niraparib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| poly-ADP-ribose polymerase inhibitors | 5222 | 1038915-60-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| 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 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Nov. 16, 2017 | EMA | Tesaro UK Limited | |
| March 27, 2017 | FDA | TESARO INC | |
| Sept. 25, 2020 | PMDA | TAKEDA PHARMACEUTICAL COMPANY LIMITED |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Platelet count decreased | 990.46 | 26.91 | 478 | 12460 | 115644 | 63360440 |
| Carbohydrate antigen 125 increased | 647.47 | 26.91 | 143 | 12795 | 2673 | 63473411 |
| Recurrent cancer | 581.09 | 26.91 | 123 | 12815 | 1864 | 63474220 |
| Disease progression | 493.40 | 26.91 | 308 | 12630 | 122450 | 63353634 |
| Malignant neoplasm progression | 401.82 | 26.91 | 234 | 12704 | 81887 | 63394197 |
| Constipation | 358.48 | 26.91 | 324 | 12614 | 224619 | 63251465 |
| Thrombocytopenia | 346.96 | 26.91 | 269 | 12669 | 150888 | 63325196 |
| Intentional underdose | 243.68 | 26.91 | 60 | 12878 | 1822 | 63474262 |
| Nausea | 224.40 | 26.91 | 517 | 12421 | 853954 | 62622130 |
| Insomnia | 186.37 | 26.91 | 224 | 12714 | 215028 | 63261056 |
| Blood pressure increased | 178.20 | 26.91 | 191 | 12747 | 161871 | 63314213 |
| Haemoglobin decreased | 164.38 | 26.91 | 174 | 12764 | 145311 | 63330773 |
| Red blood cell count decreased | 162.72 | 26.91 | 102 | 12836 | 40543 | 63435541 |
| Renal impairment | 153.49 | 26.91 | 134 | 12804 | 88221 | 63387863 |
| Heart rate increased | 121.33 | 26.91 | 121 | 12817 | 94117 | 63381967 |
| Fatigue | 121.17 | 26.91 | 425 | 12513 | 887603 | 62588481 |
| Ovarian cancer recurrent | 119.49 | 26.91 | 30 | 12908 | 987 | 63475097 |
| Myelodysplastic syndrome | 118.40 | 26.91 | 61 | 12877 | 16693 | 63459391 |
| Decreased activity | 116.28 | 26.91 | 45 | 12893 | 6275 | 63469809 |
| Anaemia | 113.21 | 26.91 | 209 | 12729 | 293221 | 63182863 |
| Tumour marker increased | 97.60 | 26.91 | 37 | 12901 | 4878 | 63471206 |
| Neutrophil count decreased | 88.84 | 26.91 | 81 | 12857 | 56325 | 63419759 |
| White blood cell count decreased | 83.28 | 26.91 | 121 | 12817 | 138983 | 63337101 |
| Product dose omission issue | 80.50 | 26.91 | 159 | 12779 | 234154 | 63241930 |
| Full blood count abnormal | 80.27 | 26.91 | 60 | 12878 | 31657 | 63444427 |
| Product dose omission in error | 75.67 | 26.91 | 35 | 12903 | 7577 | 63468507 |
| Dry mouth | 75.41 | 26.91 | 86 | 12852 | 77777 | 63398307 |
| Ovarian cancer | 70.60 | 26.91 | 31 | 12907 | 5945 | 63470139 |
| Acute myeloid leukaemia | 65.99 | 26.91 | 42 | 12896 | 17105 | 63458979 |
| Decreased appetite | 63.98 | 26.91 | 151 | 12787 | 250901 | 63225183 |
| Blood creatinine increased | 59.33 | 26.91 | 81 | 12857 | 87763 | 63388321 |
| Intestinal obstruction | 49.85 | 26.91 | 45 | 12893 | 30854 | 63445230 |
| Haematocrit decreased | 49.61 | 26.91 | 50 | 12888 | 39290 | 63436794 |
| Neuropathy peripheral | 47.52 | 26.91 | 84 | 12854 | 113583 | 63362501 |
| Drug monitoring procedure not performed | 47.41 | 26.91 | 13 | 12925 | 605 | 63475479 |
| Full blood count decreased | 46.17 | 26.91 | 40 | 12898 | 25984 | 63450100 |
| Platelet count abnormal | 41.52 | 26.91 | 18 | 12920 | 3346 | 63472738 |
| Drug hypersensitivity | 41.02 | 26.91 | 7 | 12931 | 310680 | 63165404 |
| Emotional distress | 40.36 | 26.91 | 41 | 12897 | 32508 | 63443576 |
| Swelling | 36.80 | 26.91 | 6 | 12932 | 275372 | 63200712 |
| Photosensitivity reaction | 34.91 | 26.91 | 27 | 12911 | 14967 | 63461117 |
| Metastases to peritoneum | 34.75 | 26.91 | 16 | 12922 | 3426 | 63472658 |
| Lymphangioleiomyomatosis | 34.61 | 26.91 | 8 | 12930 | 184 | 63475900 |
| Computerised tomogram abnormal | 34.53 | 26.91 | 14 | 12924 | 2203 | 63473881 |
| Arthropathy | 33.99 | 26.91 | 4 | 12934 | 234788 | 63241296 |
| Hypertension | 33.67 | 26.91 | 129 | 12809 | 279174 | 63196910 |
| Adverse drug reaction | 33.41 | 26.91 | 59 | 12879 | 79655 | 63396429 |
| Blood test abnormal | 31.80 | 26.91 | 26 | 12912 | 15603 | 63460481 |
| Joint swelling | 31.01 | 26.91 | 14 | 12924 | 327652 | 63148432 |
| Eastern Cooperative Oncology Group performance status worsened | 30.65 | 26.91 | 11 | 12927 | 1243 | 63474841 |
| Treatment failure | 29.80 | 26.91 | 3 | 12935 | 199040 | 63277044 |
| Blood magnesium decreased | 29.07 | 26.91 | 23 | 12915 | 13175 | 63462909 |
| Ileus | 28.92 | 26.91 | 24 | 12914 | 14701 | 63461383 |
| Myelosuppression | 27.83 | 26.91 | 29 | 12909 | 23674 | 63452410 |
| Headache | 27.82 | 26.91 | 222 | 12716 | 633019 | 62843065 |
| Hypersensitivity | 26.92 | 26.91 | 13 | 12925 | 292672 | 63183412 |
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Platelet count decreased | 592.58 | 25.44 | 336 | 9107 | 194328 | 79540617 |
| Recurrent cancer | 516.21 | 25.44 | 107 | 9336 | 2586 | 79732359 |
| Carbohydrate antigen 125 increased | 484.63 | 25.44 | 98 | 9345 | 2086 | 79732859 |
| Disease progression | 384.15 | 25.44 | 250 | 9193 | 184112 | 79550833 |
| Thrombocytopenia | 257.42 | 25.44 | 228 | 9215 | 265031 | 79469914 |
| Constipation | 227.42 | 25.44 | 219 | 9224 | 282831 | 79452114 |
| Intentional underdose | 204.70 | 25.44 | 49 | 9394 | 2305 | 79732640 |
| Nausea | 177.42 | 25.44 | 364 | 9079 | 956832 | 78778113 |
| Blood pressure increased | 113.13 | 25.44 | 132 | 9311 | 211228 | 79523717 |
| Insomnia | 106.79 | 25.44 | 138 | 9305 | 245032 | 79489913 |
| Ovarian cancer recurrent | 98.90 | 25.44 | 20 | 9423 | 424 | 79734521 |
| Anaemia | 97.17 | 25.44 | 182 | 9261 | 444833 | 79290112 |
| Renal impairment | 93.61 | 25.44 | 104 | 9339 | 157679 | 79577266 |
| Myelodysplastic syndrome | 93.43 | 25.44 | 53 | 9390 | 30248 | 79704697 |
| Haemoglobin decreased | 91.98 | 25.44 | 122 | 9321 | 221997 | 79512948 |
| Malignant neoplasm progression | 90.05 | 25.44 | 95 | 9348 | 135895 | 79599050 |
| Red blood cell count decreased | 88.63 | 25.44 | 65 | 9378 | 57448 | 79677497 |
| Ovarian cancer | 87.20 | 25.44 | 28 | 9415 | 3906 | 79731039 |
| Fatigue | 83.69 | 25.44 | 270 | 9173 | 929457 | 78805488 |
| Decreased activity | 79.05 | 25.44 | 32 | 9411 | 8662 | 79726283 |
| Neutrophil count decreased | 71.91 | 25.44 | 71 | 9372 | 93888 | 79641057 |
| Product dose omission in error | 65.13 | 25.44 | 27 | 9416 | 7761 | 79727184 |
| Acute myeloid leukaemia | 64.26 | 25.44 | 42 | 9401 | 30843 | 79704102 |
| White blood cell count decreased | 58.13 | 25.44 | 90 | 9353 | 188198 | 79546747 |
| Heart rate increased | 55.66 | 25.44 | 70 | 9373 | 120654 | 79614291 |
| Decreased appetite | 53.29 | 25.44 | 122 | 9321 | 342296 | 79392649 |
| Product dose omission issue | 52.30 | 25.44 | 100 | 9343 | 247437 | 79487508 |
| Tumour marker increased | 50.42 | 25.44 | 19 | 9424 | 4253 | 79730692 |
| Full blood count abnormal | 49.73 | 25.44 | 40 | 9403 | 40434 | 79694511 |
| Blood creatinine increased | 43.53 | 25.44 | 71 | 9372 | 154986 | 79579959 |
| Dry mouth | 38.91 | 25.44 | 50 | 9393 | 87969 | 79646976 |
| Intestinal obstruction | 35.68 | 25.44 | 34 | 9409 | 42986 | 79691959 |
| Neuropathy peripheral | 34.74 | 25.44 | 61 | 9382 | 141244 | 79593701 |
| Headache | 33.94 | 25.44 | 160 | 9283 | 653612 | 79081333 |
| Vomiting | 33.15 | 25.44 | 161 | 9282 | 665667 | 79069278 |
| Metastases to peritoneum | 32.69 | 25.44 | 14 | 9429 | 4358 | 79730587 |
| Full blood count decreased | 31.87 | 25.44 | 26 | 9417 | 26793 | 79708152 |
| Hypertension | 28.47 | 25.44 | 95 | 9348 | 330897 | 79404048 |
| Emotional distress | 28.33 | 25.44 | 29 | 9414 | 39940 | 79695005 |
| Lymphangioleiomyomatosis | 28.10 | 25.44 | 6 | 9437 | 167 | 79734778 |
| Haematocrit decreased | 27.35 | 25.44 | 35 | 9408 | 61277 | 79673668 |
| Computerised tomogram abnormal | 25.75 | 25.44 | 11 | 9432 | 3402 | 79731543 |
| Drug monitoring procedure not performed | 25.74 | 25.44 | 8 | 9435 | 1003 | 79733942 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | L01XK02 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS OTHER ANTINEOPLASTIC AGENTS Poly (ADP-ribose) polymerase (PARP) inhibitors |
| MeSH PA | D000970 | Antineoplastic Agents |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D000067856 | Poly(ADP-ribose) Polymerase Inhibitors |
| FDA MoA | N0000191622 | Poly(ADP-Ribose) Polymerase Inhibitors |
| FDA EPC | N0000191623 | Poly(ADP-Ribose) Polymerase Inhibitor |
| CHEBI has role | CHEBI:35610 | antineoplastic agents |
| CHEBI has role | CHEBI:62913 | PARP |
| CHEBI has role | CHEBI:68495 | Type I cell-death inducers |
| CHEBI has role | CHEBI:132992 | radiosensitizing agents |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| 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 level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 10.95 | acidic |
| pKa2 | 9.77 | Basic |
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| EQ 100MG BASE | ZEJULA | GLAXOSMITHKLINE | N208447 | March 27, 2017 | RX | 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 | RX | 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 |
| EQ 100MG BASE | ZEJULA | GLAXOSMITHKLINE | N208447 | March 27, 2017 | RX | 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 |
| EQ 100MG BASE | ZEJULA | GLAXOSMITHKLINE | N208447 | March 27, 2017 | RX | 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 | RX | 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 |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| EQ 100MG BASE | ZEJULA | GLAXOSMITHKLINE | N208447 | March 27, 2017 | RX | CAPSULE | ORAL | April 29, 2023 | MAINTENANCE TREATMENT OF ADULT PATIENTS WITH ADVANCED EPITHELIAL OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER WHO ARE IN A COMPLETE OR PARTIAL RESPONSE TO FIRST-LINE PLATINUM-BASED CHEMOTHERAPY |
| EQ 100MG BASE | ZEJULA | GLAXOSMITHKLINE | N208447 | March 27, 2017 | RX | CAPSULE | ORAL | March 27, 2024 | INDICATED FOR 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 |
| EQ 100MG BASE | ZEJULA | GLAXOSMITHKLINE | N208447 | March 27, 2017 | RX | 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 | RX | 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 |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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 | |||
| Poly [ADP-ribose] polymerase 3 | Enzyme | IC50 | 5.89 | CHEMBL | |||||
| Poly [ADP-ribose] polymerase 4 | Enzyme | IC50 | 6.48 | CHEMBL | |||||
| Poly [ADP-ribose] polymerase 10 | Enzyme | IC50 | 5.72 | CHEMBL | |||||
| Tankyrase-2 | Enzyme | IC50 | 5.29 | 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 12 | Enzyme | IC50 | 7.10 | CHEMBL | |||||
| Tankyrase-1 | Enzyme | IC50 | 6.24 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 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 |
| 8275 | IUPHAR_LIGAND_ID |
| 254987 | MMSL |
| 32539 | MMSL |
| d08539 | MMSL |
| 017145 | NDDF |
| 017146 | NDDF |
| 1193870006 | SNOMEDCT_US |
| 391000220105 | SNOMEDCT_US |
| 733733005 | SNOMEDCT_US |
| 763561009 | SNOMEDCT_US |
| 1918231 | RXNORM |
| C545685 | MESH_SUPPLEMENTAL_RECORD_UI |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| 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 | 32 sections |
| AKEEGA | HUMAN PRESCRIPTION DRUG LABEL | 2 | 57894-100 | TABLET, FILM COATED | 100 mg | ORAL | NDA | 32 sections |
| ZEJULA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69656-103 | CAPSULE | 100 mg | ORAL | NDA | 30 sections |
| ZEJULA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69656-103 | CAPSULE | 100 mg | ORAL | NDA | 30 sections |
| ZEJULA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69656-103 | CAPSULE | 100 mg | ORAL | NDA | 30 sections |
| ZEJULA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69656-103 | CAPSULE | 100 mg | ORAL | NDA | 30 sections |