molecules of the month


Inhaled dual M3 antagonist/PDE4 inhibitor

intratracheal efficacy in model, not developed

from linking M3 antag. + PDE inh. and opt.

Journal of Medicinal Chemistry

Chiesi Farmaceutici S.p.A., Parma, IT

1 min read

10. The Chiesi M3 antagonist/PDE4 inhibitor dual pharmacology molecule, compound 92a, is an inhaled compound intended for pulmonary diseases. Both M3 and PDE4 are clinically validated targets for COPD (e.g. ipratropium and roflumilast). Dual pharmacology was thought to be valuable over two independent inhibitors in part due to the potentially better lung retention and lower systemic exposure of larger molecules, as well as the simplified clinical development of one compound with one formulation. The molecule is derived from the scaffold of prior inhaled PDE4 clinical candidate CHF-6001 and an M3 receptor antagonist and demonstrates in vivo efficacy in bronchoconstriction and inflammation assays in rat after intratracheal administration. In model animals, 92a seemed to show a lower degree of nausea and…

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