Drug intelligence / Profile preview

zpl‑5212372

Development stage
Phase 2
Lead developer
Novartis
Modality
Small Molecules
Administration
Topical, Inhalation, Intranasal, Ophthalmic
01

Overview

ZPL‑5212372 is a small molecule phospholipase A2 (PLA2) inhibitor developed initially by Pfizer and later by Ziarco (a subsidiary of Novartis) as a topical treatment for inflammatory diseases affecting surfaces such as the skin, lung, nose, and eye. Its mechanism of action involves potent inhibition of cytosolic phospholipase A2 alpha (cPLA(2)α), which reduces the production of eicosanoids implicated in inflammation. Preclinical studies demonstrated that it inhibits prostaglandin D₂ and cysteinyl leukotriene release from human lung mast cells and suppresses bronchoconstriction in animal models. Clinical development included phase I/II trials for atopic dermatitis via topical application, but no further development has been reported for this or other indications such as psoriasis; its development for asthma was discontinued[1][3][4][6].

Other names
UNII-7LNI1E5EFAUNII7LNI1E5EFAUNII 7LNI1E5EFA
02

Targets

PLA2G4A (Cytosolic phospholipase A2 alpha)PLA2 (Phospholipase A2 group IID)

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