Details
Stereochemistry | ACHIRAL |
Molecular Formula | C24H23FN4O3 |
Molecular Weight | 434.4628 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
FC1=CC=C(CC2=NNC(=O)C3=C2C=CC=C3)C=C1C(=O)N4CCN(CC4)C(=O)C5CC5
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)
Molecular Formula | C24H23FN4O3 |
Molecular Weight | 434.4628 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionCurator's Comment: Description was created based on several sources, including:
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4880823/
Curator's Comment: Description was created based on several sources, including:
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4880823/
Olaparib is an oral inhibitor of poly (ADP-ribose) polymerase enzymes, including PARP1, PARP2, and PARP3 which are involved in normal cellular homeostasis, such as DNA transcription, cell cycle regulation, and DNA 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.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: P09874 Gene ID: 142.0 Gene Symbol: PARP1 Target Organism: Homo sapiens (Human) Sources: http://www.ncbi.nlm.nih.gov/pubmed/27487106 |
1.94 nM [IC50] | ||
Target ID: Q9UGN5 Gene ID: 10038.0 Gene Symbol: PARP2 Target Organism: Homo sapiens (Human) Sources: http://www.ncbi.nlm.nih.gov/pubmed/27487106 |
|||
Target ID: Q9Y6F1 Gene ID: 10039.0 Gene Symbol: PARP3 Target Organism: Homo sapiens (Human) Sources: http://www.ncbi.nlm.nih.gov/pubmed/27487106 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | LYNPARZA Approved UseMonotherapy 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 Date2014 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
6.875 ug/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT02430311 |
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: |
|
6.88 μg/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/30887180 |
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 |
|
2.97 μg/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/30887180 |
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 |
|
8.27 μg/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/30887180 |
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 |
|
3.75 μg/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/30887180 |
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 |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
43.95 ug*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT02430311 |
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: |
|
43.91 ug*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT02430311 |
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: |
|
31.68 ug*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT02430311 |
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: |
|
36.37 ug*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT02430311 |
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 Clinical Trial https://clinicaltrials.gov/ct2/show/NCT02430311 |
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: |
|
31.7 μg × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/30887180 |
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 |
|
10.9 μg × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/30887180 |
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 |
|
44 μg × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/30887180 |
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 |
|
16.7 μg × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/30887180 |
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 |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
6.52 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/30887180 |
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 |
|
7.17 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/30887180 |
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 |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
18% |
OLAPARIB plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse 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 Health Status: unhealthy 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: Anemia, Anemia... AEs leading to discontinuation/dose reduction: Anemia (grade 1-2, 24%) Sources: 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%) |
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 Health Status: unhealthy Sources: |
Disc. AE: Fatigue, Fatigue... Other AEs: Diarrhea, Diarrhea... AEs leading to discontinuation/dose reduction: Fatigue (grade 1-2, 62%) Other AEs:Fatigue (grade 3-4, 4%) Diarrhea (grade 1-2, 31%) Sources: 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%) |
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 Health Status: unhealthy Sources: |
Disc. AE: Thrombocytopenia, Myelodysplastic syndrome... AEs leading to discontinuation/dose reduction: Thrombocytopenia (9 patients) Sources: Myelodysplastic syndrome (2 patients) Acute myeloid leukemia (2 patients) |
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: Nausea, Nausea... AEs leading to discontinuation/dose reduction: Nausea (grade 1-2, 61%) Sources: 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%) |
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 Health Status: unhealthy Sources: |
Disc. AE: Myelodysplastic syndrome, Acute myeloid leukemia... AEs leading to discontinuation/dose reduction: Myelodysplastic syndrome (grade 5, <1%) Sources: Acute myeloid leukemia (grade 5, <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 Health Status: unhealthy Sources: |
Disc. AE: Pneumonitis... AEs leading to discontinuation/dose reduction: Pneumonitis (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 Health Status: unhealthy Sources: |
Other AEs: Anemia, Anemia... Other AEs: Anemia (grade 1-2, 16%) Sources: 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) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Neutropenia | 9% 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 |
Anemia | grade 1-2, 24% 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 |
Vomiting | grade 1-2, 34% 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 |
Nausea | grade 1-2, 73% 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 |
Anemia | grade 3-4, 20% 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 |
Nausea | grade 3-4, 3% 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 |
Vomiting | grade 3-4, 3% 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 |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
Thrombocytopenia | grade 1-2, 27% 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 |
Vomiting | grade 1-2, 39% 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 |
Fatigue | grade 1-2, 58% 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 |
Nausea | grade 1-2, 61% 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 |
Anemia | grade 1-2, 75% 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 |
Anemia | grade 3-4, 15% 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 |
Nausea | grade 3-4, 3% 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 |
Thrombocytopenia | grade 3-4, 3% 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 |
Vomiting | grade 3-4, 4% 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 |
Fatigue | grade 3-4, 8% 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 |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
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 Health Status: unhealthy Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical 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 victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
no | ||||
yes | ||||
yes | ||||
yes | ||||
yes | yes (co-administration study) Comment: Itraconazole (strong CYP3A inhibitor) increased the AUC of olaparib by 2.7-fold and PBPK modeling predicted that fluconazole (moderate CYP3A inhibitor) would likely increase olaparib AUC by 2-fold. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/206162Orig1s000ClinPharmR.pdf#page=4 Page: - |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
PubMed
Title | Date | PubMed |
---|---|---|
Enhanced radiosensitization of human glioma cells by combining inhibition of poly(ADP-ribose) polymerase with inhibition of heat shock protein 90. | 2009 Aug |
|
Triple-negative breast cancer: novel therapies and new directions. | 2009 Aug 20 |
|
Targeting the molecular defect in BRCA-deficient tumors for cancer therapy. | 2009 Aug 4 |
|
Converting cancer mutations into therapeutic opportunities. | 2009 Sep |
|
Prevalence and predictors of loss of wild type BRCA1 in estrogen receptor positive and negative BRCA1-associated breast cancers. | 2010 |
|
Chemotherapy resistance in metastatic breast cancer: the evolving role of ixabepilone. | 2010 |
|
Targeted therapies in epithelial ovarian cancer. | 2010 |
|
A current review of targeted therapeutics for ovarian cancer. | 2010 |
|
PARP inhibitors in BRCA1/BRCA2 germline mutation carriers with ovarian and breast cancer. | 2010 Feb 11 |
|
A high-throughput pharmaceutical screen identifies compounds with specific toxicity against BRCA2-deficient tumors. | 2010 Jan 1 |
|
Society for biomolecular sciences - 16th annual conference & exhibition - advancing the science of drug discovery. | 2010 Jun |
|
Poly(adp-ribose) polymerase inhibitors: a novel drug class with a promising future. | 2010 Mar-Apr |
|
New developments in treatment of ovarian carcinoma: focus on trabectedin. | 2010 Oct 1 |
|
Role for the mammalian Swi5-Sfr1 complex in DNA strand break repair through homologous recombination. | 2010 Oct 14 |
|
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 |
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
In Vitro Use Guide
Sources: http://www.ncbi.nlm.nih.gov/pubmed/?term=18800822
30-100 nM in SW620 cells
Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 18:03:40 GMT 2025
by
admin
on
Mon Mar 31 18:03:40 GMT 2025
|
Record UNII |
WOH1JD9AR8
|
Record Status |
Validated (UNII)
|
Record Version |
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-
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Common Name | English | ||
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Systematic Name | English | ||
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Classification Tree | Code System | Code | ||
---|---|---|---|---|
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NDF-RT |
N0000191623
Created by
admin on Mon Mar 31 18:03:40 GMT 2025 , Edited by admin on Mon Mar 31 18:03:40 GMT 2025
|
||
|
EMA ASSESSMENT REPORTS |
LYNPARZA (AUTHORIZED: OVARIAN NEOPLASMS)
Created by
admin on Mon Mar 31 18:03:40 GMT 2025 , Edited by admin on Mon Mar 31 18:03:40 GMT 2025
|
||
|
FDA ORPHAN DRUG |
419013
Created by
admin on Mon Mar 31 18:03:40 GMT 2025 , Edited by admin on Mon Mar 31 18:03:40 GMT 2025
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||
|
FDA ORPHAN DRUG |
417613
Created by
admin on Mon Mar 31 18:03:40 GMT 2025 , Edited by admin on Mon Mar 31 18:03:40 GMT 2025
|
||
|
EU-Orphan Drug |
EU/3/07/501
Created by
admin on Mon Mar 31 18:03:40 GMT 2025 , Edited by admin on Mon Mar 31 18:03:40 GMT 2025
|
||
|
FDA ORPHAN DRUG |
409213
Created by
admin on Mon Mar 31 18:03:40 GMT 2025 , Edited by admin on Mon Mar 31 18:03:40 GMT 2025
|
||
|
WHO-ATC |
L01XX46
Created by
admin on Mon Mar 31 18:03:40 GMT 2025 , Edited by admin on Mon Mar 31 18:03:40 GMT 2025
|
||
|
FDA ORPHAN DRUG |
655318
Created by
admin on Mon Mar 31 18:03:40 GMT 2025 , Edited by admin on Mon Mar 31 18:03:40 GMT 2025
|
||
|
NCI_THESAURUS |
C62554
Created by
admin on Mon Mar 31 18:03:40 GMT 2025 , Edited by admin on Mon Mar 31 18:03:40 GMT 2025
|
Code System | Code | Type | Description | ||
---|---|---|---|---|---|
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WOH1JD9AR8
Created by
admin on Mon Mar 31 18:03:40 GMT 2025 , Edited by admin on Mon Mar 31 18:03:40 GMT 2025
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PRIMARY | |||
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SUB32234
Created by
admin on Mon Mar 31 18:03:40 GMT 2025 , Edited by admin on Mon Mar 31 18:03:40 GMT 2025
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PRIMARY | |||
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100000124466
Created by
admin on Mon Mar 31 18:03:40 GMT 2025 , Edited by admin on Mon Mar 31 18:03:40 GMT 2025
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PRIMARY | |||
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m8185
Created by
admin on Mon Mar 31 18:03:40 GMT 2025 , Edited by admin on Mon Mar 31 18:03:40 GMT 2025
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PRIMARY | Merck Index | ||
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CHEMBL521686
Created by
admin on Mon Mar 31 18:03:40 GMT 2025 , Edited by admin on Mon Mar 31 18:03:40 GMT 2025
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4907
Created by
admin on Mon Mar 31 18:03:40 GMT 2025 , Edited by admin on Mon Mar 31 18:03:40 GMT 2025
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C71721
Created by
admin on Mon Mar 31 18:03:40 GMT 2025 , Edited by admin on Mon Mar 31 18:03:40 GMT 2025
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747856
Created by
admin on Mon Mar 31 18:03:40 GMT 2025 , Edited by admin on Mon Mar 31 18:03:40 GMT 2025
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8685
Created by
admin on Mon Mar 31 18:03:40 GMT 2025 , Edited by admin on Mon Mar 31 18:03:40 GMT 2025
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1597582
Created by
admin on Mon Mar 31 18:03:40 GMT 2025 , Edited by admin on Mon Mar 31 18:03:40 GMT 2025
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PRIMARY | RxNorm | ||
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7519
Created by
admin on Mon Mar 31 18:03:40 GMT 2025 , Edited by admin on Mon Mar 31 18:03:40 GMT 2025
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WOH1JD9AR8
Created by
admin on Mon Mar 31 18:03:40 GMT 2025 , Edited by admin on Mon Mar 31 18:03:40 GMT 2025
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763113-22-0
Created by
admin on Mon Mar 31 18:03:40 GMT 2025 , Edited by admin on Mon Mar 31 18:03:40 GMT 2025
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23725625
Created by
admin on Mon Mar 31 18:03:40 GMT 2025 , Edited by admin on Mon Mar 31 18:03:40 GMT 2025
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DB09074
Created by
admin on Mon Mar 31 18:03:40 GMT 2025 , Edited by admin on Mon Mar 31 18:03:40 GMT 2025
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C531550
Created by
admin on Mon Mar 31 18:03:40 GMT 2025 , Edited by admin on Mon Mar 31 18:03:40 GMT 2025
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83766
Created by
admin on Mon Mar 31 18:03:40 GMT 2025 , Edited by admin on Mon Mar 31 18:03:40 GMT 2025
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Olaparib
Created by
admin on Mon Mar 31 18:03:40 GMT 2025 , Edited by admin on Mon Mar 31 18:03:40 GMT 2025
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OLAPARIB
Created by
admin on Mon Mar 31 18:03:40 GMT 2025 , Edited by admin on Mon Mar 31 18:03:40 GMT 2025
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DTXSID60917988
Created by
admin on Mon Mar 31 18:03:40 GMT 2025 , Edited by admin on Mon Mar 31 18:03:40 GMT 2025
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N0000191622
Created by
admin on Mon Mar 31 18:03:40 GMT 2025 , Edited by admin on Mon Mar 31 18:03:40 GMT 2025
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PRIMARY | Poly(ADP-Ribose) Polymerase Inhibitors [MoA] | ||
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BC-28
Created by
admin on Mon Mar 31 18:03:40 GMT 2025 , Edited by admin on Mon Mar 31 18:03:40 GMT 2025
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PRIMARY |
Related Record | Type | Details | ||
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SOLVATE->ANHYDROUS |
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METABOLIC ENZYME -> SUBSTRATE |
MAJOR
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TRANSPORTER -> SUBSTRATE |
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EXCRETED UNCHANGED |
FECAL
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TRANSPORTER -> INHIBITOR |
INHIBITOR
IC50
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TRANSPORTER -> INHIBITOR |
The clinical relevance of these findings is unknown.
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BINDER->LIGAND |
BINDING
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SALT/SOLVATE -> PARENT |
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TRANSPORTER -> INHIBITOR |
INHIBITOR
IC50
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TRANSPORTER -> INHIBITOR |
INHIBITOR
IC50
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TRANSPORTER -> INHIBITOR |
INHIBITOR
IC50
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EXCRETED UNCHANGED |
URINE
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TRANSPORTER -> INHIBITOR |
INHIBITOR
IC50
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METABOLIC ENZYME -> INHIBITOR |
Inhibitor at higher concentrations than are clinically achieved.
MINOR
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TRANSPORTER -> INHIBITOR |
INHIBITOR
IC50
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SOLVATE->ANHYDROUS | |||
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TARGET -> INHIBITOR | |||
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TRANSPORTER -> INHIBITOR |
INHIBITOR
IC50
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SALT/SOLVATE -> PARENT |
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
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Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Volume of Distribution | PHARMACOKINETIC |
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Tmax | PHARMACOKINETIC |
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Biological Half-life | PHARMACOKINETIC |
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