Related Experiment Video

Updated: Dec 21, 2025

Scaled-Up Preparation of an Intermediate of Upatinib, ACT051-3
08:36

Scaled-Up Preparation of an Intermediate of Upatinib, ACT051-3

Published on: April 7, 2023

1.4K

A user's guide to lorlatinib

Misako Nagasaka1, Yubin Ge2, Ammar Sukari3

  • 1Karmanos Cancer Institute Wayne State University, Detroit MI, USA; St. Marianna University Graduate School of Medicine, Kawasaki, Japan.

Critical Reviews in Oncology/Hematology
|May 17, 2020
PubMed

Insights

Lorlatinib is a targeted therapy for non-small cell lung cancer with ALK gene rearrangements. This guide reviews its use, efficacy in brain metastases, and managing side effects.

Area of Science:

  • Oncology
  • Pharmacology
  • Genetics

Background:

  • Anaplastic Lymphoma Kinase (ALK) gene rearrangements occur in about 5% of non-small-cell lung cancer (NSCLC).
  • Testing for ALK rearrangements is crucial in metastatic lung adenocarcinoma due to sensitivity to ALK-targeted inhibitors.
  • Resistant ALK mutations, like G1202R, pose a challenge in NSCLC treatment.

Purpose of the Study:

  • To provide a comprehensive review of Lorlatinib, a third-generation ALK and ROS1 inhibitor.
  • To detail Lorlatinib's mechanism of action, pharmacology, and clinical trial data.
  • To offer practical guidance on managing Lorlatinib's adverse events for clinicians and researchers.

Main Methods:

  • Review of existing clinical trial data and pharmacological studies on Lorlatinib.
  • Analysis of Lorlatinib's efficacy, particularly in patients with central nervous system (CNS) metastases.
  • Examination of Lorlatinib's safety profile, including potential toxicities.

Main Results:

  • Lorlatinib demonstrates potent activity against ALK and ROS1, including resistance mutations like G1202R.
  • Excellent CNS penetration and efficacy in patients with intracranial metastases, even after prior therapies.
  • Identified potential toxicities such as neurocognitive effects and hyperlipidemia.

Conclusions:

  • Lorlatinib is an effective third-generation inhibitor for ALK-positive NSCLC, including those with brain metastases.
  • Understanding Lorlatinib's mechanism, efficacy, and adverse events is vital for optimal patient management.
  • This guide serves as a practical reference for healthcare professionals and researchers involved in ALK-targeted therapy.
Keywords:
ALK inhibitorAnaplastic lymphoma kinase rearrangementMechanism of actionPharmacologyToxicity management

More Related Videos

Utilizing 18F-FDG PET/CT Imaging and Quantitative Histology to Measure Dynamic Changes in the Glucose Metabolism in Mouse Models of Lung Cancer06:51

Utilizing 18F-FDG PET/CT Imaging and Quantitative Histology to Measure Dynamic Changes in the Glucose Metabolism in Mouse Models of Lung Cancer

Published on: July 21, 2018

18.4K
Monitoring Hippo Signaling Pathway Activity Using a Luciferase-based Large Tumor Suppressor LATS Biosensor07:16

Monitoring Hippo Signaling Pathway Activity Using a Luciferase-based Large Tumor Suppressor LATS Biosensor

Published on: September 13, 2018

20.5K

Related Concept Videos

Drug Dosage Regimen: Overview01:15

Drug Dosage Regimen: Overview

A drug dosage regimen describes the specific instructions and schedule for administering a drug to a patient. It considers factors such as drug dosage, frequency, route of administration, and duration of treatment. Designing an appropriate dosage regimen for a patient aims to achieve a target drug concentration at the site of action.
Typically, the starting dose and dosing interval are guided by the manufacturer's recommendations based on clinical trials conducted during and after drug...
4.2K
Drug Administration and Therapy Phases: Overview01:26

Drug Administration and Therapy Phases: Overview

Drugs, the chemical agents used in diagnosing, treating, or preventing diseases, undergo a four-phase process of development: pharmaceutic, pharmacokinetics, pharmacodynamics, and therapeutic.
The pharmaceutical phase focuses on leveraging the physicochemical properties of the drug to design and manufacture an effective product. Variants include orally administered tablets or capsules, topical creams or ointments, and parenteral-delivery solutions or emulsions.
The pharmacokinetic phase...
1.1K
Treatment for Pulmonary Arterial Hypertension: Receptor Tyrosine Kinase Inhibitors and Calcium Channel Blockers01:26

Treatment for Pulmonary Arterial Hypertension: Receptor Tyrosine Kinase Inhibitors and Calcium Channel Blockers

Receptor tyrosine kinase inhibitors (TKIs) and calcium channel blockers (CCBs) are two critical categories of drugs employed in the treatment of pulmonary artery hypertension (PAH). PAH is a disease that causes high blood pressure in the pulmonary arteries, resulting in chest pain, fatigue, and shortness of breath.
TKIs, such as imatinib (Gleevec), are particularly effective in tackling the growth and mitogenic factors that become upregulated in PAH patients. These factors contribute to the...
370
Antiasthma Drugs: Leukotriene Modifiers01:19

Antiasthma Drugs: Leukotriene Modifiers

Leukotriene modifiers, or cysteinyl leukotriene receptor antagonists, are medications used to manage chronic asthma. These agents target specific inflammatory mediators produced during arachidonic acid metabolism, an essential process in generating inflammation in the body.
Leukotriene modifiers work through two distinct mechanisms:
1.6K
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against...
8.5K
Routes of Drug Administration: Overview01:22

Routes of Drug Administration: Overview

Drug administration involves delivering drugs to the body through various routes, such as enteral, parenteral, and topical.
Enteral administration refers to drugs absorbed through the gastrointestinal tract. They can be swallowed (perorally), placed under the tongue (sublingually), or on the inner lining of the cheeks (buccally). Perorally administered drugs take time to be absorbed and have a slower onset of action. The rectal route is another form of enteral administration, which allows for...
9.0K