TABLE 2.

Activity of VRX-480773 against a panel of 94 clinical NNRTI-resistant HIV-1 isolates

Isolate	NNRTI mutation(s)	% of NNRTI-resistant isolatesa	Change (fold) in EC50b
			VRX-480773	Efavirenz	Nevirapine
1	103N	21.571	0.7	14.0	51.0
2	103N, 181C	6.145	10.0	>100	>100
3	181C	4.941	10.0	6.7	>100
4	100I, 103N	4.498	0.9	>100	42.0
5	106I	3.611	0.9	0.7	1.1
6	98G	2.597	2.4	2.9	5.9
7	101Q	2.534	2.2	2.5	2.8
8	103N, 225H	2.407	1.6	>100	>100
9	103N, 225H	2.407	1.0	89.0	93.0
10	188L	2.312	11.0	86.0	>100
11	103N, 108I	2.249	1.3	>100	>100
12	179D	1.932	3.3	5.7	4.2
13	190A	1.457	13.0	18.0	>100
14	181C, 190A	1.457	>100	14.0	>100
15	103N, 190A	1.425	76.0	>100	>100
16	101E	1.362	11.0	16.0	42.0
17	108I	1.362	1.5	1.7	2.3
18	103N, 181C, 190A	1.172	>100	>100	>100
19	101E, 190A	1.109	83.0	>100	>100
20	103N, 238T	1.077	0.6	31.0	>100
21	98G, 103N	1.014	4.4	>100	>100
22	101Q, 103N	0.887	5.2	>100	>100
23	101P, 103N	0.855	2.2	>100	>100
24	179E	0.824	2.4	4.1	1.9
25	103N, 108I, 181C	0.697	6.2	72.0	>100
26	103N, 188L	0.665	3.9	>10.0	>100
27	106A	0.634	6.0	5.7	>100
28	108I, 181C	0.602	14.0	5.3	>100
29	101E, 181C, 190A	0.602	>100	>100	>100
30	179A	0.570	0.6	0.5	0.4
31	106A, F227L	0.570	>100	>100	>100
32	98G, 181C	0.570	11.0	17.0	>100
33	101Q, 181C, 190A	0.570	>100	43.0	>100
34	190S	0.507	3.9	97.0	>100
35	101E, 190S	0.475	16.0	>100	>100
36	190E	0.443	>100	>100	>100
37	106I, 188L	0.443	62.0	>100	>100
38	103N, 106A	0.412	2.6	26.0	>100
39	179G	0.348	0.3	0.2	0.1
40	227L	0.348	0.47	0.80	2.10
41	103R, 179D, 188L	0.348	>100	>100	>100
42	101E, 181C	0.317	>100	>100	>100
43	103N, 106M	0.317	12.0	>100	>100
44	103N, 106I	0.317	1.8	28.0	122.0
45	103S, 190A	0.285	>100	>100	>100
46	181I	0.285	5.4	1.4	>100
47	179T	0.285	1.3	0.8	0.5
48	101E, 181C, 190S	0.285	>100	>100	>100
49	101Q, 103R	0.285	0.6	1.2	1.3
50	103R, 179D	0.285	0.3	0.9	1.3
51	103N, 108I, 225H	0.253	2.6	>100	>100
52	98G, 103N, 108I	0.253	2.2	>100	>100
53	101P, 190A	0.253	92.0	>100	>100
54	101R, 103N	0.253	1.2	37.0	>100
55	101Q, 190S	0.253	2.4	>100	>100
56	98G, 190A	0.253	16.0	64.0	>100
57	106A, 190A	0.253	>100	>100	>100
58	101Q, 181C, 190S	0.253	>100	>100	>100
59	101E, 103N	0.222	0.9	52.0	>100
60	101Q, 181C	0.222	8.9	4.4	>100
61	236L	0.222	0.9	0.2	0.5
62	101H, 190A	0.222	32.0	77.0	>100
63	98G, 188L	0.222	>100	>100	>100
64	98G, 103N, 181C	0.190	4.2	>100	>100
65	101E, 108I, 181C, 190A	0.190	>100	>100	>100
66	103N, 108I, 238T	0.190	2.5	>100	>100
67	98G, 100I, 103N	0.190	1.4	>100	>100
68	100I, 103N, 108I	0.190	1.9	>100	>100
69	103N, 188H	0.190	3.5	>100	>100
70	188H	0.190	1.6	8.7	>100
71	98G, 101E, 181C, 190A	0.190	65.0	71.0	>100
72	103Q	0.190	1.4	1.7	1.0
73	101H	0.190	2.5	4.1	12.0
74	103N, 108I, 181C, 190A	0.190	>100	>100	>100
75	179D, 188L	0.158	>100	>100	>100
76	103N, 108I, 190A	0.158	20.0	>100	>100
77	108I, 181C, 190A	0.158	>100	400	>100
78	101Q, 103N, 225H	0.158	3.9	>100	>100
79	98G, 103N, 181C, 190A	0.158	82.0	>100	>100
80	103N, 190S	0.158	18.0	>100	>100
81	106A, 181C	0.158	16.0	8.2	>100
82	98G, 108I, 181C	0.158	15.0	47.0	>100
83	238N	0.158	0.7	0.8	1.9
84	238T	0.127	2.2	3.0	100
85	103N, 238N	0.127	2.3	>100	>100
86	103S	0.127	2.7	8.6	39.0
87	230L	0.127	11.0	16.0	46.0
88	101R, 103N, 181C, 190A	0.127	>100	>100	>100
89	101E, 103N, 190A	0.127	50.0	>100	>100
90	101N, 103N	0.127	0.6	26.0	32.0
91	181V	0.127	20.0	4.5	>100
92	106L, 188L	0.127	>100	>100	>100
93	179D, 181C	0.127	>100	>100	>100
94	100F	0.127	1.8	1.6	2.4
Total		88.312

^aPrevalance of mutation patterns was determined from sequence data in the Stanford HIV Resistance database (14).

^bChanges (n-fold) in EC₅₀ relative to that against wt virus.