How Pentarins® Work

Tarveda’s proprietary Pentarins® are miniature drug conjugates, a class of cancer therapeutics uniquely designed to target, penetrate and treat solid tumors.

Pentarins are designed to maintain their miniature size and overcome biological barriers in solid tumors through two distinct capabilities as highlighted in the name “PENTARIN”:

  • Effective penetration:  The PEN in Pentarin represents the penetration into solid tumors.
  • Tumor cell targeting:  The TAR in Pentarin represents the selective tumor cell targeting.

Penetration of the Pentarin deep into the solid tumor occurs rapidly due to its small size. Due to their large size, conjugates like ADCs have restricted penetration into dense tissue of solid tumors. Pentarins, which are only a very small fraction of the size of the ADCs can effectively penetrate the tumor tissue.

Targeting ligands that consist of either a peptide or small molecule that bind to cancer cell targets including cell surface receptors and intracellular proteins. The ligands are conjugated to the therapeutic payload through an optimized chemical linker and in a manner that creates the desired efficacy.

Accumulation deep into the tumor is driven by honed biodistribution properties of Pentarins and the highly selective targeting of receptors over-expressed on the cancer cells or intracellular targets that are differentiated in cancer cells compared to normal cells.

Linker chemistry is tuned for sustained release of the drug preferentially inside the tumor cells with the timing of cleavage optimized for the biology of the target to maximize efficacy while limiting payload release outside of the tumor.

Selected payloads chosen to be effective in the tumor cells that overexpress the target for the Pentarin’s ligand.

Tuned pharmacokinetics and biodistribution enhance tumor uptake while controlling the duration of circulation in the blood to minimize potential toxicities.