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6R-RedFol-1
- Development stage
- Preclinical
- Lead developer
- Paul Scherrer Institute
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Small Molecules
- Administration
- Intravenous
01
Overview
6R-RedFol-1 is a preclinical-stage folate receptor (FR)-targeting radioconjugate developed by the Paul Scherrer Institute (PSI) and ETH Zurich, in collaboration with Merck & Cie. It is designed for radiotheranostic applications, specifically targeted radionuclide therapy and SPECT/CT imaging of folate receptor-positive cancers. Chemically, the molecule consists of a 6R-5-methyltetrahydrofolate (6R-5-MTHF) targeting moiety, a DOTA chelator (typically radiolabeled with lutetium-177 to form [177Lu]Lu-6R-RedFol-1), and a 4-(p-iodophenyl)butanoate albumin-binding entity. The integration of the albumin binder prolongs blood circulation and enhances tumor accumulation. Preclinical studies in KB tumor-bearing mice have demonstrated that [177Lu]Lu-6R-RedFol-1 achieves high tumor uptake and a superior tumor-to-kidney ratio compared to its 6S-diastereoisomer and folic acid-based counterparts, resulting in enhanced therapeutic efficacy and reduced renal toxicity.
- Other names
- 177Lu-6R-RedFol-1[177Lu]Lu-6R-RedFol-1
02
Targets
FOLR1 (FRα)
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