Interstitial cystitis

Disease ID:506
Name:Interstitial cystitis
Associated with:2 targets
1 immuno-relevant target
1 immuno-relevant ligand
Database Links
Disease Ontology: DOID:13949

Targets

FZD8
References:  1
INPP5D
Comments:  Phase 3 evaluating the SHIP1 activator rosiptor is underway (see NCT02858453).
Ligand interactions: 
Ligand Comments
rosiptor
Phase 3 study for interstitial cystitis/bladder pain syndrome is ongoing (see NCT02858453).

Ligands

Key to terms and symbols Click ligand name to view ligand summary Click column headers to sort
Ligand References Clinical and Disease comments
rosiptor
Immuno Disease Comments: Phase 3 study for interstitial cystitis/bladder pain syndrome is ongoing (see NCT02858453).
Clinical Use: AQX-1125 has reached Phase 2 clinical trial in chronic inflammatory conditions such as unstable chronic obstructive pulmonary disease (COPD) and atopic dermatitis, and Phase 3 for interstitial cystitis/bladder pain syndrome [2] (see NCT02858453). Click here to link to ClinicalTrials.gov's full list of AQX-1125 trials. | View clinical data
Bioactivity Comments: AQX-1125 activates INPP5D enzyme activity by 20% (reducing the KM from 214 (control) to 180 [3]. This reduction in KM is concentration-dependent, but the compound has no effect on the enzyme's turnover constant (kcat) or maximum velocity (Vmax), which is indicative of allosteric modulation [3]. | View biological activity

References

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1. Keay SK, Szekely Z, Conrads TP, Veenstra TD, Barchi Jr JJ, Zhang CO, Koch KR, Michejda CJ. (2004) An antiproliferative factor from interstitial cystitis patients is a frizzled 8 protein-related sialoglycopeptide. Proc. Natl. Acad. Sci. U.S.A., 101 (32): 11803-8. [PMID:15282374]

2. Nickel JC, Egerdie B, Davis E, Evans R, Mackenzie L, Shrewsbury SB. (2016) A Phase II Study of the Efficacy and Safety of the Novel Oral SHIP1 Activator AQX-1125 in Subjects with Moderate to Severe Interstitial Cystitis/Bladder Pain Syndrome. J. Urol., 196 (3): 747-54. [PMID:26968644]

3. Stenton GR, Mackenzie LF, Tam P, Cross JL, Harwig C, Raymond J, Toews J, Wu J, Ogden N, MacRury T et al.. (2013) Characterization of AQX-1125, a small-molecule SHIP1 activator: Part 1. Effects on inflammatory cell activation and chemotaxis in vitro and pharmacokinetic characterization in vivo. Br. J. Pharmacol., 168 (6): 1506-18. [PMID:23121445]