5. PK parameters and PARP inhibition following twice daily fluzoparib dosing.

PK Parameter	80 mg bid (n=10)				100 mg bid (n=13)				150 mg bid (n=13)
	Mean	SD	CV (%)		Mean	SD	CV (%)		Mean	SD	CV (%)
PK, pharmacokinetic; PARP, poly(ADP-ribose) polymerases; Tmax, time to peak concentration (Cmax); Css,max, Cmax at steady state; Css,min, minimum concentration at steady state; Css,avg, average steady-state concentration; AUC0–10 h, area under the curve from time 0 to10 h; λz, first-order rate constant of terminal phase; t1/2, terminal half-life; CLss/F, apparent total clearance of the drug at steady state; Vz/F, apparent volume of distribution; DF, coefficient of fluctuation; Rac_Cmax, accumulation in terms of Cmax; Rac_AUC, accumulation in terms of AUC; SD, standard deviation; CV, coefficient of variation.
Tmax(h)	2.50 (1.00−3.00)	−	−		3.00 (2.00−6.00)	−	−		3.00 (1.00−4.00)	−	−
Css,max(μg/mL)	5.18	1.68	32.4		5.94	2.99	50.3		8.45	1.83	21.6
Css,min(μg/mL)	2.69	1.07	39.8		3.15	1.96	62.4		4.06	1.05	25.8
Css,avg (μg/mL)	3.82	1.26	32.8		4.52	2.55	56.4		6.08	1.34	22.1
AUC0−10 h(h·μg/mL)	38.2	12.6	32.8		45.2	25.5	56.4		60.8	13.4	22.1
λz(1/h)	0.0706	0.0286	40.5		0.0763	0.0306	40.1		0.0800	0.0177	22.2
t1/2(h)	11.40	4.86	42.6		10.80	4.78	44.4		9.14	2.38	26.0
CLss/F (L/h)	2.31	0.76	32.9		2.96	1.69	57.0		2.58	0.57	22.0
Vz/F (L)	35.8	14.9	41.6		38.5	27.6	71.6		34.6	14.5	41.9
DF (%)	66.7	12.0	18.0		68.1	17.8	26.2		73.2	17.3	23.7
Rac_Cmax	2.09	0.52	24.7		1.73	0.41	23.4		1.76	0.33	18.7
Rac_AUC	2.23	0.51	22.8		2.08	0.39	18.5		1.86	0.35	18.7