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DM1-acetazolamide conjugate
- Development stage
- Preclinical
- Lead developer
- ETH Zurich
- Modality
- Prodrugs/Conditional Activator Small Molecules → Small Molecules
- Administration
- Intravenous
01
Overview
**DM1-acetazolamide conjugate** is an experimental, disulfide-linked small-molecule drug conjugate developed for carbonic anhydrase IX-expressing cancers. An acetazolamide-derived ligand binds carbonic anhydrase IX on tumor cells and delivers the maytansinoid payload DM1, a tubulin-directed cytotoxin that disrupts microtubule function. In mouse SKRC52 renal cell carcinoma xenografts, the conjugate showed potent antitumor activity and was reported to outperform sunitinib and sorafenib in that model. ([pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/24623670/))
- Other names
- acetazolamide-DM1 conjugateacetazolamide-DM-1 conjugateacetazolamide-DM 1 conjugate
02
Targets
CA9 (Carbonic anhydrase IX)TUBB (Tubulin (alpha and beta subunits))
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