Infigratinib (BGJ398): an investigational agent for the treatment of FGFR-altered intrahepatic cholangiocarcinoma

Botrus, Gehan; Raman, Puneet; Oliver, Thomas; Bekaii‐Saab, Tanios

doi:10.1080/13543784.2021.1864320

Cited by 40 publications

(19 citation statements)

References 40 publications

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“…Infigratinib (INF)formerly designated as BGJ398 (Fig. 1), is a highly potent and selective ATP-competitive inhibitor of FGFR1-3 that is currently under clinical investigation for several FGFRdriven cancers (Javle et al, 2018;Botrus et al, 2021). Notably, it has been accorded both orphan drug designation and priority review status by the U.S Food and Drug Administration (FDA) for the treatment of advanced cholangiocarcinomaa rare malignancy plagued with an extremely poor prognosis and limited therapeutic options (Mosconi et al, 2009).…”

Section: Introductionmentioning

confidence: 99%

Infigratinib Is a Reversible Inhibitor and Mechanism-Based Inactivator of Cytochrome P450 3A4

et al. 2021

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Section: Introductionmentioning

confidence: 99%

Infigratinib Is a Reversible Inhibitor and Mechanism-Based Inactivator of Cytochrome P450 3A4

et al. 2021

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“…Infigratinib (NVP-BGJ398/BGJ398) is an orally administered tyrosine kinase inhibitor of the FGFR receptor family. It also shows anti-angiogenic activity and therapeutic potential in the field of oncology: recently, it was pre-registered in Australia/Canada for the treatment of cholangiocarcinoma [ 66 ].…”

Section: Methods Of Treatmentmentioning

confidence: 99%

Advantages and Disadvantages of Different Treatment Methods in Achondroplasia: A Review

Wrobel

Pach

Beń‐Skowronek

2021

IJMS

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Achondroplasia (ACH) is a disease caused by a missense mutation in the FGFR3 (fibroblast growth factor receptor 3) gene, which is the most common cause of short stature in humans. The treatment of ACH is necessary and urgent because untreated achondroplasia has many complications, both orthopedic and neurological, which ultimately lead to disability. This review presents the current and potential pharmacological treatments for achondroplasia, highlighting the advantages and disadvantages of all the drugs that have been demonstrated in human and animal studies in different stages of clinical trials. The article includes the potential impacts of drugs on achondroplasia symptoms other than short stature, including their effects on spinal canal stenosis, the narrowing of the foramen magnum and the proportionality of body structure. Addressing these effects could significantly improve the quality of life of patients, possibly reducing the frequency and necessity of hospitalization and painful surgical procedures, which are currently the only therapeutic options used. The criteria for a good drug for achondroplasia are best met by recombinant human growth hormone at present and will potentially be met by vosoritide in the future, while the rest of the drugs are in the early stages of clinical trials.

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“…The USFDA has also approved antibodies as PKIs such as trastuzumab and bevacizumab. A few anti- [209]. US8552002B2 claims infigratinib and its salts [210].…”

Section: Expert Opinionmentioning

confidence: 99%

“…Infigratinib ( Figure 71 ) is a piperazine based pyrimidine derivative (MF: C 26 H 31 Cl 2 N 7 O 3 . H 3 PO 4 ; MW: 658.47; CAS Number: 1310746-10-1) [ 209 ]. US8552002B2 claims infigratinib and its salts [ 210 ].…”

Section: Summary Of the Patentsmentioning

confidence: 99%

Innovations and Patent Trends in the Development of USFDA Approved Protein Kinase Inhibitors in the Last Two Decades

Imran

Asdaq²,

Khan³

et al. 2021

Pharmaceuticals

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Protein kinase inhibitors (PKIs) are important therapeutic agents. As of 31 May 2021, the United States Food and Drug Administration (USFDA) has approved 70 PKIs. Most of the PKIs are employed to treat cancer and inflammatory diseases. Imatinib was the first PKI approved by USFDA in 2001. This review summarizes the compound patents and the essential polymorph patents of the PKIs approved by the USFDA from 2001 to 31 May 2021. The dates on the generic drug availability of the PKIs in the USA market have also been forecasted. It is expected that 19 and 48 PKIs will be genericized by 2025 and 2030, respectively, due to their compound patent expiry. This may reduce the financial toxicity associated with the existing PKIs. There are nearly 535 reported PKs. However, the USFDA approved PKIs target only about 10–15% of the total said PKs. As a result, there are still a large number of unexplored PKs. As the field advances during the next 20 years, one can anticipate that PKIs with many scaffolds, chemotypes, and pharmacophores will be developed.

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Infigratinib (BGJ398): an investigational agent for the treatment of FGFR-altered intrahepatic cholangiocarcinoma

Cited by 40 publications

References 40 publications

Infigratinib Is a Reversible Inhibitor and Mechanism-Based Inactivator of Cytochrome P450 3A4

Infigratinib Is a Reversible Inhibitor and Mechanism-Based Inactivator of Cytochrome P450 3A4

Advantages and Disadvantages of Different Treatment Methods in Achondroplasia: A Review

Innovations and Patent Trends in the Development of USFDA Approved Protein Kinase Inhibitors in the Last Two Decades

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