Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C19H20N4O |
Molecular Weight | 320.3883 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
NC(=O)C1=CC=CC2=CN(N=C12)C3=CC=C(C=C3)[C@@H]4CCCNC4
InChI
InChIKey=PCHKPVIQAHNQLW-CQSZACIVSA-N
InChI=1S/C19H20N4O/c20-19(24)17-5-1-3-15-12-23(22-18(15)17)16-8-6-13(7-9-16)14-4-2-10-21-11-14/h1,3,5-9,12,14,21H,2,4,10-11H2,(H2,20,24)/t14-/m1/s1
Molecular Formula | C19H20N4O |
Molecular Weight | 320.3883 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
DescriptionSources: http://adisinsight.springer.com/drugs/800028881Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/19873981 | https://www.ncbi.nlm.nih.gov/pubmed/25761096
Sources: http://adisinsight.springer.com/drugs/800028881
Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/19873981 | https://www.ncbi.nlm.nih.gov/pubmed/25761096
Niraparib (MK-4827) displays excellent PARP 1 and 2 inhibition. Inhibition of PARP in the context of defects in other DNA repair mechanisms provide a tumor specific way to kill cancer cells. Niraparib is in development with TESARO, under licence from Merck & Co, for the treatment of cancers (ovarian, fallopian tube and peritoneal cancer, breast cancer, prostate cancer and Ewing's sarcoma). Niraparib was characterized in a number of preclinical models before moving to phase I clinical trials, where it showed excellent human pharmacokinetics suitable for once a day oral dosing, achieved its pharmacodynamic target for PARP inhibition, and had promising activity in cancer patients. It is currently being tested in phase 3 clinical trials as maintenance therapy in ovarian cancer and as a treatment for breast cancer.
CNS Activity
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23482742 | http://mct.aacrjournals.org/content/14/12_Supplement_2/B168
Curator's Comment: Niraparib is able to penetrate the brain in rodents. No human data available.
Originator
Sources: http://adisinsight.springer.com/drugs/800028881
Curator's Comment: # Merck & Co. Inc.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL3105 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19873981 |
3.8 nM [IC50] | ||
Target ID: CHEMBL5366 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19873981 |
2.1 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | ZEJULA Approved UseZEJULA is a poly(ADP-ribose) polymerase (PARP) inhibitor indicated for the maintenance treatment of adult patients with recurrent epithelial
ovarian, fallopian tube, or primary peritoneal cancer who are in a complete or partial response to platinum-based chemotherapy. Launch Date2017 |
|||
Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
803.7 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/29322231 |
300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered: |
NIRAPARIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
804 ng/mL |
300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered: |
NIRAPARIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
29016.1 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/29322231 |
300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered: |
NIRAPARIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
50.5 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/29322231 |
300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered: |
NIRAPARIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
17% |
300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered: |
NIRAPARIB plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Doses
Dose | Population | Adverse events |
---|---|---|
400 mg 1 times / day steady, oral Highest studied dose Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: |
unhealthy, 59 years (range: 39–75 years) n = 6 Health Status: unhealthy Condition: advanced solid tumours Age Group: 59 years (range: 39–75 years) Sex: M+F Population Size: 6 Sources: |
DLT: Thrombocytopenia... Other AEs: Neutropenia, Neutropenia... Dose limiting toxicities: Thrombocytopenia (grade 4, 2 patients) Other AEs:Neutropenia (grade 1-2, 3 patients) Sources: Neutropenia (grade 3, 1 patient) Lymphopenia (grade 3, 1 patient) Nausea (grade 1-2, 3 patients) Vomiting (grade 1-2, 3 patients) Constipation (grade 1-2, 2 patients) Anorexia (grade 1-2, 2 patients) Fatigue (grade 1-2, 4 patients) Insomnia (grade 1-2, 2 patients) |
30 mg 1 times / day steady, oral Dose: 30 mg, 1 times / day Route: oral Route: steady Dose: 30 mg, 1 times / day Sources: |
unhealthy, 59 years (range: 39–75 years) n = 6 Health Status: unhealthy Condition: advanced solid tumours Age Group: 59 years (range: 39–75 years) Sex: M+F Population Size: 6 Sources: |
DLT: Fatigue... Dose limiting toxicities: Fatigue (grade 3, 1 patient) Sources: |
60 mg 1 times / day steady, oral Dose: 60 mg, 1 times / day Route: oral Route: steady Dose: 60 mg, 1 times / day Sources: |
unhealthy, 59 years (range: 39–75 years) n = 7 Health Status: unhealthy Condition: advanced solid tumours Age Group: 59 years (range: 39–75 years) Sex: M+F Population Size: 7 Sources: |
DLT: Pneumonitis... Dose limiting toxicities: Pneumonitis (grade 3, 1 patient) Sources: |
300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Disc. AE: Thrombocytopenia, Anemia... Other AEs: Thrombocytopenia, Thrombocytopenia... AEs leading to discontinuation/dose reduction: Thrombocytopenia (3%) Other AEs:Anemia (1%) Neutropenia (2%) Hypertension (<1%) Myelodysplastic syndrome (grade 5, 1 patient) Thrombocytopenia (grade 1-2, 32%) Sources: Thrombocytopenia (grade 3-4, 29%) Anemia (grade 1-2, 25%) Anemia (grade 3-4, 25%) Neutropenia (grade 1-2, 10%) Neutropenia (grade 3-4, 20%) Leukopenia (grade 1-2, 12%) Leukopenia (grade 3-4, 5%) Palpitations (grade 1-2, 10%) Nausea (grade 1-2, 71%) Nausea (grade 3-4, 3%) Abdominal distension (grade 1-2, 31%) Abdominal distension (grade 3-4, 2%) Vomiting (grade 1-2, 32%) Vomiting (grade 3-4, 2%) Constipation (grade 1-2, 39.2%) Constipation (grade 3-4, 0.8%) Mucositis (grade 1-2, 19.5%) Mucositis (grade 3-4, 0.5%) Stomatitis (grade 1-2, 19.5%) Stomatitis (grade 3-4, 0.5%) Diarrhea (grade 1-2, 19.7%) Diarrhea (grade 3-4, 0.3%) Dyspepsia (grade 1-2, 18%) Dry mouth (grade 1-2, 9.7%) Dry mouth (grade 3-4, 0.3%) Fatigue (grade 1-2, 49%) Fatigue (grade 1-2, 49%) Asthenia (grade 3-4, 8%) Asthenia (grade 3-4, 8%) Decreased appetite (grade 1-2, 24.7%) Decreased appetite (grade 3-4, 0.3%) Urinary tract infection (grade 1-2, 12.2%) Urinary tract infection (grade 3-4, 0.8%) Aspartate aminotransferase increased (grade 1-2, 6%) Aspartate aminotransferase increased (grade 3-4, 4%) Alanine aminotransferase increase (grade 1-2, 6%) Alanine aminotransferase increase (grade 3-4, 4%) Myalgia (grade 1-2, 18.2%) Myalgia (grade 3-4, 0.8%) Back pain (grade 1-2, 17.2%) Back pain (grade 3-4, 0.8%) Arthralgia (grade 1-2, 12.7%) Arthralgia (grade 3-4, 0.3%) Headache (grade 1-2, 25.7%) Headache (grade 3-4, 0.3%) Dizziness (grade 1-2, 18%) Dysgeusia (grade 1-2, 10%) Insomnia (grade 1-2, 26.7%) Insomnia (grade 3-4, 0.3%) Anxiety (grade 1-2, 10.7%) Anxiety (grade 3-4, 0.3%) Nasopharyngitis (grade 1-2, 23%) Dyspnea (grade 1-2, 19%) Dyspnea (grade 3-4, 1%) Cough (grade 1-2, 16%) Rash (grade 1-2, 20.5%) Rash (grade 3-4, 0.5%) Hypertension (grade 1-2, 11%) Hypertension (grade 3-4, 9%) Decreased hemoglobin (grade 1-2, 60%) Decreased hemoglobin (grade 3-4, 25%) Platelet count decreased (grade 1-2, 37%) Platelet count decreased (grade 3-4, 35%) WBC decreased (grade 1-2, 59%) WBC decreased (grade 3-4, 7%) Absolute neutrophil count decreased (grade 1-2, 32%) Absolute neutrophil count decreased (grade 3-4, 21%) Myelodysplastic syndrome (all grades, 1.4%) Tachycardia (1-10) Peripheral edema (1-10) Hypokalemia (1-10) Bronchitis (1-10) Conjunctivitis (1-10) Gamma-glutamyltransferase increased (1-10) Blood creatinine increased (1-10) Blood alkaline phosphatase increased (1-10) Weight decreased (1-10) Depression (1-10) Epistaxis (1-10) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Anorexia | grade 1-2, 2 patients | 400 mg 1 times / day steady, oral Highest studied dose Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: |
unhealthy, 59 years (range: 39–75 years) n = 6 Health Status: unhealthy Condition: advanced solid tumours Age Group: 59 years (range: 39–75 years) Sex: M+F Population Size: 6 Sources: |
Constipation | grade 1-2, 2 patients | 400 mg 1 times / day steady, oral Highest studied dose Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: |
unhealthy, 59 years (range: 39–75 years) n = 6 Health Status: unhealthy Condition: advanced solid tumours Age Group: 59 years (range: 39–75 years) Sex: M+F Population Size: 6 Sources: |
Insomnia | grade 1-2, 2 patients | 400 mg 1 times / day steady, oral Highest studied dose Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: |
unhealthy, 59 years (range: 39–75 years) n = 6 Health Status: unhealthy Condition: advanced solid tumours Age Group: 59 years (range: 39–75 years) Sex: M+F Population Size: 6 Sources: |
Nausea | grade 1-2, 3 patients | 400 mg 1 times / day steady, oral Highest studied dose Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: |
unhealthy, 59 years (range: 39–75 years) n = 6 Health Status: unhealthy Condition: advanced solid tumours Age Group: 59 years (range: 39–75 years) Sex: M+F Population Size: 6 Sources: |
Neutropenia | grade 1-2, 3 patients | 400 mg 1 times / day steady, oral Highest studied dose Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: |
unhealthy, 59 years (range: 39–75 years) n = 6 Health Status: unhealthy Condition: advanced solid tumours Age Group: 59 years (range: 39–75 years) Sex: M+F Population Size: 6 Sources: |
Vomiting | grade 1-2, 3 patients | 400 mg 1 times / day steady, oral Highest studied dose Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: |
unhealthy, 59 years (range: 39–75 years) n = 6 Health Status: unhealthy Condition: advanced solid tumours Age Group: 59 years (range: 39–75 years) Sex: M+F Population Size: 6 Sources: |
Fatigue | grade 1-2, 4 patients | 400 mg 1 times / day steady, oral Highest studied dose Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: |
unhealthy, 59 years (range: 39–75 years) n = 6 Health Status: unhealthy Condition: advanced solid tumours Age Group: 59 years (range: 39–75 years) Sex: M+F Population Size: 6 Sources: |
Lymphopenia | grade 3, 1 patient | 400 mg 1 times / day steady, oral Highest studied dose Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: |
unhealthy, 59 years (range: 39–75 years) n = 6 Health Status: unhealthy Condition: advanced solid tumours Age Group: 59 years (range: 39–75 years) Sex: M+F Population Size: 6 Sources: |
Neutropenia | grade 3, 1 patient | 400 mg 1 times / day steady, oral Highest studied dose Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: |
unhealthy, 59 years (range: 39–75 years) n = 6 Health Status: unhealthy Condition: advanced solid tumours Age Group: 59 years (range: 39–75 years) Sex: M+F Population Size: 6 Sources: |
Thrombocytopenia | grade 4, 2 patients DLT, Disc. AE |
400 mg 1 times / day steady, oral Highest studied dose Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: |
unhealthy, 59 years (range: 39–75 years) n = 6 Health Status: unhealthy Condition: advanced solid tumours Age Group: 59 years (range: 39–75 years) Sex: M+F Population Size: 6 Sources: |
Fatigue | grade 3, 1 patient DLT |
30 mg 1 times / day steady, oral Dose: 30 mg, 1 times / day Route: oral Route: steady Dose: 30 mg, 1 times / day Sources: |
unhealthy, 59 years (range: 39–75 years) n = 6 Health Status: unhealthy Condition: advanced solid tumours Age Group: 59 years (range: 39–75 years) Sex: M+F Population Size: 6 Sources: |
Pneumonitis | grade 3, 1 patient DLT |
60 mg 1 times / day steady, oral Dose: 60 mg, 1 times / day Route: oral Route: steady Dose: 60 mg, 1 times / day Sources: |
unhealthy, 59 years (range: 39–75 years) n = 7 Health Status: unhealthy Condition: advanced solid tumours Age Group: 59 years (range: 39–75 years) Sex: M+F Population Size: 7 Sources: |
Anemia | 1% Disc. AE |
300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Blood alkaline phosphatase increased | 1-10 | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Blood creatinine increased | 1-10 | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Bronchitis | 1-10 | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Conjunctivitis | 1-10 | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Depression | 1-10 | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Epistaxis | 1-10 | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Gamma-glutamyltransferase increased | 1-10 | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Hypokalemia | 1-10 | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Peripheral edema | 1-10 | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Tachycardia | 1-10 | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Weight decreased | 1-10 | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Neutropenia | 2% Disc. AE |
300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Thrombocytopenia | 3% Disc. AE |
300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Hypertension | <1% Disc. AE |
300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Myelodysplastic syndrome | all grades, 1.4% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Dysgeusia | grade 1-2, 10% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Neutropenia | grade 1-2, 10% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Palpitations | grade 1-2, 10% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Anxiety | grade 1-2, 10.7% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Hypertension | grade 1-2, 11% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Leukopenia | grade 1-2, 12% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Urinary tract infection | grade 1-2, 12.2% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Arthralgia | grade 1-2, 12.7% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Cough | grade 1-2, 16% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Back pain | grade 1-2, 17.2% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Dizziness | grade 1-2, 18% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Dyspepsia | grade 1-2, 18% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Myalgia | grade 1-2, 18.2% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Dyspnea | grade 1-2, 19% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Mucositis | grade 1-2, 19.5% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Stomatitis | grade 1-2, 19.5% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Diarrhea | grade 1-2, 19.7% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Rash | grade 1-2, 20.5% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Nasopharyngitis | grade 1-2, 23% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Decreased appetite | grade 1-2, 24.7% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Anemia | grade 1-2, 25% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Headache | grade 1-2, 25.7% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Insomnia | grade 1-2, 26.7% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Abdominal distension | grade 1-2, 31% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Absolute neutrophil count decreased | grade 1-2, 32% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Thrombocytopenia | grade 1-2, 32% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Vomiting | grade 1-2, 32% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Platelet count decreased | grade 1-2, 37% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Constipation | grade 1-2, 39.2% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Fatigue | grade 1-2, 49% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Fatigue | grade 1-2, 49% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
WBC decreased | grade 1-2, 59% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Alanine aminotransferase increase | grade 1-2, 6% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Aspartate aminotransferase increased | grade 1-2, 6% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Decreased hemoglobin | grade 1-2, 60% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Nausea | grade 1-2, 71% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Dry mouth | grade 1-2, 9.7% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Anxiety | grade 3-4, 0.3% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Arthralgia | grade 3-4, 0.3% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Decreased appetite | grade 3-4, 0.3% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Diarrhea | grade 3-4, 0.3% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Dry mouth | grade 3-4, 0.3% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Headache | grade 3-4, 0.3% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Insomnia | grade 3-4, 0.3% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Mucositis | grade 3-4, 0.5% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Rash | grade 3-4, 0.5% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Stomatitis | grade 3-4, 0.5% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Back pain | grade 3-4, 0.8% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Constipation | grade 3-4, 0.8% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Myalgia | grade 3-4, 0.8% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Urinary tract infection | grade 3-4, 0.8% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Dyspnea | grade 3-4, 1% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Abdominal distension | grade 3-4, 2% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Vomiting | grade 3-4, 2% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Neutropenia | grade 3-4, 20% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Absolute neutrophil count decreased | grade 3-4, 21% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Anemia | grade 3-4, 25% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Decreased hemoglobin | grade 3-4, 25% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Thrombocytopenia | grade 3-4, 29% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Nausea | grade 3-4, 3% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Platelet count decreased | grade 3-4, 35% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Alanine aminotransferase increase | grade 3-4, 4% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Aspartate aminotransferase increased | grade 3-4, 4% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Leukopenia | grade 3-4, 5% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
WBC decreased | grade 3-4, 7% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Asthenia | grade 3-4, 8% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Asthenia | grade 3-4, 8% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Hypertension | grade 3-4, 9% | 300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Myelodysplastic syndrome | grade 5, 1 patient Disc. AE |
300 mg 1 times / day steady, oral Recommended|MTD Dose: 300 mg, 1 times / day Route: oral Route: steady Dose: 300 mg, 1 times / day Sources: |
unhealthy n = 367 Health Status: unhealthy Condition: platinum-sensitive recurrent ovarian cancer | fallopian tube cancer|primary peritoneal cancer Population Size: 367 Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
weak [Inhibition 161 uM] | ||||
weak | ||||
weak | ||||
yes [IC50 1.21 uM] | ||||
yes [Inhibition 0.18 uM] | ||||
yes [Inhibition <0.14 uM] |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
yes | ||||
yes | ||||
yes | ||||
yes | ||||
yes | ||||
yes | ||||
yes | ||||
yes |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
PubMed
Title | Date | PubMed |
---|---|---|
Inhibition of poly(ADP-ribose) polymerase in tumors from BRCA mutation carriers. | 2009 Jul 9 |
|
Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors. | 2009 Nov 26 |
|
The Role of PARP Inhibitors in the Treatment of Gynecologic Malignancies. | 2013 Oct 1 |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: http://adisinsight.springer.com/drugs/800028881
Niraparib (PO, 110-210 mg) successfully inhibited poly(ADP-ribose) polymerase (PARP) during a phase I trial in patients with BRCA-deficient or sporadic cancers associated with homologous recombination repair defects. Niraparib (PO, 30-210 mg) was well tolerated during a phase I trial in patients with BRCA-deficient or sporadic cancers associated with homologous recombination repair defects. Maximum tolerated dose (MTD) of niraparib in patients with advanced solid tumours was 300 mg.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/19873981
Niraparib (MK-4827) inhibited proliferation of cancer cells with mutant BRCA-1 and BRCA-2 with CC(50) in the 10-100 nM range.
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 01:35:16 GMT 2023
by
admin
on
Sat Dec 16 01:35:16 GMT 2023
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Record UNII |
HMC2H89N35
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Record Status |
Validated (UNII)
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Record Version |
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-
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Code | English | ||
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Systematic Name | English | ||
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Common Name | English | ||
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Code | English | ||
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Common Name | English |
Classification Tree | Code System | Code | ||
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NDF-RT |
N0000191623
Created by
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FDA ORPHAN DRUG |
306510
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WHO-ATC |
L01XX54
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NCI_THESAURUS |
C62554
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Code System | Code | Type | Description | ||
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m11995
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DTXSID50146129
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C80059
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PRIMARY | |||
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YY-23
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PRIMARY | |||
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NIRAPARIB
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100000163082
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HMC2H89N35
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24958200
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CHEMBL1094636
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DB11793
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SUB177208
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Niraparib
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HMC2H89N35
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9526
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Related Record | Type | Details | ||
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TARGET -> INHIBITOR | |||
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OFF-TARGET->INHIBITOR |
BINDING
IC50
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BINDER->LIGAND |
BINDING
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TRANSPORTER -> SUBSTRATE |
Niraparib is a substrate of P-gp and BCRP in vitro.
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TRANSPORTER -> SUBSTRATE |
Niraparib is a substrate of P-gp and BCRP in vitro.
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EXCRETED UNCHANGED |
AMOUNT EXCRETED
URINE
|
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SALT/SOLVATE -> PARENT | |||
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SALT/SOLVATE -> PARENT | |||
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TARGET -> INHIBITOR | |||
|
TARGET -> INHIBITOR |
IC50
|
||
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SALT/SOLVATE -> PARENT | |||
|
TARGET -> INHIBITOR | |||
|
EXCRETED UNCHANGED |
AMOUNT EXCRETED
FECAL
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
METABOLITE INACTIVE -> PARENT | |||
|
METABOLITE -> PARENT |
FECAL; PLASMA; URINE
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Biological Half-life | PHARMACOKINETIC |
|
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Tmax | PHARMACOKINETIC |
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ORAL ADMINISTRATION |
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Volume of Distribution | PHARMACOKINETIC |
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