Regulon Inc., a biopharmaceutical company, engages in the discovery and development of nanopharmaceutics in oncology based on liposome encapsulation platform technology. Its products include Lipoplatin, a liposomally encapsulated cisplatin for various cancer indications, including non-small cell lung cancer and pancreatic cancer; and Lipoxal, a liposomally encapsulated oxaliplatin for colorectal cancer. The company was founded in 1997 and is based in Athens, Greece & California with operations in Europe and Asia.
Regulon's unique liposome encapsulation technology applicable to drugs, small molecules, peptides, proteins and viruses, significantly reduces the side effects of chemotherapy known to exacerbate the quality of life (QOL) of cancer patients. The firm has successfully applied this technology to encapsulate two members of the platinum family of anticancer drugs: cisplatin and oxaliplatin.
Regulon's lead product, Lipoplatin for pancreatic cancer (same drug under the name Nanoplatin for non-small cell lung cancer, NSCLC), is a liposomally encapsulated cisplatin nanoparticle. Cisplatin is the most widely-used chemotherapy drug, the gold standard for epithelial malignancies with applications to over 50% of human cancers. Lipoplatin nanoparticles, loaded with cisplatin are uptaken by tumors and metastases (10 to 200-fold higher than normal tissue) by leaking through the compromised endothelium of tumor vasculature sprouted during neoangiogenesis, a process known as extravasation, and by the avidity of tumors for nutrients with Lipoplatin disguised as a nutrient with its lipid shell. Moreover, Lipoplatin nanoparticles fuse with the cell membrane or are rapidly uptaken by cancer cells thus emptying their toxic payload inside the cell. Published Phase III studies show a lower toxicity with improved therapeutic index in adenocarcinomas of the lungs compared to cisplatin; this feature was not shown by other platinum blockbuster drugs (carboplatin, oxaliplatin). In a randomized Phase III in NSCLC, a statistically significant reduction of neutropenia, nephrotoxicity and asthenia of cisplatin was demonstrated by its replacement with Lipoplatin. Also in a randomized Phase III in nonsquamous-NSCLC the partial response for the Lipoplatin arm was 59% compared to 42% for the cisplatin arm and the difference was statistically significant (p=0.036).