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lorlatinib
- Development stage
- Approved
- Lead developer
- Pfizer
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Lorlatinib is a third-generation small molecule tyrosine kinase inhibitor developed for the treatment of non-small cell lung cancer (NSCLC) that harbors genetic alterations in the anaplastic lymphoma kinase (ALK) gene or ROS1 gene. It works by selectively inhibiting ALK and ROS1 kinases, including many mutated forms that confer resistance to earlier ALK inhibitors. Lorlatinib is notable for its ability to cross the blood-brain barrier, making it effective against brain metastases in NSCLC patients. The drug was developed and is manufactured by Pfizer. It received initial FDA approval in 2018 for use in patients with metastatic ALK-positive NSCLC who have progressed on prior ALK inhibitors.
- Brand names
- LorbrenaLorviqua
- Other names
- lorlatinibPF-06463922PF06463922PF 06463922
02
Targets
LTK (Leukocyte receptor tyrosine kinase)PTK2BROS1 (Proto-oncogene tyrosine-protein kinase ROS)NTRK1 (Tropomyosin-related receptor kinase A)FAK (Focal adhesion kinase)ALK (Anaplastic lymphoma kinase receptor tyrosine kinase)NTRK2 (Tropomyosin-related kinase receptor type B)FES (Proto-oncogene tyrosine-protein kinase Fes)NTRK3 (Tropomyosin receptor kinase C)FER (FER tyrosine kinase)TNK2 (Activated Cdc42-associated kinase 1)
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