The National Health Research Institutes (NHRI), a non-profit foundation supported by Taiwan’s Ministry of Health and Welfare, is looking for an industrial partner for further clinical development of a promising new drug against lung cancer.
Lung cancer is the leading cause of cancer death in the world, with non-small cell lung cancer (NSCLC) accounting for 85% of lung cancer deaths. In recent years, epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) have shown remarkable effects in patients with certain genetic alternations in EGFR. Use of the two first-generation EGFR-TKIs (gefitinib and erlotinib) has been limited because patients acquired resistance to them. In 2013, afatinib was approved by the U.S. Food and Drug Administration (FDA); although afatinib seems to be a more potent TKI than gefitinib or erlotinib, serious adverse reactions (skin and GI side effects) have been reported. In 2016, osimertinib (Tagrisso®) was approved for relapse patients harboring a secondary mutation (EGFRT790M) and was extended to become a first-line therapy for NSCLC in 2018. However, all the FDA-approved TKIs are not effective in patients bearing the EGFR-exon20 (~4% of EGFR mutated NSCLCs) or HER2-exon20 (2–4% in NSCLCs) insertion mutations.
NHRI is promoting an EGFR-TKI drug-development program that has the support of research projects under the Ministry of Science and Technology, including the Translational Medicine Project and the National Research Program for Biopharmaceuticals. Our team at NHRI’s Institute of Biotechnology and Pharmaceutical Research has identified DBPR112 as a potent EGFR-TKI. DBPR112 has shown good inhibition on the activities of various forms of EGFR kinases and the growths of several human lung cancer cells. DBPR112 is a new-generation EGFR-TKI that is potentially better than afatinib:
- DBPR112 displays potent activities against mutant cancer cells harboring EGFR-exon20 insertions or HER2-exon20 insertions.
- It has higher oral bioavailability.
- The pharmacokinetic properties of DBPR112 are superior to those of afatinib, demonstrating the potential of DBPR112 as a therapeutic agent for various solid tumors.
- DBPR112 shows a higher tolerated dose and less toxicity than afatinib.
In 2016, the U.S. and Taiwan FDAs approved DBPR112 for a Phase I clinical study (DBPR112-101), which is currently taking place at National Taiwan University Hospital and Taipei Medical University Hospital. Overall, the results of pre-clinical studies indicate that DBPR112 may be more tolerable than afatinib. Other than NSCLC harboring exon20 insertion mutations, DBPR112 may also be efficacious on NSCLC harboring other types of EGFR mutants, head and neck cancer, breast cancer, and esophageal cancer. Patents on DBPR112 cover the United States, Taiwan, China, Japan, and Korea.
NHRI welcomes inquiries about cooperation for further clinical development of this promising new drug.
Ashley, C.-W. Chen, Institute of Biotechnology and Pharmaceutical Research, National Health Research Institutes, TEL: +886-37-246-166 ext.35701, E-mail: firstname.lastname@example.org
Nathalie Huang, Secretariat, National Health Research Institutes, TEL: +886-37-246-166 ext.32113, E-mail: email@example.com