Uses
Pizuglanstat hydrate (TAS-205) is a hematopoietic prostaglandin D synthase (HPGDS) inhibitor. TAS-205 selectively inhibits the synthesis of prostaglandin D2 (PGD2) in cell-based enzymatic tests and in vivo models, and effectively reduces the entry of eosinophils into the nasal cavity and late-stage nasal congestion. When used in combination with montelukast (HY-13315A), TAS-205 showed a significant synergistic inhibitory effect; when used in combination with fexofenadine (HY-B0801A), it also had a certain inhibitory effect on early and late nasal congestion.
Biological Activity
TAS 205 is an inhibitor of hematopoietic prostaglandin D synthase (H-PGDS; IC50 = 55.8 nM).1 It is selective for H-PGDS over lipocalin-type PGDS (L-PGDS) at 100 μM, as well as over enzyme and receptor panels at 10 μM. TAS 205 inhibits production of prostaglandin D2 induced by A23187 in KU812 human and RBL-2H3 rat basophils with IC50 values of 78.3 and 181.3 nM, respectively. It inhibits ovalbumin-induced nasal lavage fluid eosinophil infiltration and late-phase nasal obstruction in an ovalbumin-sensitized guinea pig model of allergic rhinitis when administered at a dose of 30 mg/kg.
References
1.Aoyagi, H., Kajiwara, D., Tsunekuni, K., et al.Potential synergistic effects of novel hematopoietic prostaglandin D synthase inhibitor TAS-205 and different types of anti-allergic medicine on nasal obstruction in a Guinea pig model of experimental allergic rhinitisEur. J. Pharmacol.875173030(2020)
