HPMA-based active targeted polymer-anticancer drug conjugates

  • University Reference Number: U-6244

TECHNOLOGY SUMMARY

  • Drug delivery Pioneer, Dr. Jindřich Kopeček has innovated the next generation of Antibody Drug Conjugates (ADC) with high efficacy tumor targeting and minimal off-target toxicity. The innovative approach involves a controlled living polymerization technique which results in a well-defined semitelechelic maleimide functionalized HPMA polymer-drug conjugate, followed by specific attachment to an antibody via accessible cysteine residue to generate a homogenous ADC with adjustable amount of payload.
  • Lead ADC, RTX-P-EPI (Rituximab conjugated to Epirubicin) has been well characterized for high linker stability, homogenous ADC mixture, and ADC internalization. Both affinity and pharmacokinetics are comparable to Rituximab. Epirubucin upregulates apoptotic proteins synergizing tumor targeting efficacy of RTX with Epirubicin leading to high efficacy tumor inhibition in animal models of Lymphoma.

BENEFITS

  • Innovative polymerization linker chemistry for controlled drug payload: ADC with high specificity, affinity, desirable PK and tumor efficacy
  • Homogenous ADC mixture significantly lowers the risk of toxicity due to free drug
  • Biodegradable HPMA stable linker
  • Rapid customization for new ADC

MARKET OPPORTUNITY

  • Next generation antibodies have the potential to reach sales of $5.7b, ADCs comprise about 1/3 of this. Two ADCs have been recently FDA approved with more than 30 ADcs are in clinical development. Antibodies in clinical development have an approval success rate of 23% and ADC success rate is 35%.

TECHNOLOGY STATUS

Development Status

  • RTX-P-EPI is validated in animal models of lymphoma. Extensive characterization of MOA, ADC internalization and PK studies has been performed.

Intellectual Property

  • A new construct of antibody-drug conjugates for treatment of B-cell non-Hodgkin's lymphomas; Eur J Pharm Sci. 2017 May 30;103:36-46
  • The Light at the End of the Tunnel; Second Generation HPMA Conjugates for Cancer Treatment; In Review

INVENTOR

  • Leverages the world-renowned knowledge of drug delivery pioneer Dr. Jindrich (Henry Kopeček) who has designed, synthesized, characterized, and pursues innovation in ADC for clinical development.
  • https://faculty.utah.edu/u0032205-JINDRICH_Henry_KOPECEK/biography/index.hml

CONTACT

  • Leena Bhoite, Ph.D.
  • Technology Manager
  • 801-213-3581
  • leena.bhoite@tvc.utah.edu

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