 |
|
 TABLE 2-10:
|
Resistance Mutations (Continued)
|
|
| Drug |
Major
mutations |
Minor mutations |
Comments |
FPV
and
FPV/r |
50V, 84V |
10F/I/R/V, 32I, 46I/L,
47V, 54L/V/M, 73S,
76V, 82A/F/T/S, 90M |
50V associated with cross-resistance to LPV. 50V, 84V, 32I, 54L/M, 47V decrease DRV susceptibility. 10V, 47V, 54M, 84V decrease TPV susceptibility. PI mutations unlikely to be selected by FPV/r in PI-naive patients. |
| LPV/r |
32I,
47V/A,
82A/F/T/S |
10F/I/R/V, 20M/R,
24I, 33F, 46I/L, 50V,
53L, 54V/L/A/M/T/S,
63P, 71V/T, 73S,
76V, 84V, 90M |
Most PI-naïve patients failing LPV/r as first PI have no PI mutations. 47A confers intermediate-to-high level LPV resistance. |
| TPV/r |
33F,
82L/T,
84V |
10V, 13V, 20M/R,
35G, 36I, 43T, 46L,
47V, 54A/M/V, 58E,
69K, 74P, 83D, 90M |
Best response seen with 0-1 TPV mutations. Intermediate response with 2-7 mutations. Minimal response 8 or more mutations. |
| DRV/r |
50V,
54M/L,
76V, 84V |
11I, 32I, 33F, 47V,
74P, 89V |
Reduced response with increasing DRV mutations; poor response with ≥3 mutations. |
ATV
and
ATV/r |
50L, 84V,
88S |
10I/F/V/C, 16E,
20R/M/I/T/V, 24I,
32I, 33I/F/V, 36I/L/V,
46I/L, 48V, 53L/Y,
54L/V/M/T/A, 60E,
62V, 64I/M/V,
71V/I/T/L,
73C/S/T/A,
82A/T/F/I, 85V,
90M, 93L/M |
50L causes no PI cross-resistance, and possible hypersusceptibility to other PIs. Reduced in vivo activity associated with ≥3 of the following: 10F/V/I, 16E, 33F/I/V, 46I/L, 60E, 84V, 85V. Selection of PI mutations uncommon with ATV/r in PI-naive patients. Another report showed 75% or 0% response with 2 or > 3 of the following: 10V/I/C, 32I, 34Q, 46I/L, 53L, 54 A/M/V, 82A/F/I/T and 184 V |
| Fusion inhibitors: gp 41 mutations |
| ENF |
|
36D/S, 37V,
38A/M/E, 39R, 40H,
42T, 43D |
Mutations in other envelope regions may affect sensitivity. |
| CCR5 antagnosits: gp 120 mutations |
| MVC |
|
|
Activity is limited to patients with purely R5- tropic virus. Mutations can occur in gp120 that allow HIV binding to R5 receptors in the presence of MVC, show reduction in maximum % inhibition (MPI rather than the standard IC50). This resistance profile is too complex for listing and the frequency of these mutations is not known (Topics in HIV Med 2007; 15:119) |
|
| (continued) |
|
