SER-203
SER-203 is Serina's lead clinical candidate and entered IND-enabling studies in 2011. SER-203 is a pendant POZ with multiple molecules of the potent anti-cancer drug irinotecan attached to it, and it contains the targeting group folate at the terminus. SER-203 has been extensively evaluated in pre-clinical models of cancer and has shown remarkable efficacy; indeed, in most instances the tumors completely regress. The safety profile of SER-203 is substantially improved compared to the parent compound. Additionally, SER-203 has the unique ability to penetrate the cancer cell via a cell receptor that is often over-expressed on cancer cells. This process, known as receptor-mediated endocytosis, introduces this potent chemotherapeutic agent directly inside the cell where it is released from the polymer backbone and converted to an intermediate that inhibits replication of DNA, which triggers cell death.
Figure 1 shows the results of mouse xenograft studies with SER-203 in the KB oropharyngeal cancer line.
SER-203 is scheduled to enter human clinical trials in 2013.
Figure 1
Figure 1 : Xenograft study of Effect of Irinotecan vs SER-203 at various doses on the growth of human KB orpharyngeal cancer in nude mice. The KB oropharyngeal cancer is known to be markedly resistant to irinotecan, but SER-203 eradicates the tumor completely at medium and high doses of SER-203, and in seven of ten mice in the low dose cohort. Side effects including diarrhea and weight loss were also markedly diminished in the SER-203 cohorts (data not shown).
