Tech Forum Liposome Advanced and well-established drug delivery formulation for small molecules in oncology drug discovery and development

Even in the world of 2020s, small molecules are still a promising modality for anticancer drug development. Several novel fields of development, such as Targeting Protein Degrader (TPD), are emerging for the targets that have been considered undruggable. The design of small molecules for these hard-druggable targets inherited significant difficulties to harmonize the high affinity to the targets and other properties: pharmacokinetics, biodistribution and safety.

Liposome is a formulation technology that significantly improves the pharmacokinetics of small molecules by encapsulating in stable lipids nano capsule particles. This simple but effective delivery technology have the potential to address the pharmacokinetics, biodistribution or safety challenges of emerging small molecule anticancer drugs. In this session, the presenter will discuss that liposome has the potential to create new value in the rapidly growing field of novel small molecule oncology drugs.

As case studies, examples of liposomes that encapsulated conventional anticancer drugs: gemcitabine and topotecan will be presented. By adapting liposome formulation, these classical anticancer drugs significantly altered the tumor immune environment and dramatically enhanced the effect of immune checkpoint inhibitors in preclinical animal models. Liposomes were preferentially taken up by macrophages in the tumor. The compound in the liposomes was efficiently released from liposomes-internalized macrophages. We will also discuss a novel highly stable dihydrosphingomyelin (DHSM)-based liposome and its potential application to a wide range of small molecule anticancer drugs.

Liposome is a technology that can be adapted to a wide range of APIs, but clinical applications are still limited. One major reason is that there are several challenges in CMC development that require special techniques, equipment and expertise in manufacturing, analysis, and quality control. For example, the establishment of an In Vitro Release test method (IVR) with high recovery, reproducibility and good correlation with in vivo characteristics is required by the authority. These will be presented in this session.

Fujifilm is the CRDMO that offers these technologies for partners in the field of small molecule anticancer drug discovery and development.