Table 2 Susceptibility to integrase inhibitors and replicative capacity of site-directed mutants containing integrase mutations

From: Drug resistance emergence in macaques administered cabotegravir long-acting for pre-exposure prophylaxis during acute SHIV infection

 

EFVa

RAL

EVG

CAB

DTG

BIC

Replicative capacity (%)b

WT

0.67 (1)

2.90 (1)

1.24 (1)

1.19 (1)

1.00 (1)

1.00 (1)

100

E92Q

0.54 (0.8)

10.48 (3.6)

9.67 (7.8)

2.93 (2.5)

1.52 (1.5)

1.97 (2.0)

7.7

G140R

0.59 (0.9)

>1000 (>345)

>1000 (>807)

>1000 (>840)

>1000 (>1000)

>1000 (>1000)

1.3

E92Q/G140R

1.28 (1.9)

>1000 (>345)

>1000 (>807)

>1000 (>840)

>1000 (>1000)

>1000 (>1000)

1.3

Q124R

0.70 (1.0)

4.60 (1.6)

1.59 (1.3)

1.22 (1.0)

1.62 (1.6)

1.49 (1.5)

219

A122T

0.77 (1.2)

4.13 (1.4)

1.15 (0.9)

1.51 (1.3)

1.42 (1.4)

2.10 (2.1)

26.9

G118R

1.01 (1.5)

>1000 (>345)

>1000 (>807)

>1000 (>840)

>1000 (>1000)

>1000 (>1000)

2.3

G118R/A122T

0.72 (1.1)

>1000 (>345)

>1000 (>807)

>1000 (>840)

>1000 (>1000)

>1000 (>1000)

2.2

E92G

1.01 (1.5)

8.07 (2.8)

4.53 (3.7)

4.20 (3.5)

2.78 (2.8)

4.29 (4.3)

7.5

I72T

0.60 (0.9)

2.73 (0.9)

1.17 (0.9)

0.96 (0.8)

1.14 (1.1)

1.51 (1.5)

124

I110V

0.79 (1.2)

3.80 (1.3)

1.55 (1.3)

1.27 (1.1)

1.52 (1.5)

1.78 (1.8)

111.1

I250V

0.67 (1.0)

4.00 (1.4)

1.45 (1.2)

1.04 (0.9)

0.92 (0.9)

1.56 (1.6)

83.7

  1. Values in parenthesis represent fold-change relative to wild type integrase
  2. EFV efavirenz, RAL raltegravir, EVG elvitegravir, CAB cabotegravir, DTG dolutegravir, BIC bictegravir
  3. aEC50 value in nM
  4. bPercentage of wild type
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