There is considerable evidence that cPLA2α plays a crucial role in cancer, inflammation and fibrosis. Firstly, it has been shown in mice that both lung and intestinal tumours can be reduced by knocking out cPLA₂α. Secondly, significant overexpression of cPLA₂α mRNA has been observed in patients with various tumour types, including lung, colorectal and breast tumours. Interestingly, a high expression of cPLA2α correlates with poor prognosis, decreased overall survival, increased risk of metastases and recurrence in breast, colorectal and several other cancers. Finally, screening of genomic signature data and early pharmacological inhibition studies in pre-clinical models has indicated that cPLA₂α-inhibitors may be used as chemosensitizers in multiple cancer indications. All in all, these results validate cPLA₂α as a promising target for the development of novel cancer therapies.
The therapeutic target is the key enzyme cPLA₂α, which causes release of arachidonic acid resulting in the activation of multiple inflammatory and proliferative processes that play a fundamental role in many diseases. Inhibition of cPLA₂α is predicted to have a therapeutic effect on cancer and inflammatory diseases via a new therapeutic intervention point. Our drug candidates are both potent and selective inhibitors of cPLA₂α and have demonstrated proof-of-efficacy in multiple pre-clinical disease models. The Company’s drug candidates target indications where the unmet clinical needs are great and the market potential is significant.
We currently own a composite research portfolio comprising two families of chemical substances and a number of active compounds protected by several patent families. The Company has established proof-of-concept in psoriasis, which has provided a excellent validation of the mechanism of action. This mechanism leads to a reduced inflammatory state at the cellular level and, by extension, reduced fibrosis—that is, a slowed cell division rate—which is one of the relevant causes of negative development of inflammatory-driven cancers and chronic kidney diseases. In addition, the Company has achieved significant effects in animals as well as other findings that support the use of cPLA₂α inhibitors in cancers and kidney or lung fibrosis. These promising results bode well for the development of new cPLA2α-targeting systemic treatments for cancer indications where the medical needs are identified as significant.