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Changes in polymorphic forms can significantly influence the bioavailability of poorly soluble drugs. Although the FDA defines pharmaceutical equivalence based on having the same active ingredient, dosage form, and route of administration, it does not automatically disqualify products with different polymorphic forms. This means two products with different polymorphs can still be deemed pharmaceutically equivalent. However, polymorphic differences can affect properties like wettability,...
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Related Experiment Video

Updated: Jan 19, 2026

Initial Evaluation of Antibody-conjugates Modified with Viral-derived Peptides for Increasing Cellular Accumulation and Improving Tumor Targeting
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Small-Format Drug Conjugates: A Viable Alternative to ADCs for Solid Tumours?

Mahendra P Deonarain1,2, Gokhan Yahioglu3,4, Ioanna Stamati5

  • 1Antikor Biopharma Ltd., Stevenage Bioscience Catalyst, Gunnels Wood Road, Stevenage Herts SG12FX, UK. m.deonarain@antikor.co.uk.

Antibodies (Basel, Switzerland)
|September 24, 2019
PubMed
Summary

Smaller Antibody-Drug Conjugates (ADCs) show promise for solid tumors, overcoming limitations of larger formats. Research focuses on optimizing their pharmacokinetics for improved in vivo efficacy.

Keywords:
alternative scaffoldantibody–drug conjugatefragmentpenetrationpharmacokinetics

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Area of Science:

  • Oncology
  • Pharmacology
  • Biotechnology

Background:

  • Antibody-Drug Conjugates (ADCs) have evolved significantly over 40 years.
  • Current large-format ADCs show success in some cancers but struggle in solid tumors.
  • Smaller ADC formats are being explored for better tumor penetration and pharmacokinetics (PK).

Purpose of the Study:

  • To review research and development of smaller format drug conjugates over the last decade.
  • To assess the in vitro and in vivo potency of various small-format agents.
  • To identify strategies for optimizing small-format drug conjugates as therapeutics.

Main Methods:

  • Review of primary literature and conference proceedings.
  • Analysis of over a dozen small-format drug conjugates (1 kDa to 80 kDa).
  • Evaluation of potency with ultra-potent payloads (auristatins, maytansinoids).

Main Results:

  • Smaller format conjugates demonstrate potent in vitro activity.
  • In vivo potency is often reduced due to rapid clearance.
  • Recent conjugates incorporate ultra-potent payloads, enhancing in vitro efficacy.

Conclusions:

  • Small-format drug conjugates face challenges with in vivo pharmacokinetics.
  • Strategies to balance tumor penetration and PK are crucial for therapeutic viability.
  • Optimized small-format conjugates could offer alternatives to established large-format ADCs for solid tumors.