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. 2019 Sep 19;2(3):665–679. doi: 10.20517/cdr.2019.002

Table 2.

Pharmacological features of PARP inhibitors

PARP inhibitor (trade name) Dose/formulation Mean half-life Metabolism Renal dose adjustment Hepatic dose adjustment
Veliparib (ABT-888) Not yet approved for any indication; differing doses in clinical trials; recommended phase II dose (MTD) for single agent veliparib is 400 mg BID[54] 5.2 hours[54] Metabolism has a secondary role in clearance (mostly renal clearance). CYP2D6 is major enzyme metabolizing veliparib, with minor contribution from CYP1A2[55] Not yet available Not yet available
Rucaparib (Rubraca) Two 300 mg tablets BID 17-19 hours Primarily hepatic by CYP1A2, CYP2D6, CYP3A4 CrCl ≥ 30 mL/min: no dose adjustment necessary;
CrCl < 30 mL/min: has not been studied
Mild impairment: no dose adjustment necessary;
Moderate-severe impairment: has not been studied
Olaparib (Lynparza) Two 150 mg tablets BID, or three 100 mg tablets BID (replacing 400 mg capsules BID) 14.9 +/- 8.2 hours Primarily hepatic by CYP3A4 CrCl 51-80 mL/min: no dose adjustment;
CrCl 31-50 mL/min: dose reduction;
CrCl < 30 mL/min: has not been studied
Mild to moderate impairment: no dose adjustment necessary;
Severe impairment: has not been studied*
Niraparib (Zejula) Three 100 mg capsules once daily 36 hours Primarily by carboxylesterases CrCl ≥ 30 mL/min: no dose adjustment necessary;
CrCl < 30 mL/min: has not been studied
Mild impairment: no dose adjustment necessary;
Moderate-severe impairment: has not been studied
Talazoparib (Talzenna) 1 mg capsule once daily 90 hours Minimal hepatic metabolism; metabolic pathways include mono-oxidation, dehydrogenation, cysteine conjugation of mono-desfluoro-talazoparib, and glucuronide conjugation CrCl 60-89 mL/min: no dose adjustment;
CrCl 30-59 mL/min: dose adjustment;
CrCl < 30 mL/min: has not been studied
Mild impairment: no dose adjustment necessary;
Moderate-severe impairment: has not been studied

MTD: maximum tolerated dose; BID: twice a day; CrCl: creatinine clearance; *: For olaparib tablet formulation