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Table 7 Advances of RET-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

Selpercatinib (LOXO-292)

Retevmo

Eli Lilly and Company

RET

Metastatic RET fusion-positive NSCLC, advanced or metastatic radioactive iodine-refractory thyroid cancer, advanced or metastatic RET-mutant MTC

2020 [227, 228]

1L advanced or metastatic RET fusion-positive NSCLC

III(NCT04194944)

Advanced RET-mutant MTC

III(NCT04211337)

Pralsetinib (BLU-667)

Blueprint Medicines

RET

Advanced RET fusion-positive NSCLC

2020 [127]

RET fusion + solid tumors

I/II [128]

1L advanced RET fusion-positive NSCLC

III (NCT04222972)

  1. In the last column of “Approved years or current phases of clinical trials”: both drugs were approved by Food and Drug Administration (FDA), and we also provided their current phases of clinical trials
  2. NDA new drug application, NSCLC non-small cell lung cancer, MTC medullary thyroid cancer, RET rearranged during transfection
  3. Data source: www.fda.govwww.drugs.com, and www.clinicaltrials.gov (cutoff date: 19 July 2020)