HIV-1 integrase inhibitors are substrates for the multidrug transporter MDR1-P-glycoprotein

Retrovirology

Table 3 Induction of P-gp expression in CEM and CEMrev cell lines exposed to IINs

Compound	Concentration	Days of culture	% of P-gp expressing cells
			CEM	CEMrev
None			0	1–3
RDS 1974	10 μg/ml	104	0	25–30
RDS 1983	25 μg/ml	28	0	7–10
RDS 1984	25 μg/ml	28	0	15–18
RDS 1996	10 μg/ml	28	0	17–20
Vinblastine	10 ng/ml	28	ND*	30–35
		104	ND*	60–70

ND, not done
* % of P-gp expressing cells could not be evaluated due to VBL toxicity. Prolonged and stepwise VBL treatment induced high percentage of P-gp expressing cells [31].

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