Literature DB >> 28431340

First macrocyclic 3rd-generation ALK inhibitor for treatment of ALK/ROS1 cancer: Clinical and designing strategy update of lorlatinib.

Sulman Basit1, Zaman Ashraf2, Kwangho Lee3, Muhammad Latif4.   

Abstract

Non-small cell lung cancers (NSCLC) harboring anaplastic lymphoma kinase (ALK) gene rearrangements invariably develop resistance to 2nd-generation ALK inhibitors. Lorlatinib (PF-06463922) (6) is a 3rd-generation macrocyclic ALK-TKI that demonstrates many advantages over 2nd-generation ALK inhibitors. Lorlatinib has demonstrated decent kinase selectivity, promising pharmacokinetic profile, selective brain-penetration and strong antiproliferative activity in several ALK/ROS1-driven tumor models. The current review describes the activity spectrum, key events from discovery to clinical applications and the evidences that lorlatinib acts as an ALK/ROS1 inhibitor in clinical settings.
Copyright © 2017 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  Loratinib in phase II clinical trial; Lorlatinib third generation ALK/ROS1 inhibitor; Macrocyclic ALK inhibitor

Mesh：

Substances：

Year:  2017        PMID： 28431340     DOI： 10.1016/j.ejmech.2017.04.032

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN： 0223-5234            Impact factor:   6.514


  18 in total

1.  Macrocycle modeling in ICM: benchmarking and evaluation in D3R Grand Challenge 4.

Authors:  Polo C-H Lam; Ruben Abagyan; Maxim Totrov
Journal:  J Comput Aided Mol Des       Date:  2019-10-09       Impact factor: 3.686

Review 2.  New generation anaplastic lymphoma kinase inhibitors.

Authors:  Angelo Delmonte; Marco Angelo Burgio; Alberto Verlicchi; Giuseppe Bronte; Paola Cravero; Paola Ulivi; Giovanni Martinelli; Lucio Crinò
Journal:  Transl Lung Cancer Res       Date:  2019-11

Review 3.  Latest perspectives of orally bioavailable 2,4-diarylaminopyrimidine analogues (DAAPalogues) as anaplastic lymphoma kinase inhibitors: discovery and clinical developments.

Authors:  Muhammad Latif; Zaman Ashraf; Sulman Basit; Abdul Ghaffar; Muhammad Sohail Zafar; Aamer Saeed; Sultan Ayoub Meo
Journal:  RSC Adv       Date:  2018-05-04       Impact factor: 4.036

Review 4.  Targeting ALK Rearrangements in NSCLC: Current State of the Art.

Authors:  Ling Peng; Liping Zhu; Yilan Sun; Justin Stebbing; Giovanni Selvaggi; Yongchang Zhang; Zhentao Yu
Journal:  Front Oncol       Date:  2022-04-06       Impact factor: 5.738

Review 5.  Small molecules in targeted cancer therapy: advances, challenges, and future perspectives.

Authors:  Lei Zhong; Yueshan Li; Liang Xiong; Wenjing Wang; Ming Wu; Ting Yuan; Wei Yang; Chenyu Tian; Zhuang Miao; Tianqi Wang; Shengyong Yang
Journal:  Signal Transduct Target Ther       Date:  2021-05-31

6.  Long-term progression-free survival in an advanced lung adenocarcinoma patient harboring EZR-ROS1 rearrangement: a case report.

Authors:  Liang Dong; Jingwen Xia; Jing Zhang; Yuanyuan Zhang; Ning Zhu; Peng Zhang; Youzhi Zhang; Xiujuan Zhang; Shengqing Li
Journal:  BMC Pulm Med       Date:  2018-01-23       Impact factor: 3.317

Review 7.  Entrectinib and other ALK/TRK inhibitors for the treatment of neuroblastoma.

Authors:  Holly L Pacenta; Margaret E Macy
Journal:  Drug Des Devel Ther       Date:  2018-10-23       Impact factor: 4.162

8.  From crizotinib to lorlatinib: continuous improvement in precision treatment of ALK-positive non-small cell lung cancer.

Authors:  Robert Pirker; Martin Filipits
Journal:  ESMO Open       Date:  2019-09-08

9.  Three-Component Cascade Reaction of 1,1-Enediamines, N,N-Dimethylformamide Dimethyl Acetal, and 1,3-Dicarbonyl Compounds: Selective Synthesis of Diverse 2-Aminopyridine Derivatives.

Authors:  Quan-Xing Zi; Sheng-Jiao Yan; Chang-Long Yang; Kun Li; Jun Lin
Journal:  ACS Omega       Date:  2019-02-07

Review 10.  Mechanisms of drug resistance mediated by long non-coding RNAs in non-small-cell lung cancer.

Authors:  Manuela La Montagna; Lucy Ginn; Michela Garofalo
Journal:  Cancer Gene Ther       Date:  2020-08-25       Impact factor: 5.987
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