IDEAYA Biosciences, Inc. (Nasdaq: IDYA), a precision medicine oncology company committed to the discovery and development of targeted therapeutics, today announced the development candidate nomination of IDE251, a potential first-in-class KAT6/7 dual inhibitor.
“We are pleased to announce the nomination of IDE251 as our third development candidate this quarter and 8th development candidate in our precision medicine oncology pipeline. IDE251 has a potential first-in-class product profile and selectively inhibits two epigenetic modulators, KAT6 and KAT7, and based on the preclinical profile we believe there is an opportunity for an enriched response in 8p11 amplified cancers, which occur in 15% of breast cancers patients and in up to 17.5% in squamous NSCLC,” said Yujiro S. Hata, President and Chief Executive Officer of IDEAYA Biosciences.
“IDE251 is a promising potential first-in-class molecule designed to selectively target both KAT6 and KAT7 while sparing other structurally similar KAT family members. KAT6 and KAT7 are mechanistically intertwined epigenetic modulators of cell identity and lineage commitment programs corrupted by oncogenic transformation. Dual KAT6/7 inhibition with IDE251 delivers robust and durable anti-tumor activity, superior to KAT6 inhibition alone, in preclinical tumor models with 8p11 amplifications as well as in biomarker selected indications dependent upon lineage-specific transcription factor activity. IND-enabling studies are progressing as planned and we are targeting to bring this program to the clinic next year,” commented Michael White, Ph.D., Chief Scientific Officer, IDEAYA Biosciences.
IDE251 is an equipotent, highly selective, small molecule dual inhibitor of the lysine acetyltransferase (KAT) 6 and 7, both of which have been shown to support cancer cell survival. IND-enabling studies to support the potential clinical evaluation of IDE251 monotherapy in patients with breast and lung cancers with 8p11 amplification are ongoing, as well as additional opportunities in the setting of lineage addiction. Based on IDEAYA’s biomarker evaluation, 8p11 amplification prevalence is projected to be approximately 15% in breast cancer and 17.5% in squamous NSCLC.
IDEAYA is targeting an Investigational New Drug (IND) submission to the U.S. Food and Drug Administration (FDA) in 2025 for IDE251, subject to satisfactory completion of ongoing preclinical and IND-enabling studies.
