Drug intelligence / Profile preview

ceritinib + luminespib

Development stage
Phase 1
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Ceritinib + luminespib is an investigational combination drug regimen consisting of two small molecule inhibitors: ceritinib, an oral selective inhibitor of anaplastic lymphoma kinase (ALK), and luminespib, an intravenous inhibitor of heat shock protein 90 (Hsp90). This combination was explored in clinical trials for the treatment of adults with ALK-rearranged non-small cell lung cancer (NSCLC), particularly in patients resistant to prior ALK inhibitors. Ceritinib blocks ALK kinase signaling crucial for tumor cell survival, while luminespib inhibits Hsp90 chaperone activity, promoting degradation of oncogenic client proteins including ALK fusion proteins. The combination sought to overcome resistance to targeted monotherapy in ALK-driven NSCLC. Despite initial scientific rationale and tolerability in some dosing regimens, the combination showed limited efficacy and had a challenging safety profile, leading to early termination of clinical investigation[1][5].

Other names
ceritinib + luminespib
02

Targets

ALK (Anaplastic lymphoma kinase receptor tyrosine kinase)HSP90AA1 (Heat shock protein HSP90-alpha)INSR (Insulin receptor)IGF-1R (Insulin-like growth factor 1 receptor)TSSK1B (Testis-specific serine/threonine-protein kinase 1B)

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