Table 1

Summary of pharmacokinetic and dose schedules

PARPi	Dose	Terminal half-life	Target and affinity	Metabolism	Baseline renal adjustment	Hepatic adjustment	Food	Interaction	Storage
Olaparib tablet	300 mg twice daily DL -1: 250 mg twice daily DL -2: 200 mg twice daily Capsule formulation 400 mg twice daily DL -1: 200 mg twice daily DL -2: 100 mg twice daily* Capsule and tablet doses are not bioequivalent.	15 hours	PARP1++ PARP2++++	CYP3A4/5	Mild (CrCl 51–80 mL/min): no adjustment Moderate (CrCl 31–50 mL/min): 200 mg twice daily Severe (≤30 mL/min): no data	Mild: no adjustment Moderate-severe: no data	Can be taken with/without food. Avoid grapefruit, pomegranate, star fruit, and Seville oranges.	CYP3A inhibitor (eg, itraconazole, fluconazole. CYP3A inducer (eg, rifampizine, efivarenz) If administered with strong CYP3A inhibitor: reduce olaparib to 100 mg twice daily. Moderate inhibitor: olaparib 150 mg twice daily.	Store between 2°C and 30°C in original package
Niraparib capsule	300 mg once daily * DL -1: 200 mg once daily DL -2: 100 mg once daily	36−48 hours	PARP1+++ PARP2+++	Metabolized by carboxylesterases, to form an inactive metabolite, which undergoes glucorinidation	Mild to moderate (CrCl 30–89 mL/min): no adjustment Severe (≤30 mL/min): no data	Mild: no adjustment Moderate-severe: no data	Can be taken with/without food	Niraparib is a weak inducer of CYP1A2. Caution is recommended for drugs that are sensitive substrates of CYP1A2. Niraparib is also a substrate and weak inhibitor of P-gp, and weak inhibitor of BCRP. Caution with drugs that use these transporters.	Store up to 25°C in original package
Rucaparib tablet	600 mg twice daily DL -1: 500 mg twice daily DL -2: 400 mg twice daily DL -3: 300 mg twice daily	17–19 hours	PARP++++	Mainly CYP2D6 CYP1A2 and CYP3A4 to a lesser extent	Mild to moderate (CrCl 30–89 mL/min): no adjustment Severe (≤30 mL/min): no data	Mild: no adjustment Moderate-severe: no data	Can be taken with/without food. Rucaparib may increase the blood levels and effects of caffeine.	CYP1A2, CYP3A4, CYP2C9, CYP2C19, P-gp and BCRP inhibitor. Caution with sensitive substrates.	Store between 20°C to 25°C in original package
Veliparib capsule	With chemotherapy†: 150 mg twice daily DL -1: 100 mg twice daily DL-2: 50 mg twice daily Maintenance: 400 mg twice daily DL-1: 300 mg twice daily DL -2: 250 mg twice daily	6 hours	PARP1++ PARP2+++	Mainly CYP2D6	Mild (CrCl 60–89 mL/min): no adjustment Recommend dose adjust according to CrCl	Mild: no adjustment Moderate-severe: no data	Can be taken with/without food	Drug interactions are unlikely	Store between 15°C and 25°C in original package
Talazoparib capsule	1 mg once daily DL -1: 0.75 mg once daily DL -2: 0.5 mg once daily DL -3: 0.25 mg once daily	90 hours	PARP1++++	Minimal hepatic metabolism.	Mild (CrCl 60–89 mL/min): no adjustment Moderate (CrCl 31–59 mL/min): 0.75 mg Severe (≤30 mL/min): no data	Mild: no adjustment Moderate-severe: no data	Can be taken with/without food.	P-gp inhibitors (eg, amiodarone, carvedilol, clarithromycin, itraconazole, verapamil). Reduce talazoparib dose.	Store between 15°C and 30°C in original package

*Niraparib starting dose to be calculated based on baseline platelets and weight. If weight <77 kg or platelet count <150×10⁹ cells/L, a starting dose of 200 mg daily is recommended.
†Veliparib in combination with carboplatin and paclitaxel as part of VELIA clinical trial.
BCRP, breast cancer resistance protein; CrCl, creatinine clearance; CYP, cytochrome P450; DL, Dose level; PARPi, poly (ADP-ribose) polymerase (PARP) inhibitor; P-gp, P-glycoprotein.