Table 3.

Day 1 Plasma Pharmacokinetics Parameters After Single Subcutaneous or Oral Azacitidine Administration

Dose	No. of Patients	AUCinf(ng × h/mL)			CL/F (L/h)			Cmax (ng/mL)			Tmax (h)		Vd/F (L)			F (%)
		Mean	SD	%CV	Mean	SD	%CV	Mean	SD	%CV	Median	Range	Mean	SD	%CV	Mean	SD	Relative Oral Bioavailability
Subcutaneous, 75 mg/m2	42	1,020	440	43*	175	128	73*	650	250	39	0.50	0.2-1.1	410	410	101*	NA
Oral, mg
120	4	62	43	70	4,100	4,860	118	38	24	64	1.48	1.0-2.0	2,930	3,810	130	8.1	5.6	69
180	3	112	64	58	2,330	1,890	81	72	36	50	1.50	1.0-1.5	1,700	1,580	93	6.3	2.3	37
240	3	463	221	48	598	258	43	215	102	47	1.00	1.0-1.5	814	421	52	20.0	9.6	48
300	5	282	88	31	1,180	487	41	144	13	9.2	1.48	1.0-2.0	1,090	626	57	11.5	2.6	23
360	5	311	141	45	1,360	573	42	195	79	40	1.00	0.5-3.6	947	251	27	12.8	2.4	19
480	14	362	253	70	2,140	1,620	76	211	140	66	1.00	0.3-2.5	2,010	1,910	95	12.8	9.4	74†
600	2	502	100	20	1,220	244	20	253	29	12	1.50	1.0-2.0	1,580	1,410	89	14.9	0.8	5

Abbreviations: AUC_inf, area under the plasma concentration–time curve from time zero to infinity; CL/F, apparent total clearance; C_max, maximum observed plasma concentration; F, relative oral bioavailability; NA, not applicable; T_max, time of maximum observed plasma concentration; Vd/F, apparent volume of distribution.

^*n = 40.

^†n = 13.