rucaparib Indications/Contra | FAERs-F | FAERs-M | Orange Bk | 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:

None

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

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 1631.14 35.76 708 19786 70833 53257739
Carbohydrate antigen 125 increased 1475.88 35.76 310 20184 2258 53326314
Fatigue 1308.21 35.76 1486 19008 729020 52599552
Nausea 1139.73 35.76 1410 19084 754681 52573891
Dysgeusia 854.06 35.76 387 20107 42544 53286028
Product dose omission issue 716.08 35.76 589 19905 191031 53137541
Tumour marker increased 540.99 35.76 150 20344 3803 53324769
Adverse event 534.24 35.76 277 20217 40784 53287788
Taste disorder 433.48 35.76 149 20345 7819 53320753
Decreased appetite 426.57 35.76 466 20028 214508 53114064
Constipation 402.04 35.76 435 20059 197977 53130595
Underdose 386.59 35.76 181 20313 21341 53307231
Platelet count decreased 326.50 35.76 295 20199 107804 53220768
Accidental underdose 304.83 35.76 67 20427 615 53327957
Ovarian cancer recurrent 269.25 35.76 67 20427 1096 53327476
Blood count abnormal 263.77 35.76 137 20357 20178 53308394
Prescribed underdose 251.47 35.76 122 20372 15545 53313027
Photosensitivity reaction 202.00 35.76 101 20393 13727 53314845
Red blood cell count decreased 173.52 35.76 129 20365 35774 53292798
Renal function test abnormal 163.40 35.76 57 20437 3120 53325452
Sunburn 149.71 35.76 51 20443 2598 53325974
Vomiting 144.35 35.76 468 20026 496671 52831901
Asthenia 136.52 35.76 362 20132 343228 52985344
Blood creatinine increased 129.28 35.76 159 20335 82503 53246069
Therapy partial responder 126.77 35.76 57 20437 6106 53322466
Anaemia 124.82 35.76 306 20188 276412 53052160
Drug ineffective 115.28 35.76 88 20406 817157 52511415
Haemoglobin decreased 111.89 35.76 194 20300 137113 53191459
Liver function test increased 109.61 35.76 87 20407 26541 53302031
Abdominal pain upper 109.15 35.76 214 20280 166077 53162495
Blood magnesium decreased 104.72 35.76 62 20432 11752 53316820
Condition aggravated 100.53 35.76 3 20491 297131 53031441
Abdominal distension 94.59 35.76 134 20360 79656 53248916
Laboratory test abnormal 86.29 35.76 73 20421 24336 53304236
White blood cell count decreased 85.04 35.76 163 20331 124312 53204260
Drug hypersensitivity 82.05 35.76 5 20489 265237 53063335
Abdominal pain 80.34 35.76 248 20246 255655 53072917
Flatulence 75.81 35.76 76 20418 31441 53297131
Neuropathy peripheral 70.30 35.76 135 20359 103052 53225520
Intentional underdose 66.72 35.76 26 20468 1945 53326627
Diarrhoea 63.19 35.76 433 20061 625113 52703459
Dyspepsia 60.99 35.76 108 20386 77492 53251080
Early satiety 54.80 35.76 18 20476 818 53327754
Pneumonia 54.42 35.76 46 20448 407123 52921449
Abdominal discomfort 47.39 35.76 189 20305 220873 53107699
Fall 46.05 35.76 42 20452 358398 52970174
Swelling 39.77 35.76 12 20482 191093 53137479
Intestinal obstruction 38.12 35.76 51 20443 28690 53299882

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
Product use in unapproved indication 50.00 40.58 22 312 87182 32426010

Pharmacologic Action:

SourceCodeDescription
ATC L01XK03 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 cytostatic
CHEBI has role CHEBI:62913 poly(ADP-ribose) polymerase inhibitors

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Malignant tumor of ovary indication 363443007 DOID:2394

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 CLOVIS ONCOLOGY INC N209115 Dec. 19, 2016 RX TABLET ORAL 7351701 July 23, 2024 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 CLOVIS ONCOLOGY INC N209115 Dec. 19, 2016 RX TABLET ORAL 7351701 July 23, 2024 A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
EQ 200MG BASE RUBRACA CLOVIS ONCOLOGY INC N209115 Dec. 19, 2016 RX TABLET ORAL 7351701 July 23, 2024 A METHOD FOR TREATING OVARIAN CANCER BY ADMINISTERING RUCAPARIB, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 200MG BASE RUBRACA CLOVIS ONCOLOGY INC N209115 Dec. 19, 2016 RX TABLET ORAL 7531530 July 23, 2024 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 CLOVIS ONCOLOGY INC N209115 Dec. 19, 2016 RX TABLET ORAL 7531530 July 23, 2024 A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
EQ 200MG BASE RUBRACA CLOVIS ONCOLOGY INC N209115 Dec. 19, 2016 RX TABLET ORAL 7531530 July 23, 2024 A METHOD FOR TREATING OVARIAN CANCER BY ADMINISTERING RUCAPARIB, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 250MG BASE RUBRACA CLOVIS ONCOLOGY INC N209115 May 1, 2017 RX TABLET ORAL 7351701 July 23, 2024 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 CLOVIS ONCOLOGY INC N209115 May 1, 2017 RX TABLET ORAL 7351701 July 23, 2024 A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
EQ 250MG BASE RUBRACA CLOVIS ONCOLOGY INC N209115 May 1, 2017 RX TABLET ORAL 7351701 July 23, 2024 A METHOD FOR TREATING OVARIAN CANCER BY ADMINISTERING RUCAPARIB, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 250MG BASE RUBRACA CLOVIS ONCOLOGY INC N209115 May 1, 2017 RX TABLET ORAL 7531530 July 23, 2024 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 CLOVIS ONCOLOGY INC N209115 May 1, 2017 RX TABLET ORAL 7531530 July 23, 2024 A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
EQ 250MG BASE RUBRACA CLOVIS ONCOLOGY INC N209115 May 1, 2017 RX TABLET ORAL 7531530 July 23, 2024 A METHOD FOR TREATING OVARIAN CANCER BY ADMINISTERING RUCAPARIB, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 300MG BASE RUBRACA CLOVIS ONCOLOGY INC N209115 Dec. 19, 2016 RX TABLET ORAL 7351701 July 23, 2024 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 CLOVIS ONCOLOGY INC N209115 Dec. 19, 2016 RX TABLET ORAL 7351701 July 23, 2024 A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
EQ 300MG BASE RUBRACA CLOVIS ONCOLOGY INC N209115 Dec. 19, 2016 RX TABLET ORAL 7351701 July 23, 2024 A METHOD FOR TREATING OVARIAN CANCER BY ADMINISTERING RUCAPARIB, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 300MG BASE RUBRACA CLOVIS ONCOLOGY INC N209115 Dec. 19, 2016 RX TABLET ORAL 7531530 July 23, 2024 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 CLOVIS ONCOLOGY INC N209115 Dec. 19, 2016 RX TABLET ORAL 7531530 July 23, 2024 A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
EQ 300MG BASE RUBRACA CLOVIS ONCOLOGY INC N209115 Dec. 19, 2016 RX TABLET ORAL 7531530 July 23, 2024 A METHOD FOR TREATING OVARIAN CANCER BY ADMINISTERING RUCAPARIB, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 200MG BASE RUBRACA CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC 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 CLOVIS ONCOLOGY INC N209115 Dec. 19, 2016 RX TABLET ORAL May 15, 2023 TREATMENT OF ADULT PATIENTS WITH A DELETERIOUS BRCA MUTATION (GERMLINE AND/OR SOMATIC)-ASSOCIATED METASTATIC CASTRATION-RESISTANT PROSTATE CANCER WHO HAVE BEEN TREATED WITH ANDROGEN RECEPTOR-DIRECTED THERAPY AND A TAXANE-BASED CHEMOTHERAPY
EQ 250MG BASE RUBRACA CLOVIS ONCOLOGY INC N209115 May 1, 2017 RX TABLET ORAL May 15, 2023 TREATMENT OF ADULT PATIENTS WITH A DELETERIOUS BRCA MUTATION (GERMLINE AND/OR SOMATIC)-ASSOCIATED METASTATIC CASTRATION-RESISTANT PROSTATE CANCER WHO HAVE BEEN TREATED WITH ANDROGEN RECEPTOR-DIRECTED THERAPY AND A TAXANE-BASED CHEMOTHERAPY
EQ 300MG BASE RUBRACA CLOVIS ONCOLOGY INC N209115 Dec. 19, 2016 RX TABLET ORAL May 15, 2023 TREATMENT OF ADULT PATIENTS WITH A DELETERIOUS BRCA MUTATION (GERMLINE AND/OR SOMATIC)-ASSOCIATED METASTATIC CASTRATION-RESISTANT PROSTATE CANCER WHO HAVE BEEN TREATED WITH ANDROGEN RECEPTOR-DIRECTED THERAPY AND A TAXANE-BASED CHEMOTHERAPY
EQ 200MG BASE RUBRACA CLOVIS ONCOLOGY INC N209115 Dec. 19, 2016 RX TABLET ORAL Dec. 19, 2023 AS MONOTHERAPY FOR THE TREATMENT OF PATIENTS WITH DELETERIOUS BRCA MUTATION (GERMLINE AND/OR SOMATIC) ASSOCIATED ADVANCED OVARIAN CANCER WHO HAVE BEEN TREATED WITH TWO OR MORE CHEMOTHERAPIES
EQ 250MG BASE RUBRACA CLOVIS ONCOLOGY INC N209115 May 1, 2017 RX TABLET ORAL Dec. 19, 2023 AS MONOTHERAPY FOR THE TREATMENT OF PATIENTS WITH DELETERIOUS BRCA MUTATION (GERMLINE AND/OR SOMATIC) ASSOCIATED ADVANCED OVARIAN CANCER WHO HAVE BEEN TREATED WITH TWO OR MORE CHEMOTHERAPIES
EQ 300MG BASE RUBRACA CLOVIS ONCOLOGY INC N209115 Dec. 19, 2016 RX TABLET ORAL Dec. 19, 2023 AS MONOTHERAPY FOR THE TREATMENT OF PATIENTS WITH DELETERIOUS BRCA MUTATION (GERMLINE AND/OR SOMATIC) ASSOCIATED ADVANCED OVARIAN CANCER WHO HAVE BEEN TREATED WITH TWO OR MORE CHEMOTHERAPIES
EQ 200MG BASE RUBRACA CLOVIS ONCOLOGY INC N209115 Dec. 19, 2016 RX TABLET ORAL April 6, 2025 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
EQ 250MG BASE RUBRACA CLOVIS ONCOLOGY INC N209115 May 1, 2017 RX TABLET ORAL April 6, 2025 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
EQ 300MG BASE RUBRACA CLOVIS ONCOLOGY INC N209115 Dec. 19, 2016 RX TABLET ORAL April 6, 2025 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

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
Poly [ADP-ribose] polymerase 10 Enzyme INHIBITOR IC50 6.25 SCIENTIFIC LITERATURE
Poly [ADP-ribose] polymerase 12 Enzyme INHIBITOR IC50 5.18 SCIENTIFIC LITERATURE
Tankyrase-2 Enzyme INHIBITOR IC50 6.05 SCIENTIFIC LITERATURE
Poly [ADP-ribose] polymerase 15 Enzyme INHIBITOR IC50 4.49 SCIENTIFIC LITERATURE
Poly [ADP-ribose] polymerase 14 Enzyme INHIBITOR IC50 5.05 SCIENTIFIC LITERATURE
Tankyrase-1 Enzyme INHIBITOR IC50 6.84 SCIENTIFIC LITERATURE
Poly [ADP-ribose] polymerase 4 Enzyme INHIBITOR IC50 6.08 SCIENTIFIC LITERATURE

External reference:

IDSource
8237F3U7EH UNII
1859053-21-6 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
C531549 MESH_SUPPLEMENTAL_RECORD_UI
C520469 MESH_SUPPLEMENTAL_RECORD_UI
7736 IUPHAR_LIGAND_ID
9471 INN_ID
1862578 RXNORM
247942 MMSL
32185 MMSL
d08507 MMSL
017056 NDDF
017057 NDDF
723984009 SNOMEDCT_US
763539004 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Rubraca HUMAN PRESCRIPTION DRUG LABEL 1 69660-201 TABLET, FILM COATED 200 mg ORAL NDA 28 sections
Rubraca HUMAN PRESCRIPTION DRUG LABEL 1 69660-202 TABLET, FILM COATED 250 mg ORAL NDA 28 sections
Rubraca HUMAN PRESCRIPTION DRUG LABEL 1 69660-203 TABLET, FILM COATED 300 mg ORAL NDA 28 sections