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Updated: Aug 7, 2026

Chemical Inactivation of the E3 Ubiquitin Ligase Cereblon by Pomalidomide-based Homo-PROTACs
Published on: May 15, 2019
Bortezomib: efficacy comparisons in solid tumors and hematologic malignancies
Tommaso Caravita1, Paolo de Fabritiis, Antonio Palumbo
1Myeloma Unit, Hematology Department, St Eugenio Hospital, Rome, Italy. tcaravita@yahoo.it
Abstract:
Proteasome inhibition represents a new anticancer approach, with the potential effect of arresting tumor growth, metastasis and angiogenesis through the activation of multiple mechanisms. Bortezomib is a biologically active agent, producing predictable, dose-related and reversible proteasome inhibition; it has shown antitumor activity in various malignancies and is the first proteasome inhibitor to be used in clinical practice. Several trials demonstrated that bortezomib is relatively well tolerated, causing manageable nonhematologic and hematologic toxicity. The drug was approved in 2003 by the FDA for the treatment of patients with multiple myeloma who had received at least two prior therapies and demonstrated disease progression on the last therapy; its application was expanded recently for second-line treatment. This article summarizes the principal clinical trials of bortezomib and discusses its efficacy in solid and hematologic tumors.
Insights
Proteasome inhibition, a novel anticancer strategy, shows promise in halting tumor progression. Bortezomib, a leading proteasome inhibitor, demonstrates significant antitumor activity and manageable toxicity in clinical trials.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Proteasome inhibition is an emerging anticancer strategy.
- Bortezomib is the first clinically approved proteasome inhibitor.
- It targets tumor growth, metastasis, and angiogenesis via multiple mechanisms.
Purpose of the Study:
- To summarize clinical trials of bortezomib.
- To discuss its efficacy in various cancers.
- To highlight its role in cancer treatment.
Main Methods:
- Review of principal clinical trials.
- Analysis of bortezomib's efficacy data.
- Assessment of safety and tolerability.
Main Results:
- Bortezomib exhibits predictable, dose-related proteasome inhibition.
- Antitumor activity observed across various malignancies.
- Manageable nonhematologic and hematologic toxicity reported.
Conclusions:
- Bortezomib is an effective treatment for multiple myeloma.
- Its application is expanding to second-line treatment.
- Further research into its efficacy in solid and hematologic tumors is warranted.
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