2012
DOI: 10.1158/1535-7163.mct-11-0450
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Ponatinib (AP24534), a Multitargeted Pan-FGFR Inhibitor with Activity in Multiple FGFR-Amplified or Mutated Cancer Models

Abstract: Members of the fibroblast growth factor receptor family of kinases (FGFR1-4) are dysregulated in multiple cancers. Ponatinib (AP24534) is an oral multitargeted tyrosine kinase inhibitor being explored in a pivotal phase II trial in patients with chronic myelogenous leukemia due to its potent activity against BCR-ABL. Ponatinib has also been shown to inhibit the in vitro kinase activity of all four FGFRs, prompting us to examine its potential as an FGFR inhibitor. In Ba/F3 cells engineered to express activated … Show more

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Cited by 295 publications
(228 citation statements)
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References 46 publications
(77 reference statements)
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“…Furthermore, it has been shown to be a potent pan-FGFR inhibitor in preclinical assays. Remarkably, it was able to inhibit in vitro cell proliferation and signaling in various cell lines characterized either by FGFR amplifi cations or activating mutations ( 81 ). These recent data highlight the rationale to investigate ponatinib as a potential treatment for FGFR-driven solid tumors as well.…”
Section: Reviewmentioning
confidence: 81%
“…Furthermore, it has been shown to be a potent pan-FGFR inhibitor in preclinical assays. Remarkably, it was able to inhibit in vitro cell proliferation and signaling in various cell lines characterized either by FGFR amplifi cations or activating mutations ( 81 ). These recent data highlight the rationale to investigate ponatinib as a potential treatment for FGFR-driven solid tumors as well.…”
Section: Reviewmentioning
confidence: 81%
“…Moreover, an in vitro study has been analyzing the possibility of using Ponatinib in cancer cell lines of endometrial, bladder, gastric, breast, lung and colon cancer harboring FGFR1-4 alterations. The results are very promising since Ponatinib shows specific activity against the four receptors and it seems to work like a FGFR-pan-inhibitor (Gozgit et al, 2012). Currently, they are trying to discover novel Ponatinb anologues to reduce kinase insert domain receptor (KDR) activities (Yang et al, 2017) (I would delete this sentence).…”
Section: Ponatinibmentioning
confidence: 99%
“…Among them, regorafenib is a novel orally active multitarget compound that inhibits a number of pro-angiogenic TK receptors, including FGFR1, VEGFR2, TIE2, and PDGFR [143]; nintedanib (BIBF1120) interferes with VEGFR, PDGFR and FGFR pathways [144]; ponatinib (AP24534), mainly active on BCR-ABL, has been described to exert an anti-FGFR activity in vitro [145]. Several other small molecules, including axitinib, brivanib, cabozantinib, dovotinib, oratinib, pazopamib, sorafenib, sunitinib and vandetanib are endowed with this non-selective TKI profile (see Refs.…”
Section: Inhibition Of Signal Transduction Triggered By Fgfr Activationmentioning
confidence: 99%