Development of a First-in-Class Click Chemistry-Based Cancer Therapeutic, from Preclinical Evaluation to a First-in-Human Dose Escalation Clinical Trial.

ABSTRACT:

Purpose

Achieving precise drug activation without associated toxicities is a significant challenge in developing cancer therapeutics. Click Activated Protodrugs Against Cancer is a pretargeting approach that uses bioorthogonal click chemistry in vivo to selectively capture and activate drugs at tumors and can be applied to a wide variety of targeted therapeutics. The first-in-class Click Activated Protodrugs Against Cancer-based cancer therapeutic SQ3370 uses a clickable pretargeting agent that reacts with a chemically attenuated clickable payload of doxorubicin (Dox) and releases the active cytotoxic drug in situ.

Patients and methods

We describe the preclinical development and translation of SQ3370 to a first-in-human dose-escalation clinical trial in adult patients with a

SUBMITTER: Srinivasan S 

PROVIDER: S-EPMC12402790 | biostudies-literature | 2025 Sep

REPOSITORIES: biostudies-literature