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- Spahn, V., et al., A nontoxic pain killer designed by modeling of pathological receptor conformations. Science, 2017. 355(6328): p. 966-969; doi: 10.1126/science.aai8636.
- Pivotal study showing concept development/validation and efficacy of pH-sensitive analgesic in arthritis and post-operative pain rodent models
- Baamonde, A., et al., A low pKa ligand inhibits cancer-associated pain in mice by activating peripheral mu-opioid receptors. Sci Rep, 2020. 10(1): p. 18599;doi: 10.1038/s41598-020-75509-4.
- Key study showing efficacy of pH-sensitive analgesic in a cancer pain model in rodents
- Jagla, C., P. Martus, and C. Stein, Peripheral opioid receptor blockade increases postoperative morphine demands–a randomized, double-blind, placebo-controlled trial. Pain, 2014. 155(10): p. 2056-2062; doi: 10.1016/j.pain.2014.07.011.
- Key study showing that a large part of systemic morphine analgesia in human patients is mediated outside the brain
- Stein, C., et al., Analgesic effect of intraarticular morphine after arthroscopic knee surgery. N Engl J Med, 1991. 325: p. 1123 1126; doi: 10.1056/NEJM199110173251602.
- Key study demonstrating that clinical pain relief can be produced by activation of opioid receptors in peripheral injured tissue
- Jiménez-Vargas, N.N., et al., Agonist that activates the µ-opioid receptor in acidified microenvironments inhibits colitis pain without side effects. Gut, 2022. 71(4): p. 695-704; doi: 10.1136/gutjnl-2021-324070.
- Key study showing efficacy and lack of locomotor, respiratory and GI side effects in a colitis rodent model
- Degro, C.E., et al., Evolving acidic microenvironments during colitis provide selective analgesic targets for a pH-sensitive opioid. Pain 2023; 164: p. 2501–2515; doi: 10.1097/j.pain.0000000000002956.
- Key study showing tissue pH parallels the evolution of inflammation in a colitis model and that the pH-sensitive opioid analgesia is titrated to the degree of inflammation
- Machelska, H. and M.Ö. Celik, Advances in Achieving Opioid Analgesia Without Side Effects. Front Pharmacol, 2018. 9: p. 1388; doi: 10.3389/fphar.2018.01388.
- Informative review on the concept of pH-sensitive analgesics
- Stein, C. and S. Küchler, Targeting inflammation and wound healing by opioids. Trends Pharmacol Sci, 2013. 34(6): p. 303-312; doi: 10.1016/j.tips.2013.03.006.
- Informative review on potential anti-inflammatory benefits of our compounds
- U.S. Food and Drug Administration (FDA), Healthy Innovation, Safer Families: FDA’s 2018 Strategic Policy Roadmap, 2018. p. 1 – 18;
- FDA roadmap highlighting the critical need for safe and effective alternatives to conventional opioids