DGIdb - OLAPARIB Drug Record

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:

Drug Categories	cytochrome p-450 cyp3a4 inhibitors (moderate)
Drug Categories	cytochrome p-450 cyp3a inhibitors
FDA Approval	Ovarian cancer (with BRCA mutation)
Drug Class	Small molecule inhibitor
Drug Categories	bcrp/abcg2 inhibitors
Drug Categories	cytochrome p-450 cyp2b6 inducers (strength unknown)
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 substrates
Drug Categories	cytochrome p-450 enzyme inducers
Drug Categories	cytochrome p-450 enzyme inhibitors
Drug Categories	cytochrome p-450 substrates
Drug Categories	immunosuppressive agents
Drug Categories	p-glycoprotein inhibitors
Drug Categories	p-glycoprotein substrates

(12 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
Golan T et al., 2019, Maintenance Olaparib for Germline <i>BRCA</i>-Mutated Metastatic Pancreatic Cancer., N Engl J Med
Goff, 2013, Advanced ovarian cancer: what should be the standard of care?, J Gynecol Oncol
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.
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
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.
Moore K et al., 2018, Maintenance Olaparib in Patients with Newly Diagnosed Advanced Ovarian Cancer., N Engl J Med
Kaufman et al., 2015, Olaparib monotherapy in patients with advanced cancer and a germline BRCA1/2 mutation., J. Clin. Oncol.
Fong et al., 2009, Inhibition of poly(ADP-ribose) polymerase in tumors from BRCA mutation carriers., N. Engl. J. Med.
2017 Aug 9, Olaparib for Metastatic Breast Cancer in Patients with a Germline BRCA Mutation., N Engl J Med
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.
Robson et al., 2017, 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.
Drost et al., 2011, BRCA1 RING function is essential for tumor suppression but dispensable for therapy resistance., Cancer Cell
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
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
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
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
Weston et al., 2010, The PARP inhibitor olaparib induces significant killing of ATM-deficient lymphoid tumor cells in vitro and in vivo., Blood
Mateo et al., 2015, DNA-Repair Defects and Olaparib in Metastatic Prostate Cancer., N. Engl. J. Med.
de Bono J et al., 2020, Olaparib for Metastatic Castration-Resistant Prostate Cancer., N Engl J Med
Schmitt et al., 2017, ATM Deficiency Is Associated with Sensitivity to PARP1- and ATR Inhibitors in Lung Adenocarcinoma., Cancer Res.
Williamson et al., 2010, ATM deficiency sensitizes mantle cell lymphoma cells to poly(ADP-ribose) polymerase-1 inhibitors., Mol. Cancer Ther.
Kubota et al., 2014, Low ATM protein expression and depletion of p53 correlates with olaparib sensitivity in gastric cancer cell lines., Cell Cycle
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.
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.
Shah et al., 1975, Cardiovascular effects of beta-receptor stimulants in healthy volunteers., Indian Heart J
Silen et al., 1975, Acid-base balance in amphibian gastric mucosa., Am. J. Physiol.
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
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.
Valiakhmetova A et al., 2020, Treatment of Pediatric Glioblastoma with Combination Olaparib and Temozolomide Demonstrates 2-Year Durable Response., Oncologist
Akamatsu et al., 1975, Increase in acetyl CoA synthetase activity after phenobarbital treatment., Biochem. Pharmacol.
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
Kivlin CM et al., 2016, Poly (ADP) ribose polymerase inhibition: A potential treatment of malignant peripheral nerve sheath tumor., Cancer Biol Ther
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.
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: 3.79

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: 2.12

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type ovarian cancer

Response Type sensitive

Approval Status Preclinical - Pdx

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

Sources:
ClearityFoundationBiomarkers OncoKB PharmGKB JAX-CKB CIViC CGI
OLAPARIB PALB2

Interaction Score: 1.89

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
26510020 32343890

Sources:
CIViC
OLAPARIB PARP2

Interaction Score: 1.62

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction PARP 1, 2 & 3 inhibitor

Details of the Assay for Interaction Assayed using PARP-2 isolated from HeLa cells, in a scintillation proximity ELISA.

PMIDs:
25981132

Sources:
ClearityFoundationClinicalTrial DrugBank MyCancerGenome GuideToPharmacology ChemblInteractions
OLAPARIB BARD1

Interaction Score: 1.14

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
28389374 27197561

Sources:
CIViC
OLAPARIB PARP1

Interaction Score: 0.99

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PARP 1, 2 & 3 inhibitor

Direct Interaction yes

Details of the Assay for Interaction Assayed using PARP-1 isolated from HeLa cells, in a scintillation proximity ELISA.

PMIDs:
25981132 28454547 25144364 26650448 18800822

Sources:
ClearityFoundationClinicalTrial DTC CIViC DrugBank MyCancerGenome GuideToPharmacology ChemblInteractions
OLAPARIB FANCA

Interaction Score: 0.95

Interaction Types & Directionality:

n/a

Interaction Info:

Alteration FANCA:del

Drug family PARP inhibitor

Alteration FANCA:.

PMIDs:
None found

Sources:
CGI
OLAPARIB BAP1

Interaction Score: 0.95

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
28389374 22683710

Sources:
CIViC
OLAPARIB PARP3

Interaction Score: 0.81

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PARP 1, 2 & 3 inhibitor

Direct Interaction yes

PMIDs:
25981132

Sources:
DrugBank ChemblInteractions
OLAPARIB STAG2

Interaction Score: 0.71

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: 0.63

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
28148839

Sources:
CIViC
OLAPARIB ATM

Interaction Score: 0.48

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type lung adenocarcinoma

Response Type sensitive

Approval Status Preclinical

PMIDs:
20739657 26510020 32343890 28363999 20124459 24841718 8 2014 26282658

Sources:
ClearityFoundationBiomarkers OncoKB JAX-CKB CIViC CGI
OLAPARIB CDK12

Interaction Score: 0.47

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24240700

Sources:
CIViC
OLAPARIB BRCA1

Interaction Score: 0.45

Interaction Types & Directionality:

n/a

Interaction Info:

Alteration BRCA1:.

Drug family PARP inhibitor

Indication/Tumor Type breast cancer

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

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

Interaction Score: 0.38

Interaction Types & Directionality:

n/a

Interaction Info:

Alteration ATR:del

Alteration ATR:.

Drug family PARP inhibitor

PMIDs:
None found

Sources:
ClearityFoundationBiomarkers CGI
OLAPARIB CHEK2

Interaction Score: 0.26

Interaction Types & Directionality:

n/a

Interaction Info:

Alteration CHEK2:del

Alteration CHEK2:.

Drug family PARP inhibitor

PMIDs:
26510020 322 2015

Sources:
CGI
OLAPARIB VHL

Interaction Score: 0.22

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 MYC

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
28490518

Sources:
CIViC
OLAPARIB CHEK1

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
28490518

Sources:
CIViC
OLAPARIB PGR

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
FDA PharmGKB
OLAPARIB ERBB2

Interaction Score: 0.04

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:
FDA PharmGKB JAX-CKB
OLAPARIB HDAC2

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

Drug family PARP inhibitor

Alteration HDAC2:.

PMIDs:
None found

Sources:
CGI
OLAPARIB MET

Interaction Score: 0.03

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 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: 0.02

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 ESR2

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
OLAPARIB ESR1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
FDA PharmGKB
OLAPARIB IDH1

Interaction Score: 0.01

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

DrugBank: DB09074

Version: 5.1.7

Alternate Names:

OLAPARIB DrugBank Drug Name

763113-22-0 CAS Number

Lynparza Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Categories antineoplastic agents

Publications:

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

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.

CGI: Olaparib

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Mateo et al., 2015, DNA-Repair Defects and Olaparib in Metastatic Prostate Cancer., N. Engl. J. Med.

Shah et al., 1975, Cardiovascular effects of beta-receptor stimulants in healthy volunteers., Indian Heart J

Silen et al., 1975, Acid-base balance in amphibian gastric mucosa., Am. J. Physiol.

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 <i>BRCA</i>-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:
GuideToPharmacology: 187051821
- Version: 29-September-2020
Alternate Names:

OLAPARIB GuideToPharmacology Ligand Name

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:

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

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

Direct Interaction	yes
Mechanism of Interaction	PARP 1, 2 & 3 inhibitor
Details of the Assay for Interaction	Assayed using PARP-2 isolated from HeLa cells, in a scintillation proximity ELISA.

Alteration	FANCA:del
Drug family	PARP inhibitor
Alteration	FANCA:.

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

Indication/Tumor Type	lung adenocarcinoma
Response Type	sensitive
Approval Status	Preclinical

Alteration	BRCA1:.
Drug family	PARP inhibitor
Indication/Tumor Type	breast cancer

Alteration	CHEK2:del
Alteration	CHEK2:.
Drug family	PARP inhibitor

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

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

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

Evidence Type	Actionable
Approval Status	Preclinical
Response Type	sensitive

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

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

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

OLAPARIB	DrugBank Drug Name
763113-22-0	CAS Number
Lynparza	Drug Brand

Drug Type	small molecule
Drug Groups	approved
Drug Categories	antineoplastic agents

AZD2281	Development Name
OLAPARIB	Generic Name
LYNPARZA	Trade Name

OLAPARIB	Primary Drug Name
OLAPARIB	Drug Generic Name
AZD2281	Drug Synonym

OLAPARIB Drug Record

OLAPARIB chembl:CHEMBL521686 ApprovedAntineoplasticImmunotherapy

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

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

PMIDs: 25883215

Sources: JAX-CKB

Interaction Types & Directionality: n/a

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

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

Sources: ClearityFoundationBiomarkers OncoKB PharmGKB JAX-CKB CIViC CGI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 26510020 32343890

Sources: CIViC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction PARP 1, 2 & 3 inhibitor Details of the Assay for Interaction Assayed using PARP-2 isolated from HeLa cells, in a scintillation proximity ELISA.

PMIDs: 25981132

Sources: ClearityFoundationClinicalTrial DrugBank MyCancerGenome GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 28389374 27197561

Sources: CIViC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction PARP 1, 2 & 3 inhibitor Direct Interaction yes Details of the Assay for Interaction Assayed using PARP-1 isolated from HeLa cells, in a scintillation proximity ELISA.

PMIDs: 25981132 28454547 25144364 26650448 18800822

Sources: ClearityFoundationClinicalTrial DTC CIViC DrugBank MyCancerGenome GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info: Alteration FANCA:del Drug family PARP inhibitor Alteration FANCA:.

PMIDs: None found

Sources: CGI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 28389374 22683710

Sources: CIViC

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: 25981132

Sources: DrugBank ChemblInteractions

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

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 28148839

Sources: CIViC

Interaction Types & Directionality: n/a

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

PMIDs: 20739657 26510020 32343890 28363999 20124459 24841718 8 2014 26282658

Sources: ClearityFoundationBiomarkers OncoKB JAX-CKB CIViC CGI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24240700

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info: Alteration BRCA1:. Drug family PARP inhibitor Indication/Tumor Type breast cancer

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

Sources: ClearityFoundationBiomarkers OncoKB PharmGKB JAX-CKB CIViC CGI

Interaction Types & Directionality: n/a

Interaction Info: Alteration ATR:del Alteration ATR:. Drug family PARP inhibitor

PMIDs: None found

Sources: ClearityFoundationBiomarkers CGI

Interaction Types & Directionality: n/a

Interaction Info: Alteration CHEK2:del Alteration CHEK2:. Drug family PARP inhibitor

PMIDs: 26510020 322 2015

Sources: CGI

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

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 28490518

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 28490518

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type osteosarcoma

Response Type predicted – sensitive

Approval Status Preclinical

PMIDs:
25883215

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type ovarian cancer

Response Type sensitive

Approval Status Preclinical - Pdx

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

Sources:
ClearityFoundationBiomarkers OncoKB PharmGKB JAX-CKB CIViC CGI

Interaction Types & Directionality:

n/a

PMIDs:
26510020 32343890

Sources:
CIViC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction PARP 1, 2 & 3 inhibitor

Details of the Assay for Interaction Assayed using PARP-2 isolated from HeLa cells, in a scintillation proximity ELISA.

PMIDs:
25981132

Sources:
ClearityFoundationClinicalTrial DrugBank MyCancerGenome GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
28389374 27197561

Sources:
CIViC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PARP 1, 2 & 3 inhibitor

Direct Interaction yes

Details of the Assay for Interaction Assayed using PARP-1 isolated from HeLa cells, in a scintillation proximity ELISA.

PMIDs:
25981132 28454547 25144364 26650448 18800822

Sources:
ClearityFoundationClinicalTrial DTC CIViC DrugBank MyCancerGenome GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

n/a

Interaction Info:

Alteration FANCA:del

Drug family PARP inhibitor

Alteration FANCA:.

PMIDs:
None found

Sources:
CGI

Interaction Types & Directionality:

n/a

PMIDs:
28389374 22683710

Sources:
CIViC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction PARP 1, 2 & 3 inhibitor

Direct Interaction yes

PMIDs:
25981132

Sources:
DrugBank ChemblInteractions

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

Interaction Types & Directionality:

n/a

PMIDs:
28148839

Sources:
CIViC

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type lung adenocarcinoma

Response Type sensitive

Approval Status Preclinical

PMIDs:
20739657 26510020 32343890 28363999 20124459 24841718 8 2014 26282658

Sources:
ClearityFoundationBiomarkers OncoKB JAX-CKB CIViC CGI

Interaction Types & Directionality:

n/a

PMIDs:
24240700

Sources:
CIViC

Interaction Types & Directionality:

n/a

Interaction Info:

Alteration BRCA1:.

Drug family PARP inhibitor

Indication/Tumor Type breast cancer

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

Sources:
ClearityFoundationBiomarkers OncoKB PharmGKB JAX-CKB CIViC CGI

Interaction Types & Directionality:

n/a

Interaction Info:

Alteration ATR:del

Alteration ATR:.

Drug family PARP inhibitor

PMIDs:
None found

Sources:
ClearityFoundationBiomarkers CGI

Interaction Types & Directionality:

n/a

Interaction Info:

Alteration CHEK2:del

Alteration CHEK2:.

Drug family PARP inhibitor

PMIDs:
26510020 322 2015

Sources:
CGI

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

Interaction Types & Directionality:

n/a

PMIDs:
28490518

Sources:
CIViC

Interaction Types & Directionality:

n/a

PMIDs:
28490518

Sources:
CIViC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
FDA PharmGKB

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:
FDA PharmGKB JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Drug family PARP inhibitor

Alteration HDAC2:.

PMIDs:
None found

Sources:
CGI