Drug intelligence / Profile preview

fulvestrant + ribociclib + spartalizumab

Development stage
Discontinued
Lead developer
Novartis
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intramuscular, Intravenous
01

Overview

This is a combination therapy consisting of fulvestrant (an estrogen receptor antagonist), ribociclib (a CDK4/6 inhibitor), and spartalizumab (a PD-1 inhibitor). The combination was investigated in a phase I clinical trial for patients with hormone receptor (HR)-positive/HER2-negative metastatic breast cancer. The therapy showed limited efficacy with only two confirmed partial responses (13.3%) observed. However, the combination demonstrated elevated hepatotoxicity, with grade 3-4 hypertransaminasemia occurring in 46.7% (AST) and 40.0% (ALT) of patients, which ultimately precluded further development of this specific combination.

02

Targets

CDK4 (Cyclin-dependent kinase 4)ESR1 (ERα)ESR2 (ERβ)CDK6 (Cyclin-dependent kinase 6)PDCD1 (Programmed cell death protein 1 receptor)

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