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Kazia Therapeutics acquires SETDB1 inhibitor platform from QIMR Berghofer

A preclinical bicyclic peptide targeting a disease-associated nuclear SETDB1 complex sits at the center of an in-licensing agreement announced April 13...

Edited by Robert McTiernan··2 min read

Kazia Therapeutics (Nasdaq: KZIA) and QIMR Berghofer Medical Research Institute announced an in-licensing agreement focused on a preclinical bicyclic peptide targeting a disease-associated nuclear SETDB1 complex. Kazia has acquired global rights to the SETDB1 epigenetic drug development platform, including lead candidate MSETC, a bicyclic peptide designed to restore immune signaling in tumors that have become resistant to checkpoint inhibitors. The Brisbane-based research institute, a Queensland government-established non-profit founded in 1945, retains an interest via a tiered revenue-sharing structure.

Kazia paid an upfront of approximately USD 1.39 million. The agreement carries no clinical or regulatory milestone obligations, with economics structured entirely as a tiered revenue share tied to development progress. Rates were not disclosed.

Deal context

MSETC is described by Kazia as targeting a novel, disease-associated nuclear SETDB1 complex rather than the isolated enzyme. SETDB1 — also known as KMT1E or ESET — is a histone methyltransferase that catalyzes trimethylation of histone H3 at lysine 9, a repressive chromatin mark associated with silencing of tumor suppressor genes and immune recognition pathways. Preclinical literature has linked SETDB1 overexpression to immune evasion across multiple solid tumor types, with inhibition shown to restore interferon signaling and enhance antigen presentation. MSETC's bicyclic peptide format is structurally relevant here: the constrained two-ring architecture enables engagement of protein-protein interaction surfaces within multi-protein nuclear assemblies — interfaces that conventional small molecules typically cannot access. The platform also incorporates an AI-integrated discovery engine that Kazia says enabled rapid optimization of MSETC and retains the capacity to generate additional candidates. MSETC is in preclinical development, with IND-enabling studies the next defined milestone.

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The SETDB1 program extends a pipeline that Kazia has been building around complementary layers of tumor biology. Paxalisib, its lead clinical asset and a PI3K/Akt/mTOR pathway inhibitor originally licensed from Genentech in 2016. The molecule has completed a Phase II/III study in glioblastoma and remains in trials across breast cancer, brain metastases, diffuse midline gliomas, and primary CNS lymphoma. NDL2, a preclinical nuclear PD-L1 protein degrader, targets an intracellular resistance mechanism distinct from antibody-based checkpoint approaches. The SETDB1 program adds a chromatin-level immune reactivation angle, which Kazia frames as addressing tumor immune evasion upstream of the transcriptional and protein-level mechanisms covered by paxalisib and NDL2 respectively. EVT801, a VEGFR3 inhibitor licensed from Evotec in April 2021, also sits in the pipeline. The company has indicated it intends to leverage shared CRO infrastructure across the SETDB1 and NDL2 programs to contain costs during IND-enabling work.

Kazia has framed the SETDB1 program as a candidate for early strategic partnering given its applicability across tumor types and its mechanistic relevance to checkpoint inhibitor resistance, a setting where combination approaches are actively sought by larger oncology developers.

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