DGIdb - RUCAPARIB Drug Record

RUCAPARIB chembl:CHEMBL1173055 ApprovedAntineoplastic

Alternate Names:

AG-014699
RUCAPARIB
AG-14447
AG014699
PF-01367338
AG14447
RUBRACA
chemidplus:283173-50-2
pubchem.compound:9931954
drugbank:12332
chembl:CHEMBL1173055
rxcui:1862579

Drug Info:

FDA Approval	Ovarian cancer (with BRCA mutation)
Drug Class	Small molecule inhibitor

(11 More Sources)

Publications:

Du et al., 2016, Blocking c-Met-mediated PARP1 phosphorylation enhances anti-tumor effects of PARP inhibitors., Nat. Med.
Drew et al., 2016, Phase 2 multicentre trial investigating intermittent and continuous dosing schedules of the poly(ADP-ribose) polymerase inhibitor rucaparib in germline BRCA mutation carriers with advanced ovarian and breast cancer., Br. J. Cancer
Shroff RT et al., 2018, Rucaparib Monotherapy in Patients With Pancreatic Cancer and a Known Deleterious <i>BRCA</i> Mutation., JCO Precis Oncol
Swisher et al., 2017, Rucaparib in relapsed, platinum-sensitive high-grade ovarian carcinoma (ARIEL2 Part 1): an international, multicentre, open-label, phase 2 trial., Lancet Oncol.
Wang et al., 2016, RING domain-deficient BRCA1 promotes PARP inhibitor and platinum resistance., J. Clin. Invest.
Kondrashova O et al., 2017 Sep, Secondary Somatic Mutations Restoring <i>RAD51C</i> and <i>RAD51D</i> Associated with Acquired Resistance to the PARP Inhibitor Rucaparib in High-Grade Ovarian Carcinoma., Cancer Discov
Sulkowski et al., 2017, 2-Hydroxyglutarate produced by neomorphic IDH mutations suppresses homologous recombination and induces PARP inhibitor sensitivity., Sci Transl Med
Chatterjee et al., 2013, PARP inhibition sensitizes to low dose-rate radiation TMPRSS2-ERG fusion gene-expressing and PTEN-deficient prostate cancer cells., PLoS ONE
Solomon et al., 2011, Mutational inactivation of STAG2 causes aneuploidy in human cancer., Science
Bailey et al., 2014, Glioblastoma cells containing mutations in the cohesin component STAG2 are sensitive to PARP inhibition., Mol. Cancer Ther.

RUCAPARIB PARP2

Interaction Score: 1.1

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PARP 1, 2 and 3 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
MyCancerGenome ClearityFoundationClinicalTrial ChemblInteractions PharmGKB
RUCAPARIB PARP1

Interaction Score: 0.97

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
None found

Sources:
TALC MyCancerGenome ClearityFoundationClinicalTrial ChemblInteractions GuideToPharmacology PharmGKB
RUCAPARIB BRCA2

Interaction Score: 0.77

Interaction Types & Directionality:

n/a

Interaction Info:

Drug family PARP inhibitor

Alteration BRCA2:.

Indication/Tumor Type ovarian cancer

PMIDs:
26779812 27002934 30051098 27908594

Sources:
ClearityFoundationBiomarkers JAX-CKB CGI CIViC PharmGKB OncoKB
RUCAPARIB PARP3

Interaction Score: 0.77

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PARP 1, 2 and 3 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions PharmGKB
RUCAPARIB STAG2

Interaction Score: 0.72

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type glioblastoma multiforme

Response Type sensitive

Approval Status Preclinical

PMIDs:
21852505 24356817

Sources:
JAX-CKB
RUCAPARIB PALB2

Interaction Score: 0.64

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
CIViC
RUCAPARIB SLC47A2

Interaction Score: 0.64

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
RUCAPARIB SLC47A1

Interaction Score: 0.48

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
RUCAPARIB SLC22A6

Interaction Score: 0.24

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
RUCAPARIB BRCA1

Interaction Score: 0.22

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type ovarian carcinoma

Response Type sensitive

Approval Status Clinical Study

PMIDs:
27454289 27002934 26779812 28588062 27908594

Sources:
ClearityFoundationBiomarkers JAX-CKB CGI CIViC PharmGKB OncoKB
RUCAPARIB ATR

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
ClearityFoundationBiomarkers
RUCAPARIB SLC22A8

Interaction Score: 0.15

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
RUCAPARIB DYRK1A

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
RUCAPARIB SLCO1B3

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
RUCAPARIB CYP2C8

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
RUCAPARIB ABCC4

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
RUCAPARIB PRKD2

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
RUCAPARIB PIM1

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
RUCAPARIB UGT1A1

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
RUCAPARIB PTEN

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy AZD6482 + Rucaparib

Indication/Tumor Type triple-receptor negative breast cancer

Response Type sensitive

PMIDs:
23565244

Sources:
JAX-CKB
RUCAPARIB SLCO1B1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
RUCAPARIB CDK1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
RUCAPARIB ATM

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
ClearityFoundationBiomarkers
RUCAPARIB MET

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type breast cancer

combination therapy Foretinib + Rucaparib

Approval Status Preclinical - Cell line xenograft

PMIDs:
26779812

Sources:
JAX-CKB
RUCAPARIB ABCG2

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
RUCAPARIB IDH1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell culture

Response Type sensitive

PMIDs:
28148839

Sources:
JAX-CKB
RUCAPARIB YES1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
RUCAPARIB ABCB1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
RUCAPARIB CYP1A2

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB FDA
RUCAPARIB CYP2D6

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB FDA
RUCAPARIB CYP2C9

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
RUCAPARIB CYP2C19

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
RUCAPARIB CYP3A4

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB

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

RUBRACA Trade Name

RUCAPARIB Generic Name

Drug Info:

Drug Class Small molecule inhibitor

FDA Approval Ovarian cancer (with BRCA mutation)

Publications:

JAX-CKB: Rucaparib

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Kondrashova O et al., 2017 Sep, Secondary Somatic Mutations Restoring RAD51C and RAD51D Associated with Acquired Resistance to the PARP Inhibitor Rucaparib in High-Grade Ovarian Carcinoma., Cancer Discov

Du et al., 2016, Blocking c-Met-mediated PARP1 phosphorylation enhances anti-tumor effects of PARP inhibitors., Nat. Med.

Drew et al., 2016, Phase 2 multicentre trial investigating intermittent and continuous dosing schedules of the poly(ADP-ribose) polymerase inhibitor rucaparib in germline BRCA mutation carriers with advanced ovarian and breast cancer., Br. J. Cancer

CIViC: RUCAPARIB

Version: 14-September-2020

Alternate Names:

Drug Info:

Publications:

Swisher et al., 2017, Rucaparib in relapsed, platinum-sensitive high-grade ovarian carcinoma (ARIEL2 Part 1): an international, multicentre, open-label, phase 2 trial., Lancet Oncol.

Shroff RT et al., 2018, Rucaparib Monotherapy in Patients With Pancreatic Cancer and a Known Deleterious BRCA Mutation., JCO Precis Oncol

TALC: RUCAPARIB
- Version: 12-May-2016
Alternate Names:

RUCAPARIB Drug Generic Name

RUCAPARIB Primary Drug Name

Drug Info:

Publications:
DTC: RUCAPARIB
- Version: 02-September-2020
Alternate Names:

CHEMBL1173055 ChEMBL Drug ID

Drug Info:

Publications:
GuideToPharmacology: 223366069
- Version: 29-September-2020
Alternate Names:

RUCAPARIB GuideToPharmacology Ligand Name

Drug Info:

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

D01SHZ TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL1173055
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ClearityFoundationBiomarkers: RUCAPARIB
- Version: 26-July-2013
Alternate Names:

Drug Info:

Publications:
ClearityFoundationClinicalTrial: RUCAPARIB
- Version: 15-June-2013
Alternate Names:

Drug Info:

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

Drug Info:

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

Drug Info:

Publications:
OncoKB: Rucaparib
- Version: 23-July-2020
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL1173055
- Version: chembl_23
Alternate Names:

Drug Info:

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

Drug Info:

Publications:

Mechanism of Interaction	PARP 1, 2 and 3 inhibitor
Direct Interaction	yes

Specific Action of the Ligand	Inhibition
Endogenous Drug?	False
Direct Interaction?	True

Drug family	PARP inhibitor
Alteration	BRCA2:.
Indication/Tumor Type	ovarian cancer

Indication/Tumor Type	glioblastoma multiforme
Response Type	sensitive
Approval Status	Preclinical

Indication/Tumor Type	ovarian carcinoma
Response Type	sensitive
Approval Status	Clinical Study

combination therapy	AZD6482 + Rucaparib
Indication/Tumor Type	triple-receptor negative breast cancer
Response Type	sensitive

Indication/Tumor Type	breast cancer
combination therapy	Foretinib + Rucaparib
Approval Status	Preclinical - Cell line xenograft

Evidence Type	Actionable
Approval Status	Preclinical - Cell culture
Response Type	sensitive

antagonist (inhibitory)
inhibitor (inhibitory)

antagonist (inhibitory)
inhibitor (inhibitory)

antagonist (inhibitory)
inhibitor (inhibitory)

RUCAPARIB Drug Record

RUCAPARIB chembl:CHEMBL1173055 ApprovedAntineoplastic

Alternate Names:

Drug Info:

Publications:

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

Interaction Info: Mechanism of Interaction PARP 1, 2 and 3 inhibitor Direct Interaction yes

PMIDs: None found

Sources: MyCancerGenome ClearityFoundationClinicalTrial ChemblInteractions PharmGKB

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

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

PMIDs: None found

Sources: TALC MyCancerGenome ClearityFoundationClinicalTrial ChemblInteractions GuideToPharmacology PharmGKB

Interaction Types & Directionality: n/a

Interaction Info: Drug family PARP inhibitor Alteration BRCA2:. Indication/Tumor Type ovarian cancer

PMIDs: 26779812 27002934 30051098 27908594

Sources: ClearityFoundationBiomarkers JAX-CKB CGI CIViC PharmGKB OncoKB

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

Interaction Info: Mechanism of Interaction PARP 1, 2 and 3 inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions PharmGKB

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type glioblastoma multiforme Response Type sensitive Approval Status Preclinical

PMIDs: 21852505 24356817

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type ovarian carcinoma Response Type sensitive Approval Status Clinical Study

PMIDs: 27454289 27002934 26779812 28588062 27908594

Sources: ClearityFoundationBiomarkers JAX-CKB CGI CIViC PharmGKB OncoKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: ClearityFoundationBiomarkers

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PARP 1, 2 and 3 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
MyCancerGenome ClearityFoundationClinicalTrial ChemblInteractions PharmGKB

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
None found

Sources:
TALC MyCancerGenome ClearityFoundationClinicalTrial ChemblInteractions GuideToPharmacology PharmGKB

Interaction Types & Directionality:

n/a

Interaction Info:

Drug family PARP inhibitor

Alteration BRCA2:.

Indication/Tumor Type ovarian cancer

PMIDs:
26779812 27002934 30051098 27908594

Sources:
ClearityFoundationBiomarkers JAX-CKB CGI CIViC PharmGKB OncoKB

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PARP 1, 2 and 3 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions PharmGKB

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type glioblastoma multiforme

Response Type sensitive

Approval Status Preclinical

PMIDs:
21852505 24356817

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
CIViC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type ovarian carcinoma

Response Type sensitive

Approval Status Clinical Study

PMIDs:
27454289 27002934 26779812 28588062 27908594

Sources:
ClearityFoundationBiomarkers JAX-CKB CGI CIViC PharmGKB OncoKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
ClearityFoundationBiomarkers

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy AZD6482 + Rucaparib

Indication/Tumor Type triple-receptor negative breast cancer

Response Type sensitive

PMIDs:
23565244

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
ClearityFoundationBiomarkers

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type breast cancer

combination therapy Foretinib + Rucaparib

Approval Status Preclinical - Cell line xenograft

PMIDs:
26779812

Sources:
JAX-CKB