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KIT-MMAE
- Development stage
- Preclinical
- Modality
- RNA Aptamers → RNA Therapeutics → Nucleic Acid Therapeutics, DNA Aptamers → DNA Therapeutics → Nucleic Acid Therapeutics
- Administration
- Intravenous
01
Overview
KIT-MMAE is an aptamer-drug conjugate (ApDC) designed for the treatment of KIT-positive acute myeloid leukemia (AML). It consists of a KIT-targeting aptamer, identified via SELEX, covalently linked to the cytotoxic payload monomethyl auristatin E (MMAE). The conjugate specifically binds to the KIT (CD117) receptor on the surface of AML cells and is internalized primarily through caveolae-mediated endocytosis. Once inside the cell, MMAE is released to inhibit tubulin polymerization, leading to cell cycle arrest and apoptosis. Preclinical studies in xenograft and patient-derived xenograft (PDX) models have demonstrated significant tumor growth inhibition and a favorable safety profile, suggesting its potential as a precision therapy for KIT-positive AML.
- Other names
- KIT-targeted aptamer-monomethyl auristatin E conjugateKIT-targeted ApDC
02
Targets
KIT (c-KIT proto-oncogene receptor tyrosine kinase)TUBB (Tubulin (alpha and beta subunits))
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