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AAZ+-ValCit-MMAE
- Development stage
- Preclinical
- Lead developer
- Philogen
- Modality
- Prodrugs/Conditional Activator Small Molecules → Small Molecules
- Administration
- Intravenous
01
Overview
**AAZ+-ValCit-MMAE** is an investigational carbonic anhydrase IX-targeted small molecule-drug conjugate. It couples an affinity-matured acetazolamide-derived CAIX ligand to the microtubule-disrupting cytotoxin monomethyl auristatin E through a valine-citrulline cleavable linker and a p-aminobenzyl self-immolative spacer. The conjugate was evaluated preclinically in CAIX-positive renal cell carcinoma models, where it showed antitumor activity, and its activity was substantially enhanced by co-administration with the tumor-targeted immunocytokine L19-IL2. ([aacrjournals.org](https://aacrjournals.org/clincancerres/article/24/15/3656/80996/Enhanced-Therapeutic-Activity-of-Non-Internalizing))
- Other names
- AAZ + ValCit-MMAE
02
Targets
CA9 (Carbonic anhydrase IX)TUBB (Tubulin (alpha and beta subunits))
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