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Table 11 Advances of KIT/PDGFR-TKIs

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

Drug

Brand name

Manufacturer

Targets

Applications of diseases

Approval year or current phase of clinical trials

Imatinib

Gleevec

Novartis Oncology

Bcr-Abl, KIT, PDGFR

Advanced Philadelphia chromosome positive chronic myeloid leukemia

2001

1L KIT + unrectable or metastatic GIST

2002

Other hematological cancer

 

Sunitinib

Sutent

Pfizer Inc

KIT, PDGFR, VEGFR1-2, FLT3

GIST after disease progression on or intolerance to imatinib

2006 [172]

Regorafenib

Stivarga

Bayer

KIT, PDGFR, VEGFR1-3, TIE2, FGFR, BRAF, RET

Locally advanced, unresectable, or metastatic GIST previously treated with imatinib and sunitinib

2013 [173]

Avapritinib

Ayvakit

Blueprint Medicines

KIT, PDGFR

Unresectable or metastatic GIST harboring PDGFRA exon 18 mutation

2020 [176]

 ≥ 4L and PDGFRA exon 18 mutant GIST

I [176]

Locally advanced unresectable or metastatic GIST who previously received imatinib and 1 or 2 other TKIs

III (NCT03465722)

Ripretinib (DCC-2618)

Qinlock

Deciphera

KIT, PDGFR

Advanced GIST who have received prior treatment with 3 or more TKIs including imatinib

2020 [177]

 Advanced GIST after disease progression on or intolerance to imatinib

III (NCT03673501)

Investigational drugs

 PLX-9486

Plexxikon

KIT

Combined with pexidartinib for KIT + GIST

[179]

  1. In the last column of “Approval 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); if a drug is under investigation, we provided current phases of its clinical trials
  2. GIST Gastrointestinal stromal tumor, TKIs tyrosine kinase inhibitors, PDGFR platelet-derived growth factor receptor
  3. Data source: www.fda.govwww.drugs.com, and www.clinicaltrials.gov (cutoff date: 19 July 2020)