TABLE 1.

Distribution of [¹⁴C]E5531 in plasma samples from five human subjects^a

Subject	Total cholesterol level (mg/dl)	% of added drug recovered in:			% Recovery of total drug
		HDL fraction	LDL-VLDL fraction	LPDP fraction
I	83	81.1 ± 0.3	8.9 ± 0.1	0.8 ± 0.2	90.8 ± 3.5
II	161	71.4 ± 1.3	18.0 ± 0.3	2.2 ± 1.1	91.6 ± 4.1
III	190	73.8 ± 0.3	20.1 ± 0.3	0.8 ± 0.2	94.7 ± 7.4
IV	206	59.8 ± 2.5	25.5 ± 0.5	5.9 ± 1.4	91.2 ± 4.4
V	236	66.3 ± 1.9	33.1 ± 1.2	6.3 ± 0.3	105.7 ± 0.8

^aPlasma was incubated for 5 min at 37°C with 0.64 μM [¹⁴C]E5531, separated into lipoprotein and lipoprotein-deficient fractions by affinity chromatography and centrifugation, and assayed for radioactivity as described in the Materials and Methods section. Data are expressed as means ± standard deviations; n equals 3 individual replicates for subjects I to III, n equals 5 individual replicates for subject IV, and n equals 6 individual replicates for subject V. LPDP, lipoprotein-deficient plasma which contains albumin and alpha-1-glycoprotein; VLDL includes chylomicrons. Binding in the HDL fraction demonstrates an inverse trend with the total cholesterol level (r = 0.819; P = 0.0902), while the amount of drug recovered in the LDL-VLDL fraction increased as a function of increasing total cholesterol level (r = 0.965;P = 0.0078).