How Hot is the Third-generation EGFR-TKI?

Third-generation EGFR-TKI becoming a R&D hotspot

Sales of Osimertinib Approaching RMB 2 Billion in China in 2018

BPI-7711 of Beta Pharma into Phase III Clinical Trial.

Beta Pharma has recently started the Phase III clinical trial of BPI-7711 as a first-line therapy of non-small cell lung cancer (NSCLC), which has enrolled 294 participants, with gefitinib as the comparator.

BPI-7711 is a third-generation EGFR-TKI, making Beta Pharma the fourth Chinese pharmaceutical enterprises and hospital medical supply companies that enter the Phase III clinical trial of the variety following ACEA, Hansoh, and Allist.

Third-generation EGFR-TKI becoming a R&D hotspot

EGFR-TKI stands for epidermal growth factor receptor-tyrosine kinase inhibitor which is a targeted drug produced accompanying the cancer molecular typing and molecular biology development, and inhibits the whole pathway transduction and tumor growth by inhibiting nodes in intracellular signaling pathways, wherein, EGFR-TKI has become the drug of first choice recommended by NCCN for the big cancer type: EGFR-positive NSCLC (accounting for about 30% of lung cancers) owing to its prominent clinical efficacy. After over a decade of R&D, the EGFR-TKIs currently in the market are mainly divided into three generations:

 (Organized according to public data)

The third-generation EGFR-TKI mainly targets patients with T790M resistance mutation. T790M gene mutation is the major mutation type (accounting for about 50%) of resistance after using EGFR-TKI. The first-generation and second-generation EGFR-TKIs are ineffective against T790M because the latter has a small domain, which is difficult for conventional drugs to bind to. As a result, the third generation has become the R&D hotspot of the giants.

Sales of Osimertinib Approaching RMB 2 Billion in China in 2018

Avitinib, the first Chinese-produced third-generation EGFR-TKI, to be marketed soon

As the first third-generation EGFR-TKI independently developed by ACEA, avitinib maleate can inhibit EGFR L858R, Exon19del, and T790M mutation, and is used to treat NSCLC with EGFR mutation or resistance mutation. As an original new drug supported by China’s National S&T Major Project for Major New Drug Invention during the 12th Five-year Plan period, the drug has a global compound patent, and will be marketed soon. ACEA is now preparing for the marketing, and has determined the trade name to be Aoweikai, with the application process as follows:

The only fly in the ointment is that the penetration of the blood-brain barrier (BBB) by avitinib is far lower than that by osimertinib; the drug still could achieve good efficacy in patients with brain metastases and partly damaged BBB, however, meningeal metastases differ greatly from brain parenchyma metastases.

Hansoh, Allist, Beta Pharma, and Betta following closely

Besides ACEA, the third-generation EGFR-TKIs of Hansoh, Allist, and Beta Pharma have all entered Phase III clinical trials.

 (Organized according to open data)

The next 5 years will be the harvest period of the third-generation EGFR-TKIs as the drugs have successively entered Phase III clinical trials.

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