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
| 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 |
| Molecular Formula | C7H8O3S |
| Molecular Weight | 172.202 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
DescriptionSources: http://adisinsight.springer.com/drugs/800033477https://www.ncbi.nlm.nih.gov/pubmed/23881923Curator'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: http://adisinsight.springer.com/drugs/800033477https://www.ncbi.nlm.nih.gov/pubmed/23881923
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
BMN-673 (8R,9S) is the (8R,9S) enantiomer of BMN-673, known as talazoparib. BMN 673 is a novel inhibitor of nuclear enzyme poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity.
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 |
|---|---|---|---|---|
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 plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
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 |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
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 plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
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 |
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 Health Status: unhealthy Age Group: 31 - 75 years Sex: F 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
Disc. AE: Thrombocytopenia, Thrombocytopenia... AEs leading to discontinuation/dose reduction: Thrombocytopenia (grade 3, 16.67%) Sources: Thrombocytopenia (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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
Other AEs: Decreased hemoglobin, Leukocyte count decreased... Other AEs: Decreased hemoglobin (grade 1-4, 90%) Sources: Leukocyte 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
Disc. AE: Anemia, Accidental overdose... AEs leading to discontinuation/dose reduction: Anemia (2%) Sources: Accidental 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
Other AEs: Anemia, Neutropenia... Other AEs: Anemia (32%) Sources: Neutropenia (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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
Other AEs: Anemia, Neutropenia... Other AEs: Anemia (grade 1-4, 53%) Sources: Neutropenia (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 Health Status: unhealthy Age Group: 31 - 75 years Sex: F 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 Health Status: unhealthy Age Group: 31 - 75 years Sex: F 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 Health Status: unhealthy Age Group: 31 - 75 years Sex: F 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
| 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: |
unhealthy, unknown Health Status: unhealthy Age Group: unknown Sex: F Sources: |
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 |
|---|---|---|
| PARP inhibitors: A new era of targeted therapy. | 2015-05 |
|
| Structural basis for the inhibition of poly(ADP-ribose) polymerases 1 and 2 by BMN 673, a potent inhibitor derived from dihydropyridophthalazinone. | 2014-09 |
|
| Trapping of PARP1 and PARP2 by Clinical PARP Inhibitors. | 2012-11-01 |
|
| Cooperation of breast cancer proteins PALB2 and piccolo BRCA2 in stimulating homologous recombination. | 2010-10 |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: http://adisinsight.springer.com/drugs/800033477
Signs of activity of talazoparib were observed at 100 µg/day doses, and the maximum tolerated dose was 1.0 mg/day
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23881923
Talazoparib (BMN 673) induces DNA damage at picomolar concentrations
| Substance Class |
Chemical
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C62554
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| Related Record | Type | Details | ||
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PARENT -> SALT/SOLVATE |
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ACTIVE MOIETY |
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