-yl-1-(3-pyridin-3-yl-propyl)-butyl ester
bdbm50109811
1,7-dipyridin-3-ylheptan-4-yl (2s)-1-[2-oxo-2-(3,4,5-trimethoxyphenyl)acetyl]piperidine-2-carboxylate
159997-94-1
3kg76x4kjk ,
4-(3-pyridyl)-1-(3-(-pyridyl)propyl)butyl(s)-1-((3,4,5-trimethoxyphenyl)glyoxyloyl)pipecolate
unii-3kg76x4kjk
4-(3-pyridyl)-1-(3-(3-pyridyl)propyl)butyl(s)-1-((3,4,5-trimethoxyphenyl)glyoxyloyl)pipecolate
2-piperidinecarboxylic acid, 1-(oxo(3,4,5-trimethoxyphenyl)acetyl)-, 4-(3-pyridinyl)-1-(3-(3-pyridinyl)propyl)butyl ester, (s)-
biricodar [inn]
biricodar [mi]
biricodar [who-dd]
DB04851
SCHEMBL154547
HY-13574A
CS-7427
DTXSID50893944
Q4916332
vx710
gtpl11741
MS-30647
AKOS040741361

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Patients were treated every 21 days until progression or intolerable adverse events (AEs)."( A phase II study of the safety and efficacy of the multidrug resistance inhibitor VX-710 combined with doxorubicin and vincristine in patients with recurrent small cell lung cancer.
Gandhi, L; Harding, MW; Johnson, BE; Langer, CJ; Lynch, TJ; Moore, M; Neubauer, M; Ross, HJ, 2007
)
0.34

Compound-Compound Interactions

ExcerptReferenceRelevance
"To evaluate the feasibility of administering biricodar (VX-710; Incel, Vertex Pharmaceuticals Inc, Cambridge, MA), an agent that modulates multidrug resistance (MDR) conferred by overexpression of both the multidrug resistance gene product (MDR1) P-glycoprotein and the MDR-associated protein (MRP) in vitro, in combination with paclitaxel."( Phase I and pharmacokinetic study of paclitaxel in combination with biricodar, a novel agent that reverses multidrug resistance conferred by overexpression of both MDR1 and MRP.
Aylesworth, C; Campbell, E; Chaturvedi, P; Drengler, R; Eckhardt, SG; Hammond, L; Harding, MW; Kraynak, M; Rowinsky, EK; Smith, L; Stephenson, J; Villalona, M; Von Hoff, DD; Wang, YM, 1998
)
0.8
" In combination with paclitaxel, biologically relevant VX-710 plasma concentrations are achieved and sustained for 24 hours, which simulates optimal pharmacologic conditions required for MDR reversal in vitro."( Phase I and pharmacokinetic study of paclitaxel in combination with biricodar, a novel agent that reverses multidrug resistance conferred by overexpression of both MDR1 and MRP.
Aylesworth, C; Campbell, E; Chaturvedi, P; Drengler, R; Eckhardt, SG; Hammond, L; Harding, MW; Kraynak, M; Rowinsky, EK; Smith, L; Stephenson, J; Villalona, M; Von Hoff, DD; Wang, YM, 1998
)
0.54
" A Phase II study was designed to evaluate VX-710 in combination with doxorubicin and vincristine in patients with sensitive, recurrent small cell lung cancer (SCLC)."( A phase II study of the safety and efficacy of the multidrug resistance inhibitor VX-710 combined with doxorubicin and vincristine in patients with recurrent small cell lung cancer.
Gandhi, L; Harding, MW; Johnson, BE; Langer, CJ; Lynch, TJ; Moore, M; Neubauer, M; Ross, HJ, 2007
)
0.34
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
alpha-amino acid esterThe amino acid ester derivative obtained the formal condensation of an alpha-amino acid with an alcohol.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (5)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ATP-dependent translocase ABCB1Mus musculus (house mouse)IC50 (µMol)5.00000.06404.012610.0000AID67783
Multidrug resistance-associated protein 1 Homo sapiens (human)IC50 (µMol)5.18000.00153.71109.6600AID46488
Peptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)IC50 (µMol)0.01700.00040.39373.6000AID672586
Peptidyl-prolyl cis-trans isomerase FKBP4Homo sapiens (human)IC50 (µMol)7.37000.01605.12878.0000AID672588
Peptidyl-prolyl cis-trans isomerase FKBP5Homo sapiens (human)IC50 (µMol)8.52008.52008.52008.5200AID672587
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (56)

Processvia Protein(s)Taxonomy
leukotriene metabolic processMultidrug resistance-associated protein 1 Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 1 Homo sapiens (human)
response to xenobiotic stimulusMultidrug resistance-associated protein 1 Homo sapiens (human)
cobalamin transportMultidrug resistance-associated protein 1 Homo sapiens (human)
sphingolipid biosynthetic processMultidrug resistance-associated protein 1 Homo sapiens (human)
cellular response to oxidative stressMultidrug resistance-associated protein 1 Homo sapiens (human)
heme catabolic processMultidrug resistance-associated protein 1 Homo sapiens (human)
xenobiotic transportMultidrug resistance-associated protein 1 Homo sapiens (human)
phospholipid translocationMultidrug resistance-associated protein 1 Homo sapiens (human)
positive regulation of inflammatory responseMultidrug resistance-associated protein 1 Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 1 Homo sapiens (human)
cell chemotaxisMultidrug resistance-associated protein 1 Homo sapiens (human)
transepithelial transportMultidrug resistance-associated protein 1 Homo sapiens (human)
cyclic nucleotide transportMultidrug resistance-associated protein 1 Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 1 Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 1 Homo sapiens (human)
sphingolipid translocationMultidrug resistance-associated protein 1 Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 1 Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 1 Homo sapiens (human)
cellular response to amyloid-betaMultidrug resistance-associated protein 1 Homo sapiens (human)
carboxylic acid transmembrane transportMultidrug resistance-associated protein 1 Homo sapiens (human)
xenobiotic transport across blood-brain barrierMultidrug resistance-associated protein 1 Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 1 Homo sapiens (human)
protein peptidyl-prolyl isomerizationPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
heart morphogenesisPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
protein foldingPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
'de novo' protein foldingPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
regulation of skeletal muscle contraction by regulation of release of sequestered calcium ionPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
protein maturation by protein foldingPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
positive regulation of protein bindingPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
regulation of protein localizationPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
negative regulation of activin receptor signaling pathwayPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
protein refoldingPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
T cell activationPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
regulation of immune responsePeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
ventricular cardiac muscle tissue morphogenesisPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
regulation of ryanodine-sensitive calcium-release channel activityPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
heart trabecula formationPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
calcium ion transmembrane transportPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
supramolecular fiber organizationPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
regulation of amyloid precursor protein catabolic processPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
amyloid fibril formationPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
protein foldingPeptidyl-prolyl cis-trans isomerase FKBP4Homo sapiens (human)
steroid hormone receptor complex assemblyPeptidyl-prolyl cis-trans isomerase FKBP4Homo sapiens (human)
copper ion transportPeptidyl-prolyl cis-trans isomerase FKBP4Homo sapiens (human)
embryo implantationPeptidyl-prolyl cis-trans isomerase FKBP4Homo sapiens (human)
negative regulation of neuron projection developmentPeptidyl-prolyl cis-trans isomerase FKBP4Homo sapiens (human)
androgen receptor signaling pathwayPeptidyl-prolyl cis-trans isomerase FKBP4Homo sapiens (human)
prostate gland developmentPeptidyl-prolyl cis-trans isomerase FKBP4Homo sapiens (human)
negative regulation of microtubule polymerization or depolymerizationPeptidyl-prolyl cis-trans isomerase FKBP4Homo sapiens (human)
negative regulation of microtubule polymerizationPeptidyl-prolyl cis-trans isomerase FKBP4Homo sapiens (human)
protein-containing complex localizationPeptidyl-prolyl cis-trans isomerase FKBP4Homo sapiens (human)
male sex differentiationPeptidyl-prolyl cis-trans isomerase FKBP4Homo sapiens (human)
chaperone-mediated protein foldingPeptidyl-prolyl cis-trans isomerase FKBP4Homo sapiens (human)
protein peptidyl-prolyl isomerizationPeptidyl-prolyl cis-trans isomerase FKBP4Homo sapiens (human)
protein foldingPeptidyl-prolyl cis-trans isomerase FKBP5Homo sapiens (human)
response to bacteriumPeptidyl-prolyl cis-trans isomerase FKBP5Homo sapiens (human)
chaperone-mediated protein foldingPeptidyl-prolyl cis-trans isomerase FKBP5Homo sapiens (human)
protein peptidyl-prolyl isomerizationPeptidyl-prolyl cis-trans isomerase FKBP5Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (33)

Processvia Protein(s)Taxonomy
ATP bindingMultidrug resistance-associated protein 1 Homo sapiens (human)
ABC-type vitamin B12 transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 1 Homo sapiens (human)
ATPase-coupled lipid transmembrane transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
sphingolipid transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
carboxylic acid transmembrane transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 1 Homo sapiens (human)
peptidyl-prolyl cis-trans isomerase activityPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
transforming growth factor beta receptor bindingPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
protein bindingPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
macrolide bindingPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
FK506 bindingPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
channel regulator activityPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
signaling receptor inhibitor activityPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
type I transforming growth factor beta receptor bindingPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
transmembrane transporter bindingPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
I-SMAD bindingPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
activin receptor bindingPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
RNA bindingPeptidyl-prolyl cis-trans isomerase FKBP4Homo sapiens (human)
peptidyl-prolyl cis-trans isomerase activityPeptidyl-prolyl cis-trans isomerase FKBP4Homo sapiens (human)
protein bindingPeptidyl-prolyl cis-trans isomerase FKBP4Homo sapiens (human)
ATP bindingPeptidyl-prolyl cis-trans isomerase FKBP4Homo sapiens (human)
GTP bindingPeptidyl-prolyl cis-trans isomerase FKBP4Homo sapiens (human)
FK506 bindingPeptidyl-prolyl cis-trans isomerase FKBP4Homo sapiens (human)
protein-macromolecule adaptor activityPeptidyl-prolyl cis-trans isomerase FKBP4Homo sapiens (human)
heat shock protein bindingPeptidyl-prolyl cis-trans isomerase FKBP4Homo sapiens (human)
copper-dependent protein bindingPeptidyl-prolyl cis-trans isomerase FKBP4Homo sapiens (human)
nuclear glucocorticoid receptor bindingPeptidyl-prolyl cis-trans isomerase FKBP4Homo sapiens (human)
tau protein bindingPeptidyl-prolyl cis-trans isomerase FKBP4Homo sapiens (human)
phosphoprotein bindingPeptidyl-prolyl cis-trans isomerase FKBP4Homo sapiens (human)
peptidyl-prolyl cis-trans isomerase activityPeptidyl-prolyl cis-trans isomerase FKBP5Homo sapiens (human)
protein bindingPeptidyl-prolyl cis-trans isomerase FKBP5Homo sapiens (human)
FK506 bindingPeptidyl-prolyl cis-trans isomerase FKBP5Homo sapiens (human)
protein-macromolecule adaptor activityPeptidyl-prolyl cis-trans isomerase FKBP5Homo sapiens (human)
heat shock protein bindingPeptidyl-prolyl cis-trans isomerase FKBP5Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (22)

Processvia Protein(s)Taxonomy
plasma membraneMultidrug resistance-associated protein 1 Homo sapiens (human)
basal plasma membraneMultidrug resistance-associated protein 1 Homo sapiens (human)
membraneMultidrug resistance-associated protein 1 Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 1 Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 1 Homo sapiens (human)
lateral plasma membraneMultidrug resistance-associated protein 1 Homo sapiens (human)
extracellular exosomeMultidrug resistance-associated protein 1 Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 1 Homo sapiens (human)
cytoplasmPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
cytosolPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
terminal cisternaPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
membranePeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
sarcoplasmic reticulumPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
Z discPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
cytoplasmic side of membranePeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
ryanodine receptor complexPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
sarcoplasmic reticulum membranePeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
cytoplasmPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
nucleoplasmPeptidyl-prolyl cis-trans isomerase FKBP4Homo sapiens (human)
mitochondrionPeptidyl-prolyl cis-trans isomerase FKBP4Homo sapiens (human)
cytosolPeptidyl-prolyl cis-trans isomerase FKBP4Homo sapiens (human)
microtubulePeptidyl-prolyl cis-trans isomerase FKBP4Homo sapiens (human)
neuronal cell bodyPeptidyl-prolyl cis-trans isomerase FKBP4Homo sapiens (human)
axonal growth conePeptidyl-prolyl cis-trans isomerase FKBP4Homo sapiens (human)
perinuclear region of cytoplasmPeptidyl-prolyl cis-trans isomerase FKBP4Homo sapiens (human)
extracellular exosomePeptidyl-prolyl cis-trans isomerase FKBP4Homo sapiens (human)
protein-containing complexPeptidyl-prolyl cis-trans isomerase FKBP4Homo sapiens (human)
cytoplasmPeptidyl-prolyl cis-trans isomerase FKBP4Homo sapiens (human)
cytoplasmPeptidyl-prolyl cis-trans isomerase FKBP5Homo sapiens (human)
nucleoplasmPeptidyl-prolyl cis-trans isomerase FKBP5Homo sapiens (human)
cytosolPeptidyl-prolyl cis-trans isomerase FKBP5Homo sapiens (human)
membranePeptidyl-prolyl cis-trans isomerase FKBP5Homo sapiens (human)
extracellular exosomePeptidyl-prolyl cis-trans isomerase FKBP5Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (6)

Assay IDTitleYearJournalArticle
AID46488Inhibition of multidrug resistance associated protein type 1 (MRP1) assayed by an accumulation assay in COR.L23/R cells2002Bioorganic & medicinal chemistry letters, Feb-25, Volume: 12, Issue:4
Studies on quinazolinones as dual inhibitors of Pgp and MRP1 in multidrug resistance.
AID680676TP_TRANSPORTER: increase in mitoxantrone intracellular accumulation (Mitoxantrone: 3 uM, VX-710: 2.5 uM) in A2780/Dx5b cells2004Clinical cancer research : an official journal of the American Association for Cancer Research, Mar-01, Volume: 10, Issue:5
VX-710 (biricodar) increases drug retention and enhances chemosensitivity in resistant cells overexpressing P-glycoprotein, multidrug resistance protein, and breast cancer resistance protein.
AID67783Inhibitory activity against P-glycoprotein (Pgp) using accumulation assay for Pgp expressing EMT6/AR1.0 cells.2002Bioorganic & medicinal chemistry letters, Feb-25, Volume: 12, Issue:4
Studies on quinazolinones as dual inhibitors of Pgp and MRP1 in multidrug resistance.
AID672588Binding affinity to FKBP52 FK1 domain by fluorescence polarization assay2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
Evaluation of synthetic FK506 analogues as ligands for the FK506-binding proteins 51 and 52.
AID672587Binding affinity to FKBP51 FK1 domain by fluorescence polarization assay2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
Evaluation of synthetic FK506 analogues as ligands for the FK506-binding proteins 51 and 52.
AID672586Binding affinity to FKBP12 by fluorescence polarization assay2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
Evaluation of synthetic FK506 analogues as ligands for the FK506-binding proteins 51 and 52.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (27)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's4 (14.81)18.2507
2000's16 (59.26)29.6817
2010's2 (7.41)24.3611
2020's5 (18.52)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 20.93

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index20.93 (24.57)
Research Supply Index3.56 (2.92)
Research Growth Index5.18 (4.65)
Search Engine Demand Index18.60 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (20.93)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials7 (25.93%)5.53%
Reviews5 (18.52%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other15 (55.56%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]