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RUCAPARIB Drug Record

  • Summary
  • Interactions
  • Claims
  • 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
    Drug Categories antineoplastic and immunomodulating agents
    Drug Categories bcrp/abcg2 inhibitors
    Drug Categories bcrp/abcg2 substrates
    Drug Categories cytochrome p-450 cyp1a2 inducers
    Drug Categories cytochrome p-450 cyp1a2 inducers (moderate)
    Drug Categories cytochrome p-450 cyp1a2 inhibitors
    Drug Categories cytochrome p-450 cyp1a2 inhibitors (weak)
    Drug Categories cytochrome p-450 cyp1a2 substrates with a narrow therapeutic index
    Drug Categories cytochrome p-450 cyp2c19 inhibitors
    Drug Categories cytochrome p-450 cyp2c19 inhibitors (weak)
    Drug Categories cytochrome p-450 cyp2c8 inhibitors
    Drug Categories cytochrome p-450 cyp2c8 inhibitors (weak)
    Drug Categories cytochrome p-450 cyp2c9 inhibitors
    Drug Categories cytochrome p-450 cyp2c9 inhibitors (strength unknown)
    Drug Categories cytochrome p-450 cyp2d6 inhibitors
    Drug Categories cytochrome p-450 cyp2d6 inhibitors (moderate)
    Drug Categories cytochrome p-450 cyp2d6 substrates with a narrow therapeutic index
    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 (weak)
    Drug Categories cytochrome p-450 cyp3a4 substrates with a narrow therapeutic index
    Drug Categories cytochrome p-450 cyp3a5 inhibitors
    Drug Categories cytochrome p-450 cyp3a5 inhibitors (strength unknown)
    Drug Categories cytochrome p-450 cyp3a7 inhibitors
    Drug Categories cytochrome p-450 cyp3a7 inhibitors (strength unknown)
    Drug Categories cytochrome p-450 enzyme inducers
    Drug Categories cytochrome p-450 enzyme inhibitors
    Drug Categories cytochrome p-450 substrates
    Drug Categories heterocyclic compounds, fused-ring
    Drug Categories mate 1 inhibitors
    Drug Categories mate 2 inhibitors
    Drug Categories mate inhibitors
    Drug Categories oat1/slc22a6 inhibitors
    Drug Categories oat3/slc22a8 inhibitors
    Drug Categories oatp1b1/slco1b1 inhibitors
    Drug Categories oatp1b3 inhibitors
    Drug Categories oct1 inhibitors
    Drug Categories p-glycoprotein inhibitors
    Drug Categories p-glycoprotein substrates
    Drug Categories ugt1a1 inhibitors
    (12 More Sources)

    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.
    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
    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
    Wang et al., 2016, RING domain-deficient BRCA1 promotes PARP inhibitor and platinum resistance., J. Clin. Invest.
    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: 1.23

    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:
    ClearityFoundationClinicalTrial PharmGKB DrugBank MyCancerGenome ChemblInteractions

  • RUCAPARIB   PARP3

    Interaction Score: 0.74

    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:
    PharmGKB DrugBank ChemblInteractions

  • RUCAPARIB   BRCA2

    Interaction Score: 0.69

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    27908594 26779812 27002934 30051098


    Sources:
    ClearityFoundationBiomarkers OncoKB PharmGKB JAX-CKB CIViC CGI

  • RUCAPARIB   STAG2

    Interaction Score: 0.65

    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: 0.57

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    CIViC

  • RUCAPARIB   SLC47A2

    Interaction Score: 0.57

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • RUCAPARIB   PARP1

    Interaction Score: 0.52

    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:
    ClearityFoundationClinicalTrial PharmGKB DrugBank TALC MyCancerGenome GuideToPharmacology ChemblInteractions

  • RUCAPARIB   SLC47A1

    Interaction Score: 0.43

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • RUCAPARIB   BRCA1

    Interaction Score: 0.2

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    28588062 27908594 26779812 27002934 27454289


    Sources:
    ClearityFoundationBiomarkers OncoKB PharmGKB JAX-CKB CIViC CGI

  • RUCAPARIB   ATR

    Interaction Score: 0.17

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    ClearityFoundationBiomarkers

  • RUCAPARIB   SLC22A6

    Interaction Score: 0.17

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • RUCAPARIB   SLC22A8

    Interaction Score: 0.11

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • RUCAPARIB   DYRK1A

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • RUCAPARIB   SLCO1B3

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • RUCAPARIB   CYP2C8

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • RUCAPARIB   ABCC4

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • RUCAPARIB   PRKD2

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • RUCAPARIB   UGT1A1

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • RUCAPARIB   PIM1

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • RUCAPARIB   PTEN

    Interaction Score: 0.03

    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: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • RUCAPARIB   ATM

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    ClearityFoundationBiomarkers

  • RUCAPARIB   CDK1

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • RUCAPARIB   MET

    Interaction Score: 0.03

    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:
    FDA PharmGKB

  • RUCAPARIB   CYP2D6

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    FDA PharmGKB

  • 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:
    RUCAPARIB Generic Name
    RUBRACA Trade Name

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

    Publications:

  • DrugBank: DB12332

    • Version: 5.1.7

    Alternate Names:
    RUCAPARIB DrugBank Drug Name
    283173-50-2 CAS Number
    Rubraca Drug Brand

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

    Publications:

  • JAX-CKB: Rucaparib

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    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
    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 <i>BRCA</i> Mutation., JCO Precis Oncol

  • TALC: RUCAPARIB

    • Version: 12-May-2016

    Alternate Names:
    RUCAPARIB Primary Drug Name
    RUCAPARIB Drug Generic 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:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

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DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21