Drug intelligence / Profile preview

fluzoparib + iodine-125

Development stage
Unknown
Lead developer
Hengrui Pharmaceutical
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Oral, Interstitial
01

Overview

Fluzoparib + iodine-125 is a combination therapy regimen currently under investigation for the treatment of advanced unresectable soft tissue sarcoma. Fluzoparib is an orally bioavailable small molecule inhibitor of poly (ADP-ribose) polymerase (PARP) 1 and 2, enzymes that play a critical role in the repair of single-strand DNA breaks. By inhibiting these enzymes, fluzoparib prevents the repair of DNA damage, leading to the accumulation of double-strand breaks and subsequent cell death, particularly in tumors with existing DNA repair deficiencies. In this specific clinical context, fluzoparib is utilized as a radiosensitizer to enhance the therapeutic efficacy of iodine-125 (125I) radioactive seed implantation (brachytherapy). The 125I seeds provide continuous, localized, low-dose-rate radiation directly to the tumor site. The combination aims to synergistically increase DNA damage and inhibit repair mechanisms, thereby improving local tumor control in patients with inoperable sarcomas. This approach is being evaluated in Phase II clinical trials led by investigator Fujun Zhang.

Brand names
AiRuiYi
Other names
fluzoparib hydrochloride125I brachytherapyRadioactive iodine-125 seeds
02

Targets

PARP2 (Poly (adp-ribose) polymerase 2)

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