Peringatan Keamanan

There is limited information on lethal doses and overdose of infigratinib. In clinical trials, infigratinib was associated with ocular toxicity (retinal pigment epithelial detachment), hyperphosphatemia leading to soft tissue mineralization, and embryo-fetal toxicity.L34299

Infigratinib

DB11886

small molecule approved investigational

Deskripsi

Infigratinib is a pan-fibroblast growth factor receptor (FGFR) kinase inhibitor. By inhibiting the FGFR pathway, which is often aberrated in cancers such as cholangiocarcinoma, infigratinib suppresses tumour growth.A235174 Cholangiocarcinoma is the most common primary malignancy affecting the biliary tract and the second most common primary hepatic malignancy.A198963 Infitratinib is a pan-FGFR inhibitor, as it is an ATP-competitive inhibitor of all four FGFR receptor subtypes.A235174

On May 28, 2021, the FDA granted accelerated approval to infigratinib - under the market name Truseltiq - for the treatment of previously treated, unresectable locally advanced or metastatic cholangiocarcinoma in adults with a fibroblast growth factor receptor 2 (FGFR2) fusion or another rearrangement as detected by an FDA-approved test.L34304 This approval follows pemigatinib, another FGFR inhibitor approved by the FDA for the same therapeutic indication.

Struktur Molekul 2D

Berat 560.475
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The geometric mean (CV%) terminal half-life of infigratinib was 33.5 h (39%) at steady state. [L34299]
Volume Distribusi At steady state, the geometric mean (CV%) apparent volume of distribution of infigratinib was 1600 L (33%). In rats receiving a single oral dose, infigratinib had brain-to-plasma concentration ratios (based on AUC<sub>0-inf</sub>) of 0.682.[L34299]
Klirens (Clearance) The geometric mean (CV%) total apparent clearance (CL/F) of infigratinib was 33.1 L/h (59%) at steady state.[L34299]

Absorpsi

Mean (%CV) Cmax is 282.5 ng/mL (54%) and AUC0-24h is 3780 ngxh/mL (59%) for infigratinib. Infigratinib Cmax and AUC increase more than proportionally across the dose range of 5 to 150 mg and steady state is achieved within 15 days. At steady state, median time to achieve peak infigratinib plasma concentration (Tmax) is six hours, with a range between two and seven hours.L34299 Mean (%CV) Cmax is 42.1 ng/mL (65%) for BHS697 and 15.7 ng/mL (92%) for CQM157. Mean (%CV) AUC0-24h is 717 ngxh/mL (55%) for BHS697 and 428 ngxh/mL (72%) for CQM157. In healthy subjects, a high-fat and high-calorie meal increased AUCinf of infigratinib by 80%-120% and Cmax by 60%-80%. The median Tmax also shifted from four hours to six hours. A low-fat low-calorie meal increased the mean AUCinf of infigratinib by 70% and Cmax by 90%/L34299

Metabolisme

According to in vitro findings, about 94% of infigratinib is metabolized by CYP3A4 and about 6% of the drug is metabolized by flavin-containing monooxygenase 3 (FMO3). About 38% of the dose is circulating parent drug in the plasma and BHS697 and CQM157 are two major metabolites of infigratinib that are each found at >10% of the dose. They are pharmacologically active, with BHS697 representing about 16% to 33% of the overall pharmacological activity of infigratinib and CQM157 contributing to about 9% to 12%. BHS697 undergoes further metabolism mediated by CYP3A4 and CQM157 is metabolized through both Phase I and Phase II biotransformation pathways.L34299 The exact metabolic pathways and the structure of BHS697 and CQM157 are not fully characterized.

Rute Eliminasi

Following administration of a single oral dose of radiolabeled infigratinib in healthy subjects, approximately 77% of the dose was recovered in feces, where 3.4% of the dose was in the unchanged parent form. About 7.2% was recovered in urine with 1.9% of the dose was unchanged.L34299

Interaksi Makanan

2 Data
  • 1. Take on an empty stomach. Take drug at least 1 hour before or 2 hours after food, at approximately the same time each day. Food increases the systemic exposure to infigratinib.
  • 2. Take with a full glass of water. Do not crush, chew or dissolve.

Interaksi Obat

585 Data
Acetaminophen The serum concentration of Acetaminophen can be increased when it is combined with Infigratinib.
Propacetamol The serum concentration of Propacetamol can be increased when it is combined with Infigratinib.
Pitolisant The serum concentration of Infigratinib can be decreased when it is combined with Pitolisant.
Metreleptin The metabolism of Infigratinib can be increased when combined with Metreleptin.
Felbamate The metabolism of Infigratinib can be increased when combined with Felbamate.
Genistein The metabolism of Infigratinib can be increased when combined with Genistein.
Oritavancin The metabolism of Infigratinib can be increased when combined with Oritavancin.
Rufinamide The metabolism of Infigratinib can be increased when combined with Rufinamide.
Armodafinil The metabolism of Infigratinib can be increased when combined with Armodafinil.
Glycerol phenylbutyrate The metabolism of Infigratinib can be increased when combined with Glycerol phenylbutyrate.
Eslicarbazepine acetate The metabolism of Infigratinib can be increased when combined with Eslicarbazepine acetate.
Lesinurad The metabolism of Infigratinib can be increased when combined with Lesinurad.
Asunaprevir The metabolism of Infigratinib can be increased when combined with Asunaprevir.
Sarilumab The metabolism of Infigratinib can be increased when combined with Sarilumab.
Esketamine The metabolism of Infigratinib can be increased when combined with Esketamine.
Calcitriol The metabolism of Infigratinib can be increased when combined with Calcitriol.
Vitamin E The metabolism of Infigratinib can be increased when combined with Vitamin E.
Flunisolide The metabolism of Infigratinib can be increased when combined with Flunisolide.
Troglitazone The metabolism of Infigratinib can be increased when combined with Troglitazone.
Butalbital The metabolism of Infigratinib can be increased when combined with Butalbital.
Topiramate The metabolism of Infigratinib can be increased when combined with Topiramate.
Flucloxacillin The metabolism of Infigratinib can be increased when combined with Flucloxacillin.
Clobazam The metabolism of Infigratinib can be increased when combined with Clobazam.
Aminoglutethimide The metabolism of Infigratinib can be increased when combined with Aminoglutethimide.
Beclomethasone dipropionate The metabolism of Infigratinib can be increased when combined with Beclomethasone dipropionate.
Griseofulvin The metabolism of Infigratinib can be increased when combined with Griseofulvin.
Secobarbital The metabolism of Infigratinib can be increased when combined with Secobarbital.
Betamethasone The metabolism of Infigratinib can be increased when combined with Betamethasone.
Chlorpromazine The metabolism of Infigratinib can be increased when combined with Chlorpromazine.
Dicloxacillin The metabolism of Infigratinib can be increased when combined with Dicloxacillin.
Rofecoxib The metabolism of Infigratinib can be increased when combined with Rofecoxib.
Fluocinolone acetonide The metabolism of Infigratinib can be increased when combined with Fluocinolone acetonide.
Medroxyprogesterone acetate The metabolism of Infigratinib can be increased when combined with Medroxyprogesterone acetate.
Rifabutin The metabolism of Infigratinib can be increased when combined with Rifabutin.
Triamcinolone The metabolism of Infigratinib can be increased when combined with Triamcinolone.
Testosterone The metabolism of Infigratinib can be increased when combined with Testosterone.
Clofibrate The metabolism of Infigratinib can be increased when combined with Clofibrate.
Hydrocortisone The metabolism of Infigratinib can be increased when combined with Hydrocortisone.
Mometasone The metabolism of Infigratinib can be increased when combined with Mometasone.
Hydrocortamate The metabolism of Infigratinib can be increased when combined with Hydrocortamate.
Oxcarbazepine The metabolism of Infigratinib can be increased when combined with Oxcarbazepine.
Phenylbutazone The metabolism of Infigratinib can be increased when combined with Phenylbutazone.
Methylphenobarbital The metabolism of Infigratinib can be increased when combined with Methylphenobarbital.
Terbinafine The metabolism of Infigratinib can be increased when combined with Terbinafine.
Prednisolone The metabolism of Infigratinib can be increased when combined with Prednisolone.
Ethanol The metabolism of Infigratinib can be increased when combined with Ethanol.
Norgestimate The metabolism of Infigratinib can be increased when combined with Norgestimate.
Methylprednisolone The metabolism of Infigratinib can be increased when combined with Methylprednisolone.
Clobetasol propionate The metabolism of Infigratinib can be increased when combined with Clobetasol propionate.
Probenecid The metabolism of Infigratinib can be increased when combined with Probenecid.
Fluocinonide The metabolism of Infigratinib can be increased when combined with Fluocinonide.
Sulfinpyrazone The metabolism of Infigratinib can be increased when combined with Sulfinpyrazone.
Thiamylal The metabolism of Infigratinib can be increased when combined with Thiamylal.
Rifapentine The metabolism of Infigratinib can be increased when combined with Rifapentine.
Budesonide The metabolism of Infigratinib can be increased when combined with Budesonide.
Corticotropin The metabolism of Infigratinib can be increased when combined with Corticotropin.
Cefradine The metabolism of Infigratinib can be increased when combined with Cefradine.
Amobarbital The metabolism of Infigratinib can be increased when combined with Amobarbital.
Aprobarbital The metabolism of Infigratinib can be increased when combined with Aprobarbital.
Cortisone acetate The metabolism of Infigratinib can be increased when combined with Cortisone acetate.
Barbital The metabolism of Infigratinib can be increased when combined with Barbital.
Deferasirox The metabolism of Infigratinib can be increased when combined with Deferasirox.
Clevidipine The metabolism of Infigratinib can be increased when combined with Clevidipine.
Fosaprepitant The metabolism of Infigratinib can be increased when combined with Fosaprepitant.
Seratrodast The metabolism of Infigratinib can be increased when combined with Seratrodast.
Perampanel The metabolism of Infigratinib can be increased when combined with Perampanel.
Formestane The metabolism of Infigratinib can be increased when combined with Formestane.
Fluprednidene The metabolism of Infigratinib can be increased when combined with Fluprednidene.
Fluocortolone The metabolism of Infigratinib can be increased when combined with Fluocortolone.
Barbexaclone The metabolism of Infigratinib can be increased when combined with Barbexaclone.
Difluocortolone The metabolism of Infigratinib can be increased when combined with Difluocortolone.
Meprednisone The metabolism of Infigratinib can be increased when combined with Meprednisone.
Dexamethasone isonicotinate The metabolism of Infigratinib can be increased when combined with Dexamethasone isonicotinate.
Deflazacort The metabolism of Infigratinib can be increased when combined with Deflazacort.
Cortivazol The metabolism of Infigratinib can be increased when combined with Cortivazol.
Prednylidene The metabolism of Infigratinib can be increased when combined with Prednylidene.
Cloprednol The metabolism of Infigratinib can be increased when combined with Cloprednol.
Estradiol acetate The metabolism of Infigratinib can be increased when combined with Estradiol acetate.
Estradiol benzoate The metabolism of Infigratinib can be increased when combined with Estradiol benzoate.
Estradiol cypionate The metabolism of Infigratinib can be increased when combined with Estradiol cypionate.
Estradiol dienanthate The metabolism of Infigratinib can be increased when combined with Estradiol dienanthate.
Estradiol valerate The metabolism of Infigratinib can be increased when combined with Estradiol valerate.
Mometasone furoate The metabolism of Infigratinib can be increased when combined with Mometasone furoate.
Hydrocortisone acetate The metabolism of Infigratinib can be increased when combined with Hydrocortisone acetate.
Hydrocortisone butyrate The metabolism of Infigratinib can be increased when combined with Hydrocortisone butyrate.
Hydrocortisone succinate The metabolism of Infigratinib can be increased when combined with Hydrocortisone succinate.
Eslicarbazepine The metabolism of Infigratinib can be increased when combined with Eslicarbazepine.
Prednisolone phosphate The metabolism of Infigratinib can be increased when combined with Prednisolone phosphate.
Prednisolone hemisuccinate The metabolism of Infigratinib can be increased when combined with Prednisolone hemisuccinate.
Prednisone acetate The metabolism of Infigratinib can be increased when combined with Prednisone acetate.
Clocortolone acetate The metabolism of Infigratinib can be increased when combined with Clocortolone acetate.
Melengestrol acetate The metabolism of Infigratinib can be increased when combined with Melengestrol acetate.
Betamethasone phosphate The metabolism of Infigratinib can be increased when combined with Betamethasone phosphate.
Cortisone The metabolism of Infigratinib can be increased when combined with Cortisone.
Prednisolone acetate The metabolism of Infigratinib can be increased when combined with Prednisolone acetate.
Citalopram The metabolism of Infigratinib can be decreased when combined with Citalopram.
Ranolazine The metabolism of Infigratinib can be decreased when combined with Ranolazine.
Ethambutol The metabolism of Infigratinib can be decreased when combined with Ethambutol.
Mirtazapine The metabolism of Infigratinib can be decreased when combined with Mirtazapine.
Fluoxetine The metabolism of Infigratinib can be decreased when combined with Fluoxetine.

Target Protein

Fibroblast growth factor receptor 1 FGFR1
Fibroblast growth factor receptor 2 FGFR2
Fibroblast growth factor receptor 3 FGFR3
Fibroblast growth factor receptor 4 FGFR4

Referensi & Sumber

Artikel (PubMed)
  • PMID: 33307867
    Botrus G, Raman P, Oliver T, Bekaii-Saab T: Infigratinib (BGJ398): an investigational agent for the treatment of FGFR-altered intrahepatic cholangiocarcinoma. Expert Opin Investig Drugs. 2021 Apr;30(4):309-316. doi: 10.1080/13543784.2021.1864320. Epub 2021 Jan 4.
  • PMID: 27928095
    Blechacz B: Cholangiocarcinoma: Current Knowledge and New Developments. Gut Liver. 2017 Jan 15;11(1):13-26. doi: 10.5009/gnl15568.
  • PMID: 32370101
    Lima NC, Atkinson E, Bunney TD, Katan M, Huang PH: Targeting the Src Pathway Enhances the Efficacy of Selective FGFR Inhibitors in Urothelial Cancers with FGFR3 Alterations. Int J Mol Sci. 2020 May 1;21(9). pii: ijms21093214. doi: 10.3390/ijms21093214.

Contoh Produk & Brand

Produk: 8 • International brands: 1
Produk
  • Truseltiq
    Capsule • 100 mg/1 • Oral • US • Approved
  • Truseltiq
    Capsule • 75 mg/1 • Oral • US • Approved
  • Truseltiq
    Capsule • 50 mg/1 • Oral • US • Approved
  • Truseltiq
    Capsule • 125 mg/1 • Oral • US • Approved
  • Truseltiq
    Capsule • 75 mg / dose • Oral • Canada • Approved
  • Truseltiq
    Capsule • 100 mg / dose • Oral • Canada • Approved
  • Truseltiq
    Capsule • 50 mg / dose • Oral • Canada • Approved
  • Truseltiq
    Capsule • 125 mg / dose • Oral • Canada • Approved
International Brands
  • Truseltiq — BridgeBio Pharma, Inc.

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