niraparib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
poly-ADP-ribose polymerase inhibitors 5222 1038915-60-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • niraparib hydrochloride
  • niraparib HCl
  • MK-4827
  • niraparib
  • niraparib tosylate monohydrate
  • niraparib tosylate
  • zejula
Niraparib is an inhibitor of poly(ADP-ribose) polymerase (PARP) enzymes, PARP-1 and PARP-2, which play a role in DNA repair. In vitro studies have shown that niraparib-induced cytotoxicity may involve inhibition of PARP enzymatic activity and increased formation of PARP-DNA complexes resulting in DNA damage, apoptosis and cell death. Increased niraparib-induced cytotoxicity was observed in tumor cell lines with or without deficiencies in BRCA1/2. Niraparib decreased tumor growth in mouse xenograft models of human cancer cell lines with deficiencies in BRCA1/2 and in human patient-derived xenograft tumor models with homologous recombination deficiency that had either mutated or wild type BRCA1/2.
  • Molecular weight: 320.40
  • Formula: C19H20N4O
  • CLOGP: 2.79
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 2
  • TPSA: 72.94
  • ALOGS: -4.33
  • ROTB: 3
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.30 g O

ADMET properties:

PropertyValueReference
S (Water solubility) 0.70 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Bocci G, Oprea TI, Benet LZ
BA (Bioavailability) 37 %

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 0.553 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 4.764 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 5.358 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 4.529 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 25.880 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 55.560 % High 1
herg hERG pIC50 5.398 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 1.384 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 3.148 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 32.720 % High 1
kinase-safety-class AAK1,ACVR2A,ACVR2B,ACVRL1,AKT1,AKT2,AKT3,ALK,AURKA,AURKB,AURKC,AXL,BRAF,CAMK2A,CAMK2B,CAMK2D,CAMK2G,CDK1,CDK16,CDK5,CDK7,CDK9,CHEK1,CLK2,CLK4,CSF1R,DDR1,DYRK1A,DYRK1B,DYRK2,EGFR,EIF2AK3,EPHA2,EPHB4,ERBB2,FLT3,FLT4,GAK,GRK1,GRK2,GSK3B,HASPIN,IKBKB,INSR,IRAK1,IRAK3,IRAK4,ITK,JAK1,JAK2,JAK3,KDR,KIT,LCK,LRRK2,LYN,MAP2K1,MAP2K6,MAP3K1,MAP3K10,MAP3K11,MAP3K14,MAP3K21,MAP3K7,MAP4K1,MAP4K2,MAP4K3,MAP4K5,MAPK1,MAPK10,MAPK12,MAPK3,MAPK7,MAPK9,MARK4,MELK,MET,MINK1,MKNK1,MKNK2,NTRK1,NTRK2,NTRK3,NUAK1,PAK2,PAK4,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIM2,PRKAA1,PRKAA2,PRKACA,PRKCD,PRKCZ,PRKDC,ROCK1,ROCK2,SGK1,SIK2,SIK3,SRC,STK17A,STK33,STK4,SYK,TEK,TGFBR1,TNIK,TTK,TYRO3,ULK1,ULK2 115
kinase-selectivity-class AAK1,ACVR2B,AKT1,AKT2,AKT3,ALK,AURKB,AURKC,AXL,BRAF,CAMK2A,CAMK2B,CAMK2D,CDK4,CDK9,CHEK1,CLK2,CLK4,CSF1R,DYRK1B,EGFR,EIF2AK3,FLT3,GAK,HASPIN,IGF1R,INSR,IRAK1,IRAK4,JAK1,JAK2,KDR,KIT,LRRK2,MAP3K10,MAP3K11,MAP3K14,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAPK1,MAPK7,MARK1,MARK3,MARK4,MELK,NTRK1,NTRK3,NUAK1,PAK4,PDK1,PDPK1,PIM3,PRKAA1,PRKAA2,PRKCD,ROCK1,ROCK2,SIK2,SIK3,STK33,STK4,SYK,TNIK,TNK1,TTK,TYRO3,ULK1,ULK2 70
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 6.714 High 1
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 6.516 High 1
mh-clint Mouse hepatocyte intrinsic clearance 13.996 High 1
mppb Mouse plasma protein binding (% unbound) 22.990 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 21.777 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 52.930 % High 1
rat-kpuu-brain Rat brain Kpuu 0.044 % High 1
rh-clint Rat hepatocyte intrinsic clearance 4.887 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 60.990 % High 1
rppb Rat plasma protein binding (% unbound) 30.240 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 731.139 uM High 1

Approvals:

DateAgencyCompanyOrphan
Sept. 25, 2020 PMDA TAKEDA PHARMACEUTICAL COMPANY LIMITED
Nov. 16, 2017 EMA Tesaro UK Limited
March 27, 2017 FDA TESARO INC

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Platelet count decreased 1152.48 27.04 513 13487 136456 90477991
Carbohydrate antigen 125 increased 665.75 27.04 143 13857 3123 90611324
Recurrent cancer 583.09 27.04 122 13878 2337 90612110
Disease progression 494.97 27.04 305 13695 156310 90458137
Thrombocytopenia 413.00 27.04 304 13696 208421 90406026
Constipation 380.24 27.04 327 13673 280068 90334379
Malignant neoplasm progression 286.88 27.04 188 13812 106682 90507765
Nausea 260.50 27.04 544 13456 1109772 89504675
Intentional underdose 255.13 27.04 60 13940 1989 90612458
Myelodysplastic syndrome 243.43 27.04 99 13901 20804 90593643
Haemoglobin decreased 231.47 27.04 195 13805 161761 90452686
Blood pressure increased 223.16 27.04 208 13792 197009 90417438
Red blood cell count decreased 198.05 27.04 110 13890 46241 90568206
Renal impairment 191.12 27.04 146 13854 105275 90509172
Insomnia 188.35 27.04 244 13756 333230 90281217
Ovarian cancer recurrent 184.59 27.04 44 13956 1546 90612901
Anaemia 176.03 27.04 243 13757 352559 90261888
Fatigue 152.39 27.04 455 13545 1153568 89460879
Decreased activity 135.18 27.04 50 13950 8142 90606305
Heart rate increased 133.15 27.04 122 13878 112780 90501667
Product dose omission issue 124.91 27.04 187 13813 291500 90322947
White blood cell count decreased 116.24 27.04 136 13864 166973 90447474
Tumour marker increased 112.85 27.04 40 13960 5767 90608680
Acute myeloid leukaemia 110.65 27.04 57 13943 20583 90593864
Neutrophil count decreased 99.66 27.04 85 13915 71447 90543000
Full blood count abnormal 89.86 27.04 61 13939 36536 90577911
Ovarian cancer 68.44 27.04 29 13971 6738 90607709
Blood creatinine increased 64.65 27.04 79 13921 101307 90513140
Decreased appetite 62.49 27.04 162 13838 376378 90238069
Intestinal obstruction 61.91 27.04 49 13951 37082 90577365
Product dose omission in error 57.16 27.04 37 13963 20466 90593981
Therapy cessation 56.41 27.04 46 13954 36315 90578132
Neuropathy peripheral 55.91 27.04 86 13914 136884 90477563
Full blood count decreased 51.26 27.04 40 13960 29649 90584798
Haematocrit decreased 46.92 27.04 44 13956 41788 90572659
Photosensitivity reaction 46.87 27.04 31 13969 17776 90596671
Platelet count abnormal 45.25 27.04 19 13981 4316 90610131
Drug hypersensitivity 44.09 27.04 9 13991 463600 90150847
Emotional distress 43.90 27.04 40 13960 36622 90577825
Myeloid leukaemia 43.22 27.04 11 13989 508 90613939
Swelling 42.28 27.04 7 13993 419051 90195396
Headache 39.14 27.04 247 13753 862499 89751948
Pancytopenia 38.90 27.04 68 13932 120195 90494252
Drug monitoring procedure not performed 38.68 27.04 11 13989 776 90613671
Glossodynia 38.36 27.04 3 13997 321776 90292671
Blood test abnormal 37.85 27.04 29 13971 20923 90593524
Ileus 36.89 27.04 26 13974 16520 90597927
Joint swelling 36.59 27.04 16 13984 503284 90111163
Haematotoxicity 35.87 27.04 23 13977 12512 90601935
Blood magnesium decreased 35.78 27.04 25 13975 15668 90598779
Dry mouth 35.54 27.04 84 13916 183975 90430472
Coronavirus infection 34.75 27.04 17 13983 5498 90608949
Adverse drug reaction 33.93 27.04 63 13937 116638 90497809
Lymphangioleiomyomatosis 33.69 27.04 8 13992 276 90614171
Treatment failure 33.17 27.04 4 13996 303924 90310523
Metastases to peritoneum 32.92 27.04 15 13985 4140 90610307
Computerised tomogram abnormal 32.52 27.04 13 13987 2606 90611841
Hepatic enzyme increased 32.28 27.04 8 13992 360728 90253719
Ovarian epithelial cancer recurrent 30.64 27.04 5 13995 21 90614426
Palpitations 30.39 27.04 66 13934 136662 90477785
Small intestinal obstruction 29.07 27.04 25 13975 21209 90593238
Eastern Cooperative Oncology Group performance status worsened 28.94 27.04 11 13989 1928 90612519
Laboratory test abnormal 28.93 27.04 34 13966 41820 90572627
Feeling abnormal 28.74 27.04 73 13927 167162 90447285
Hospice care 28.25 27.04 18 13982 9686 90604761
Myelosuppression 28.22 27.04 38 13962 53553 90560894
General physical health deterioration 27.91 27.04 10 13990 355105 90259342
Hypersensitivity 27.83 27.04 18 13982 454659 90159788
Pneumonia 27.47 27.04 35 13965 638024 89976423

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Platelet count decreased 612.48 27.11 331 9592 230112 110349264
Recurrent cancer 520.18 27.11 107 9816 3316 110576060
Carbohydrate antigen 125 increased 496.69 27.11 98 9825 2449 110576927
Disease progression 351.72 27.11 237 9686 243797 110335579
Thrombocytopenia 292.71 27.11 245 9678 348640 110230736
Constipation 239.27 27.11 221 9702 357565 110221811
Intentional underdose 214.28 27.11 49 9874 2503 110576873
Myelodysplastic syndrome 199.73 27.11 87 9836 37397 110541979
Nausea 186.53 27.11 367 9556 1235323 109344053
Blood pressure increased 141.09 27.11 143 9780 258230 110321146
Haemoglobin decreased 123.76 27.11 131 9792 248596 110330780
Ovarian cancer recurrent 119.94 27.11 24 9899 643 110578733
Insomnia 119.37 27.11 154 9769 360436 110218940
Red blood cell count decreased 116.59 27.11 73 9850 65850 110513526
Anaemia 114.52 27.11 188 9735 546898 110032478
Renal impairment 107.73 27.11 107 9816 188338 110391038
Acute myeloid leukaemia 104.13 27.11 56 9867 38054 110541322
Fatigue 102.29 27.11 288 9635 1215670 109363706
Decreased activity 91.02 27.11 35 9888 10939 110568437
Malignant neoplasm progression 88.62 27.11 93 9830 174474 110404902
White blood cell count decreased 77.39 27.11 99 9824 229291 110350085
Product dose omission issue 73.18 27.11 115 9808 321667 110257709
Neutrophil count decreased 71.52 27.11 70 9853 120871 110458505
Ovarian cancer 70.93 27.11 23 9900 4373 110575003
Heart rate increased 68.33 27.11 74 9849 143760 110435616
Tumour marker increased 63.85 27.11 22 9901 5038 110574338
Decreased appetite 54.50 27.11 127 9796 475719 110103657
Myeloid leukaemia 43.08 27.11 11 9912 894 110578482
Full blood count abnormal 41.92 27.11 37 9886 56015 110523361
Headache 41.85 27.11 173 9750 882204 109697172
Product dose omission in error 41.44 27.11 26 9897 23486 110555890
Blood creatinine increased 41.00 27.11 65 9858 182824 110396552
Intestinal obstruction 39.53 27.11 35 9888 53192 110526184
Neuropathy peripheral 37.84 27.11 62 9861 179215 110400161
Full blood count decreased 34.11 27.11 26 9897 32073 110547303
Ovarian epithelial cancer recurrent 33.97 27.11 5 9918 18 110579358
Photosensitivity reaction 32.32 27.11 23 9900 25566 110553810
Emotional distress 30.37 27.11 28 9895 44819 110534557
Metastases to peritoneum 29.78 27.11 13 9910 5597 110573779
Small intestinal obstruction 29.71 27.11 24 9899 32189 110547187

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01XK02 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
OTHER ANTINEOPLASTIC AGENTS
Poly (ADP-ribose) polymerase (PARP) inhibitors
ATC L01XK52 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
OTHER ANTINEOPLASTIC AGENTS
Poly (ADP-ribose) polymerase (PARP) inhibitors
MeSH PA D000067856 Poly(ADP-ribose) Polymerase Inhibitors
MeSH PA D000970 Antineoplastic Agents
MeSH PA D004791 Enzyme Inhibitors
FDA MoA N0000191622 Poly(ADP-Ribose) Polymerase Inhibitors
FDA EPC N0000191623 Poly(ADP-Ribose) Polymerase Inhibitor
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:62913 EC 2.4.2.30 (NAD<small><sup>+</small></sup> ADP-ribosyltransferase) inhibitor
CHEBI has role CHEBI:68495 apoptosis inducer
CHEBI has role CHEBI:132992 radiosensitizing agent

Related Drugs by ATC class:

L01XK Poly (ADP-ribose) polymerase (PARP) inhibitors 4 drugs
abiraterone acetateolaparibrucaparibtalazoparib tosylate

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Carcinoma in situ of fallopian tube indication 92591008
Malignant epithelial tumor of ovary indication 254849005
Malignant tumor of ovary indication 363443007 DOID:2394
Malignant tumor of peritoneum indication 363492001
Hormone refractory prostate cancer indication 427492003




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 10.95 acidic
pKa2 9.77 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 100MG BASE ZEJULA GLAXOSMITHKLINE N208447 March 27, 2017 DISCN CAPSULE ORAL 8071579 Aug. 12, 2027 A METHOD OF TREATMENT OF ADVANCED OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER ASSOCIATED WITH HOMOLOGOUS RECOMBINATION DEFICIENCY (HRD) POSITIVE STATUS
EQ 100MG BASE ZEJULA GLAXOSMITHKLINE N208447 March 27, 2017 DISCN CAPSULE ORAL 8143241 Aug. 12, 2027 A METHOD OF TREATMENT OF ADVANCED OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER ASSOCIATED WITH HOMOLOGOUS RECOMBINATION DEFICIENCY (HRD) POSITIVE STATUS
EQ 100MG BASE ZEJULA GLAXOSMITHKLINE N214876 April 26, 2023 RX TABLET ORAL 8071579 Aug. 12, 2027 A METHOD OF TREATMENT OF ADVANCED OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER ASSOCIATED WITH HOMOLOGOUS RECOMBINATION DEFICIENCY (HRD) POSITIVE STATUS
EQ 100MG BASE ZEJULA GLAXOSMITHKLINE N214876 April 26, 2023 RX TABLET ORAL 8143241 Aug. 12, 2027 A METHOD OF TREATMENT OF ADVANCED OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER ASSOCIATED WITH HOMOLOGOUS RECOMBINATION DEFICIENCY (HRD) POSITIVE STATUS
EQ 200MG BASE ZEJULA GLAXOSMITHKLINE N214876 April 26, 2023 RX TABLET ORAL 8071579 Aug. 12, 2027 A METHOD OF TREATMENT OF ADVANCED OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER ASSOCIATED WITH HOMOLOGOUS RECOMBINATION DEFICIENCY (HRD) POSITIVE STATUS
EQ 200MG BASE ZEJULA GLAXOSMITHKLINE N214876 April 26, 2023 RX TABLET ORAL 8143241 Aug. 12, 2027 A METHOD OF TREATMENT OF ADVANCED OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER ASSOCIATED WITH HOMOLOGOUS RECOMBINATION DEFICIENCY (HRD) POSITIVE STATUS
EQ 300MG BASE ZEJULA GLAXOSMITHKLINE N214876 April 26, 2023 RX TABLET ORAL 8071579 Aug. 12, 2027 A METHOD OF TREATMENT OF ADVANCED OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER ASSOCIATED WITH HOMOLOGOUS RECOMBINATION DEFICIENCY (HRD) POSITIVE STATUS
EQ 300MG BASE ZEJULA GLAXOSMITHKLINE N214876 April 26, 2023 RX TABLET ORAL 8143241 Aug. 12, 2027 A METHOD OF TREATMENT OF ADVANCED OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER ASSOCIATED WITH HOMOLOGOUS RECOMBINATION DEFICIENCY (HRD) POSITIVE STATUS
500MG;EQ 100MG BASE AKEEGA JANSSEN BIOTECH N216793 Aug. 11, 2023 RX TABLET ORAL 8071579 Aug. 12, 2027 A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
500MG;EQ 100MG BASE AKEEGA JANSSEN BIOTECH N216793 Aug. 11, 2023 RX TABLET ORAL 8071579 Aug. 12, 2027 A METHOD FOR TREATING METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA2-MUTATION
500MG;EQ 100MG BASE AKEEGA JANSSEN BIOTECH N216793 Aug. 11, 2023 RX TABLET ORAL 8143241 Aug. 12, 2027 A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
500MG;EQ 100MG BASE AKEEGA JANSSEN BIOTECH N216793 Aug. 11, 2023 RX TABLET ORAL 8143241 Aug. 12, 2027 A METHOD FOR TREATING METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA2-MUTATION
500MG;EQ 50MG BASE AKEEGA JANSSEN BIOTECH N216793 Aug. 11, 2023 RX TABLET ORAL 8071579 Aug. 12, 2027 A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
500MG;EQ 50MG BASE AKEEGA JANSSEN BIOTECH N216793 Aug. 11, 2023 RX TABLET ORAL 8071579 Aug. 12, 2027 A METHOD FOR TREATING METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA2-MUTATION
500MG;EQ 50MG BASE AKEEGA JANSSEN BIOTECH N216793 Aug. 11, 2023 RX TABLET ORAL 8143241 Aug. 12, 2027 A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
500MG;EQ 50MG BASE AKEEGA JANSSEN BIOTECH N216793 Aug. 11, 2023 RX TABLET ORAL 8143241 Aug. 12, 2027 A METHOD FOR TREATING METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA2-MUTATION
EQ 100MG BASE ZEJULA GLAXOSMITHKLINE N208447 March 27, 2017 DISCN CAPSULE ORAL 8859562 Aug. 4, 2031 A METHOD OF TREATMENT OF ADVANCED OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER ASSOCIATED WITH HOMOLOGOUS RECOMBINATION DEFICIENCY (HRD) POSITIVE STATUS
EQ 100MG BASE ZEJULA GLAXOSMITHKLINE N214876 April 26, 2023 RX TABLET ORAL 8859562 Aug. 4, 2031 A METHOD OF TREATMENT OF ADVANCED OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER ASSOCIATED WITH HOMOLOGOUS RECOMBINATION DEFICIENCY (HRD) POSITIVE STATUS
EQ 200MG BASE ZEJULA GLAXOSMITHKLINE N214876 April 26, 2023 RX TABLET ORAL 8859562 Aug. 4, 2031 A METHOD OF TREATMENT OF ADVANCED OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER ASSOCIATED WITH HOMOLOGOUS RECOMBINATION DEFICIENCY (HRD) POSITIVE STATUS
EQ 300MG BASE ZEJULA GLAXOSMITHKLINE N214876 April 26, 2023 RX TABLET ORAL 8859562 Aug. 4, 2031 A METHOD OF TREATMENT OF ADVANCED OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER ASSOCIATED WITH HOMOLOGOUS RECOMBINATION DEFICIENCY (HRD) POSITIVE STATUS
500MG;EQ 100MG BASE AKEEGA JANSSEN BIOTECH N216793 Aug. 11, 2023 RX TABLET ORAL 8859562 Aug. 4, 2031 A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
500MG;EQ 100MG BASE AKEEGA JANSSEN BIOTECH N216793 Aug. 11, 2023 RX TABLET ORAL 8859562 Aug. 4, 2031 A METHOD FOR TREATING METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA2-MUTATION
500MG;EQ 50MG BASE AKEEGA JANSSEN BIOTECH N216793 Aug. 11, 2023 RX TABLET ORAL 8859562 Aug. 4, 2031 A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
500MG;EQ 50MG BASE AKEEGA JANSSEN BIOTECH N216793 Aug. 11, 2023 RX TABLET ORAL 8859562 Aug. 4, 2031 A METHOD FOR TREATING METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA2-MUTATION
500MG;EQ 100MG BASE AKEEGA JANSSEN BIOTECH N216793 Aug. 11, 2023 RX TABLET ORAL 11207311 July 28, 2037 A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
500MG;EQ 100MG BASE AKEEGA JANSSEN BIOTECH N216793 Aug. 11, 2023 RX TABLET ORAL 11207311 July 28, 2037 A METHOD FOR TREATING METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA2-MUTATION
500MG;EQ 100MG BASE AKEEGA JANSSEN BIOTECH N216793 Aug. 11, 2023 RX TABLET ORAL 11986468 July 28, 2037 A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
500MG;EQ 100MG BASE AKEEGA JANSSEN BIOTECH N216793 Aug. 11, 2023 RX TABLET ORAL 11986468 July 28, 2037 A METHOD FOR TREATING METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA2-MUTATION
500MG;EQ 100MG BASE AKEEGA JANSSEN BIOTECH N216793 Aug. 11, 2023 RX TABLET ORAL 11986469 July 28, 2037 A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
500MG;EQ 100MG BASE AKEEGA JANSSEN BIOTECH N216793 Aug. 11, 2023 RX TABLET ORAL 11986469 July 28, 2037 A METHOD FOR TREATING METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA2-MUTATION
500MG;EQ 100MG BASE AKEEGA JANSSEN BIOTECH N216793 Aug. 11, 2023 RX TABLET ORAL 11986470 July 28, 2037 A METHOD FOR TREATING METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA2-MUTATION
500MG;EQ 100MG BASE AKEEGA JANSSEN BIOTECH N216793 Aug. 11, 2023 RX TABLET ORAL 11992486 July 28, 2037 A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
500MG;EQ 100MG BASE AKEEGA JANSSEN BIOTECH N216793 Aug. 11, 2023 RX TABLET ORAL 11992486 July 28, 2037 A METHOD FOR TREATING METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA2-MUTATION
500MG;EQ 100MG BASE AKEEGA JANSSEN BIOTECH N216793 Aug. 11, 2023 RX TABLET ORAL 12383543 July 28, 2037 A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
500MG;EQ 100MG BASE AKEEGA JANSSEN BIOTECH N216793 Aug. 11, 2023 RX TABLET ORAL 12383543 July 28, 2037 A METHOD FOR TREATING METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA2-MUTATION
500MG;EQ 50MG BASE AKEEGA JANSSEN BIOTECH N216793 Aug. 11, 2023 RX TABLET ORAL 11207311 July 28, 2037 A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
500MG;EQ 50MG BASE AKEEGA JANSSEN BIOTECH N216793 Aug. 11, 2023 RX TABLET ORAL 11207311 July 28, 2037 A METHOD FOR TREATING METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA2-MUTATION
500MG;EQ 50MG BASE AKEEGA JANSSEN BIOTECH N216793 Aug. 11, 2023 RX TABLET ORAL 11986468 July 28, 2037 A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
500MG;EQ 50MG BASE AKEEGA JANSSEN BIOTECH N216793 Aug. 11, 2023 RX TABLET ORAL 11986468 July 28, 2037 A METHOD FOR TREATING METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA2-MUTATION
500MG;EQ 50MG BASE AKEEGA JANSSEN BIOTECH N216793 Aug. 11, 2023 RX TABLET ORAL 11986469 July 28, 2037 A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
500MG;EQ 50MG BASE AKEEGA JANSSEN BIOTECH N216793 Aug. 11, 2023 RX TABLET ORAL 11986469 July 28, 2037 A METHOD FOR TREATING METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA2-MUTATION
500MG;EQ 50MG BASE AKEEGA JANSSEN BIOTECH N216793 Aug. 11, 2023 RX TABLET ORAL 11986470 July 28, 2037 A METHOD FOR TREATING METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA2-MUTATION
500MG;EQ 50MG BASE AKEEGA JANSSEN BIOTECH N216793 Aug. 11, 2023 RX TABLET ORAL 11992486 July 28, 2037 A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
500MG;EQ 50MG BASE AKEEGA JANSSEN BIOTECH N216793 Aug. 11, 2023 RX TABLET ORAL 11992486 July 28, 2037 A METHOD FOR TREATING METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA2-MUTATION
500MG;EQ 50MG BASE AKEEGA JANSSEN BIOTECH N216793 Aug. 11, 2023 RX TABLET ORAL 12383543 July 28, 2037 A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
500MG;EQ 50MG BASE AKEEGA JANSSEN BIOTECH N216793 Aug. 11, 2023 RX TABLET ORAL 12383543 July 28, 2037 A METHOD FOR TREATING METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA2-MUTATION
EQ 100MG BASE ZEJULA GLAXOSMITHKLINE N208447 March 27, 2017 DISCN CAPSULE ORAL 11673877 March 27, 2038 A METHOD OF TREATMENT OF OVARIAN CANCER OR FALLOPIAN TUBE CANCER
EQ 100MG BASE ZEJULA GLAXOSMITHKLINE N208447 March 27, 2017 DISCN CAPSULE ORAL 11673877 March 27, 2038 A METHOD OF TREATMENT OF RECURRENT OVARIAN CANCER OR FALLOPIAN TUBE CANCER ASSOCIATED WITH DELETERIOUS OR SUSPECTED DELETERIOUS GERMLINE BRCA-MUTATION
EQ 100MG BASE ZEJULA GLAXOSMITHKLINE N214876 April 26, 2023 RX TABLET ORAL 11673877 March 27, 2038 A METHOD OF TREATMENT OF OVARIAN CANCER OR FALLOPIAN TUBE CANCER
EQ 100MG BASE ZEJULA GLAXOSMITHKLINE N214876 April 26, 2023 RX TABLET ORAL 11673877 March 27, 2038 A METHOD OF TREATMENT OF RECURRENT OVARIAN CANCER OR FALLOPIAN TUBE CANCER ASSOCIATED WITH DELETERIOUS OR SUSPECTED DELETERIOUS GERMLINE BRCA-MUTATION
EQ 200MG BASE ZEJULA GLAXOSMITHKLINE N214876 April 26, 2023 RX TABLET ORAL 11673877 March 27, 2038 A METHOD OF TREATMENT OF OVARIAN CANCER OR FALLOPIAN TUBE CANCER
EQ 200MG BASE ZEJULA GLAXOSMITHKLINE N214876 April 26, 2023 RX TABLET ORAL 11673877 March 27, 2038 A METHOD OF TREATMENT OF RECURRENT OVARIAN CANCER OR FALLOPIAN TUBE CANCER ASSOCIATED WITH DELETERIOUS OR SUSPECTED DELETERIOUS GERMLINE BRCA-MUTATION
EQ 300MG BASE ZEJULA GLAXOSMITHKLINE N214876 April 26, 2023 RX TABLET ORAL 11673877 March 27, 2038 A METHOD OF TREATMENT OF OVARIAN CANCER OR FALLOPIAN TUBE CANCER
EQ 300MG BASE ZEJULA GLAXOSMITHKLINE N214876 April 26, 2023 RX TABLET ORAL 11673877 March 27, 2038 A METHOD OF TREATMENT OF RECURRENT OVARIAN CANCER OR FALLOPIAN TUBE CANCER ASSOCIATED WITH DELETERIOUS OR SUSPECTED DELETERIOUS GERMLINE BRCA-MUTATION
500MG;EQ 100MG BASE AKEEGA JANSSEN BIOTECH N216793 Aug. 11, 2023 RX TABLET ORAL 11673877 March 27, 2038 A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
500MG;EQ 100MG BASE AKEEGA JANSSEN BIOTECH N216793 Aug. 11, 2023 RX TABLET ORAL 11673877 March 27, 2038 A METHOD FOR TREATING METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA2-MUTATION
500MG;EQ 50MG BASE AKEEGA JANSSEN BIOTECH N216793 Aug. 11, 2023 RX TABLET ORAL 11673877 March 27, 2038 A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
500MG;EQ 50MG BASE AKEEGA JANSSEN BIOTECH N216793 Aug. 11, 2023 RX TABLET ORAL 11673877 March 27, 2038 A METHOD FOR TREATING METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA2-MUTATION

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
500MG;EQ 100MG BASE AKEEGA JANSSEN BIOTECH N216793 Aug. 11, 2023 RX TABLET ORAL Aug. 11, 2026 NEW PRODUCT
500MG;EQ 50MG BASE AKEEGA JANSSEN BIOTECH N216793 Aug. 11, 2023 RX TABLET ORAL Aug. 11, 2026 NEW PRODUCT
EQ 100MG BASE ZEJULA GLAXOSMITHKLINE N208447 March 27, 2017 DISCN CAPSULE ORAL Oct. 23, 2026 TX OF ADULTS W/ ADV OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER TREATED W/ >=3 PRIOR CHEMO REGIMENS & CANCER ASSOCIATED W/ HRD+ STATUS DEFINED BY A DELETERIOUS OR SUSPECTED DELETERIOUS BRCA MUTATION
EQ 100MG BASE ZEJULA GLAXOSMITHKLINE N208447 March 27, 2017 DISCN CAPSULE ORAL April 29, 2027 INDICATED FOR THE MAINTENANCE TREATMENT OF ADULT PATIENTS WITH ADVANCED EPITHELIAL OVARIAN CANCER WHO ARE IN A COMPLETE OR PARTIAL RESPONSE TO FIRST-LINE PLATINUM-BASED CHEMOTHERAPY
500MG;EQ 100MG BASE AKEEGA JANSSEN BIOTECH N216793 Aug. 11, 2023 RX TABLET ORAL Dec. 12, 2028 NIRAPARIB/ABIRATERONE ACETATE IN FIXED DOSE COMBINATION WITH PREDNISONE FOR THE TREATMENT OF ADULTS WITH DELETERIOUS OR SUSPECTED DELETERIOUS BRCA2-MUTATED METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER
500MG;EQ 50MG BASE AKEEGA JANSSEN BIOTECH N216793 Aug. 11, 2023 RX TABLET ORAL Dec. 12, 2028 NIRAPARIB/ABIRATERONE ACETATE IN FIXED DOSE COMBINATION WITH PREDNISONE FOR THE TREATMENT OF ADULTS WITH DELETERIOUS OR SUSPECTED DELETERIOUS BRCA2-MUTATED METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Poly [ADP-ribose] polymerase 2 Enzyme INHIBITOR IC50 8.68 IUPHAR DRUG LABEL
Poly [ADP-ribose] polymerase 1 Enzyme INHIBITOR IC50 8.42 IUPHAR DRUG LABEL
Tankyrase-2 Enzyme IC50 5.29 CHEMBL
Tankyrase-1 Enzyme IC50 6.24 CHEMBL
Poly [ADP-ribose] polymerase 3 Enzyme IC50 5.89 CHEMBL
Poly [ADP-ribose] polymerase 4 Enzyme IC50 6.48 CHEMBL
Dual specificity tyrosine-phosphorylation-regulated kinase 1B Kinase IC50 6.59 CHEMBL
Poly [ADP-ribose] polymerase 12 Enzyme IC50 7.10 CHEMBL
Poly [ADP-ribose] polymerase 14 Enzyme IC50 5.76 CHEMBL
Poly [ADP-ribose] polymerase 15 Enzyme IC50 4.54 CHEMBL
Poly [ADP-ribose] polymerase 10 Enzyme IC50 5.72 CHEMBL
Dual specificity tyrosine-phosphorylation-regulated kinase 1A Kinase IC50 6.53 CHEMBL

External reference:

IDSource
HMC2H89N35 UNII
1038915-64-8 SECONDARY_CAS_RN
1613220-15-7 SECONDARY_CAS_RN
4036640 VANDF
C2744440 UMLSCUI
CHEBI:176844 CHEBI
3JD PDB_CHEM_ID
CHEMBL1094636 ChEMBL_ID
24958200 PUBCHEM_CID
DB11793 DRUGBANK_ID
D10140 KEGG_DRUG
CHEMBL3989922 ChEMBL_ID
9526 INN_ID
C545685 MESH_SUPPLEMENTAL_RECORD_UI
8275 IUPHAR_LIGAND_ID
1193870006 SNOMEDCT_US
391000220105 SNOMEDCT_US
733733005 SNOMEDCT_US
763561009 SNOMEDCT_US
254987 MMSL
32539 MMSL
d08539 MMSL
017145 NDDF
017146 NDDF
1918231 RXNORM
HMC2H89N35 INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
ZEJULA HUMAN PRESCRIPTION DRUG LABEL 1 0173-0909 TABLET, FILM COATED 100 mg ORAL NDA 27 sections
ZEJULA HUMAN PRESCRIPTION DRUG LABEL 1 0173-0912 TABLET, FILM COATED 200 mg ORAL NDA 27 sections
ZEJULA HUMAN PRESCRIPTION DRUG LABEL 1 0173-0915 TABLET, FILM COATED 300 mg ORAL NDA 27 sections
AKEEGA HUMAN PRESCRIPTION DRUG LABEL 2 57894-050 TABLET, FILM COATED 50 mg ORAL NDA 33 sections
AKEEGA HUMAN PRESCRIPTION DRUG LABEL 2 57894-100 TABLET, FILM COATED 100 mg ORAL NDA 33 sections