U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ACHIRAL
Molecular Formula C19H18FN3O
Molecular Weight 323.3648
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of RUCAPARIB

SMILES

CNCc1ccc(cc1)-c2c3CCNC(=O)c4cc(cc(c34)[nH]2)F

InChI

InChIKey=HMABYWSNWIZPAG-UHFFFAOYSA-N
InChI=1S/C19H18FN3O/c1-21-10-11-2-4-12(5-3-11)18-14-6-7-22-19(24)15-8-13(20)9-16(23-18)17(14)15/h2-5,8-9,21,23H,6-7,10H2,1H3,(H,22,24)

HIDE SMILES / InChI

Molecular Formula C19H18FN3O
Molecular Weight 323.3648
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Rucaparib is a poly (ADP-ribose) polymerase (PARP) inhibitor indicated for the treatment of advanced mutant BRCA ovarian cancer. Rucaparib is being investigated in clinical trials against prostate cancer, breast cancer and other neoplasms.

Originator

Curator's Comment:: Rucaparib was identified in a collaboration between the Northern Institute of Cancer Research (NICR), Cancer Research UK and Agouron Pharmaceuticals. It was then licensed to Phizer, and later rigths to its development and commercialization were sold to Clovis Oncology.

Approval Year

Targets

Targets

Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
RUBRACA

Approved Use

RUBRACA is a poly (ADP-ribose) polymerase (PARP) inhibitor indicated 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. Select patients for therapy based on an FDA-approved companion diagnostic for RUBRACA.

Launch Date

1482883200000
Primary
Primary
Primary
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
629 ng/mL
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
RUCAPARIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
5740 ng × h/mL
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
RUCAPARIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
15.2 h
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
RUCAPARIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
Doses

Doses

DosePopulationAdverse events​
840 mg 2 times / day steady, oral
Highest studied dose
Dose: 840 mg, 2 times / day
Route: oral
Route: steady
Dose: 840 mg, 2 times / day
Sources:
unhealthy, 51 years (range: 21–71 years)
Health Status: unhealthy
Age Group: 51 years (range: 21–71 years)
Sex: M+F
Sources:
Other AEs: Asthenia, Fatigue...
Other AEs:
Asthenia (33.3%)
Fatigue (33.3%)
Nausea (100%)
Vomiting (66.7%)
Diarrhea (100%)
Decreased appetite (33.3%)
Alanine aminotransferase increase (33.3%)
Transaminases increased (33.3%)
Headache (33.3%)
Abdominal pain (33.3%)
Dysgeusia (14.3%)
Dyspnea (33.3%)
Sources:
18 mg/m2 1 times / day multiple, intravenous
Dose: 18 mg/m2, 1 times / day
Route: intravenous
Route: multiple
Dose: 18 mg/m2, 1 times / day
Sources:
unhealthy, 52 years (range: 23–72 years)
Health Status: unhealthy
Age Group: 52 years (range: 23–72 years)
Sex: F
Sources:
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 31 - 86 years)
Health Status: unhealthy
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Sources:
Disc. AE: Fatigue, Asthenia...
AEs leading to
discontinuation/dose reduction:
Fatigue (2%)
Asthenia (2%)
Sources:
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 31 - 86 years)
Health Status: unhealthy
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Sources:
Disc. AE: Intestinal obstruction, Small intestinal obstruction...
AEs leading to
discontinuation/dose reduction:
Intestinal obstruction (1.7%)
Small intestinal obstruction (1.7%)
Nausea (1.3%)
Abdominal pain (1.1%)
Abdominal pain upper (1.1%)
Sources:
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 31 - 86 years)
Health Status: unhealthy
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Sources:
Disc. AE: Anemia, Fatigue...
AEs leading to
discontinuation/dose reduction:
Anemia (21.2%)
Fatigue (19.8%)
Asthenia (19.8%)
Hemoglobin decreased (21.2%)
Nausea (17.2%)
Vomiting (11.4%)
Alanine aminotransferase increased (9.8%)
Thrombocytopenia (9.8%)
Platelet count decreased (6.6%)
Neutrophil count decreased (6.3%)
Neutropenia (6.3%)
Blood creatinine increased (5%)
Abdominal pain (4.7%)
Abdominal pain upper (4.7%)
Sources:
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 86 years
Health Status: unhealthy
Age Group: 86 years
Sex: M
Sources:
Disc. AE: Torsades de pointes...
AEs leading to
discontinuation/dose reduction:
Torsades de pointes (grade 5, 1 patient)
Sources:
AEs

AEs

AESignificanceDosePopulation
Diarrhea 100%
840 mg 2 times / day steady, oral
Highest studied dose
Dose: 840 mg, 2 times / day
Route: oral
Route: steady
Dose: 840 mg, 2 times / day
Sources:
unhealthy, 51 years (range: 21–71 years)
Health Status: unhealthy
Age Group: 51 years (range: 21–71 years)
Sex: M+F
Sources:
Nausea 100%
840 mg 2 times / day steady, oral
Highest studied dose
Dose: 840 mg, 2 times / day
Route: oral
Route: steady
Dose: 840 mg, 2 times / day
Sources:
unhealthy, 51 years (range: 21–71 years)
Health Status: unhealthy
Age Group: 51 years (range: 21–71 years)
Sex: M+F
Sources:
Dysgeusia 14.3%
840 mg 2 times / day steady, oral
Highest studied dose
Dose: 840 mg, 2 times / day
Route: oral
Route: steady
Dose: 840 mg, 2 times / day
Sources:
unhealthy, 51 years (range: 21–71 years)
Health Status: unhealthy
Age Group: 51 years (range: 21–71 years)
Sex: M+F
Sources:
Abdominal pain 33.3%
840 mg 2 times / day steady, oral
Highest studied dose
Dose: 840 mg, 2 times / day
Route: oral
Route: steady
Dose: 840 mg, 2 times / day
Sources:
unhealthy, 51 years (range: 21–71 years)
Health Status: unhealthy
Age Group: 51 years (range: 21–71 years)
Sex: M+F
Sources:
Alanine aminotransferase increase 33.3%
840 mg 2 times / day steady, oral
Highest studied dose
Dose: 840 mg, 2 times / day
Route: oral
Route: steady
Dose: 840 mg, 2 times / day
Sources:
unhealthy, 51 years (range: 21–71 years)
Health Status: unhealthy
Age Group: 51 years (range: 21–71 years)
Sex: M+F
Sources:
Asthenia 33.3%
840 mg 2 times / day steady, oral
Highest studied dose
Dose: 840 mg, 2 times / day
Route: oral
Route: steady
Dose: 840 mg, 2 times / day
Sources:
unhealthy, 51 years (range: 21–71 years)
Health Status: unhealthy
Age Group: 51 years (range: 21–71 years)
Sex: M+F
Sources:
Decreased appetite 33.3%
840 mg 2 times / day steady, oral
Highest studied dose
Dose: 840 mg, 2 times / day
Route: oral
Route: steady
Dose: 840 mg, 2 times / day
Sources:
unhealthy, 51 years (range: 21–71 years)
Health Status: unhealthy
Age Group: 51 years (range: 21–71 years)
Sex: M+F
Sources:
Dyspnea 33.3%
840 mg 2 times / day steady, oral
Highest studied dose
Dose: 840 mg, 2 times / day
Route: oral
Route: steady
Dose: 840 mg, 2 times / day
Sources:
unhealthy, 51 years (range: 21–71 years)
Health Status: unhealthy
Age Group: 51 years (range: 21–71 years)
Sex: M+F
Sources:
Fatigue 33.3%
840 mg 2 times / day steady, oral
Highest studied dose
Dose: 840 mg, 2 times / day
Route: oral
Route: steady
Dose: 840 mg, 2 times / day
Sources:
unhealthy, 51 years (range: 21–71 years)
Health Status: unhealthy
Age Group: 51 years (range: 21–71 years)
Sex: M+F
Sources:
Headache 33.3%
840 mg 2 times / day steady, oral
Highest studied dose
Dose: 840 mg, 2 times / day
Route: oral
Route: steady
Dose: 840 mg, 2 times / day
Sources:
unhealthy, 51 years (range: 21–71 years)
Health Status: unhealthy
Age Group: 51 years (range: 21–71 years)
Sex: M+F
Sources:
Transaminases increased 33.3%
840 mg 2 times / day steady, oral
Highest studied dose
Dose: 840 mg, 2 times / day
Route: oral
Route: steady
Dose: 840 mg, 2 times / day
Sources:
unhealthy, 51 years (range: 21–71 years)
Health Status: unhealthy
Age Group: 51 years (range: 21–71 years)
Sex: M+F
Sources:
Vomiting 66.7%
840 mg 2 times / day steady, oral
Highest studied dose
Dose: 840 mg, 2 times / day
Route: oral
Route: steady
Dose: 840 mg, 2 times / day
Sources:
unhealthy, 51 years (range: 21–71 years)
Health Status: unhealthy
Age Group: 51 years (range: 21–71 years)
Sex: M+F
Sources:
Asthenia 2%
Disc. AE
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 31 - 86 years)
Health Status: unhealthy
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Sources:
Fatigue 2%
Disc. AE
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 31 - 86 years)
Health Status: unhealthy
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Sources:
Abdominal pain upper 1.1%
Disc. AE
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 31 - 86 years)
Health Status: unhealthy
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Sources:
Abdominal pain 1.1%
Disc. AE
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 31 - 86 years)
Health Status: unhealthy
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Sources:
Nausea 1.3%
Disc. AE
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 31 - 86 years)
Health Status: unhealthy
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Sources:
Intestinal obstruction 1.7%
Disc. AE
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 31 - 86 years)
Health Status: unhealthy
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Sources:
Small intestinal obstruction 1.7%
Disc. AE
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 31 - 86 years)
Health Status: unhealthy
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Sources:
Vomiting 11.4%
Disc. AE
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 31 - 86 years)
Health Status: unhealthy
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Sources:
Nausea 17.2%
Disc. AE
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 31 - 86 years)
Health Status: unhealthy
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Sources:
Asthenia 19.8%
Disc. AE
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 31 - 86 years)
Health Status: unhealthy
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Sources:
Fatigue 19.8%
Disc. AE
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 31 - 86 years)
Health Status: unhealthy
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Sources:
Anemia 21.2%
Disc. AE
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 31 - 86 years)
Health Status: unhealthy
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Sources:
Hemoglobin decreased 21.2%
Disc. AE
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 31 - 86 years)
Health Status: unhealthy
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Sources:
Abdominal pain upper 4.7%
Disc. AE
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 31 - 86 years)
Health Status: unhealthy
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Sources:
Abdominal pain 4.7%
Disc. AE
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 31 - 86 years)
Health Status: unhealthy
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Sources:
Blood creatinine increased 5%
Disc. AE
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 31 - 86 years)
Health Status: unhealthy
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Sources:
Neutropenia 6.3%
Disc. AE
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 31 - 86 years)
Health Status: unhealthy
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Sources:
Neutrophil count decreased 6.3%
Disc. AE
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 31 - 86 years)
Health Status: unhealthy
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Sources:
Platelet count decreased 6.6%
Disc. AE
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 31 - 86 years)
Health Status: unhealthy
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Sources:
Alanine aminotransferase increased 9.8%
Disc. AE
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 31 - 86 years)
Health Status: unhealthy
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Sources:
Thrombocytopenia 9.8%
Disc. AE
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 31 - 86 years)
Health Status: unhealthy
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Sources:
Torsades de pointes grade 5, 1 patient
Disc. AE
600 mg 2 times / day steady, oral
Recommended
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy, 86 years
Health Status: unhealthy
Age Group: 86 years
Sex: M
Sources:
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no [Inhibition 300 uM]
no [Inhibition 300 uM]
no [Inhibition 300 uM]
no [Inhibition 300 uM]
no
no
no
no
no
strong [IC50 0.19 uM]
strong [IC50 0.63 uM]
yes [IC50 12.9 uM]
yes (co-administration study)
Comment: warfarin AUC increased 1.49-fold
Page: 14
yes [IC50 169 uM]
weak (co-administration study)
yes [IC50 3.55 uM]
yes (co-administration study)
Comment: caffeine AUC increased 2.55-fold
Page: 14
yes [IC50 31 uM]
yes [IC50 4.3 uM]
yes [IC50 41.6 uM]
yes [IC50 5.42 uM]
yes (co-administration study)
Comment: omeprazole AUC increased 1.55-fold
Page: 14
yes [IC50 55 uM]
yes
yes
yes
yes
yes
yes
yes (co-administration study)
Comment: midazolam AUC increased 1.38-fold
Page: 14
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
no (pharmacogenomic study)
Comment: based on population PK analyses there appeared to be no significant difference in steady-state exposure of rucaparib among CYP2D6 phenotypes
Page: 56, 59, 65
yes
yes
yes
yes
yes
yes
no (pharmacogenomic study)
Comment: based on population PK analyses there appeared to be no significant difference in steady-state exposure of rucaparib among CYP1A2 phenotypes
Page: 1
Tox targets

Tox targets

PubMed

PubMed

TitleDatePubMed
Potentiation of temozolomide and topotecan growth inhibition and cytotoxicity by novel poly(adenosine diphosphoribose) polymerase inhibitors in a panel of human tumor cell lines.
2000 Jul
Preclinical selection of a novel poly(ADP-ribose) polymerase inhibitor for clinical trial.
2007 Mar
Patents

Sample Use Guides

Recommended dose is 600 mg orally twice daily with or without food.
Route of Administration: Oral
Exponentially proliferating cells were plated into six-well plates and incubated for 48 hours to allow cells to reach their optimum proliferation rate. AG014699 at 0, 0.1, 1.0, 10.0, 30.0, 50.0, or 100 μM in 1% dimethyl sulfoxide was added to the wells and incubated for 24 hours. Control cells received no AG014699 but were treated with medium containing 1% dimethyl sulfoxide for 24 hours. Cells were harvested and cultured in drug-free medium in 90-mm Petri dishes for up to 21 days, depending on the proliferation rate of the individual cell line. Colonies were fixed in methanol and acetic acid (3:1 vol/vol), stained with methyl violet 10B, and counted with an automated colony counter (Oxford Optronix, Oxford, UK). Data are expressed as the percentage of colonies in AG014699-treated cultures compared with that in control cultures. AG014699 (≤10 μM) was cytotoxic to cells with mutated BRCA1/2 or XRCC3 and to UACC3199 cells with epigenetically silenced BRCA1 but not to cells without BRCA1/2 or XRCC3 mutations or that were heterozygous for BRCA2 mutation
Substance Class Chemical
Created
by admin
on Sat Jun 26 11:50:03 UTC 2021
Edited
by admin
on Sat Jun 26 11:50:03 UTC 2021
Record UNII
8237F3U7EH
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
RUCAPARIB
INN   USAN   WHO-DD  
INN   USAN  
Official Name English
6H-AZEPINO(5,4,3-CD)INDOL-6-ONE, 8-FLUORO-1,3,4,5-TETRAHYDRO-2-(4-((METHYLAMINO)METHYL)PHENYL)-
Systematic Name English
RUCAPARIB [USAN]
Common Name English
RUCAPARIB [INN]
Common Name English
6H-PYRROLO(4,3,2-EF)(2)BENZAZEPIN-6-ONE, 8-FLUORO-1,3,4,5-TETRAHYDRO-2-(4-((METHYLAMINO)METHYL)PHENYL)-
Systematic Name English
RUCAPARIB [WHO-DD]
Common Name English
AG-14447
Code English
8-FLUORO-2-(4-((METHYLAMINO)METHYL)PHENYL)-1,3,4,5-TETRAHYDRO-6H-AZEPINO(5,4,3-CD)INDOL-6-ONE
Systematic Name English
RUCAPARIB [MI]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C62554
Created by admin on Sat Jun 26 11:50:04 UTC 2021 , Edited by admin on Sat Jun 26 11:50:04 UTC 2021
WHO-ATC L01XX55
Created by admin on Sat Jun 26 11:50:04 UTC 2021 , Edited by admin on Sat Jun 26 11:50:04 UTC 2021
NDF-RT N0000191623
Created by admin on Sat Jun 26 11:50:04 UTC 2021 , Edited by admin on Sat Jun 26 11:50:04 UTC 2021
FDA ORPHAN DRUG 374712
Created by admin on Sat Jun 26 11:50:04 UTC 2021 , Edited by admin on Sat Jun 26 11:50:04 UTC 2021
EU-Orphan Drug EU/3/12/1049
Created by admin on Sat Jun 26 11:50:04 UTC 2021 , Edited by admin on Sat Jun 26 11:50:04 UTC 2021
Code System Code Type Description
FDA UNII
8237F3U7EH
Created by admin on Sat Jun 26 11:50:04 UTC 2021 , Edited by admin on Sat Jun 26 11:50:04 UTC 2021
PRIMARY
EVMPD
SUB74859
Created by admin on Sat Jun 26 11:50:04 UTC 2021 , Edited by admin on Sat Jun 26 11:50:04 UTC 2021
PRIMARY
DRUG BANK
DB12332
Created by admin on Sat Jun 26 11:50:04 UTC 2021 , Edited by admin on Sat Jun 26 11:50:04 UTC 2021
PRIMARY
PUBCHEM
9931954
Created by admin on Sat Jun 26 11:50:04 UTC 2021 , Edited by admin on Sat Jun 26 11:50:04 UTC 2021
PRIMARY
DRUG CENTRAL
5203
Created by admin on Sat Jun 26 11:50:04 UTC 2021 , Edited by admin on Sat Jun 26 11:50:04 UTC 2021
PRIMARY
ChEMBL
CHEMBL1173055
Created by admin on Sat Jun 26 11:50:04 UTC 2021 , Edited by admin on Sat Jun 26 11:50:04 UTC 2021
PRIMARY
RXCUI
1862579
Created by admin on Sat Jun 26 11:50:04 UTC 2021 , Edited by admin on Sat Jun 26 11:50:04 UTC 2021
PRIMARY
CAS
283173-50-2
Created by admin on Sat Jun 26 11:50:04 UTC 2021 , Edited by admin on Sat Jun 26 11:50:04 UTC 2021
PRIMARY
INN
9471
Created by admin on Sat Jun 26 11:50:04 UTC 2021 , Edited by admin on Sat Jun 26 11:50:04 UTC 2021
PRIMARY
LACTMED
Rucaparib
Created by admin on Sat Jun 26 11:50:04 UTC 2021 , Edited by admin on Sat Jun 26 11:50:04 UTC 2021
PRIMARY
NCI_THESAURUS
C137800
Created by admin on Sat Jun 26 11:50:04 UTC 2021 , Edited by admin on Sat Jun 26 11:50:04 UTC 2021
PRIMARY
EPA CompTox
283173-50-2
Created by admin on Sat Jun 26 11:50:04 UTC 2021 , Edited by admin on Sat Jun 26 11:50:04 UTC 2021
PRIMARY
MERCK INDEX
M11980
Created by admin on Sat Jun 26 11:50:04 UTC 2021 , Edited by admin on Sat Jun 26 11:50:04 UTC 2021
PRIMARY
WIKIPEDIA
RUCAPARIB
Created by admin on Sat Jun 26 11:50:04 UTC 2021 , Edited by admin on Sat Jun 26 11:50:04 UTC 2021
PRIMARY
NDF-RT
N0000191622
Created by admin on Sat Jun 26 11:50:04 UTC 2021 , Edited by admin on Sat Jun 26 11:50:04 UTC 2021
PRIMARY Poly(ADP-Ribose) Polymerase Inhibitors [MoA]
Related Record Type Details
TRANSPORTER -> SUBSTRATE
TARGET -> INHIBITOR
IC50
TRANSPORTER -> INHIBITOR
MODERATE
SALT/SOLVATE -> PARENT
METABOLIC ENZYME -> INHIBITOR
REVERSIBLE
TRANSPORTER -> SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
MAJOR
TRANSPORTER -> INHIBITOR
METABOLIC ENZYME -> SUBSTRATE
In vitro, rucaparib was metabolized primarily by CYP2D6 and to a lesser extent by CYP1A2 and CYP3A4.
METABOLIC ENZYME -> INHIBITOR
REVERSIBLE
METABOLIC ENZYME -> INHIBITOR
TARGET -> INHIBITOR
IC50
BINDER->LIGAND
BINDING
METABOLIC ENZYME -> INHIBITOR
REVERSIBLE
SALT/SOLVATE -> PARENT
METABOLIC ENZYME -> SUBSTRATE
In vitro, rucaparib was metabolized primarily by CYP2D6 and to a lesser extent by CYP1A2 and CYP3A4.
METABOLIC ENZYME -> INHIBITOR
REVERSIBLE
METABOLIC ENZYME -> INDUCER
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
Tmax PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC
blood-to-plasma ratio PHARMACOKINETIC