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OLAPARIB Drug Record

  • Summary
  • Interactions
  • Claims
  • OLAPARIB chembl:CHEMBL521686 ApprovedAntineoplasticImmunotherapy

    Alternate Names:

    LYNPARZA
    AZ2281
    AZD-2281
    AZ-2281
    KU-0059436
    OLAPARIB
    AZD2281
    KEYLYNK-010 COMPONENT OLAPARIB
    OLAPARIB COMPONENT OF KEYLYNK-010
    KU-59436
    4-(3-{[4-(CYCLOPROPYLCARBONYL)PIPERAZIN-1-YL]CARBONYL}-4-FLUOROBENZYL)PHTHALAZIN-1(2H)-ONE
    KU59436
    1-(CYCLOPROPYLCARBONYL)-4-[5-[(3,4-DIHYDRO-4-OXO-1-PHTHALAZINYL)METHYL]-2-FLUOROBENZOYL]PIPERAZINE
    LYNPARZA®
    pubchem.compound:23725625
    drugbank:09074
    rxcui:1597582
    chembl:CHEMBL521686
    chemidplus:763113-22-0

    Drug Info:

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

    Publications:

    Wang et al., 2016, Effective use of PI3K inhibitor BKM120 and PARP inhibitor Olaparib to treat PIK3CA mutant ovarian cancer., Oncotarget
    Frankum et al., 2015, Complementary genetic screens identify the E3 ubiquitin ligase CBLC, as a modifier of PARP inhibitor sensitivity., Oncotarget
    Mo et al., 2016, mTOR Inhibitors Suppress Homologous Recombination Repair and Synergize with PARP Inhibitors via Regulating SUV39H1 in BRCA-Proficient Triple-Negative Breast Cancer., Clin. Cancer Res.
    Drost et al., 2011, BRCA1 RING function is essential for tumor suppression but dispensable for therapy resistance., Cancer Cell
    Drost et al., 2016, BRCA1185delAG tumors may acquire therapy resistance through expression of RING-less BRCA1., J. Clin. Invest.
    Hunter et al., 2014, Dual targeting of hypoxia and homologous recombination repair dysfunction in triple-negative breast cancer., Mol. Cancer Ther.
    Kaufman et al., 2015, Olaparib monotherapy in patients with advanced cancer and a germline BRCA1/2 mutation., J. Clin. Oncol.
    Tutt et al., 2010, Oral poly(ADP-ribose) polymerase inhibitor olaparib in patients with BRCA1 or BRCA2 mutations and advanced breast cancer: a proof-of-concept trial., Lancet
    2017 Aug 9, Olaparib for Metastatic Breast Cancer in Patients with a Germline BRCA Mutation., N Engl J Med
    Gelmon et al., 2011, Olaparib in patients with recurrent high-grade serous or poorly differentiated ovarian carcinoma or triple-negative breast cancer: a phase 2, multicentre, open-label, non-randomised study., Lancet Oncol.
    Liu et al., 2014, Combination cediranib and olaparib versus olaparib alone for women with recurrent platinum-sensitive ovarian cancer: a randomised phase 2 study., Lancet Oncol.
    Fong et al., 2009, Inhibition of poly(ADP-ribose) polymerase in tumors from BRCA mutation carriers., N. Engl. J. Med.
    Robson et al., 2017, Olaparib for Metastatic Breast Cancer in Patients with a Germline BRCA Mutation., N. Engl. J. Med.
    Goff, 2013, Advanced ovarian cancer: what should be the standard of care?, J Gynecol Oncol
    Golan T et al., 2019, Maintenance Olaparib for Germline <i>BRCA</i>-Mutated Metastatic Pancreatic Cancer., N Engl J Med
    Marshall CH et al., 2019, Differential Response to Olaparib Treatment Among Men with Metastatic Castration-resistant Prostate Cancer Harboring BRCA1 or BRCA2 Versus ATM Mutations., Eur Urol
    Moore K et al., 2018, Maintenance Olaparib in Patients with Newly Diagnosed Advanced Ovarian Cancer., N Engl J Med
    Ledermann J et al., 2014, Olaparib maintenance therapy in patients with platinum-sensitive relapsed serous ovarian cancer: a preplanned retrospective analysis of outcomes by BRCA status in a randomised phase 2 trial., Lancet Oncol
    Caulfield SE et al., 2019, Olaparib: A Novel Therapy for Metastatic Breast Cancer in Patients With a <i>BRCA</i>1/2 Mutation., J Adv Pract Oncol
    Bajrami et al., 2014, Genome-wide profiling of genetic synthetic lethality identifies CDK12 as a novel determinant of PARP1/2 inhibitor sensitivity., Cancer Res.
    Sulkowski et al., 2017, 2-Hydroxyglutarate produced by neomorphic IDH mutations suppresses homologous recombination and induces PARP inhibitor sensitivity., Sci Transl Med
    Verhagen et al., 2015, Extent of radiosensitization by the PARP inhibitor olaparib depends on its dose, the radiation dose and the integrity of the homologous recombination pathway of tumor cells., Radiother Oncol
    Kubota et al., 2014, Low ATM protein expression and depletion of p53 correlates with olaparib sensitivity in gastric cancer cell lines., Cell Cycle
    Mateo et al., 2015, DNA-Repair Defects and Olaparib in Metastatic Prostate Cancer., N. Engl. J. Med.
    Williamson et al., 2010, ATM deficiency sensitizes mantle cell lymphoma cells to poly(ADP-ribose) polymerase-1 inhibitors., Mol. Cancer Ther.
    Weston et al., 2010, The PARP inhibitor olaparib induces significant killing of ATM-deficient lymphoid tumor cells in vitro and in vivo., Blood
    Bang et al., 2015, Randomized, Double-Blind Phase II Trial With Prospective Classification by ATM Protein Level to Evaluate the Efficacy and Tolerability of Olaparib Plus Paclitaxel in Patients With Recurrent or Metastatic Gastric Cancer., J. Clin. Oncol.
    Schmitt et al., 2017, ATM Deficiency Is Associated with Sensitivity to PARP1- and ATR Inhibitors in Lung Adenocarcinoma., Cancer Res.
    Moroi et al., 1975, Comparison between procaine and isocarboxazid metabolism in vitro by a liver microsomal amidase-esterase., Biochem. Pharmacol.
    Poole-Wilson et al., 1975, Effect of pH on ionic exchange and function in rat and rabbit myocardium., Am. J. Physiol.
    de Bono J et al., 2020, Olaparib for Metastatic Castration-Resistant Prostate Cancer., N Engl J Med
    Valiakhmetova A et al., 2020, Treatment of Pediatric Glioblastoma with Combination Olaparib and Temozolomide Demonstrates 2-Year Durable Response., Oncologist
    Stachelek et al., 2015, YU238259 Is a Novel Inhibitor of Homology-Dependent DNA Repair That Exhibits Synthetic Lethality and Radiosensitization in Repair-Deficient Tumors., Mol. Cancer Res.
    Kortmann et al., 2011, Tumor growth inhibition by olaparib in BRCA2 germline-mutated patient-derived ovarian cancer tissue xenografts., Clin. Cancer Res.
    Shah et al., 1975, Cardiovascular effects of beta-receptor stimulants in healthy volunteers., Indian Heart J
    Akamatsu et al., 1975, Increase in acetyl CoA synthetase activity after phenobarbital treatment., Biochem. Pharmacol.
    Tan et al., 1975, Characteristics of the dephosphorylated form of phosphorylase purified from rat liver and measurement of its activity in crude liver preparations., Biochim. Biophys. Acta
    1991, Thallium scintigraphy., Lancet
    Menear et al., 2008, 4-[3-(4-cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: a novel bioavailable inhibitor of poly(ADP-ribose) polymerase-1., J. Med. Chem.
    Kivlin CM et al., 2016, Poly (ADP) ribose polymerase inhibition: A potential treatment of malignant peripheral nerve sheath tumor., Cancer Biol Ther
    Pignochino Y et al., 2017, PARP1 expression drives the synergistic antitumor activity of trabectedin and PARP1 inhibitors in sarcoma preclinical models., Mol Cancer
    Gilabert M et al., 2014, Poly(ADP-ribose) polymerase 1 (PARP1) overexpression in human breast cancer stem cells and resistance to olaparib., PLoS One
    Parrotta R et al., 2017, A Novel BRCA1-Associated Protein-1 Isoform Affects Response of Mesothelioma Cells to Drugs Impairing BRCA1-Mediated DNA Repair., J Thorac Oncol
    Peña-Llopis S et al., 2012, BAP1 loss defines a new class of renal cell carcinoma., Nat Genet
    Sen et al., 2017, CHK1 Inhibition in Small-Cell Lung Cancer Produces Single-Agent Activity in Biomarker-Defined Disease Subsets and Combination Activity with Cisplatin or Olaparib., Cancer Res.
    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.
    Du et al., 2016, Blocking c-Met-mediated PARP1 phosphorylation enhances anti-tumor effects of PARP inhibitors., Nat. Med.
    Okazaki et al., 2017, Glutaminase and poly(ADP-ribose) polymerase inhibitors suppress pyrimidine synthesis and VHL-deficient renal cancers., J. Clin. Invest.
    Ozden O et al., 2016, Expression of an Oncogenic BARD1 Splice Variant Impairs Homologous Recombination and Predicts Response to PARP-1 Inhibitor Therapy in Colon Cancer., Sci Rep
  • OLAPARIB   CBLC

    Interaction Score: 4.58

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type osteosarcoma
    Response Type predicted – sensitive
    Approval Status Preclinical

    PMIDs:
    25883215


    Sources:
    JAX-CKB

  • OLAPARIB   BRCA2

    Interaction Score: 2.47

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type ovarian cancer
    Response Type sensitive
    Approval Status Preclinical - Pdx

    PMIDs:
    32043779 28792849 21862407 25218906 19553641 25366685 28578601 26510020 23346317 26546619 26116172 20609467 21097693 322 15 75 1682772 31157963 30345884 24882434 32343890 30797618


    Sources:
    ClearityFoundationBiomarkers JAX-CKB CIViC PharmGKB OncoKB

  • OLAPARIB   PALB2

    Interaction Score: 2.29

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    26510020 32343890


    Sources:
    CIViC

  • OLAPARIB   PARP1

    Interaction Score: 1.91

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    25981132 18800822 26650448 28454547 25144364


    Sources:
    DTC MyCancerGenome ClearityFoundationClinicalTrial ChemblInteractions CIViC

  • OLAPARIB   BARD1

    Interaction Score: 1.37

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27197561 28389374


    Sources:
    CIViC

  • OLAPARIB   PARP2

    Interaction Score: 1.31

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    25981132


    Sources:
    MyCancerGenome ClearityFoundationClinicalTrial ChemblInteractions

  • OLAPARIB   BAP1

    Interaction Score: 1.14

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    28389374 22683710


    Sources:
    CIViC

  • OLAPARIB   PARP3

    Interaction Score: 0.92

    Interaction Types & Directionality:
    inhibitor (inhibitory)

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

    PMIDs:
    25981132


    Sources:
    ChemblInteractions

  • OLAPARIB   STAG2

    Interaction Score: 0.86

    Interaction Types & Directionality:
    n/a

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

    PMIDs:
    21852505 24356817


    Sources:
    JAX-CKB

  • OLAPARIB   IDH2

    Interaction Score: 0.76

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    28148839


    Sources:
    CIViC

  • OLAPARIB   CDK12

    Interaction Score: 0.57

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24240700


    Sources:
    CIViC

  • OLAPARIB   ATM

    Interaction Score: 0.55

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type lung adenocarcinoma
    Response Type sensitive
    Approval Status Preclinical

    PMIDs:
    24841718 26510020 20124459 20739657 26282658 28363999 8 2014 32343890


    Sources:
    ClearityFoundationBiomarkers JAX-CKB CIViC OncoKB

  • OLAPARIB   BRCA1

    Interaction Score: 0.52

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type breast cancer
    Response Type sensitive
    Approval Status Phase II

    PMIDs:
    26546619 22172724 27454287 25193512 25366685 20609467 28792849 21862407 25218906 19553641 28578601 23346317 31157963 30797618 30345884 24882434 31538027


    Sources:
    ClearityFoundationBiomarkers JAX-CKB CIViC PharmGKB OncoKB

  • OLAPARIB   VHL

    Interaction Score: 0.31

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy BPTES + Olaparib
    Indication/Tumor Type renal cell carcinoma
    Response Type sensitive

    PMIDs:
    28346230


    Sources:
    JAX-CKB

  • OLAPARIB   ATR

    Interaction Score: 0.29

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    ClearityFoundationBiomarkers

  • OLAPARIB   CHEK1

    Interaction Score: 0.14

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    28490518


    Sources:
    CIViC

  • OLAPARIB   MYC

    Interaction Score: 0.11

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    28490518


    Sources:
    CIViC

  • OLAPARIB   PGR

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB FDA

  • OLAPARIB   ERBB2

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type Her2-receptor negative breast cancer
    Response Type predicted – sensitive
    Approval Status Phase III

    PMIDs:
    None found


    Sources:
    JAX-CKB PharmGKB FDA

  • OLAPARIB   MET

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type triple-receptor negative breast cancer
    Response Type sensitive
    Approval Status Preclinical

    PMIDs:
    26779812


    Sources:
    JAX-CKB

  • OLAPARIB   ESR2

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • OLAPARIB   KRAS

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Evidence Type Actionable
    Approval Status Preclinical
    Response Type sensitive

    PMIDs:
    28363999


    Sources:
    JAX-CKB

  • OLAPARIB   PIK3CA

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy BKM120 + Olaparib
    Indication/Tumor Type ovarian cancer
    Response Type sensitive

    PMIDs:
    26909613


    Sources:
    JAX-CKB

  • OLAPARIB   PTEN

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy AZD6482 + Olaparib
    Indication/Tumor Type triple-receptor negative breast cancer
    Response Type sensitive

    PMIDs:
    None found


    Sources:
    JAX-CKB

  • OLAPARIB   ESR1

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB FDA

  • OLAPARIB   IDH1

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type Advanced Solid Tumor
    Response Type sensitive
    Approval Status Preclinical - Cell culture

    PMIDs:
    28148839


    Sources:
    JAX-CKB CIViC

  • OLAPARIB   TP53

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type breast cancer
    Response Type decreased response
    Approval Status Preclinical

    PMIDs:
    22172724


    Sources:
    JAX-CKB

  • MyCancerGenome: OLAPARIB

    • Version: 20-Jun-2017

    Alternate Names:
    AZD2281 Development Name
    OLAPARIB Generic Name
    LYNPARZA Trade Name

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

    Publications:

  • DTC: OLAPARIB

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL521686 ChEMBL Drug ID

    Drug Info:

    Publications:
    Menear et al., 2008, 4-[3-(4-cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: a novel bioavailable inhibitor of poly(ADP-ribose) polymerase-1., J. Med. Chem.

  • JAX-CKB: Olaparib

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Wang et al., 2016, Effective use of PI3K inhibitor BKM120 and PARP inhibitor Olaparib to treat PIK3CA mutant ovarian cancer., Oncotarget
    Frankum et al., 2015, Complementary genetic screens identify the E3 ubiquitin ligase CBLC, as a modifier of PARP inhibitor sensitivity., Oncotarget
    Weston et al., 2010, The PARP inhibitor olaparib induces significant killing of ATM-deficient lymphoid tumor cells in vitro and in vivo., Blood

  • CIViC: OLAPARIB

    • Version: 14-September-2020

    Alternate Names:

    Drug Info:

    Publications:
    Golan T et al., 2019, Maintenance Olaparib for Germline &lt;i&gt;BRCA&lt;/i&gt;-Mutated Metastatic Pancreatic Cancer., N Engl J Med
    Goff, 2013, Advanced ovarian cancer: what should be the standard of care?, J Gynecol Oncol
    Moore K et al., 2018, Maintenance Olaparib in Patients with Newly Diagnosed Advanced Ovarian Cancer., N Engl J Med

  • TTD: Olaparib

    • Version: 2020.06.01

    Alternate Names:
    D0J9HW TTD Drug ID

    Drug Info:

    Publications:

  • TALC: OLAPARIB

    • Version: 12-May-2016

    Alternate Names:
    OLAPARIB Primary Drug Name
    OLAPARIB Drug Generic Name
    AZD2281 Drug Synonym

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL521686

    • Version: chembl_23

    Alternate Names:

    Drug Info:

    Publications:

  • PharmGKB: olaparib

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL521686

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • ClearityFoundationBiomarkers: OLAPARIB

    • Version: 26-July-2013

    Alternate Names:

    Drug Info:

    Publications:

  • ClearityFoundationClinicalTrial: OLAPARIB

    • Version: 15-June-2013

    Alternate Names:

    Drug Info:

    Publications:

  • OncoKB: Olaparib

    • Version: 23-July-2020

    Alternate Names:

    Drug Info:

    Publications:

  • FDA: Olaparib

    • 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.

The dgidb.org website does not provide any medical or healthcare products, services or advice, and is not for medical emergencies or urgent situations. IF YOU THINK YOU MAY HAVE A MEDICAL EMERGENCY, CALL YOUR DOCTOR OR 911 IMMEDIATELY. Information contained on this website is not a substitute for a doctor's medical judgment or advice. We recommend that you discuss your specific, individual health concerns with your doctor or health care professional.

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