Drug intelligence / Profile preview

tirapazamine + KN046

Development stage
Unknown
Lead developer
AlphaMab Oncology
Modality
Bispecific Antibodies → Multispecific Antibodies → Engineered Antibody Formats → Antibody-Based Therapeutics, Small Molecules, Fc-Fusion Proteins → Carrier/Scaffold Proteins → Recombinant Proteins and Enzymes
Administration
Intra-arterial, Intravenous
01

Overview

Tirapazamine + KN046 is a combination therapy comprising the bioreductive small molecule tirapazamine and the bispecific antibody KN046. Tirapazamine (SR-4233) is a hypoxia-activated cytotoxin that selectively targets hypoxic tumor cells by inducing DNA strand breaks and inhibiting topoisomerase II under low-oxygen conditions. KN046 is a recombinant humanized bispecific antibody targeting both Programmed Death-Ligand 1 (PD-L1) and Cytotoxic T-Lymphocyte-Associated Protein 4 (CTLA-4). This combination is primarily investigated for the treatment of liver metastases from colorectal cancer, utilizing transarterial tirapazamine injection followed by embolization (TATE) to create a hypoxic environment that activates tirapazamine while KN046 provides dual immune checkpoint blockade.

Other names
TATE + KN046tirapazamine plus KN046
02

Targets

CTLA-4 (Cytotoxic t-lymphocyte–associated protein 4)CD274 (Programmed cell death protein 1 ligand 1)

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