Drug intelligence / Profile preview

BL-8040 + pembrolizumab + liposomal irinotecan + 5-fluorouracil + leucovorin

Development stage
Unknown
Lead developer
BioLineRx
Modality
Nanoparticles → Drug Delivery Systems, Small Molecules, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Subcutaneous, Intravenous
01

Overview

This combination regimen consists of five therapeutics: BL-8040 (motixafortide), pembrolizumab, liposomal irinotecan (Onivyde), 5-fluorouracil, and leucovorin. BL-8040 is a CXCR4 antagonist, which disrupts the CXCL12/CXCR4 axis, enhancing immune cell infiltration and reducing immunosuppressive myeloid-derived suppressor cells in the tumor microenvironment. Pembrolizumab is a monoclonal antibody checkpoint inhibitor targeting programmed cell death protein 1 (PD-1) on T cells, thereby enabling immune-mediated destruction of tumor cells. Liposomal irinotecan inhibits topoisomerase I, interrupting DNA replication in cancer cells. 5-fluorouracil is a pyrimidine antimetabolite inhibiting thymidylate synthase, leading to impaired DNA synthesis; leucovorin enhances the activity of 5-fluorouracil. This regimen is under clinical investigation primarily for second-line treatment of metastatic pancreatic ductal adenocarcinoma, aiming to synergize immune modulation with cytotoxic chemotherapy[1][3][5].

Other names
pembrolizumabliposomal irinotecan5-fluorouracilleucovorin
02

Targets

TOP1 (DNA Topoisomerase I)PDCD1 (Programmed cell death protein 1 receptor)CXCR4 (C-X-C motif chemokine receptor 4)TS (Thymidylate synthase)

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