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

Stem definitionDrug idCAS RN
poly-ADP-ribose polymerase inhibitors 5203 283173-50-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • rucaparib
  • rucaparib camsylate
  • AG-14447
  • rucaparib phosphate
  • AG-14699
  • AG014699
  • PF01367338
  • PF-1367338-BW
  • CO-338
  • rubraca
  • rucaparib camphorsulfonate
Rucaparib is an inhibitor of poly (ADP-ribose) polymerase (PARP) enzymes, including PARP-1, PARP-2, and PARP-3, which play a role in DNA repair. In vitro studies have shown that rucaparib-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 rucaparib-induced cytotoxicity was observed in tumor cell lines with deficiencies in BRCA1/2 and other DNA repair genes. Rucaparib has been shown to decrease tumor growth in mouse xenograft models of human cancer with or without deficiencies in BRCA.
  • Molecular weight: 323.37
  • Formula: C19H18FN3O
  • CLOGP: 3.01
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 3
  • TPSA: 56.92
  • ALOGS: -4.45
  • ROTB: 3
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
1.20 g O

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 3.28 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 4.31 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 16.60 hours Lombardo F, Berellini G, Obach RS
S (Water solubility) 1 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 1.106 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 19.275 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 1.977 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 6.442 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 25.610 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 47.180 % High 1
herg hERG pIC50 4.843 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 1.119 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 4.093 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 30.730 % High 1
kinase-safety-class AAK1,ABL2,ACVR2A,ACVR2B,ACVRL1,AKT2,AKT3,ALK,AURKA,AURKB,AURKC,AXL,BLK,BMX,BRAF,BTK,CAMK1,CAMK2A,CAMK2B,CAMK2D,CAMK2G,CDK1,CDK14,CDK16,CDK19,CDK2,CDK3,CDK4,CDK5,CDK6,CDK7,CDK9,CHEK1,CHEK2,CHUK,CLK2,CLK4,CSF1R,CSK,DDR1,DYRK1A,DYRK1B,DYRK2,EGFR,EIF2AK3,EPHA2,EPHB1,EPHB4,ERBB2,FGFR1,FLT1,FLT3,FLT4,FYN,GAK,GRK1,GRK2,GSK3A,GSK3B,HASPIN,HIPK2,IGF1R,IKBKB,INSR,IRAK1,IRAK3,IRAK4,ITK,JAK1,JAK2,JAK3,KDR,KIT,LCK,LRRK2,LYN,MAP2K1,MAP2K6,MAP3K1,MAP3K10,MAP3K11,MAP3K14,MAP3K19,MAP3K2,MAP3K21,MAP3K3,MAP3K7,MAP3K9,MAP4K1,MAP4K2,MAP4K3,MAP4K5,MAPK1,MAPK10,MAPK15,MAPK7,MAPK8,MAPK9,MARK1,MARK2,MARK3,MARK4,MELK,MET,MINK1,MKNK2,MST1R,MTOR,NTRK1,NTRK2,NTRK3,NUAK1,PAK1,PAK2,PAK4,PAK5,PDGFRB,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PIM1,PIM2,PIM3,PLK4,PRKAA1,PRKAA2,PRKACA,PRKCA,PRKCD,PRKCZ,PRKD1,PRKDC,PTK2,RET,ROCK1,ROCK2,RPS6KA1,SGK1,SIK2,SIK3,SRC,STK10,STK16,STK17A,STK3,STK33,STK4,SYK,TBK1,TEK,TGFBR1,TNIK,TNK1,TTK,TYRO3,UHMK1,ULK1,ULK2,YES1,ZAP70 165
kinase-selectivity-class AAK1,ACVR2A,ACVR2B,AKT2,ALK,AURKA,AURKB,AURKC,AXL,BLK,BRAF,CAMK2A,CAMK2B,CAMK2D,CDK1,CDK16,CDK2,CDK3,CDK4,CDK6,CDK7,CDK9,CHEK1,CLK2,CLK4,CSF1R,CSK,DDR1,DYRK1A,DYRK1B,DYRK3,EGFR,EIF2AK3,EPHA2,EPHB4,ERBB2,FGFR1,FLT3,FLT4,FYN,GAK,GSK3A,GSK3B,HIPK2,IGF1R,INSR,IRAK1,IRAK3,IRAK4,JAK1,JAK2,KDR,LCK,LRRK2,MAP2K6,MAP3K10,MAP3K11,MAP3K21,MAP3K7,MAP3K9,MAP4K1,MAP4K3,MAP4K5,MAPK1,MAPK12,MAPK7,MARK1,MARK2,MARK3,MARK4,MELK,MET,MINK1,MST1R,NTRK1,NTRK3,NUAK1,PAK4,PDGFRB,PDK1,PDPK1,PIM3,PRKAA1,PRKAA2,PRKACA,PRKCD,PRKCZ,PTK2,RET,ROCK1,ROCK2,SGK1,SIK2,SIK3,SRC,STK10,STK16,STK17A,STK33,STK4,SYK,TEK,TNIK,TTK,TYRO3,ULK1,ULK2,YES1 108
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 12.246 High 1
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 11.482 High 1
mh-clint Mouse hepatocyte intrinsic clearance 20.512 High 1
mppb Mouse plasma protein binding (% unbound) 23.820 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 14.962 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 49.770 % High 1
rat-kpuu-brain Rat brain Kpuu 0.028 % High 1
rh-clint Rat hepatocyte intrinsic clearance 11.588 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 61.420 % High 1
rppb Rat plasma protein binding (% unbound) 34.110 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 704.693 uM High 1

Approvals:

DateAgencyCompanyOrphan
May 24, 2018 EMA Clovis Oncology UK Limited
Dec. 19, 2016 FDA Clovis Oncology, 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
Malignant neoplasm progression 1792.62 35.53 734 20205 106136 90501372
Carbohydrate antigen 125 increased 1607.05 35.53 318 20621 2948 90604560
Fatigue 1395.22 35.53 1500 19439 1152523 89454985
Nausea 1297.98 35.53 1419 19520 1108897 89498611
Dysgeusia 964.69 35.53 386 20553 52174 90555334
Product dose omission issue 777.25 35.53 596 20343 291091 90316417
Tumour marker increased 554.66 35.53 149 20790 5658 90601850
Constipation 463.38 35.53 436 20503 279959 90327549
Adverse event 409.30 35.53 283 20656 117135 90490373
Decreased appetite 408.26 35.53 467 20472 376073 90231435
Platelet count decreased 403.61 35.53 298 20641 136671 90470837
Underdose 316.22 35.53 181 20758 53836 90553672
Accidental underdose 307.40 35.53 67 20872 1024 90606484
Ovarian cancer recurrent 282.28 35.53 67 20872 1523 90605985
Full blood count abnormal 256.21 35.53 138 20801 36459 90571049
Photosensitivity reaction 223.41 35.53 100 20839 17707 90589801
Taste disorder 213.35 35.53 148 20791 61398 90546110
Red blood cell count decreased 208.09 35.53 131 20808 46220 90561288
Anaemia 197.75 35.53 318 20621 352484 90255024
Blood creatinine increased 173.23 35.53 161 20778 101225 90506283
Sunburn 164.68 35.53 51 20888 3216 90604292
Haemoglobin decreased 163.27 35.53 194 20745 161762 90445746
Asthenia 161.32 35.53 370 20569 533381 90074127
Vomiting 160.67 35.53 471 20468 787822 89819686
Renal function test abnormal 142.72 35.53 56 20883 7135 90600373
Prescribed underdose 133.67 35.53 122 20817 74897 90532611
Condition aggravated 119.87 35.53 4 20935 595541 90011967
White blood cell count decreased 112.19 35.53 164 20775 166945 90440563
Blood magnesium decreased 112.08 35.53 60 20879 15633 90591875
Drug ineffective 102.41 35.53 102 20837 1384196 89223312
Abdominal pain 95.55 35.53 252 20687 395469 90212039
Abdominal distension 94.71 35.53 133 20806 130468 90477040
Neuropathy peripheral 94.20 35.53 136 20803 136834 90470674
Diarrhoea 89.24 35.53 440 20499 938750 89668758
Flatulence 89.17 35.53 75 20864 41292 90566216
Therapy partial responder 88.25 35.53 58 20881 21985 90585523
Abdominal pain upper 84.51 35.53 216 20723 332458 90275050
Laboratory test abnormal 84.33 35.53 73 20866 41781 90565727
Drug hypersensitivity 84.07 35.53 6 20933 463603 90143905
Intentional underdose 78.64 35.53 26 20913 2023 90605485
Liver function test increased 63.85 35.53 88 20851 84767 90522741
Swelling 62.07 35.53 11 20928 419047 90188461
Arthropathy 55.59 35.53 9 20930 366233 90241275
Early satiety 54.59 35.53 18 20921 1389 90606119
General physical health deterioration 53.28 35.53 9 20930 355106 90252402
Joint swelling 53.05 35.53 25 20914 503275 90104233
Dehydration 52.17 35.53 129 20810 194318 90413190
Intestinal obstruction 50.33 35.53 52 20887 37079 90570429
Drug interaction 48.88 35.53 4 20935 276449 90331059
Discomfort 48.42 35.53 4 20935 274331 90333177
Lower respiratory tract infection 46.10 35.53 3 20936 250656 90356852
Pneumonia 44.68 35.53 49 20890 638010 89969498
Glossodynia 44.38 35.53 10 20929 321769 90285739
Wheezing 43.35 35.53 3 20936 238077 90369431
Small intestinal obstruction 42.69 35.53 37 20902 21197 90586311
Confusional state 42.54 35.53 18 20921 386187 90221321
Urticaria 40.64 35.53 11 20928 312723 90294785
Mobility decreased 38.39 35.53 6 20933 250728 90356780
Thrombocytopenia 36.83 35.53 119 20820 208606 90398902
Asthma 36.61 35.53 6 20933 242154 90365354
Aspartate aminotransferase increased 36.14 35.53 76 20863 102861 90504647
Type 2 diabetes mellitus 35.75 35.53 3 20936 203241 90404267
Musculoskeletal stiffness 35.68 35.53 12 20927 296520 90310988
Hypertension 35.60 35.53 32 20907 457500 90150008

FDA Adverse Event Reporting System (Male)

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
Malignant neoplasm progression 56.10 39.02 26 441 108374 42512494

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
Fatigue 972.22 34.79 932 12241 1215026 109361100
Carbohydrate antigen 125 increased 970.96 34.79 180 12993 2367 110573759
Nausea 814.23 34.79 854 12319 1234836 109341290
Dysgeusia 634.81 34.79 257 12916 69728 110506398
Malignant neoplasm progression 516.46 34.79 297 12876 174270 110401856
Product dose omission issue 477.37 34.79 355 12818 321427 110254699
Tumour marker increased 437.84 34.79 105 13068 4955 110571171
Constipation 314.95 34.79 292 12881 357494 110218632
Decreased appetite 277.59 34.79 311 12862 475535 110100591
Underdose 253.49 34.79 132 13041 63422 110512704
Accidental underdose 250.52 34.79 52 13121 1253 110574873
Platelet count decreased 177.46 34.79 175 12998 230268 110345858
Prescribed underdose 153.49 34.79 96 13077 65078 110511048
Ovarian cancer recurrent 148.13 34.79 30 13143 637 110575489
Adverse event 134.29 34.79 108 13065 108701 110467425
Red blood cell count decreased 130.33 34.79 87 13086 65836 110510290
Vomiting 129.84 34.79 314 12859 910361 109665765
Taste disorder 121.40 34.79 83 13090 65304 110510822
Full blood count abnormal 120.60 34.79 78 13095 55974 110520152
Anaemia 117.46 34.79 223 12950 546863 110029263
Photosensitivity reaction 116.03 34.79 58 13115 25531 110550595
Sunburn 107.32 34.79 34 13139 4514 110571612
Asthenia 101.65 34.79 241 12932 688758 109887368
Haemoglobin decreased 96.75 34.79 133 13040 248594 110327532
Renal function test abnormal 91.83 34.79 36 13137 8910 110567216
Blood magnesium decreased 86.77 34.79 44 13129 19952 110556174
Diarrhoea 79.60 34.79 306 12867 1139199 109436927
Abdominal pain upper 71.90 34.79 140 13033 348971 110227155
Abdominal pain 70.73 34.79 175 12998 512814 110063312
Condition aggravated 68.48 34.79 5 13168 734831 109841295
White blood cell count decreased 63.90 34.79 105 13068 229285 110346841
Blood creatinine increased 61.06 34.79 91 13082 182798 110393328
Liver function test increased 54.95 34.79 60 13113 88488 110487638
Flatulence 54.39 34.79 47 13126 52102 110524024
Abdominal distension 54.03 34.79 84 13089 175019 110401107
Intentional underdose 51.72 34.79 17 13156 2535 110573591
Neuropathy peripheral 49.82 34.79 82 13091 179195 110396931
Drug interaction 47.74 34.79 3 13170 500180 110075946
Drug ineffective 46.02 34.79 69 13104 1520471 109055655
Drug hypersensitivity 42.51 34.79 3 13170 454087 110122039
Dehydration 42.34 34.79 99 13074 279412 110296714
Laboratory test abnormal 40.54 34.79 37 13136 44042 110532084
Intestinal obstruction 40.06 34.79 40 13133 53187 110522939
Abdominal discomfort 39.82 34.79 120 13053 393738 110182388
Small intestinal obstruction 39.74 34.79 32 13141 32181 110543945

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01XK03 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:22587 antiviral agent
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

Related Drugs by ATC class:

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

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

DiseaseRelationSNOMED_IDDOID
Malignant tumor of ovary indication 363443007 DOID:2394




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 11.08 acidic
pKa2 13.73 acidic
pKa3 9.45 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 200MG BASE RUBRACA PHARMAAND N209115 Dec. 19, 2016 RX TABLET ORAL 8071579 Aug. 12, 2027 A METHOD FOR TREATING EPITHELIAL OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 200MG BASE RUBRACA PHARMAAND N209115 Dec. 19, 2016 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
EQ 200MG BASE RUBRACA PHARMAAND N209115 Dec. 19, 2016 RX TABLET ORAL 8071579 Aug. 12, 2027 A METHOD FOR TREATING OVARIAN CANCER BY ADMINISTERING RUCAPARIB, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 200MG BASE RUBRACA PHARMAAND N209115 Dec. 19, 2016 RX TABLET ORAL 8143241 Aug. 12, 2027 A METHOD FOR TREATING EPITHELIAL OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 200MG BASE RUBRACA PHARMAAND N209115 Dec. 19, 2016 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
EQ 200MG BASE RUBRACA PHARMAAND N209115 Dec. 19, 2016 RX TABLET ORAL 8143241 Aug. 12, 2027 A METHOD FOR TREATING OVARIAN CANCER BY ADMINISTERING RUCAPARIB, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 250MG BASE RUBRACA PHARMAAND N209115 May 1, 2017 RX TABLET ORAL 8071579 Aug. 12, 2027 A METHOD FOR TREATING EPITHELIAL OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 250MG BASE RUBRACA PHARMAAND N209115 May 1, 2017 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
EQ 250MG BASE RUBRACA PHARMAAND N209115 May 1, 2017 RX TABLET ORAL 8071579 Aug. 12, 2027 A METHOD FOR TREATING OVARIAN CANCER BY ADMINISTERING RUCAPARIB, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 250MG BASE RUBRACA PHARMAAND N209115 May 1, 2017 RX TABLET ORAL 8143241 Aug. 12, 2027 A METHOD FOR TREATING EPITHELIAL OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 250MG BASE RUBRACA PHARMAAND N209115 May 1, 2017 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
EQ 250MG BASE RUBRACA PHARMAAND N209115 May 1, 2017 RX TABLET ORAL 8143241 Aug. 12, 2027 A METHOD FOR TREATING OVARIAN CANCER BY ADMINISTERING RUCAPARIB, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 300MG BASE RUBRACA PHARMAAND N209115 Dec. 19, 2016 RX TABLET ORAL 8071579 Aug. 12, 2027 A METHOD FOR TREATING EPITHELIAL OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 300MG BASE RUBRACA PHARMAAND N209115 Dec. 19, 2016 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
EQ 300MG BASE RUBRACA PHARMAAND N209115 Dec. 19, 2016 RX TABLET ORAL 8071579 Aug. 12, 2027 A METHOD FOR TREATING OVARIAN CANCER BY ADMINISTERING RUCAPARIB, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 300MG BASE RUBRACA PHARMAAND N209115 Dec. 19, 2016 RX TABLET ORAL 8143241 Aug. 12, 2027 A METHOD FOR TREATING EPITHELIAL OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 300MG BASE RUBRACA PHARMAAND N209115 Dec. 19, 2016 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
EQ 300MG BASE RUBRACA PHARMAAND N209115 Dec. 19, 2016 RX TABLET ORAL 8143241 Aug. 12, 2027 A METHOD FOR TREATING OVARIAN CANCER BY ADMINISTERING RUCAPARIB, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 200MG BASE RUBRACA PHARMAAND N209115 Dec. 19, 2016 RX TABLET ORAL 9861638 Feb. 10, 2031 A METHOD FOR TREATING EPITHELIAL OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 200MG BASE RUBRACA PHARMAAND N209115 Dec. 19, 2016 RX TABLET ORAL 9861638 Feb. 10, 2031 A METHOD FOR TREATING OVARIAN CANCER BY ADMINISTERING RUCAPARIB, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 250MG BASE RUBRACA PHARMAAND N209115 May 1, 2017 RX TABLET ORAL 9861638 Feb. 10, 2031 A METHOD FOR TREATING EPITHELIAL OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 250MG BASE RUBRACA PHARMAAND N209115 May 1, 2017 RX TABLET ORAL 9861638 Feb. 10, 2031 A METHOD FOR TREATING OVARIAN CANCER BY ADMINISTERING RUCAPARIB, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 300MG BASE RUBRACA PHARMAAND N209115 Dec. 19, 2016 RX TABLET ORAL 9861638 Feb. 10, 2031 A METHOD FOR TREATING EPITHELIAL OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 300MG BASE RUBRACA PHARMAAND N209115 Dec. 19, 2016 RX TABLET ORAL 9861638 Feb. 10, 2031 A METHOD FOR TREATING OVARIAN CANCER BY ADMINISTERING RUCAPARIB, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 200MG BASE RUBRACA PHARMAAND N209115 Dec. 19, 2016 RX TABLET ORAL 8859562 Aug. 4, 2031 A METHOD FOR TREATING EPITHELIAL OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 200MG BASE RUBRACA PHARMAAND N209115 Dec. 19, 2016 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
EQ 200MG BASE RUBRACA PHARMAAND N209115 Dec. 19, 2016 RX TABLET ORAL 8859562 Aug. 4, 2031 A METHOD FOR TREATING OVARIAN CANCER BY ADMINISTERING RUCAPARIB, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 250MG BASE RUBRACA PHARMAAND N209115 May 1, 2017 RX TABLET ORAL 8859562 Aug. 4, 2031 A METHOD FOR TREATING EPITHELIAL OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 250MG BASE RUBRACA PHARMAAND N209115 May 1, 2017 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
EQ 250MG BASE RUBRACA PHARMAAND N209115 May 1, 2017 RX TABLET ORAL 8859562 Aug. 4, 2031 A METHOD FOR TREATING OVARIAN CANCER BY ADMINISTERING RUCAPARIB, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 300MG BASE RUBRACA PHARMAAND N209115 Dec. 19, 2016 RX TABLET ORAL 8859562 Aug. 4, 2031 A METHOD FOR TREATING EPITHELIAL OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 300MG BASE RUBRACA PHARMAAND N209115 Dec. 19, 2016 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
EQ 300MG BASE RUBRACA PHARMAAND N209115 Dec. 19, 2016 RX TABLET ORAL 8859562 Aug. 4, 2031 A METHOD FOR TREATING OVARIAN CANCER BY ADMINISTERING RUCAPARIB, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 200MG BASE RUBRACA PHARMAAND N209115 Dec. 19, 2016 RX TABLET ORAL 10130636 Aug. 17, 2035 A METHOD FOR TREATING EPITHELIAL OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 200MG BASE RUBRACA PHARMAAND N209115 Dec. 19, 2016 RX TABLET ORAL 10130636 Aug. 17, 2035 A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
EQ 200MG BASE RUBRACA PHARMAAND N209115 Dec. 19, 2016 RX TABLET ORAL 10130636 Aug. 17, 2035 A METHOD FOR TREATING OVARIAN CANCER BY ADMINISTERING RUCAPARIB, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 200MG BASE RUBRACA PHARMAAND N209115 Dec. 19, 2016 RX TABLET ORAL 10130636 Aug. 17, 2035 MAINTENANCE TREATMENT OF RECURRENT EPITHELIAL OVARIAN, FALLOPIAN TUBE OR PRIMARY PERITONEAL CANCER, WHO ARE IN A COMPLETE OR PARTIAL RESPONSE TO PLATINUM-BASED CHEMOTHERAPY
EQ 250MG BASE RUBRACA PHARMAAND N209115 May 1, 2017 RX TABLET ORAL 10130636 Aug. 17, 2035 A METHOD FOR TREATING EPITHELIAL OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 250MG BASE RUBRACA PHARMAAND N209115 May 1, 2017 RX TABLET ORAL 10130636 Aug. 17, 2035 A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
EQ 250MG BASE RUBRACA PHARMAAND N209115 May 1, 2017 RX TABLET ORAL 10130636 Aug. 17, 2035 A METHOD FOR TREATING OVARIAN CANCER BY ADMINISTERING RUCAPARIB, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 250MG BASE RUBRACA PHARMAAND N209115 May 1, 2017 RX TABLET ORAL 10130636 Aug. 17, 2035 MAINTENANCE TREATMENT OF RECURRENT EPITHELIAL OVARIAN, FALLOPIAN TUBE OR PRIMARY PERITONEAL CANCER, WHO ARE IN A COMPLETE OR PARTIAL RESPONSE TO PLATINUM-BASED CHEMOTHERAPY
EQ 300MG BASE RUBRACA PHARMAAND N209115 Dec. 19, 2016 RX TABLET ORAL 10130636 Aug. 17, 2035 A METHOD FOR TREATING EPITHELIAL OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 300MG BASE RUBRACA PHARMAAND N209115 Dec. 19, 2016 RX TABLET ORAL 10130636 Aug. 17, 2035 A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
EQ 300MG BASE RUBRACA PHARMAAND N209115 Dec. 19, 2016 RX TABLET ORAL 10130636 Aug. 17, 2035 A METHOD FOR TREATING OVARIAN CANCER BY ADMINISTERING RUCAPARIB, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 300MG BASE RUBRACA PHARMAAND N209115 Dec. 19, 2016 RX TABLET ORAL 10130636 Aug. 17, 2035 MAINTENANCE TREATMENT OF RECURRENT EPITHELIAL OVARIAN, FALLOPIAN TUBE OR PRIMARY PERITONEAL CANCER, WHO ARE IN A COMPLETE OR PARTIAL RESPONSE TO PLATINUM-BASED CHEMOTHERAPY

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 200MG BASE RUBRACA PHARMAAND N209115 Dec. 19, 2016 RX TABLET ORAL Dec. 17, 2028 EXPANSION TO THE TREATMENT OF ADULT PATIENTS WITH A DELETERIOUS BRCA MUTATION (GERMLINE AND/OR SOMATIC)-ASSOCIATED METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC) INDICATION
EQ 250MG BASE RUBRACA PHARMAAND N209115 May 1, 2017 RX TABLET ORAL Dec. 17, 2028 EXPANSION TO THE TREATMENT OF ADULT PATIENTS WITH A DELETERIOUS BRCA MUTATION (GERMLINE AND/OR SOMATIC)-ASSOCIATED METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC) INDICATION
EQ 300MG BASE RUBRACA PHARMAAND N209115 Dec. 19, 2016 RX TABLET ORAL Dec. 17, 2028 EXPANSION TO THE TREATMENT OF ADULT PATIENTS WITH A DELETERIOUS BRCA MUTATION (GERMLINE AND/OR SOMATIC)-ASSOCIATED METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC) INDICATION

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Poly [ADP-ribose] polymerase 2 Enzyme INHIBITOR IC50 7.55 SCIENTIFIC LITERATURE DRUG LABEL
Poly [ADP-ribose] polymerase 1 Enzyme INHIBITOR IC50 8.50 SCIENTIFIC LITERATURE DRUG LABEL
Poly [ADP-ribose] polymerase 3 Enzyme INHIBITOR IC50 6.39 SCIENTIFIC LITERATURE DRUG LABEL
Serine/threonine-protein kinase pim-3 Kinase IC50 6.36 CHEMBL
Dual specificity tyrosine-phosphorylation-regulated kinase 1A Kinase IC50 5.63 CHEMBL
Mono [ADP-ribose] polymerase PARP16 Enzyme Kd 5.54 CHEMBL
Poly [ADP-ribose] polymerase 9 Enzyme Kd 5.51 CHEMBL
Tankyrase-2 Enzyme INHIBITOR IC50 6.05 SCIENTIFIC LITERATURE
DNA polymerase alpha catalytic subunit Enzyme IC50 9.40 CHEMBL
Poly [ADP-ribose] polymerase 4 Enzyme INHIBITOR IC50 6.08 SCIENTIFIC LITERATURE
Poly [ADP-ribose] polymerase 10 Enzyme INHIBITOR IC50 6.25 SCIENTIFIC LITERATURE
Poly [ADP-ribose] polymerase 12 Enzyme INHIBITOR IC50 5.18 SCIENTIFIC LITERATURE
Poly [ADP-ribose] polymerase 14 Enzyme INHIBITOR IC50 5.05 SCIENTIFIC LITERATURE
Poly [ADP-ribose] polymerase 15 Enzyme INHIBITOR IC50 4.49 SCIENTIFIC LITERATURE
Tankyrase-1 Enzyme INHIBITOR IC50 6.84 SCIENTIFIC LITERATURE
Cyclin-dependent kinase 16 Kinase IC50 6.42 CHEMBL
Dual specificity tyrosine-phosphorylation-regulated kinase 1B Kinase IC50 6.13 CHEMBL

External reference:

IDSource
8237F3U7EH UNII
1859053-21-6 SECONDARY_CAS_RN
459868-92-9 SECONDARY_CAS_RN
4036311 VANDF
C3661315 UMLSCUI
CHEBI:134689 CHEBI
RPB PDB_CHEM_ID
CHEMBL1173055 ChEMBL_ID
9931954 PUBCHEM_CID
DB12332 DRUGBANK_ID
D10079 KEGG_DRUG
CHEMBL3833368 ChEMBL_ID
CHEMBL2105733 ChEMBL_ID
9471 INN_ID
C531549 MESH_SUPPLEMENTAL_RECORD_UI
7736 IUPHAR_LIGAND_ID
C520469 MESH_SUPPLEMENTAL_RECORD_UI
1217204001 SNOMEDCT_US
723984009 SNOMEDCT_US
763539004 SNOMEDCT_US
247942 MMSL
32185 MMSL
d08507 MMSL
017056 NDDF
017057 NDDF
1862578 RXNORM

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Rubraca HUMAN PRESCRIPTION DRUG LABEL 1 82154-0783 TABLET, FILM COATED 200 mg ORAL NDA 30 sections
Rubraca HUMAN PRESCRIPTION DRUG LABEL 1 82154-0784 TABLET, FILM COATED 250 mg ORAL NDA 30 sections
Rubraca HUMAN PRESCRIPTION DRUG LABEL 1 82154-0785 TABLET, FILM COATED 300 mg ORAL NDA 30 sections