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firtecan pegol
- Development stage
- Phase 2
- Lead developer
- Belrose Pharma
- Modality
- Small Molecules, Biodegradable Polymers → Polymer-based Nanoparticles → Nanoparticles → Drug Delivery Systems
- Administration
- Intravenous
01
Overview
Firtecan pegol is a polyethylene glycol (PEG) conjugate of 7-ethyl-10-hydroxycamptothecin (SN38), the active metabolite of irinotecan. It is designed as an antineoplastic agent to deliver SN38 directly to tumor cells, bypassing the need for metabolic conversion required by irinotecan. After administration, hydrolysis releases SN38, which selectively stabilizes topoisomerase I-DNA covalent complexes, resulting in DNA breaks and apoptosis in cancer cells. PEGylation improves solubility and pharmacokinetics compared to unmodified SN38. Firtecan pegol has been investigated primarily for metastatic breast cancer (Phase II), colorectal cancer (Phase II), neuroblastoma (Phase I/II; orphan drug status), solid tumors (Phase I/II), and lymphoma (development discontinued). Developers include Enzon Pharmaceuticals, Belrose Pharma, and the National Cancer Institute[1][2][3][4][5].
- Brand names
- EZN-2208EZN2208EZN 2208
- Other names
- firtecan pegol
02
Targets
TOP1 (DNA Topoisomerase I)
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