Benefits of Miniature Drug Conjugates and History of the Field

Targeted drug conjugates – which link targeting agents to potent cell-killing payloads – have been a highly successful approach for creating effective cancer therapies while reducing the toxicity associated with non-targeted payloads.

  • The first generation of these targeted drug conjugates are antibody drug conjugates (ADCs) based on the use of antibodies as the targeting agent, building on the breadth of recent antibody drug development in a variety of therapeutic settings. ADCs have been developed for both hematologic and solid tumors, and patients are benefitting from these therapies in both settings. The specificity of the antibody coupled with the long circulation time allows the ADC to bind to the targeted tumor tissue and expose the cell to the potent cytotoxic payload. While ADCs have shown promise, there appear to be certain limitations in efficacy for their widespread use, notably in solid tumors or other cancers where penetration and efficacy have been elusive
  • The small size of miniature drug conjugates overcomes one of the key biological barriers experienced with today’s targeted drug conjugates because they are designed to address the challenge of penetration into dense solid tumor tissue. By using a targeting ligand much smaller than an antibody, such as peptides, small molecules, or small protein scaffolds, miniature drug conjugates are able to rapidly penetrate into the tumor tissue. Particularly in solid tumors, miniature drug conjugates have attributes that allow them to effectively penetrate dense tumor tissue and the associated extracellular matrix, resulting in the unprecedented ability to therapeutically penetrate and target tumors. Yet, pharmacokinetic and biodistribution challenges have impacted the efficacy of miniature drug conjugates to date.
  • Tarveda’s innovative use of inherent miniature drug conjugate design features to create Pentarins® produces distinct therapeutic features. Traditionally, miniature drug conjugates as a drug class have faced a limitation of poor circulation time. By the intentional selection of an appropriate targeting ligand, payload and optimized linker, Tarveda has demonstrated that it is possible to tune the pharmacokinetics and biodistribution of the Pentarins to achieve robust efficacy in solid tumors.
  • Pentarins®: Overcoming the biological barriers hindering penetration into the dense tissue of solid tumors

    Tarveda’s innovative Pentarin platform enables the creation of novel, miniature drug conjugates that penetrate solid tumors and target tumor cells.

    The approach with Pentarins builds on this significant class of cancer medicines – including antibody drug conjugates – and evolves the therapeutic capabilities even further. With a unique structure, the tuning of pharmacokinetics and biodistribution, and miniature size, Pentarins are designed to enable the penetration of the conjugates into the tumor tissue where they either selectively bind to tumor cells and become internalized or, alternatively, diffuse into the cells and selectively bind to the tumor-specific, intracellular target with the subsequent release of the potent cell-killing payload in each case.