Drug intelligence / Profile preview

[18F]PARPi

Development stage
Phase 2
Lead developer
Ariceum Therapeutics
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Positron Emitters → Radiopharmaceuticals, Small Molecules
Administration
Intravenous
01

Overview

[18F]PARPi is a fluorine‑18 labeled small molecule radiopharmaceutical designed as a positron emission tomography (PET) imaging agent for in vivo visualization of poly(ADP-ribose) polymerase 1 (PARP1). It is structurally based on the olaparib scaffold, with a 2H-phthalazin‑1-one core conjugated to a [^18F]-fluorobenzoic acid moiety. The compound binds specifically and with high affinity to PARP1, enabling non-invasive imaging of PARP expression and activity in tumors. Preclinical studies have demonstrated its favorable pharmacokinetics, high specificity for PARP1-expressing cells, and good stability in vivo. Its primary clinical application under investigation is as an imaging biomarker for brain tumors such as glioblastoma multiforme and other solid tumors expressing elevated levels of PARP1[1][2][5].

Other names
1(2H)-phthalazinone, 4-((4-fluoro-3-((4-(4-(fluoro-18f)benzoyl)-1-piperazinyl)carbonyl)phenyl)methyl)-ATD 001ATD001ATD-001BDC-003BDC003BDC 003F‑18 PARP
02

Targets

PARP1 (Poly (adp-ribose) polymerase 1)PARP2 (Poly (adp-ribose) polymerase 2)

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