{"id":43975,"date":"2022-05-17T09:01:14","date_gmt":"2022-05-17T07:01:14","guid":{"rendered":"https:\/\/pharma-trend.com\/en\/ionctura-to-present-at-asco-encouraging-phase-ib-refractory-uveal-melanoma-data-for-first-semi-allosteric-pi3k%ce%b4-inhibitor-ioa-244\/"},"modified":"2022-05-17T09:01:14","modified_gmt":"2022-05-17T07:01:14","slug":"ionctura-to-present-at-asco-encouraging-phase-ib-refractory-uveal-melanoma-data-for-first-semi-allosteric-pi3k%ce%b4-inhibitor-ioa-244","status":"publish","type":"post","link":"https:\/\/pharma-trend.com\/en\/ionctura-to-present-at-asco-encouraging-phase-ib-refractory-uveal-melanoma-data-for-first-semi-allosteric-pi3k%ce%b4-inhibitor-ioa-244\/","title":{"rendered":"iOnctura to present at ASCO encouraging Phase Ib refractory uveal melanoma data for first semi-allosteric PI3K\u03b4 inhibitor, IOA-244"},"content":{"rendered":"
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GENEVA–(BUSINESS WIRE)–iOnctura SA<\/a>, a clinical-stage oncology company targeting key resistance mechanisms in solid tumors, announced today that it will present Phase Ib data on its lead pipeline asset, IOA-244, the highly differentiated novel phosphoinositide 3-kinase delta (PI3K\u03b4) inhibitor, at the 2022 ASCO (American Society of Clinical Oncology) Annual Meeting, taking place June 3-7 in Chicago.\n<\/p>\n

<\/a><\/p>\n

\n\u201cWe believe IOA-244 has a wider therapeutic window than other molecules in the PI3K\u03b4 inhibitor class because of its unique semi-allosteric binding properties,\u201d said Catherine Pickering, PhD, CEO of iOnctura. \u201dThe data presented at ASCO will show that IOA-244 has potentially best-in-class tolerability and impressive overall survival in refractory uveal melanoma patients. We are looking forward to presenting the data and accelerating development of IOA-244 to treat uveal melanoma and other solid tumors.\u201d\n<\/p>\n

\nHigh expression of PI3K\u03b4 in both cancer cells and in the tumor immune landscape is a contributing factor to many solid tumor types escaping the host\u2019s immune response. This is achieved by tumors, in part, through PI3k\u03b4-mediated upregulation of T regulatory (Treg) cells, making the tumors \u201dcold\u201d, or difficult to detect by the body\u2019s immune system. IOA-244 inhibition of PI3k\u03b4 blocks proliferation of Treg cells, thus making \u201ccold\u201d tumors \u201chot\u201d, unveiling them to immune system detection and facilitating an anti-tumor immune response.\n<\/p>\n

\nExquisite selectivity for PI3K\u03b4 over other subtypes, including the closely related PI3K\u03b3, taken together with IOA-244\u2019s unique semi-allosteric mechanism, which is achieved through differentiated binding to the PI3k\u03b4 protein\u2019s kinase domain, represents a unique first-in-class mechanism in solid tumors. This mechanism may allow IOA-244 to lock the kinase in its resting state, completely preventing initiation of downstream cell signalling pathways normally triggered when it is activated at the cell membrane.\n<\/p>\n

\n\u201cWe believe IOA-244\u2019s semi-allosteric non-ATP competitive mechanism may block Treg upregulation and simultaneously avoid initiating other signalling cascades that may lead to toxicities,\u201d explained Lars Van Der Veen, PhD, CTO of iOnctura. \u201cOther PI3k\u03b4 inhibitors are thought to act on PI3k\u03b4 by blocking the ATP pocket without preventing the kinase from being activated at the cell membrane.\u201d\n<\/p>\n

\nIOA-244 is being investigated in the DIONE-01 Phase I trial in metastatic cancers. The objective of Part A, now complete, was to determine the safety, tolerability, and dosage of IOA-244 in cancer patients to determine the biologically effective dose range. The continuing Part B of the study consists of expansion cohorts of patients with different tumor types, including patients with metastatic uveal melanoma. The poster at ASCO will include Phase Ib data from DIONE-01 in refractory uveal melanoma patients.\n<\/p>\n

\nDetails of the presentation:<\/b>\n<\/p>\n