Drug intelligence / Profile preview

NXP900 + lorlatinib

Development stage
Unknown
Lead developer
Nuvectis Pharma
Modality
Small Molecules
Administration
Oral
01

Overview

NXP900 + Lorbrena (lorlatinib) is a combination therapy under clinical development by Nuvectis Pharma for the treatment of advanced, anaplastic lymphoma kinase (ALK)-positive non-small cell lung cancer (NSCLC). NXP900 is a first-in-class, highly selective oral small-molecule inhibitor of the SRC family of kinases (SFKs), specifically targeting SRC and YES1. Unlike traditional multi-kinase inhibitors that bind SRC in its active 'open' conformation, NXP900 locks the kinase in its native inactive 'closed' conformation (Type 1.5 inhibition), thereby blocking both its catalytic activity and scaffolding functions. Lorbrena (lorlatinib), developed by Pfizer, is an FDA-approved third-generation ALK tyrosine kinase inhibitor. The combination is designed to overcome acquired resistance to ALK inhibitors, which often arises through bypass signaling pathways mediated by SFK activation, YES1 amplification, and YAP1 nuclear localization. By simultaneously inhibiting ALK and the SRC/YES1/YAP1 bypass pathway, this combination aims to prevent or reverse resistance and improve clinical outcomes in patients with ALK-positive NSCLC who have progressed on prior ALK inhibitor therapies.

Other names
Lorbrena + NXP 900Lorbrena + NXP900Lorbrena + eCF506NXP 900 + LorbrenaNXP 900 + lorlatinibNXP900 + LorbrenaNXP900 + PF-06463922NXP900 + lorlatinibPF-06463922 + NXP900PF-06463922 + eCF506eCF506 + LorbrenaeCF506 + PF-06463922eCF506 + lorlatiniblorlatinib + eCF506lorlatinib + NXP 900lorlatinib + NXP900
02

Targets

ALK (Anaplastic lymphoma kinase receptor tyrosine kinase)SRC (Proto-oncogene tyrosine-protein kinase Src)YES1 (YES proto-oncogene 1 tyrosine kinase)

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