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) [3]. 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].
|
|
No information available. |
Summary of 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. |
Mechanism Of Action and Pharmacodynamic Effects ![]() |
AQX-1125 activates INPP5D to bring about reduced cytokine production and inhibition of mast cell activation, and thereby reduces inflammation [3]. |
Clinical Trials | |||||
Clinical Trial ID | Title | Type | Source | Comment | References |
NCT02858453 | Efficacy and Safety of 2 Doses of AQX-1125 in Subjects With Interstitial Cystitis / Bladder Pain Syndrome | Phase 3 Interventional | Aquinox Pharmaceuticals (Canada) Inc. |