Protectan Technology: entolimod (CBLB502) & CBLB612

Protectans, including entolimod (CBLB502) and CBLB612, are engineered derivatives of natural apoptosis-suppressing factors produced by microbes that are part of the human microflora.12, 8 The activity of these microbial products and related Protectans derives from their ability to bind to and stimulate a particular class of cell surface receptors called Toll-Like Receptors (TLRs).7

Signaling through these TLRs leads to activation of the pro-survival NF-kB pathway.4 Activation of the NF-kB pathway drives expression of numerous genes, including those encoding inhibitors of apoptosis, scavengers of reactive oxygen species, anti-microbial proteins and cytokines. Due to differences in the cellular signaling pathways (including NF-kB) of tumor and normal cells, Protectans prevent apoptosis in normal cells, yet have no effect on the death of tumor cells, which occurs through non-apoptotic mechanisms.10, 11

The particular TLRs targeted by entolimod (CBLB502) and CBLB612 (TLR5 and TLR2, respectively) are expressed on a unique subset of cell types and mobilize unique downstream pathways. This leads to biological effects that are highly desirable from a therapeutic standpoint within well tolerated dose range.12, 9

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