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Identification
NameABT-263
Accession NumberDB05764
TypeSmall Molecule
GroupsInvestigational
DescriptionABT-263 is an orally bioavailable small molecule inhibitor of Bcl-2 family proteins. It is a substance being studied in the treatment of lymphomas and other types of cancer. It blocks some of the enzymes that keep cancer cells from dying.
Structure
Thumb
SynonymsNot Available
External Identifiers Not Available
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIINot Available
CAS numberNot Available
WeightNot Available
Chemical FormulaNot Available
InChI KeyNot Available
InChINot Available
IUPAC NameNot Available
SMILESNot Available
Pharmacology
IndicationInvestigated for use/treatment in lung cancer and lymphoma (unspecified).
Structured Indications Not Available
PharmacodynamicsNot Available
Mechanism of actionABT-263 targets the Bcl-2 family of proteins, the major negative regulators of apoptosis. The Bcl-2 proteins, including Bcl-2, Bcl-xL, and Bcl-w, work by binding to two other groups of proteins-the executioners (Bax, Bak) that actually start the destruction pathway, and the sentinel proteins. Cancer cells frequently overexpress the Bcl-2-like proteins, and thus, when they sustain DNA damage-from radiation, for example-they continue growing. Preventing the Bcl-2-like proteins from binding to the executioners might be able to trigger cell death in the tumor.
TargetKindPharmacological actionActionsOrganismUniProt ID
Apoptosis regulator Bcl-2ProteinunknownNot AvailableHumanP10415 details
Bcl-2-like protein 2ProteinunknownNot AvailableHumanQ92843 details
Bcl2-associated agonist of cell deathProteinunknownNot AvailableHumanQ92934 details
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half life14-25 hours
ClearanceNot Available
ToxicityNot Available
Affected organismsNot Available
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of ABT-263.Approved
AnvirzelAnvirzel may decrease the cardiotoxic activities of ABT-263.Investigational
BevacizumabBevacizumab may increase the cardiotoxic activities of ABT-263.Approved, Investigational
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with ABT-263.Approved
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of ABT-263.Approved, Investigational
DeslanosideDeslanoside may decrease the cardiotoxic activities of ABT-263.Approved
DigitoxinDigitoxin may decrease the cardiotoxic activities of ABT-263.Approved
DigoxinDigoxin may decrease the cardiotoxic activities of ABT-263.Approved
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with ABT-263.Approved, Investigational
OuabainOuabain may decrease the cardiotoxic activities of ABT-263.Approved
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with ABT-263.Approved, Vet Approved
TrastuzumabTrastuzumab may increase the cardiotoxic activities of ABT-263.Approved, Investigational
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General References
  1. Lock R, Carol H, Houghton PJ, Morton CL, Kolb EA, Gorlick R, Reynolds CP, Maris JM, Keir ST, Wu J, Smith MA: Initial testing (stage 1) of the BH3 mimetic ABT-263 by the pediatric preclinical testing program. Pediatr Blood Cancer. 2008 Jun;50(6):1181-9. [PubMed:18085673 ]
External LinksNot Available
ATC CodesNot Available
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
ADMET
Predicted ADMET featuresNot Available
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage formsNot Available
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental PropertiesNot Available
Predicted PropertiesNot Available
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Taxonomy
ClassificationNot classified

Targets

Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Ubiquitin protein ligase binding
Specific Function:
Suppresses apoptosis in a variety of cell systems including factor-dependent lymphohematopoietic and neural cells. Regulates cell death by controlling the mitochondrial membrane permeability. Appears to function in a feedback loop system with caspases. Inhibits caspase activity either by preventing the release of cytochrome c from the mitochondria and/or by binding to the apoptosis-activating f...
Gene Name:
BCL2
Uniprot ID:
P10415
Molecular Weight:
26265.66 Da
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Protein homodimerization activity
Specific Function:
Promotes cell survival. Blocks dexamethasone-induced apoptosis. Mediates survival of postmitotic Sertoli cells by suppressing death-promoting activity of BAX.
Gene Name:
BCL2L2
Uniprot ID:
Q92843
Molecular Weight:
20746.24 Da
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Protein kinase binding
Specific Function:
Promotes cell death. Successfully competes for the binding to Bcl-X(L), Bcl-2 and Bcl-W, thereby affecting the level of heterodimerization of these proteins with BAX. Can reverse the death repressor activity of Bcl-X(L), but not that of Bcl-2 (By similarity). Appears to act as a link between growth factor receptor signaling and the apoptotic pathways.
Gene Name:
BAD
Uniprot ID:
Q92934
Molecular Weight:
18391.765 Da
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Drug created on November 18, 2007 11:27 / Updated on August 17, 2016 12:24