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.15, 11 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).10

Signaling through these TLRs leads to activation of the pro-survival NF-kB pathway.7 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.13, 14

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.15, 12

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