SQP22

SQP22 is a click-activated protodrug of monomethyl auristatin E (MMAE), a potent antimitotic agent that inhibits tubulin polymerization. Developed by Shasqi using its Click Activated Protodrugs Against Cancer (CAPAC) platform, SQP22 is modified with a trans-cyclooctene (TCO) moiety that significantly reduces its systemic cytotoxicity. The drug is designed to be selectively activated at the tumor site through a bioorthogonal click chemistry reaction with a tetrazine-modified activator, such as SQL70 (a tetrazine-modified hyaluronate) or SQT01 (a tetrazine-modified HER2-targeting fragment). This approach allows for the delivery of high doses of the cytotoxic payload directly to the tumor while minimizing off-target effects. Preclinical studies in murine tumor models, including Karpas 299 and RENCA, have demonstrated significant antitumor effects when SQP22 is paired with its corresponding activators.

Other names

monomethyl auristatin E protodrugMMAE protodrug