Infigratinib

Identification

Summary

Infigratinib is an FGFR inhibitor used to treat locally advanced or metastatic cholangiocarcinoma in adults with a fibroblast growth factor receptor 2 (FGFR2) rearrangement.

Brand Names
Truseltiq
Generic Name
Infigratinib
DrugBank Accession Number
DB11886
Background

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.1 Cholangiocarcinoma is the most common primary malignancy affecting the biliary tract and the second most common primary hepatic malignancy.2 Infitratinib is a pan-FGFR inhibitor, as it is an ATP-competitive inhibitor of all four FGFR receptor subtypes.1

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.5 This approval follows pemigatinib, another FGFR inhibitor approved by the FDA for the same therapeutic indication.

Type
Small Molecule
Groups
Approved, Investigational
Structure
Thumb
Weight
Average: 560.475
Monoisotopic: 559.186543307
Chemical Formula
C26H31Cl2N7O3
Synonyms
  • Infigratinib
External IDs
  • BGJ 398
  • BGJ-398
  • BGJ398
  • NVP-BGJ398
  • WHO 10032

Pharmacology

Indication

Infigratinib is indicated 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.4

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Infigratinib is an anti-tumour agent that works to suppress tumour growth in cholangiocarcinoma. It exhibits anti-tumour activity in mouse and rat xenograft models of human tumours with activating FGFR2 or FGFR3 alterations, such as FGFR2-TTC28 or FGFR2-TRA2B fusions.4 In clinical trials, patients with cholangiocarcinoma who were treated with infigratinib had an overall response rate of 23% - where one patient had a complete response - and a duration of response of 5.5 months, with a range between 0.03 and 28.3 months.4,5 Some patients with cancers with FGFR mutations display intrinsic resistance to infigratinib, leading to negligible therapeutic efficacy: investigations are ongoing to target molecular pathways to combat drug resistance.3

Mechanism of action

Fibroblast growth factor receptors (FGFRs) are tyrosine kinase receptors that play a role in cell proliferation, differentiation, migration, survival, and angiogenesis. Upon binding of extracellular signals, primarily fibroblast growth factors, FGFR dimerizes to promote phosphorylation of downstream molecules and activation of the Ras-mitogen-activated protein kinase (MAPK) pathway. In some cancers, the FGFR signalling pathway is aberrant and disrupted, leading to unregulated cell proliferation and growth, including malignant cells. Alterations in the FGFR receptors, including mutations, amplifications, and fusions, are associated with a wide array of neoplasms, including prostate, urothelial, ovarian, breast, and liver cancer.1 In particular, FGFR2 fusion is closely related to intrahepatic cholangiocarcinoma: recent studies show that up to 45% of patients with intrahepatic cholangiocarcinoma exhibited gene rearrangements resulting in FGFR2 fusion proteins.2 Alterations in FGFR in tumours can lead to constitutive FGFR signalling, supporting the proliferation and survival of malignant cells.4 Infigratinib is a reversible, non-competitive 1 inhibitor of all four FGFR subtypes - FGFR1, FGFR2, FGFR3, and FGFR4 - that blocks FGFR signalling and inhibits cell proliferation in cancer cell lines with activating FGFR amplification, mutations, or fusions. Out of the four FGFR subtypes, infigratinib has the highest affinity for FGFR1, FGFR2, and FGFR3.4 Infigratinib binds to the allosteric site between the two kinase lobes of the FGFR - or more specifically, to the ATP-binding cleft. Binding to this cleft prevents autophosphorylation of the receptor and blocks downstream signalling cascades that would otherwise activate MAPK.1

TargetActionsOrganism
AFibroblast growth factor receptor 1
inhibitor
Humans
AFibroblast growth factor receptor 2
inhibitor
Humans
AFibroblast growth factor receptor 3
inhibitor
Humans
AFibroblast growth factor receptor 4
inhibitor
Humans
Absorption

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.4

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%/4

Volume of distribution

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 AUC0-inf) of 0.682.4

Protein binding

Infigratinib is about 96.8% bound to plasma proteins, primarily to lipoprotein. Protein binding is concentration-dependent.4

Metabolism

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.4 The exact metabolic pathways and the structure of BHS697 and CQM157 are not fully characterized.

Route of elimination

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.4

Half-life

The geometric mean (CV%) terminal half-life of infigratinib was 33.5 h (39%) at steady state. 4

Clearance

The geometric mean (CV%) total apparent clearance (CL/F) of infigratinib was 33.1 L/h (59%) at steady state.4

Adverse Effects
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Toxicity

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.4

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbaloparatideThe therapeutic efficacy of Abaloparatide can be decreased when used in combination with Infigratinib.
AbametapirThe serum concentration of Infigratinib can be increased when it is combined with Abametapir.
AbirateroneThe metabolism of Infigratinib can be decreased when combined with Abiraterone.
AcetaminophenThe serum concentration of Acetaminophen can be increased when it is combined with Infigratinib.
AcetazolamideThe metabolism of Infigratinib can be decreased when combined with Acetazolamide.
AldesleukinThe metabolism of Infigratinib can be decreased when combined with Aldesleukin.
AlmasilateThe serum concentration of Infigratinib can be decreased when it is combined with Almasilate.
AluminiumThe serum concentration of Infigratinib can be decreased when it is combined with Aluminium.
Aluminium phosphateThe serum concentration of Infigratinib can be decreased when it is combined with Aluminium phosphate.
Aluminum hydroxideThe serum concentration of Infigratinib can be decreased when it is combined with Aluminum hydroxide.
Interactions
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Food Interactions
  • 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.
  • Take with a full glass of water. Do not crush, chew or dissolve.

Products

Products
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Product Ingredients
IngredientUNIICASInChI Key
Infigratinib acetate03D0789NYP1310746-17-8XHCQHOGMMJKLRU-UHFFFAOYSA-N
Infigratinib hydrochlorideWY8VD4RV771310746-15-6VBAIJSJSFCXDJB-UHFFFAOYSA-N
Infigratinib mesylateE223Z0KWCC1310746-12-3BXJJFNXYWJLBOS-UHFFFAOYSA-N
Infigratinib phosphate58BH47BV6S1310746-10-1GUQNHCGYHLSITB-UHFFFAOYSA-N
International/Other Brands
Truseltiq (BridgeBio Pharma, Inc.)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
TruseltiqCapsule125 mg/1OralQed Therapeutics, Inc.2021-05-28Not applicableUS flag
TruseltiqCapsule100 mg/1OralQed Therapeutics, Inc.2021-05-28Not applicableUS flag
TruseltiqCapsule50 mg/1OralQed Therapeutics, Inc.2021-05-28Not applicableUS flag
TruseltiqCapsule75 mg/1OralQed Therapeutics, Inc.2021-05-28Not applicableUS flag

Categories

Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as phenylpiperazines. These are compounds containing a phenylpiperazine skeleton, which consists of a piperazine bound to a phenyl group.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Diazinanes
Sub Class
Piperazines
Direct Parent
Phenylpiperazines
Alternative Parents
N-arylpiperazines / Dimethoxybenzenes / N-phenylureas / Methoxyanilines / Dialkylarylamines / Dichlorobenzenes / Phenoxy compounds / Anisoles / Alkyl aryl ethers / N-alkylpiperazines
show 13 more
Substituents
1,3-dichlorobenzene / Alkyl aryl ether / Amine / Aminopyrimidine / Aniline or substituted anilines / Anisole / Aromatic heteromonocyclic compound / Aryl chloride / Aryl halide / Azacycle
show 35 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
N-arylpiperazine, ureas, aminopyrimidine, dichlorobenzene, N-alkylpiperazine (CHEBI:63451)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
A4055ME1VK
CAS number
872511-34-7
InChI Key
QADPYRIHXKWUSV-UHFFFAOYSA-N
InChI
InChI=1S/C26H31Cl2N7O3/c1-5-34-10-12-35(13-11-34)18-8-6-17(7-9-18)31-21-15-22(30-16-29-21)33(2)26(36)32-25-23(27)19(37-3)14-20(38-4)24(25)28/h6-9,14-16H,5,10-13H2,1-4H3,(H,32,36)(H,29,30,31)
IUPAC Name
3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-(6-{[4-(4-ethylpiperazin-1-yl)phenyl]amino}pyrimidin-4-yl)-1-methylurea
SMILES
CCN1CCN(CC1)C1=CC=C(NC2=CC(=NC=N2)N(C)C(=O)NC2=C(Cl)C(OC)=CC(OC)=C2Cl)C=C1

References

General References
  1. 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. [Article]
  2. Blechacz B: Cholangiocarcinoma: Current Knowledge and New Developments. Gut Liver. 2017 Jan 15;11(1):13-26. doi: 10.5009/gnl15568. [Article]
  3. 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. [Article]
  4. FDA Approved Drug Products: TRUSELTIQ (infigratinib) capsules, for oral use [Link]
  5. FDA Drug Approvals and Databases: FDA grants accelerated approval to infigratinib for metastatic cholangiocarcinoma [Link]
PubChem Compound
53235510
PubChem Substance
347828222
ChemSpider
26333103
BindingDB
50355393
RxNav
2550729
ChEBI
63451
ChEMBL
CHEMBL1852688
ZINC
ZINC000072105034
PDBe Ligand
07J
Wikipedia
Infigratinib
PDB Entries
3tt0

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3RecruitingTreatmentAdvanced Cholangiocarcinoma / FGFR2 Gene Mutation1
3RecruitingTreatmentUpper Tract Urothelial Carcinomas / Urothelial Bladder Cancer1
2Active Not RecruitingTreatmentMelanomas1
2CompletedTreatmentRecurrent Glioblastoma or Other Glioma Subtypes1
2RecruitingTreatmentAchondroplasia1
2RecruitingTreatmentAdvanced Cholangiocarcinoma / FGFR2 Gene Mutation1
2RecruitingTreatmentAdvanced Malignant Solid Neoplasm / Cholangiocarcinomas / Metastatic Malignant Solid Neoplasm / Refractory Malignant Solid Neoplasm1
2TerminatedTreatmentFGFR Gene Amplification / FGFR1 Gene Amplification / FGFR2 Gene Amplification / FGFR2 Gene Mutation / FGFR3 Gene Mutation / Head and Neck Squamous Cell Carcinoma (HNSCC) / Human Papillomavirus Infections / Recurrent Head and Neck Carcinoma / Recurrent Nasopharynx Carcinoma / Recurrent Oropharyngeal Squamous Cell Carcinoma1
2TerminatedTreatmentMalignancies, Hematologic / Tumors, Solid1
2TerminatedTreatmentOncogenic Osteomalacia / Tumor-Induced Osteomalacia1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
CapsuleOral100 mg/1
CapsuleOral125 mg/1
CapsuleOral50 mg/1
CapsuleOral75 mg/1
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
boiling point (°C)747.9http://file.medchemexpress.com/batch_PDF/HY-13311/Infigratinib-SDS-MedChemExpress.pdf
Predicted Properties
PropertyValueSource
Water Solubility0.0299 mg/mLALOGPS
logP4.68ALOGPS
logP4.78ChemAxon
logS-4.3ALOGPS
pKa (Strongest Acidic)9.98ChemAxon
pKa (Strongest Basic)8.23ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count8ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area95.09 Å2ChemAxon
Rotatable Bond Count8ChemAxon
Refractivity152.71 m3·mol-1ChemAxon
Polarizability58.51 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Targets

Drugtargets
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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
Curator comments
Infigratinib binds to FGFR1 with IC50 value of 1.1 nM. Its major metabolites, BHS697 and CQM157, have similar in vitro binding affinities for FGFR1, FGFR2, and FGFR3.
General Function
Protein tyrosine kinase activity
Specific Function
Tyrosine-protein kinase that acts as cell-surface receptor for fibroblast growth factors and plays an essential role in the regulation of embryonic development, cell proliferation, differentiation ...
Gene Name
FGFR1
Uniprot ID
P11362
Uniprot Name
Fibroblast growth factor receptor 1
Molecular Weight
91866.935 Da
References
  1. FDA Approved Drug Products: TRUSELTIQ (infigratinib) capsules, for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
Curator comments
Infigratinib binds to FGFR2 with IC50 value of 1.0 nM. Its major metabolites, BHS697 and CQM157, have similar in vitro binding affinities for FGFR1, FGFR2, and FGFR3.
General Function
Protein tyrosine kinase activity
Specific Function
Tyrosine-protein kinase that acts as cell-surface receptor for fibroblast growth factors and plays an essential role in the regulation of cell proliferation, differentiation, migration and apoptosi...
Gene Name
FGFR2
Uniprot ID
P21802
Uniprot Name
Fibroblast growth factor receptor 2
Molecular Weight
92024.29 Da
References
  1. FDA Approved Drug Products: TRUSELTIQ (infigratinib) capsules, for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
Curator comments
Infigratinib binds to FGFR3 with IC50 value of 2.0 nM. Its major metabolites, BHS697 and CQM157, have similar in vitro binding affinities for FGFR1, FGFR2, and FGFR3.
General Function
Protein tyrosine kinase activity
Specific Function
Tyrosine-protein kinase that acts as cell-surface receptor for fibroblast growth factors and plays an essential role in the regulation of cell proliferation, differentiation and apoptosis. Plays an...
Gene Name
FGFR3
Uniprot ID
P22607
Uniprot Name
Fibroblast growth factor receptor 3
Molecular Weight
87708.905 Da
References
  1. FDA Approved Drug Products: TRUSELTIQ (infigratinib) capsules, for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
Curator comments
Infigratinib binds to FGFR4 with IC50 value of 61 nM. Its major metabolites, BHS697 and CQM157, have similar in vitro binding affinities for FGFR4.
General Function
Protein tyrosine kinase activity
Specific Function
Tyrosine-protein kinase that acts as cell-surface receptor for fibroblast growth factors and plays a role in the regulation of cell proliferation, differentiation and migration, and in regulation o...
Gene Name
FGFR4
Uniprot ID
P22455
Uniprot Name
Fibroblast growth factor receptor 4
Molecular Weight
87953.535 Da
References
  1. FDA Approved Drug Products: TRUSELTIQ (infigratinib) capsules, for oral use [Link]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. FDA Approved Drug Products: TRUSELTIQ (infigratinib) capsules, for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Trimethylamine monooxygenase activity
Specific Function
Involved in the oxidative metabolism of a variety of xenobiotics such as drugs and pesticides. It N-oxygenates primary aliphatic alkylamines as well as secondary and tertiary amines. Plays an impor...
Gene Name
FMO3
Uniprot ID
P31513
Uniprot Name
Dimethylaniline monooxygenase [N-oxide-forming] 3
Molecular Weight
60032.975 Da
References
  1. FDA Approved Drug Products: TRUSELTIQ (infigratinib) capsules, for oral use [Link]

Carriers

Kind
Protein group
Organism
Humans
Pharmacological action
No
Actions
Binder
General Function
Phospholipid transporter activity
Specific Function
Participates in the reverse transport of cholesterol from tissues to the liver for excretion by promoting cholesterol efflux from tissues and by acting as a cofactor for the lecithin cholesterol ac...

Components:
References
  1. FDA Approved Drug Products: TRUSELTIQ (infigratinib) capsules, for oral use [Link]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
Inhibitor
Curator comments
Infigratinib and its metabolites BHS697 and CQM157 have a low potential to inhibit P-gp at clinically relevant concentrations
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. FDA Approved Drug Products: TRUSELTIQ (infigratinib) capsules, for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
Inhibitor
Curator comments
Infigratinib and its metabolites BHS697 and CQM157 have a low potential to inhibit BCRP at clinically relevant concentrations
General Function
Xenobiotic-transporting atpase activity
Specific Function
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
Gene Name
ABCG2
Uniprot ID
Q9UNQ0
Uniprot Name
ATP-binding cassette sub-family G member 2
Molecular Weight
72313.47 Da
References
  1. FDA Approved Drug Products: TRUSELTIQ (infigratinib) capsules, for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Inhibitor
General Function
Monovalent cation:proton antiporter activity
Specific Function
Solute transporter for tetraethylammonium (TEA), 1-methyl-4-phenylpyridinium (MPP), cimetidine, N-methylnicotinamide (NMN), metformin, creatinine, guanidine, procainamide, topotecan, estrone sulfat...
Gene Name
SLC47A1
Uniprot ID
Q96FL8
Uniprot Name
Multidrug and toxin extrusion protein 1
Molecular Weight
61921.585 Da
References
  1. FDA Approved Drug Products: TRUSELTIQ (infigratinib) capsules, for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Inhibitor
Curator comments
Infigratinib has a low potential to inhibit BSEP at clinically relevant concentrations.
General Function
Transporter activity
Specific Function
Involved in the ATP-dependent secretion of bile salts into the canaliculus of hepatocytes.
Gene Name
ABCB11
Uniprot ID
O95342
Uniprot Name
Bile salt export pump
Molecular Weight
146405.83 Da
References
  1. FDA Approved Drug Products: TRUSELTIQ (infigratinib) capsules, for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Inhibitor
Curator comments
Infigratinib has a low potential to inhibit OCT1 at clinically relevant concentrations.
General Function
Secondary active organic cation transmembrane transporter activity
Specific Function
Translocates a broad array of organic cations with various structures and molecular weights including the model compounds 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), N-1-methylnico...
Gene Name
SLC22A1
Uniprot ID
O15245
Uniprot Name
Solute carrier family 22 member 1
Molecular Weight
61153.345 Da
References
  1. FDA Approved Drug Products: TRUSELTIQ (infigratinib) capsules, for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Inhibitor
Curator comments
Infigratinib has a low potential to inhibit OCT2 at clinically relevant concentrations.
General Function
Quaternary ammonium group transmembrane transporter activity
Specific Function
Mediates tubular uptake of organic compounds from circulation. Mediates the influx of agmatine, dopamine, noradrenaline (norepinephrine), serotonin, choline, famotidine, ranitidine, histamin, creat...
Gene Name
SLC22A2
Uniprot ID
O15244
Uniprot Name
Solute carrier family 22 member 2
Molecular Weight
62579.99 Da
References
  1. FDA Approved Drug Products: TRUSELTIQ (infigratinib) capsules, for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Inhibitor
Curator comments
Infigratinib has a low potential to inhibit MATE-2K at clinically relevant concentrations.
General Function
Drug transmembrane transporter activity
Specific Function
Solute transporter for tetraethylammonium (TEA), 1-methyl-4-phenylpyridinium (MPP), cimetidine, N-methylnicotinamide, metformin, creatinine, guanidine, procainamide, topotecan, estrone sulfate, acy...
Gene Name
SLC47A2
Uniprot ID
Q86VL8
Uniprot Name
Multidrug and toxin extrusion protein 2
Molecular Weight
65083.915 Da
References
  1. FDA Approved Drug Products: TRUSELTIQ (infigratinib) capsules, for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Inhibitor
Curator comments
The metabolites of infigratinib - BHS697 and CQM157 - have a low potential to inhibit OATP1B1 and OATP1B3 at clinically relevant concentrations.
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland...
Gene Name
SLCO1B1
Uniprot ID
Q9Y6L6
Uniprot Name
Solute carrier organic anion transporter family member 1B1
Molecular Weight
76447.99 Da
References
  1. FDA Approved Drug Products: TRUSELTIQ (infigratinib) capsules, for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Inhibitor
Curator comments
The metabolites of infigratinib - BHS697 and CQM157 - have a low potential to inhibit OATP1B1 and OATP1B3 at clinically relevant concentrations.
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotre...
Gene Name
SLCO1B3
Uniprot ID
Q9NPD5
Uniprot Name
Solute carrier organic anion transporter family member 1B3
Molecular Weight
77402.175 Da
References
  1. FDA Approved Drug Products: TRUSELTIQ (infigratinib) capsules, for oral use [Link]

Drug created on October 20, 2016 20:57 / Updated on June 02, 2021 20:03