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Cited by 89Natural Compounds in Disease TreatmentCell death mechanisms and regulationNatural product bioactivities and synthesis

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Phase I dose-escalation study of F60008, a novel apoptosis inducer, in patients with advanced solid tumours

Kitzen, J.J.E.M., de Jonge, M.J.A., Lamers, C.H.J., Eskens, F.A.L.M., van der Biessen, D., van Doorn, L., ter Steeg, J., Brandely, M., Puozzo, Ch., Verweij, J.·2009·European Journal of Cancer
DOI 10.1016/j.ejca.2009.01.026
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Abstract

Resistance of cancer cells to cytotoxic therapy can be caused by the activation of strong anti-apoptotic effectors, for example NF-kappaB. Therefore, compounds that inhibit NF-kappaB stimulation might overcome chemotherapy resistance. F60008, a semi-synthetic derivate of triptolide, is converted to triptolide in vivo and activates apoptosis in human tumour cells. We performed a phase I and pharmacological study of F60008 given intravenously as a weekly infusion for 2 weeks every 3 weeks in patients with advanced solid tumours. Twenty patients were enrolled, and a total of 35 cycles were administered. The most frequent haematological side-effect was mild grade 1-2 anaemia. Non-haematological toxicities included fatigue, nausea, vomiting, diarrhoea and constipation, all grade 1-2. Two lethal events were observed in which an increase in caspase-3 activity and overt apoptosis in monocytes and neutrophils could be seen. Pharmacokinetic studies showed high inter-individual variability and rendered F60008 a far from optimal derivate of triptolide.

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Crossref · 10.1016/j.ejca.2009.01.026

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  • Due to significant variability among patients and high toxicity in some, F60008 cannot be considered an appropriate derivative of triptolide for cancer patients.

    “However, due to significant variability among patients and high toxicity in some, F60008 cannot be considered as an appropriate derivative of TPL for cancer patients.92”

    From Drug repurposing for cancer therapy (2024) · cites this paper as [92]

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References 24 · Cited by 89

Research works printed but not linked: 22

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Metadata

Authors
Kitzen, J. J. E. M., de Jonge, M. J. A., Lamers, C. H. J., Eskens, F. A. L. M., van der Biessen, D., van Doorn, L., ter Steeg, J., Brandely, M., Puozzo, C., & Verweij, J.
Affiliations
  • Erasmus MC (NL)
  • Pierre Fabre (France) (FR)
Corresponding author
Kitzen, J.J.E.M.
ORCID
Venue
European Journal of Cancer
Publisher
Elsevier BV
Published
2009-07
Volume
45
Issue
10
Pages
1764-1772
ISSN
0959-8049 (ISSN-L)
DOI
10.1016/j.ejca.2009.01.026
OpenAlex
W2034612383
Cited by
89
References
24
Citations by year
2026: 2 · 2025: 5 · 2024: 8 · 2023: 3 · 2022: 7 · 2021: 4 · 2020: 4 · 2019: 4 · 2018: 3 · 2017: 5 · 2016: 6 · 2015: 6 · 2014: 7 · 2013: 4 · 2012: 9
FWCI
17.17
Type
journal article
Language
en
Open access
closed
Licence
www.elsevier.com/tdm/userlicense/1.0/ (tdm)
Locations
  • European Journal of Cancer (publishedVersion)
  • PubMed (publishedVersion)
  • EUR Research Repository (Erasmus University Rotterdam) (publishedVersion)
  • EUR Research Repository (Erasmus University Rotterdam) (submittedVersion)
Topics
  • Health Sciences › Medicine › Complementary and alternative medicine › Natural Compounds in Disease Treatment
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Cell death mechanisms and regulation
  • Physical Sciences › Chemistry › Organic Chemistry › Natural product bioactivities and synthesis
Keywords
apoptosis inducers, NF-κB inhibition, chemoresistance, advanced solid tumors, dose escalation, pharmacokinetics, hematologic toxicity, caspase-3, neutrophil apoptosis, monocytes
MeSH terms
Adult, Aged, Anemia, Diterpenes, Dose-Response Relationship, Drug, Drug Administration Schedule, Female, Humans, Leukocytes, Male, Middle Aged, Neoplasms, Phenanthrenes, Apoptosis, Antineoplastic Agents, Alkylating

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