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Parkinson's disease (PD)

Adenosine A2A receptor (ADORA2A); monoamine oxidase B (MAO-B)

In vitro studies suggest dual antagonists of ADORA2A and MAO-B could be useful for treating PD. Both proteins are known targets in PD. In vitro, the lead molecule from a series of benzothiazinones selectively antagonized human ADORA2A with an IC50 value of 39.5 nM and MAO-B with an IC50 value of 34.9 nM. Next steps include evaluating other members of the compound series in mice.
Kyowa Hakko Kirin Co. Ltd. markets the ADORA2A antagonist Nouriast istradefylline to treat PD.
At least seven other companies have ADORA2A antagonists in Phase III or earlier testing to treat PD.
Teva Pharmaceutical Industries Ltd. and H. Lundbeck A/S market Azilect rasagiline, an irreversible selective inhibitor of MAO-B, to treat PD.
Valeant Pharmaceuticals International Inc. markets the MAO-B inhibitor Zelapar selegiline for the same indication.
At least six other MAO-B inhibitors are in Phase III or earlier testing to treat PD.

SciBX 6(21); doi:10.1038/scibx.2013.526
Published online May 30, 2013

Compound series covered by pending patents; available for licensing

Stöβel, A. et al. J. Med. Chem.; published online April 30, 2013;
Contact: Christa E. Müller, PharmaCenter Bonn, Bonn, Germany
Contact: Michael Gütschow, same affiliation as above