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olaptesed pegol + pembrolizumab + nanoliposomal irinotecan + 5-fluorouracil + leucovorin

Development stage
Preclinical
Lead developer
TME Pharma
Modality
RNA Aptamers → RNA Therapeutics → Nucleic Acid Therapeutics, Nanoparticles → Drug Delivery Systems, Small Molecules, Monoclonal Antibodies → Antibody-Based Therapeutics, DNA Aptamers → DNA Therapeutics → Nucleic Acid Therapeutics
Administration
Intravenous
01

Overview

This is a **multi-agent chemotherapy and immunotherapy combination regimen**. - **Olaptesed pegol** is a CXCL12 inhibitor (a Spiegelmer, also known as NOX-A12) that blocks the CXCL12/CXCR4 axis, facilitating the influx of immune effector cells into the tumor microenvironment and enhancing response to immune checkpoint inhibitors[1][3][5]. - **Pembrolizumab** is a monoclonal antibody immune checkpoint inhibitor targeting PD-1, blocking its interaction with PD-L1/PD-L2, thus promoting anti-tumor immune activity[1][3]. - **Nanoliposomal irinotecan** (nal-IRI, branded as Onivyde) is a liposomally encapsulated topoisomerase I inhibitor delivering irinotecan more efficiently to tumor tissue[2][4][6]. - **5-fluorouracil** is a pyrimidine analogue antimetabolite inhibiting thymidylate synthase, impairing DNA synthesis in cancer cells[4][6]. - **Leucovorin** (folinic acid) potentiates the effects of 5-fluorouracil by enhancing binding to thymidylate synthase[4][6]. This regimen is investigational in solid tumors (colorectal, pancreatic cancer, and glioblastoma), typically in patients refractory to standard therapies[1][3][4][6].

Other names
olaptesed pegolpembrolizumabnanoliposomal irinotecan5-fluorouracilleucovorin
02

Targets

PDCD1 (Programmed cell death protein 1 receptor)CXCL12 (C-X-C motif chemokine ligand 12)TOP1 (DNA Topoisomerase I)TS (Thymidylate synthase)

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