helping patients who have limited or no cancer treatment options because of EGFR-TKI resistant tumors
Epidermal Growth Factor Receptor (EGFR) drives cancer progression in a large number of solid tumors in patients. EGFR inhibitors are the standard of care for most of these patients. Patients may respond to treatment initially, but nearly all will develop resistance within a year.
EGFR activity is important for driving tumor growth, but the protein itself is essential for the tumor’s survival. University of Michigan team Mukesh Nyati, PhD. and Theodore Lawrence, M.D., Ph.D., found that degrading EGFR kills cancer cells selectively by specifically targeting this receptor, which is more effective than inhibiting EGFR aone.
Nyati and Lawrence, along with Christopher Whitehead, Ph.D., M.B.A., developed DGD1202, a small molecule that is selectively effective in inducing phosphorylated-EGFR degradation in tumors, including tyrosine kinase inhibitors (TKI)-resistant tumors.
This new approach will be more effective and less toxic to normal tissues than current strategies being used because of the extraordinary selectivity of DGD1202.
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DGD1202 provides a treatment option for EGFR-driven TKI resistant patients who have developed resistance to all other currently available therapeutic alternatives.
DGD1202 has been developed and tested in a variety of in vitro and in vivo models for efficacy.
DGD1202 does not affect the EGFR in adjacent host tissue and does not manifest toxicities seen with other TKI agents.
- Intellectual Property: One issued patent for background IP, one patent filed for composition of matter and methods of use
- Regulatory Pathway: Begin discussions with regulatory consultants regarding the quickest path to an Investigational New Drug (IND) approval
- Complete Business Formation: Experienced senior management team in place, formally licensed to a biotechnology company
- Engage Investors: A large number of interested investors
- Product Launch: Initial clinical indication in TKI resistant non-small cell lung cancer population
- Obtain a co-crystal of EGFR bound with DGD1202
- Conduct in vivo tests to assess pharmacokinetics (PK) and pharmacodynamics (PD) of DGD1202 and determine the maximally tolerated dose (MTD) by clinically relevant routes of administration
- Establish correlation between the route of administration, dose, and duration of treatment (schedule) in mice
- Conduct efficacy and long-term safety of DGD1202 in multiple TKI-resistant, EGFR-dependent tumor models