Another important milestone in the process of accelerating the clinical development of TY-9591 — On March 22, 2022, the Phase II clinical trial of TY-9591 in the treatment of EGFR-mutated NSCLC with brain metastases was successfully initiated in the Affiliated Cancer Hospital of Chinese Academy of Medical Sciences!

Source：www.chinadrugtrials.org.cn

This is an open, multicenter Phase II clinical study（CTR20212878）, initiated by TYK Medicines, Inc. （hereinafter referred as to TYK Medicines）, and led by Yuankai Shi of Cancer Hospital of Chinese Academy of Medical Sciences, to include EGFR-sensitive mutation-positive NSCLC patients with parenchymal or pia metastases to evaluate the efficacy and safety of TY-9591 in the treatment of EGFR mutation-positive NSCLC with brain metastases or leptomeningeal metastases.

The incidence of brain metastases in advanced NSCLC is as high as 57%, and the average natural survival of patients is only 1-2 months, which is seriously life-threatening and seriously affects the quality of life. The therapeutic effect of traditional clinical therapies such as radiotherapy and chemotherapy is very limited. The efficacy of first-generation EGFR-TKIs was poor, and the efficacy data of third-generation EGFR-TKIs were only from the subgroup analysis in clinical studies. Currently, no effective drugs for this indication have been approved globally, and there are still unmet clinical needs and difficulties.

The preclinical study (CTR20212878) indicated that TY-9591 tablets had high bioavailability and could penetrate the blood-brain barrier. Phase I trial showed both intracranial ORR and systemic ORR up to 100% in 9 patients with measurable CNS lesion, and intracranial lesions in 2 patients were complete responses. The clinical safety of TY-9591 is generally controllable. Common adverse reactions such as decreased blood count and other abnormalities in laboratory tests are mostly grade 1-2.

Professor Yuankai Shi said that with the increase in lung cancer therapy and the extension of patients’ survival, controlling and even preventing brain metastases plays a key role. TY-9591 tablets showed a significant effect on patients with brain metastases of NSCLC in the phase I study, both intracranial and extracranial lesions can response, and has good safety, which is expected to bring new hope for patients with NSCLC brain metastases.

It is worth mentioning that for the clinical research of EGFR-TKI, the team led by Professor Shi Yuankai has never stopped. The outstanding data produced in the research and development process has repeatedly earned the attention and recognition of the international oncology community. It is believed that under the leadership of Professor Yuankai Shi, this study will further speed up the clinical trial process, yield compelling results sooner, and bring benefits to more patients as quickly as possible.

About TY-9591

TY-9591 is an orally, irreversible, third-generation inhibitor of Epidermal Growth Factor Receptor (EGFR) harboring sensitising-mutations (EGFRm) and TKI-resistance mutation T790M, individually developed by TYK Medicines, Inc. TY-9591 has good stability, high bioavailability, and is capable of penetrating the blood-brain barrier to achieve intracranial efficacy. With similar efficacy and development characteristics to Osimertinib, TY-9591 differs in its drug metabolism characteristics, which can significantly reduce the production of toxic metabolites AZD5104 (TY-9591-D1) and reduce toxic side effects, thus suggesting a potentially wider clinical therapeutic window. TY-9591 is a potent inhibitor for the first-line treatment of adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) with activating EGFR mutation (including exon 19 deletions or exon 21 L858R substitution mutation) or the treatment of adult patients with advanced EGFR mutation positive NSCLC with central nervous system metastases.

About TYK Medicines, Inc.

TYK Medicines is an innovative biotechnology company based in China, facing the global, focusing on researching and developing international cutting-edge new drugs. The company has established a high-efficiency innovative drug research and development platform, with fully functioned instruments, covering multiple pharmaceutical fields including drug synthesis, biological fermentation, drug analysis, bioanalysis, and formulation research, and is committed to becoming the best domestic and world-class new drug research and development company.