Drug intelligence / Profile preview

brostallicin + cisplatin

Development stage
Phase 2
Lead developer
Sobi
Modality
Small Molecules
Administration
Intravenous
01

Overview

Brostallicin + cisplatin is a combination chemotherapy regimen used primarily in the treatment of advanced solid tumors, including metastatic triple-negative breast cancer. Brostallicin is a synthetic second-generation DNA minor groove binder that covalently binds to DNA within the minor groove, interfering with DNA division and leading to tumor cell death. It shows enhanced antitumor activity particularly in cells resistant to other anticancer agents due to high glutathione S-transferase (GST) and glutathione content. Cisplatin is a platinum-based chemotherapeutic agent that causes DNA crosslinking and damage, leading to apoptosis of cancer cells. Preclinical studies demonstrated more than additive antitumor effects when brostallicin was combined with cisplatin, especially when cisplatin was administered before brostallicin, without additional toxicity. Clinical trials have shown manageable hematologic toxicities and encouraging anti-tumor activity including disease stabilization and confirmed tumor responses in heavily pretreated patients with metastatic triple-negative breast cancer.[1][2][3][5][6] The combination is under clinical investigation for efficacy in various solid tumors including metastatic breast cancer.[4]

02

Targets

Pt-DNA adduct (DNA-oxaliplatin adduct)

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