Drug intelligence / Profile preview

PEG-talazoparib

Development stage
Preclinical
Lead developer
ProLynx
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

PEG-talazoparib (PLX376) is a long-acting prodrug of talazoparib, a potent poly(ADP-ribose) polymerase (PARP) inhibitor. It is designed for intravenous administration, potentially every two weeks, to maintain therapeutic levels of talazoparib within its known therapeutic window. The drug is being developed by ProLynx for oncology indications. Its mechanism of action involves the active component, talazoparib, which inhibits PARP enzymes, particularly PARP1 and PARP2. This inhibition leads to the trapping of PARP on damaged DNA, interfering with DNA repair processes and ultimately causing cell death, especially in cancer cells with homologous recombination deficiencies, such as those with BRCA1/2 mutations.

02

Targets

MRP (Multidrug resistance-associated protein family)ABCG2 (Breast cancer resistance protein)PARP2 (Poly (adp-ribose) polymerase 2)

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