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tirapazamine + pembrolizumab
- Development stage
- Unknown
- Lead developer
- Teclison
- Modality
- Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
- Administration
- Intraarterial (tirapazamine Via Trans‑arterial Embolization), Intravenous (pembrolizumab Infusion)
01
Overview
Tirapazamine + pembrolizumab is an investigational combination therapy for cancer that pairs two distinct agents with complementary mechanisms. Tirapazamine is a bioreductive small molecule prodrug that becomes cytotoxic under hypoxic conditions typical of solid tumors; it generates DNA-damaging free radicals selectively in low-oxygen tumor regions. Pembrolizumab is a monoclonal antibody immune checkpoint inhibitor targeting the programmed cell death protein 1 (PD-1) receptor on T cells; it blocks PD-1 interaction with its ligands to enhance anti-tumor immune responses. The combination aims to exploit tumor hypoxia for direct cytotoxicity while simultaneously unleashing immune-mediated tumor destruction. This regimen has been studied using trans-arterial tirapazamine embolization (TATE) followed by intravenous administration of pembrolizumab in patients with liver metastases from colorectal cancer and non-small cell lung cancer[1][2][3][7].
- Brand names
- Keytruda
- Other names
- trans-arterial tirapazamine embolization + pembrolizumabTATE + pembrolizumab
02
Targets
PDCD1 (Programmed cell death protein 1 receptor)
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