Dosing & Uses
Dosage Forms & Strengths
capsule
- 0.1mg
- 0.25mg
- 0.35mg
- 0.5mg
- 0.75mg
- 1mg
Breast Cancer
Indicated for adults with deleterious or suspected deleterious germline BRCA-mutated (gBRCAm) HER2-negative locally advanced or metastatic breast cancer
1 mg PO qDay with or without food
Continue until disease progression or unacceptable toxicity occurs
Metastatic Castration-Resistant Prostate Cancer
Indicated in combination with enzalutamide for homologous recombination repair (HRR) gene-mutated metastatic castration-resistant prostate cancer (mCRPC)
0.5 mg PO qDay (in combination with enzalutamide)
Continue until disease progression or unacceptable toxicity
Patients should also receive a gonadotropin-releasing hormone (GnRH) analog concurrently or should have had bilateral orchiectomy
Dosage Modifications
Dose reduction levels for adverse reactions for breast cancer
- First dose reduction: 0.75 mg qDay
- Second dose reduction: 0.5 mg qDay
- Third dose reduction: 0.25 mg qDay
- Discontinue treatment if >3 dose reductions are required
Dose reduction levels for adverse reactions for mCRPC
- First dose reduction: 0.35 mg qDay
- Second dose reduction: 0.25 mg qDay
- Third dose reduction: 0.1 mg qDay
- Discontinue treatment if >3 dose reductions are required
- Refer to enzalutamide prescribing information for dose modifications for adverse reactions
Hemoglobin <8 g/dL
- Withhold until levels resolve to hemoglobin ≥9 g/dL
- Resume treatment at reduced dose
Platelet count <50,000/mcL
- Withhold until levels resolve to platelet count ≥75,000/mcL
- Resume treatment at reduced dose
Neutrophil count <1000/mcL
- Withhold until levels resolve to neutrophil count ≥1500/mcL
- Resume treatment at reduced dose
Nonhematologic Grade ≥3
- Withhold until resolve to Grade ≤1
- Consider resuming at a reduced dose or discontinue
Coadministration with P-glycoprotein (P-gp) inhibitors
-
Breast cancer
- P-gp inhibitors (ie, amiodarone, carvedilol, clarithromycin, itraconazole, verapamil): Avoid use; if coadministration cannot be avoided, reduce talazoparib dose to 0.75 mg qDay
- Once P-gp inhibitors are discontinued, increase talazoparib dose (after 3-5 half-lives of the inhibitor) to dose used before initiating the P-gp inhibitor
- Other P-gp inhibitors that were not specifically studied in preclinical trials may also increase talazoparib systemic exposure; if coadministered, cautiously monitor
Renal impairment
-
Breast cancer
- Mild (CrCl 60-89 mL/min): No dosage adjustment required
- Moderate (CrCl 30-59 mL/min): Reduce to 0.75 mg qDay
- Severe (CrCl 15-29 mL/min): Reduce to 0.5 mg qDay
- Hemodialysis: Not studied
-
mCRPC
- Mild (CrCl 60-89 mL/min): No dosage adjustment required
- Moderate (CrCl 30-59 mL/min): Reduce to 0.35 mg qDay
- Severe (CrCl 15-29 mL/min): Reduce to 0.25 mg qDay
- Hemodialysis: Not studied
Hepatic impairment
- Mild-to-severe: No dosage adjustment necessary
Dosing Considerations
Verify pregnancy in females of reproductive potential before initiating treatment
Patient selection
- Breast cancer: Select patients based on presence of germline BRCA mutations
- mCRPC: Select patients based on presence of HRR gene mutations
- Information on FDA-approved tests is available at http://www.fda.gov/companiondiagnostics
<18 years: Safety and efficacy not established
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (0)
Serious - Use Alternative (33)
- acalabrutinib
acalabrutinib will increase the level or effect of talazoparib by Other (see comment). Avoid or Use Alternate Drug. BCRP inhibitors may increase systemic exposure of talazoparib (a BCRP substrate). If coadministration cannot be avoided, monitor for potential adverse reactions.
- amiodarone
amiodarone will increase the level or effect of talazoparib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If coadministration with certain P-gp inhibitors (ie, amiodarone, carvedilol, clarithromycin, itraconazole, verapamil) cannot be avoided, reduce talazoparib dose to 0.75 mg qDay. Once P-gp inhibitors are discontinued, increase talazoparib dose (after 3-5 half-lives of the inhibitor) to dose used prior to initiating the P-gp inhibitor(s).
- carvedilol
carvedilol will increase the level or effect of talazoparib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If coadministration with certain P-gp inhibitors (ie, amiodarone, carvedilol, clarithromycin, itraconazole, verapamil) cannot be avoided, reduce talazoparib dose to 0.75 mg qDay. Once P-gp inhibitors are discontinued, increase talazoparib dose (after 3-5 half-lives of the inhibitor) to dose used prior to initiating the P-gp inhibitor(s).
- clarithromycin
clarithromycin will increase the level or effect of talazoparib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If coadministration with certain P-gp inhibitors (ie, amiodarone, carvedilol, clarithromycin, itraconazole, verapamil) cannot be avoided, reduce talazoparib dose to 0.75 mg qDay. Once P-gp inhibitors are discontinued, increase talazoparib dose (after 3-5 half-lives of the inhibitor) to dose used prior to initiating the P-gp inhibitor(s).
- cobicistat
cobicistat will increase the level or effect of talazoparib by Other (see comment). Avoid or Use Alternate Drug. BCRP inhibitors may increase systemic exposure of talazoparib (a BCRP substrate). If coadministration cannot be avoided, monitor for potential adverse reactions.
- cyclosporine
cyclosporine will increase the level or effect of talazoparib by Other (see comment). Avoid or Use Alternate Drug. BCRP inhibitors may increase systemic exposure of talazoparib (a BCRP substrate). If coadministration cannot be avoided, monitor for potential adverse reactions.
- dabrafenib
dabrafenib will increase the level or effect of talazoparib by Other (see comment). Avoid or Use Alternate Drug. BCRP inhibitors may increase systemic exposure of talazoparib (a BCRP substrate). If coadministration cannot be avoided, monitor for potential adverse reactions.
- dipyridamole
dipyridamole will increase the level or effect of talazoparib by Other (see comment). Avoid or Use Alternate Drug. BCRP inhibitors may increase systemic exposure of talazoparib (a BCRP substrate). If coadministration cannot be avoided, monitor for potential adverse reactions.
- eltrombopag
eltrombopag will increase the level or effect of talazoparib by Other (see comment). Avoid or Use Alternate Drug. BCRP inhibitors may increase systemic exposure of talazoparib (a BCRP substrate). If coadministration cannot be avoided, monitor for potential adverse reactions.
- eluxadoline
eluxadoline will increase the level or effect of talazoparib by Other (see comment). Avoid or Use Alternate Drug. BCRP inhibitors may increase systemic exposure of talazoparib (a BCRP substrate). If coadministration cannot be avoided, monitor for potential adverse reactions.
- etrasimod
etrasimod, talazoparib. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug. Risk of additive immune system effects with etrasimod has not been studied in combination with antineoplastic, immune-modulating, or noncorticosteroid immunosuppressive therapies. Avoid coadministration during and in the weeks following administration of etrasimod.
- gefitinib
gefitinib will increase the level or effect of talazoparib by Other (see comment). Avoid or Use Alternate Drug. BCRP inhibitors may increase systemic exposure of talazoparib (a BCRP substrate). If coadministration cannot be avoided, monitor for potential adverse reactions.
- imatinib
imatinib will increase the level or effect of talazoparib by Other (see comment). Avoid or Use Alternate Drug. BCRP inhibitors may increase systemic exposure of talazoparib (a BCRP substrate). If coadministration cannot be avoided, monitor for potential adverse reactions.
- itraconazole
itraconazole will increase the level or effect of talazoparib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If coadministration with certain P-gp inhibitors (ie, amiodarone, carvedilol, clarithromycin, itraconazole, verapamil) cannot be avoided, reduce talazoparib dose to 0.75 mg qDay. Once P-gp inhibitors are discontinued, increase talazoparib dose (after 3-5 half-lives of the inhibitor) to dose used prior to initiating the P-gp inhibitor(s).
- ketoconazole
ketoconazole will increase the level or effect of talazoparib by Other (see comment). Avoid or Use Alternate Drug. BCRP inhibitors may increase systemic exposure of talazoparib (a BCRP substrate). If coadministration cannot be avoided, monitor for potential adverse reactions.
- lapatinib
lapatinib will increase the level or effect of talazoparib by Other (see comment). Avoid or Use Alternate Drug. BCRP inhibitors may increase systemic exposure of talazoparib (a BCRP substrate). If coadministration cannot be avoided, monitor for potential adverse reactions.
- lasmiditan
lasmiditan increases levels of talazoparib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.
lasmiditan increases levels of talazoparib by Other (see comment). Avoid or Use Alternate Drug. Comment: Lasmiditan inhibits BCRP in vitro. Avoid coadministration of lasmiditan with BCRP substrates. - leniolisib
leniolisib will increase the level or effect of talazoparib by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP inhibitor, may increase systemic exposure of BCRP substrates
- levoketoconazole
levoketoconazole will increase the level or effect of talazoparib by Other (see comment). Avoid or Use Alternate Drug. BCRP inhibitors may increase systemic exposure of talazoparib (a BCRP substrate). If coadministration cannot be avoided, monitor for potential adverse reactions.
- osimertinib
osimertinib will increase the level or effect of talazoparib by Other (see comment). Avoid or Use Alternate Drug. BCRP inhibitors may increase systemic exposure of talazoparib (a BCRP substrate). If coadministration cannot be avoided, monitor for potential adverse reactions.
- pantoprazole
pantoprazole will increase the level or effect of talazoparib by Other (see comment). Avoid or Use Alternate Drug. BCRP inhibitors may increase systemic exposure of talazoparib (a BCRP substrate). If coadministration cannot be avoided, monitor for potential adverse reactions.
- ponatinib
ponatinib will increase the level or effect of talazoparib by Other (see comment). Avoid or Use Alternate Drug. BCRP inhibitors may increase systemic exposure of talazoparib (a BCRP substrate). If coadministration cannot be avoided, monitor for potential adverse reactions.
- regorafenib
regorafenib will increase the level or effect of talazoparib by Other (see comment). Avoid or Use Alternate Drug. BCRP inhibitors may increase systemic exposure of talazoparib (a BCRP substrate). If coadministration cannot be avoided, monitor for potential adverse reactions.
- rolapitant
rolapitant will increase the level or effect of talazoparib by Other (see comment). Avoid or Use Alternate Drug. BCRP inhibitors may increase systemic exposure of talazoparib (a BCRP substrate). If coadministration cannot be avoided, monitor for potential adverse reactions.
- safinamide
safinamide will increase the level or effect of talazoparib by Other (see comment). Avoid or Use Alternate Drug. BCRP inhibitors may increase systemic exposure of talazoparib (a BCRP substrate). If coadministration cannot be avoided, monitor for potential adverse reactions.
- sotorasib
sotorasib will decrease the level or effect of talazoparib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If use is unavoidable, refer to the prescribing information of the P-gp substrate for dosage modifications.
- stiripentol
stiripentol will increase the level or effect of talazoparib by Other (see comment). Avoid or Use Alternate Drug. BCRP inhibitors may increase systemic exposure of talazoparib (a BCRP substrate). If coadministration cannot be avoided, monitor for potential adverse reactions.
- sunitinib
sunitinib will increase the level or effect of talazoparib by Other (see comment). Avoid or Use Alternate Drug. BCRP inhibitors may increase systemic exposure of talazoparib (a BCRP substrate). If coadministration cannot be avoided, monitor for potential adverse reactions.
- tepotinib
tepotinib will increase the level or effect of talazoparib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If concomitant use unavoidable, reduce the P-gp substrate dosage if recommended in its approved product labeling.
- vandetanib
vandetanib will increase the level or effect of talazoparib by Other (see comment). Avoid or Use Alternate Drug. BCRP inhibitors may increase systemic exposure of talazoparib (a BCRP substrate). If coadministration cannot be avoided, monitor for potential adverse reactions.
- velpatasvir
velpatasvir will increase the level or effect of talazoparib by Other (see comment). Avoid or Use Alternate Drug. BCRP inhibitors may increase systemic exposure of talazoparib (a BCRP substrate). If coadministration cannot be avoided, monitor for potential adverse reactions.
- vemurafenib
vemurafenib will increase the level or effect of talazoparib by Other (see comment). Avoid or Use Alternate Drug. BCRP inhibitors may increase systemic exposure of talazoparib (a BCRP substrate). If coadministration cannot be avoided, monitor for potential adverse reactions.
- verapamil
verapamil will increase the level or effect of talazoparib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If coadministration with certain P-gp inhibitors (ie, amiodarone, carvedilol, clarithromycin, itraconazole, verapamil) cannot be avoided, reduce talazoparib dose to 0.75 mg qDay. Once P-gp inhibitors are discontinued, increase talazoparib dose (after 3-5 half-lives of the inhibitor) to dose used prior to initiating the P-gp inhibitor(s).
Monitor Closely (40)
- azithromycin
azithromycin will increase the level or effect of talazoparib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Talazoparib is a P-glycoprotein (P-gp) substrate; coadministration with P-gp inhibitors may increase talazoparib systemic exposure.
- berotralstat
berotralstat will increase the level or effect of talazoparib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Monitor or titrate P-gp substrate dose if coadministered.
- darolutamide
darolutamide will increase the level or effect of talazoparib by Other (see comment). Modify Therapy/Monitor Closely. Darolutamide is a BCRP inhibitor. Avoid coadministration with BCRP inhibitors. If use is unavoidable, closely monitor for adverse reactions and consider dose reduction of BCRP substrate drug (refer BCRP substrate prescribing information).
- dronedarone
dronedarone will increase the level or effect of talazoparib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Talazoparib is a P-glycoprotein (P-gp) substrate; coadministration with P-gp inhibitors may increase talazoparib systemic exposure.
- elagolix
elagolix will increase the level or effect of talazoparib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Talazoparib is a P-glycoprotein (P-gp) substrate; coadministration with P-gp inhibitors may increase talazoparib systemic exposure.
- eliglustat
eliglustat will increase the level or effect of talazoparib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Talazoparib is a P-glycoprotein (P-gp) substrate; coadministration with P-gp inhibitors may increase talazoparib systemic exposure.
- encorafenib
encorafenib will increase the level or effect of talazoparib by Other (see comment). Modify Therapy/Monitor Closely. Encorafenib (a BCRP inhibitor) may increase the concentration and toxicities of BCRP substrates. Closely monitor for signs and symptoms of increased exposure and consider adjusting the dose of these substrates.
- erythromycin base
erythromycin base will increase the level or effect of talazoparib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Talazoparib is a P-glycoprotein (P-gp) substrate; coadministration with P-gp inhibitors may increase talazoparib systemic exposure.
- erythromycin ethylsuccinate
erythromycin ethylsuccinate will increase the level or effect of talazoparib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Talazoparib is a P-glycoprotein (P-gp) substrate; coadministration with P-gp inhibitors may increase talazoparib systemic exposure.
- erythromycin lactobionate
erythromycin lactobionate will increase the level or effect of talazoparib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Talazoparib is a P-glycoprotein (P-gp) substrate; coadministration with P-gp inhibitors may increase talazoparib systemic exposure.
- erythromycin stearate
erythromycin stearate will increase the level or effect of talazoparib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Talazoparib is a P-glycoprotein (P-gp) substrate; coadministration with P-gp inhibitors may increase talazoparib systemic exposure.
- flibanserin
flibanserin will increase the level or effect of talazoparib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Talazoparib is a P-glycoprotein (P-gp) substrate; coadministration with P-gp inhibitors may increase talazoparib systemic exposure.
- fostamatinib
fostamatinib will increase the level or effect of talazoparib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Talazoparib is a P-glycoprotein (P-gp) substrate; coadministration with P-gp inhibitors may increase talazoparib systemic exposure.
- fostemsavir
fostemsavir will increase the level or effect of talazoparib by Other (see comment). Modify Therapy/Monitor Closely. Fostemsavir inhibits BCRP transporters. If possible, avoid coadministration or modify dose of BCRP substrate coadministered with fostemsavir.
- glecaprevir/pibrentasvir
glecaprevir/pibrentasvir will increase the level or effect of talazoparib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Talazoparib is a P-glycoprotein (P-gp) substrate; coadministration with P-gp inhibitors may increase talazoparib systemic exposure.
- grapefruit
grapefruit will increase the level or effect of talazoparib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Talazoparib is a P-glycoprotein (P-gp) substrate; coadministration with P-gp inhibitors may increase talazoparib systemic exposure.
- ibrutinib
ibrutinib will increase the level or effect of talazoparib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Talazoparib is a P-glycoprotein (P-gp) substrate; coadministration with P-gp inhibitors may increase talazoparib systemic exposure.
- istradefylline
istradefylline will increase the level or effect of talazoparib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Istradefylline 40 mg/day increased peak levels and AUC of P-gp substrates in clinical trials. Consider dose reduction of sensitive P-gp substrates.
- ivacaftor
ivacaftor will increase the level or effect of talazoparib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Ivacaftor and its M1 metabolite has the potential to inhibit P-gp; may significantly increase systemic exposure to sensitive P-gp substrates with a narrow therapeutic index.
- ketoconazole
ketoconazole will increase the level or effect of talazoparib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Talazoparib is a P-glycoprotein (P-gp) substrate; coadministration with P-gp inhibitors may increase talazoparib systemic exposure.
- ledipasvir/sofosbuvir
ledipasvir/sofosbuvir will increase the level or effect of talazoparib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Talazoparib is a P-glycoprotein (P-gp) substrate; coadministration with P-gp inhibitors may increase talazoparib systemic exposure.
- levoketoconazole
levoketoconazole will increase the level or effect of talazoparib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Talazoparib is a P-glycoprotein (P-gp) substrate; coadministration with P-gp inhibitors may increase talazoparib systemic exposure.
- lomitapide
lomitapide will increase the level or effect of talazoparib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Talazoparib is a P-glycoprotein (P-gp) substrate; coadministration with P-gp inhibitors may increase talazoparib systemic exposure.
- lonafarnib
lonafarnib will increase the level or effect of talazoparib by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. Lonafarnib is a weak P-gp inhibitor. Monitor for adverse reactions if coadministered with P-gp substrates where minimal concentration changes may lead to serious or life-threatening toxicities. Reduce P-gp substrate dose if needed.
- lopinavir
lopinavir will increase the level or effect of talazoparib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Talazoparib is a P-glycoprotein (P-gp) substrate; coadministration with P-gp inhibitors may increase talazoparib systemic exposure.
- mefloquine
mefloquine will increase the level or effect of talazoparib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Talazoparib is a P-glycoprotein (P-gp) substrate; coadministration with P-gp inhibitors may increase talazoparib systemic exposure.
- momelotinib
momelotinib increases toxicity of talazoparib by plasma protein binding competition. Modify Therapy/Monitor Closely. Momelotinib (BCRP inhibitor) may increase exposure of BCRP substrates, which may increase the risk of BCRP substrate adverse reactions. Dose adjustment of other BCRP substrates may necessary.
- neratinib
neratinib will increase the level or effect of talazoparib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Talazoparib is a P-glycoprotein (P-gp) substrate; coadministration with P-gp inhibitors may increase talazoparib systemic exposure.
- ombitasvir/paritaprevir/ritonavir & dasabuvir (DSC)
ombitasvir/paritaprevir/ritonavir & dasabuvir (DSC) will increase the level or effect of talazoparib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Talazoparib is a P-glycoprotein (P-gp) substrate; coadministration with P-gp inhibitors may increase talazoparib systemic exposure.
- oteseconazole
oteseconazole will increase the level or effect of talazoparib by Other (see comment). Modify Therapy/Monitor Closely. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.
- posaconazole
posaconazole will increase the level or effect of talazoparib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Talazoparib is a P-glycoprotein (P-gp) substrate; coadministration with P-gp inhibitors may increase talazoparib systemic exposure.
- propafenone
propafenone will increase the level or effect of talazoparib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Talazoparib is a P-glycoprotein (P-gp) substrate; coadministration with P-gp inhibitors may increase talazoparib systemic exposure.
- quinidine
quinidine will increase the level or effect of talazoparib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Talazoparib is a P-glycoprotein (P-gp) substrate; coadministration with P-gp inhibitors may increase talazoparib systemic exposure.
- quinine
quinine will increase the level or effect of talazoparib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Talazoparib is a P-glycoprotein (P-gp) substrate; coadministration with P-gp inhibitors may increase talazoparib systemic exposure.
- ranolazine
ranolazine will increase the level or effect of talazoparib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Talazoparib is a P-glycoprotein (P-gp) substrate; coadministration with P-gp inhibitors may increase talazoparib systemic exposure.
- ritonavir
ritonavir will increase the level or effect of talazoparib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Talazoparib is a P-glycoprotein (P-gp) substrate; coadministration with P-gp inhibitors may increase talazoparib systemic exposure.
- siponimod
siponimod and talazoparib both increase immunosuppressive effects; risk of infection. Use Caution/Monitor. Caution if coadministered because of additive immunosuppressive effects during such therapy and in the weeks following administration. When switching from drugs with prolonged immune effects, consider the half-life and mode of action of these drugs to avoid unintended additive immunosuppressive effects.
- tafamidis
tafamidis will increase the level or effect of talazoparib by Other (see comment). Use Caution/Monitor. Tafamidis inhibits breast cancer resistant protein (BCRP) in vitro and may increase exposure of BCRP substrates following tafamidis or tafamidis meglumine administration. Dosage adjustment of these BCRP substrates may be necessary.
- tafamidis meglumine
tafamidis meglumine will increase the level or effect of talazoparib by Other (see comment). Use Caution/Monitor. Tafamidis inhibits breast cancer resistant protein (BCRP) in vitro and may increase exposure of BCRP substrates following tafamidis or tafamidis meglumine administration. Dosage adjustment of these BCRP substrates may be necessary.
- tucatinib
tucatinib will increase the level or effect of talazoparib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Consider reducing the dosage of P-gp substrates, where minimal concentration changes may lead to serious or life-threatening toxicities.
Minor (0)
Adverse Effects
Adverse effects include all grades unless otherwise stated
>10%
Decreased hemoglobin (90%)
Decreased leukocytes (84%)
Decreased lymphocytes (76%)
Decreased neutrophils (68%)
Fatigue (62%)
Decreased platelets (55%)
Increased glucose (54%)
Anemia (53%)
Nausea (49%)
Increased AST (37%)
Increased alkaline phosphatase (36%)
Neutropenia (35%)
Increased ALT (33%)
Headache (33%)
Decreased calcium (28%)
Thrombocytopenia (27%)
Vomiting (25%)
Alopecia (25%)
Diarrhea (22%)
Decreased appetite (21%)
Abdominal pain (19%)
Dizziness (17%)
Leukopenia (17%)
Grade 3
- Decreased hemoglobin (39%)
- Anemia (38%)
- Neutropenia (18%)
- Decreased neutrophils (17%)
- Decreased lymphocytes (17%)
- Decreased leukocytes (14%)
- Thrombocytopenia (11%)
- Decreased platelets (11%)
1-10%
Dysgeusia (10%)
Dyspepsia (10%)
Stomatitis (8%)
Lymphopenia (7%)
Grade 3
- Decreased platelets (4%)
- Decreased neutrophils (3%)
- Fatigue (3%)
- Increased glucose (2%)
- Increased alkaline phosphate (2%)
- Vomiting (2%)
- Headache (2%)
- Increased AST/ALT (1-2%)
- Decreased calcium (1%)
Grade 4
- Thrombocytopenia (4%)
- Neutropenia (3%)
- Anemia (1%)
<1%
Decreased appetite, Grade 3
Nausea, Grade 3
Decreased lymphocytes, Grade 4
Decreased leukocytes, Grade 4
Warnings
Contraindications
None
Cautions
Based on its mechanism of action and findings from animal data, fetal harm may occur when administered to a pregnant woman (see Pregnancy)
Myelosuppression
- Myelosuppression (eg, anemia, leukopenia/neutropenia, and/or thrombocytopenia) reported; monitor blood counts monthly during treatment
- If hematological toxicities do not resolve within 28 days, discontinue therapy and refer patient to a hematologist for further investigations including bone marrow analysis and blood sample for cytogenetics
Myelodysplastic syndrome/acute myeloid leukemia
- Myelodysplastic syndrome/acute myeloid leukemia (MDS/AML) reported; MDS/AML reported (0.3%) in solid tumor in clinical studies; duration of treatment in these patients prior to developing MDS/AML was 4 months and 24 months, respectively
- Do not start until patients have adequately recovered from hematological toxicity caused by previous chemotherapy; Monitor blood counts monthly during treatment
- For prolonged hematological toxicities, interrupt and monitor blood cell counts weekly until recovery; if levels do not recover within 4 weeks, refer patient to a hematologist for further investigations
- If MDS/AML is confirmed, discontinue treatment
Drug interactions overview
- P-gp and BCRP transporters substrate
-
Effect of P-gp inhibitors
- Coadministration with P-gp inhibitors may increase talazoparib exposure
- In clinical studies, coadministration with P-gp inhibitors (ie, amiodarone, carvedilol, clarithromycin, itraconazole, verapamil) resulted in an ~45% increase in talazoparib exposure and an increase in the rate of talazoparib dose reduction
- When coadministering with P-gp inhibitors not listed above, monitor for potential increased adverse reactions
-
Effect of BCRP inhibitors
- Coadministration with BCRP inhibitors may increase talazoparib exposure
- If coadministration cannot be avoided, monitor potential increased adverse reactions when coadministering
Pregnancy
Pregnancy
Based on findings from animal studies and its mechanism of action, embryofetal harm may occur when administered to pregnant females
No data available on use in pregnant females to inform a drug-associated risk
Verify pregnancy status in females of reproductive potential prior to initiating treatment
Animal data
- Administration to pregnant rats during organogenesis caused fetal malformations and structural skeletal variations and embryofetal death at maternal exposures that were 0.24 times the AUC in patients receiving the recommended dose of 1 mg qDay
Contraception
- Females of reproductive potential: Use effective contraception during treatment and for ≥7 months following the last dose
- Males with female partners of reproductive potential and pregnant partners: Use effective contraception during treatment and for ≥4 months following the last dose
Infertility
- Based on animal studies, impaired fertility in males of reproductive potential may occur
Lactation
There are no data on the presence of talazoparib in human milk, its effects on milk production, or on breastfed children
Advise lactating women not to breastfeed during treatment and for ≥1 month after the final dose
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Poly ADP ribose polymerase (PARP) inhibitor; PARP enzymes are involved in normal cellular homeostasis, such as DNA transcription, cell cycle regulation, and DNA repair
Absorption
Peak plasma concentration, steady-state: 16.4 ng/mL
Peak plasma time: 1-2 hr
AUC, steady-state: 208 ng·hr/mL
Steady-state reached within 2-3 weeks
Food effect
- Following a single oral 0.5-mg dose with high-fat, high-calorie food (~800-1000 calories with 150, 250, and 500-600 calories from protein, carbohydrate, and fat, respectively), mean peak plasma concentration of talazoparib was decreased by 46%, the median peak plasma time was delayed from 1-4 hr, and AUC was not affected
Distribution
Vd: 420 L
Protein bound: 74%
Metabolism
Undergoes minimal hepatic metabolism
Identified metabolic pathways of talazoparib in humans include mono-oxidation, dehydrogenation, cysteine conjugation of mono-desfluoro-talazoparib, and glucuronide conjugation
Elimination
Half-life: 90 hr
Clearance: 6.45 L/hr
Excretion: Urine (~68.7% [54.6% unchanged]), feces (19.7% [13.6% unchanged])
Administration
Oral Administration
Administer orally with or without food
Swallow hard capsules whole; do not open or dissolve
If patient vomits or misses a dose, do not take an additional dose; take next dose at usual time
Storage
Capsules: Store at 20-25ºC (68-77ºF); excursions permitted between 15-30ºC (59-86ºF)
Images
Formulary
Adding plans allows you to compare formulary status to other drugs in the same class.
To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.
Adding plans allows you to:
- View the formulary and any restrictions for each plan.
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- Compare formulary status to other drugs in the same class.
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