Table 6.

Effect of food on the pharmacokinetics of PARP inhibitors after a single dose

PARP inhibitor	Condition	N	Dose (mg)	t½ (h)	Tmax (h)	Cmax (ng/mL)	AUC0–last (ng × h/mL)	AUC0–∞ (ng × h/mL)	Result meal vs fasted state	References
Olaparib capsules	High-fat meal	31	400	12.20 ± 4.53a	4.03 (2.00–8.03)a	6,070 (45.1%)a	64,620 (63.3%)a	65,440 (64.2%)a	↓ t½ 34% ↑ Tmax 134% ↔Cmax ↑AUC0–last 22% ↑AUC0–∞ 19%	[139]
	Standard meal	31	400	15.42 ± 5.92a	4.00 (1.00–8.00)b	6,970 (45.9%)b	67,710 (86.4%)c	70,190 (80.5%)a	↓ t½ 16% ↑ Tmax 133% ↑Cmax 10% ↑AUC0–last 20% ↑AUC0–∞ 21%
	Fasted	31	400	18.39 ± 6.99b	1.72 (0.92–4.05)d	6,350 (40.9%)d	58,400 (75.6%)d	61,060 (78.1%)b
Olaparib tablets	High-fat meal	54	300	11.1 ± 4.09e	4.00 (1.00–12.0)	5,480 (40.5%)	46,000 (56.6%)e	45,400 (57.1%)e	↔ t½ ↑ Tmax 167% ↓Cmax 21% ↑AUC0–last 8% ↑AUC0–∞ 8%	[36]
	Fasted	55	300	12.2 ± 5.31f	1.50 (0.50–5.85)	7,000 (35.0%)	43,600 (54.3%)f	43,000 (55.2%)g
Niraparib	High-fat meal	15	300	47.9 ± 17.5h	8.0 ± 4.9i	582.1 (39%)	27,186.4 (52%)	31,194 (54%)h	↔ t½ ↑ Tmax 128% ↓Cmax 27% ↔AUC0–last ↔AUC0–∞	[61]
	Fasted	16	300	50.5 ± 17.9	3.5 ± 1.2i	803.7 (50%)	28,638.1 (63%)	29,016.1 (63%)j
Rucaparib	High-fat meal	26	600	16.8 ± 9.5k	7.83 (1.5–24.45)	959 (73%)	13,900l (74%)	NR	↔ t½ ↑ Tmax 95% ↑Cmax 20% ↑AUC0–24h 38%	[91]
	Fasted	26	600	18.7 ± 9.9m	4.02 (0.53–24.83)	819 (84%)	10,000l (76%)	NR
Talazoparib	High-fat meal	18	0.5	113.6 ± 38.3	4.00 (0.75–5.00)	0.996 (22%)	58.215 (19%)	61.065 (19%)	↔ t½ ↑ Tmax 300% ↓Cmax 46% ↔AUC0–last ↔AUC0–∞	[102]
	Fasted	18	0.5 g	116.7 ± 31.9	1.00 (0.50–1.52)	1.849 (41%)	59.694 (19%)	62.551 (18%)

AUC area under the plasma concentration–time curve, AUC_0–24h AUC from zero to 24 hours, AUC_0–last AUC from zero to the last measurable timepoint, AUC_0–∞ AUC from zero to infinity, C_max maximum plasma concentration, CV% percentage coefficient of variation, N number of subjects, NR not reported, PARP poly (ADP-ribose) polymerase, SD standard deviation, t_½ elimination half-life, T_max time to maximum plasma concentration, ↑ indicates increase, ↓ indicates decrease, ↔ indicates no change

Data are presented as mean (CV%) for C_max, AUC_0–last and AUC_0–∞, as median (range) for t_max and mean ± SD for t_1/2

^aBased on 27 patients

^bBased on 29 patients

^cBased on 28 patients

^dBased on 30 patients

^eBased on 51 patients

^fBased on 54 patients

^gBased on 52 patients

^hBased on 14 patients

ⁱt_max is presented as mean ± SD

^jBased on 15 patients

^kBased on 11 patients

^lAUC_0–24h,^m based on 19 patients