Literature DB >> 26968644

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 Curtis Nickel1, Blair Egerdie2, Edward Davis3, Robert Evans4, Lloyd Mackenzie5, Stephen B Shrewsbury5.   

Abstract

PURPOSE: In this 6-week, randomized, double-blind, placebo controlled, multicenter trial we assessed the effect of the novel SHIP1 (SH2-containing inositol-5'-phosphatase 1) activator AQX-1125 on bladder pain and urinary symptoms in patients with interstitial cystitis/bladder pain syndrome.
MATERIALS AND METHODS: Women with interstitial cystitis/bladder pain syndrome and a mean pain score of 5 or greater on an 11-point scale despite treatment were randomized to AQX-1125 or placebo orally once daily for 6 weeks. Average and maximum pain scores (daily) and urinary frequency (before visits) were recorded by e-diary and at clinic visits. The O'Leary-Sant ICSI (Interstitial Cystitis Symptom Index) and ICPI (Interstitial Cystitis Problem Index), BPIC-SS (Bladder Pain Interstitial Cystitis Symptom Score) and SF-12v2® questionnaires were administered. Safety was monitored through 6 weeks of treatment and 4 weeks of followup.
RESULTS: A total of 37 patients received oral AQX-1125 and 32 received placebo. At 6 weeks average daily pain on an e-diary decreased by 2.4 points for AQX-1125 vs 1.4 for placebo (p = 0.061), while average pain at clinic decreased by 2.6 vs 1.1 (p = 0.008), maximum daily pain on e-diary diary decreased by 2.6 vs 1.4 (p = 0.030) and maximum pain at clinic decreased by 2.8 vs 1.1 (p = 0.028). AQX-1125 reduced ICSI by 3.8 points vs 1.4 for placebo (p = 0.005), ICPI by 3.6 points vs 1.6 (p = 0.014) and BPIC-SS by 8.8 points vs 4.0 (p = 0.011). Urinary frequency decreased on AQX-1125 by 3.6 voids per 24 hours vs 0.8 for placebo (p = 0.040). Adverse event rates were similar for AQX-1125 and placebo (51.4% and 78.1%, respectively). No serious adverse events were reported.
CONCLUSIONS: Women with moderate to severe interstitial cystitis/bladder pain syndrome who were treated with the oral SHIP1 activator AQX-1125 reported significantly reduced bladder pain and improved urinary symptoms at 6 weeks. AQX-1125 was well tolerated. AQX-1125 may be a potential new treatment for interstitial cystitis/bladder pain syndrome. It warrants further investigation.
Copyright © 2016 American Urological Association Education and Research, Inc. Published by Elsevier Inc. All rights reserved.

Entities:  

Keywords:  4-(4-(aminomethyl)-7a-methyl-1-methylideneoctahydro-1H-inden-5-yl)-3-(hydroxymethyl)-4-methylcyclohexan-1-ol; cystitis, interstitial; pain; questionnaires; urinary bladder

Mesh:

Substances:

Year:  2016        PMID: 26968644     DOI: 10.1016/j.juro.2016.03.003

Source DB:  PubMed          Journal:  J Urol        ISSN: 0022-5347            Impact factor:   7.450


  11 in total

1.  Pain: SHIP-1 activation for IC/BPS?

Authors:  Peter Sidaway
Journal:  Nat Rev Urol       Date:  2016-03-31       Impact factor: 14.432

2.  AQX-1125, small molecule SHIP1 activator inhibits bleomycin-induced pulmonary fibrosis.

Authors:  Jennifer Cross; Grant R Stenton; Curtis Harwig; Csaba Szabo; Tiziana Genovese; Rosanna Di Paola; Emanuale Esposito; Salvatore Cuzzocrea; Lloyd F Mackenzie
Journal:  Br J Pharmacol       Date:  2017-08-11       Impact factor: 8.739

Review 3.  Efficacy and safety comparison of pharmacotherapies for interstitial cystitis and bladder pain syndrome: a systematic review and Bayesian network meta-analysis.

Authors:  Xing-Peng Di; De-Yi Luo; Xi Jin; Wan-Yu Zhao; Hong Li; Kun-Jie Wang
Journal:  Int Urogynecol J       Date:  2021-02-27       Impact factor: 2.894

4.  Synthetic studies on the indane SHIP1 agonist AQX-1125.

Authors:  Otto M Dungan; Shawn Dormann; Sandra Fernandes; Brian C Duffy; Daniel G Effiong; William G Kerr; John D Chisholm
Journal:  Org Biomol Chem       Date:  2022-05-18       Impact factor: 3.890

5.  Interventions for treating people with symptoms of bladder pain syndrome: a network meta-analysis.

Authors:  Mari Imamura; Neil W Scott; Sheila A Wallace; Joseph A Ogah; Abigail A Ford; Yann A Dubos; Miriam Brazzelli
Journal:  Cochrane Database Syst Rev       Date:  2020-07-30

Review 6.  Current Pharmacologic Approaches in Painful Bladder Research: An Update.

Authors:  Karl-Erik Andersson; Lori Birder
Journal:  Int Neurourol J       Date:  2017-12-31       Impact factor: 2.835

7.  SHIP1 Activator AQX-1125 Regulates Osteogenesis and Osteoclastogenesis Through PI3K/Akt and NF-κb Signaling.

Authors:  Xudong Xie; Liangcong Hu; Bobin Mi; Adriana C Panayi; Hang Xue; Yiqiang Hu; Guodong Liu; Lang Chen; Chenchen Yan; Kangkang Zha; Ze Lin; Wu Zhou; Fei Gao; Guohui Liu
Journal:  Front Cell Dev Biol       Date:  2022-04-04

8.  Current best practice management of interstitial cystitis/bladder pain syndrome.

Authors:  Esther Han; Laura Nguyen; Larry Sirls; Kenneth Peters
Journal:  Ther Adv Urol       Date:  2018-03-19

Review 9.  Targeting SHIP1 and SHIP2 in Cancer.

Authors:  Chiara Pedicone; Shea T Meyer; John D Chisholm; William G Kerr
Journal:  Cancers (Basel)       Date:  2021-02-20       Impact factor: 6.639

10.  Treatment with low-energy shock wave alleviates pain in an animal model of uroplakin 3A-induced autoimmune interstitial cystitis/painful bladder syndrome.

Authors:  Huixi Li; Zhichao Zhang; Jing Peng; Zhongcheng Xin; Meng Li; Bicheng Yang; Dong Fang; Yuan Tang; Yinglu Guo
Journal:  Investig Clin Urol       Date:  2019-08-30
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