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Table 1 Targets and phase of clinical development of ALK inhibitors

From: Role and targeting of anaplastic lymphoma kinase in cancer

Drug

Targets

Phase of clinical development

References

Crizotinib

ALK

c-MET

ROS1

Indication worldwide for therapy of NSCLC harbouring ALK gene rearrangement in first and second line

• Shaw AT, et al. NEJM 2013 [32]

• Solomon BJ, et al. NEJM 2014 [33]

Alectinib

ALK, including ALK secondary mutationsRET

- Approval from FDA (December 2015) and EMA (February 2017) in second line therapy of NSCLC harbouring ALK gene after progression to crizotinib

- FDA granted fast approval in first line setting based on results of phase II and III clinical trials

• Larkins E, et al. CCR 2016 [52]

• Shaw AT, et al. Lancet Oncol 2016 [56]

• Hida T, et al. Lancet 2017 [59]

• Peters S, et al. NEJM 2017 [60]

Ceritinib

ALK, including ALK secondary mutations

IGF-1R

ROS1

STK22D

- Recent fast approval from FDA in second line therapy of NSCLC harbouring ALK gene after progression to crizotinib (May 2017) based on results of phase II clinical trials

• Crinò L, et al. JCO 2016 [48]

• Shaw AT, et al. JTO 2016 [47]

Brigatinib

ALK, including ALK secondary mutations

ROS1

EGFR

NTRK1

- Recent fast approval from FDA in second line therapy of NSCLC harbouring ALK gene after progression to crizotinib (April 2017) based on results of phase II clinical trials

• Markham A, et al. Drugs 2017 [61]

Lorlatanib

ALK and ROS1, including all known their mutant forms

Ongoing phase III trials in NSCLC first line versus crizotinib

ClinicalTrials.gov, NCT03052608

Entrectinib

ALK, Including ALK secondary mutations

NTRK1, 2, and 3

ROS1

Ongoing phase II basket trial

STARTRK-2 (NCT02568267)

• Drilon A, et al. Cancer Discovery 2017 [63]