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Synonyms: AQX-1125 | AQX1125
Compound class: Synthetic organic
Comment: Rosiptor (AQX-1125) is an investigational allosteric activator of the SH2 domain-containing inositol 5'-phosphatase 1, SHIP1 (HGNC gene symbol INPP5D) . SHIP1 is a negative regulatory phosphatase in the PI3K pathway, a signalling pathway that plays a central role in cellular activation, proliferation, and survival, and which is strongly implicated in inflammatory disorders and cancer. Agonists that activate SHIP1 are being actively developed (as alternatives to direct PI3K inhibitors) for their potential anti-inflammatory action. AQX-1125 is claimed in patent WO2014158654, where it appears to be referred to as compound 9 (without the acetate) .
1. Mackenzie LF, MacRury TB, Harwig C, Bogucki D, Raymond JR, Pettigrew JD. (2014)
Ship1 modulators and methods related thereto.
Patent number: WO2014158654. Assignee: Aquinox Pharmaceuticals Inc.. Priority date: 14/03/2013. Publication date: 02/10/2014.
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]