VAL-083 (dianhydrogalactitol) is a “first-in-class” small-molecule chemotherapy agent, being developed by DelMar Pharmaceuticals.
VAL-083 is approved in China for the treatment of lung cancer and chronic myelogenous leukemia (a disease in which the bone marrow makes too many white blood cells), but with limited use due to a lack of data.
How VAL-083 works
VAL-083 has a unique anti-cancer mechanism that is distinct from platinum-based chemotherapy agents. It is an N7-bifunctional DNA alkylating agent. Alkylating agents are compounds that work by adding an alkyl group to proteins that make up the DNA molecule, stopping the strands of the double helix from connecting as they should. This leads to the breakage of DNA strands, affecting the ability of the cancer cell to multiply.
Other differences include VAL-083 targeting a different position in the DNA compared to other chemotherapeutics, and crosslinking opposite DNA strands as opposed to the same strand, as does cisplatin, for example.
The drug is also less susceptible to resistance mediated by the p53 gene and can cross the blood-brain barrier and accumulate in tumor tissue, which is important in patients whose lung cancer has spread to the brain.
The p53 gene has an important role in protecting the human body from cancer and is also responsible for the start of programmed cell death (apoptosis), which happens when a cell becomes damaged or cancerous. People with NSCLC usually have a mutation in the p53 gene, and these mutations are associated with chemotherapy resistance and poor treatment outcomes.
Two separate in vivo studies indicate that VAL-083 alone or when combined with cisplatin, is superior to cisplatin alone, suggesting a clinical potential in NSCLC resistant to tyrosine kinase inhibitors.
These results suggest that VAL-083 may be a viable treatment option for people with NSCLC who have failed regular chemotherapy and support the benefit as part of a platinum-based combination therapy in new patients.
DelMar plans to initiate a clinical study in NSCLC in collaboration with Guangxi Wuzhou Pharma, from China, which will fund the study.
Note: Lung Cancer News Today is strictly a news and information website about the disease. It does not provide medical advice, diagnosis, or treatment. This content is not intended to be a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition. Never disregard professional medical advice or delay in seeking it because of something you have read on this website.