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C&EN: Click chemistry sees first use in humans

October 23, 2020

Targeting mechanism could help to avoid side effects of powerful anticancer drug
By Mark Peplow

A therapy that relies on click chemistry to target a powerful cancer drug at tumor cells, sparing healthy ones, has entered Phase 1 clinical trials. It marks the first time that a click chemistry reaction has been carried out inside a patient’s body, according to Shasqi, the San Francisco–based biotech firm that developed the therapy.

The work marks a milestone in bioorthogonal chemistry, which relies on reactions that can run inside living organisms without disrupting biochemical processes. So-called click reactions have become a mainstay of this approach because they occur exclusively between two synthetic molecules, rapidly and irreversibly clicking them together. Researchers already use bioorthogonal chemistry to tag biomolecules with imaging agents, such as fluorescent probes; and it has helped to manufacture targeted therapeutics, such as antibody-drug conjugates, that have subsequently entered clinical trials.

Read the full article on the C&EN website