Lipoplatin™

Liposomally encapsulated cisplatin, currently in clinical trials for a variety of cancer indications, including pivotal EMA Phase III trials for non-small cell lung cancer (NSCLC) and pancreatic cancer.

Regulon has recently successfully completed a non-inferiority investigator-led randomized Phase III trial and, for the first time in the history of chemotherapy, Lipoplatin™ has shown a statistically-significant increase in response rate in lung adenocarcinomas compared to cisplatin and with a significant reduction of all toxicities. Neither carboplatin, nor oxaliplatin, two globally approved blockbuster drugs, had shown similar results. Indeed both drugs show inferiority to cisplatin in efficacy in lung cancer; furthermore, carboplatin displays a higher myelotoxicity and oxaliplatin a higher neurotoxicity than cisplatin at their recommended doses. On the contrary, Lipoplatin™ has shown lower nephro-, neuro-, myelo; and GI-track toxicities over cisplatin. The superiority in efficacy over cisplatin against NSCLC adenocarcinomas and with a simultaneous reduction in all toxicities of cisplatin has been enthusiastically accepted by the oncology society internationally. The drug has also a plethora of pharmacoeconomic benefits. Under the name Nanoplatin™, the lead drug of Regulon has received the consent of EMA for a registrational Phase III across EU expected to lead to MA for lung adenocarcinomas (specifically non-squamous-NSCLC) in combination with pemetrexed (Alimta® of Lilly) in a superiority to cisplatin trial. The results of this study are expected to emerge by Q4 2012 and to demonstrate a higher overall survival (OS) and a higher progression-free survival (PFS) with a significant reduction of all side effects of cisplatin. These results will justify a high pricing of Nanoplatin™. Lipoplatin™ aspires to become a first line treatment for NSCLC based on the non-inferiority randomized Phase III study. This is the biggest cancer indication comprising 16% of all human cancers globally. Because cisplatin is used in more than 50% of human cancers, oncologists may start using the drug in more cases. Under the name Lipoplatin™ the lead drug of Regulon has received the orphan drug status against pancreatic cancer by EMA. The Company plans for clinical studies in gastric and triple-negative breast cancers. Thus, more indications for Lipoplatin prescriptions will follow later.

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Lipoxal™

Liposomally encapsulated oxaliplatin, that has enter Phase II trials for colorectal cancer. A Phase I study was published on this product. Lipoxal also represents a triumphal formulation as oxaliplatin's liposomal entrapment has met with many technical difficulties as that of cisplatin. Both lead product candidates have clinically demonstrated the ability to target and reduce tumors with lower toxicity levels than when unencapsulated. They can be more effective at treating tumors because of their reduced toxicity which allows more frequent and higher dose treatments and because of their higher concentration in tumors and metastases compared to normal tissues, a property explaining their reduced side effects.

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