Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C19H14F2N6O |
Molecular Weight | 380.3509 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CN1N=CN=C1[C@@H]2[C@H](NC3=CC(F)=CC4=C3C2=NNC4=O)C5=CC=C(F)C=C5
InChI
InChIKey=HWGQMRYQVZSGDQ-HZPDHXFCSA-N
InChI=1S/C19H14F2N6O/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/h2-8,15-16,24H,1H3,(H,26,28)/t15-,16-/m1/s1
Molecular Formula | C19H14F2N6O |
Molecular Weight | 380.3509 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
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 |
PubMed
Title | Date | PubMed |
---|---|---|
Cooperation of breast cancer proteins PALB2 and piccolo BRCA2 in stimulating homologous recombination. | 2010 Oct |
|
Trapping of PARP1 and PARP2 by Clinical PARP Inhibitors. | 2012 Nov 1 |
|
Structural basis for the inhibition of poly(ADP-ribose) polymerases 1 and 2 by BMN 673, a potent inhibitor derived from dihydropyridophthalazinone. | 2014 Sep |
|
PARP inhibitors: A new era of targeted therapy. | 2015 May |
Patents
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 08:20:43 GMT 2023
by
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on
Sat Dec 16 08:20:43 GMT 2023
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Record UNII |
9QHX048FRV
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Record Status |
Validated (UNII)
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Record Version |
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Official Name | English | ||
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Code | English | ||
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Systematic Name | English | ||
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Code | English | ||
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Common Name | English | ||
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Common Name | English | ||
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Code | English |
Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C62554
Created by
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WHO-ATC |
L01XX60
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NDF-RT |
N0000191623
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Code System | Code | Type | Description | ||
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BC-63
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9QHX048FRV
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2099704
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1207456-01-6
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9QHX048FRV
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SUB180394
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Talazoparib
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Talazoparib
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135565082
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m12100
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9868
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DTXSID001025928
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DB11760
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C95733
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CHEMBL3137320
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100000166294
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Related Record | Type | Details | ||
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BINDER->LIGAND |
In vitro, protein binding of talazoparib is 74% and is independent of talazoparib concentration.
BINDING
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SALT/SOLVATE -> PARENT |
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TRANSPORTER -> SUBSTRATE |
Co-administration with BCRP inhibitors may increase talazoparib exposure.
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TRANSPORTER -> SUBSTRATE |
Co-administration of talazoparib with certain P-gp inhibitors including amiodarone, carvedilol, clarithromycin, itraconazole, and verapamil in the clinical studies (PRP-001, PRP-002, ABRAZO and EMBRACA) increased talazoparib exposure by 44.7%, in conjunction with an increased rate of Talzenna dose reductions (41%).
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EXCRETED UNCHANGED |
FECAL
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EXCRETED UNCHANGED |
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TARGET -> INHIBITOR |
IC50
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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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Tmax | PHARMACOKINETIC |
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Biological Half-life | PHARMACOKINETIC |
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Volume of Distribution | PHARMACOKINETIC |
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