Developing targeted theranostics for the detection and treatment of cancer and other diseases

e are a group of scientists and physicians working at Memorial Sloan Kettering Cancer Center. Our goal is the development of new targeted pharmaceuticals for medical diagnosis and/or therapy, or “theranositcs.” Through our research, we identify cancer or disease biomarkers and develop molecular agents to target them. Targeting probes we have utilized include nanoparticles, small molecule drugs, peptides, and antibodies. We chemically couple these molecular targeting probes to imaging agents such as medical radionuclides or optical fluorophores to enable non-invasive patient imaging of disease, and/or to drugs or other therapeutic payloads to deliver pharmaceuticals to the target site of disease.

ur ultimate goal is to translate these new agents into clinical use. Through our efforts and collaborations, we have been involved with first-in-human studies for novel PET tracers in clinical trials.

Kishore Pillarsetty is an Attending in Department of Radiology and serves as the Director of Preclinical Radiochemistry and Training in the Department of Radiology at MSK. He also holds joint appointment as a Professor of Radiochemistry and Radiopharmacy in Radiology at Weill Cornell Medicine. His laboratory broadly focusses on the development of molecularly targeted diagnostic agents based on radiopharmaceuticals and optical imaging agents that can serve as tools to understand the biology of the system. Leveraging the knowledge gained on biological drivers and markers, companion therapeutic agents are also being developed in his laboratory. Dr. Pillarsetty obtained his bachelor’s degree in Mathematics, Physics and Chemistry from Osmania University; master’s degree in Chemistry from University of Hyderabad and PhD in Chemistry from University of Missouri-Columbia. He performed his post-doctoral training under the mentorship of Drs. Ron Blasberg and Ron Finn at MSK before his appointment in the Department of Radiology.

Biomarkers of cancer include the PARP family of DNA repair enzymes. One particular member of this family, PARP1, has been targeted with inhibitor drugs as a cancer treatment. However, PARP inhibitor drugs can also be modified with fluorescent or radioactive groups. Because PARP1 enzymes are often present in higher levels in the nuclei of cancer cells, labeled inihibitors of PARP1 can also function as agents for cancer detection. We are developing derivatives of these drugs coupled to fluorescent molecules and radiotracers for the detection and monitoring of cancer.