U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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
Structure of TALAZOPARIB

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

HIDE SMILES / InChI

Description
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.

CNS Activity

CNS Non-penetrant
1014
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.

Originator

Approval Year

2018
436
Targets

Targets

Primary TargetPharmacologyConditionPotency
Inhibitor
8297
 1.2 nM [Ki]
Inhibitor
8297
 0.87 nM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8429
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

2018
Primary
Phase III
656
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
16.4 ng/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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

AUC

ValueDoseCo-administeredAnalytePopulation
208 ng × h/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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

T1/2

ValueDoseCo-administeredAnalytePopulation
90 h
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://clincancerres.aacrjournals.org/content/clincanres/25/9/2717.full.pdf
unhealthy, 31 - 75 years
n = 84
Health Status: unhealthy
Condition: breast cancer
Age Group: 31 - 75 years
Sex: F
Population Size: 84
Sources:
https://clincancerres.aacrjournals.org/content/clincanres/25/9/2717.full.pdf
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:
https://clincancerres.aacrjournals.org/content/clincanres/25/9/2717.full.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
Page: 66
unhealthy, unknown
n = 6
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 6
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
Page: 66
Disc. AE: Thrombocytopenia, Thrombocytopenia...
AEs leading to
discontinuation/dose reduction:
Thrombocytopenia (grade 3, 16.67%)
Thrombocytopenia (grade 4, 16.67%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
Page: 66
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 6
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 6
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
Page: 127
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
Page: 127
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
Page: 127
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
Page: 128
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
Page: 128
Other AEs: Anemia, Neutropenia...
Other AEs:
Anemia (32%)
Neutropenia (15%)
Thrombocytopenia (6%)
Anemia (>5)
Neutropenia (>5)
Thrombocytopenia (>5)
Platelet count decreased (>5)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
Page: 128
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 5
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 5
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 5
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:
https://clincancerres.aacrjournals.org/content/clincanres/25/9/2717.full.pdf
unhealthy, 31 - 75 years
n = 84
Health Status: unhealthy
Condition: breast cancer
Age Group: 31 - 75 years
Sex: F
Population Size: 84
Sources:
https://clincancerres.aacrjournals.org/content/clincanres/25/9/2717.full.pdf
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:
https://clincancerres.aacrjournals.org/content/clincanres/25/9/2717.full.pdf
unhealthy, 31 - 75 years
n = 84
Health Status: unhealthy
Condition: breast cancer
Age Group: 31 - 75 years
Sex: F
Population Size: 84
Sources:
https://clincancerres.aacrjournals.org/content/clincanres/25/9/2717.full.pdf
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:
https://clincancerres.aacrjournals.org/content/clincanres/25/9/2717.full.pdf
unhealthy, 31 - 75 years
n = 84
Health Status: unhealthy
Condition: breast cancer
Age Group: 31 - 75 years
Sex: F
Population Size: 84
Sources:
https://clincancerres.aacrjournals.org/content/clincanres/25/9/2717.full.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
Page: 66
unhealthy, unknown
n = 6
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 6
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
Page: 66
unhealthy, unknown
n = 6
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 6
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 6
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 6
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 6
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 6
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 6
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 6
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 6
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 6
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 6
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 6
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 6
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 6
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 6
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 6
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 6
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 6
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 6
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 6
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 6
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 6
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 6
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 6
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 6
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 6
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
Page: 127
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
Page: 127
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
Page: 127
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
Page: 127
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
Page: 127
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
Page: 127
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
Page: 127
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
Page: 127
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
Page: 127
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
Page: 127
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
Page: 127
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
Page: 127
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
Page: 128
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
Page: 128
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
Page: 128
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
Page: 128
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
Page: 128
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
Page: 128
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
Page: 128
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/211651Orig1s000MultidisciplineR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 5
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 5
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 5
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 5
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 5
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 5
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 5
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 5
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 5
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 5
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 5
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 5
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 5
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 5
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 5
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 5
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 5
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 5
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 5
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 5
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 5
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 5
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 5
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 5
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 5
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 5
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 5
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 5
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 5
unhealthy, unknown
n = 286
Health Status: unhealthy
Condition: breast cancer
Age Group: unknown
Sex: F
Population Size: 286
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211651s000lbl.pdf
Page: 5
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
inducer
781
inhibitor
1767
inhibitor
1852
inhibitor
1612

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP1A2
1524

CYP2B6
810

CYP2C8
911

CYP2C19
1478

CYP3A4/5
278

UGT1A1
204

UGT1A4
77

UGT1A6
108

UGT1A9
116

UGT2B7
146

UGT2B15
64

BSEP
402
P-gp
1537

BCRP
561

OAT1
326

OAT3
339

OCT1
327

OCT2
355

OATP1B1
406

OATP1B3
350

MATE1
135

MATE2
96

BSEP
52

hepatic enzymes
2
CYP1A2
701

CYP2B6
547
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
BSEP
403
 no
CYP1A2
1692
 no
CYP1A2
1692
 no
CYP2B6
1001
 no
CYP2B6
1001
 no
CYP2C19
1553
 no
CYP2C8
965
 no
CYP2C9
1819
 no
CYP2D6
1891
 no
CYP3A4
1925
 no
CYP3A4/5
335
 no
UGT1A1
254
 no
UGT1A4
80
 no
UGT1A6
141
 no
UGT1A9
121
 no
UGT2B15
64
 no
UGT2B7
157
 no
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
hepatic enzymes
2
 minor
BSEP
52
 no
MATE1
135
 no
MATE2
96
 no
OAT1
326
 no
OAT3
339
 no
OATP1B1
406
 no
OATP1B3
350
 no
OCT1
327
 no
OCT2
355
 no
BCRP
561
 yes
P-gp
1537
 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

TargetModalityActivityMetaboliteClinical evidence
hERG
1647
Sourcing

Sourcing

Vendor/AggregatorIDURL
AK Scientific, Inc. (AKSCI)
X5821
http://www.aksci.com/item_detail.php?cat=X5821
AbMole Bioscience
1732
http://www.abmole.com/product.asp?id=1732
AbMole Bioscience
M1732
http://www.abmole.com/products/bmn673.html
Achemtek
0102-014244
http://www.achemtek.com/1207456-01-6
Acorn PharmaTech
ACN-053048
http://www.acornpharmatech.com/
Ambinter
Amb24093138
http://www.ambinter.com/reference/24093138
ApexBio Technology
A3246
http://www.apexbt.com/bmn-673-8r-9s.html
Aurora Fine Chemicals LLC
K16.649.136
http://online.aurorafinechemicals.com/info?ID=K16.649.136
Aurum Pharmatech LLC
S-7826
http://www.Aurumpharmatech.com/Product/ProductDetails/S_7826
Axon MedChem
2502
https://www.axonmedchem.com/product/2502
BioCrick
BCC2205
http://www.biocrick.com/BMN-673-BCC2205.html
Boerchem
BC600324
http://www.boerchem.com/?product_43159.html
Chem Scene
CS-0937
http://www.chemscene.com/1207456-01-6.html
Chemspace
CSSB00015188901
https://chem-space.com/CSSB00015188901
Chemspace
CSSB00025726212
https://chem-space.com/CSSB00025726212
DC Chemicals
DC2008
http://www.dcchemicals.com/product_show-Talazoparib_BMN_673_.html
Excenen
EX-A1356
http://www.excenen.com/searchresultlist.php?id=1207456-01-6
Lab Network
LN01262559
https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01262559
Matrix Scientific
131612
https://www.matrixscientific.com/131612.html
MedChem Express
HY-16106
https://www.medchemexpress.com/BMN-673.html
MolPort
MolPort-042-652-822
https://www.molport.com/shop/molecule-link/MolPort-042-652-822
MuseChem
I000776
https://www.musechem.com/product/I000776.html
Selleck Chemicals
S7048
http://www.selleckchem.com/products/bmn-673.html
Sinfoo Biotech
S061615
http://www.sinfoobiotech.com/product/1065028
Smolecule
S002091
http://www.smolecule.com/products/s002091
Smolecule
S548582
http://www.smolecule.com/products/s548582
Synblock Inc
SB16478
http://www.synblock.com/product/1207456-01-6.html
THE BioTek
bt-253535
https://www.thebiotek.com/product/inhibitors/bt-253535
THE BioTek
bt-287988
https://www.thebiotek.com/product/inhibitors/bt-287988
eNovation Chemicals
D596724
https://www.enovationchem.com/ProductDetails.asp?ProductID=D596724
eNovation Chemicals
Y0974305
https://www.enovationchem.com/ProductDetails.asp?ProductID=Y0974305
iChemical
EBD2207497
http://www.ichemical.com/products/1207456-01-6.html?utm_source=PubChem&utm_medium=website&utm_campaign=product%20catalogs
PubMed

PubMed

TitleDatePubMed
Patents

Patents

WO/2015/164586A1
2
WO/2016/018089A1
2

Sample Use Guides

In Vivo Use Guide
Unknown
Route of Administration: Unknown
In Vitro Use Guide
Unknown
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
PF-06944076
Code 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 [WHO-DD]
Common Name English
TALAZOPARIB [MI]
Common Name English
LT-673
Code English
Classification Tree Code System Code
NCI_THESAURUS C62554
Created by admin on Sat Dec 16 08:20:43 GMT 2023 , Edited by admin on Sat Dec 16 08:20:43 GMT 2023
WHO-ATC L01XX60
Created by admin on Sat Dec 16 08:20:43 GMT 2023 , Edited by admin on Sat Dec 16 08:20:43 GMT 2023
NDF-RT N0000191623
Created by admin on Sat Dec 16 08:20:43 GMT 2023 , Edited by admin on Sat Dec 16 08:20:43 GMT 2023
Code System Code Type Description
USAN
BC-63
Created by admin on Sat Dec 16 08:20:43 GMT 2023 , Edited by admin on Sat Dec 16 08:20:43 GMT 2023
PRIMARY
DAILYMED
9QHX048FRV
Created by admin on Sat Dec 16 08:20:43 GMT 2023 , Edited by admin on Sat Dec 16 08:20:43 GMT 2023
PRIMARY
RXCUI
2099704
Created by admin on Sat Dec 16 08:20:43 GMT 2023 , Edited by admin on Sat Dec 16 08:20:43 GMT 2023
PRIMARY
CAS
1207456-01-6
Created by admin on Sat Dec 16 08:20:43 GMT 2023 , Edited by admin on Sat Dec 16 08:20:43 GMT 2023
PRIMARY
FDA UNII
9QHX048FRV
Created by admin on Sat Dec 16 08:20:43 GMT 2023 , Edited by admin on Sat Dec 16 08:20:43 GMT 2023
PRIMARY
EVMPD
SUB180394
Created by admin on Sat Dec 16 08:20:43 GMT 2023 , Edited by admin on Sat Dec 16 08:20:43 GMT 2023
PRIMARY
LACTMED
Talazoparib
Created by admin on Sat Dec 16 08:20:43 GMT 2023 , Edited by admin on Sat Dec 16 08:20:43 GMT 2023
PRIMARY
WIKIPEDIA
Talazoparib
Created by admin on Sat Dec 16 08:20:43 GMT 2023 , Edited by admin on Sat Dec 16 08:20:43 GMT 2023
PRIMARY
PUBCHEM
135565082
Created by admin on Sat Dec 16 08:20:43 GMT 2023 , Edited by admin on Sat Dec 16 08:20:43 GMT 2023
PRIMARY
MERCK INDEX
m12100
Created by admin on Sat Dec 16 08:20:43 GMT 2023 , Edited by admin on Sat Dec 16 08:20:43 GMT 2023
PRIMARY
INN
9868
Created by admin on Sat Dec 16 08:20:43 GMT 2023 , Edited by admin on Sat Dec 16 08:20:43 GMT 2023
PRIMARY
EPA CompTox
DTXSID001025928
Created by admin on Sat Dec 16 08:20:43 GMT 2023 , Edited by admin on Sat Dec 16 08:20:43 GMT 2023
PRIMARY
DRUG BANK
DB11760
Created by admin on Sat Dec 16 08:20:43 GMT 2023 , Edited by admin on Sat Dec 16 08:20:43 GMT 2023
PRIMARY
NCI_THESAURUS
C95733
Created by admin on Sat Dec 16 08:20:43 GMT 2023 , Edited by admin on Sat Dec 16 08:20:43 GMT 2023
PRIMARY
ChEMBL
CHEMBL3137320
Created by admin on Sat Dec 16 08:20:43 GMT 2023 , Edited by admin on Sat Dec 16 08:20:43 GMT 2023
PRIMARY
SMS_ID
100000166294
Created by admin on Sat Dec 16 08:20:43 GMT 2023 , Edited by admin on Sat Dec 16 08:20:43 GMT 2023
PRIMARY
ACTIVE MOIETY
Structure of TALAZOPARIB
SALT/SOLVATE (PARENT)
Structure of TALAZOPARIB TOSYLATE
NIH
NCATS
PRIVACY ACT
ACCESSIBILITY
DISCLAIMER
HHS VULNERABILITY DISCLOSURE
For language access assistance, contact the NCATS Public Information Officer
National Center for Advancing Translational Sciences (NCATS),
6701 Democracy Boulevard, Bethesda MD 20892-4874 • 301-594-8966