Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C19H14F2N6O.C7H8O3S |
Molecular Weight | 552.552 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=CC=C(C=C1)S(O)(=O)=O.CN2N=CN=C2[C@@H]3[C@H](NC4=CC(F)=CC5=C4C3=NNC5=O)C6=CC=C(F)C=C6
InChI
InChIKey=QUQKKHBYEFLEHK-QNBGGDODSA-N
InChI=1S/C19H14F2N6O.C7H8O3S/c1-27-18(22-8-23-27)15-16(9-2-4-10(20)5-3-9)24-13-7-11(21)6-12-14(13)17(15)25-26-19(12)28;1-6-2-4-7(5-3-6)11(8,9)10/h2-8,15-16,24H,1H3,(H,26,28);2-5H,1H3,(H,8,9,10)/t15-,16-;/m1./s1
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/23881923http://adisinsight.springer.com/drugs/800033477Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/26652717 | https://www.ncbi.nlm.nih.gov/pubmed/23881923 | https://www.fda.gov/Drugs/InformationOnDrugs/ApprovedDrugs/ucm623540.htm
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23881923http://adisinsight.springer.com/drugs/800033477
Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/26652717 | https://www.ncbi.nlm.nih.gov/pubmed/23881923 | https://www.fda.gov/Drugs/InformationOnDrugs/ApprovedDrugs/ucm623540.htm
Talazoparib (BMN 673) demonstrates excellent potency, inhibiting PARP1 and PARP2 enzyme activity. It inhibits PARP-mediated PARylation in a whole-cell assay and prevents proliferation of cancer cells carrying mutant BRCA1/2. Talazoparib is orally available, displaying favorable pharmacokinetic properties and remarkable antitumor efficacy in the BRCA1 mutant MX-1 breast cancer xenograft model following oral administration as a single-agent or in combination with chemotherapy agents such as temozolomide and cisplatin. Medivation (a subsidiary of Pfizer) is developing talazoparib (MDV 3800, formerly BMN 673 and LT 673) for the treatment of genetically defined cancers. On October 16, 2018, the FDA approved talazoparib (TALZENNA, Pfizer Inc.) for patients with deleterious or suspected deleterious germline BRCA-mutated (gBRCAm), HER2‑negative locally advanced or metastatic breast cancer.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL3105 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26652717 |
1.2 nM [Ki] | ||
Target ID: CHEMBL5366 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26652717 |
0.87 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | TALZENNA Approved UseTALZENNA is a poly (ADP-ribose) polymerase (PARP) inhibitor indicated for the treatment of adult patients with deleterious or suspected deleterious germline BRCA-mutated (gBRCAm) HER2-negative locally advanced or metastatic breast cancer. Select patients for therapy based on an FDA-approved companion diagnostic for TALZENNA. Launch Date2018 |
|||
Primary | Unknown Approved UseUnknown |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
16.4 ng/mL |
1 mg 1 times / day steady-state, oral dose: 1 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
TALAZOPARIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
9.97 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31489639/ |
1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered: |
TALAZOPARIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED |
|
19.8 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31489639/ |
1 mg 1 times / day steady-state, oral dose: 1 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
TALAZOPARIB unknown | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
208 ng × h/mL |
1 mg 1 times / day steady-state, oral dose: 1 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
TALAZOPARIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
193 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31489639/ |
1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered: |
TALAZOPARIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED |
|
196 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31489639/ |
1 mg 1 times / day steady-state, oral dose: 1 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
TALAZOPARIB unknown | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
90 h |
1 mg 1 times / day steady-state, oral dose: 1 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
TALAZOPARIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
26% |
1 mg 1 times / day steady-state, oral dose: 1 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
TALAZOPARIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
1 mg 1 times / day steady, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: steady Dose: 1 mg, 1 times / day Sources: |
unhealthy, 31 - 75 years n = 84 Health Status: unhealthy Condition: breast cancer Age Group: 31 - 75 years Sex: F Population Size: 84 Sources: |
Disc. AE: Anemia, Function liver abnormal... Other AEs: Myelosuppression... AEs leading to discontinuation/dose reduction: Anemia (1 patient) Other AEs:Function liver abnormal (2 patients) Myelosuppression (23 patients) Sources: |
1.1 mg 1 times / day multiple, oral MTD Dose: 1.1 mg, 1 times / day Route: oral Route: multiple Dose: 1.1 mg, 1 times / day Sources: Page: 66 |
unhealthy, unknown n = 6 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 6 Sources: Page: 66 |
Disc. AE: Thrombocytopenia, Thrombocytopenia... AEs leading to discontinuation/dose reduction: Thrombocytopenia (grade 3, 16.67%) Sources: Page: 66Thrombocytopenia (grade 4, 16.67%) |
1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 6 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 6 |
Other AEs: Decreased hemoglobin, Leukocyte count decreased... Other AEs: Decreased hemoglobin (grade 1-4, 90%) Sources: Page: 6Leukocyte count decreased (grade 1-4, 84%) Neutropenia (grade 1-4, 68%) Lymphocyte count low (grade 1-4, 76%) Platelets decreased (grade 1-4, 55%) Glucose increased (grade 1-4, 54%) Aspartate aminotransferase increase (grade 1-4, 37%) Alkaline phosphatase increased (grade 1-4, 36%) Alanine aminotransferase increase (grade 1-4, 33%) Calcium decreased (grade 1-4, 28%) Decreased hemoglobin (grade 3, 39%) Leukocyte count decreased (grade 3, 14%) Neutropenia (grade 3, 17%) Lymphocyte count low (grade 3, 17%) Platelets decreased (grade 3, 11%) Glucose increased (grade 3, 2%) Aspartate aminotransferase increase (grade 3, 2%) Alkaline phosphatase increased (grade 3, 2%) Alanine aminotransferase increase (grade 3, 1%) Calcium decreased (grade 3, 1%) Leukocyte count decreased (grade 4, 0%) Neutropenia (grade 4, 3%) Lymphocyte count low (grade 4, 1%) Platelets decreased (grade 4, 4%) |
1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 127 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 127 |
Disc. AE: Anemia, Accidental overdose... AEs leading to discontinuation/dose reduction: Anemia (2%) Sources: Page: 127Accidental overdose (1%) Cerebral hemorrhage (1%) Dyspnea (1%) Glioblastoma multiforme (1%) Headache (1%) Metastases to meninges (1%) Neutropenia (1%) Chronic obstructive airways disease (1%) Thrombocytopenia (1%) Transient ischemic attack (1%) Vomiting (1%) |
1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 128 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 128 |
Other AEs: Anemia, Neutropenia... Other AEs: Anemia (32%) Sources: Page: 128Neutropenia (15%) Thrombocytopenia (6%) Anemia (>5) Neutropenia (>5) Thrombocytopenia (>5) Platelet count decreased (>5) |
1 mg 1 times / day steady, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: steady Dose: 1 mg, 1 times / day Sources: Page: 5 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 5 |
Other AEs: Anemia, Neutropenia... Other AEs: Anemia (grade 1-4, 53%) Sources: Page: 5Neutropenia (grade 1-4, 35%) Thrombocytopenia (grade 1-4, 27%) Decreased appetite (grade 1-4, 21%) Headache (grade 1-4, 33%) Nausea (grade 1-4, 49%) Vomiting (grade 1-4, 25%) Diarrhea (grade 1-4, 22%) Alopecia (grade 1-4, 25%) Fatigue (grade 1-4, 62%) Anemia (grade 3, 38%) Neutropenia (grade 3, 18%) Thrombocytopenia (grade 3, 11%) Decreased appetite (grade 3, <1%) Headache (grade 3, 2%) Nausea (grade 3, <1%) Vomiting (grade 3, 2%) Diarrhea (grade 3, 1%) Fatigue (grade 3, 3%) Anemia (grade 4, 1%) Neutropenia (grade 4, 3%) Thrombocytopenia (grade 4, 4%) Abdominal pain (19%) Dizziness (17%) Leukopenia (17%) Dysgeusia (10%) Dyspepsia (10%) Stomatitis (8%) Lymphopenia (7%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Anemia | 1 patient Disc. AE |
1 mg 1 times / day steady, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: steady Dose: 1 mg, 1 times / day Sources: |
unhealthy, 31 - 75 years n = 84 Health Status: unhealthy Condition: breast cancer Age Group: 31 - 75 years Sex: F Population Size: 84 Sources: |
Function liver abnormal | 2 patients Disc. AE |
1 mg 1 times / day steady, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: steady Dose: 1 mg, 1 times / day Sources: |
unhealthy, 31 - 75 years n = 84 Health Status: unhealthy Condition: breast cancer Age Group: 31 - 75 years Sex: F Population Size: 84 Sources: |
Myelosuppression | 23 patients | 1 mg 1 times / day steady, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: steady Dose: 1 mg, 1 times / day Sources: |
unhealthy, 31 - 75 years n = 84 Health Status: unhealthy Condition: breast cancer Age Group: 31 - 75 years Sex: F Population Size: 84 Sources: |
Thrombocytopenia | grade 3, 16.67% Disc. AE |
1.1 mg 1 times / day multiple, oral MTD Dose: 1.1 mg, 1 times / day Route: oral Route: multiple Dose: 1.1 mg, 1 times / day Sources: Page: 66 |
unhealthy, unknown n = 6 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 6 Sources: Page: 66 |
Thrombocytopenia | grade 4, 16.67% Disc. AE |
1.1 mg 1 times / day multiple, oral MTD Dose: 1.1 mg, 1 times / day Route: oral Route: multiple Dose: 1.1 mg, 1 times / day Sources: Page: 66 |
unhealthy, unknown n = 6 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 6 Sources: Page: 66 |
Calcium decreased | grade 1-4, 28% | 1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 6 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 6 |
Alanine aminotransferase increase | grade 1-4, 33% | 1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 6 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 6 |
Alkaline phosphatase increased | grade 1-4, 36% | 1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 6 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 6 |
Aspartate aminotransferase increase | grade 1-4, 37% | 1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 6 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 6 |
Glucose increased | grade 1-4, 54% | 1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 6 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 6 |
Platelets decreased | grade 1-4, 55% | 1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 6 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 6 |
Neutropenia | grade 1-4, 68% | 1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 6 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 6 |
Lymphocyte count low | grade 1-4, 76% | 1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 6 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 6 |
Leukocyte count decreased | grade 1-4, 84% | 1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 6 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 6 |
Decreased hemoglobin | grade 1-4, 90% | 1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 6 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 6 |
Alanine aminotransferase increase | grade 3, 1% | 1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 6 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 6 |
Calcium decreased | grade 3, 1% | 1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 6 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 6 |
Platelets decreased | grade 3, 11% | 1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 6 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 6 |
Leukocyte count decreased | grade 3, 14% | 1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 6 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 6 |
Lymphocyte count low | grade 3, 17% | 1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 6 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 6 |
Neutropenia | grade 3, 17% | 1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 6 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 6 |
Alkaline phosphatase increased | grade 3, 2% | 1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 6 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 6 |
Aspartate aminotransferase increase | grade 3, 2% | 1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 6 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 6 |
Glucose increased | grade 3, 2% | 1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 6 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 6 |
Decreased hemoglobin | grade 3, 39% | 1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 6 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 6 |
Leukocyte count decreased | grade 4, 0% | 1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 6 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 6 |
Lymphocyte count low | grade 4, 1% | 1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 6 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 6 |
Neutropenia | grade 4, 3% | 1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 6 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 6 |
Platelets decreased | grade 4, 4% | 1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 6 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 6 |
Accidental overdose | 1% Disc. AE |
1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 127 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 127 |
Cerebral hemorrhage | 1% Disc. AE |
1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 127 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 127 |
Chronic obstructive airways disease | 1% Disc. AE |
1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 127 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 127 |
Dyspnea | 1% Disc. AE |
1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 127 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 127 |
Glioblastoma multiforme | 1% Disc. AE |
1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 127 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 127 |
Headache | 1% Disc. AE |
1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 127 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 127 |
Metastases to meninges | 1% Disc. AE |
1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 127 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 127 |
Neutropenia | 1% Disc. AE |
1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 127 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 127 |
Thrombocytopenia | 1% Disc. AE |
1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 127 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 127 |
Transient ischemic attack | 1% Disc. AE |
1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 127 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 127 |
Vomiting | 1% Disc. AE |
1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 127 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 127 |
Anemia | 2% Disc. AE |
1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 127 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 127 |
Neutropenia | 15% | 1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 128 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 128 |
Anemia | 32% | 1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 128 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 128 |
Thrombocytopenia | 6% | 1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 128 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 128 |
Anemia | >5 | 1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 128 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 128 |
Neutropenia | >5 | 1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 128 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 128 |
Platelet count decreased | >5 | 1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 128 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 128 |
Thrombocytopenia | >5 | 1 mg 1 times / day multiple, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: Page: 128 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 128 |
Dysgeusia | 10% | 1 mg 1 times / day steady, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: steady Dose: 1 mg, 1 times / day Sources: Page: 5 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 5 |
Dyspepsia | 10% | 1 mg 1 times / day steady, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: steady Dose: 1 mg, 1 times / day Sources: Page: 5 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 5 |
Dizziness | 17% | 1 mg 1 times / day steady, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: steady Dose: 1 mg, 1 times / day Sources: Page: 5 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 5 |
Leukopenia | 17% | 1 mg 1 times / day steady, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: steady Dose: 1 mg, 1 times / day Sources: Page: 5 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 5 |
Abdominal pain | 19% | 1 mg 1 times / day steady, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: steady Dose: 1 mg, 1 times / day Sources: Page: 5 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 5 |
Lymphopenia | 7% | 1 mg 1 times / day steady, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: steady Dose: 1 mg, 1 times / day Sources: Page: 5 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 5 |
Stomatitis | 8% | 1 mg 1 times / day steady, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: steady Dose: 1 mg, 1 times / day Sources: Page: 5 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 5 |
Decreased appetite | grade 1-4, 21% | 1 mg 1 times / day steady, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: steady Dose: 1 mg, 1 times / day Sources: Page: 5 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 5 |
Diarrhea | grade 1-4, 22% | 1 mg 1 times / day steady, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: steady Dose: 1 mg, 1 times / day Sources: Page: 5 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 5 |
Alopecia | grade 1-4, 25% | 1 mg 1 times / day steady, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: steady Dose: 1 mg, 1 times / day Sources: Page: 5 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 5 |
Vomiting | grade 1-4, 25% | 1 mg 1 times / day steady, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: steady Dose: 1 mg, 1 times / day Sources: Page: 5 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 5 |
Thrombocytopenia | grade 1-4, 27% | 1 mg 1 times / day steady, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: steady Dose: 1 mg, 1 times / day Sources: Page: 5 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 5 |
Headache | grade 1-4, 33% | 1 mg 1 times / day steady, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: steady Dose: 1 mg, 1 times / day Sources: Page: 5 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 5 |
Neutropenia | grade 1-4, 35% | 1 mg 1 times / day steady, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: steady Dose: 1 mg, 1 times / day Sources: Page: 5 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 5 |
Nausea | grade 1-4, 49% | 1 mg 1 times / day steady, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: steady Dose: 1 mg, 1 times / day Sources: Page: 5 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 5 |
Anemia | grade 1-4, 53% | 1 mg 1 times / day steady, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: steady Dose: 1 mg, 1 times / day Sources: Page: 5 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 5 |
Fatigue | grade 1-4, 62% | 1 mg 1 times / day steady, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: steady Dose: 1 mg, 1 times / day Sources: Page: 5 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 5 |
Diarrhea | grade 3, 1% | 1 mg 1 times / day steady, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: steady Dose: 1 mg, 1 times / day Sources: Page: 5 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 5 |
Thrombocytopenia | grade 3, 11% | 1 mg 1 times / day steady, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: steady Dose: 1 mg, 1 times / day Sources: Page: 5 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 5 |
Neutropenia | grade 3, 18% | 1 mg 1 times / day steady, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: steady Dose: 1 mg, 1 times / day Sources: Page: 5 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 5 |
Headache | grade 3, 2% | 1 mg 1 times / day steady, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: steady Dose: 1 mg, 1 times / day Sources: Page: 5 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 5 |
Vomiting | grade 3, 2% | 1 mg 1 times / day steady, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: steady Dose: 1 mg, 1 times / day Sources: Page: 5 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 5 |
Fatigue | grade 3, 3% | 1 mg 1 times / day steady, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: steady Dose: 1 mg, 1 times / day Sources: Page: 5 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 5 |
Anemia | grade 3, 38% | 1 mg 1 times / day steady, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: steady Dose: 1 mg, 1 times / day Sources: Page: 5 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 5 |
Decreased appetite | grade 3, <1% | 1 mg 1 times / day steady, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: steady Dose: 1 mg, 1 times / day Sources: Page: 5 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 5 |
Nausea | grade 3, <1% | 1 mg 1 times / day steady, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: steady Dose: 1 mg, 1 times / day Sources: Page: 5 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 5 |
Anemia | grade 4, 1% | 1 mg 1 times / day steady, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: steady Dose: 1 mg, 1 times / day Sources: Page: 5 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 5 |
Neutropenia | grade 4, 3% | 1 mg 1 times / day steady, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: steady Dose: 1 mg, 1 times / day Sources: Page: 5 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 5 |
Thrombocytopenia | grade 4, 4% | 1 mg 1 times / day steady, oral Recommended Dose: 1 mg, 1 times / day Route: oral Route: steady Dose: 1 mg, 1 times / day Sources: Page: 5 |
unhealthy, unknown n = 286 Health Status: unhealthy Condition: breast cancer Age Group: unknown Sex: F Population Size: 286 Sources: Page: 5 |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Drug as perpetrator
Drug as victim
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf Page: 37.0 |
Name | Type | Language | ||
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Official Name | English | ||
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Common Name | English | ||
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Code | English | ||
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Common Name | English | ||
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Brand Name | English | ||
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Systematic Name | English | ||
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Common Name | English | ||
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Common Name | English | ||
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Systematic Name | English | ||
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Common Name | English |
Classification Tree | Code System | Code | ||
---|---|---|---|---|
|
NCI_THESAURUS |
C62554
Created by
admin on Sat Dec 16 07:53:47 GMT 2023 , Edited by admin on Sat Dec 16 07:53:47 GMT 2023
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Code System | Code | Type | Description | ||
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2099703
Created by
admin on Sat Dec 16 07:53:47 GMT 2023 , Edited by admin on Sat Dec 16 07:53:47 GMT 2023
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PRIMARY | |||
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DTXSID301026468
Created by
admin on Sat Dec 16 07:53:47 GMT 2023 , Edited by admin on Sat Dec 16 07:53:47 GMT 2023
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PRIMARY | |||
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C152494
Created by
admin on Sat Dec 16 07:53:47 GMT 2023 , Edited by admin on Sat Dec 16 07:53:47 GMT 2023
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PRIMARY | |||
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02WK9U5NZC
Created by
admin on Sat Dec 16 07:53:47 GMT 2023 , Edited by admin on Sat Dec 16 07:53:47 GMT 2023
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PRIMARY | |||
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BC-64
Created by
admin on Sat Dec 16 07:53:47 GMT 2023 , Edited by admin on Sat Dec 16 07:53:47 GMT 2023
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PRIMARY | |||
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DBSALT002816
Created by
admin on Sat Dec 16 07:53:47 GMT 2023 , Edited by admin on Sat Dec 16 07:53:47 GMT 2023
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PRIMARY | |||
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m12100
Created by
admin on Sat Dec 16 07:53:47 GMT 2023 , Edited by admin on Sat Dec 16 07:53:47 GMT 2023
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PRIMARY | |||
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1373431-65-2
Created by
admin on Sat Dec 16 07:53:47 GMT 2023 , Edited by admin on Sat Dec 16 07:53:47 GMT 2023
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PRIMARY | |||
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300000011235
Created by
admin on Sat Dec 16 07:53:47 GMT 2023 , Edited by admin on Sat Dec 16 07:53:47 GMT 2023
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PRIMARY | |||
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135565654
Created by
admin on Sat Dec 16 07:53:47 GMT 2023 , Edited by admin on Sat Dec 16 07:53:47 GMT 2023
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PRIMARY | |||
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5300
Created by
admin on Sat Dec 16 07:53:47 GMT 2023 , Edited by admin on Sat Dec 16 07:53:47 GMT 2023
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PRIMARY | |||
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CHEMBL3137320
Created by
admin on Sat Dec 16 07:53:47 GMT 2023 , Edited by admin on Sat Dec 16 07:53:47 GMT 2023
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PRIMARY | |||
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02WK9U5NZC
Created by
admin on Sat Dec 16 07:53:47 GMT 2023 , Edited by admin on Sat Dec 16 07:53:47 GMT 2023
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PRIMARY |
ACTIVE MOIETY
SUBSTANCE RECORD