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Progress and Future Directions with Peptide-Drug Conjugates for Targeted Cancer Therapy
Oncopeptides AB, Vastra Tradgardsgatan 15, SE-11153 Stockholm, Sweden..
KTH, School of Biotechnology (BIO), Centres, Albanova VinnExcellence Center for Protein Technology, ProNova. KTH, School of Engineering Sciences in Chemistry, Biotechnology and Health (CBH), Protein Science, Protein Technology. KTH, Centres, Science for Life Laboratory, SciLifeLab.ORCID iD: 0000-0002-6104-6446
KTH, School of Biotechnology (BIO), Centres, Albanova VinnExcellence Center for Protein Technology, ProNova. KTH, Centres, Science for Life Laboratory, SciLifeLab.ORCID iD: 0000-0003-4214-6991
Oncopeptides AB, Vastra Tradgardsgatan 15, SE-11153 Stockholm, Sweden..
2021 (English)In: Molecules, ISSN 1431-5157, E-ISSN 1420-3049, Vol. 26, no 19, article id 6042Article, review/survey (Refereed) Published
Abstract [en]

We review drug conjugates combining a tumor-selective moiety with a cytotoxic agent as cancer treatments. Currently, antibody-drug conjugates (ADCs) are the most common drug conjugates used clinically as cancer treatments. While providing both efficacy and favorable tolerability, ADCs have limitations due to their size and complexity. Peptides as tumor-targeting carriers in peptide-drug conjugates (PDCs) offer a number of benefits. Melphalan flufenamide (melflufen) is a highly lipophilic PDC that takes a novel approach by utilizing increased aminopeptidase activity to selectively increase the release and concentration of cytotoxic alkylating agents inside tumor cells. The only other PDC approved currently for clinical use is Lu-177-dotatate, a targeted form of radiotherapy combining a somatostatin analog with a radionuclide. It is approved as a treatment for gastroenteropancreatic neuroendocrine tumors. Results with other PDCs combining synthetic analogs of natural peptide ligands with cytotoxic agents have been mixed. The field of drug conjugates as drug delivery systems for the treatment of cancer continues to advance with the application of new technologies. Melflufen provides a paradigm for rational PDC design, with a targeted mechanism of action and the potential for deepening responses to treatment, maintaining remissions, and eradicating therapy-resistant stem cells.

Place, publisher, year, edition, pages
MDPI AG , 2021. Vol. 26, no 19, article id 6042
Keywords [en]
peptide-drug conjugates, cancer, tumor-targeting drug conjugates, cytotoxic agent
National Category
Cancer and Oncology
Identifiers
URN: urn:nbn:se:kth:diva-304215DOI: 10.3390/molecules26196042ISI: 000707248700001PubMedID: 34641586Scopus ID: 2-s2.0-85116578795OAI: oai:DiVA.org:kth-304215DiVA, id: diva2:1609030
Note

QC 20211105

Available from: 2021-11-05 Created: 2021-11-05 Last updated: 2023-08-28Bibliographically approved

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Nilvebrant, JohanNygren, Per-Åke

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Albanova VinnExcellence Center for Protein Technology, ProNovaProtein TechnologyScience for Life Laboratory, SciLifeLab
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