TABLE 2.
In vitro drug concentration | Breakthrough frequency (resistance development) |
|||||||
---|---|---|---|---|---|---|---|---|
BIC+FTC+TAF |
DTG+FTC+TAF |
DTG+3TC |
DTG+RPV |
|||||
VB (n/N; %) [first day of VB] | With resistance, Na | VB (n/N; %) [first day of VB]b | With resistance, Na | VB (n/N; %) [first day of VB] | With resistance, Na | VB (n/N; %) [first day of VB] | With resistance, Na | |
C min | 0/60; 0 [NA] | 0 | 0/48; 0 [NA] | 0 | 0/60; 0 [NA] | 0 | 0/48; 0 [NA] | 0 |
Cmin−1 | 0/36; 0 [NA] | 0 | 0/48; 0 [NA] | 0 | 0/36; 0 [NA] | 0 | 0/48; 0 [NA] | 0 |
Cmin−2 | 0/60; 0 [NA] | 0 | 0/48; 0 [NA] | 0 | 41/60; 68 [14] | 13; RT, M184V/I (4), V75I (3); IN, G140E/R (2), E157K (2), L74M (1), S153F (1) | 0/48; 0 [NA] | 0 |
Cmin−3 | 3/36; 8 [21] | 0 | 1/48; 2 [25] | 0 | 36/36; 100 [7] | 3; RT, none; IN, L74M (2), V72A (1), S153F (1) | 7/48; 15 [14] | 1; RT, M230I; IN, none |
Cmin−4 | 18/36; 50 [15] | 3; RT, M184I (2); IN, G163R (1) | 48/48; 100 [11] | 6; RT, M184V (1), K219R (1); IN, Q148R (2), Q95R (1), H51Y (1), S153F (1) | 36/36; 100 [5] | 2; RT, none; IN, R263K (2), L74M (1) | 45/48; 94 [8] | 20; RT, E138K (8), K101E (3), M230I (2), V90I (2), V106I (1), Y181C (1), H221Y (1); IN, H51Y (2), R263K (1), M50I (1), Q95R (1), A128T (1), S153F (1), G163R (1) |
Reverse transcriptase (RT) substitutions are shown in plain text. Integrase (IN) substitutions are shown in italics. Some viral breakthrough supernatants had more than one emergent resistance mutation, as listed here: DTG+3TC Cmin−3, 1 L74M+S153F in IN; DTG+3TC Cmin−4, 1 L74M+R263K in IN; DTG+FTC+TAF Cmin−4, 1 M184V in RT + Q95R in IN; DTG+RPV Cmin−4, 1 V90I+V106I+E138K in RT, 1 Y181C in RT + H51Y in IN, 1 E138K in RT + H51Y in IN, 1 E138K in RT + Q95R in IN, and 1 E138K in RT + A128T in IN.
VB, viral breakthrough; NA, not applicable.