acetazolamide + MMAE

**acetazolamide + MMAE** is a small molecule-drug conjugate (SMDC) composed of acetazolamide, a heteroaromatic sulfonamide that selectively binds to carbonic anhydrase IX (CAIX) on renal cell carcinoma cells, covalently linked via a cleavable dipeptide linker (most often valine-citrulline or valine-alanine) to monomethyl auristatin E (MMAE), a potent antimitotic cytotoxic agent. This targeted drug exploits the tumor-selective CAIX expression to localize and deliver the MMAE payload extracellularly at the tumor site. Upon cleavage of the linker by extracellular proteases, MMAE is released, resulting in the death of CAIX-positive tumor cells. Unlike antibody-drug conjugates, this SMDC does not depend on cellular internalization for payload release, and achieves high tumor-blood ratios, especially in renal cell carcinoma models. Developed primarily for kidney cancer, acetazolamide + MMAE shows promising anti-tumor efficacy with minimal off-target toxicity and superior serum stability when utilizing valine-citrulline or valine-alanine linkers[1][2].

Brand names

acetazolamide + MMAE

Other names

acetazolamide-MMAE conjugateAAZ-MMAE-SMDCacetazolamide small molecule-drug conjugate with monomethyl auristatin E