Introduction to CT-262

A compound with these five characteristics would be a major advance in the treatment of cancer.

CT-262 is a prodrug delivery system that selectively releases a highly cytotoxic moiety intracellularly in cancer cells, sparing healthy cells.
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• Active moiety is an analogue of duocarmycin with highly potent antitumor activity

• Novel design – nothing like it examined previously - creates potential for major advance in the treatment of cancer

• Prodrug is inactive and highly stable in plasma, greatly limiting the potential for off-target toxicity

• Selective intracellular release in cancer cells of toxic duocarmycin moiety – free drug - from prodrug driven by protein in cytosol of cancer cells that does not appear to be meaningfully present in healthy cells

• Targeting of cancer cells not dependent upon presence of cell surface antigen – all cancer cells targeted

 

• CT-262 highly efficacious in in vivo xenograft and transgenic cancer models, as well as in organoid models highly predictive of efficacy in humans

 

• Low toxicity, low myelosuppression that typically limits chemotherapy

 

• Not subject to traditional mechanisms of resistance (unable to raise resistance to date)

​Combination of results from preclinical efficacy studies and safety evaluations demonstrate CT-262 is highly efficacious and broadly active, and suggests the compound has a wide therapeutic window.
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CT-262 is a Prodrug That is Selectively Activated in Cancer Cells
​and Targets DNA to Induce Programmed Cell Death

CT-262 is an analogue of duocarmycin, a natural product with potent anti-tumor activity.  

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CT-262 Undergoes a Two-Step Process for Selective Activation Inside Cancer Cells Delivering Primed Drugs Selectively to Cancer Cells

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Contrast With Traditional Chemotherapy – Potential for Wide Therapeutic Window

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Selective Activation Shown in Mice with Breast Cancer: Inactive Prodrug is Converted to Primed Drug in Breast Cancer Tissue but Not in Normal Breast Tissue
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Highly Potent & Broadly Active in a Range of Human Cancers

Data demonstrate CT-262 is readily converted from inactive form to cytotoxic form in human cancers.

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CT-262 Shows Pronounced Activity Against Highly Resistant Human NSCLC ​in Murine Xenograft Model 

CT-262 inhibits tumor growth in a dose-dependent manner and continues inhibition after the last dose.

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CT-262 is Highly Potent, Efficacious and Broadly Active in Organoid Models of Cancer ​that are Predictive of Human Efficacy

Data demonstrate CT-262 is readily converted from inactive form to cytotoxic form in human cancers.

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CT-262 Should Be Much Less Susceptible to Cancer Cell Resistance Mechanisms Than Leading Therapies  

The promise of CT-262