Benefits of ConjuChem Technology

The Benefits of ConjuChem Technology

Until recently, the field of peptide therapeutics has not been widely explored clinically, despite the significant progress made in the generation of candidates coming from advances in phage display, combinatorial libraries, and the advent of proteomics. This has been due to the belief that no short-acting peptide can overcome poor patient compliance and high manufacturing costs.

The Drug Affinity Complex (DAC™) and Preformed Conjugate-Drug Affinity Complex (PC-DAC™) technology platforms developed by ConjuChem provide a solution to the challenges of protecting peptides from peptidase degradation and subsequent rapid kidney clearance. These technology platforms attempt to give long circulating half-lives to potent peptide drugs that would normally be rapidly degraded and cleared.

Long Half-Life in the Body

While natural peptides are usually degraded and cleared rapidly from the circulation because of their short half-lives, the covalent attachment of a DAC™ or PC-DAC™ to albumin has been shown to retard peptide clearance mechanisms. This characteristic permits the half-lives of the DAC™ and PC-DAC™ albumin bioconjugates to remain similar to the long half-life of albumin—typically greater than 10 days in humans. This provides a long duration of effect for the drug, as compared with the short duration of effect for the original peptide.

Attachment to Cysteine 34: a Key Advantage of our Technology

The DAC™ and PC-DAC™ complexes target a single site on albumin called cysteine-34. The reactive chemical group used as part of the DAC™ and PC-DAC™ complexes is highly selective for thiol chemical groups, such as the ones found on cysteine-34. The attachment to cysteine 34 provides properties that are difficult or impossible to obtain through attachment to other sites on albumin. Cysteine 34 is involved in the covalent attachment of many natural entities present in the body, such as wastes and process byproducts, and helps remove them. The Company is thus mimicking a natural phenomenon with its DAC™ and PC-DAC™ technology platforms such that several therapeutic benefits result from that phenomenon (particularly in terms of half-life and immunogenicity).

Extensive Tissue Distribution, Interpatient Variability, and Limited Central Nervous System Side Effects

Albumin is the main component of blood and is a constituent in a majority of all blood proteins. It circulates in the blood and is present in most tissues and organs throughout the body. Using albumin as a carrier for DAC™ and PC-DAC™ complexes reduces interpatient variability. The bioconjugates retain the extensive distribution profile of albumin—including dispersion throughout all tissues, with the exception of the central nervous system (CNS) because albumin does not readily cross the blood-brain barrier. The extensive distribution profile of albumin allows ConjuChem to target a variety of disease states using DAC™ and PC-DAC™ bioconjugates with albumin as a carrier. Also, because albumin does not readily cross the blood-brain barrier, the risk of serious CNS side effects is greatly reduced.

Managing Growth

ConjuChem currently has the capacity to conduct multiple research programs simultaneously. ConjuChem contracts out its clinical trial and manufacturing requirements to contract research organizations and other third-party vendors, and it expects to continue to do so in the future.