Results of transport studies for [14C]DTG (3 μM) in MDCKII-MDR1 or MDCKII-BCRP cell monolayersa
| MDCKII Cell Line | GF120918b | Rate Apical to Basolateral | Rate B→A | Apical Efflux Ratio | Apical to Basolateral Mass Balance | B→A Mass Balance |
|---|---|---|---|---|---|---|
| pmol/min/cm2 | % | |||||
| MDR1 | — | 7.3 ± 0.52 | 28 ± 3.1 | 3.8 | 84 ± 7.1 | 84 ± 4.5 |
| MDR1 | + | 4.7 ± 0.04 | 3.5 ± 0.07 | 0.74 | 84 ± 1.9 | 75 ± 1.7 |
| BCRP | — | 2.5 ± 0.24 | 7.8 ± 0.29 | 3.1 | 81 ± 3.4 | 85 ± 3.5 |
| BCRP | + | 4.2 ± 0.09 | 3.3 ± 0.06 | 0.80 | 81 ± 2.1 | 76 ± 2.4 |
↵a Data are the mean ± S.D. from three monolayers over 90 min using Dulbecco’s Modified Eagle’s medium as the transport buffer. All donor compartments contained Lucifer yellow (100 μM) to determine monolayer integrity (pass criterion P 7.4 ≤ 50 nm/s). Amprenavir served as a positive control for Pgp efflux and cimetidine for BCRP efflux. The measured radiochemical purity of [14C]DTG was >98% and no metabolic or chemical degradation was detected during the studies.
↵b GF120918 was used in both donor and receiver compartments at 2 μM for Pgp and BCRP.