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IgG1-Dolaflexin
- Development stage
- Discontinued
- Lead developer
- Mersana Therapeutics
- Modality
- Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
IgG1-Dolaflexin is a nonbinding control antibody-drug conjugate (ADC) developed by Mersana Therapeutics to evaluate the non-specific activity of the Dolaflexin platform in preclinical research. It consists of the humanized IgG1 monoclonal antibody rituximab (Rituxan) conjugated to the Dolaflexin polymer-based linker-payload system. The Dolaflexin platform enables a high drug-to-antibody ratio (DAR), typically ranging from 10 to 18, carrying the antimitotic payload auristatin F-hydroxypropylamide (AF-HPA). AF-HPA inhibits tubulin polymerization, leading to cell cycle arrest in the G2/M phase. In studies of target-specific ADCs like XMT-1536, IgG1-Dolaflexin serves as a negative control to distinguish between target-mediated antitumor activity and non-specific effects or bystander killing associated with the payload and linker platform.
- Other names
- nonbinding control Dolaflexin ADCrituximab-Dolaflexin
02
Targets
TUBB (Tubulin (alpha and beta subunits))
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