TACH101: A Potent, First-In-Class KDM4 Inhibitor for Advanced Cancers

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Grant Award Details

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Grant Application Details

Application Title:

TACH101: A Potent, First-In-Class KDM4 Inhibitor for Advanced Cancers

Public Abstract:
Therapeutic Candidate or Device

TACH101 is a first-in-class small molecule inhibitor of KDM4 histone demethylase, an epigenetic modifier important for cancer stem cell proliferation.


Colorectal Cancer

Therapeutic Mechanism

TACH101 is intended to target colorectal cancer (CRC) stem cells as well as the bulk tumor by inhibiting proliferation. In CRC animal models, TACH101 treatment reduced the number of cells with cancer stem cell features and reduced the number of tumor-initiating cells. TACH101 also significantly slowed tumor growth in CRC models and showed high sensitivity in CRC with Microsatellite Instability High (MSI-H) status.

Unmet Medical Need

Late stage CRC patients receive chemotherapy with survival typically not exceeding 2 yrs. TACH101 showed potent anti-tumor activity in CRC animal models, including MSI-H CRC which accounts for 15% of cases and do not respond to chemotherapy due to deficiency in DNA repair mechanisms.

Project Objective

Phase 1a/1b trial completed

Major Proposed Activities

  • Complete Phase 1a dose escalation study to assess safety and recommended phase 2 dose (RP2D) of TACH101
  • Complete Phase 1b dose expansion study to assess effect of TACH101 in specific cancer types (CRC and GI cancers)
  • Complete analyses of blood samples from enrolled patients to assess genomic biomarkers that may inform of a responder population
Statement of Benefit to California:
California has a CRC incidence rate of ~32 per 100,000 people per year. With a population of ~39 million people, ~12,500 have CRC and about 22% will be diagnosed with late stage disease (SEER 2022). Thus, TACH101 has the potential to help ~2,750 advanced CRC patients in CA a year. In addition, the proposed project plan utilizes California-based resources (e.g., clinical site, PK vendor, Biomarker vendor, Manufacturing vendor), aligning with CIRM's mission to support CA-based infrastructure.