Identification

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.

Structure
Thumb
Synonyms
  • 4-(3-{[4-(cyclopropylcarbonyl)piperazin-1-yl]carbonyl}-4-fluorobenzyl)phthalazin-1(2H)-one
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
LynparzaCapsule50 mg/1OralAstraZeneca Pharmaceuticals LP2014-12-242020-03-31Us
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
  • Indicated for the maintenance treatment of adult patients with recurrent epithelial ovarian, fallopian tube or primary peritoneal cancer, who are in a complete or partial response to platinum-based chemotherapy.

  • Indicated as monotherapy in patients with deleterious or suspected deleterious germline BRCA mutated (as detected by an FDA-approved test) advanced ovarian cancer who have been treated with three or more prior lines of chemotherapy.

  • Indicated for the treatment of patients with germline breast cancer susceptibility gene (BRCA) mutated, human epidermal growth factor receptor 2 (HER2)-negative metastatic breast cancer, who have been previously treated with chemotherapy.

Associated Conditions
Pharmacodynamics
Not Available
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. 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.

TargetActionsOrganism
APoly [ADP-ribose] polymerase 1
inhibitor
Human
APoly [ADP-ribose] polymerase 2
inhibitor
Human
APoly [ADP-ribose] polymerase 3
inhibitor
Human
Absorption

Peak plasma concentrations achieved typically between 1 to 3 hours following oral administration of olaparib in capsule formulation.

Volume of distribution

167 +/-196 L following a single dose of 400mg olaparib.

Protein binding

Approximately 82%.

Metabolism

Primarily CYP3A4 in vitro.

Route of elimination

44% via the urine and 42% via the feces.

Half life

11.9 hours, standard deviation 4.8 hours.

Clearance

8.6 +/- 7.1L/h.

Toxicity

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

Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(R)-warfarinThe metabolism of (R)-warfarin can be decreased when combined with Olaparib.
(S)-WarfarinThe metabolism of (S)-Warfarin can be decreased when combined with Olaparib.
2-MethoxyethanolThe risk or severity of adverse effects can be increased when 2-Methoxyethanol is combined with Olaparib.
3,5-diiodothyropropionic acidThe metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Olaparib.
4-hydroxycoumarinThe metabolism of 4-hydroxycoumarin can be decreased when combined with Olaparib.
5-androstenedioneThe metabolism of 5-androstenedione can be decreased when combined with Olaparib.
6-Deoxyerythronolide BThe metabolism of Olaparib can be decreased when combined with 6-Deoxyerythronolide B.
6-O-benzylguanineThe metabolism of 6-O-benzylguanine can be decreased when 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.
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]
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 (297 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0RecruitingNot AvailableEndometrial Carcinoma1
0RecruitingBasic ScienceCancer of the Ovary1
0RecruitingTreatmentCancer of the Ovary1
0RecruitingTreatmentPulmonary Arterial Hypertension (PAH)1
1Active Not RecruitingBasic ScienceTumors, Solid2
1Active Not RecruitingOtherTumors, Solid2
1Active Not RecruitingTreatmentAdvanced Ovarian Cancer / Carboplatin / Paclitaxel / Triple Negative Metastatic Breast Cancer1
1Active Not RecruitingTreatmentAdvanced Solid Tumors1
1Active Not RecruitingTreatmentBRCA1 Protein / BRCA2 Protein / Neoplasms, Ovarian1
1Active Not RecruitingTreatmentBone Tumors / Soft Tissue Sarcoma (STS)1
1Active Not RecruitingTreatmentCancer of the Ovary / Cancer, Breast1
1Active Not RecruitingTreatmentCancer of the Ovary / Fallopian Tube Cancer / Primary Peritoneal Cancer1
1Active Not RecruitingTreatmentTumors, Solid1
1CompletedTreatmentAdvanced Solid Malignancies1
1CompletedTreatmentAdvanced Solid Malignancies / Malignancies1
1CompletedTreatmentAdvanced Solid Tumours1
1CompletedTreatmentBrain and Central Nervous System Tumors1
1CompletedTreatmentCancer of the Ovary / Cancer, Breast / Cervical Cancers / Endometrial Cancers / Fallopian Tube Cancer / Primary Peritoneal Cancer1
1CompletedTreatmentCancer, Breast1
1CompletedTreatmentCancer, Breast / 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
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 Metastatic / Cancer, Breast1
1Not Yet RecruitingTreatmentMalignant Lymphomas1
1Not Yet RecruitingTreatmentSquamous Cell Carcinoma of the Head and Neck (SCCHN)1
1RecruitingOtherProstate Cancer1
1RecruitingTreatmentAdvanced Cancers1
1RecruitingTreatmentAdvanced Solid Tumours1
1RecruitingTreatmentAnatomic 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
1RecruitingTreatmentBreast Neoplasm Malignant Female / Breast Neoplasms, Triple-Negative / Radiotherapy Side Effect1
1RecruitingTreatmentCancer of the Ovary / Cancer, Advanced / Cancer, Breast1
1RecruitingTreatmentCancer of the Ovary / Malignant Lymphomas / Malignant Solid Tumours1
1RecruitingTreatmentCarcinoma of the Oesophagus1
1RecruitingTreatmentEstrogen Receptor Negative / HER2/Neu Negative / High Grade Fallopian Tube Serous Adenocarcinoma / High Grade Ovarian Serous Adenocarcinoma / Metastatic Malignant Solid Neoplasm / Metastatic Solid Neoplasm / 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
1RecruitingTreatmentInflammatory Breast Carcinoma / Locally Advanced Malignant Neoplasm / Triple-Negative Invasive Breast Carcinoma1
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
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 / Prostatic Neoplasms1
1RecruitingTreatmentMuscle Invasive Bladder Cancer1
1RecruitingTreatmentOvarian, Breast, and Second-Line Small Cell Lung Cancer / Refractory Solid Tumours / Relapsed Small Cell Lung Cancer (SCLC)1
1RecruitingTreatmentSoft-Tissue Sarcoma1
1RecruitingTreatmentTumors, Solid1
1Unknown StatusTreatmentCancer, Advanced1
1WithdrawnTreatmentSquamous Cell Carcinoma (SCC)1
1, 2Active Not RecruitingTreatmentCancer, Breast / Malignant Female Reproductive System Neoplasm1
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 RecruitingTreatmentStage III Ovarian Cancer / Stage IV Ovarian Cancer / Uterine Malignancies1
1, 2Not Yet RecruitingTreatmentAdenocarcinoma, Prostate / Castration Levels of Testosterone / Castration-Resistant Prostate Carcinoma / Metastatic Malignant Neoplasm in the Bone / PSA Progression1
1, 2Not Yet RecruitingTreatmentMalignant Lymphomas / Malignant Neoplasms Stated as Primary Lymphoid Haematopoietic1
1, 2Not Yet RecruitingTreatmentRecurrent Endometrial Cancer1
1, 2RecruitingDiagnosticOral Squamous Cell Carcinoma (OSCC)1
1, 2RecruitingTreatmentAbdominal wall neoplasm / Cancer of the Ovary / Fallopian Tube Cancer1
1, 2RecruitingTreatmentAdenocarcinomas of the Gastroesophageal Junction / Advanced Gastric Cancer / Metastatic Malignant Neoplasm in the Lymph Nodes / Recurrent Gastric Carcinoma / Stage IV Gastric Cancer AJCC v71
1, 2RecruitingTreatmentAdvanced Solid Tumors / Cancer of the Ovary / Cancer, Advanced / Cancer, Breast / Endometrial Cancers1
1, 2RecruitingTreatmentBreast / Lung Cancer Small Cell Lung Cancer (SCLC) / Malignant Neoplasm of Stomach / Ovarian1
1, 2RecruitingTreatmentCancer of the Ovary / Cancer, Breast / Colorectal Cancers / Lung Cancers / Prostate Cancer / Triple Negative Breast Cancer (TNBC)1
1, 2RecruitingTreatmentCancer, Breast1
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 / Small Cell Lung Carcinoma / Tumors, Solid1
1, 2RecruitingTreatmentLung Cancer Small Cell Lung Cancer (SCLC)1
1, 2RecruitingTreatmentMalignant Gliomas / PARP Inhibitor / Radiotherapy1
1, 2RecruitingTreatmentNeoplasms, Breast1
1, 2RecruitingTreatmentPrimary Peritoneal Carcinoma1
1, 2WithdrawnTreatmentCancer of the Breast1
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 RecruitingTreatmentCancer of the Ovary2
2Active Not RecruitingTreatmentCancer, Breast / Ovarian Carcinoma1
2Active Not RecruitingTreatmentCancer, Breast / Triple Negative Breast Cancer (TNBC)1
2Active Not RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
2Active Not RecruitingTreatmentMalignant Neoplasm of Stomach1
2Active Not RecruitingTreatmentMetastatic Castration Resistant Prostate Cancer1
2Active Not RecruitingTreatmentNeoplasms, Breast1
2CompletedTreatmentCancer of the Ovary3
2CompletedTreatmentColorectal Cancers1
2CompletedTreatmentEwing's Sarcoma (ES)1
2CompletedTreatmentNeoplasms, Ovarian2
2Not Yet RecruitingBasic ScienceRenal Cell Adenocarcinoma1
2Not Yet RecruitingOtherNeoplasms, Breast1
2Not Yet RecruitingTreatmentAbnormal DNA Repair / ATM Gene Mutation / ATR Gene Mutation / BAP1 Gene Mutation / BARD1 Gene Mutation / BLM Gene Mutation / BRCA1 Gene Mutation / Brca2 Gene Mutation / BRIP1 Gene Mutation / CHEK1 Gene Mutation / CHEK2 Gene Mutation / FANCC Gene Mutation / FANCD2 Gene Mutation / FANCE Gene Mutation / FANCF 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
2Not Yet RecruitingTreatmentBladder Cancers1
2Not Yet RecruitingTreatmentCancers With DNA Repair-Deficiency1
2Not Yet RecruitingTreatmentClear Cell Renal Cell Carcinoma / Locally Advance Pancreatic Ductal Adenocarcinoma / Locally Advanced Malignant Solid Neoplasm / Metastatic Malignant Solid Neoplasm / Metastatic Renal Cell Carcinoma / Pancreatic Ductal Adenocarcinoma / Stage III Pancreatic Cancer AJCC v8 / Stage III Renal Cell Cancer AJCC v8 / Stage IV Pancreatic Cancer AJCC v8 / Stage IV Renal Cell Cancer AJCC v8 / Urothelial carcinoma ureter metastatic1
2Not Yet RecruitingTreatmentEndometrial Carcinoma1
2Not Yet RecruitingTreatmentLung Cancer Small Cell Lung Cancer (SCLC)1
2Not Yet RecruitingTreatmentMutant High Grade Glioma / Recurrent IDH / Recurrent IDH-mutant High Grade Glioma1
2Not Yet RecruitingTreatmentNeoplasms, Advanced Solid1
2RecruitingScreeningAdvanced Malignant Solid Neoplasm / Ann Arbor Stage III Childhood Non-Hodgkin Lymphoma / Ann Arbor Stage IV Childhood Non-Hodgkin Lymphoma / Childhood Langerhans Cell Histiocytosis / 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 Solid Neoplasm / Recurrent Neuroblastoma / Recurrent Osteosarcoma / Recurrent Peripheral Primitive Neuroectodermal Tumor / Recurrent Rhabdoid Tumor / Refractory Central Nervous System Neoplasm / Refractory Childhood Malignant Germ Cell Tumor / Refractory Ewing Sarcoma / Refractory Glioma / Refractory Hepatoblastoma / Refractory Langerhans cell histiocytosis / 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
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 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 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 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 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 Prostate1
2RecruitingTreatmentAdenocarcinoma, Prostate / Castration Levels of Testosterone / Castration-Resistant Prostate Carcinoma / PSA Level Greater Than or Equal to One / PSA Progression1
2RecruitingTreatmentAdvanced Breast Cancer1
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 Langerhans cell histiocytosis / Refractory Malignant Solid Neoplasm / Refractory Neuroblastoma / Refractory Non-Hodgkin's lymphoma / Rhabdoid Tumors / Stage III Childhood Non-Hodgkin Lymphoma / Stage IV Childhood Non-Hodgkin Lymphoma / Wilms' tumor1
2RecruitingTreatmentAdvanced Ovarian Cancer1
2RecruitingTreatmentAdvanced Solid Tumors / Multiple Myeloma (MM) / Non-Hodgkin's Lymphoma (NHL)2
2RecruitingTreatmentBRCA1 Gene Mutation / Brca2 Gene Mutation / Estrogen Receptor Negative / HER2/Neu Negative / 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
2RecruitingTreatmentCancer of Unknown Primary Site1
2RecruitingTreatmentCancer of the Ovary2
2RecruitingTreatmentCancer of the Ovary / Debulking Surgical Procedures / Fallopian Tube Cancer / Neoadjuvant Treatment1
2RecruitingTreatmentCancer, Breast1
2RecruitingTreatmentCarcinosarcoma / Neoplasms, Endometrial1
2RecruitingTreatmentCastration Levels of Testosterone / Castration-Resistant Prostate Carcinoma / Hormone-Resistant Prostate Cancer / Metastatic Hormone Refractory Prostate Cancer / Prostate Adenocarcinoma With Focal Neuroendocrine Differentiation / Prostate Carcinoma Metastatic in the Bone / Prostate Small Cell Carcinoma / PSA Progression / Stage IV Prostate Adenocarcinoma / Stage IV Prostate Adenocarcinoma AJCC v71
2RecruitingTreatmentEndometrial 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
2RecruitingTreatmentInflammatory Breast Carcinoma1
2RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)2
2RecruitingTreatmentLung Cancer Small Cell Lung Cancer (SCLC)1
2RecruitingTreatmentMalignancies1
2RecruitingTreatmentMalignancies / Neoplasms / Tumors1
2RecruitingTreatmentMalignant Neoplasm of Pancreas2
2RecruitingTreatmentMalignant Solid Neoplasms1
2RecruitingTreatmentMesothelioma1
2RecruitingTreatmentMetastatic Breast Cancer (MBC)1
2RecruitingTreatmentMetastatic Hormone Refractory Prostate Cancer1
2RecruitingTreatmentMetastatic Triple Negative Breast Cancer1
2RecruitingTreatmentMetastatic Urothelial Cancer1
2RecruitingTreatmentNeoplasms, Germ Cell and Embryonal1
2RecruitingTreatmentNeoplasms, Ovarian1
2RecruitingTreatmentOvarian Epithelial Cancer1
2RecruitingTreatmentPlatinum Refractory Extensive-Stage Small Cell Lung Carcinoma1
2RecruitingTreatmentPlatinum-resistant Recurrent Ovarian Cancer1
2RecruitingTreatmentProstate1
2RecruitingTreatmentProstate Cancer / Prostate Cancer Aggressiveness1
2RecruitingTreatmentRare Tumor / Refractory Tumors1
2RecruitingTreatmentRecurrent Fallopian Tube Carcinoma / Recurrent Ovarian Carcinoma / Recurrent Primary Peritoneal Carcinoma / Refractory Ovarian Carcinoma1
2RecruitingTreatmentRecurrent Platinum Resistant Ovarian Cancer1
2RecruitingTreatmentRelapsed Ovarian Cancer, BRCA Mutation, Platinum Sensitivity1
2RecruitingTreatmentSquamous Cell Carcinoma of the Head and Neck (SCCHN)1
2RecruitingTreatmentUrinary Bladder Neoplasms1
2SuspendedTreatmentAdvanced 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
2SuspendedTreatmentExtensive Stage Lung Small Cell Carcinoma / Extensive Stage Small Cell Lung Carcinoma / Small Cell Lung Carcinoma1
2SuspendedTreatmentRecurrent Glioblastoma1
2WithdrawnTreatmentCancer of the Ovary / Fallopian Tube Cancer / Malignant Peritoneal Neoplasm1
2, 3RecruitingTreatmentCancer, Breast1
2, 3SuspendedTreatmentDeleterious 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 RecruitingTreatmentMalignant Neoplasm of Stomach1
3Active Not RecruitingTreatmentRelapsed Ovarian Cancer, BRCA Mutation, Platinum Sensitivity1
3Not Yet RecruitingTreatmentAbdominal wall neoplasm / Cancer of the Ovary / Fallopian Tube Cancer1
3Not Yet RecruitingTreatmentAdvanced Ovarian Cancer1
3Not Yet RecruitingTreatmentCancer of the Ovary1
3RecruitingPreventionCancer, Breast1
3RecruitingTreatmentCancer of the Ovary1
3RecruitingTreatmentFollowing Complete or Partial Response to Platinum Based Chemotherapy / Platinum Sensitive / Recurrent Ovarian Cancer1
3RecruitingTreatmentGermline BRCA1/2 Mutations and / Metastatic Adenocarcinoma of the Pancreas1
3RecruitingTreatmentGermline BRCA1/2 Mutations / HER2-ve Metastatic Breast Cancer / Somatic BRCA1/2 Mutations1
3RecruitingTreatmentMetastatic Castration Resistant Prostate Cancer1
3RecruitingTreatmentNon-Germline BRCA Mutated Ovarian Cancer1
3RecruitingTreatmentOvarian Epithelial Cancer1
3WithdrawnTreatmentPlatinum Sensitive Relapsed Ovarian Cancer1
4Active Not RecruitingOtherBRCA or HRR+ Mutated Ovarian Cancer Patients / BRCAm Ovarian Cancer1
Not AvailableApproved for MarketingNot AvailableCancer of the Ovary1
Not AvailableNo Longer AvailableNot AvailablePSR Ovarian Cancer With a BRCA Mutation1
Not AvailableRecruitingTreatmentCancer of the Ovary1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
CapsuleOral50 mg
CapsuleOral50 mg/1
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

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
Human
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
Human
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
Human
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
Human
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]
Kind
Protein
Organism
Human
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]

Drug created on May 14, 2015 14:38 / Updated on December 10, 2018 13:38