Evaluation of the therapeutic index of a novel phosphodiesterase 4B-selective inhibitor over phosphodiesterase 4D in mice

J Pharmacol Sci. 2013;123(3):219-26. doi: 10.1254/jphs.13103fp. Epub 2013 Oct 22.

Abstract

Phosphodiesterase 4 (PDE4) inhibitors have been developed for the treatment of pulmonary inflammatory diseases, but their clinical use was dose-limited by mainly gastric adverse effects. Recent studies suggested PDE4B-selective inhibitors over PDE4D are supposed to display a wider therapeutic index than subtype non-selective PDE4 inhibitors such as roflumilast. Compound A was identified as an orally active PDE4B-selective inhibitor over PDE4D both in humans (80-fold selective) and mice (29-fold selective). In this study, the therapeutic effects of compound A and roflumilast were evaluated on lipopolysaccaride (LPS) injection-induced plasma TNF-α elevation and on LPS inhalation-induced pulmonary neutrophilia in mice. The inhibitory effect on gastric emptying in mice was evaluated as a gastric adverse effect. The therapeutic index for TNF-α production (TI(TNF) = ID50 in gastric emptying / ID50 in LPS injection-induced plasma TNF-α elevation) of compound A was larger than roflumilast (9.0 and 0.2, respectively), whereas the therapeutic index for pulmonary neutrophilia (TI(Neu) = ID50 in gastric emptying / ID50 in LPS inhalation-induced pulmonary neutrophilia) of compound A was comparable to roflumilast (1.0 and 0.5, respectively). In conclusion, the TI(Neu) of compound A was not superior compared to that of roflumilast in spite of its high selectivity for PDE4B over PDE4D in mice.

MeSH terms

  • Administration, Ophthalmic
  • Aminopyridines / administration & dosage
  • Aminopyridines / adverse effects
  • Aminopyridines / therapeutic use*
  • Animals
  • Benzamides / administration & dosage
  • Benzamides / adverse effects
  • Benzamides / therapeutic use*
  • Cyclic Nucleotide Phosphodiesterases, Type 4 / metabolism*
  • Cyclopropanes / administration & dosage
  • Cyclopropanes / adverse effects
  • Cyclopropanes / therapeutic use
  • Gastric Emptying / drug effects
  • Heterocyclic Compounds, 2-Ring / adverse effects
  • Heterocyclic Compounds, 2-Ring / therapeutic use*
  • Humans
  • Leukocyte Disorders / chemically induced
  • Leukocyte Disorders / drug therapy*
  • Lipopolysaccharides
  • Male
  • Mice
  • Mice, Inbred BALB C
  • Neutrophil Infiltration
  • Neutrophils*
  • Phenylacetates / adverse effects
  • Phenylacetates / therapeutic use*
  • Phosphodiesterase 4 Inhibitors / administration & dosage
  • Phosphodiesterase 4 Inhibitors / adverse effects
  • Phosphodiesterase 4 Inhibitors / therapeutic use*
  • Pneumonia / chemically induced
  • Pneumonia / drug therapy*
  • Tumor Necrosis Factor-alpha / blood

Substances

  • 2-(4-((2-(3-fluoro-4-methoxyphenyl)-7,8-dihydro-6H-thiopyrano(3,2-d)pyrimidin-4-yl)amino)phenyl)acetic acid
  • Aminopyridines
  • Benzamides
  • Cyclopropanes
  • Heterocyclic Compounds, 2-Ring
  • Lipopolysaccharides
  • Phenylacetates
  • Phosphodiesterase 4 Inhibitors
  • Tumor Necrosis Factor-alpha
  • Roflumilast
  • Cyclic Nucleotide Phosphodiesterases, Type 4