Effects of futibatinib: A Synthesis of Findings from 21 Studies

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Original Abstract of the Article

Major research findings

Futibatinib is a covalent FGFR1-4 inhibitor that has been shown to be effective in treating patients with advanced intrahepatic cholangiocarcinoma harboring FGFR2 gene fusions/rearrangements. 4 . It was approved by the US Food and Drug Administration (FDA) for this indication. 4 . Futibatinib is also effective against a broad spectrum of tumors, including cholangiocarcinoma, gastric, urothelial, central nervous system, head and neck, and breast cancer. 13 . It has shown to be particularly effective in patients with FGFR2 aberrations, including fusions, rearrangements, and copy number gains. 2 . In patients with FGFR2 fusions, futibatinib showed an overall response rate (ORR) of 42% and a median duration of response (DoR) of 9.7 months. 7 . Additionally, futibatinib demonstrates efficacy in overcoming FGFR1 mutant resistance in vitro and in vivo. 16 . This is significant because many FGFR inhibitors are ineffective against these mutations. 16 . Several studies evaluated the pharmacokinetics of futibatinib in healthy subjects and patients with different liver function impairments. Futibatinib was rapidly absorbed, with a median time to peak drug concentration of 1.0 hour. 6 . Futibatinib is mainly eliminated through feces, with minimal urinary excretion. 6 . No clinically relevant changes in futibatinib pharmacokinetics were observed in subjects with mild, moderate, or severe hepatic impairment. 4 . This suggests that dose adjustments are not necessary in patients with hepatic impairment. 4 . Futibatinib's effect on cardiac repolarization was also studied in healthy subjects. The study found that futibatinib did not prolong QTc interval at therapeutic or supratherapeutic doses. 10 . The study described in 12 investigated the role of Grb2 and PLCγ1 in BCR-FGFR1-driven cell proliferation. It was found that BCR-FGFR1 requires both Grb2 and PLCγ1 binding partners for cell proliferation. 12 . This suggests that targeting these interactions might be a promising therapeutic strategy. 12 .

Benefits and risks

Benefit summary

Futibatinib shows promise as a treatment for various types of cancer, particularly those with FGFR2 aberrations. 13 , 7 , 2 . It is well-tolerated by patients, even those with hepatic impairment. 4 . Furthermore, futibatinib does not significantly affect cardiac function. 10 .

Risk summary

Futibatinib can cause a number of side effects, including hyperphosphatemia, musculoskeletal pain, constipation, diarrhea, fatigue, dry mouth, alopecia, stomatitis, and abdominal pain. 7 . It can also lead to ocular toxicity, such as dry eye, keratitis, and retinal epithelial detachment. 7 .

Comparison of studies

Similarities between studies

Multiple studies confirm the effectiveness of futibatinib in treating cholangiocarcinoma with FGFR2 aberrations. 13 , 7 , 2 . Moreover, most studies indicate that futibatinib is effective against a wide variety of cancer types, including cholangiocarcinoma, gastric, urothelial, central nervous system, head and neck, and breast cancer. 13 .

Differences between studies

The efficacy of futibatinib may vary depending on the type of cancer and the specific patient. 13 . The side effects of futibatinib can also vary between patients. 7 .

Consistency and contradictions of findings

Multiple clinical trials support the effectiveness of futibatinib in treating patients with FGFR2 fusions or rearrangements. 13 , 7 , 2 . However, the data also suggest that not all patients respond to the treatment and that resistance can occur. 3 . It's important to remember that treatment response and side effects can vary between individuals. 13 , 7 .

Considerations for real-world application

While futibatinib shows promise in treating certain cancers, it's essential to understand that it is not a cure-all and can have significant side effects. 7 . Careful monitoring by a healthcare professional is crucial when considering futibatinib treatment. 7 .

Limitations of current research

The research on futibatinib is still ongoing and more studies are needed to fully understand its long-term effects, side effects, and interactions with other medications. 3 .

Future research directions

Further research is needed to assess the long-term effects and side effects of futibatinib. 3 . Investigating the combination of futibatinib with other therapies and exploring mechanisms of resistance are also important areas for future research. 3 .

Conclusion

Futibatinib demonstrates significant potential in treating certain cancers, particularly those with FGFR2 aberrations. 13 , 7 , 2 . It is well-tolerated and has a relatively safe profile. 4 . However, it is important to be aware of its potential side effects and to discuss the risks and benefits with a healthcare professional before starting treatment. 7 . Further research is needed to better understand futibatinib's long-term effects and potential for combination therapy.

Literature analysis of 21 papers
Positive Content
21
Neutral Content
0
Negative Content
0
Article Type
1
0
0
6
21
1.

Convergent MAPK pathway alterations mediate acquired resistance to FGFR inhibitors in FGFR2 fusion-positive cholangiocarcinoma.

Author: DiPeriTimothy P, ZhaoMing, EvansKurt W, VaradarajanKaushik, MossTyler, ScottStephen, KahleMichael P, ByrnesCharnel C, ChenHuiqin, LeeSunyoung S, HalimAbdel-Baset, HiraiHiroshi, WacheckVolker, KwongLawrence N, RodonJordi, JavleMilind, Meric-BernstamFunda

FGFRi sensitivity
MEK inhibition
FGFRi resistance
MAPK pathway alterations

This study investigated mechanisms of acquired resistance to fibroblast growth factor receptor (FGFR) inhibitors (FGFRi) in patients with FGFR2-fusion-positive cholangiocarcinoma. The study found that convergent genomic evolution in the MAPK pathway may be a mechanism of acquired resistance.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

2.

Infigratinib for the Treatment of Metastatic or Locally Advanced Cholangiocarcinoma With Known FGFR2 Gene Fusions or Rearrangements.

Author: WhiteKathryn, AnwarAhmed I, JinKevin, BollichVictoria, KelkarRucha A, TalbotNorris C, KlapperRachel J, AhmadzadehShahab, ViswanathOmar, VarrassiGiustino, ShekoohiSahar, KayeAlan D

CCA treatment
Resistance

This review discusses the development of infigratinib, a selective FGFR2 inhibitor, for the treatment of cholangiocarcinoma (CCA).

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.

Language : English

3.

Landscape of Clinical Resistance Mechanisms to FGFR Inhibitors in FGFR2-Altered Cholangiocarcinoma.

Author: WuQibiao, EllisHaley, SiravegnaGiulia, MichelAlexa G, NordenBryanna L, Fece de la CruzFerran, BalasooriyaEranga Roshan, ZhenYuanli, SilveiraVanessa S, CheJianwei, CorcoranRyan B, BardeesyNabeel

FGFR2-altered cholangiocarcinoma treatment
Acquired resistance
Secondary FGFR mutations

FGFR inhibitors are effective in treating FGFR2-altered cholangiocarcinoma. However, resistance to these drugs can develop, limiting their clinical benefit. This study seeks to identify mechanisms of resistance to FGFR inhibitors and validate findings in model systems.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

4.

A phase I, open-label, single-dose study to evaluate the effect of hepatic impairment on the pharmacokinetics and safety of futibatinib.

Author: GaoLing, YamamiyaIkuo, PintiMark, RondonJuan Carlos, MarburyThomas, TomlinsonGareth, MakrisLukas, HangaiNanae, WacheckVolker

Intrahepatic cholangiocarcinoma treatment

Futibatinib is a FGFR1-4 inhibitor approved for advanced intrahepatic cholangiocarcinoma. This phase I trial assessed its pharmacokinetics, safety, and tolerability in subjects with impaired hepatic function. Results showed that futibatinib dose adjustments are not required in patients with mild, moderate, or severe hepatic impairment, as changes in pharmacokinetic parameters were not clinically relevant.

Clinical Trial, Phase IThe first stage of clinical trials in humans. Evaluates the safety, tolerability, and pharmacokinetics of a new drug/treatment.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

5.

Pharmacological profile of novel anti-cancer drugs approved by USFDA in 2022: A Review.

Author: SangwanKavita, SharmaVipasha, GoyalParveen Kumar

Lower drug costs
New cancer treatments

In 2022, the Food and Drug Administration (FDA) approved twelve new drug therapies for managing various cancers.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

6.

Evaluation of the Mass Balance and Metabolic Profile of Futibatinib in Healthy Participants.

Author: YamamiyaIkuo, HuntAllen, YamashitaFumiaki, SonnichsenDaryl, MutoToshiharu, HeYaohua, BenhadjiKarim A

Rapid absorption
Well-tolerated

Futibatinib is a selective, irreversible fibroblast growth factor receptor 1-4 inhibitor that has been approved for the treatment of FGFR2 rearrangement-positive cholangiocarcinoma. This Phase I study evaluated the mass balance and metabolic profile of futibatinib in healthy participants. The drug was rapidly absorbed and excreted primarily in feces. Futibatinib was well-tolerated in this study.

Clinical Trial, Phase IThe first stage of clinical trials in humans. Evaluates the safety, tolerability, and pharmacokinetics of a new drug/treatment.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

8.

Updates in the use of targeted therapies for the treatment of cholangiocarcinoma.

Author: LodlEmma, RamnaraignBrian, SahinIlyas, WheelerSarah

CCA treatment
Prognosis improvement
Targeted therapies

This review describes past and current treatment strategies for cholangiocarcinoma (CCA), with a focus on FDA-approved targeted therapies. Targeted therapies have significantly improved the prognosis for advanced or metastatic CCA.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.

Language : English

9.

Futibatinib for <i>FGFR2</i>-Rearranged Intrahepatic Cholangiocarcinoma.

Author: GoyalLipika, Meric-BernstamFunda, HollebecqueAntoine, ValleJuan W, MorizaneChigusa, KarasicThomas B, AbramsThomas A, FuruseJunji, KelleyRobin K, CassierPhilippe A, KlümpenHeinz-Josef, ChangHeung-Moon, ChenLi-Tzong, TaberneroJosep, OhDo-Youn, MahipalAmit, MoehlerMarkus, MitchellEdith P, KomatsuYoshito, MasudaKunihiro, AhnDaniel, EpsteinRobert S, HalimAbdel-Baset, FuYao, SalimiTehseen, WacheckVolker, HeYaohua, LiuMei, BenhadjiKarim A, BridgewaterJohn A,

ICCC treatment
Poor prognosis

Alterations in fibroblast growth factor receptor 2 (FGFR2) are promising drug targets for intrahepatic cholangiocarcinoma. Futibatinib, a next-generation FGFR inhibitor, has shown antitumor activity in patients with FGFR-altered tumors and preclinical activity against acquired resistance mutations.

Clinical Trial, Phase IIA Phase II trial is a trial that further evaluates the efficacy and safety of a new drug or treatment, whose safety has been confirmed to some extent in a Phase I trial, in a small number of patients.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Multicenter StudyResearch conducted in collaboration with multiple research institutions. It aims to collect a wide range of data and obtain more generalizable results.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

10.

Effect of Futibatinib on Cardiac Repolarization: Results of a Randomized, Controlled, Double-Blind, QT/QTc, Phase 1 Study in Healthy Subjects.

Author: YamamiyaIkuo, LesterRobert, SonnichsenDaryl, MinaMark, HeYaohua, BenhadjiKarim A

No QTcF prolongation

This study assessed the effects of futibatinib, a fibroblast growth factor receptor (FGFR) 1-4 inhibitor, on the QTcF interval in healthy subjects. A four-period, crossover, phase 1 thorough QT/QTc study compared single doses of futibatinib at therapeutic and supratherapeutic doses to placebo and a positive control. The study found no significant prolongation of QTcF or effects on other cardiac measures at therapeutic or supratherapeutic doses, suggesting a favorable cardiac safety profile for futibatinib.

Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.
Clinical Trial, Phase IThe first stage of clinical trials in humans. Evaluates the safety, tolerability, and pharmacokinetics of a new drug/treatment.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

11.

Phase I study of the irreversible fibroblast growth factor receptor 1-4 inhibitor futibatinib in Japanese patients with advanced solid tumors.

Author: DoiToshihiko, ShitaraKohei, KojimaTakashi, KubokiYasutoshi, MatsubaraNobuaki, BandoHideaki, YohKiyotaka, NaitoYoichi, HiraiHiroshi, KurokawaYukinori, KatoTerufumi, MorizaneChigusa

Antitumor activity
Decreased appetite
Hyperphosphatemia

This study investigated the safety and effectiveness of futibatinib, an FGFR inhibitor, in patients with advanced solid tumors. The drug was well tolerated, with hyperphosphatemia and decreased appetite as the most common side effects. Futibatinib showed antitumor activity in patients with FGF/FGFR abnormalities, particularly those with gastric cancer and high FGFR2 copy numbers.

Clinical Trial, Phase IThe first stage of clinical trials in humans. Evaluates the safety, tolerability, and pharmacokinetics of a new drug/treatment.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

12.

Proteomic analysis reveals dual requirement for Grb2 and PLCγ1 interactions for BCR-FGFR1-Driven 8p11 cell proliferation.

Author: PeirisMalalage N, MeyerApril N, WardaDalida, CamposAlexandre Rosa, DonoghueDaniel J

Effective against BCR-FGFR1

This study investigated the role of Grb2 and PLCγ1 in the BCR-FGFR1 fusion protein-driven proliferation of hematopoietic cells. It identified key effector proteins and demonstrated the efficacy of PLCγ1 and FGFR inhibitors in blocking cell proliferation.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, N.I.H., ExtramuralResearch funding provided by the NIH to external research institutions and researchers.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

13.

Futibatinib, an Irreversible FGFR1-4 Inhibitor, in Patients with Advanced Solid Tumors Harboring <i>FGF</i>/<i>FGFR</i> Aberrations: A Phase I Dose-Expansion Study.

Author: Meric-BernstamFunda, BahledaRastislav, HierroCinta, SansonMarc, BridgewaterJohn, ArkenauHendrik-Tobias, TranBen, KelleyRobin Kate, ParkJoon Oh, JavleMilind, HeYaohua, BenhadjiKarim A, GoyalLipika

Cancer treatment
FGFR inhibitor efficacy
Genomic selection trials
Diarrhea
Hyperphosphatemia
Nausea

Futibatinib is a highly selective, irreversible FGFR1-4 inhibitor that showed an objective response rate (ORR) of 13.7% in a phase I dose-expansion trial of 197 patients with advanced solid tumors. The drug was effective across a range of tumors, including cholangiocarcinoma, gastric, urothelial, central nervous system, head and neck, and breast cancer, with both known and previously uncharacterized FGFR1-3 aberrations. The highest activity was seen in FGFR2 fusion/rearrangement-positive intrahepatic cholangiocarcinoma (ORR, 25.4%). Some patients with acquired resistance to a prior FGFR inhibitor also experienced responses with futibatinib. The most common treatment-emergent adverse events were hyperphosphatemia (81.2%), diarrhea (33.5%), and nausea (30.4%).

Clinical Trial, Phase IThe first stage of clinical trials in humans. Evaluates the safety, tolerability, and pharmacokinetics of a new drug/treatment.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

14.

FGFR Inhibitors: Clinical Activity and Development in the Treatment of Cholangiocarcinoma.

Author: KingGentry, JavleMilind

CCA treatment
FGFR targeting

This review explores the role of the fibroblast growth factor receptor (FGFR) signaling pathway in cholangiocarcinoma (CCA), an aggressive cancer with a poor prognosis. The review discusses genetic alterations in FGFR identified in CCA patients and highlights the development of therapeutic strategies targeting this pathway, offering potential avenues for improved treatment.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.

Language : English

17.

Dermatologic Adverse Events Associated with Selective Fibroblast Growth Factor Receptor Inhibitors: Overview, Prevention, and Management Guidelines.

Author: LacoutureMario E, SibaudVincent, AnadkatMilan J, KaffenbergerBenjamin, LeventhalJonathan, GuindonKathleen, Abou-AlfaGhassan

Cancer treatment
Skin reactions

This study reviews the dermatologic adverse events associated with FGFR inhibitors, a new type of drug used to treat certain types of cancer. The study found that the most common side effects are those affecting the skin, hair, and nails.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, N.I.H., ExtramuralResearch funding provided by the NIH to external research institutions and researchers.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.

Language : English

18.

Futibatinib Is a Novel Irreversible FGFR 1-4 Inhibitor That Shows Selective Antitumor Activity against FGFR-Deregulated Tumors.

Author: SootomeHiroshi, FujitaHidenori, ItoKenjiro, OchiiwaHiroaki, FujiokaYayoi, ItoKimihiro, MiuraAkihiro, SagaraTakeshi, ItoSatoru, OhsawaHirokazu, OtsukiSachie, FunabashiKaoru, YashiroMasakazu, MatsuoKenichi, YonekuraKazuhiko, HiraiHiroshi

Cancer treatment

This study examines the preclinical profile of futibatinib, a structurally novel, irreversible FGFR1-4 inhibitor.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

19.

Phase I, first-in-human study of futibatinib, a highly selective, irreversible FGFR1-4 inhibitor in patients with advanced solid tumors.

Author: BahledaR, Meric-BernstamF, GoyalL, TranB, HeY, YamamiyaI, BenhadjiK A, MatosI, ArkenauH-T

tumor treatment
safety

This first-in-human phase I dose-escalation trial investigates the safety and pharmacokinetics/pharmacodynamics of futibatinib, an oral FGFR inhibitor, in patients with advanced solid tumors. Futibatinib has potent preclinical activity against tumors with FGFR aberrations.

Clinical Trial, Phase IThe first stage of clinical trials in humans. Evaluates the safety, tolerability, and pharmacokinetics of a new drug/treatment.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

20.

The role of fibroblast growth factor receptor (FGFR) protein-tyrosine kinase inhibitors in the treatment of cancers including those of the urinary bladder.

Author: RoskoskiRobert

Cancer treatment
Hyperphosphatemia

This review discusses the human fibroblast growth factor family and the development of inhibitors for their associated receptors (FGFRs). The FDA approval of erdafitinib for urinary bladder cancers may stimulate further research on FGFR-driven neoplasms.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.

Language : English

21.

Evaluation of Potential Food Effects and Drug Interactions With Lansoprazole in Healthy Adult Volunteers Receiving Futibatinib.

Author: YamamiyaIkuo, HuntAllen, YamashitaFumiaki, SonnichsenDaryl, HeYaohua, BenhadjiKarim A

Futibatinib bioavailability unaffected
Futibatinib may be used with acid-reducing agents
Futibatinib may be used with food

This study investigates the impact of food and proton pump inhibitors (PPIs) on the pharmacokinetics and safety of futibatinib, an oral FGFR inhibitor. Futibatinib is being investigated for the treatment of FGFR-aberrant tumors. The study found that food reduced the bioavailability of futibatinib, but the effect was not clinically significant. PPIs had no significant impact on futibatinib exposure. These findings suggest that futibatinib can be taken with or without food and concomitantly with PPIs.

Clinical Trial, Phase IThe first stage of clinical trials in humans. Evaluates the safety, tolerability, and pharmacokinetics of a new drug/treatment.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

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