Lorlatinib

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Lorlatinib
Lorlatinib Structure.svg
Clinical data
Routes of
administration
PO
ATC code
Legal status
Legal status
  • experimental
Identifiers
CAS Number
ChemSpider
KEGG
ChEBI
ECHA InfoCard100.245.079 Edit this at Wikidata
Chemical and physical data
FormulaC22H20FN5O2
Molar mass405.433 g·mol−1
3D model (JSmol)

Lorlatinib (PF-6463922) is an anti-neoplastic drug developed by Pfizer. It is an orally-administered small molecule inhibitor of ROS1 and ALK.

In 2015, FDA granted Pfizer orphan drug status for lorlatinib for the treatment of non-small cell lung cancer.[1]

Lorlatinib is able to cross the blood-brain barrier.[2]

Clinical studies[edit]

Several clinical trials are ongoing. A phase II trial comparing avelumab alone and in combination with lorlatinib or crizotinib for non-small cell lung cancer is expected to be complete in late 2017. A phase II trial comparing lorlatinib with crizotinib is expected to be complete in mid-2018.[3] A phase II trial for treatment of ALK-positive or ROS1-positive non-small cell lung cancer with CNS metastases is not expected to be complete until 2023.[4] Preclinical studies are investigating lorlatinib for treatment of neuroblastoma.

In 2017, Pfizer announced that lorlatinib was shown to have activitiy against lung and brain tumors in people with ALK or ROS1 positive advanced non–small cell lung cancer.[5]

In 2018, the FDA approved lortalinib for second or third line treatment of ALK-positive metastatic non-small cell lung cancer.[6]

References[edit]

  1. ^ http://drugspider.com/drug/lorlatinib
  2. ^ "NCI Drug Dictionary". National Cancer Institute.
  3. ^ "A Study Of PF-06463922 An ALK/ROS1 Inhibitor In Patients With Advanced Non Small Cell Lung Cancer With Specific Molecular Alterations - Full Text View - ClinicalTrials.gov".
  4. ^ "A Study of Lorlatinib in Advanced ALK and ROS1 Rearranged Lung Cancer With CNS Metastasis in the Absence of Measurable Extracranial Lesions - Full Text View - ClinicalTrials.gov".
  5. ^ http://www.ascopost.com/News/58148
  6. ^ "FDA approves lorlatinib for second- or third-line treatment of ALK-positive metastatic NSCLC".