- CFI-400945 is a first-in-class, orally active small molecule that selectively inhibits PLK4 (Polo-Like Kinase 4), a key regulator of centriole duplication and the overexpression of which is associated with adverse survival outcomes in cancer patients
- Inhibition of PLK4 exacerbates the genomic instability in cancer cells, forcing cell death
- In preclinical murine models, CFI-400945 demonstrated strong efficacy in a large number of patient-derived xenografts from heavily pre-treated patients
- We are currently conducting multiple clinical trials across a variety of cancer indications including breast cancer, prostate cancer, and AML
- More than 50 patients have been treated with CFI-400945 to date; thus far the candidate has been well tolerated by patients, with reversible neutropenia emerging as the most common adverse event, and durable clinical responses in an unselected patient population
- We believe CFI-400945 may have applicability in a variety of hematologic and solid tumor cancers as monotherapy and in combination with PD-1/PD-L1 inhibitors
- CFI-402257 is a potent, highly selective, orally active small molecule inhibitor of TTK (Tyrosine Threonine Kinase), a protein kinase that is essential for genomic stability during cell division
- Inhibition of TTK allows cancer cells to progress through mitosis in the presence of misaligned chromosomes, resulting in eventual cell death
- In preclinical studies, CFI-402257 demonstrated robust suppression of tumor growth across numerous cancer types in vitro and in vivo.
- In clinical trials to date across a variety of advanced cancers, there have been no drug-related adverse events reported, and durable single agent responses
- CFI-402257 is being evaluated in a number of Phase 1 and 2 clinical trials in advanced cancers , both as monotherapy and in combination with other agents.
- CFI-402411 is a novel, highly orally available immunomodulatory small molecule inhibitor of HPK1 (Hematopoietic Progenitor Kinase 1), a critical regulator of immune cell activation, antigen presentation, and T cell responses to immunosuppressive factors
- Inhibition of HPK1 has been shown to activate T cells, B cells, and dendritic cells
- Regulatory filings are in progress, and clinical trials of CFI-402411 are expected to initiate in early 2020
- CFI-402411 has the potential to be an effective treatment in a wide range of cancers as a monotherapy, and in combination with other agents including checkpoint inhibitors.
