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Targeted Therapy

Targeted therapy for prostate cancer is a type of therapy that identifies, or “targets”, a particular genetic mutation in the tumor. The goal is to interfere with the specific molecules that drive the growth of the tumor. A targeted therapy approach is a form of personalized cancer treatment, or precision medicine, and is oftentimes associated with fewer side effects than other treatments. Targeted therapies may be used by themselves or in combination with other therapies.

To better understand precision medicine and targeted prostate cancer treatments, view, download, or print the document below:

Precision Medicine in Prostate Cancer

PARP Inhibitors

PARP inhibitors are a type of targeted therapy for prostate cancer. They target mutations in the BRCA genes (BRCA1 and BRCA2), therefore are only used in patients who are known to have a mutation in their BRCA gene. 

In 2020, two oral medications that are part of an exciting class of drugs called PARP inhibitors were approved by the FDA for treatment of certain types of advanced prostate cancer. PARP inhibitors affect how DNA is repaired in cancer cells. Previously, PARP inhibitors were approved to treat women with certain breast, ovarian, and pancreatic cancers.

How do PARP inhibitors work?

There are two major ways to repair DNA damage in cells. If one fails, the other can make up the difference. PARP inhibitors interrupt (or prevent) one DNA repair system from working. Cells with mutations like BRCA1 and BRCA2 have a decreased ability to repair DNA damage in the second system. If both ways to repair the DNA in a tumor cell are stopped, DNA damage adds up and that causes the tumor cells to die.

Watch ZERO’s President and CEO, Jamie Bearse discuss new prostate cancer treatment news (5/29/2020)

PSMA-Targeted Therapies

PSMA, or prostate-specific membrane antigen, is a protein found on the surface of normal prostate cells. It is found in higher amounts on prostate cancer cells. It is present in more than 80% of prostate cancer cells in men with prostate cancer. PSMA has been the subject of extensive and promising research over the last several decades. It is now used as a target for imaging to diagnose metastatic or recurrent prostate cancer, and it is also being explored as a target for medications that can treat prostate cancer.

How is PSMA targeted for treating prostate cancer?

Targeting PSMA enables treatment to focus on the prostate cancer cells rather than healthy cells in the body. This allows a precision medicine approach to treatment. PSMA treatments will likely be made available to patients who have high levels of PSMA protein detected on their cancer cells using a PSMA PET scan.

Lutetium Lu 177 vipivotide tetraxetan (Pluvicto®), also know as Lu-PSMA, is a PSMA-targeted Radioligand Therapy (RLT) approved by the FDA in 2022 to treat metastatic castration-resistant prostate cancer (mCRPC). Several PSMA-targeted therapies are being explored for prostate cancer, including other radioligand therapies, antibody-drug conjugates, cellular immunotherapy, photodynamic therapy, imaging-guided surgery, and others.



  1. https://www.nature.com/articles/s41391-021-00394-5#:~:text=1%3A%20Tumor%20therapies%20targeting%20PSMA,and%20ultrasound%2Dmediated%20nanobubble%20destruction
  2. https://www.targetedonc.com/view/psma-directed-therapies-and-diagnostics-expand-their-scope-in-prostate-cancer