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Details

Stereochemistry ABSOLUTE
Molecular Formula C19H14F2N6O
Molecular Weight 380.3516
Optical Activity UNSPECIFIED
Defined Stereocenters 2 / 2
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of TALAZOPARIB

SMILES

Cn1c([C@]2([H])[C@@]([H])(c3ccc(cc3)F)Nc4cc(cc5c4c2nnc5O)F)ncn1

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

HIDE SMILES / InChI

Molecular Formula C19H14F2N6O
Molecular Weight 380.3516
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 2 / 2
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment:: 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.

CNS Activity

Curator's Comment:: This lack of intracranial efficacy is associated with limited brain distribution due to active efflux mediated by Mdr1 at the blood-brain barrier (animal study). No human data available.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
1.19999999999999996 nM [Ki]
0.869999999999999996 nM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
TALZENNA

Approved Use

TALZENNA 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 Date

1539561600000
Primary
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
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
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
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

AUC

ValueDoseCo-administeredAnalytePopulation
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
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
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

T1/2

ValueDoseCo-administeredAnalytePopulation
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

Funbound

ValueDoseCo-administeredAnalytePopulation
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

Doses

DosePopulationAdverse 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)
Function liver abnormal (2 patients)
Other AEs:
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
Disc. AE: Thrombocytopenia, Thrombocytopenia...
AEs leading to
discontinuation/dose reduction:
Thrombocytopenia (grade 3, 16.67%)
Thrombocytopenia (grade 4, 16.67%)
Sources:
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%)
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%)
Sources:
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
Disc. AE: Anemia, Accidental overdose...
AEs leading to
discontinuation/dose reduction:
Anemia (2%)
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%)
Sources:
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
Other AEs: Anemia, Neutropenia...
Other AEs:
Anemia (32%)
Neutropenia (15%)
Thrombocytopenia (6%)
Anemia (>5)
Neutropenia (>5)
Thrombocytopenia (>5)
Platelet count decreased (>5)
Sources:
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%)
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%)
Sources:
AEs

AEs

AESignificanceDosePopulation
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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

Overview

Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
minor
no
no
no
no
no
no
no
no
no
yes
yes
yes (co-administration study)
Comment: itraconazole increases talazoparib AUC >50%; rifampicin did not inrease talazoparib AUC; both increased talazoparib plasma concentrations by 40% and 37%, respectively
Tox targets

Tox targets

PubMed

PubMed

TitleDatePubMed
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

Sample Use Guides

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
Talazoparib (BMN 673) induces DNA damage at picomolar concentrations
Substance Class Chemical
Created
by admin
on Sat Jun 26 11:31:42 UTC 2021
Edited
by admin
on Sat Jun 26 11:31:42 UTC 2021
Record UNII
9QHX048FRV
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
TALAZOPARIB
INN   USAN  
USAN   INN  
Official Name English
BMN 673
Code English
TALAZOPARIB [INN]
Common Name English
3H-PYRIDO(4,3,2-DE)PHTHALAZIN-3-ONE, 5-FLUORO-8-(4-FLUOROPHENYL)-2,7,8,9-TETRAHYDRO-9-(1-METHYL-1H-1,2,4-TRIAZOL-5-YL)-, (8S,9R)-
Systematic Name English
TALAZOPARIB [USAN]
Common Name English
BMN-673
Code English
(8S,9R)-5-FLUORO-8-(4-FLUOROPHENYL)-9-(1-METHYL-1H-1,2,4-TRIAZOL-5-YL)-2,7,8,9-TETRAHYDRO-3H-PYRIDO(4,3,2-DE)PHTHALAZIN-3-ONE
Systematic Name English
TALAZOPARIB [MI]
Common Name English
LT-673
Code English
TALAZOPARIB [WHO-DD]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C62554
Created by admin on Sat Jun 26 11:31:42 UTC 2021 , Edited by admin on Sat Jun 26 11:31:42 UTC 2021
WHO-ATC L01XX60
Created by admin on Sat Jun 26 11:31:42 UTC 2021 , Edited by admin on Sat Jun 26 11:31:42 UTC 2021
NDF-RT N0000191623
Created by admin on Sat Jun 26 11:31:42 UTC 2021 , Edited by admin on Sat Jun 26 11:31:42 UTC 2021
Code System Code Type Description
RXCUI
2099704
Created by admin on Sat Jun 26 11:31:42 UTC 2021 , Edited by admin on Sat Jun 26 11:31:42 UTC 2021
PRIMARY
CAS
1207456-01-6
Created by admin on Sat Jun 26 11:31:42 UTC 2021 , Edited by admin on Sat Jun 26 11:31:42 UTC 2021
PRIMARY
FDA UNII
9QHX048FRV
Created by admin on Sat Jun 26 11:31:42 UTC 2021 , Edited by admin on Sat Jun 26 11:31:42 UTC 2021
PRIMARY
EVMPD
SUB180394
Created by admin on Sat Jun 26 11:31:42 UTC 2021 , Edited by admin on Sat Jun 26 11:31:42 UTC 2021
PRIMARY
LACTMED
Talazoparib
Created by admin on Sat Jun 26 11:31:42 UTC 2021 , Edited by admin on Sat Jun 26 11:31:42 UTC 2021
PRIMARY
PUBCHEM
135565082
Created by admin on Sat Jun 26 11:31:42 UTC 2021 , Edited by admin on Sat Jun 26 11:31:42 UTC 2021
PRIMARY
MERCK INDEX
M12100
Created by admin on Sat Jun 26 11:31:42 UTC 2021 , Edited by admin on Sat Jun 26 11:31:42 UTC 2021
PRIMARY
INN
9868
Created by admin on Sat Jun 26 11:31:42 UTC 2021 , Edited by admin on Sat Jun 26 11:31:42 UTC 2021
PRIMARY
DRUG BANK
DB11760
Created by admin on Sat Jun 26 11:31:42 UTC 2021 , Edited by admin on Sat Jun 26 11:31:42 UTC 2021
PRIMARY
NCI_THESAURUS
C95733
Created by admin on Sat Jun 26 11:31:42 UTC 2021 , Edited by admin on Sat Jun 26 11:31:42 UTC 2021
PRIMARY
ChEMBL
CHEMBL3137320
Created by admin on Sat Jun 26 11:31:42 UTC 2021 , Edited by admin on Sat Jun 26 11:31:42 UTC 2021
PRIMARY
Related Record Type Details
BINDER->LIGAND
In vitro, protein binding of talazoparib is 74% and is independent of talazoparib concentration.
BINDING
TRANSPORTER -> SUBSTRATE
Co-administration with BCRP inhibitors may increase talazoparib exposure.
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%).
EXCRETED UNCHANGED
FECAL
EXCRETED UNCHANGED
TARGET -> INHIBITOR
IC50
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Tmax PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC