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
- 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
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Unresectable, locally advanced cholangiocarcinomas •••••••••••• ••••• ••••• •••• •••••••••••••• •••••••••• ••••••• ••••••• Treatment of Unresectable, metastatic cholangiocarcinomas •••••••••••• ••••• ••••• •••• •••••••••••••• •••••••••• ••••••• ••••••• - Contraindications & Blackbox Warnings
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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
Target Actions Organism AFibroblast growth factor receptor 1 inhibitorHumans AFibroblast growth factor receptor 2 inhibitorHumans AFibroblast growth factor receptor 3 inhibitorHumans AFibroblast growth factor receptor 4 inhibitorHumans - 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 Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAbametapir The serum concentration of Infigratinib can be increased when it is combined with Abametapir. Abatacept The metabolism of Infigratinib can be increased when combined with Abatacept. Abemaciclib The metabolism of Abemaciclib can be decreased when combined with Infigratinib. Acalabrutinib The metabolism of Acalabrutinib can be decreased when combined with Infigratinib. Acenocoumarol The metabolism of Acenocoumarol can be decreased when combined with Infigratinib. - 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
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Product Ingredients
Ingredient UNII CAS InChI Key Infigratinib acetate 03D0789NYP 1310746-17-8 XHCQHOGMMJKLRU-UHFFFAOYSA-N Infigratinib hydrochloride WY8VD4RV77 1310746-15-6 VBAIJSJSFCXDJB-UHFFFAOYSA-N Infigratinib mesylate E223Z0KWCC 1310746-12-3 BXJJFNXYWJLBOS-UHFFFAOYSA-N Infigratinib phosphate 58BH47BV6S 1310746-10-1 GUQNHCGYHLSITB-UHFFFAOYSA-N - International/Other Brands
- Truseltiq (BridgeBio Pharma, Inc.)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Truseltiq Capsule 50 mg / dose Oral Qed Therapeutics, Inc. Not applicable Not applicable Canada Truseltiq Capsule 125 mg/1 Oral Qed Therapeutics, Inc. 2021-05-28 Not applicable US Truseltiq Capsule 100 mg/1 Oral Qed Therapeutics, Inc. 2021-05-28 Not applicable US Truseltiq Capsule 100 mg / dose Oral Qed Therapeutics, Inc. Not applicable Not applicable Canada Truseltiq Capsule 50 mg/1 Oral Qed Therapeutics, Inc. 2021-05-28 Not applicable US
Categories
- ATC Codes
- L01EN03 — Infigratinib
- Drug Categories
- Amides
- Antineoplastic Agents
- Antineoplastic and Immunomodulating Agents
- BCRP/ABCG2 Inhibitors
- BCRP/ABCG2 Substrates
- Benzene Derivatives
- BSEP/ABCB11 Inhibitors
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A4 Substrates (strength unknown)
- Cytochrome P-450 Substrates
- Fibroblast Growth Factor 2, antagonists & inhibitors
- Fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitors
- Kinase Inhibitor
- MATE 1 Inhibitors
- MATE 2 Inhibitors
- MATE inhibitors
- OATP1B1/SLCO1B1 Inhibitors
- OATP1B3 inhibitors
- OCT1 inhibitors
- OCT2 Inhibitors
- P-glycoprotein inhibitors
- P-glycoprotein substrates
- Protein Kinase Inhibitors
- Receptor, Fibroblast Growth Factor, Type 1, antagonists & inhibitors
- Receptors, Fibroblast Growth Factor, antagonists & inhibitors
- Tyrosine Kinase Inhibitors
- 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
- 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]
- Blechacz B: Cholangiocarcinoma: Current Knowledge and New Developments. Gut Liver. 2017 Jan 15;11(1):13-26. doi: 10.5009/gnl15568. [Article]
- 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]
- FDA Approved Drug Products: TRUSELTIQ (infigratinib) capsules, for oral use [Link]
- FDA Drug Approvals and Databases: FDA grants accelerated approval to infigratinib for metastatic cholangiocarcinoma [Link]
- External Links
- PubChem Compound
- 53235510
- PubChem Substance
- 347828222
- ChemSpider
- 26333103
- BindingDB
- 50355393
- 2550729
- ChEBI
- 63451
- ChEMBL
- CHEMBL1852688
- ZINC
- ZINC000072105034
- PDBe Ligand
- 07J
- Wikipedia
- Infigratinib
- PDB Entries
- 3tt0
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 3 Enrolling by Invitation Treatment Achondroplasia 1 3 Terminated Treatment Cholangiocarcinoma Advanced / FGFR2 Gene Mutation 1 3 Terminated Treatment Upper Tract Urothelial Carcinomas / Urothelial Bladder Cancer 1 2 Active Not Recruiting Treatment Advanced Malignant Solid Tumor / Cholangiocarcinoma / Metastatic Malignant Solid Neoplasms / Refractory Malignant Solid Neoplasm 1 2 Completed Treatment Melanoma 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Capsule Oral 100 mg / dose Capsule Oral 100 mg/1 Capsule Oral 125 mg/1 Capsule Oral 125 mg / dose Capsule Oral 50 mg/1 Capsule Oral 50 mg / dose Capsule Oral 75 mg/1 Capsule Oral 75 mg / dose - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US10278969 No 2019-05-07 2034-12-11 US US9067896 No 2015-06-30 2026-12-20 US US8552002 No 2013-10-08 2029-08-25 US US11160804 No 2021-11-02 2034-12-11 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source boiling point (°C) 747.9 http://file.medchemexpress.com/batch_PDF/HY-13311/Infigratinib-SDS-MedChemExpress.pdf - Predicted Properties
Property Value Source Water Solubility 0.0299 mg/mL ALOGPS logP 4.68 ALOGPS logP 4.78 Chemaxon logS -4.3 ALOGPS pKa (Strongest Acidic) 9.98 Chemaxon pKa (Strongest Basic) 8.23 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 8 Chemaxon Hydrogen Donor Count 2 Chemaxon Polar Surface Area 95.09 Å2 Chemaxon Rotatable Bond Count 8 Chemaxon Refractivity 152.71 m3·mol-1 Chemaxon Polarizability 58.51 Å3 Chemaxon Number of Rings 4 Chemaxon Bioavailability 1 Chemaxon Rule of Five No Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 208.53435 predictedDeepCCS 1.0 (2019) [M+H]+ 210.92992 predictedDeepCCS 1.0 (2019) [M+Na]+ 216.84242 predictedDeepCCS 1.0 (2019)
Targets
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- FDA Approved Drug Products: TRUSELTIQ (infigratinib) capsules, for oral use [Link]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInhibitor
- 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
- FDA Approved Drug Products: TRUSELTIQ (infigratinib) capsules, for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInhibitor
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- FDA Approved Drug Products: TRUSELTIQ (infigratinib) capsules, for oral use [Link]
Drug created at October 20, 2016 20:57 / Updated at October 02, 2021 21:28