The Platform for Developing Brain-Penetrant Drugs

The cure of various brain diseases has long been hampered by the lack of brain-penetrant drugs, of which the development is intrinsically challenging due to the complex blood-brain barrier (BBB) structure of the brain that may prevent more than 98% of drugs from entering the brain. Hyperway has been able to probe into this niche area due to the efforts of our many experienced medicinal chemists who have profound insights into drug design and synthesis technology, Hyperway has developed a highly integrated system, using our state-of-art technology and equipment, that allows the design, synthesis, screening, pharmacokinetic uation, and toxicology optimization to be performed in a most efficient manner.

At present, this platform has quickly contributed to our drug pipelines, including several lead compounds with a brain penetration rate of more than 60%. These compounds will soon be tested in treating primary or secondary brain cancers, autoimmune diseases, pain, etc. Among these, HBW-3210, a reversible 3rd-generation Bruton’s Tyrosine Kinase (BTK) inhibitor, has already obtained an implied license for clinical trials for treating primary/secondary central nervous system lymphoma (PCNSL/SCNSL) in October 2022.

Representative Program HBW-3210  

In addition to its promising potency as an irreversible BTKi that is effective in C481 mutation, HBW-3210 is brain-permeable (rat brain permeability: > 60%). As compared head-to-head with competitors in a preclinical animal model, HBW-3210 is significantly superior in its efficacy, and can overcome the problem of drug resistance caused by C481S mutation! These results have been published as abstracts in American Society of Clinical Oncology (2021) and European Hematology Association (2021), respectively. On Oct.14, 2022, HBW-3210 obtained an implied license for clinical trials for treating PCNSL/SCNSL.