Phase I and pharmacokinetic study of E7070, a novel sulfonamide, given at a daily times five schedule in patients with solid tumors. A study by the EORTC-Early Clinical Studies Group (ECSG)

Punt, C.J.A.; Fumoleau, P.; van de Walle, B.; Faber, M.N.; Ravic, M.; Campone, M.

doi:10.1023/a:1012287111922

Cited by 59Cancer therapeutics and mechanismsCancer Treatment and PharmacologyStatistical Methods in Clinical Trials

Phase I and pharmacokinetic study of E7070, a novel sulfonamide, given at a daily times five schedule in patients with solid tumors. A study by the EORTC-Early Clinical Studies Group (ECSG)

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Punt, C.J.A., Fumoleau, P., van de Walle, B., Faber, M.N., Ravic, M., Campone, M.·2001·Annals of Oncology

DOI 10.1023/a:1012287111922

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Abstract

Background E7070 is a novel antitumor sulfonamide which blocks the cell in G1 phase. A phase I study was initiated to investigate the toxicity, maximum tolerated dose (MTD), and pharmacokinetics of this compound when administered intravenously at a daily times five schedule once every three weeks.Patients and methods Patients with solid tumors not amenable to standard forms of therapy were eligible. E7070 was administered to cohorts of 3-6 patients per dose level, the starting dose was 10 mg/m2/day. Dose escalation was performed according to a Fibonacci-like scheme.Results Thirty-three patients entered the study. At E7070 doses of 200 and 160 mg/m2/day dose-limiting toxicities occurred, which consisted of febrile neutropenia, thrombocytopenia. diarrhea, skin folliculitis, asthenia, and stomatitis. The pharmacokinetic profile of E7070 at this schedule is non-linear with increasing dose. A partial response was observed in a patient with heavily pretreated breast cancer. Disease stabilizations and some minor responses were also documented.Conclusions Myelosuppression is the predominant toxicity of E7070. Clinical efficacy with E7070 was observed. The recommended dose for further studies at this daily times five schedule is 130 mg/m2/day.

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Kinetic and structural analyses revealed relatively weak drug-protein interactions stabilized by ternary docking across broad protein-protein interfaces, resulting in highly selective drug-dependent degradation of RBM39 and its paralogue RBM23.
“Kinetic and structural analyses revealed relatively weak drug–protein interactions that are stabilized by ternary docking across broad protein–protein interfaces, which results in highly selective drug-dependent protein degradation of RBM39 and its paralogue RBM23179–181.”
From Cancer therapies based on targeted protein degradation — lessons learned with lenalidomide (2021) · cites this paper as [179]
Two additional, entirely distinct classes of small-molecule molecular glue degraders have been discovered.
“Two additional, entirely distinct classes of small-molecule molecular glue degraders have been discovered.”
From Cancer therapies based on targeted protein degradation — lessons learned with lenalidomide (2021) · cites this paper as [179]
RBM39 (CAPERα) is the direct molecular target responsible for the antitumour effect of aryl sulfonamides, which recruit RBM39 to CRL4DCAF15 for polyubiquitination and proteasomal degradation.
“Two independent groups identified RNA-binding motif protein 39 (RBM39, also known as CAPERα), a nuclear protein involved in pre-mRNA splicing, as the direct molecular target responsible for the antitumour effect of these sulfonamides, which recruit this splicing factor to the CRL4DCAF15 E3 ubiquitin ligase for polyubiquitination and subsequent proteasomal degradation177–179.”
From Cancer therapies based on targeted protein degradation — lessons learned with lenalidomide (2021) · cites this paper as [179]

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Authors: Punt, C. J. A., Fumoleau, P., van de Walle, B., Faber, M. N., Ravic, M., & Campone, M.
Affiliations: Radboud University Medical Center (NL)
Corresponding author: Punt, C.J.A.
ORCID: Punt, C.J.A.
Fumoleau, P.
Campone, M.
Venue: Annals of Oncology
Publisher: Elsevier BV
Published: 2001-09
Volume: 12
Issue: 9
Pages: 1289-1293
ISSN: 0923-7534 (ISSN-L)
DOI: 10.1023/a:1012287111922
OpenAlex: W2271112841
Cited by: 57
References: 1
Citations by year: 2025: 4 · 2024: 2 · 2023: 1 · 2022: 4 · 2021: 4 · 2020: 3 · 2017: 1 · 2014: 1
FWCI: 2.31
Type: journal article
Language: en
Open access: bronze
doi.org
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
www.elsevier.com/open-access/userlicense/1.0/ (vor, 6688 d)
Locations: Annals of Oncology (publishedVersion)
PubMed (publishedVersion)
Pure Amsterdam UMC (publishedVersion)
Data Archiving and Networked Services (DANS) (submittedVersion)
Radboud Repository (Radboud University) (submittedVersion)
Topics: Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Cancer therapeutics and mechanisms
Health Sciences › Medicine › Oncology › Cancer Treatment and Pharmacology
Physical Sciences › Mathematics › Statistics and Probability › Statistical Methods in Clinical Trials
Keywords: sulfonamides, anticancer agents, G1 cell cycle arrest, solid tumors, maximum tolerated dose, dose-limiting toxicity, myelosuppression, febrile neutropenia, thrombocytopenia, pharmacokinetics, nonlinear pharmacokinetics, breast cancer, dose escalation, recommended dose
MeSH terms: Adult, Aged, Antineoplastic Agents, Dose-Response Relationship, Drug, Drug Administration Schedule, Female, Humans, Male, Middle Aged, Neoplasms, Neutropenia, Sulfonamides, Thrombocytopenia, Treatment Outcome, Maximum Tolerated Dose

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Phase I and pharmacokinetic study of E7070, a novel sulfonamide, given at a daily times five schedule in patients with solid tumors. A study by the EORTC-Early Clinical Studies Group (ECSG)

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