Identification

Logo pink
Are you a
new drug developer?
Contact us to learn more about our customized products and solutions.
Logo pink
Stay in the know!
As part of our commitment to providing the most up-to-date drug information, we will be releasing #DrugBankUpdates with our newly added curated drug pages.
#DrugBankUpdates
Name
Olaparib
Accession Number
DB09074  (DB05940)
Type
Small Molecule
Groups
Approved
Description

Olaparib is an inhibitor of poly (ADP-ribose) polymerase (PARP) enzymes, including PARP1, PARP2, and PARP3. PARP enzymes are involved in normal cellular homeostasis, such as DNA transcription, cell cycle regulation, and DNA repair. Olaparib has been shown to inhibit growth of select tumor cell lines in vitro and decrease tumor growth in mouse xenograft models of human cancer both as monotherapy or following platinum-based chemotherapy. Increased cytotoxicity and anti-tumor activity following treatment with olaparib were noted in cell lines and mouse tumor models with deficiencies in BRCA. In vitro studies have shown that olaparib-induced cytotoxicity may involve inhibition of PARP enzymatic activity and increased formation of PARP-DNA complex, resulting in disruption of cellular homeostasis and cell death.

Olaparib is available as oral tablets marketed under the brand name Lynparza and was initially indicated as a maintenance therapy or monotherapy for the treatment of adult patients with recurrent epithelial ovarian, fallopian tube or primary peritoneal cancer. On January 12, 2018, FDA expanded the approved use of Lynparza to include chemotherapy-experienced patients with germline breast cancer susceptibility gene (BRCA) mutated, human epidermal growth factor receptor 2 (HER2)-negative metastatic breast cancer. In a randomized clinical trial involving patients with HER2-negative metastatic breast cancer with a germline BRCA mutation, the median progression-free survival for patients taking Lynparza was 7 months compared to 4.2 months for patients taking chemotherapy only. Patient selection for this newly-approved indication can be performed based on an FDA-approved genetic test, called the BRACAnalysis CDx.

Moreover, in December of 2018 the FDA further approved the categorization and use of Lynparza (olaparib) as frontline maintenance therapy in ovarian cancer, making the medication the first time a PARP inhibitor has been approved in the first-line maintenance setting 7. This new approval for frontline maintenance now allows patients who have had surgery and complete or partial response to platinum-based therapy after being first diagnosed with the cancer to be treated with olaparib to decrease the risk of recurrence or delay it significantly 7. This approval is based on findings from the phase 3 SOLO-1 trial for olaparib, which demonstrated the capacity for the agent to reduce the risk of disease progression or death by 70% in patients with BRCA-mutant advanced ovarian cancer who were in complete or partial response to platinum-based chemotherapy 7. It is expected that the ability to offer this important first-line maintenance treatment option to eligible patients may slow down or even stop the natural course of disease progression 7.

Structure
Thumb
Synonyms
  • 4-(3-{[4-(cyclopropylcarbonyl)piperazin-1-yl]carbonyl}-4-fluorobenzyl)phthalazin-1(2H)-one
  • Olaparib
External IDs
AZD 2281 / AZD-2281 / AZD2281 / KU-0059436 / KU-59436 / KU59436
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
LynparzaCapsule50 mgOralAstra Zeneca2016-05-16Not applicableCanada
LynparzaTablet, film coated150 mg/1OralAstraZeneca Pharmaceuticals LP2017-08-17Not applicableUs
LynparzaTablet, film coated100 mg/1OralAstraZeneca Pharmaceuticals LP2017-08-17Not applicableUs
LynparzaTablet150 mgOralAstra Zeneca2018-05-23Not applicableCanada
LynparzaCapsule50 mg/1OralAstraZeneca Pharmaceuticals LP2014-12-242020-03-31Us
LynparzaTablet100 mgOralAstra Zeneca2018-05-23Not applicableCanada
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

    Learn more
Categories
UNII
WOH1JD9AR8
CAS number
763113-22-0
Weight
Average: 434.4628
Monoisotopic: 434.175418827
Chemical Formula
C24H23FN4O3
InChI Key
FDLYAMZZIXQODN-UHFFFAOYSA-N
InChI
InChI=1S/C24H23FN4O3/c25-20-8-5-15(14-21-17-3-1-2-4-18(17)22(30)27-26-21)13-19(20)24(32)29-11-9-28(10-12-29)23(31)16-6-7-16/h1-5,8,13,16H,6-7,9-12,14H2,(H,27,30)
IUPAC Name
4-{[3-(4-cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorophenyl]methyl}phthalazin-1-ol
SMILES
OC1=NN=C(CC2=CC(C(=O)N3CCN(CC3)C(=O)C3CC3)=C(F)C=C2)C2=CC=CC=C12

Pharmacology

Indication

Olaparib is a poly (ADP-ribose) polymerase (PARP) inhibitor indicated for the treatment of:

(I) Ovarian cancer, in which the medication is intended for [a] the maintenance treatment of adult patients with recurrent epithelial ovarian, fallopian tube or primary peritoneal cancer, who are in complete or partial response to platinum-based chemotherapy, or [b] for the treatment of adult patients with deleterious or suspected deleterious germline BRCA-mutated (gBRCAm) advanced ovarian cancer who have been treated with three or more prior lines of chemotherapy Label. Select patients for therapy based on an FDA-approved companion diagnostic for olaparib Label.

[II] Breast cancer, in which the medication is intended for use in patients with deleterious or suspected deleterious gBRCAm, human epidermal growth factor receptor 2 (HER2)-negative metastatic breast cancer who have previously been treated with chemotherapy in the neoadjuvant, adjuvant or metastatic setting. Patients with hormone receptor (HR)-positive breast cancer should have been treated with a prior endocrine therapy or be considered inappropriate for endocrine treatment Label. Select patients for therapy based on an FDA-approved companion diagnostic for olaparib Label.

Associated Conditions
Pharmacodynamics

The effect of olaparib on cardiac repolarization was assessed in 119 patients following a single dose of 300 mg and in 109 patients following multiple dosing of 300 mg twice daily Label. No clinically relevant effect of olaparib on QT interval was observed Label.

Mechanism of action

Olaparib is an inhibitor of poly (ADP-ribose) polymerase (PARP) enzymes, including PARP1, PARP2, and PARP3. PARP enzymes are involved in normal cellular homeostasis, such as DNA transcription, cell cycle regulation, and DNA repair Label. Olaparib has been shown to inhibit growth of select tumor cell lines in vitro and decrease tumor growth in mouse xenograft models of human cancer both as monotherapy or following platinum-based chemotherapy Label. Increased cytotoxicity and anti-tumor activity following treatment with olaparib were noted in cell lines and mouse tumor models with deficiencies in BRCA Label. In vitro studies have shown that olaparib-induced cytotoxicity may involve inhibition of PARP enzymatic activity and increased formation of PARP-DNA complex, resulting in disruption of cellular homeostasis and cell death Label.

TargetActionsOrganism
APoly [ADP-ribose] polymerase 1
inhibitor
Humans
APoly [ADP-ribose] polymerase 2
inhibitor
Humans
APoly [ADP-ribose] polymerase 3
inhibitor
Humans
Additional Data Available
Adverse Effects

Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

Learn more
Additional Data Available
Contraindications

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

Learn more
Additional Data Available
Blackbox Warnings

Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.

Learn more
Absorption

Following oral administration, the absorption of olaparib is very rapid and can reach a peak concentration ranging between 4.7 and 9.1 mcg/ml after 1-3 hours. The reported AUC of olaparib after a dose of 200 mg is of 25.8 mcg.h/L and this AUC can be increased by 26% with constant administration. The consumption of a high-fat diet with olaparib can only decrease the tmax but do not have an effect in the peak concentration.6

Volume of distribution

After administration of a dose of 100 mg/kg, the reported volume of distribution was of 40.3 L.6

Protein binding

In vitro studies have reported that the plasma protein binding of olaparib was reported to be of 82%.5

Metabolism

Olaparib is extensively metabolized in the liver by the action of CYP3A isoenzymes.9 From the administered dose, the unchanged form of olaparib accounted for 70% of the circulating dose and it was considered the major component in urine and feces.8

The metabolic pathway of olaparib is mainly attributable to oxidation reactions with subsequent glucuronide and sulfate conjugation. However, the over 20 metabolites found in plasma, urine, and feces represented a minor portion of the administered dose. The major circulating metabolites were represented by the mono-oxygenated form and the piperazin-3-ol form.8

Route of elimination

From the administered dose, approximately 86% of the administered dose is recovered after 7 days from which 44% is found in the urine and 42% is obtained in feces.8

Half life

The reported elimination half-life ranges between 5 to 11 hours.6

Clearance

The total clearance of olaparib was reported to be 4.6 L/h.6

Toxicity

The most commonly reported side effects reported during clinical trials included cough, constipation, dysgeusia, peripheral deem, back pain, dizziness, headache, urinary tract infection, dyspnea, and rash Label 8,9. Myelodysplastic syndrome/Acute Myeloid Leukemia (MDS/AML) was reported in 2% of patients with deleterious or suspected deleterious germline BRCA-mutated advanced cancers Label 8,9. The majority of cases were fatal and the duration of therapy with olaparib in patients who developed secondary cancers varied from <6 months to >2 years Label 8,9. Complete blood count should be tested at baseline and monthly following therapy initiation to monitor for MDS/AML Label 8,9. Pneumonitis, including fatal cases, occurred in <1% of patients treated with olaparib Label 8,9. Patients should be monitored for new or worsening respiratory symptoms such as dyspnea, fever, cough, or wheezing Label 8,9. Olaparib was found to be teratogenic and causes embryo-fetal toxicity in rats Label 8,9. It should, therefore, be avoided during pregnancy and its use should be combined with effective contraception during treatment Label 8,9.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
(R)-warfarinThe serum concentration of (R)-warfarin can be increased when it is combined with Olaparib.
(S)-WarfarinThe serum concentration of (S)-Warfarin can be increased when it is combined with Olaparib.
2-MethoxyethanolThe risk or severity of adverse effects can be increased when 2-Methoxyethanol is combined with Olaparib.
9-(N-methyl-L-isoleucine)-cyclosporin AThe risk or severity of adverse effects can be increased when Olaparib is combined with 9-(N-methyl-L-isoleucine)-cyclosporin A.
9-aminocamptothecinThe metabolism of 9-aminocamptothecin can be decreased when combined with Olaparib.
AbataceptThe metabolism of Olaparib can be increased when combined with Abatacept.
AbciximabThe risk or severity of bleeding can be increased when Abciximab is combined with Olaparib.
AbemaciclibOlaparib may decrease the excretion rate of Abemaciclib which could result in a higher serum level.
AbetimusThe risk or severity of adverse effects can be increased when Abetimus is combined with Olaparib.
AcalabrutinibThe metabolism of Olaparib can be decreased when combined with Acalabrutinib.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

    Learn more
  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

    Learn more
  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

    Learn more
  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

    Learn more
Food Interactions
Not Available

References

Synthesis Reference

Menear KA, Adcock C, Boulter R, Cockcroft XL, Copsey L, Cranston A, Dillon KJ, Drzewiecki J, Garman S, Gomez S, Javaid H, Kerrigan F, Knights C, Lau A, Loh VM Jr, Matthews IT, Moore S, O'Connor MJ, Smith GC, Martin NM: 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. 2008 Oct 23;51(20):6581-91. doi: 10.1021/jm8001263. Epub 2008 Sep 19. Pubmed

General References
  1. Frampton JE: Olaparib: a review of its use as maintenance therapy in patients with ovarian cancer. BioDrugs. 2015 Apr;29(2):143-50. doi: 10.1007/s40259-015-0125-6. [PubMed:25899311]
  2. Menear KA, Adcock C, Boulter R, Cockcroft XL, Copsey L, Cranston A, Dillon KJ, Drzewiecki J, Garman S, Gomez S, Javaid H, Kerrigan F, Knights C, Lau A, Loh VM Jr, Matthews IT, Moore S, O'Connor MJ, Smith GC, Martin NM: 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. 2008 Oct 23;51(20):6581-91. doi: 10.1021/jm8001263. Epub 2008 Sep 19. [PubMed:18800822]
  3. Hay T, Matthews JR, Pietzka L, Lau A, Cranston A, Nygren AO, Douglas-Jones A, Smith GC, Martin NM, O'Connor M, Clarke AR: Poly(ADP-ribose) polymerase-1 inhibitor treatment regresses autochthonous Brca2/p53-mutant mammary tumors in vivo and delays tumor relapse in combination with carboplatin. Cancer Res. 2009 May 1;69(9):3850-5. doi: 10.1158/0008-5472.CAN-08-2388. Epub 2009 Apr 21. [PubMed:19383921]
  4. Rottenberg S, Jaspers JE, Kersbergen A, van der Burg E, Nygren AO, Zander SA, Derksen PW, de Bruin M, Zevenhoven J, Lau A, Boulter R, Cranston A, O'Connor MJ, Martin NM, Borst P, Jonkers J: High sensitivity of BRCA1-deficient mammary tumors to the PARP inhibitor AZD2281 alone and in combination with platinum drugs. Proc Natl Acad Sci U S A. 2008 Nov 4;105(44):17079-84. doi: 10.1073/pnas.0806092105. Epub 2008 Oct 29. [PubMed:18971340]
  5. Irwin CP, Portorreal Y, Brand C, Zhang Y, Desai P, Salinas B, Weber WA, Reiner T: PARPi-FL--a fluorescent PARP1 inhibitor for glioblastoma imaging. Neoplasia. 2014 May;16(5):432-40. doi: 10.1016/j.neo.2014.05.005. Epub 2014 Jun 23. [PubMed:24970386]
  6. Solimando DA Jr, Waddell JA: Nivolumab and Olaparib. Hosp Pharm. 2015 May;50(5):356-66. doi: 10.1310/hpj5005-356. [PubMed:26405320]
  7. FDA Approves Olaparib as Frontline Maintenance Therapy in Ovarian Cancer Press Release [Link]
  8. Olaparib New Zealand Data Sheet [Link]
  9. Linparza (olaparib) drug monograph [File]
External Links
KEGG Drug
D09730
ChemSpider
23343272
BindingDB
27566
ChEBI
83766
ChEMBL
CHEMBL521686
HET
09L
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Olaparib
ATC Codes
L01XX46 — Olaparib
AHFS Codes
  • 10:00.00 — Antineoplastic Agents
PDB Entries
3u9y / 4tkg / 4tvj / 5ds3
FDA label
Download (481 KB)
MSDS
Download (109 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0Active Not RecruitingTreatmentOvarian Cancer1
0RecruitingBasic ScienceBreast Cancer / Ovarian Cancer1
0RecruitingBasic ScienceOvarian Cancer1
0RecruitingTreatmentBRCA-Mutated Ovarian Carcinoma / BRCA1 Gene Mutation / Brca2 Gene Mutation / High Grade Fallopian Tube Serous Adenocarcinoma / High Grade Ovarian Serous Adenocarcinoma / Primary Peritoneal High Grade Serous Adenocarcinoma / Stage III Fallopian Tube Cancer AJCC v8 / Stage III Ovarian Cancer AJCC v8 / Stage III Primary Peritoneal Cancer AJCC v8 / Stage IIIA Fallopian Tube Cancer AJCC v8 / Stage IIIA Ovarian Cancer AJCC v8 / Stage IIIA Primary Peritoneal Cancer AJCC v8 / Stage IIIA1 Fallopian Tube Cancer AJCC v8 / Stage IIIA1 Ovarian Cancer AJCC v8 / Stage IIIA2 Fallopian Tube Cancer AJCC v8 / Stage IIIA2 Ovarian Cancer AJCC v8 / Stage IIIB Fallopian Tube Cancer AJCC v8 / Stage IIIB Ovarian Cancer AJCC v8 / Stage IIIB Primary Peritoneal Cancer AJCC v8 / Stage IIIC Fallopian Tube Cancer AJCC v8 / Stage IIIC Ovarian Cancer AJCC v8 / Stage IIIC Primary Peritoneal Cancer AJCC v8 / Stage IV Fallopian Tube Cancer AJCC v8 / Stage IV Ovarian Cancer AJCC v8 / Stage IV Primary Peritoneal Cancer AJCC v8 / Stage IVA Fallopian Tube Cancer AJCC v8 / Stage IVA Ovarian Cancer AJCC v8 / Stage IVA Primary Peritoneal Cancer AJCC v8 / Stage IVB Fallopian Tube Cancer AJCC v8 / Stage IVB Ovarian Cancer AJCC v8 / Stage IVB Primary Peritoneal Cancer AJCC v81
0RecruitingTreatmentPulmonary Arterial Hypertension (PAH)1
1Active Not RecruitingBasic ScienceTumors, Solid1
1Active Not RecruitingOtherTumors, Solid2
1Active Not RecruitingTreatmentAdvanced Ovarian Cancer / Carboplatin / Paclitaxel / Triple Negative Metastatic Breast Cancer1
1Active Not RecruitingTreatmentAdvanced Solid Tumors1
1Active Not RecruitingTreatmentAdvanced Solid Tumours1
1Active Not RecruitingTreatmentAnatomic Stage IV Breast Cancer AJCC v8 / Estrogen Receptor Negative / HER2/Neu Negative / Progesterone Receptor Negative / Prognostic Stage IV Breast Cancer AJCC v8 / Triple-Negative Breast Carcinoma1
1Active Not RecruitingTreatmentBRCA1 Protein / BRCA2 Protein / Neoplasms, Ovarian1
1Active Not RecruitingTreatmentBone Tumors / Soft Tissue Sarcoma (STS)1
1Active Not RecruitingTreatmentBreast Cancer / Ovarian Cancer1
1Active Not RecruitingTreatmentFallopian Tube Cancer / Ovarian Cancer / Primary Peritoneal Cancer1
1Active Not RecruitingTreatmentInflammatory Breast Carcinoma / Locally Advanced Malignant Neoplasm / Triple-Negative Invasive Breast Carcinoma1
1Active Not RecruitingTreatmentMalignant Solid Tumours1
1Active Not RecruitingTreatmentMuscle Invasive Bladder Cancer1
1Active Not RecruitingTreatmentTumors, Solid1
1CompletedNot AvailableTumors, Solid3
1CompletedBasic ScienceTumors, Solid1
1CompletedOtherProstate Cancer1
1CompletedOtherTumors, Solid1
1CompletedTreatmentAdvanced Solid Malignancies1
1CompletedTreatmentAdvanced Solid Malignancies / Malignancies1
1CompletedTreatmentAdvanced Solid Tumours1
1CompletedTreatmentBrain and Central Nervous System Tumors1
1CompletedTreatmentBreast Cancer / Cancer, Advanced / Ovarian Cancer1
1CompletedTreatmentBreast Cancer / Cervical Cancers / Endometrial Cancers / Fallopian Tube Cancer / Ovarian Cancer / Primary Peritoneal Cancer1
1CompletedTreatmentBreast Cancer / Metastatic Breast Cancer (MBC) / Triple Negative Breast Cancer (TNBC)1
1CompletedTreatmentColorectal Cancers1
1CompletedTreatmentMalignant Neoplasm of Pancreas1
1CompletedTreatmentMalignant Solid Tumours1
1CompletedTreatmentMelanoma Neoplasms1
1CompletedTreatmentNeoplasms1
1CompletedTreatmentNeoplasms Metastasis2
1CompletedTreatmentNeoplasms, Pancreatic1
1CompletedTreatmentOvarian, Breast, and Second-Line Small Cell Lung Cancer / Refractory Solid Tumours / Relapsed Small Cell Lung Cancer (SCLC)1
1CompletedTreatmentSquamous Cell Carcinoma of the Head and Neck (SCCHN)1
1Not Yet RecruitingTreatmentAdvanced Breast Cancer / BRCA1 Mutations / BRCA2 Mutation / Locally Advanced Breast Cancer (LABC) / Metastatic Breast Cancer (MBC)1
1Not Yet RecruitingTreatmentBreast Cancer / Breast Cancer Metastatic1
1Not Yet RecruitingTreatmentPulmonary Arterial Hypertension (PAH)1
1Not Yet RecruitingTreatmentSquamous Cell Carcinoma of the Head and Neck (SCCHN)1
1RecruitingTreatmentAdvanced Malignant Solid Neoplasm / ARID1A Gene Mutation / ATM Gene Mutation / ATRX Gene Mutation / BARD1 Gene Mutation / BRCA1 Gene Mutation / Brca2 Gene Mutation / BRIP1 Gene Mutation / CDK12 Gene Mutation / CHEK1 Gene Mutation / CHEK2 Gene Mutation / FANCA Gene Mutation / FANCL Gene Mutation / Metastatic Malignant Solid Neoplasm / MRE11 Gene Mutation / MSH2 Gene Mutation / PALB2 Gene Mutation / PARP1 Gene Mutation / PIK3CA Gene Mutation / POLD1 Gene Mutation / PPP2R2A Gene Mutation / PTEN gene mutation / RAD51B Gene Mutation / RAD51C Gene Mutation / RAD51D Gene Mutation / RAD54L Gene Mutation / Unresectable Malignant Solid Neoplasm / XRCC2 Gene Mutation1
1RecruitingTreatmentAcute Myelogenous Leukaemia (AML) / Breast Cancer / Malignant Neoplasm of Pancreas / Prostate Cancer1
1RecruitingTreatmentAdvanced Cancers / Advanced Malignant Neoplasm / Recurrent Malignant Neoplasm / Refractory Malignant Neoplasm1
1RecruitingTreatmentBreast Neoplasm Malignant Female / Breast Neoplasms, Triple-Negative / Radiotherapy Side Effect1
1RecruitingTreatmentCarcinoma of the Oesophagus1
1RecruitingTreatmentEstrogen Receptor Negative / HER2/Neu Negative / High Grade Fallopian Tube Serous Adenocarcinoma / High Grade Ovarian Serous Adenocarcinoma / Metastatic Breast Carcinoma / Metastatic Malignant Solid Neoplasm / Metastatic Solid Neoplasm / Platinum Resistant Primary Peritoneal Cancer / Platinum-Resistant Fallopian Tube Carcinoma / Platinum-Resistant Ovarian Carcinoma / Platinum-Resistant Primary Peritoneal Carcinoma / Primary Peritoneal High Grade Serous Adenocarcinoma / Progesterone Receptor Negative / Recurrent Breast Carcinoma / Recurrent Fallopian Tube Carcinoma / Recurrent Ovarian Carcinoma / Recurrent Primary Peritoneal Carcinoma / Triple-Negative Breast Carcinoma / Unresectable Malignant Solid Neoplasm / Unresectable Solid Neoplasm1
1RecruitingTreatmentEwing's Sarcoma (ES)1
1RecruitingTreatmentHead and Neck Carcinoma1
1RecruitingTreatmentHead and Neck Squamous Cell Carcinoma (HNSCC)1
1RecruitingTreatmentLaryngeal Cancer Stage II / Laryngeal Cancer Stage III / Neoplasms, Head and Neck / Squamous Cell Carcinoma (SCC)1
1RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
1RecruitingTreatmentLung Cancer Small Cell Lung Cancer (SCLC) / Small Cell Lung Cancer Extensive Stage1
1RecruitingTreatmentLung Cancer Small Cell Lung Cancer (SCLC) / Small Cell Lung Carcinoma1
1RecruitingTreatmentMalignant Lymphomas / Malignant Neoplasms Stated as Primary Lymphoid Haematopoietic / Recurrent Diffuse Large B-Cell Lymphoma / Recurrent T-Cell Non-Hodgkin Lymphoma / Refractory Diffuse Large B Cell Lymphoma / Refractory Hodgkin Lymphoma / Refractory T-Cell Non-Hodgkin Lymphoma1
1RecruitingTreatmentMalignant Lymphomas / Malignant Solid Tumours / Ovarian Cancer1
1RecruitingTreatmentMalignant Neoplasm of Breast / Malignant Neoplasms of Digestive Organs / Malignant Neoplasms of Female Genital Organs / Malignant Neoplasms of Male Genital Organs / Malignant Neoplasms of Thyroid and Other Endocrine Glands1
1RecruitingTreatmentMetastatic Castration Resistant Prostate Cancer (mCRPC)1
1RecruitingTreatmentMetastatic Castration Resistant Prostate Cancer / Prostatic Neoplasms1
1RecruitingTreatmentMetastatic Malignant Neoplasm in the Chest Wall / Metastatic Melanoma / Recurrent Breast Carcinoma1
1RecruitingTreatmentSoft-Tissue Sarcoma1
1RecruitingTreatmentSolid Tumor, Adult1
1RecruitingTreatmentTumors, Solid1
1TerminatedTreatmentBreast Cancer1
1Unknown StatusTreatmentCancer, Advanced1
1WithdrawnTreatmentMalignant Lymphomas1
1WithdrawnTreatmentSquamous Cell Carcinoma (SCC)1
1, 2Active Not RecruitingTreatmentBrca1 Mutation Carrier / Brca2 Mutation Carrier / Breast Cancer / Endometrial Adenocarcinomas / Estrogen Receptor Negative / HER2/Neu Negative / High Grade Ovarian Serous Adenocarcinoma / Malignant Female Reproductive System Neoplasm / Progesterone Receptor Negative / Recurrent Breast Carcinoma / Recurrent Fallopian Tube Carcinoma / Recurrent Ovarian Carcinoma / Recurrent Primary Peritoneal Carcinoma / Recurrent Uterine Corpus Carcinoma / Stage III Uterine Corpus Cancer AJCC v7 / Stage IV Breast Cancer AJCC v6 and v7 / Stage IV Uterine Corpus Cancer AJCC v7 / Triple-Negative Breast Carcinoma1
1, 2Active Not RecruitingTreatmentDeleterious BRCA1 Gene Mutation / Deleterious BRCA2 Gene Mutation / Estrogen Receptor Negative / HER2/Neu Negative / Ovarian Endometrioid Adenocarcinoma / Ovarian Serous Adenocarcinoma / Ovarian Serous Cystadenocarcinoma / Ovarian Serous Surface Papillary Adenocarcinoma / Progesterone Receptor Negative / Recurrent Breast Carcinoma / Recurrent Fallopian Tube Carcinoma / Recurrent Ovarian Carcinoma / Recurrent Primary Peritoneal Carcinoma / Triple-Negative Breast Carcinoma1
1, 2Active Not RecruitingTreatmentPrimary Peritoneal Carcinoma1
1, 2Active Not RecruitingTreatmentStage III Ovarian Cancer / Stage IV Ovarian Cancer / Uterine Malignancies1
1, 2CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
1, 2Not Yet RecruitingTreatmentFallopian Tube Cancer / Fallopian Tube Carcinosarcoma / Fallopian Tube Clear Cell Adenocarcinoma / Fallopian Tube Endometrioid Adenocarcinoma / High Grade Fallopian Tube Serous Adenocarcinoma / High Grade Ovarian Serous Adenocarcinoma / Ovarian Carcinosarcoma / Ovarian Clear Cell Adenocarcinoma / Ovarian Endometrioid Adenocarcinoma / Primary Peritoneal Serous Adenocarcinoma / Recurrent Endometrial Carcinoma / Recurrent Ovarian Carcinoma / Recurrent Primary Peritoneal Carcinoma1
1, 2Not Yet RecruitingTreatmentGastroenteropancreatico Tumors / Neuroendocrine Neoplasms / Neuroendocrine Tumors1
1, 2Not Yet RecruitingTreatmentRecurrent Endometrial Cancer1
1, 2RecruitingDiagnosticOral Squamous Cell Carcinoma (OSCC)1
1, 2RecruitingTreatmentAbdominal wall neoplasm / Fallopian Tube Cancer / Ovarian Cancer1
1, 2RecruitingTreatmentAdenocarcinoma, Prostate / Castration Levels of Testosterone / Castration-Resistant Prostate Carcinoma / Metastatic Malignant Neoplasm in the Bone / Prostate Carcinoma Metastatic in the Bone / PSA Level Greater Than or Equal to Two / PSA Progression / Testosterone Less Than 50 ng/dL1
1, 2RecruitingTreatmentAdenocarcinomas of the Gastroesophageal Junction / Advanced Gastric Cancer / Metastatic Esophageal Carcinoma / Metastatic Gastric carcinoma / Metastatic Gastroesophageal Junction Adenocarcinoma / Metastatic Malignant Neoplasm in the Lymph Nodes / Progressive Disease / Recurrent Esophageal Carcinoma / Recurrent Gastric Carcinoma / Recurrent Gastroesophageal Junction Adenocarcinoma / Stage III Esophageal Cancer AJCC v7 / Stage III Gastric Cancer AJCC v7 / Stage IIIA Esophageal Cancer AJCC v7 / Stage IIIA Gastric Cancer AJCC v7 / Stage IIIB Esophageal Cancer AJCC v7 / Stage IIIB Gastric Cancer AJCC v7 / Stage IIIC Esophageal Cancer AJCC v7 / Stage IIIC Gastric Cancer AJCC v7 / Stage IV Esophageal Cancer AJCC v7 / Stage IV Gastric Cancer AJCC v7 / Unresectable Esophageal Carcinoma / Unresectable Gastric Carcinoma / Unresectable Gastroesophageal Junction Adenocarcinoma1
1, 2RecruitingTreatmentAdv Solid Malig - H&N SCC, ATM Pro / Def NSCLC, Gastric & Breast Cancer / Advanced Solid Malignancies, Head and Neck Squamous Cell Carinoma, and ATM Deficient NSCLC Adenocarcinoma, Gastric Cancer and Gastro-oesophageal Junction1
1, 2RecruitingTreatmentAdvanced Malignancies1
1, 2RecruitingTreatmentAdvanced Solid Tumors / Breast Cancer / Cancer, Advanced / Endometrial Cancers / Ovarian Cancer1
1, 2RecruitingTreatmentBreast Cancer1
1, 2RecruitingTreatmentBreast Cancer / Colorectal Cancers / Lung Cancers / Neoplasms, Breast / Neoplasms, Colorectal / Ovarian Cancer / Prostate Cancer / Triple Negative Breast Cancer (TNBC)1
1, 2RecruitingTreatmentBreast / Lung Cancer Small Cell Lung Cancer (SCLC) / Malignant Neoplasm of Stomach / Ovarian1
1, 2RecruitingTreatmentChildren, Adolescents and Young Adults With Refractory or Recurrent Malignancies1
1, 2RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC) / Lung Cancer Small Cell Lung Cancer (SCLC) / Lung Cancers / Neoplasms, Lung / Prostate Cancer / Small Cell Lung Carcinoma / Transitional Cell Carcinoma / Tumors, Solid / Urothelial Cancer1
1, 2RecruitingTreatmentLung Cancer Small Cell Lung Cancer (SCLC)1
1, 2RecruitingTreatmentMalignant Gliomas / PARP Inhibitor / Radiotherapy1
1, 2RecruitingTreatmentNeoplasms, Breast1
2Active Not RecruitingBasic ScienceBreast Cancer1
2Active Not RecruitingTreatmentAdenocarcinoma of the Prostate1
2Active Not RecruitingTreatmentAdvanced Tumours / Breast / Ovarian / Pancreatic / Prostate1
2Active Not RecruitingTreatmentBRCA1 Gene Mutation / Brca2 Gene Mutation / Deleterious BRCA1 Gene Mutation / Deleterious BRCA2 Gene Mutation / Fallopian Tube Endometrioid Adenocarcinoma / Fallopian Tube Serous Adenocarcinoma / High Grade Ovarian Serous Adenocarcinoma / Ovarian Endometrioid Tumor / Primary Peritoneal Serous Adenocarcinoma / Recurrent Fallopian Tube Carcinoma / Recurrent Ovarian Carcinoma / Recurrent Primary Peritoneal Carcinoma1
2Active Not RecruitingTreatmentBreast Cancer / Ovarian Carcinoma1
2Active Not RecruitingTreatmentBreast Cancer / Triple Negative Breast Cancer (TNBC)1
2Active Not RecruitingTreatmentCastration Levels of Testosterone / Castration-Resistant Prostate Carcinoma / Hormone-Resistant Prostate Cancer / Metastatic Hormone Refractory Prostate Cancer / Prostate Adenocarcinoma With Focal Neuroendocrine Differentiation / Prostate Adenocarcinoma With Neuroendocrine Differentiation / Prostate Carcinoma Metastatic in the Bone / Prostate Small Cell Carcinoma / PSA Progression / Stage IV Prostate Adenocarcinoma / Stage IV Prostate Adenocarcinoma AJCC v71
2Active Not RecruitingTreatmentEndometrial Undifferentiated Carcinoma / Endometrioid Adenocarcinoma / Recurrent Endometrial Serous Adenocarcinoma / Recurrent Uterine Corpus Carcinoma / Stage IV Uterine Corpus Cancer AJCC v7 / Stage IVA Uterine Corpus Cancer AJCC v7 / Stage IVB Uterine Corpus Cancer AJCC v71
2Active Not RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
2Active Not RecruitingTreatmentMalignancies1
2Active Not RecruitingTreatmentMalignant Neoplasm of Stomach1
2Active Not RecruitingTreatmentMetastatic Breast Cancer (MBC)1
2Active Not RecruitingTreatmentMetastatic Castration Resistant Prostate Cancer1
2Active Not RecruitingTreatmentMetastatic Non-Small Cell Lung Cancer1
2Active Not RecruitingTreatmentNeoplasms, Breast1
2Active Not RecruitingTreatmentNeoplasms, Germ Cell and Embryonal1
2Active Not RecruitingTreatmentNeoplasms, Ovarian1
2Active Not RecruitingTreatmentOvarian Cancer3
2Active Not RecruitingTreatmentRecurrent Glioblastoma1
2Active Not RecruitingTreatmentRecurrent Platinum Resistant Ovarian Cancer1
2Active Not RecruitingTreatmentRelapsed Ovarian Cancer, BRCA Mutation, Platinum Sensitivity1
2Active Not RecruitingTreatmentUrinary Bladder Neoplasms1
2CompletedTreatmentColorectal Cancers1
2CompletedTreatmentEwing's Sarcoma (ES)1
2CompletedTreatmentNeoplasms, Ovarian2
2CompletedTreatmentOvarian Cancer1
2Not Yet RecruitingBasic ScienceRenal Cell Adenocarcinoma1
2Not Yet RecruitingOtherNeoplasms, Breast1
2Not Yet RecruitingTreatmentARID1A Gene Mutation / ATM Gene Mutation / ATR Gene Mutation / Bile duct adenocarcinoma / BRCA1 Gene Mutation / Brca2 Gene Mutation / BRIP1 Gene Mutation / CHEK2 Gene Mutation / EMSY Gene Mutation / Fanconi Anemia Complementation Group Gene Mutation / Metastatic Bile Duct Carcinoma / MRE11 Gene Mutation / NBN Gene Mutation / PALB2 Gene Mutation / PTEN Gene Deletion / RAD51 Gene Mutation1
2Not Yet RecruitingTreatmentAcute Myeloid Leukemia Arising From Previous Myelodysplastic Syndrome / Acute, recurrent Myeloid Leukemia / IDH1 NP_005887.2:p.R132C / IDH1 NP_005887.2:p.R132G / IDH1 NP_005887.2:p.R132H / IDH1 NP_005887.2:p.R132L / IDH1 NP_005887.2:p.R132S / IDH1 NP_005887.2:p.R132V / IDH2 NP_002159.2:p.R140L / IDH2 NP_002159.2:p.R140Q / IDH2 NP_002159.2:p.R140W / IDH2 NP_002159.2:p.R140X / IDH2 NP_002159.2:p.R172G / IDH2 NP_002159.2:p.R172K / IDH2 NP_002159.2:p.R172M / IDH2 NP_002159.2:p.R172S / IDH2 NP_002159.2:p.R172W / Myelodysplastic Syndrome / Refractory Acute Myeloid Leukemia / Therapy-Related Acute Myeloid Leukemia1
2Not Yet RecruitingTreatmentAdenocarcinoma of the Prostate / Prostate Cancer1
2Not Yet RecruitingTreatmentAdvanced Breast Carcinoma / Anatomic Stage III Breast Cancer AJCC v8 / Anatomic Stage IIIA Breast Cancer AJCC v8 / Anatomic Stage IIIB Breast Cancer AJCC v8 / Anatomic Stage IIIC Breast Cancer AJCC v8 / Anatomic Stage IV Breast Cancer AJCC v8 / Germline BRCA1 Gene Mutation / Germline BRCA2 Gene Mutation / HER2/Neu Negative / Metastatic Breast Carcinoma / Prognostic Stage III Breast Cancer AJCC v8 / Prognostic Stage IIIA Breast Cancer AJCC v8 / Prognostic Stage IIIB Breast Cancer AJCC v8 / Prognostic Stage IIIC Breast Cancer AJCC v8 / Prognostic Stage IV Breast Cancer AJCC v81
2Not Yet RecruitingTreatmentAdvanced Soft Tissue Sarcoma1
2Not Yet RecruitingTreatmentCancers With DNA Repair-Deficiency1
2Not Yet RecruitingTreatmentCholangiocarcinomas / Gliomas / IDH Mutation / Tumors, Solid1
2Not Yet RecruitingTreatmentEndometrial Carcinoma1
2Not Yet RecruitingTreatmentGynaecological Cancers1
2Not Yet RecruitingTreatmentIDH1 Gene Mutation / IDH2 Gene Mutation / Malignant Solid Neoplasm / Progressive Disease / Refractory Cholangiocarcinoma / Refractory Malignant Solid Neoplasm1
2Not Yet RecruitingTreatmentMetastatic Sarcoma / Sarcomas1
2Not Yet RecruitingTreatmentTumors, Solid1
2RecruitingOtherAdvanced Breast Cancer1
2RecruitingScreeningAdvanced Malignant Solid Neoplasm / Ann Arbor Stage III Childhood Non-Hodgkin Lymphoma / Ann Arbor Stage III Non-Hodgkin Lymphoma / Ann Arbor Stage IV Childhood Non-Hodgkin Lymphoma / Ann Arbor Stage IV Non-Hodgkin Lymphoma / Childhood Langerhans Cell Histiocytosis / Ependymoma, Recurrent / Histiocytic Sarcoma (HS) / Juvenile Xanthogranuloma / Langerhans Cell Histiocytosis (LCH) / Malignant Gliomas / Malignant Lymphomas / Recurrent Central Nervous System Neoplasm / Recurrent Childhood Ependymoma / Recurrent Childhood Malignant Germ Cell Tumor / Recurrent Childhood Medulloblastoma / Recurrent Childhood Non-Hodgkin Lymphoma / Recurrent Childhood Rhabdomyosarcoma / Recurrent Childhood Soft Tissue Sarcoma / Recurrent Ewing Sarcoma / Recurrent Gliomas / Recurrent Hepatoblastoma / Recurrent Langerhans Cell Histiocytosis / Recurrent Malignant Germ Cell Tumor / Recurrent Malignant Solid Neoplasm / Recurrent Medulloblastoma / Recurrent Neuroblastoma / Recurrent Non-Hodgkin Lymphoma / Recurrent Osteosarcoma / Recurrent Peripheral Primitive Neuroectodermal Tumor / Recurrent Rhabdoid Tumor / Recurrent Soft Tissue Sarcoma / Refractory Central Nervous System Neoplasm / Refractory Childhood Malignant Germ Cell Tumor / Refractory Ewing Sarcoma / Refractory Glioma / Refractory Hepatoblastoma / Refractory Langerhans cell histiocytosis / Refractory Malignant Germ Cell Tumor / Refractory Malignant Solid Neoplasm / Refractory Medulloblastoma / Refractory Neuroblastoma / Refractory Non-Hodgkin's lymphoma / Refractory Osteosarcoma / Refractory Peripheral Primitive Neuroectodermal Tumor / Refractory Rhabdoid Tumor / Refractory Rhabdomyosarcoma / Rhabdoid Tumors / Stage III Childhood Non-Hodgkin Lymphoma / Stage III Osteosarcoma / Stage III Osteosarcoma AJCC v7 / Stage III Soft Tissue Sarcoma / Stage III Soft Tissue Sarcoma AJCC v7 / Stage IV Childhood Non-Hodgkin Lymphoma / Stage IV Osteosarcoma / Stage IV Osteosarcoma AJCC v7 / Stage IV Soft Tissue Sarcoma / Stage IV Soft Tissue Sarcoma AJCC v7 / Stage IVA Osteosarcoma / Stage IVA Osteosarcoma AJCC v7 / Stage IVB Osteosarcoma / Stage IVB Osteosarcoma AJCC v7 / Wilms' tumor1
2RecruitingTreatmentABL1 Gene Mutation / Abnormal DNA Repair / Advanced Urothelial Carcinoma / ATM Gene Mutation / ATR Gene Mutation / ATRX Gene Mutation / BAP1 Gene Mutation / BARD1 Gene Mutation / BLM Gene Mutation / BRCA1 Gene Mutation / Brca2 Gene Mutation / BRD4 Gene Mutation / BRIP1 Gene Mutation / CCND1 Gene Mutation / CHEK1 Gene Mutation / CHEK2 Gene Mutation / DOT1L Gene Mutation / FANCC Gene Mutation / FANCD2 Gene Mutation / FANCE Gene Mutation / FANCF Gene Mutation / FANCG Gene Mutation / FANCL Gene Mutation / IKBKE Gene Mutation / MEN1 Gene Mutation / MLH1 Gene Mutation / MSH2 Gene Mutation / MSH6 Gene Mutation / MUTYH Gene Mutation / NPM1 Gene Mutation / PALB2 Gene Mutation / PMS2 Gene Mutation / POLD1 Gene Mutation / POLE Gene Mutation / PRKDC Gene Mutation / RAD50 Gene Mutation / RAD51 Gene Mutation / SMARCB1 Gene Mutation / Stage III Bladder Urothelial Carcinoma AJCC v6 and v7 / Stage IV Bladder Urothelial Carcinoma AJCC v7 / STK11 Gene Mutation / Transitional Cell Carcinoma / Urothelial carcinoma ureter metastatic1
2RecruitingTreatmentATM Biallelic Inactivation / ATM Gene Mutation / ATM Monoallelic Inactivation / BRCA1 Biallelic Inactivation / BRCA1 Gene Mutation / BRCA2 Biallelic Inactivation / Brca2 Gene Mutation / FANCA Biallelic Inactivation / Homologous Recombination Deficiency / PALB2 Biallelic Inactivation / PALB2 Gene Mutation / Prostate Adenocarcinoma Without Evidence of Neuroendocrine Differentiation / Stage I Prostate Cancer AJCC v8 / Stage II Prostate Cancer AJCC v8 / Stage IIA Prostate Cancer AJCC v8 / Stage IIB Prostate Cancer AJCC v8 / Stage IIC Prostate Cancer AJCC v81
2RecruitingTreatmentATM Gene Mutation / Breast Cancer Invasive Nos / BRIP1 Gene Mutation / CHEK2 Gene Mutation / Metastatic Breast Cancer (MBC) / NBN Gene Mutation / PALB2 Gene Mutation / RAD51 Gene Mutation / Somatic Mutation Breast Cancer (BRCA1) / Somatic Mutation Breast Cancer (BRCA2)1
2RecruitingTreatmentAbnormal DNA Repair / Hormone-Resistant Prostate Cancer / Metastatic Hormone Refractory Prostate Cancer / Prostate Cancer Metastatic Castration-Resistant / Stage IV Prostate Cancer1
2RecruitingTreatmentAdenocarcinoma of the Pancreas / BRCA1 wt Allele / BRCA2 wt Allele / Estrogen Receptor Negative / HER2/Neu Negative / Pancreatic Adenocarcinoma Metastatic / Pancreatic Ductal Adenocarcinoma / Progesterone Receptor Negative / Recurrent Breast Carcinoma / Recurrent Non-Small Cell Lung Carcinoma / Recurrent Pancreatic Carcinoma / Recurrent Small Cell Lung Carcinoma / Stage III Breast Cancer / Stage III Breast Cancer AJCC V7 / Stage III Lung Non-Small Cell Cancer AJCC v7 / Stage III Lung Small Cell Carcinoma AJCC v7 / Stage III Non-Small Cell Lung Cancer / Stage III Non-Small Cell Lung Cancer AJCC v7 / Stage III Pancreatic Cancer / Stage III Pancreatic Cancer AJCC v6 and v7 / Stage III Small Cell Lung Carcinoma / Stage III Small Cell Lung Carcinoma AJCC v7 / Stage IIIA Breast Cancer / Stage IIIA Breast Cancer AJCC v7 / Stage IIIA Lung Non-Small Cell Cancer AJCC v7 / Stage IIIA Lung Small Cell Carcinoma AJCC v7 / Stage IIIA Non-Small Cell Lung Cancer / Stage IIIA Non-Small Cell Lung Cancer AJCC v7 / Stage IIIA Small Cell Lung Carcinoma / Stage IIIA Small Cell Lung Carcinoma AJCC v7 / Stage IIIB Breast Cancer / Stage IIIB Breast Cancer AJCC v7 / Stage IIIB Lung Non-Small Cell Cancer AJCC v7 / Stage IIIB Lung Small Cell Carcinoma AJCC v7 / Stage IIIb Non-small Cell Lung Cancer / Stage IIIB Non-Small Cell Lung Cancer AJCC v7 / Stage IIIB Small Cell Lung Carcinoma / Stage IIIB Small Cell Lung Carcinoma AJCC v7 / Stage IIIC Breast Cancer / Stage IIIC Breast Cancer AJCC v7 / Stage IV Breast Cancer / Stage IV Breast Cancer AJCC v6 and v7 / Stage IV Lung Non-Small Cell Cancer AJCC v7 / Stage IV Lung Small Cell Carcinoma AJCC v7 / Stage IV Non-Small Cell Lung Cancer / Stage IV Non-Small Cell Lung Cancer AJCC v7 / Stage IV Pancreatic Cancer / Stage IV Pancreatic Cancer AJCC v6 and v7 / Stage IV Small Cell Lung Carcinoma / Stage IV Small Cell Lung Carcinoma AJCC v7 / Stage IVA Pancreatic Cancer / Stage IVB Pancreatic Cancer / Triple-Negative Breast Carcinoma / Unresectable Pancreatic Carcinoma1
2RecruitingTreatmentAdenocarcinoma of the Pancreas / Leiomyosarcomas / Mismatch Repair Proficient Colorectal Cancer1
2RecruitingTreatmentAdenocarcinoma, Prostate / Castration Levels of Testosterone / Castration-Resistant Prostate Carcinoma / PSA Level Greater Than or Equal to One / PSA Progression1
2RecruitingTreatmentAdvanced Breast Cancer2
2RecruitingTreatmentAdvanced Cancers Harbouring Mutations in HRG1
2RecruitingTreatmentAdvanced Gastric Cancer1
2RecruitingTreatmentAdvanced Malignant Solid Neoplasm / Ann Arbor Stage III Childhood Non-Hodgkin Lymphoma / Ann Arbor Stage IV Childhood Non-Hodgkin Lymphoma / Deleterious ATM Gene Mutation / Deleterious BRCA1 Gene Mutation / Deleterious BRCA2 Gene Mutation / Deleterious RAD51C Gene Mutation / Deleterious RAD51D Gene Mutation / Histiocytosis / Low Grade Glioma (LGG) / Malignant Gliomas / Recurrent Childhood Central Nervous System Neoplasm / Recurrent Childhood Ependymoma / Recurrent Childhood Malignant Germ Cell Tumor / Recurrent Childhood Non-Hodgkin Lymphoma / Recurrent Childhood Rhabdomyosarcoma / Recurrent Childhood Soft Tissue Sarcoma / Recurrent Ewing Sarcoma/Peripheral Primitive Neuroectodermal Tumor / Recurrent Gliomas / Recurrent Hepatoblastoma / Recurrent Langerhans Cell Histiocytosis / Recurrent Malignant Solid Neoplasm / Recurrent Medulloblastoma / Recurrent Neuroblastoma / Recurrent Osteosarcoma / Refractory Central Nervous System Neoplasm / Refractory Childhood Malignant Germ Cell Tumor / Refractory Ependymoma / Refractory Ewing Sarcoma/Peripheral Primitive Neuroectodermal Tumor / Refractory Glioma / Refractory Hepatoblastoma / Refractory Langerhans cell histiocytosis / Refractory Malignant Glioma / Refractory Malignant Solid Neoplasm / Refractory Medulloblastoma / Refractory Neuroblastoma / Refractory Non-Hodgkin's lymphoma / Refractory Osteosarcoma / Refractory Rhabdomyosarcoma / Refractory Soft Tissue Sarcoma / Rhabdoid Tumors / Stage III Childhood Non-Hodgkin Lymphoma / Stage IV Childhood Non-Hodgkin Lymphoma / Wilms' tumor1
2RecruitingTreatmentAdvanced Malignant Solid Neoplasm / Glioblastomas / Grade II Glioma / IDH1 Gene Mutation / IDH2 Gene Mutation / Recurrent Cholangiocarcinoma / Recurrent Gliomas / Recurrent Malignant Solid Neoplasm / WHO Grade II Glioma / WHO Grade III Glioma1
2RecruitingTreatmentAdvanced Ovarian Cancer1
2RecruitingTreatmentAdvanced Solid Tumors / Multiple Myeloma (MM) / Non-Hodgkin's Lymphoma (NHL)2
2RecruitingTreatmentBRCA 1 /2 and / or HRD / Breast Cancer / HRpos Breast Neoplasms / Triple Negative Breast Neoplasms1
2RecruitingTreatmentBRCA Wild Type Platinum Sensitive Recurrent Ovarian Cancer1
2RecruitingTreatmentBRCA1 Gene Mutation / Brca2 Gene Mutation / Estrogen Receptor Negative / HER2/Neu Negative / Homologous Recombination Deficiency / Locally Advanced Unresectable Breast Carcinoma / Metastatic Breast Carcinoma / Progesterone Receptor Negative / Recurrent Breast Carcinoma / Stage III Breast Cancer / Stage III Breast Cancer AJCC V7 / Stage IIIA Breast Cancer / Stage IIIA Breast Cancer AJCC v7 / Stage IIIB Breast Cancer / Stage IIIB Breast Cancer AJCC v7 / Stage IIIC Breast Cancer / Stage IIIC Breast Cancer AJCC v7 / Stage IV Breast Cancer / Stage IV Breast Cancer AJCC v6 and v7 / Triple-Negative Breast Carcinoma1
2RecruitingTreatmentBRCA1 Gene Mutation / Brca2 Gene Mutation / Ovarian Serous Adenocarcinoma / Recurrent Fallopian Tube Carcinoma / Recurrent Ovarian Carcinoma / Recurrent Primary Peritoneal Carcinoma1
2RecruitingTreatmentBladder Cancers1
2RecruitingTreatmentBreast Cancer1
2RecruitingTreatmentBreast Cancer / ER-Negative PR-Negative HER2-Negative Breast Cancer / ER-Negative PR-Negative HER2-Negative Breast Neoplasms / Metastatic Triple Negative Breast Cancer / Triple Negative Breast Cancer (TNBC) / Triple-Negative Breast Cancer (TNBC) / Triple-Negative Breast Neoplasms1
2RecruitingTreatmentBreast Cancer / Neoplasms, Breast / Tumors, Breast1
2RecruitingTreatmentCancer of Unknown Primary Site1
2RecruitingTreatmentCarcinosarcoma / Neoplasms, Endometrial1
2RecruitingTreatmentClear Cell Renal Cell Carcinoma / Locally Advance Pancreatic Ductal Adenocarcinoma / Locally Advanced Malignant Solid Neoplasm / Locally Advanced Pancreatic Cancer / Metastatic Malignant Solid Neoplasm / Metastatic Renal Cell Carcinoma / Pancreatic Cancer Metastatic / Pancreatic Ductal Adenocarcinoma / Stage III Pancreatic Cancer / Stage III Pancreatic Cancer AJCC v8 / Stage III Renal Cell Cancer / Stage III Renal Cell Cancer AJCC v8 / Stage IV Pancreatic Cancer / Stage IV Pancreatic Cancer AJCC v8 / Stage IV Renal Cell Cancer / Stage IV Renal Cell Cancer AJCC v8 / Urothelial carcinoma ureter metastatic1
2RecruitingTreatmentDebulking Surgical Procedures / Fallopian Tube Cancer / Neoadjuvant Treatment / Ovarian Cancer1
2RecruitingTreatmentA Germline or Somatic BRCA Mutation, or a Deleterious Alteration of Other Genes Involved in Homologous Recombination Repair (HRR) or in MSI Status / ER-positive and HER2-negative Metastatic or Locally Advanced Breast Cancer1
2RecruitingTreatmentEndometrium Cancer / Neoplasms, Endometrial / Uterine Neoplasms1
2RecruitingTreatmentFallopian Tube Carcinosarcoma / Fallopian Tube Clear Cell Adenocarcinoma / Fallopian Tube Transitional Cell Carcinoma / Fallopian Tube Undifferentiated Carcinoma / Germline BRCA1 Gene Mutation / Germline BRCA2 Gene Mutation / High Grade Fallopian Tube Serous Adenocarcinoma / High Grade Ovarian Serous Adenocarcinoma / Ovarian Clear Cell Tumor / Ovarian Seromucinous Carcinoma / Ovarian Undifferentiated Carcinoma / Platinum-Sensitive Fallopian Tube Carcinoma / Platinum-Sensitive Ovarian Carcinoma / Platinum-Sensitive Primary Peritoneal Carcinoma / Primary Peritoneal Carcinosarcoma / Primary Peritoneal Clear Cell Carcinoma / Primary Peritoneal High Grade Serous Adenocarcinoma / Primary Peritoneal Transitional Cell Carcinoma / Primary Peritoneal Undifferentiated Carcinoma / Recurrent Fallopian Tube Carcinoma / Recurrent Ovarian Endometrioid Adenocarcinoma / Recurrent Ovarian Serous Adenocarcinoma / Recurrent Ovarian Transitional Cell Carcinoma / Recurrent Primary Peritoneal Carcinoma1
2RecruitingTreatmentGastro-oesophageal Junction Cancer / Malignant Neoplasm of Esophagus / Malignant Neoplasm of Stomach1
2RecruitingTreatmentHigh Grade Serous Carcinoma1
2RecruitingTreatmentInflammatory Breast Carcinoma1
2RecruitingTreatmentKidney Cancer Metastatic / Metastatic Renal Cell Carcinoma / Renal Cancers / Renal Carcinoma / Renal Cell Adenocarcinoma1
2RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)2
2RecruitingTreatmentLung Cancer Small Cell Lung Cancer (SCLC)2
2RecruitingTreatmentMalignancies / Neoplasms / Tumors1
2RecruitingTreatmentMalignant Neoplasm of Pancreas1
2RecruitingTreatmentMalignant Neoplasm of Pancreas / Pancreatic Adenocarcinoma Metastatic / Pancreatic Ductal Adenocarcinoma / Stage IV Pancreatic Cancer AJCC v6 and v71
2RecruitingTreatmentMalignant Solid Neoplasms1
2RecruitingTreatmentMesothelioma1
2RecruitingTreatmentMetastatic Hormone Refractory Prostate Cancer1
2RecruitingTreatmentMetastatic Triple Negative Breast Cancer1
2RecruitingTreatmentMetastatic Urothelial Cancer1
2RecruitingTreatmentMutant High Grade Glioma / Recurrent IDH / Recurrent IDH-mutant High Grade Glioma1
2RecruitingTreatmentNeoplasms, Advanced Solid1
2RecruitingTreatmentNon-small Cell Lung Cancer NSCLC1
2RecruitingTreatmentOvarian Cancer1
2RecruitingTreatmentOvarian Epithelial Cancer1
2RecruitingTreatmentOvarian Epithelial Cancer / Relapses1
2RecruitingTreatmentPlatinum Refractory Extensive-Stage Small Cell Lung Carcinoma1
2RecruitingTreatmentPlatinum-resistant Recurrent Ovarian Cancer1
2RecruitingTreatmentProstate1
2RecruitingTreatmentProstate Cancer2
2RecruitingTreatmentProstate Cancer / Prostate Cancer Aggressiveness1
2RecruitingTreatmentRare Tumor / Refractory Tumors1
2RecruitingTreatmentRecurrent Fallopian Tube Carcinoma / Recurrent Ovarian Carcinoma / Recurrent Primary Peritoneal Carcinoma / Refractory Ovarian Carcinoma1
2RecruitingTreatmentResectable Pancreatic Ductal Adenocarcinoma / Stage 0 Pancreatic Cancer AJCC v8 / Stage I Pancreatic Cancer AJCC v8 / Stage IA Pancreatic Cancer AJCC v8 / Stage IB Pancreatic Cancer AJCC v8 / Stage II Pancreatic Cancer AJCC v8 / Stage IIA Pancreatic Cancer AJCC v8 / Stage IIB Pancreatic Cancer AJCC v8 / Stage III Pancreatic Cancer AJCC v81
2RecruitingTreatmentSquamous Cell Carcinoma of the Head and Neck (SCCHN)1
2RecruitingTreatmentStage III Uterine Corpus Leiomyosarcoma AJCC v8 / Stage IIIA Uterine Corpus Leiomyosarcoma AJCC v8 / Stage IIIB Uterine Corpus Leiomyosarcoma AJCC v8 / Stage IIIC Uterine Corpus Leiomyosarcoma AJCC v8 / Stage IV Uterine Corpus Leiomyosarcoma AJCC v8 / Stage IVA Uterine Corpus Leiomyosarcoma AJCC v8 / Stage IVB Uterine Corpus Leiomyosarcoma AJCC v81
2RecruitingTreatmentTriple Negative Breast Cancer (TNBC)1
2SuspendedTreatmentExtensive Stage Lung Small Cell Carcinoma / Extensive Stage Small Cell Lung Carcinoma / Small Cell Lung Carcinoma1
2WithdrawnTreatmentFallopian Tube Cancer / Malignant Peritoneal Neoplasm / Ovarian Cancer1
2, 3RecruitingTreatmentBreast Cancer1
2, 3RecruitingTreatmentDeleterious BRCA1 Gene Mutation / Deleterious BRCA2 Gene Mutation / Fallopian Tube Clear Cell Adenocarcinoma / Fallopian Tube Endometrioid Adenocarcinoma / Fallopian Tube Mucinous Adenocarcinoma / Fallopian Tube Serous Adenocarcinoma / Fallopian Tube Transitional Cell Carcinoma / Fallopian Tube Undifferentiated Carcinoma / Malignant Ovarian Mixed Epithelial Tumor / Ovarian Clear Cell Adenocarcinoma / Ovarian Endometrioid Adenocarcinoma / Ovarian Mucinous Adenocarcinoma / Ovarian Seromucinous Carcinoma / Ovarian Serous Adenocarcinoma / Ovarian Transitional Cell Carcinoma / Ovarian Undifferentiated Carcinoma / Primary Peritoneal Serous Adenocarcinoma / Recurrent Fallopian Tube Carcinoma / Recurrent Ovarian Carcinoma / Recurrent Primary Peritoneal Carcinoma / Undifferentiated Fallopian Tube Carcinoma / Undifferentiated Ovarian Carcinoma1
3Active Not RecruitingTreatmentAdvanced Ovarian Cancer / BRCA Mutation / Complete Response / FIGO Stage III-IV / First Line Platinum Chemotherapy / Newly Diagnosed / Partial Response1
3Active Not RecruitingTreatmentBRCA 1 Gene Mutation / BRCA 2 Gene Mutation / Breast Cancer Metastatic1
3Active Not RecruitingTreatmentBRCA Mutated / Following Complete or Partial Response to Platinum Based Chemotherapy / Platinum Sensitive / Recurrent Ovarian Cancer1
3Active Not RecruitingTreatmentBRCA Rearrangement / Deleterious BRCA1 Gene Mutation / Deleterious BRCA2 Gene Mutation / Endometrial Undifferentiated Carcinoma / Fallopian Tube Clear Cell Adenocarcinoma / Fallopian Tube Transitional Cell Carcinoma / Fallopian Tube Undifferentiated Carcinoma / Malignant Ovarian Mixed Epithelial Tumor / Ovarian Clear Cell Adenocarcinoma / Ovarian Endometrioid Tumor / Ovarian Seromucinous Carcinoma / Ovarian Serous Tumor / Ovarian Transitional Cell Carcinoma / Ovarian Undifferentiated Carcinoma / Recurrent Fallopian Tube Carcinoma / Recurrent Ovarian Carcinoma / Recurrent Ovarian Endometrioid Adenocarcinoma / Recurrent Primary Peritoneal Carcinoma / Undifferentiated Fallopian Tube Carcinoma / Undifferentiated Ovarian Carcinoma1
3Active Not RecruitingTreatmentBreast Cancer1
3Active Not RecruitingTreatmentFollowing Complete or Partial Response to Platinum Based Chemotherapy / Platinum Sensitive / Recurrent Ovarian Cancer1
3Active Not RecruitingTreatmentGermline BRCA1/2 Mutations and / Metastatic Adenocarcinoma of the Pancreas1
3Active Not RecruitingTreatmentGermline BRCA1/2 Mutations / HER2-ve Metastatic Breast Cancer / Somatic BRCA1/2 Mutations1
3Active Not RecruitingTreatmentMalignant Neoplasm of Stomach1
3Active Not RecruitingTreatmentMetastatic Castration Resistant Prostate Cancer1
3Active Not RecruitingTreatmentNon-Germline BRCA Mutated Ovarian Cancer1
3Active Not RecruitingTreatmentRelapsed Ovarian Cancer, BRCA Mutation, Platinum Sensitivity1
3RecruitingHealth Services ResearchSoft Tissue Sarcoma (STS)1
3RecruitingTreatmentAbdominal wall neoplasm / Fallopian Tube Cancer / Ovarian Cancer1
3RecruitingTreatmentAdvanced Ovarian Cancer1
3RecruitingTreatmentBreast Cancer1
3RecruitingTreatmentCarcinoma, Non-squamous Non-small-cell Lung1
3RecruitingTreatmentCarcinoma, Squamous Cell, Non-small-cell Lung1
3RecruitingTreatmentMetastatic Castration Resistant Prostate Cancer1
3RecruitingTreatmentOvarian Cancer2
3RecruitingTreatmentOvarian Epithelial Cancer1
3RecruitingTreatmentProstatic Neoplasms1
3WithdrawnTreatmentPlatinum Sensitive Relapsed Ovarian Cancer1
4Active Not RecruitingOtherBRCA or HRR+ Mutated Ovarian Cancer Patients / BRCAm Ovarian Cancer1
4Not Yet RecruitingTreatmentMelanoma1
Not AvailableActive Not RecruitingTreatmentOvarian Cancer1
Not AvailableApproved for MarketingNot AvailableOvarian Cancer1
Not AvailableCompletedNot AvailableEndometrial Carcinoma1
Not AvailableNo Longer AvailableNot AvailablePSR Ovarian Cancer With a BRCA Mutation1
Not AvailableRecruitingNot AvailableRelapsed Ovarian Cancers Patients1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
CapsuleOral50 mg
CapsuleOral50 mg/1
TabletOral100 mg
TabletOral150 mg
Tablet, film coatedOral100 mg/1
Tablet, film coatedOral150 mg/1
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US8859562No2014-10-142031-08-04Us
US8912187No2014-12-162024-03-12Us
US8143241No2012-03-272027-08-12Us
US7449464No2008-11-112024-10-11Us
US8247416No2012-08-212028-09-24Us
US7151102No2006-12-192022-04-29Us
US7981889No2011-07-192024-10-11Us
US8475842No2013-07-022029-12-31Us
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

    Learn more

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.119 mg/mLALOGPS
logP2.68ALOGPS
logP2.32ChemAxon
logS-3.6ALOGPS
pKa (Strongest Acidic)8.75ChemAxon
pKa (Strongest Basic)2.24ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area86.63 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity118.63 m3·mol-1ChemAxon
Polarizability44.03 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as phthalazinones. These are compounds containing a phthalazine bearing a ketone group.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Diazanaphthalenes
Sub Class
Benzodiazines
Direct Parent
Phthalazinones
Alternative Parents
2-halobenzoic acids and derivatives / Benzamides / Benzoyl derivatives / Fluorobenzenes / Pyridazines and derivatives / Piperazines / Aryl fluorides / Cyclopropanecarboxylic acids and derivatives / Vinylogous halides / Tertiary carboxylic acid amides
show 8 more
Substituents
Phthalazinone / 2-halobenzoic acid or derivatives / Halobenzoic acid or derivatives / Benzoic acid or derivatives / Benzamide / Benzoyl / Fluorobenzene / Halobenzene / Monocyclic benzene moiety / Benzenoid
show 23 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
cyclopropanes, monofluorobenzenes, phthalazines, N-acylpiperazine (CHEBI:83766)

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Zinc ion binding
Specific Function
Involved in the base excision repair (BER) pathway, by catalyzing the poly(ADP-ribosyl)ation of a limited number of acceptor proteins involved in chromatin architecture and in DNA metabolism. This ...
Gene Name
PARP1
Uniprot ID
P09874
Uniprot Name
Poly [ADP-ribose] polymerase 1
Molecular Weight
113082.945 Da
References
  1. Verhagen CV, de Haan R, Hageman F, Oostendorp TP, Carli AL, O'Connor MJ, Jonkers J, Verheij M, van den Brekel MW, Vens C: 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. 2015 Sep;116(3):358-65. doi: 10.1016/j.radonc.2015.03.028. Epub 2015 May 13. [PubMed:25981132]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Nad+ adp-ribosyltransferase activity
Specific Function
Involved in the base excision repair (BER) pathway, by catalyzing the poly(ADP-ribosyl)ation of a limited number of acceptor proteins involved in chromatin architecture and in DNA metabolism. This ...
Gene Name
PARP2
Uniprot ID
Q9UGN5
Uniprot Name
Poly [ADP-ribose] polymerase 2
Molecular Weight
66205.31 Da
References
  1. Verhagen CV, de Haan R, Hageman F, Oostendorp TP, Carli AL, O'Connor MJ, Jonkers J, Verheij M, van den Brekel MW, Vens C: 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. 2015 Sep;116(3):358-65. doi: 10.1016/j.radonc.2015.03.028. Epub 2015 May 13. [PubMed:25981132]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Nad+ adp-ribosyltransferase activity
Specific Function
Involved in the base excision repair (BER) pathway, by catalyzing the poly(ADP-ribosyl)ation of a limited number of acceptor proteins involved in chromatin architecture and in DNA metabolism. This ...
Gene Name
PARP3
Uniprot ID
Q9Y6F1
Uniprot Name
Poly [ADP-ribose] polymerase 3
Molecular Weight
60069.7 Da
References
  1. Verhagen CV, de Haan R, Hageman F, Oostendorp TP, Carli AL, O'Connor MJ, Jonkers J, Verheij M, van den Brekel MW, Vens C: 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. 2015 Sep;116(3):358-65. doi: 10.1016/j.radonc.2015.03.028. Epub 2015 May 13. [PubMed:25981132]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Verhagen CV, de Haan R, Hageman F, Oostendorp TP, Carli AL, O'Connor MJ, Jonkers J, Verheij M, van den Brekel MW, Vens C: 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. 2015 Sep;116(3):358-65. doi: 10.1016/j.radonc.2015.03.028. Epub 2015 May 13. [PubMed:25981132]
  2. Linparza (olaparib) drug monograph [File]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
Molecular Weight
56277.81 Da
References
  1. Verhagen CV, de Haan R, Hageman F, Oostendorp TP, Carli AL, O'Connor MJ, Jonkers J, Verheij M, van den Brekel MW, Vens C: 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. 2015 Sep;116(3):358-65. doi: 10.1016/j.radonc.2015.03.028. Epub 2015 May 13. [PubMed:25981132]
  2. Olaparib Health Canada Product Monograph [File]
  3. Olaparib EMA Label [File]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 Da

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Olaparib New Zealand Data Sheet [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
Gene Name
ABCG2
Uniprot ID
Q9UNQ0
Uniprot Name
ATP-binding cassette sub-family G member 2
Molecular Weight
72313.47 Da
References
  1. Olaparib New Zealand Data Sheet [Link]

Drug created on May 14, 2015 14:38 / Updated on November 16, 2019 10:43