Our pipeline

The first allosteric modulator of PI3Kδ, with a unique chemical structure and binding mode.

Allosteric modulation changes the 3D structure of a protein thereby affecting its activity. The phosphatidylinositol 3-kinase (PI3K) signalling pathway is one of the most commonly dysregulated pathways in cancer. PI3Kδ is one of four isoforms of the catalytic subunit of PI3K kinase. Whilst its expression is normally restricted to immune cells such as regulatory T cells and myeloid-derived suppressive cells, some cancers express high levels of PI3Kδ which acts to promote tumor growth and survival.

Roginolisib has exquisite selectivity over other isoforms and highly favourable pharmaceutical properties. It is being developed for indications burdened by immune mediated resistance and a high expression of PI3Kδ in cancer cells and tumor-infiltrating immune cells.

Roginolisib is an orally dosed small molecule that has shown preclinically to revert immunosuppression and inhibit the growth and proliferation of cancer cells with high PI3Kδ expression.

Clinical data generated to-date has shown the drug to have an exceptional safety profile and promising clinical activity in solid tumors and hematological malignancies. Five Phase II studies are in planning with 4 of these involving randomization versus standard of care.

The only autotaxin inhibitor currently in clinical development to treat cancer.

It distinctively inhibits both the catalytic and the chaperone activities of the enzyme. Autotaxin (ATX) is an extracellular enzyme that generates and transports lysophosphatidic acid (LPA). LPA is a bioactive phospholipid that stimulates the proliferation, migration and survival of many cell types and has been implicated in a wide range of diseases, including cancer.

Cambritaxestat has excellent potency and specificity. It is being developed as a first-in-class therapy for highly fibrotic tumours that overexpress ATX including pancreatic, liver, colorectal, ovarian and breast cancers. We are the first company to bring an ATX inhibitor to the clinic to treat cancer..

Cambritaxestat is an orally dosed small molecule that has shown preclinically to inhibit the growth and proliferation of cancer cells, stimulate immune cell infiltration into tumors and inhibit the development of fibrosis.

A Phase 1b study of cambritaxestat in combination with chemotherapy in metastatic pancreatic cancer is ongoing.

A novel small molecule TGF-β pathway inhibitor.

Activation of the transforming growth factor beta (TGF-β) signaling pathway in tumors correlates with tumor aggressiveness, immune escape and resistance to therapy.

We are developing IOA-359, a novel small molecule TGF-β pathway inhibitor, in solid tumors. By characterising the resistance mechanisms that typically arise when targeting the TGF-β pathway alone, our data-driven precision oncology methods are being used to design novel combination treatments that promise to override tumor survival pathways.