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[177Lu]Lu-NeoB + ribociclib + fulvestrant

Development stage
Unknown
Lead developer
Advanced Accelerator Applications
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous ([177Lu]Lu-NeoB), Oral (ribociclib), Intramuscular (fulvestrant)
01

Overview

**[177Lu]Lu-NeoB + ribociclib + fulvestrant** is a multi-agent combination therapy comprising three agents: - **[177Lu]Lu-NeoB**: A radiopharmaceutical targeting the gastrin-releasing peptide receptor (GRPR), delivering the beta-emitter lutetium-177 to GRPR-expressing tumors for targeted radioligand therapy[1][3][5]. - **Ribociclib**: An orally available selective small molecule inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), used primarily in hormone receptor-positive, HER2-negative advanced breast cancer by blocking cell cycle progression[2][4][6]. - **Fulvestrant**: A selective estrogen receptor degrader (SERD), antagonizing the estrogen receptor and leading to its degradation, used in hormone receptor-positive advanced breast cancer[2][4]. This specific triple combination does not appear to be standard or widely studied in clinical trials together. Each component is known for its efficacy in solid tumors: [177Lu]Lu-NeoB is investigational for various cancers with GRPR expression, ribociclib plus fulvestrant is approved for HR+/HER2- advanced breast cancer, and fulvestrant is a standard endocrine therapy. The combination would theoretically provide targeted radiotherapy, cell cycle arrest, and endocrine blockade.

Brand names
Kisqali
Other names
Lutetium-177 NeoBLutetium177 NeoBLutetium 177 NeoB[177Lu]Lu-NeoBribociclib succinatefulvestrant acetate
02

Targets

CDK6 (Cyclin-dependent kinase 6)GRPR (Gastrin-releasing peptide receptor)ER (Estrogen receptor)CDK4 (Cyclin-dependent kinase 4)

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