TABLE 6.
Resistance selection with NNRTIs in HIV-1 subtype B virus in the presence of 10% FBS or 50% HS under high-MOI conditionse
| Serum | Inhibitor | Concn (nM) | Expt 1 |
Expt 2 |
Expt 3 |
|||
|---|---|---|---|---|---|---|---|---|
| Ta | Mutation(s) | T | Mutation(s) | T | Mutation | |||
| 10% FBS | MK-4965 | 40 | 13 | V106A | 13 | V106A | 15 | V106A |
| 200 | NBb | NAd | NB | NA | 36 | V106A | ||
| 1,000 | NB*c | NA | NB* | NA | NB* | NA | ||
| EFV | 40 | 12 | L100I | 13 | L100I | 12 | K103N | |
| 200 | NB | NA | NB | NA | NB | NA | ||
| 1,000 | NB | NA | NB | NA | 34 | G190V | ||
| ETV | 40 | NB | NA | 28 | Y181C | NB | NA | |
| 200 | NB | NA | NB | NA | NB | NA | ||
| 1,000 | NB | NA | NB | NA | NB | NA | ||
| 50% HS | MK-4965 | 200 | 13 | V106A | 10 | V106A | ||
| 500 | 15 | V106A | 15 | V106A | ||||
| 1,250 | 20 | V106A/V189I/V108I | 20 | V106A | ||||
| EFV | 200 | 13 | Q197(Q/K) | 13 | L100I | |||
| 500 | 15 | L100(L/I)/Y188(Y/L/F)/R463(R/K) | 15 | K103N/S191(S/F)/L283(L/F) | ||||
| 1,250 | 15 | K103N | NB | NA | ||||
| ETV | 200 | 15 | Y181C | 15 | Y181C | |||
| 500 | NB | NA | NB | NA | ||||
| 1,250 | NB | NA | NB | NA | ||||
a
T, time (in days).
b
NB, no breakthrough.
c
NB*, minor cell lysis was observed.
d
NA, not applicable.
e
Amino acids in parentheses indicate a mixture of the wild-type residue and the emerging mutation.