Antibody-drug conjugate (ADC) in clinical application (Approved/BLA, phaseI/II/III)

There are currently 82 novel ADCs in 150 active clinical trials registered with clinicaltrials.gov for cancer patients. Most of the ADCs are currently under investigation in phase 1 trials, while a small percentage has advanced to phase 3. Of the 150 ongoing trials, more than 80% are evaluating ADC safety and efficacy in solid tumors whereas less than 20% are trials for hematological malignancies. There are 43 disclosed targets organized here by the number of ADCs designed to recognize them. Most of these targets are under evaluation by a single ADC, while some are being investigated by several different ADCs. Of the 82 novel ADCs, followed by DNA-damaging molecules, topoisomerase I inhibitors, and finally unique payloads such as TLR agonists, a BCL2-xL inhibitor, and an RNA polymerase II inhibitor. Many payloads can’t be disclosed. Most ADCs under clinical investigation either utilize the conventional cysteine conjugation strategy or site-specific conjugation linker while few conjugate to surface lysines. 2