Drug intelligence / Profile preview

mipasetamab uzoptirine + gemcitabine

Development stage
Discontinued
Lead developer
ADC Therapeutics
Modality
Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

**Mipasetamab uzoptirine + gemcitabine** is a combination therapy under clinical investigation for advanced solid tumors, including sarcomas and pancreatic cancer. Mipasetamab uzoptirine (ADCT-601) is an antibody-drug conjugate targeting AXL, a receptor tyrosine kinase overexpressed in multiple malignancies and implicated in tumor progression and therapeutic resistance. The antibody is site-specifically conjugated via GlycoConnect technology to a pyrrolobenzodiazepine (PBD) dimer cytotoxin (SG3199) using a cleavable Val-Ala linker. Upon binding to AXL-expressing tumor cells, the ADC is internalized, releasing the cytotoxic payload that induces DNA interstrand cross-links and irreparable DNA damage, resulting in tumor cell death. Gemcitabine is a nucleoside analog chemotherapy that inhibits DNA synthesis by incorporation into DNA and subsequent chain termination, blocking cell proliferation and inducing apoptosis. Preclinical studies show synergy between mipasetamab uzoptirine and gemcitabine, supporting the rationale for this combination in resistant and heterogeneous solid tumors[2][3][4][7].

Other names
ADCT-601 + gemcitabine
02

Targets

AXL (AXL receptor tyrosine kinase)DNA polymerase family

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