New SOLVO Science Letter is out now

May 12, 2011

Overexpression of P-gp (MDR1) does not confer resistance to its selective substrate Seliciclib

One of the great challenges of development of anticancer therapeutics is their transporter interaction profile. It is desirable that the drug is a substrate of a lumenally located efflux transporter in the blood-brain barrier endothelial cells as this would reduce brain penetration, hence central toxicity of the drug. As most chemotherapeutics are administered intravenously an efflux transporter interaction would not significantly alter systemic exposition of the drug. However, if a drug is a substrate of an efflux transporter it may lead to resistance. This resistance can be overcome by high passive permeability. This study shows that optimal balance of efflux transporter interaction and passive permeability may lead to a favourable profile. It also shows that in vitro assays are available to assist drug discovery & development efforts (Rajnai et al 2010) Read the full SOLVO Science Letter

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