Table 2.

PK Concentration Ranges

Study	Route	Sample Collected	AUC (h*µM)	HL (h)	C max (µM)	T max (h)	CL
5-AZA PK	IV	Plasma	2.4–3.2	0.25–0.29	4.6–7.6	0.5	95.4–130.0 l/h/ m2
		Ventricular CSF	3 samples quantifiable (n = 2) Not detectable (n = 1)
	IT-V	Plasma	0.17–0.44	0.52–1.4	0.15–0.33	0.08–1.0
		Lumbar CSF	1234.6–5368.4	0.49–0.91	1035.3–3015.7	0.45–1.1	0.13–0.55 ml/ min
	IT-L	Plasma	0.24–0.74	0.28–1.8	0.16–1.54	0.08–0.5
		Ventricular CSF	7.5–19.3	0.52–0.84	6.1–9.8	0.5–1.1	35.3–91.0 ml/ min
5-AZA MD/PK	IT-C	Plasma	0.14–0.18	1.1–1.3	0.06–0.10	0.50
		Subarachnoid CSF	187.6–1313.6	0.7–1.3	57.5–753.9	0.5–2.0	0.52–3.6 ml/ min
5-AZA and inulin PK	IT-V	Plasma	2 samples quantifiable (n = 2) at 2 h Not detectable (n = 1)
		Lumbar CSF	1108.91–2747.94	0.75–2.2	434.0–1820.64	0.32–1.0	0.25–0.62 ml/ min

CSF, cerebrospinal fluid; PK, pharmacokinetics; IV, intravenous; AUC, area under the curve; HL, half-life; CL, clearance; 5-AZA, 5-azacytidine; MD, microdialysis; IT-V, intraventricular; IT-L, intralumbar; IT-C, intracisternal.

A mean CSF flow rate of 0.018 ± 0.003 ml/min was determined by IT-V administration of inulin.