TABLE 3.
Activities of dapivirine compared to those of other NNRTIs against a range of HIV-1 subtypes
| Virus ID | Pol subtype | NNRTI mutationsb | Fold change in IC50a
|
|||
|---|---|---|---|---|---|---|
| Dapivirine | NVP | DLV | EFV | |||
| V022808 | CRF02_AG | None | 1 | 0.8 | 0.6 | 0.9 |
| V022825 | CRF02_AG | None | 0.8 | 0.7 | 1.9 | 0.8 |
| V022826 | CRF02_AG | None | 1 | 0.4 | 1.3 | 0.4 |
| V022830 | CRF02_AG | None | 1.6 | 1.3 | 0.9 | 1.2 |
| V022820 | CRF01_AE | None | 0.9 | 1.3 | 3.3 | 0.8 |
| V022821 | CRF01_AE | None | 1.7 | 1.2 | 2.3 | 1.3 |
| V022822 | CRF01_AE | None | 0.9 | 0.8 | 2.7 | 0.7 |
| V029521 | CRF01_AE | None | 3.5 | 1.4 | 4.4 | 1.6 |
| V029525 | CRF01_AE | None | 2.6 | 7 | 20 | 2.1 |
| V022807 | B | None | 1.1 | 3.4 | 3.6 | 1.4 |
| V022809 | B | None | 1.5 | 5 | 2.6 | 2.8 |
| V022810 | B | A98(S/A), K101R | 1.6 | 1.7 | 2.7 | 0.8 |
| V022811 | B | None | 3.1 | 3.4 | 3.7 | 1.5 |
| V022812 | B | V179I | 2 | 0.8 | 6 | 0.3 |
| V022813 | B | None | 0.7 | 1 | 0.7 | 0.6 |
| V022814 | B | None | 0.8 | 2.4 | 1.9 | 0.7 |
| V022815 | B | None | 2.2 | 1 | 4.9 | 2.9 |
| V022816 | C | None | 1.8 | 3.8 | 5.3 | 0.6 |
| V022817 | C | None | 0.7 | ND | 5.1 | 1.5 |
| V022829 | C | None | 1 | 0.6 | 2.7 | 0.4 |
| V022831 | C | None | 0.8 | 0.9 | 2.6 | 0.6 |
| V022832 | D | None | 0.7 | 0.9 | 1.1 | 0.3 |
| V022818 | D | None | 1.4 | 0.5 | 0.9 | 0.4 |
| V022819 | D | None | 1.5 | 1 | 2.3 | 0.5 |
| V022823 | CRF05_DF | None | 0.7 | 0.9 | 0.6 | 0.8 |
| V022824 | CRF05_DF | V106I | 0.7 | 3.1 | 1.3 | 0.3 |
| V022833 | CRF05_DF | V179I | 1 | 1.7 | 0.6 | 0.9 |
| V029522 | F | None | 1.5 | 2.1 | 3.1 | 1 |
| V022827 | H | V179I | 0.9 | 0.4 | 0.3 | 0.3 |
| V022828 | H | K101Q, V179I | 1.5 | 1.1 | 2 | 0.5 |
| V029523 | H | K101Q, V179I | 1.4 | 1.4 | 2.6 | 0.8 |
| V029524 | O | A98G, V179E, Y181C | 150 | 89 | 140 | 42 |
a
NNRTI activity was evaluated using MT-4 cells. Data are mean changes (n-fold) in the IC50 (medians for ≥3 experiments), calculated as the IC50 for the tested virus divided by the IC50 for the wild-type virus (HIV-1IIIB), tested in parallel. The IC50s for the wild-type virus were 0.9 nM (dapivirine), 77.1 nM (NVP), 16.1 nM (DLV), and 1.0 nM (EFV). ND, not determined.
b
Mutations at amino acid positions associated with NNRTI resistance (positions 98, 100, 101, 103, 106, 108, 179, 181, 188, 190, 234, 225, 227, and 236) are listed.