Small Molecule Drug Conjugates

Small Molecule Drug Conjugates

Low molecular weight compounds can be used as alternatives to antibodies for tumor targeting applications. Our proprietary DNA-Encoded Libraries (DELs) greatly facilitate the ligand discovery process from millions of molecules. In analogy to Antibody Drug Conjugates (ADCs), Small Molecule Drug Conjugates (SMDCs) feature cytotoxic drugs and other bioactive payloads which are selectively guided to the site of disease by small molecule ligands.

The advantages of SMDCs over ADCs include their fast extravasation, a deep penetration of solid tumors and a favorable manufacturability (i.e., lower cost-of-goods and faster development).

Due to the technological advancements using DEL, we are able to generate small molecule ligands with antibody-like properties featuring ultra-high affinity to their target antigen and long residence time at the tumor site.

Philochem has identified and patented a number of pathology-associated targets, their corresponding ligands and appropriate linkers for the development of SMDCs.

SELECTED REFERENCES

Cazzamalli et al. (2018) Clin Cancer Res, 24, 3656-67
Cazzamalli et al. (2018) J Am Chem Soc, 140, 1617-21
Cazzamalli et al. (2017) J Control Release, 246, 39-45
Cazzamalli et al. (2016) Mol Cancer Ther, 15, 2926-35
Krall et al. (2016) J Nucl Med, 57, 943-9
Wichert et al. (2015) Nat Chem, 7, 241-9
Casi & Neri (2015) J Med Chem, 58, 8751-61
Krall et al. (2014) Chem Sci, 5, 3640-4
Krall et al. (2014) Angew Chem Int Ed, 53, 4231-35
Krall et al. (2013) Angew Chem Int Ed Engl, 52, 1384-402
Müller et al. (2013) J Nucl Med, 54, 124-31
Ahlskog et al. (2009) Bioorg Med Chem Lett, 19, 4581-6
Dumelin et al. (2008) Angew Chem Int Ed Engl, 47, 3196-201

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