PROTAC is an attractive technology in drug discovery. Researchers successfully discovered an orally available PROTAC degrader SIAIS164018 which degrades not only ALK or mutant EGFR but also oncoproteins involved in metastasis. SIAIS164018 is orally bioavailable and well tolerated in vivo. Pharmacokinetic and maximal tolerated dose (MTD) assays were performed by Medicilon.

Reference:

Chaowei Ren, et al. Discovery of a Brigatinib Degrader SIAIS164018 with Destroying Metastasis-Related Oncoproteins and a Reshuffling Kinome Profile. J Med Chem. 2021 Jul 8;64(13):9152-9165. doi: 10.1021/acs.jmedchem.1c00373.