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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 IDs Not Available
Product Ingredients 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
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
Pharmacogenomic Effects/ADRs Not Available
Interactions
Drug Interactions
DrugInteractionDrug group
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of ABT-263.Approved
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
OleandrinAnvirzel may decrease the cardiotoxic activities of ABT-263.Experimental
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
Clinical Trials
Clinical Trials
PhaseStatusPurposeConditionsCount
1Active Not RecruitingTreatmentCD20-Positive Lymphoid Malignancies / Chronic Lymphoid Leukemia / Hematological Malignancy / Non-Hodgkin's Lymphoma (NHL)1
1CompletedNot AvailableHealthy Female Subjects1
1CompletedTreatmentChronic Lymphocytic Leukaemia (CLL)1
1CompletedTreatmentChronic Lymphocytic Leukaemia (CLL) / Leukemias / Lymphoma NOS1
1CompletedTreatmentChronic Lymphocytic Leukaemia (CLL) / Lymphoma NOS / Tumors, Solid1
1CompletedTreatmentLymphoid Malignancies / Tumors, Solid1
1CompletedTreatmentLymphoma, Including Chronic Lymphocytic Leukemia / Tumors, Solid1
1CompletedTreatmentTumors, Solid5
1RecruitingTreatmentEGFR Activating Mutation / Recurrent Non-Small Cell Lung Carcinoma / Stage III Non-Small Cell Lung Cancer / Stage IIIA Non-Small Cell Lung Cancer / Stage IIIB Non-Small Cell Lung Cancer / Stage IV Non-Small Cell Lung Cancer1
1RecruitingTreatmentRecurrent Hepatocellular Carcinoma / Solid Neoplasms / Stage IV Hepatocellular Carcinoma1
1, 2CompletedTreatmentSmall Cell Lung Cancer (SCLC) / Small Cell Lung Carcinoma1
1, 2RecruitingTreatmentAdvanced Malignant Solid Neoplasm / Extensive Stage Small Cell Lung Carcinoma / KRAS Gene Mutation / Metastatic Malignant Solid Neoplasm / Metastatic Solid Neoplasm / Neoplasms, Advanced Solid / NRAS Gene Mutation / Recurrent Colorectal Carcinoma / Recurrent Lung Carcinoma / Recurrent Non-Small Cell Lung Carcinoma / Recurrent Pancreatic Carcinoma / Recurrent Small Cell Lung Carcinoma / Solid Neoplasms / Stage III Colorectal Cancer / Stage III Lung Cancer / Stage III Pancreatic Cancer / Stage IIIA Colorectal Cancer / Stage IIIA Non-Small Cell Lung Cancer / Stage IIIB Colorectal Cancer / Stage IIIB Non-Small Cell Lung Cancer / Stage IIIC Colorectal Cancer / Stage IV Colorectal Cancer / Stage IV Lung Cancer / Stage IV Non-Small Cell Lung Cancer / Stage IV Pancreatic Cancer / Stage IVA Colorectal Cancer / Stage IVB Colorectal Cancer1
1, 2RecruitingTreatmentMetastatic Melanoma / Recurrent Melanoma / Solid Neoplasms / Stage IIIA Skin Melanoma / Stage IIIB Skin Melanoma / Stage IIIC Skin Melanoma / Stage IV Skin Melanoma1
2Active Not RecruitingTreatmentChronic Lymphocytic Leukaemia (CLL)1
2Active Not RecruitingTreatmentPlatinum-resistant or Refractory Ovarian Cancer1
2CompletedBasic ScienceChronic Lymphocytic Leukaemia (CLL)1
2CompletedTreatmentCarcinoma of the Prostate1
2CompletedTreatmentChronic Lymphocytic Leukaemia (CLL)1
2CompletedTreatmentChronic Lymphoid Leukemia / Follicular Lymphoma (FL) / Lymphoid Malignancies / Mantle Cell Lymphoma (MCL) / Non-Hodgkin's Lymphoma (NHL) / Peripheral T-Cell Lymphoma (PTCL)1
2WithdrawnTreatmentB-Cell Chronic Lymphocytic Leukemia1
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage formsNot Available
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental PropertiesNot Available
Predicted PropertiesNot Available
Predicted ADMET featuresNot 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