Drug intelligence / Profile preview

PEN-866 + niraparib

Development stage
Unknown
Lead developer
Tarveda Therapeutics
Modality
Peptide-Drug Conjugates → Peptide Conjugates → Peptides, Small Molecules
Administration
Intravenous, Oral
01

Overview

**PEN-866 + niraparib** is an investigational combination therapy featuring two components. PEN-866 is a miniature drug conjugate comprising a camptothecin payload linked to a targeting molecule, typically designed to deliver cytotoxic activity to tumors, while niraparib is a small molecule inhibitor of poly(ADP-ribose) polymerase (PARP), a DNA repair enzyme. The combination is intended to leverage DNA damage from camptothecin delivered by PEN-866 and potentiate its effect by inhibiting repair via PARP blockade from niraparib. This approach aims to enhance antitumor efficacy, particularly in cancers with homologous recombination repair deficiencies or increased sensitivity to DNA damage.

Other names
PEN-866PEN866PEN 866niraparib
02

Targets

PARP1 (Poly (adp-ribose) polymerase 1)HSP90AA1 (Heat shock protein HSP90-alpha)TOP1 (DNA Topoisomerase I)

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