Table 5.
Summary of antiviral nucleoside analogs as substrates and modulators of human efflux transporters
| Transporter (Km (mM)) | MATE1 | MATE2K | BCRP | P-gp | MRP2 | MRP4 | Ref |
|---|---|---|---|---|---|---|---|
|
| |||||||
| Gene | SLC47A1 | SLC47A2 | ABCG2 | ABCB1 | ABCC2 | ABCC4 | |
|
| |||||||
| Remdesivir | - | - | - | sub | - | - | [11,76] |
| ninh | ninh | inh | |||||
|
| |||||||
| GS-441524 | nsub | nsub | sub | sub | - | - | [11,76] |
| ninh | ninh | ||||||
|
| |||||||
| GS-704277 | nsub | nsub | - | - | - | - | [11,76] |
| inh | ninh | ||||||
|
| |||||||
| Didanosine | - | - | nsub | - | - | sub | [156] |
| ninh | |||||||
|
| |||||||
| Adefovir | - | - | nsub | nsub | sub | [152,157] | |
|
| |||||||
| Tenofovir disoproxil fumarate | - | - | sub | sub | - | sub | [12,87,158,159] |
| inh | |||||||
|
| |||||||
| Tenofovir alafenamide fumarate | - | - | sub | sub | - | - | [153,160] |
| ninh | |||||||
|
| |||||||
| Tenofovir | - | nsub | nsub | nsub | sub | [78,129,161] | |
| - | - | inh | |||||
|
| |||||||
| Acyclovir | sub | sub | - | - | - | - | [162] |
|
| |||||||
| Ganciclovir | sub | sub | - | - | - | sub | [162,163] |
|
| |||||||
| Entecavir | - | - | sub | - | - | sub | [136,164] |
|
| |||||||
| Abacavir | nsub | nsub | sub | sub | nsub | nsub | [137] |
| ninh | ninh | ninh | ninh | ||||
|
| |||||||
| Zalcitabine | - | - | inh | - | - | - | [129] |
|
| |||||||
| Lamivudine | sub | sub | sub (0.2) | sub (weak) | - | sub | [21,40,164–166] |
|
| |||||||
| Emtricitabine | sub | - | nsub | nsub | nsub | - | [141,167,168] |
| ind | inh | ||||||
|
| |||||||
| Molnupiravir | nsub | nsub | [169] | ||||
| ninh | ninh | ninh | ninh | ninh | |||
|
| |||||||
| EIDD-1931 | nsub | nsub | [169] | ||||
|
| |||||||
| Zidovudine | - | - | sub | sub/nsub | - | sub | [21,22,40,129,152–154] |
| inh | ninh | ||||||
|
| |||||||
| Zidovudine MP | - | - | sub | - | - | sub | [40,152] |
|
| |||||||
| Stavudine | - | - | - | ind | - | - | [167] |
|
| |||||||
| Sofosbuvir | - | - | sub | sub | - | - | [13] |
| ninh | ninh | ||||||
|
| |||||||
| GS-331007 | nsub | - | nsub | nsub | - | - | [13] |
| ninh | ninh | ninh | |||||
|
| |||||||
| ninh | ninh | ninh | ninh | ninh | |||
Abbreviation: MP: monophosphate; nsub: not a substrate; sub: substrate; ninh: not an inhibitor; inh: inhibitor; ind: inducer; -: no information reported; Km (mM) value reported is labeled in bracket.