TABLE 1.
Correlation coefficients of plasma and tissue concentrations for 6 antiretrovirals
| Tissuea | Antiretrovirals and correlation coefficientsb |
|||||
|---|---|---|---|---|---|---|
| FTC | TFV | EFV | ATV | RAL | MVC | |
| Brain | ||||||
| hu-HSC | −0.3 | 0.2 | 0.5 | 0.1 | −0.1 | 0.5 |
| BLT | 0.3 | 0.3 | — | 0.6c | 0.4 | 0.5 |
| NHP | 0.7c | 0.7c | 0.98c | 0.1 | 0.2 | 0.3 |
| Human | 0.9 | 0.8 | 0.8 | N1 | N1 | — |
| Lymph node | ||||||
| hu-HSC | −0.5 | 0.3 | BLQ | BLQ | BLQ | BLQ |
| BLT | 0.2 | 0.7c | — | BLQ | BLQ | BLQ |
| NHP | 0.9c | 0.6c | 0.8c | 0.5 | 0.3 | 0.7 |
| Human | 0.9c | 0.5 | 0.03 | 1.0 | N1 | — |
| Spleen | ||||||
| hu-HSC | 0.5 | 0.4 | 0.4 | 0.7c | 0.4 | 0.5 |
| BLT | 0.6 | 0.6 | — | 0.3 | 0.06 | 0.9c |
| NHP | 0.8c | 0.6c | 0.9c | 0.7 | −0.2 | 0.8c |
| Human | 0.91c | 0.6 | −1.0 | 1.0 | N1 | — |
| Ileum | ||||||
| hu-HSC | N1 | 0.5c | N1 | 0.4 | 1.0 | BLQ |
| BLT | N1 | 0.1 | — | 0.7 | 0.1 | 0.1 |
| NHP | 0.2 | 0.5c | 0.8c | −0.4 | −0.1 | −0.1 |
| Human | 1.0 | 0.2 | N1 | N1 | N1 | N1 |
| Rectum | ||||||
| hu-HSC | N1 | 0.4 | −1.0 | −0.5 | −0.5 | BLQ |
| BLT | −0.1 | 0.1 | — | −0.1 | 0.2 | −0.3 |
| NHP | −0.1 | 0.2 | 0.6 | 0.2 | 0.4 | 0.8c |
| Human | 0.8 | −0.4 | N1 | N1 | N1 | N1 |
| Testes | ||||||
| hu-HSC | — | — | — | — | — | — |
| BLT | — | — | — | — | — | — |
| NHP | 0.6c | 0.1 | 0.7 | 0.3 | 0.1 | 0.1 |
| Human | — | — | — | — | — | — |
| FGT | ||||||
| hu-HSC | 0.7c | 0.5 | 0.6 | 0.7c | 0.5 | 0.8c |
| BLT | 0.3 | −0.04 | — | 0.4 | 0.3 | 0.2 |
| NHP | 0.1 | 0.6 | 1.0 | −0.5 | −1.0 | 0.5 |
| Human | — | — | — | — | — | — |
a
BLT mice were not dosed with EFV due to toxicity concerns. Testes were only evaluated in NHPs. FGT, female genital tract.
b
ATV, atazanavir; EFV, efavirenz; FTC, emtricitabine; MVC, maraviroc; RAL, raltegravir; TFV, tenofovir; —, tissues not evaluated; N1, correlation coefficient not evaluable due to only one pair of plasma and tissue concentrations; BLQ, below the limit of quantification.
c
P < 0.05 via Spearman’s rank correlation.