(1) Anticancer drugs were coupled through noncleavable linkers to murine mAbs. (2) Evaluations showed that they were only moderately potent and less active than the parent drugs. (3) Examples: KS1/4-methotrexate and BR96-doxorubicin.
(1) Huge improvements in mAbs technology were made, increasing selective binding to tumor cells and reducing crossreactivity with healthy cells. Payloads with smaller molecules were also discovered. (2) Examples: brentuximab vedotin, ado-trastuzumab emtansine, and inotuzumab ozogamicin.
(1) Site-specific conjugation was developed, improving the therapeutic index, stability, and potency. (2) Examples: MEDI4276, vadastuximab talirine, and IMGN779.
