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Details

Stereochemistry ABSOLUTE
Molecular Formula C19H18FN3O.C10H16O4S
Molecular Weight 555.6629
Optical Activity UNSPECIFIED
Defined Stereocenters 2 / 2
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of RUCAPARIB CAMSYLATE

SMILES

CNCc1ccc(cc1)-c2c3CCNC(=O)c4cc(cc(c34)[nH]2)F.CC1(C)[C@]2([H])CC[C@@]1(CS(=O)(=O)O)C(=O)C2

InChI

InChIKey=INBJJAFXHQQSRW-STOWLHSFSA-N
InChI=1S/C19H18FN3O.C10H16O4S/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;1-9(2)7-3-4-10(9,8(11)5-7)6-15(12,13)14/h2-5,8-9,21,23H,6-7,10H2,1H3,(H,22,24);7H,3-6H2,1-2H3,(H,12,13,14)/t;7-,10-/m.1/s1

HIDE SMILES / InChI

Molecular Formula C10H16O4S
Molecular Weight 232.2981
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 2 / 2
E/Z Centers 0
Optical Activity UNSPECIFIED

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

Primary TargetPharmacologyConditionPotency
0.804 nM [IC50]
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

1.4828832E12
Primary
Unknown

Approved Use

Unknown
Primary
Unknown

Approved Use

Unknown
Primary
Unknown

Approved Use

Unknown
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)
n = 3
Health Status: unhealthy
Age Group: 51 years (range: 21–71 years)
Sex: M+F
Population Size: 3
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)
n = 33
Health Status: unhealthy
Age Group: 52 years (range: 23–72 years)
Sex: F
Population Size: 33
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)
n = 377
Health Status: unhealthy
Condition: ovarian cancer
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Population Size: 377
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: Page: p. 11-77
unhealthy, 62 years (range: 31 - 86 years)
n = 378
Health Status: unhealthy
Condition: ovarian cancer
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Population Size: 378
Sources: Page: p. 11-77
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: Page: p. 11-77
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: Page: p. 11-81
unhealthy, 62 years (range: 31 - 86 years)
n = 378
Health Status: unhealthy
Condition: ovarian cancer
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Population Size: 378
Sources: Page: p. 11-81
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: Page: p. 11-81
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
n = 1
Health Status: unhealthy
Age Group: 86 years
Sex: M
Population Size: 1
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)
n = 3
Health Status: unhealthy
Age Group: 51 years (range: 21–71 years)
Sex: M+F
Population Size: 3
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)
n = 3
Health Status: unhealthy
Age Group: 51 years (range: 21–71 years)
Sex: M+F
Population Size: 3
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)
n = 3
Health Status: unhealthy
Age Group: 51 years (range: 21–71 years)
Sex: M+F
Population Size: 3
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)
n = 3
Health Status: unhealthy
Age Group: 51 years (range: 21–71 years)
Sex: M+F
Population Size: 3
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)
n = 3
Health Status: unhealthy
Age Group: 51 years (range: 21–71 years)
Sex: M+F
Population Size: 3
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)
n = 3
Health Status: unhealthy
Age Group: 51 years (range: 21–71 years)
Sex: M+F
Population Size: 3
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)
n = 3
Health Status: unhealthy
Age Group: 51 years (range: 21–71 years)
Sex: M+F
Population Size: 3
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)
n = 3
Health Status: unhealthy
Age Group: 51 years (range: 21–71 years)
Sex: M+F
Population Size: 3
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)
n = 3
Health Status: unhealthy
Age Group: 51 years (range: 21–71 years)
Sex: M+F
Population Size: 3
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)
n = 3
Health Status: unhealthy
Age Group: 51 years (range: 21–71 years)
Sex: M+F
Population Size: 3
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)
n = 3
Health Status: unhealthy
Age Group: 51 years (range: 21–71 years)
Sex: M+F
Population Size: 3
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)
n = 3
Health Status: unhealthy
Age Group: 51 years (range: 21–71 years)
Sex: M+F
Population Size: 3
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)
n = 377
Health Status: unhealthy
Condition: ovarian cancer
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Population Size: 377
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)
n = 377
Health Status: unhealthy
Condition: ovarian cancer
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Population Size: 377
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: Page: p. 11-77
unhealthy, 62 years (range: 31 - 86 years)
n = 378
Health Status: unhealthy
Condition: ovarian cancer
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Population Size: 378
Sources: Page: p. 11-77
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: Page: p. 11-77
unhealthy, 62 years (range: 31 - 86 years)
n = 378
Health Status: unhealthy
Condition: ovarian cancer
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Population Size: 378
Sources: Page: p. 11-77
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: Page: p. 11-77
unhealthy, 62 years (range: 31 - 86 years)
n = 378
Health Status: unhealthy
Condition: ovarian cancer
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Population Size: 378
Sources: Page: p. 11-77
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: Page: p. 11-77
unhealthy, 62 years (range: 31 - 86 years)
n = 378
Health Status: unhealthy
Condition: ovarian cancer
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Population Size: 378
Sources: Page: p. 11-77
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: Page: p. 11-77
unhealthy, 62 years (range: 31 - 86 years)
n = 378
Health Status: unhealthy
Condition: ovarian cancer
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Population Size: 378
Sources: Page: p. 11-77
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: Page: p. 11-81
unhealthy, 62 years (range: 31 - 86 years)
n = 378
Health Status: unhealthy
Condition: ovarian cancer
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Population Size: 378
Sources: Page: p. 11-81
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: Page: p. 11-81
unhealthy, 62 years (range: 31 - 86 years)
n = 378
Health Status: unhealthy
Condition: ovarian cancer
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Population Size: 378
Sources: Page: p. 11-81
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: Page: p. 11-81
unhealthy, 62 years (range: 31 - 86 years)
n = 378
Health Status: unhealthy
Condition: ovarian cancer
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Population Size: 378
Sources: Page: p. 11-81
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: Page: p. 11-81
unhealthy, 62 years (range: 31 - 86 years)
n = 378
Health Status: unhealthy
Condition: ovarian cancer
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Population Size: 378
Sources: Page: p. 11-81
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: Page: p. 11-81
unhealthy, 62 years (range: 31 - 86 years)
n = 378
Health Status: unhealthy
Condition: ovarian cancer
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Population Size: 378
Sources: Page: p. 11-81
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: Page: p. 11-81
unhealthy, 62 years (range: 31 - 86 years)
n = 378
Health Status: unhealthy
Condition: ovarian cancer
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Population Size: 378
Sources: Page: p. 11-81
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: Page: p. 11-81
unhealthy, 62 years (range: 31 - 86 years)
n = 378
Health Status: unhealthy
Condition: ovarian cancer
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Population Size: 378
Sources: Page: p. 11-81
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: Page: p. 11-81
unhealthy, 62 years (range: 31 - 86 years)
n = 378
Health Status: unhealthy
Condition: ovarian cancer
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Population Size: 378
Sources: Page: p. 11-81
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: Page: p. 11-81
unhealthy, 62 years (range: 31 - 86 years)
n = 378
Health Status: unhealthy
Condition: ovarian cancer
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Population Size: 378
Sources: Page: p. 11-81
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: Page: p. 11-81
unhealthy, 62 years (range: 31 - 86 years)
n = 378
Health Status: unhealthy
Condition: ovarian cancer
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Population Size: 378
Sources: Page: p. 11-81
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: Page: p. 11-81
unhealthy, 62 years (range: 31 - 86 years)
n = 378
Health Status: unhealthy
Condition: ovarian cancer
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Population Size: 378
Sources: Page: p. 11-81
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: Page: p. 11-81
unhealthy, 62 years (range: 31 - 86 years)
n = 378
Health Status: unhealthy
Condition: ovarian cancer
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Population Size: 378
Sources: Page: p. 11-81
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: Page: p. 11-81
unhealthy, 62 years (range: 31 - 86 years)
n = 378
Health Status: unhealthy
Condition: ovarian cancer
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Population Size: 378
Sources: Page: p. 11-81
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: Page: p. 11-81
unhealthy, 62 years (range: 31 - 86 years)
n = 378
Health Status: unhealthy
Condition: ovarian cancer
Age Group: 62 years (range: 31 - 86 years)
Sex: F
Population Size: 378
Sources: Page: p. 11-81
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
n = 1
Health Status: unhealthy
Age Group: 86 years
Sex: M
Population Size: 1
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: 14.0
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: 14.0
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: 14.0
yes [IC50 55 uM]
yes
yes
yes
yes
yes
yes
yes (co-administration study)
Comment: midazolam AUC increased 1.38-fold
Page: 14.0
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: 1.0
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
Anticancer chemosensitization and radiosensitization by the novel poly(ADP-ribose) polymerase-1 inhibitor AG14361.
2004 Jan 7
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 11:03:23 UTC 2021
Edited
by admin
on Sat Jun 26 11:03:23 UTC 2021
Record UNII
41AX9SJ8KO
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
RUCAPARIB CAMSYLATE
USAN  
USAN  
Official Name English
RUCAPARIB CAMSYLATE [MI]
Common Name English
RUCAPARIB CAMSYLATE [USAN]
Common Name English
RUBRACA
Brand Name English
RUCAPARIB CAMSYLATE [ORANGE BOOK]
Common Name English
RUCAPARIB CAMSYLATE [WHO-DD]
Common Name English
C0-338
Code English
8-FLUORO-2-(4-((METHYLAMINO)METHYL)PHENYL)-1,3,4,5-TETRAHYDRO-6H-PYRROLO(4,3,2-EF)(2)BENZAZEPIN-6-ONE (7,7-DIMETHYL-2-OXOBICYCLO(2.2.1)HEPTAN-1-YL)METHANESULFONATE (1:1)
Systematic Name English
PF-1367338-BW
Code English
BICYCLO(2.2.1)HEPTANE-1-METHANESULFONIC ACID, 7,7-DIMETHYL-2-OXO-, (1S,4R)-, COMPD. WITH 8-FLUORO-1,3,4,5-TETRAHYDRO-2-(4-((METHYLAMINO)METHYL)PHENYL)-6H-PYRROLO(4,3,2-EF)(2)BENZAZEPIN-6-ONE (1:1)
Systematic Name English
Classification Tree Code System Code
NCI_THESAURUS C62554
Created by admin on Sat Jun 26 11:03:23 UTC 2021 , Edited by admin on Sat Jun 26 11:03:23 UTC 2021
Code System Code Type Description
RXCUI
1862578
Created by admin on Sat Jun 26 11:03:23 UTC 2021 , Edited by admin on Sat Jun 26 11:03:23 UTC 2021
PRIMARY
EVMPD
SUB183557
Created by admin on Sat Jun 26 11:03:23 UTC 2021 , Edited by admin on Sat Jun 26 11:03:23 UTC 2021
PRIMARY
DRUG BANK
DBSALT001982
Created by admin on Sat Jun 26 11:03:23 UTC 2021 , Edited by admin on Sat Jun 26 11:03:23 UTC 2021
PRIMARY
FDA UNII
41AX9SJ8KO
Created by admin on Sat Jun 26 11:03:23 UTC 2021 , Edited by admin on Sat Jun 26 11:03:23 UTC 2021
PRIMARY
CAS
1859053-21-6
Created by admin on Sat Jun 26 11:03:23 UTC 2021 , Edited by admin on Sat Jun 26 11:03:23 UTC 2021
PRIMARY
MERCK INDEX
M11980
Created by admin on Sat Jun 26 11:03:23 UTC 2021 , Edited by admin on Sat Jun 26 11:03:23 UTC 2021
PRIMARY
NCI_THESAURUS
C131178
Created by admin on Sat Jun 26 11:03:23 UTC 2021 , Edited by admin on Sat Jun 26 11:03:23 UTC 2021
PRIMARY
CAS
1327258-57-0
Created by admin on Sat Jun 26 11:03:23 UTC 2021 , Edited by admin on Sat Jun 26 11:03:23 UTC 2021
NON-SPECIFIC STOICHIOMETRY
PUBCHEM
121490161
Created by admin on Sat Jun 26 11:03:23 UTC 2021 , Edited by admin on Sat Jun 26 11:03:23 UTC 2021
PRIMARY
Related Record Type Details
PARENT -> SALT/SOLVATE
Related Record Type Details
ACTIVE MOIETY