LIPAX™: NEOLIPOSOMAL INTRACAVITARY PACLITAXEL TECHNOLOGY FOR TARGETED CHEMOTHERAPY

LiPax is a proprietary neoliposomal intracavitary paclitaxel drug delivery platform designed to enhance the therapeutic index of proven oncology agents, which results in more effective treatments for intracavitary cancers. LiPax™, is a locally delivered formulation of the well-established chemotherapy drug, paclitaxel. It has completed a Phase 1-2a clinical trial for non-muscle invasive bladder cancer (NMIBC) and has demonstrated impressive clinical activity while being very well tolerated and safe. LiPax is also in development for malignant pleural effusion (MPE), intraperitoneal carcinoma (ovarian) and upper tract urothelial carcinoma (UTUC).

Paclitaxel is still the most widely used chemotherapy agent worldwide; however, its use leads to severe chemotherapy related side effects. It is known to be highly active in systemic application for urothelial carcinomas, is lipophilic and not solubilized in the acidic environment of the bladder. It is known to cause systemic toxicity resulting in severe side effects such as peripheral neuropathy, hearing loss, low blood count, and hair loss among others. Paclitaxel has not been formulated or approved to be used intravesically in its existing formulations. By utilizing LiPax to enhance permeation and solubility, we have overcome the barriers to intravesical delivery of paclitaxel with no systemic exposure. Preclinical and clinical studies have demonstrated superior efficacy of intracavitary delivery, and we attribute the success of this drug delivery model to the following key differentiators: 

LETHALITY

The effectiveness of paclitaxel against various types of cancer is well established. Laboratory tests have demonstrated that formulating paclitaxel as LiPax enhances its lethality by a factor of more than 200-fold against T24 human cancer cells compared to Mitomycin C (MMC). Consequently, smaller concentrations of LiPax will be required to achieve the same or greater response rates in patients.

PERSISTENCE

Current intravesical treatments, such as MMC, have not been formulated or approved for the hostile and acidic bladder environment and as such have very limited effectiveness after a patient’s voiding of the bladder urine. Unlike existing treatments, LiPax is lipophilic and adheres to the urothelium which enables adherence of LiPax on the bladder wall, persisting as a reservoir of high concentration drug. Studies have shown that liposomes can persist on the bladder wall for multiple days after instillation and provide patients with sustained exposure to the active chemotherapy agent long after treatment.

PENETRATION

In contrast to current treatments that are mostly hydrophilic, LiPax’s lipophilic structure penetrates deep into the target tissue (e.g. bladder wall). Ex vivo studies have confirmed lethal concentrations of paclitaxel extending into the muscle layer but not beyond the bladder wall. Promising complete response rates have been achieved in nude mice studies, confirming effective localized targeting of tumor cells without any systemic exposure or toxicity.