DGIdb - VENETOCLAX Drug Record

VENETOCLAX chembl:CHEMBL3137309 ApprovedAntineoplastic

Alternate Names:

VENETOCLAX
RG-7601
ABT-199
RG7601
VENCLEXTA
GDC-0199
4-{4-[(4'-CHLORO-5,5-DIMETHYL[3,4,5,6-TETRAHYDRO[1,1'-BIPHENYL]]-2-YL)METHYL]PIPERAZIN-1-YL}-N-(3-NITRO-4-{[(OXAN-4-YL)METHYL]AMINO}BENZENE-1-SULFONYL)-2-[(1H-PYRROLO[2,3-B]PYRIDIN-5-YL)OXY]BENZAMIDE
rxcui:1747556
pubchem.compound:49846579
chembl:CHEMBL3137309
drugbank:11581
chemidplus:1257044-40-8

Drug Info:

FDA Approval	Chronic lymphocytic leukemia (with 17p deletion)
Drug Class	Small molecule inhibitor
Drug Groups	investigational
Drug Categories	antineoplastic agents
Drug Categories	antineoplastic and immunomodulating agents
Drug Categories	bcl-2 inhibitor
Drug Categories	bcrp/abcg2 inhibitors
Drug Categories	cytochrome p-450 cyp3a inhibitors
Drug Categories	cytochrome p-450 cyp3a substrates
Drug Categories	cytochrome p-450 cyp3a4 inhibitors
Drug Categories	cytochrome p-450 cyp3a4 inhibitors (moderate)
Drug Categories	cytochrome p-450 cyp3a4 substrates with a narrow therapeutic index
Drug Categories	cytochrome p-450 enzyme inhibitors
Drug Categories	cytochrome p-450 substrates
Drug Categories	increased cellular death
Drug Categories	narrow therapeutic index drugs
Drug Categories	oatp1b1/slco1b1 inhibitors
Drug Categories	p-glycoprotein inhibitors
Drug Categories	p-glycoprotein substrates
Drug Categories	p-glycoprotein substrates with narrow therapeutic index

(8 More Sources)

Publications:

Konopleva et al., 2016, Efficacy and Biological Correlates of Response in a Phase II Study of Venetoclax Monotherapy in Patients with Acute Myelogenous Leukemia., Cancer Discov
Huemer F et al., 2019, Durable remissions with venetoclax monotherapy in secondary AML refractory to hypomethylating agents and high expression of BCL-2 and/or BIM., Eur J Haematol
Anderson et al., 2016, PIK3CA mutations enable targeting of a breast tumor dependency through mTOR-mediated MCL-1 translation., Sci Transl Med
Davids et al., 2013, ABT-199: taking dead aim at BCL-2., Cancer Cell
Tausch E et al., 2019, Venetoclax resistance and acquired <i>BCL2</i> mutations in chronic lymphocytic leukemia., Haematologica
Blombery P et al., 2019, Acquisition of the Recurrent Gly101Val Mutation in BCL2 Confers Resistance to Venetoclax in Patients with Progressive Chronic Lymphocytic Leukemia., Cancer Discov
Blombery P et al., 2020, Multiple BCL2 mutations cooccurring with Gly101Val emerge in chronic lymphocytic leukemia progression on venetoclax., Blood
Souers et al., 2013, ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets., Nat. Med.
King AC et al., 2017, Venetoclax: A First-in-Class Oral BCL-2 Inhibitor for the Management of Lymphoid Malignancies., Ann Pharmacother
Lucas F et al., 2020, Novel BCL2 mutations in venetoclax-resistant, ibrutinib-resistant CLL patients with BTK/PLCG2 mutations., Blood
Birkinshaw RW et al., 2019, Structures of BCL-2 in complex with venetoclax reveal the molecular basis of resistance mutations., Nat Commun
Blombery P et al., 2019, Characterization of a novel venetoclax resistance mutation (BCL2 Phe104Ile) observed in follicular lymphoma., Br J Haematol

VENETOCLAX IDH2

Interaction Score: 4.42

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type acute myeloid leukemia

Response Type predicted – sensitive

Approval Status Phase II

PMIDs:
27520294 30725494

Sources:
FDA PharmGKB JAX-CKB CIViC CGI
VENETOCLAX IGH

Interaction Score: 3.79

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
FDA
VENETOCLAX BCL2

Interaction Score: 1.16

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Note that this Ki is below the detection limit of the assay.

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
23410971 31004028 30514704 31951646 23291630 28056525 32232486 31160589 31234236

Sources:
CIViC TTD DrugBank MyCancerGenome GuideToPharmacology ChemblInteractions
VENETOCLAX BCL2L2

Interaction Score: 0.63

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
VENETOCLAX NPM1

Interaction Score: 0.47

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
FDA PharmGKB
VENETOCLAX BCL2L1

Interaction Score: 0.38

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
VENETOCLAX MCL1

Interaction Score: 0.08

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
VENETOCLAX FLT3

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
FDA PharmGKB
VENETOCLAX PTEN

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy BEZ235 + Venetoclax

Indication/Tumor Type breast cancer

Response Type no benefit

PMIDs:
27974663

Sources:
JAX-CKB
VENETOCLAX BRAF

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell culture

Response Type no benefit

PMIDs:
27974663

Sources:
JAX-CKB
VENETOCLAX IDH1

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type acute myeloid leukemia

Response Type predicted – sensitive

Approval Status Phase II

PMIDs:
27520294 30725494

Sources:
FDA PharmGKB JAX-CKB CIViC CGI
VENETOCLAX KRAS

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Venetoclax + VX-11e

Indication/Tumor Type colorectal cancer

Response Type no benefit

PMIDs:
27974663

Sources:
JAX-CKB
VENETOCLAX ABL1

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Dasatinib;Venetoclax

Drug family BCR-ABL inhibitor 2nd gen;BCL2 inhibitor

Alteration ABL1__BCR

PMIDs:
None found

Sources:
CGI
VENETOCLAX PIK3CA

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy BEZ235 + Venetoclax

Indication/Tumor Type breast cancer

Response Type no benefit

PMIDs:
27974663

Sources:
JAX-CKB
VENETOCLAX TP53

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
FDA PharmGKB

DrugBank: DB11581

Version: 5.1.7

Alternate Names:

VENETOCLAX DrugBank Drug Name

1257044-40-8 CAS Number

Venclexta Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups investigational

Publications:

Davids et al., 2013, ABT-199: taking dead aim at BCL-2., Cancer Cell

Souers et al., 2013, ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets., Nat. Med.

King AC et al., 2017, Venetoclax: A First-in-Class Oral BCL-2 Inhibitor for the Management of Lymphoid Malignancies., Ann Pharmacother

MyCancerGenome: VENETOCLAX
- Version: 20-Jun-2017
Alternate Names:

VENCLEXTA Trade Name

Drug Info:

Drug Class Small molecule inhibitor

FDA Approval Chronic lymphocytic leukemia (with 17p deletion)

Publications:

JAX-CKB: Venetoclax

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Anderson et al., 2016, PIK3CA mutations enable targeting of a breast tumor dependency through mTOR-mediated MCL-1 translation., Sci Transl Med

Konopleva et al., 2016, Efficacy and Biological Correlates of Response in a Phase II Study of Venetoclax Monotherapy in Patients with Acute Myelogenous Leukemia., Cancer Discov

CIViC: VENETOCLAX

Version: 14-September-2020

Alternate Names:

Drug Info:

Publications:

Huemer F et al., 2019, Durable remissions with venetoclax monotherapy in secondary AML refractory to hypomethylating agents and high expression of BCL-2 and/or BIM., Eur J Haematol

Tausch E et al., 2019, Venetoclax resistance and acquired <i>BCL2</i> mutations in chronic lymphocytic leukemia., Haematologica

Blombery P et al., 2019, Acquisition of the Recurrent Gly101Val Mutation in BCL2 Confers Resistance to Venetoclax in Patients with Progressive Chronic Lymphocytic Leukemia., Cancer Discov

GuideToPharmacology: 252166530
- Version: 29-September-2020
Alternate Names:

VENETOCLAX GuideToPharmacology Ligand Name

Drug Info:

Publications:
TTD: GDC-0199
- Version: 2020.06.01
Alternate Names:

D00PBX TTD Drug ID

Drug Info:

Publications:
TTD: RG7601
- Version: 2020.06.01
Alternate Names:

D0I6OI TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL3137309
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
PharmGKB: venetoclax
- Version: 18-August-2020
Alternate Names:

Drug Info:

Publications:
FDA: Venetoclax
- Version: 04-September-2020
Alternate Names:

Drug Info:

Publications:
CGI: Venetoclax
- Version: 27-September-2017
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL3137309
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:

Indication/Tumor Type	acute myeloid leukemia
Response Type	predicted – sensitive
Approval Status	Phase II

Details of the Assay for Interaction	Note that this Ki is below the detection limit of the assay.
Specific Action of the Ligand	Antagonist
Endogenous Drug?	False

combination therapy	BEZ235 + Venetoclax
Indication/Tumor Type	breast cancer
Response Type	no benefit

Evidence Type	Actionable
Approval Status	Preclinical - Cell culture
Response Type	no benefit

combination therapy	Venetoclax + VX-11e
Indication/Tumor Type	colorectal cancer
Response Type	no benefit

combination therapy	Dasatinib;Venetoclax
Drug family	BCR-ABL inhibitor 2nd gen;BCL2 inhibitor
Alteration	ABL1__BCR

VENETOCLAX	DrugBank Drug Name
1257044-40-8	CAS Number
Venclexta	Drug Brand

Drug Type	small molecule
Drug Groups	approved
Drug Groups	investigational

antagonist (inhibitory)
inhibitor (inhibitory)

VENETOCLAX Drug Record

VENETOCLAX chembl:CHEMBL3137309 ApprovedAntineoplastic

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type acute myeloid leukemia Response Type predicted – sensitive Approval Status Phase II

PMIDs: 27520294 30725494

Sources: FDA PharmGKB JAX-CKB CIViC CGI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: FDA

Interaction Types & Directionality: antagonist (inhibitory) inhibitor (inhibitory)

Interaction Info: Details of the Assay for Interaction Note that this Ki is below the detection limit of the assay. Specific Action of the Ligand Antagonist Endogenous Drug? False

PMIDs: 23410971 31004028 30514704 31951646 23291630 28056525 32232486 31160589 31234236

Sources: CIViC TTD DrugBank MyCancerGenome GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False Direct Interaction? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: FDA PharmGKB

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False Direct Interaction? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False Direct Interaction? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: FDA PharmGKB

Interaction Types & Directionality: n/a

Interaction Info: combination therapy BEZ235 + Venetoclax Indication/Tumor Type breast cancer Response Type no benefit

PMIDs: 27974663

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: Evidence Type Actionable Approval Status Preclinical - Cell culture Response Type no benefit

PMIDs: 27974663

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type acute myeloid leukemia Response Type predicted – sensitive Approval Status Phase II

PMIDs: 27520294 30725494

Sources: FDA PharmGKB JAX-CKB CIViC CGI

Interaction Types & Directionality: n/a

Interaction Info: combination therapy Venetoclax + VX-11e Indication/Tumor Type colorectal cancer Response Type no benefit

PMIDs: 27974663

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: combination therapy Dasatinib;Venetoclax Drug family BCR-ABL inhibitor 2nd gen;BCL2 inhibitor Alteration ABL1__BCR

PMIDs: None found

Sources: CGI

Interaction Types & Directionality: n/a

Interaction Info: combination therapy BEZ235 + Venetoclax Indication/Tumor Type breast cancer Response Type no benefit

PMIDs: 27974663

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: FDA PharmGKB

DrugBank: DB11581

Alternate Names: VENETOCLAX DrugBank Drug Name 1257044-40-8 CAS Number Venclexta Drug Brand

Drug Info: Drug Type small molecule Drug Groups approved Drug Groups investigational

MyCancerGenome: VENETOCLAX

Alternate Names: VENCLEXTA Trade Name

Drug Info: Drug Class Small molecule inhibitor FDA Approval Chronic lymphocytic leukemia (with 17p deletion)

Publications:

JAX-CKB: Venetoclax

Alternate Names:

Drug Info:

CIViC: VENETOCLAX

Alternate Names:

Drug Info:

GuideToPharmacology: 252166530

Alternate Names: VENETOCLAX GuideToPharmacology Ligand Name

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type acute myeloid leukemia

Response Type predicted – sensitive

Approval Status Phase II

PMIDs:
27520294 30725494

Sources:
FDA PharmGKB JAX-CKB CIViC CGI

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
FDA

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Note that this Ki is below the detection limit of the assay.

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
23410971 31004028 30514704 31951646 23291630 28056525 32232486 31160589 31234236

Sources:
CIViC TTD DrugBank MyCancerGenome GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
FDA PharmGKB

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
FDA PharmGKB

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy BEZ235 + Venetoclax

Indication/Tumor Type breast cancer

Response Type no benefit

PMIDs:
27974663

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell culture

Response Type no benefit

PMIDs:
27974663

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type acute myeloid leukemia

Response Type predicted – sensitive

Approval Status Phase II

PMIDs:
27520294 30725494

Sources:
FDA PharmGKB JAX-CKB CIViC CGI

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Venetoclax + VX-11e

Indication/Tumor Type colorectal cancer

Response Type no benefit

PMIDs:
27974663

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Dasatinib;Venetoclax

Drug family BCR-ABL inhibitor 2nd gen;BCL2 inhibitor

Alteration ABL1__BCR

PMIDs:
None found

Sources:
CGI

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy BEZ235 + Venetoclax

Indication/Tumor Type breast cancer

Response Type no benefit

PMIDs:
27974663

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
FDA PharmGKB

Alternate Names:

VENETOCLAX DrugBank Drug Name

1257044-40-8 CAS Number

Venclexta Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups investigational

Alternate Names:

VENCLEXTA Trade Name

Drug Info:

Drug Class Small molecule inhibitor

FDA Approval Chronic lymphocytic leukemia (with 17p deletion)

Alternate Names:

VENETOCLAX GuideToPharmacology Ligand Name

Alternate Names:

D00PBX TTD Drug ID

Alternate Names:

D0I6OI TTD Drug ID