The Naga Vara Kishore Pillarsetty Lab

Targeted Theranostics Laboratory

Molecularly targeted therapy modulates a dysregulated target(s) and/or biologic pathway(s) that provides survival advantage for cancer cells. This targeting enables achieve selective destruction of cancer cells while minimizing harm to normal cells. We work on the development and clinical translation of molecular imaging and therapeutic agents that can 1) identify dysregulated pathways noninvasively; 2) serve as prognostic indicators of response and/or monitor response to therapy; 3) aid in understanding drug pharmacokinetics; and 4) take advantage of target overexpression to develop companion radiotherapeutics. The molecular imaging agent can be a small molecule, peptide, antibody, or a nanoparticle and conjugated to a radioactive or optically active or therapeutic payload depending on the intended application. We have leveraged targets such as PSMA, epichaperome, PARP, Na_V1.7, and GLP1R to develop targeted theranostics. By collaborating with other laboratories and clinicians at Memorial Sloan Kettering Cancer Center, we have been able to translate several molecular imaging agents for first-in-human studies;  These include epichaperome-specific PET probes [¹²⁴I]-PU-H71 (Pillarsetty et al. 2019, NCT01269593, NCT01393509) and ^[124I]-PU-AD (Bolaender et al. 2021, NCT03371420), PARP-specific fluorescent intraoperative probe PARPi-FL (Kossatz et al 2020, NCT03085147), and several other PET probes that have entered clinical trials at MSKCC. In addition, we are actively exploring new targets that include mucins, ATM, ATR, DLL3 etc. to develop novel targeted theranostics.