Rosiptor (AQX-1125)

The SHIP1 Pathway - Highlighting the Role of Rosiptor

The SHIP1 Pathway - Highlighting the Role of Rosiptor


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Aquinox’s lead product candidate rosiptor (AQX-1125) has generated clinical data from eight completed clinical trials, including two proof-of-concept trials, one in COPD and one in allergic asthma, demonstrating anti-inflammatory activity with a tolerability profile similar to placebo. Overall, approximately 395 subjects have received rosiptor. Phase 2 clinical trial results in female subjects with interstitial cystitis (IC/BPS) were published in the Journal of Urology in 2016, available here, and a Phase 3 clinical trial in IC/BPS completed enrollment in the first quarter of 2018. Additionally, a Phase 2 proof-of-concept trial evaluating the efficacy and safety of rosiptor in chronic prostatitis/chronic pelvic pain syndrome (CP/CPPS) was initiated in the second quarter of 2018.

The eight completed clinical trials have demonstrated that rosiptor:

  • has desirable pharmacokinetic, absorption, and excretion properties that make it suitable for once-daily oral administration;

  • has anti-inflammatory and anti-inflammatory pain properties consistent with those exhibited in preclinical studies; and

  • is generally well-tolerated, exhibiting mild to moderate adverse events primarily related to gastrointestinal upset that resolve without treatment or long-term effects.

Rosiptor is an activator of SHIP1, which reduces the activity of the PI3K cellular signaling pathway. Over-activity of the PI3K pathway can cause immune cells to produce an abundance of pro-inflammatory signaling molecules and increase their migration to and concentration in tissues, resulting in excessive or chronic inflammation. By activating SHIP1, rosiptor is believed to decrease the inflammatory process, thereby reducing inflammation and inflammatory pain.