TABLE 1.
The four FDA approved PARP inhibitors.
| Mechanism of action | ||||
|---|---|---|---|---|
| Brand name | Manufacture | Catalytic inhibition (PARP1)* | Trapping* | |
| Niraparib | ZEJULA | Merck/Tesaro/GSK | Yes (+) | Yes (3X) |
| Olaparib | LYNPARZA | KuDOS Pharmaceutical/AstraZeneca | Yes (++) | Yes (1X) |
| Rucaparib | RUBRACA | Agouron Pharmaceuticals/Clovis Oncology | Yes (+++) | Yes (1X) |
| Talazoparib | TALENNA | LEAD Therapeutics/Pfizer | Yes (++++) | Yes (100X) |
Notes: “+” signs indicate the qualitative potency of inhibiting the enzymatic activity of PARP1. “1X, 3X, and 100X” indicates the relative potency of trapping PARP1 on DNA.
*Rudolph, J.; Jung, K.; Luger, K., Inhibitors of PARP: Number crunching and structure gazing. Proc Natl Acad Sci U S A 2022, 119 (11), e2121979119.