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DFRF4539A
- Development stage
- Phase 1
- Lead developer
- Genentech
- Modality
- Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
DFRF4539A is a Genentech-developed, investigational anti-Fc receptor-like protein 5 antibody-drug conjugate for relapsed or refractory multiple myeloma. It comprises a humanized IgG1 anti-FcRH5 antibody linked through a protease-cleavable maleimidocaproyl-valine-citrulline-p-aminobenzyloxycarbonyl linker to monomethyl auristatin E. Following FcRH5-mediated binding and internalization by myeloma cells, lysosomal cleavage releases MMAE, which inhibits tubulin polymerization, causing G2/M arrest and apoptosis. In a 39-patient phase 1 trial, activity was limited, and further development for multiple myeloma was stopped. ([pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/30718503/?dopt=Abstract))
- Other names
- DFRF-4539ADFRF4539ADFRF 4539ARG7598RG-7598RG 7598
02
Targets
FCRL5 (Fc receptor-like protein 5)TUBB (Tubulin (alpha and beta subunits))
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