TABLE 5.

Pharmacokinetic properties of expanded spectrum NNRTIs

NNRTI	Concn (μM) at 24 h ina:		t1/2 (h)	Free drug concn (nM) at 24 h	t1/2 (h)	Ratio of trough level of free drug in chimpanzees: IC90 of free drug
	Rhesus monkey	Chimpanzee				Wild type	K103N	K103N-V108I	K103N-P225H	K103N-L100I
DPC 082	0.64	4.7	5.9	141	14.2	128	13	1.2	1.5	0.5
DPC 083	6.84	7.6	24	152	85.7	190	14	4.3	2.8	0.2
DPC 961	0.38	12.7	4.8	191	76.0	318	62	16	8.3	0.6
DPC 963	0.22	6.2	4.8	174	19.6	348	44	13	10	0.5
Efavirenz	0.36	2.7	NAb	6–15	NA	12–30	0.4–0.9	0.09–0.2	0.07–0.2	0.003–0.008

^aEach drug was administered to rhesus monkeys orally at 10 mg/kg. Data for chimpanzees, which were given 2 mg/kg, are extrapolated from data for rhesus monkeys. 

^bNA, not available.