EGFR inhibitor development home: target degradation

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EGFR mutation is a driving factor of NSCLC, which is more common in Asian patients, and is closely related to the growth, metastasis, proliferation and anti-apoptosis of cancer cells

Source: Reference [1]

EGFR inhibitors (EGFR-TKIs) have brought the dawn of treatment for NSCLC patients, and they still play an important role in clinical practice

Source: Reference [2]

In the face of this deadlock, EGFR degradants may be a new hope for EGFR targeted therapy.

Source: C4 therapeutics

The biggest advantage of EGFR degradants is that they can target a variety of drug-resistant mutations and have a wide range of potential applicable populations

Source: C4 therapeutics

Source: C4 therapeutics

For example, in the preclinical animal transplantation model of CFT8919, oral administration showed obvious protein degradation function and tumor suppression effect

Source: C4 therapeutics

Source: C4 therapeutics

Moreover, CFT8919 also has good central system activity and has therapeutic potential in brain metastasis models

Source: C4 therapeutics

The unsatisfactory performance of EGFR monoclonal antibodies in the clinic has left room for imagination for double antibodies and ADC drugs

Source: ASCO2021

In short, a small molecule degradation agent with convenient oral administration and cost advantages, if it shows a therapeutic effect in accordance with the mechanism in the clinic, it will also have an impact on antibodies, double antibodies or ADCs

As for that, the endless problem of drug resistance

Reference

[1]Shu Fang, Zhehai Wang.

[2]Chee-Seng Tan, et al.