Table 2.
Effect of antiretroviral drugs on liver cytochromes CYP2C9 and CYP3A4
| CYP2C9 | CYP3A4 | |
|---|---|---|
| Protease inhibitors | ||
| Saquinavir | Inhibition | Inhibition |
| Tipranavir | Induction | Inhibition |
| Ritonavir a | Modest Inductiona | Strong Inhibitiona |
| Atazanavir | Inhibition | Modest Inhibition |
| Darunavir | Induction | Modest Inhibition |
| Lopinavir | Induction | Strong Inhibition |
| Nelfinavir | Induction | Induction/inhibition |
| Indinavir | No significant effect | Inhibition |
| Non‐nucleoside reverse‐transcriptase inhibitors | ||
| Delavirdine | Inhibition | Inhibition |
| Efavirenz | Modest Inhibition | Modest Induction |
| Nevirapine | Induction | Strong Induction |
| Etravirine | Inhibition | Modest Induction |
| Rilpivirine | No significant effect | Induction |
| Doravirine | – | Substrate |
| CCR5 inhibitor | ||
| Maraviroc | – | Substrate |
| Integrase inhibitors | ||
| Raltegravir | – | – |
| Dolutegravir | – | Substrate |
| Elvitegravir | Modest Induction | Inhibition |
| Cobicistat b | – | Strong Inhibition |
| Bictegravir | – | Substrate |
a
Ritonavir is used only as low ‘boosting’ dose (100–200 mg) in association with other PIs to enhance their pharmacokinetic properties by inhibiting CYP3A4
b
Not an integrase inhibitor and available in combination with elvitegravir, atazanavir and darunavir