Drug intelligence / Profile preview

177Lu-PSMA-617 + niraparib + abiraterone acetate + prednisone

Development stage
Unknown
Lead developer
Baptist Health South Florida
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Beta-minus Emitters → Radiopharmaceuticals, Gamma Emitters → Radiopharmaceuticals, Small Molecules
Administration
Intravenous, Oral
01

Overview

This investigational combination therapy is being evaluated in the Phase 1/2 LUNAAR trial (NCT05567952) for the treatment of metastatic castration-resistant prostate cancer (mCRPC). The regimen integrates three distinct therapeutic modalities: radioligand therapy with 177Lu-PSMA-617 (Pluvicto), which delivers targeted beta-particle radiation to cells expressing prostate-specific membrane antigen (PSMA); PARP inhibition with niraparib, which disrupts DNA repair mechanisms; and androgen biosynthesis inhibition with abiraterone acetate (administered as a fixed-dose combination with niraparib, known as Akeega). Prednisone is included to manage the mineralocorticoid effects of abiraterone. This multi-pronged approach aims to enhance anti-tumor activity by combining targeted radiation with the inhibition of DNA damage response and androgen receptor signaling pathways. The study is sponsored by Baptist Health South Florida.

Brand names
Akeega
Other names
Lutetium Lu 177 vipivotide tetraxetan + niraparib + abiraterone acetate + prednisone177Lu-PSMA-617 + Niraparib/Abiraterone + Prednisone
02

Targets

CYP17A1 (Steroid 17-alpha-hydroxylase/C17,20 lyase)GR (Glucocorticoid receptor)PARP1 (Poly (adp-ribose) polymerase 1)Pol II (RNA polymerase II elongation factors)PSMA (Prostate-specific membrane antigen)

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