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Table 2 Advances of ALK/ROS1-TKIs

From: Tyrosine kinase inhibitors for solid tumors in the past 20 years (2001–2020)

Drug

Brand name

Manufacturer

Targets

Applications of diseases

Approved years or current phases of clinical trials

Crizotinib

Xalkori

Pfizer Inc

ALK, ROS1, MET

Locally advanced or metastatic ALK + NSCLC

2011 [50]

Metastatic ROS1 + NSCLC

2016 [67]

Advanced METex14 + or MET-amplified NSCLC

ongoing [134, 135]

Alectinib

Alecensa

Genentech Inc

ALK

Unresectable, advanced or recurrent ALK + NSCLC

2014§

2L metastatic ALK + NSCLC, 1L metastatic ALK + NSCLC

2015,  2017 [55, 56]

Ceritinib

Zykardia

Novartis

ALK, ROS1

2L metastatic ALK + NSCLC

2014

1L metastatic ALK + NSCLC

2017 [198]

Advanced ROS1 + NSCLC

II [199]

Brigatinib

Alunbrig

Takeda

ALK

2L metastatic ALK + NSCLC

2017

1L metastatic ALK + NSCLC

2020 [58, 59]

Combined with cetuximab for EGFR/T790M/cis-C797S NSCLC

[43]

Ensartinib

-

Beta/Xcovery Holdings Inc

ALK

2L metastatic ALK + NSCLC

2019 a priority review by NMPA [52]

Entrectinib

Rozlytrek

Genentech Inc

ROS1, TRK, ALK

Metastatic ROS1 + NSCLC

2019 [68]

TRK fusion + solid tumors

2019 [200]

Lorlatinib

Lorbrena

Pfizer Inc

ALK, ROS1

 2-3L metastatic ALK + NSCLC

2018§ [64]

Investigational drugs

Repotrectinib

-

Turning Point

ROS1, TRK, ALK

Advanced ROS1 + NSCLC

I [70]

DS-6051b

-

Daiichi Sankyo

ROS1, TRK

ROS1 + NSCLC

I [72]

TRK + /ROS1 + solid tumors

I [201]

WX-0593

-

Qilun

ALK, ROS1

ALK + or ROS1+ NSCLC

I [61]

CT-707

-

Centaurus

ALK, FAK, Pyk2

2L advanced ALK + NSCLC

I [62]

CT-3505

-

Shouyao Holdings

ALK

ALK + NSCLC

I (ChiCTR1900025619)

  1. In the last column of “Approved years or current phases of clinical trials”, if a drug has been approved, we provided data of the year of its approval by Food and Drug Administration (FDA), except alectinib and lorlatinib with a superscript “§” which means they were firstly approved by Ministry of Health, Labor and Welfare (MHLW); if a drug is under investigation, we provided current phases of its clinical trials
  2. FAK focal adhesion kinase, Pyk2 proline-rich tyrosine kinase-2, EMA European Medicines Agency, NMPA National Medical Products Administration, ALK anaplastic lymphocyte kinase, ROS1 ROS proto-oncogene 1
  3. Data source: www.fda.govwww.drugs.com, and www.clinicaltrials.gov (cutoff date: 19 July 2020)