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PF-06650808
- Development stage
- Unknown
- Lead developer
- Pfizer
- Modality
- Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
PF-06650808 is a novel antibody-drug conjugate (ADC) developed to target Notch3-expressing tumor cells. It consists of a humanized IgG1 monoclonal antibody directed against the Notch3 receptor, chemically linked via a cleavable maleimidocapronic-valinecitruline-p-aminobenzylooxycarbonyl (vc) linker to an auristatin-based cytotoxic payload. Upon binding to Notch3 on cancer cells, the ADC is internalized and trafficked into lysosomes where proteolytic enzymes cleave the linker, releasing the cytotoxic agent directly inside tumor cells. This targeted delivery aims to maximize antitumor activity while minimizing systemic toxicity. PF-06650808 has been evaluated in phase I clinical trials for advanced solid tumors, particularly breast cancer, showing manageable safety and early signs of antitumor activity[1][4][7].
- Other names
- Anti-NOTCH3 ADCAnti-NOTCH-3 ADCAnti-NOTCH 3 ADC
02
Targets
NOTCH (Neurogenic locus notch homolog protein 3)
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