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Details

Stereochemistry ACHIRAL
Molecular Formula C24H23FN4O3
Molecular Weight 434.4637
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of OLAPARIB

SMILES

c1ccc2c(c1)c(Cc3ccc(c(c3)C(=O)N4CCN(CC4)C(=O)C5CC5)F)nnc2O

InChI

InChIKey=FDLYAMZZIXQODN-UHFFFAOYSA-N
InChI=1S/C24H23FN4O3/c25-20-8-5-15(14-21-17-3-1-2-4-18(17)22(30)27-26-21)13-19(20)24(32)29-11-9-28(10-12-29)23(31)16-6-7-16/h1-5,8,13,16H,6-7,9-12,14H2,(H,27,30)

HIDE SMILES / InChI

Description
Curator's Comment:: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4880823/

repair. Olaparib has shown activity in ovarian and breast tumors with known BRCA mutations and was the first FDA approved drug in this class. Lynparza (olaparib) is indicated for treatment of gBRCA-mutated advanced ovarian cancer. Its use together with other chemotherapy medicines can lead to increased effects on the blood resulting in reduction in the numbers of white blood cells and platelets, and anaemia.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Target ID: P09874
Gene ID: 142
Gene Symbol: PARP1
Target Organism: Homo sapiens (Human)
1.93999999999999995 nM [IC50]
Target ID: Q9UGN5
Gene ID: 10038
Gene Symbol: PARP2
Target Organism: Homo sapiens (Human)
Target ID: Q9Y6F1
Gene ID: 10039
Gene Symbol: PARP3
Target Organism: Homo sapiens (Human)
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
LYNPARZA

Approved Use

Monotherapy in patients with deleterious or suspected deleterious germline BRCA mutated advanced ovarian cancer who have been treated with three or more prior lines of chemotherapy.

Launch Date

1418947200000
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
2.97 μg/mL
100 mg 2 times / day multiple, oral
dose: 100 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
OLAPARIB blood
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
6.88 μg/mL
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OLAPARIB blood
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
3.75 μg/mL
100 mg 2 times / day steady-state, oral
dose: 100 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
OLAPARIB blood
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
8.27 μg/mL
300 mg 2 times / day steady-state, oral
dose: 300 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
OLAPARIB blood
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
6.875 ug/mL
300 mg single, oral
dose: 300 mg
route of administration: oral
experiment type: single
co-administered:
OLAPARIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
10.9 μg × h/mL
100 mg 2 times / day multiple, oral
dose: 100 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
OLAPARIB blood
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
31.7 μg × h/mL
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OLAPARIB blood
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
16.7 μg × h/mL
100 mg 2 times / day steady-state, oral
dose: 100 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
OLAPARIB blood
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
44 μg × h/mL
300 mg 2 times / day steady-state, oral
dose: 300 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
OLAPARIB blood
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
31.68 ug*h/mL
300 mg single, oral
dose: 300 mg
route of administration: oral
experiment type: single
co-administered:
OLAPARIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
43.91 ug*h/mL
300 mg 2 times / day single, oral
dose: 300 mg
route of administration: oral
experiment type: single
co-administered:
OLAPARIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
43.9499999999999 ug*h/mL
300 mg 2 times / day single, oral
dose: 300 mg
route of administration: oral
experiment type: single
co-administered:
OLAPARIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
36.37 ug*h/mL
300 mg single, oral
dose: 300 mg
route of administration: oral
experiment type: single
co-administered:
OLAPARIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
36.53 ug*h/mL
300 mg single, oral
dose: 300 mg
route of administration: oral
experiment type: single
co-administered:
OLAPARIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
7.17 h
100 mg 2 times / day multiple, oral
dose: 100 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
OLAPARIB blood
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
6.52 h
300 mg single, oral
dose: 300 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
OLAPARIB blood
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
18%
OLAPARIB plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
600 mg 2 times / day steady, oral
Highest studied dose
Dose: 600 mg, 2 times / day
Route: oral
Route: steady
Dose: 600 mg, 2 times / day
Sources:
unhealthy
300 mg 2 times / day steady, oral
Recommended
unhealthy
Disc. AE: Anemia, Anemia...
AEs leading to
discontinuation/dose reduction:
Anemia (grade 1-2, 24%)
Anemia (grade 3-4, 20%)
Neutropenia (9%)
Nausea (grade 1-2, 73%)
Nausea (grade 3-4, 3%)
Vomiting (grade 1-2, 34%)
Vomiting (grade 3-4, 3%)
Sources:
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Disc. AE: Fatigue, Fatigue...
Other AEs: Diarrhea, Diarrhea...
AEs leading to
discontinuation/dose reduction:
Fatigue (grade 1-2, 62%)
Fatigue (grade 3-4, 4%)
Other AEs:
Diarrhea (grade 1-2, 31%)
Diarrhea (grade 3-4, 2%)
Abscess oral (grade 1-2, 19%)
Aphthous ulcer (grade 1-2, 19%)
Gingival abscess (grade 1-2, 19%)
Gingival disorder (grade 1-2, 19%)
Gingival pain (grade 1-2, 19%)
Gingivitis (grade 1-2, 19%)
Mouth ulceration (grade 1-2, 19%)
Mucosal infection (grade 1-2, 19%)
Mucosal inflammation (grade 1-2, 19%)
Oral candidiasis (grade 1-2, 19%)
Oral discomfort (grade 1-2, 19%)
Oral herpes (grade 1-2, 19%)
Oral infection (grade 1-2, 19%)
Oral mucosal erythema (grade 1-2, 19%)
Oral pain (grade 1-2, 19%)
Oropharyngeal discomfort (grade 1-2, 19%)
Oropharyngeal pain (grade 1-2, 19%)
Abscess oral (grade 3-4, 1%)
Aphthous ulcer (grade 3-4, 1%)
Gingival abscess (grade 3-4, 1%)
Gingival disorder (grade 3-4, 1%)
Gingival pain (grade 3-4, 1%)
Gingivitis (grade 3-4, 1%)
Mouth ulceration (grade 3-4, 1%)
Mucosal infection (grade 3-4, 1%)
Mucosal inflammation (grade 3-4, 1%)
Oral candidiasis (grade 3-4, 1%)
Oral discomfort (grade 3-4, 1%)
Oral herpes (grade 3-4, 1%)
Oral infection (grade 3-4, 1%)
Oral mucosal erythema (grade 3-4, 1%)
Oral pain (grade 3-4, 1%)
Oropharyngeal discomfort (grade 3-4, 1%)
Oropharyngeal pain (grade 3-4, 1%)
Nasopharyngitis (grade 1-4, 36%)
Sinusitis (grade 1-4, 36%)
Rhinitis (grade 1-4, 36%)
Influenza (grade 1-4, 36%)
Decreased appetite (grade 1-4, 22%)
Arthralgia (grade 1-4, 30%)
Myalgia (grade 1-4, 30%)
Dysgeusia (grade 1-4, 27%)
Headache (grade 1-2, 25%)
Headache (grade 3-4, 1%)
Rash (<20%)
Cough (<20%)
Dyspepsia (<20%)
Leukopenia (<20%)
Hypomagnesemia (<20%)
Dizziness (<20%)
Thrombocytopenia (<20%)
Creatinine increased (<20%)
Lymphopenia (<20%)
Edema (<20%)
Mean corpuscular volume increased (grade 1-4, 89%)
Decreased hemoglobin (grade 1-2, 66%)
Decreased hemoglobin (grade 3-4, 17%)
Leukocyte count decreased (grade 1-2, 64%)
Leukocyte count decreased (grade 3-4, 5%)
Lymphocyte count low (grade 1-2, 56%)
Lymphocyte count low (grade 3-4, 11%)
Absolute neutrophil count decreased (grade 1-2, 44%)
Absolute neutrophil count decreased (grade 3-4, 7%)
Creatinine serum increased (grade 1-4, 44%)
Platelets decreased (grade 1-2, 40%)
Platelets decreased (grade 3-4, 2%)
Sources:
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Disc. AE: Thrombocytopenia, Myelodysplastic syndrome...
AEs leading to
discontinuation/dose reduction:
Thrombocytopenia (9 patients)
Myelodysplastic syndrome (2 patients)
Acute myeloid leukemia (2 patients)
Sources:
400 mg 2 times / day steady, oral
Recommended|MTD
unhealthy
Disc. AE: Nausea, Nausea...
AEs leading to
discontinuation/dose reduction:
Nausea (grade 1-2, 61%)
Nausea (grade 3-4, 3%)
Vomiting (grade 1-2, 39%)
Vomiting (grade 3-4, 4%)
Fatigue (grade 1-2, 58%)
Fatigue (grade 3-4, 8%)
Anemia (grade 1-2, 75%)
Anemia (grade 3-4, 15%)
Thrombocytopenia (grade 1-2, 27%)
Thrombocytopenia (grade 3-4, 3%)
Sources:
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Other AEs: Anemia, Anemia...
Other AEs:
Anemia (grade 1-2, 16%)
Anemia (grade 3-4, 18%)
Abdominal discomfort (grade 1-2, 35%)
Abdominal discomfort (grade 3-4, 8%)
Decreased appetite (grade 1-2, 21%)
Decreased appetite (grade 3-4, 1%)
Diarrhea (grade 1-2, 30%)
Diarrhea (grade 3-4, 1%)
Dyspepsia (grade 1-4, 25%)
Asthenia (grade 1-2, 58%)
Asthenia (grade 3-4, 8%)
Nasopharyngitis (grade 1-4, 26%)
Arthralgia (grade 1-4, 21%)
Musculoskeletal pain (grade 1-4, 21%)
Myalgia (grade 1-4, 22%)
Neutropenia (grade 1-2, 18%)
Neutropenia (grade 3-4, 7%)
Lymphopenia (grade 1-2, 39%)
Lymphopenia (grade 3-4, 17%)
Mean corpuscular volume increased (grade 1-4, 57%)
Creatinine increased (grade 1-2, 28%)
Creatinine increased (grade 3-4, 2%)
Cough (10-20)
Constipation (10-20)
Dysgeusia (10-20)
Peripheral edema (10-20)
Back pain (10-20)
Dizziness (10-20)
Headache (10-20)
Urinary tract infection (10-20)
Dyspnea (10-20)
Rash (10-20)
Leukopenia (1-10)
Stomatitis (1-10)
Peripheral neuropathy (1-10)
Pyrexia (1-10)
Hypomagnesemia (1-10)
Hyperglycemia (1-10)
Anxiety (1-10)
Depression (1-10)
Insomnia (1-10)
Dysuria (1-10)
Urinary incontinence (1-10)
Vulvovaginal disorder (1-10)
Dry skin (1-10)
Eczema (1-10)
Pruritis (1-10)
Hypertension (1-10)
Venous thrombosis (1-10)
Hot flush (1-10)
Sources:
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Disc. AE: Myelodysplastic syndrome, Acute myeloid leukemia...
AEs leading to
discontinuation/dose reduction:
Myelodysplastic syndrome (grade 5, <1%)
Acute myeloid leukemia (grade 5, <1%)
Sources:
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Disc. AE: Pneumonitis...
AEs leading to
discontinuation/dose reduction:
Pneumonitis (grade 5, <1%)
Sources:
AEs

AEs

AESignificanceDosePopulation
Neutropenia 9%
Disc. AE
300 mg 2 times / day steady, oral
Recommended
unhealthy
Anemia grade 1-2, 24%
Disc. AE
300 mg 2 times / day steady, oral
Recommended
unhealthy
Vomiting grade 1-2, 34%
Disc. AE
300 mg 2 times / day steady, oral
Recommended
unhealthy
Nausea grade 1-2, 73%
Disc. AE
300 mg 2 times / day steady, oral
Recommended
unhealthy
Anemia grade 3-4, 20%
Disc. AE
300 mg 2 times / day steady, oral
Recommended
unhealthy
Nausea grade 3-4, 3%
Disc. AE
300 mg 2 times / day steady, oral
Recommended
unhealthy
Vomiting grade 3-4, 3%
Disc. AE
300 mg 2 times / day steady, oral
Recommended
unhealthy
Cough <20%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Creatinine increased <20%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Dizziness <20%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Dyspepsia <20%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Edema <20%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Hypomagnesemia <20%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Leukopenia <20%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Lymphopenia <20%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Rash <20%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Thrombocytopenia <20%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Abscess oral grade 1-2, 19%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Aphthous ulcer grade 1-2, 19%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Gingival abscess grade 1-2, 19%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Gingival disorder grade 1-2, 19%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Gingival pain grade 1-2, 19%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Gingivitis grade 1-2, 19%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Mouth ulceration grade 1-2, 19%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Mucosal infection grade 1-2, 19%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Mucosal inflammation grade 1-2, 19%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Oral candidiasis grade 1-2, 19%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Oral discomfort grade 1-2, 19%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Oral herpes grade 1-2, 19%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Oral infection grade 1-2, 19%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Oral mucosal erythema grade 1-2, 19%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Oral pain grade 1-2, 19%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Oropharyngeal discomfort grade 1-2, 19%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Oropharyngeal pain grade 1-2, 19%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Headache grade 1-2, 25%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Diarrhea grade 1-2, 31%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Platelets decreased grade 1-2, 40%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Absolute neutrophil count decreased grade 1-2, 44%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Lymphocyte count low grade 1-2, 56%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Fatigue grade 1-2, 62%
Disc. AE
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Leukocyte count decreased grade 1-2, 64%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Decreased hemoglobin grade 1-2, 66%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Decreased appetite grade 1-4, 22%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Dysgeusia grade 1-4, 27%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Arthralgia grade 1-4, 30%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Myalgia grade 1-4, 30%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Influenza grade 1-4, 36%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Nasopharyngitis grade 1-4, 36%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Rhinitis grade 1-4, 36%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Sinusitis grade 1-4, 36%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Creatinine serum increased grade 1-4, 44%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Mean corpuscular volume increased grade 1-4, 89%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Abscess oral grade 3-4, 1%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Aphthous ulcer grade 3-4, 1%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Gingival abscess grade 3-4, 1%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Gingival disorder grade 3-4, 1%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Gingival pain grade 3-4, 1%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Gingivitis grade 3-4, 1%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Headache grade 3-4, 1%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Mouth ulceration grade 3-4, 1%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Mucosal infection grade 3-4, 1%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Mucosal inflammation grade 3-4, 1%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Oral candidiasis grade 3-4, 1%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Oral discomfort grade 3-4, 1%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Oral herpes grade 3-4, 1%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Oral infection grade 3-4, 1%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Oral mucosal erythema grade 3-4, 1%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Oral pain grade 3-4, 1%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Oropharyngeal discomfort grade 3-4, 1%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Oropharyngeal pain grade 3-4, 1%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Lymphocyte count low grade 3-4, 11%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Decreased hemoglobin grade 3-4, 17%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Diarrhea grade 3-4, 2%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Platelets decreased grade 3-4, 2%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Fatigue grade 3-4, 4%
Disc. AE
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Leukocyte count decreased grade 3-4, 5%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Absolute neutrophil count decreased grade 3-4, 7%
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Acute myeloid leukemia 2 patients
Disc. AE
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Myelodysplastic syndrome 2 patients
Disc. AE
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Thrombocytopenia 9 patients
Disc. AE
300 mg 2 times / day steady, oral
Recommended
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy
Thrombocytopenia grade 1-2, 27%
Disc. AE
400 mg 2 times / day steady, oral
Recommended|MTD
unhealthy
Vomiting grade 1-2, 39%
Disc. AE
400 mg 2 times / day steady, oral
Recommended|MTD
unhealthy
Fatigue grade 1-2, 58%
Disc. AE
400 mg 2 times / day steady, oral
Recommended|MTD
unhealthy
Nausea grade 1-2, 61%
Disc. AE
400 mg 2 times / day steady, oral
Recommended|MTD
unhealthy
Anemia grade 1-2, 75%
Disc. AE
400 mg 2 times / day steady, oral
Recommended|MTD
unhealthy
Anemia grade 3-4, 15%
Disc. AE
400 mg 2 times / day steady, oral
Recommended|MTD
unhealthy
Nausea grade 3-4, 3%
Disc. AE
400 mg 2 times / day steady, oral
Recommended|MTD
unhealthy
Thrombocytopenia grade 3-4, 3%
Disc. AE
400 mg 2 times / day steady, oral
Recommended|MTD
unhealthy
Vomiting grade 3-4, 4%
Disc. AE
400 mg 2 times / day steady, oral
Recommended|MTD
unhealthy
Fatigue grade 3-4, 8%
Disc. AE
400 mg 2 times / day steady, oral
Recommended|MTD
unhealthy
Anxiety 1-10
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Depression 1-10
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Dry skin 1-10
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Dysuria 1-10
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Eczema 1-10
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Hot flush 1-10
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Hyperglycemia 1-10
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Hypertension 1-10
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Hypomagnesemia 1-10
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Insomnia 1-10
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Leukopenia 1-10
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Peripheral neuropathy 1-10
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Pruritis 1-10
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Pyrexia 1-10
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Stomatitis 1-10
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Urinary incontinence 1-10
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Venous thrombosis 1-10
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Vulvovaginal disorder 1-10
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Back pain 10-20
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Constipation 10-20
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Cough 10-20
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Dizziness 10-20
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Dysgeusia 10-20
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Dyspnea 10-20
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Headache 10-20
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Peripheral edema 10-20
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Rash 10-20
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Urinary tract infection 10-20
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Anemia grade 1-2, 16%
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Neutropenia grade 1-2, 18%
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Decreased appetite grade 1-2, 21%
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Creatinine increased grade 1-2, 28%
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Diarrhea grade 1-2, 30%
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Abdominal discomfort grade 1-2, 35%
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Lymphopenia grade 1-2, 39%
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Asthenia grade 1-2, 58%
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Arthralgia grade 1-4, 21%
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Musculoskeletal pain grade 1-4, 21%
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Myalgia grade 1-4, 22%
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Dyspepsia grade 1-4, 25%
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Nasopharyngitis grade 1-4, 26%
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Mean corpuscular volume increased grade 1-4, 57%
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Decreased appetite grade 3-4, 1%
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Diarrhea grade 3-4, 1%
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Lymphopenia grade 3-4, 17%
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Anemia grade 3-4, 18%
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Creatinine increased grade 3-4, 2%
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Neutropenia grade 3-4, 7%
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Abdominal discomfort grade 3-4, 8%
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Asthenia grade 3-4, 8%
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Acute myeloid leukemia grade 5, <1%
Disc. AE
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Myelodysplastic syndrome grade 5, <1%
Disc. AE
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
Pneumonitis grade 5, <1%
Disc. AE
400 mg 2 times / day steady, oral
Recommended|MTD
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no [Inhibition >100 uM]
no [Inhibition >100 uM]
no [Inhibition >100 uM]
no [Inhibition >100 uM]
no [Inhibition >100 uM]
no [Inhibition >100 uM]
no [Inhibition >100 uM]
no [Inhibition >100 uM]
no
no
no
no
no
yes [IC50 18.4 uM]
yes [IC50 19.9 uM]
yes [IC50 20.3 uM]
yes [IC50 37.9 uM]
yes [IC50 47.1 uM]
yes [IC50 5.5 uM]
yes [Inhibition 100 uM]
yes
yes
yes
yes
yes
Drug as victimTox targets

Tox targets

PubMed

PubMed

TitleDatePubMed
Tailored targeted therapy for all: a realistic and worthwhile objective?
2009
Enhanced radiosensitization of human glioma cells by combining inhibition of poly(ADP-ribose) polymerase with inhibition of heat shock protein 90.
2009 Aug
Targeting the molecular defect in BRCA-deficient tumors for cancer therapy.
2009 Aug 4
Inhibition of poly(ADP-ribose) polymerase in tumors from BRCA mutation carriers.
2009 Jul 9
BRCA1/2 genetic background-based therapeutic tailoring of human ovarian cancer: hope or reality?
2009 Oct 13
Recent advances in managing triple-negative breast cancers.
2009 Sep 28
Chemotherapy resistance in metastatic breast cancer: the evolving role of ixabepilone.
2010
Present and future evolution of advanced breast cancer therapy.
2010
Estrogen receptor positive breast cancers in BRCA1 mutation carriers: clinical risk factors and pathologic features.
2010
A current review of targeted therapeutics for ovarian cancer.
2010
The Emerging Role of PARP Inhibitors in the Treatment of Epithelial Ovarian Cancer.
2010
Are current development programs realising the full potential of new agents?
2010 Dec 20
Sensitivity and acquired resistance of BRCA1;p53-deficient mouse mammary tumors to the topoisomerase I inhibitor topotecan.
2010 Feb 15
Sensitization to radiation and alkylating agents by inhibitors of poly(ADP-ribose) polymerase is enhanced in cells deficient in DNA double-strand break repair.
2010 Jun
Society for biomolecular sciences - 16th annual conference & exhibition - advancing the science of drug discovery.
2010 Jun
Multiple roles of BRIT1/MCPH1 in DNA damage response, DNA repair, and cancer suppression.
2010 May
Molecule of the month. Olaparib.
2010 Nov
Targeting poly(ADP-ribose) polymerase activity for cancer therapy.
2010 Nov
The PARP inhibitor olaparib induces significant killing of ATM-deficient lymphoid tumor cells in vitro and in vivo.
2010 Nov 25
Central nervous system penetration and enhancement of temozolomide activity in childhood medulloblastoma models by poly(ADP-ribose) polymerase inhibitor AG-014699.
2010 Nov 9
Targeted therapies: PARP inhibitor olaparib is safe and effective in patients with BRCA1 and BRCA2 mutations.
2010 Oct
Cooperation of breast cancer proteins PALB2 and piccolo BRCA2 in stimulating homologous recombination.
2010 Oct
New developments in treatment of ovarian carcinoma: focus on trabectedin.
2010 Oct 1
Treatment options for patients with triple-negative breast cancer.
2010 Oct 27
Favorable response to doxorubicin combination chemotherapy does not yield good clinical outcome in patients with metastatic breast cancer with triple-negative phenotype.
2010 Oct 5
Gateways to clinical trials.
2010 Sep
Checkpoint signaling, base excision repair, and PARP promote survival of colon cancer cells treated with 5-fluorodeoxyuridine but not 5-fluorouracil.
2011
5-Benzamidoisoquinolin-1-ones and 5-(ω-carboxyalkyl)isoquinolin-1-ones as isoform-selective inhibitors of poly(ADP-ribose) polymerase 2 (PARP-2).
2011 Apr 14
Identification of human triple-negative breast cancer subtypes and preclinical models for selection of targeted therapies.
2011 Jul
BAP1 loss defines a new class of renal cell carcinoma.
2012 Jun 10
Trapping of PARP1 and PARP2 by Clinical PARP Inhibitors.
2012 Nov 1
Lessons learned from the fate of AstraZeneca's drug pipeline: a five-dimensional framework.
2014 Jun
5-Fluorouracil-induced RNA stress engages a TRAIL-DISC-dependent apoptosis axis facilitated by p53.
2015 Dec 22
DNA-Repair Defects and Olaparib in Metastatic Prostate Cancer.
2015 Oct 29
Patents

Sample Use Guides

400 mg (eight 50 mg capsules) taken twice daily, for a total daily dose of 800 mg. Continue treatment until disease progression or unacceptable toxicity.
Route of Administration: Oral
30-100 nM in SW620 cells
Name Type Language
OLAPARIB
DASH   INN   MART.   MI   USAN   VANDF   WHO-DD  
USAN   INN  
Official Name English
AZD2281
Code English
KEYLYNK-010 COMPONENT OLAPARIB
Code English
OLAPARIB [USAN]
Common Name English
OLAPARIB [ORANGE BOOK]
Common Name English
OLAPARIB [WHO-DD]
Common Name English
NSC-747856
Code English
OLAPARIB [JAN]
Common Name English
AZ2281
Code English
OLAPARIB [VANDF]
Common Name English
KU-0059436
Code English
OLAPARIB [INN]
Common Name English
1(2H)-PHTHALAZINONE, 4-((3-((4-(CYCLOPROPYLCARBONYL)-1-PIPERAZINYL)CARBONYL)-4-FLUOROPHENYL)METHYL)-
Systematic Name English
PIPERAZINE, 1-(CYCLOPROPYLCARBONYL)-4-(5-((3,4-DIHYDRO-4-OXO-1-PHTHALAZINYL)METHYL)-2-FLUOROBENZOYL)-
Systematic Name English
LYNPARZA
Brand Name English
4-((3-((4-(CYCLOPROPYLCARBONYL)PIPERAZIN-1-YL)CARBONYL)-4-FLUOROPHENYL)METHYL)PHTHALAZIN-1(2H)-ONE
Systematic Name English
AZD-2281
Code English
OLAPARIB [MI]
Common Name English
KU-59436
Code English
OLAPARIB COMPONENT OF KEYLYNK-010
Code English
OLAPARIB [MART.]
Common Name English
AZ-2281
Code English
Classification Tree Code System Code
NDF-RT N0000191623
Created by admin on Fri Jun 25 21:54:31 UTC 2021 , Edited by admin on Fri Jun 25 21:54:31 UTC 2021
EMA ASSESSMENT REPORTS LYNPARZA (AUTHORIZED: OVARIAN NEOPLASMS)
Created by admin on Fri Jun 25 21:54:31 UTC 2021 , Edited by admin on Fri Jun 25 21:54:31 UTC 2021
FDA ORPHAN DRUG 417613
Created by admin on Fri Jun 25 21:54:31 UTC 2021 , Edited by admin on Fri Jun 25 21:54:31 UTC 2021
EU-Orphan Drug EU/3/07/501
Created by admin on Fri Jun 25 21:54:31 UTC 2021 , Edited by admin on Fri Jun 25 21:54:31 UTC 2021
FDA ORPHAN DRUG 409213
Created by admin on Fri Jun 25 21:54:31 UTC 2021 , Edited by admin on Fri Jun 25 21:54:31 UTC 2021
WHO-ATC L01XX46
Created by admin on Fri Jun 25 21:54:31 UTC 2021 , Edited by admin on Fri Jun 25 21:54:31 UTC 2021
FDA ORPHAN DRUG 655318
Created by admin on Fri Jun 25 21:54:31 UTC 2021 , Edited by admin on Fri Jun 25 21:54:31 UTC 2021
NCI_THESAURUS C62554
Created by admin on Fri Jun 25 21:54:31 UTC 2021 , Edited by admin on Fri Jun 25 21:54:31 UTC 2021
FDA ORPHAN DRUG 419013
Created by admin on Fri Jun 25 21:54:31 UTC 2021 , Edited by admin on Fri Jun 25 21:54:31 UTC 2021
Code System Code Type Description
EVMPD
SUB32234
Created by admin on Fri Jun 25 21:54:31 UTC 2021 , Edited by admin on Fri Jun 25 21:54:31 UTC 2021
PRIMARY
MERCK INDEX
M8185
Created by admin on Fri Jun 25 21:54:31 UTC 2021 , Edited by admin on Fri Jun 25 21:54:31 UTC 2021
PRIMARY Merck Index
ChEMBL
CHEMBL521686
Created by admin on Fri Jun 25 21:54:31 UTC 2021 , Edited by admin on Fri Jun 25 21:54:31 UTC 2021
PRIMARY
DRUG CENTRAL
4907
Created by admin on Fri Jun 25 21:54:31 UTC 2021 , Edited by admin on Fri Jun 25 21:54:31 UTC 2021
PRIMARY
NCI_THESAURUS
C71721
Created by admin on Fri Jun 25 21:54:31 UTC 2021 , Edited by admin on Fri Jun 25 21:54:31 UTC 2021
PRIMARY
INN
8685
Created by admin on Fri Jun 25 21:54:31 UTC 2021 , Edited by admin on Fri Jun 25 21:54:31 UTC 2021
PRIMARY
RXCUI
1597582
Created by admin on Fri Jun 25 21:54:31 UTC 2021 , Edited by admin on Fri Jun 25 21:54:31 UTC 2021
PRIMARY RxNorm
IUPHAR
7519
Created by admin on Fri Jun 25 21:54:31 UTC 2021 , Edited by admin on Fri Jun 25 21:54:31 UTC 2021
PRIMARY
FDA UNII
WOH1JD9AR8
Created by admin on Fri Jun 25 21:54:31 UTC 2021 , Edited by admin on Fri Jun 25 21:54:31 UTC 2021
PRIMARY
CAS
763113-22-0
Created by admin on Fri Jun 25 21:54:31 UTC 2021 , Edited by admin on Fri Jun 25 21:54:31 UTC 2021
PRIMARY
PUBCHEM
23725625
Created by admin on Fri Jun 25 21:54:31 UTC 2021 , Edited by admin on Fri Jun 25 21:54:31 UTC 2021
PRIMARY
DRUG BANK
DB09074
Created by admin on Fri Jun 25 21:54:31 UTC 2021 , Edited by admin on Fri Jun 25 21:54:31 UTC 2021
PRIMARY
MESH
C531550
Created by admin on Fri Jun 25 21:54:31 UTC 2021 , Edited by admin on Fri Jun 25 21:54:31 UTC 2021
PRIMARY
LACTMED
Olaparib
Created by admin on Fri Jun 25 21:54:31 UTC 2021 , Edited by admin on Fri Jun 25 21:54:31 UTC 2021
PRIMARY
WIKIPEDIA
OLAPARIB
Created by admin on Fri Jun 25 21:54:31 UTC 2021 , Edited by admin on Fri Jun 25 21:54:31 UTC 2021
PRIMARY
NDF-RT
N0000191622
Created by admin on Fri Jun 25 21:54:31 UTC 2021 , Edited by admin on Fri Jun 25 21:54:31 UTC 2021
PRIMARY Poly(ADP-Ribose) Polymerase Inhibitors [MoA]