idiopathic

GLPG2938 (1-(2-Ethoxy-6-(trifluoromethyl)pyridin-4-yl)-3-((5-methyl-6-(1-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl)pyridazin-3-yl)methyl)urea) is a potent and selective antagonist of S1P2.

TD139 is a small molecule inhibitor of inhaled galectin-3 (Gal-3) with potential anti-fibrotic activity, commonly used in the study of idiopathic pulmonary fibrosis.

Autotaxin-IN-4 is an Autotaxin inhibitor. It has the potential to treat idiopathic pulmonary fibrosis.

Bersiporocin is a novel prolyl-tRNA synthetase (PRS) inhibitor that exerts antifibrotic effects through downregulation of collagen synthesis and is well tolerated in the clinic. In cellular and animal models of idiopathic pulmonary fibrosis (IPF), DWN12088 significantly reduced collagen synthesis and improved lung function.

Elobixibat (A 3309) is an inhibitor of the ileal bile acid transporter (IC50: 0.13 nM, 0.53 nM, and 5.8 nM for mouse, human, and canine IBAT). Elobixibat can be used in studies about chronic idiopathic constipation.

LPA1 receptor antagonist 1(LPA1 R antagonist 1) is a selective and potent lysophosphatidic acid (LPA1) receptor antagonist (IC50 : 25 nM) for the study of idiopathic pulmonary fibrosis.

Ebastine (Kestine) (trade names Evastin, Kestine, Ebastel, Aleva) is a non-sedating H1 antihistamine. It does not penetrate the blood-brain barrier and thus allows an effective block of the H1 receptor in peripheral tissue without a central side effect, i. e not causing sedation or drowsiness.

Mizolastine (SL 850324) (IC50= 47 nM) is a histamine H1-receptor antagonist.It is used in the treatment of allergic reactions such as hay fever (seasonal allergic rhinitis), hives.

Rasagiline Mesylate (AGN1135) is a novel MAO-B inhibitor, which can treat idiopathic Parkinson's disease.

Levocetirizine Dihydrochloride (Xyzal Dihydrochloride) is a third-generation peripheral H1-receptor antagonist. Acting as an antihistaminic agent, it specifically targets the histamine H1-receptor. Levocetirizine Dihydrochloride is the R-enantiomer of Cetirizine, which gives it a higher affinity for the H1-receptor than the S-enantiomer. Due to this enhanced affinity, Levocetirizine Dihydrochloride is effective in treating allergic rhinitis and chronic idiopathic urticaria.

Macitentan (ACT-064992) is an endothelin receptor antagonist utilized in the treatment of pulmonary arterial hypertension (PAH).

Pidotimod is a synthetic dipeptide with immunomodulatory properties.

Quinine is a natural cinchona alkaloid that has been used for centuries in the prevention and therapy of malaria. Quinine is also used for idiopathic muscle cramps. Quinine therapy has been associated with rare instances of hypersensitivity reactions which can be accompanied by hepatitis and mild jaundice.

BAY-6672 is a selective human prostaglandin F (FP) receptor antagonist that is highly potent (IC50=11 nM), orally available and well permeable. It exerts antifibrotic effects by inhibiting prostaglandin F2α (PGF₂α) activity through antagonizing the FP receptor, and has in vivo efficacy in animal models of idiopathic pulmonary fibrosis (IPF).

Ziritaxestat (GLPG1690), an autotaxin inhibitor, currently being evaluated in an exploratory phase 2 study in idiopathic pulmonary fibrosis patients.

Astemizole (Laridal) is a synthetic piperidinyl-benzimidazol derivative with antiallergic properties, acts as a reversible competitive inhibitor of histamine H1 receptors, with less anticholinergic effects compared to related agents. It is a long-acting, non-sedative antihistaminic used in the treatment of seasonal allergic rhinitis, asthma, allergic conjunctivitis, and chronic idiopathic urticaria.

TGFβ1-IN-2, a derivative of diarylacylhydrazones, effectively inhibits fibroblast activation and proliferation and holds potential for idiopathic pulmonary fibrosis (IPF) research [1].

BMS-986278 is an orally active and potent hemophosphatidic acid receptor 1 (LPA1) antagonist with Kb values of 6.9 nM and 4.0 nM for human and mouse LPA1, respectively.BMS-986278 may be investigated for use in idiopathic pulmonary fibrosis.

TGFβ1-IN-3, a diarylhydrazone derivative, inhibits fibroblast activation and proliferation, positioning it as a candidate compound for the treatment of idiopathic pulmonary fibrosis (IPF).

Macitentan n-butyl analogue, a derivative of Macitentan, functions as an orally active dual antagonist targeting both endothelin ETA and ETB receptors. This compound shows promise for treating idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH), leveraging its non-peptide structure for potential therapeutic applications.

INS018 055 (TNIK&MAP4K4-IN-2) is a highly efficient TNIK and MAP4K4 inhibitor with antifibrotic activity. It can be used in research on idiopathic pulmonary fibrosis.

STAT3-IN-39 (compound 10K) is an orally active inhibitor of STAT3, demonstrating effective inhibition of STAT3 phosphorylation with an IC50 of 0.47 μM in NIH-3T3 cells. It hinders TGF-β1-induced fibrotic responses and prevents epithelial-mesenchymal transition in A549 cells. STAT3-IN-39 is applicable for research related to idiopathic pulmonary fibrosis.

Vixarelimab (KPL-716) is a human anti-oncostatin M (OSM) monoclonal antibody with affinity for the beta chain of the OSM receptor, inhibiting IL-31 and OSM signaling. It can be used to study severe nodular itch and idiopathic pulmonary fibrosis.

Lubiprostone (RU-0211), an activator of ClC-2 chloride channels, is used in the therapy of idiopathic chronic constipation.