Insects for Drug Discovery – University of Copenhagen

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Department of Pharmacy > Research > Section of Analytical Biosciences > Drug Metabolism Lab > Insects

Insects for Drug Discovery

 

Characterization of drug metabolizing enzymes and membrane transporters in locusts.

The Blood Brain Barrier (BBB) is one of the major obstacles in drug development, and it is important to know whether a drug candidate penetrates the BBB or not.
Despite significant progress, the existing in vitro models lack predictability and many are time consuming. In vivo models are expensive and therefore it is important to exclude as many poor drug candidates as early in the process as possible.

Insects, and specifically the locust, have recently been subject to increased interest in drug development. It has been shown, that the locust brain has an efflux transporter that is functionally similar to the mammalian transporter P-glycoprotein. The locust is advantageous over a number of other insects due to the relatively large size.

In order to use insects as an in vivo model, it is necessary to characterize the entire organism including metabolism and elimination. Oxidative metabolism using cytochrome P450 enzymes (phase I metabolism) have been reported as well as conjugation mechanisms (phase II metabolism).

Currently, the group is working on characterization of drug metabolizing enzymes as well as membrane transporters in insects used as in vivo and ex vivo BBB models.
This is an important part of an overall vision to establish insects, specifically the locust, as a novel model organism to assess brain permeability of new chemical entities (NCEs) during preclinical drug development.