NAV

Pemigatinib

Identification

Summary

Pemigatinibis a kinase inhibitor used to treat locally advanced or metastatic, unresectable cholangiocarcinoma in previously treated adult patients.

Brand Names
Pemazyre
Generic Name
Pemigatinib
DrugBank Accession Number
DB15102
Background

Pemigatinib is a small molecule kinase inhibitor with antitumour activity. It works by inhibiting fibroblast growth factor receptors (FGFRs), which are receptor tyrosine kinases that activate signalling pathways in tumour cells.1FGFRs gained attention as potential therapeutic targets in selected cancers, as FGFR gene alterations were observed in a wide variety of cancers including those of the urinary bladder, breast, ovary, prostate, endometrium, lung, and stomach.4Deregulated FGFR signalling pathway can lead the development of oncogenes and tumour-promoting physiological processes, such as cancer cell proliferation, enhanced angiogenesis, and evasion of cell death.2

In April 2020, pemigatinib was approved by the FDA for the treatment of unresectable locally advanced or metastatic cholangiocarcinoma in previously treated adult patients with a fibroblast growth factor receptor 2 (FGFR2) gene fusion or other rearrangements as detected by an FDA-approved test.6Cholangiocarcinoma is the most common primary malignancy affecting the biliary tract and the second most common primary hepatic malignancy. This malignancy accounts for 15% to 20% of primary hepatobiliary malignancies, which account for 13% of overall cancer-related global mortality. With increasing research on the pathogenesis of cholangiocarcinoma and potential therapeutic targets for anticancer drug treatment, recent studies show that up to 45% of patients with intrahepatic cholangiocarcinoma exhibited gene rearrangements resulting in oncogenic fibroblast growth factor 2 (FGFR2) fusion proteins.3The FDA-approved indication for pemigatinib was granted under accelerated approval based on the overall response rate and duration of response in pre-marketing clinical trials. Pemigatinib is marketed under the brand name Pemazyre, and it is available as oral tablets.5

Type
Small Molecule
Groups
Approved, Investigational
Structure
 3D
Similar Structures
Weight
Average: 487.508
Monoisotopic: 487.203110695
Chemical Formula
C24H27F2N5O4
Synonyms
  • INCB054828
  • Pemigatinib

Pharmacology

Indication

Pemigatinib is indicated for the treatment of unresectable locally advanced or metastatic cholangiocarcinoma in previously-treated adult patients with a fibroblast growth factor receptor 2 (FGFR2) fusion or other rearrangement as detected by an FDA-approved test.5

It is also indicated for the treatment of adults with relapsed or refractory myeloid/lymphoid neoplasms (MLNs) with FGFR1 rearrangement.7

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Associated Conditions
Contraindications & Blackbox Warnings
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Pharmacodynamics

Pemigatinib is a small molecule kinase inhibitor that exerts anti-tumour activity through inhibition of fibroblast growth factor receptors (FGFRs).2With an IC50of less than 2 nM, pemigatinib displays potent inhibition of FGFR1, FGFR2, and FGFR3. In mouse xenograft models of human tumours with FGFR1, FGFR2, or FGFR3 alterations, pemigatinib exhibited potent anti-tumour activity by suppressing the growth of xenografted tumour models. It also showed efficacy against a patient-derived xenograft model of cholangiocarcinoma that expressed an oncogenic FGFR2 Transformer-2 beta homolog (TRA2b) fusion protein.2,5Pemigatinib also inhibited FGFR4in vitro, however at a concentration approximately 100 times higher than those that inhibit FGFR1, 2, and 3.5

Mechanism of action

Fibroblast growth factor receptor (FGFR) is a receptor tyrosine kinase involved in activating signalling pathways that promote cell proliferation, survival, and migration, as well as growth arrest and cellular differentiation.2The initiation of the FGFR signalling pathway requires the binding of its natural ligand, fibroblast growth factor (FGF). Once FGF binds to the extracellular ligand-binding domain of the receptor, FGFRs dimerize and autophosphorylate the tyrosine residue in the intracellular tyrosine-kinase domain, leading to the activation of the tyrosine kinase.1Downstream cascades involve phosphorylation of multiple intracellular signalling proteins, such as phosphatidylinositol 3 kinase (PI3K)-AKT and RAS/mitogen-activated protein kinase (MAPK), and phospholipase Cγ, which activates the protein kinase C pathway.2,1FGFR-mediated pathway ultimately promotes cell growth, differentiation, survival, angiogenesis, and organogenesis, depending on cell type. Expressed in different isoforms in various tissues and cell lines, FGFRs are not constitutively active in normal cells.1However, FGFR1, FGFR2, or FGFR3 alterations in certain tumours can lead to constitutive FGFR activation and aberrant FGFR signalling, supporting the proliferation and survival of malignant cells.5

Pemigatinib inhibits FGFR1, FGFR2, and FGFR3, blocking their signalling pathways and decreasing cell viability in cancer cell lines with activating FGFR amplification and fusions that resulted in constitutive activation of FGFR signalling.5Genetic alterations in FGFR1, FGFR2, and FGFR3 (such as amplification, missense, or fusion mutations in the coding region) leading to constitutive activation of FGFR signalling pathways are observed in various tumours.1,4However, alterations in FGFR genes are demonstrated in selected patients and do not always imply oncogene development. Therefore, it is imperative that fusion or rearrangement of FGFRs are demonstrated through tests prior to initiation of drug therapy.2

Target Actions Organism
AFibroblast growth factor receptor 1
inhibitor
 Humans
AFibroblast growth factor receptor 2
inhibitor
 Humans
AFibroblast growth factor receptor 3
inhibitor
 Humans
UFibroblast growth factor receptor 4
inhibitor
 Humans
Absorption

Following administration of a single oral dose of 13.5 mg pemigatinib, the median Tmax was 1.13 (0.50-6.00) hours. The steady state was reached within 4 days following repeated once daily dosing, with the median drug accumulation ratio of 1.63 (range 0.63 to 3.28). Steady-state concentration of pemigatinib increased in a dose-proportional manner over the dose range of 1 to 20 mg, which is about 0.07 to 1.5 times the recommended dose. The mean steady-state AUC and Cmax were 2620 nM x h (54% CV) and 236 nM, respectively.5

Volume of distribution

The apparent volume of distribution was 235 L (60.8% CV) following a single oral dose of 13.5 mg pemigatinib.5

Protein binding

Thein vitroserum protein binding of pemigatinib was 90.6% at drug concentrations ranging from 1 to 10 µM.5

Metabolism

Pemigatinib is predominantly metabolized by the CYP3A4 enzymein vitro.5Its specific metabolic pathway and resulting metabolites have not yet been characterized.

Route of elimination

Following oral administration of a single radiolabeled dose of 11 mg pemigatinib, about 82.4% of the dose was recovered in feces. Of this recovered drug, about 1.4% of the dose was unchanged parent compound. About 12.6% of the dose was recovered in urine, where 1% of the dose was unchanged.5

Half-life

Following administration of a single oral dose of 13.5 mg pemigatinib, the geometric mean elimination half-life (t½) of pemigatinib was 15.4 (51.6% CV) hours.5

Clearance

Following administration of a single oral dose of 13.5 mg pemigatinib, the geometric mean apparent clearance (CL/F) was 10.6 L/h (54% CV).5

Adverse Effects
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Toxicity

There is limited information on the LD50value and overdose profile of pemigatinib.

In animal studies, pemigatinib caused fetal harm and embryo-fetal death in pregnant rats. FDA advises nursing women to avoid breastfeeding when receiving pemigatinib. Physeal and cartilage dysplasia were present in multiple bones of rats and non-human primates with pemigatinib exposures lower than the human exposure at the clinical dose of 13.5 mg.5

Pathways
Not Available
Pharmacogenomic Effects/ADRsBrowse all" title="" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
Not Available

Interactions

Drug InteractionsLearn More" title="" 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
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Abametapir The serum concentration of Pemigatinib can be increased when it is combined with Abametapir.
Ambroxol The risk or severity of methemoglobinemia can be increased when Pemigatinib is combined with Ambroxol.
Amiodarone The metabolism of Pemigatinib can be decreased when combined with Amiodarone.
Amprenavir The metabolism of Pemigatinib can be decreased when combined with Amprenavir.
Apalutamide The metabolism of Pemigatinib can be increased when combined with Apalutamide.
Aprepitant The metabolism of Pemigatinib can be decreased when combined with Aprepitant.
Articaine The risk or severity of methemoglobinemia can be increased when Pemigatinib is combined with Articaine.
Atazanavir The metabolism of Pemigatinib can be decreased when combined with Atazanavir.
Avanafil The serum concentration of Avanafil can be increased when it is combined with Pemigatinib.
Benzocaine The risk or severity of methemoglobinemia can be increased when Pemigatinib is combined with Benzocaine.
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Food Interactions
  • Avoid grapefruit products. Grapefruit may increase drug levels and adverse effects.
  • Take at the same time every day.
  • Take with or without food. A high-fat or high-calorie meal does not have clinically significant effects on drug concentrations.

Products

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Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image
Pemazyre Tablet 13.5 mg Oral Incyte Corporation 2021-11-26 Not applicable Canada flag
Pemazyre Tablet 13.5 mg/1 Oral Incyte Corporation 2020-04-17 Not applicable US flag
Pemazyre Tablet 9 mg Oral Incyte Biosciences Distribution B.V. 2021-05-07 Not applicable EU flag
Pemazyre Tablet 4.5 mg Oral Incyte Biosciences Distribution B.V. 2021-05-07 Not applicable EU flag
Pemazyre Tablet 9 mg Oral Incyte Corporation 2021-11-30 Not applicable Canada flag
Pemazyre Tablet 13.5 mg Oral Incyte Biosciences Distribution B.V. 2021-05-07 Not applicable EU flag
Pemazyre Tablet 9 mg/1 Oral Incyte Corporation 2020-04-17 Not applicable US flag
Pemazyre Tablet 9 mg Oral Incyte Biosciences Distribution B.V. 2021-05-07 Not applicable EU flag
Pemazyre Tablet 4.5 mg Oral Incyte Biosciences Distribution B.V. 2021-05-07 Not applicable EU flag
Pemazyre Tablet 4.5 mg Oral Incyte Corporation 2022-01-06 Not applicable Canada flag

Categories

ATC Codes
L01EN02 — Pemigatinib
Drug Categories
Classification
Not classified
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
Y6BX7BL23K
CAS number
1513857-77-6
InChI Key
HCDMJFOHIXMBOV-UHFFFAOYSA-N
InChI
InChI=1S/C24H27F2N5O4/c1-4-30-21-14(11-27-23-16(21)9-15(28-23)13-29-5-7-35-8-6-29)12-31(24(30)32)22-19(25)17(33-2)10-18(34-3)20(22)26/h9-11H,4-8,12-13H2,1-3H3,(H,27,28)
IUPAC Name
11-(2,6-difluoro-3,5-dimethoxyphenyl)-13-ethyl-4-[(morpholin-4-yl)methyl]-5,7,11,13-tetraazatricyclo[7.4.0.0^{2,6}]trideca-1,3,6,8-tetraen-12-one
SMILES
CCN1C(=O)N(CC2=CN=C3NC(CN4CCOCC4)=CC3=C12)C1=C(F)C(OC)=CC(OC)=C1F

References

General References
  1. Casadei C, Dizman N,谢皮G, Cursano MC,低音部U, Santini D, Pal SK, De Giorgi U: Targeted therapies for advanced bladder cancer: new strategies with FGFR inhibitors. Ther Adv Med Oncol. 2019 Nov 25;11:1758835919890285. doi: 10.1177/1758835919890285. eCollection 2019. [Article]
  2. Liu PCC, Koblish H, Wu L, Bowman K, Diamond S, DiMatteo D, Zhang Y, Hansbury M, Rupar M, Wen X, Collier P, Feldman P, Klabe R, Burke KA, Soloviev M, Gardiner C, He X, Volgina A, Covington M, Ruggeri B, Wynn R, Burn TC, Scherle P, Yeleswaram S, Yao W, Huber R, Hollis G: INCB054828 (pemigatinib), a potent and selective inhibitor of fibroblast growth factor receptors 1, 2, and 3, displays activity against genetically defined tumor models. PLoS One. 2020 Apr 21;15(4):e0231877. doi: 10.1371/journal.pone.0231877. eCollection 2020. [Article]
  3. Blechacz B: Cholangiocarcinoma: Current Knowledge and New Developments. Gut Liver. 2017 Jan 15;11(1):13-26. doi: 10.5009/gnl15568. [Article]
  4. Roskoski R Jr: The role of fibroblast growth factor receptor (FGFR) protein-tyrosine kinase inhibitors in the treatment of cancers including those of the urinary bladder. Pharmacol Res. 2020 Jan;151:104567. doi: 10.1016/j.phrs.2019.104567. Epub 2019 Nov 23. [Article]
  5. FDA Approved Drug Products: PEMAZYRE (pemigatinib) tablets, for oral use [Link]
  6. FDA Resources for Information | Approved Drugs: FDA grants accelerated approval to pemigatinib for cholangiocarcinoma with an FGFR2 rearrangement or fusion [Link]
  7. FDA Approved Drug Products: PEMAZYRE (pemigatinib) tablets, for oral use (August 2022) [Link]
Human Metabolome Database
HMDB0304863
ChemSpider
68007304
BindingDB
301310
RxNav
2359268
ChEMBL
CHEMBL4297522
PDBe Ligand
8ZF
Wikipedia
Pemigatinib
PDB Entries
7wcl

Clinical Trials

Clinical TrialsLearn More" title="" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count
3 Recruiting Treatment Metastatic Cholangiocarcinoma/Unresectable Cholangiocarcinoma 1
2 Active Not Recruiting Treatment Advanced Malignant Neoplasm 1
2 Active Not Recruiting Treatment Cancer of Unknown Primary Site 1
2 Active Not Recruiting Treatment Cholangiocarcinoma 1
2 Active Not Recruiting Treatment FGFR1 Gene Amplification/FGFR1 Gene Mutation/FGFR1 Gene Translocation/FGFR2 Gene Amplification/FGFR2 Gene Mutation/FGFR2 Gene Translocation/FGFR3 Gene Amplification/FGFR3 Gene Mutation/FGFR3 Gene Translocation/Stage III Colorectal Cancer AJCC v8/Stage IIIA Colorectal Cancer AJCC v8/Stage IIIB Colorectal Cancer AJCC v8/阶段IIIC结肠直肠癌AJCC v8/Stage IV Colorectal Cancer/Stage IV Colorectal Cancer AJCC v8/Stage IVA Colorectal Cancer AJCC v8/Stage IVB Colorectal Cancer AJCC v8/Stage IVC Colorectal Cancer AJCC v8/Unresectable Colorectal Carcinoma 1
2 Active Not Recruiting Treatment Myeloproliferative Neoplasms (MPNs) 1
2 Completed Treatment Cholangiocarcinoma 1
2 Completed Treatment Urothelial Cancer 1
2 Not Yet Recruiting Treatment Advanced Intrahepatic Cholangiocarcinoma 1
2 Not Yet Recruiting Treatment Advanced Non-Small Cell Lung Cancer (NSCLC) 1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
Form Route Strength
Tablet Oral 13.5 mg/1
Tablet Oral 13.5 mg
Tablet Oral 4.5 mg
Tablet Oral 4.5 mg/1
Tablet Oral 9 mg/1
Tablet Oral 9 mg
Prices
Not Available
Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region
US10131667 No 2018-11-20 2033-06-12 US flag
US9611267 No 2017-04-04 2035-01-30 US flag
US11466004 No 2019-05-03 2039-05-03 US flag

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
Property Value Source
Water Solubility 0.144 mg/mL ALOGPS
logP 2.26 ALOGPS
logP 1.82 Chemaxon
logS -3.5 ALOGPS
pKa (Strongest Acidic) 13.88 Chemaxon
pKa最强(基本) 5.9 Chemaxon
Physiological Charge 0 Chemaxon
Hydrogen Acceptor Count 6 Chemaxon
Hydrogen Donor Count 1 Chemaxon
Polar Surface Area 83.16 Å2 Chemaxon
Rotatable Bond Count 6 Chemaxon
Refractivity 125.32 m3·mol-1 Chemaxon
Polarizability 49.93 Å3 Chemaxon
Number of Rings 5 Chemaxon
Bioavailability 1 Chemaxon
Rule of Five Yes 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
Not Available

Targets

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Details 1.Fibroblast growth factor receptor 1
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
Curator comments
在刘的临床表征研究et al. (2020), the IC50 value was 0.4 nM.
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
分子量
91866.935 Da
References
  1. Liu PCC, Koblish H, Wu L, Bowman K, Diamond S, DiMatteo D, Zhang Y, Hansbury M, Rupar M, Wen X, Collier P, Feldman P, Klabe R, Burke KA, Soloviev M, Gardiner C, He X, Volgina A, Covington M, Ruggeri B, Wynn R, Burn TC, Scherle P, Yeleswaram S, Yao W, Huber R, Hollis G: INCB054828 (pemigatinib), a potent and selective inhibitor of fibroblast growth factor receptors 1, 2, and 3, displays activity against genetically defined tumor models. PLoS One. 2020 Apr 21;15(4):e0231877. doi: 10.1371/journal.pone.0231877. eCollection 2020. [Article]
  2. FDA Approved Drug Products: PEMAZYRE (pemigatinib) tablets, for oral use [Link]
Details 2.Fibroblast growth factor receptor 2
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
Curator comments
在刘的临床表征研究et al. (2020), the IC50 value was 0.5 nM.
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
分子量
92024.29 Da
References
  1. Liu PCC, Koblish H, Wu L, Bowman K, Diamond S, DiMatteo D, Zhang Y, Hansbury M, Rupar M, Wen X, Collier P, Feldman P, Klabe R, Burke KA, Soloviev M, Gardiner C, He X, Volgina A, Covington M, Ruggeri B, Wynn R, Burn TC, Scherle P, Yeleswaram S, Yao W, Huber R, Hollis G: INCB054828 (pemigatinib), a potent and selective inhibitor of fibroblast growth factor receptors 1, 2, and 3, displays activity against genetically defined tumor models. PLoS One. 2020 Apr 21;15(4):e0231877. doi: 10.1371/journal.pone.0231877. eCollection 2020. [Article]
  2. FDA Approved Drug Products: PEMAZYRE (pemigatinib) tablets, for oral use [Link]
Details 3.Fibroblast growth factor receptor 3
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
Curator comments
在刘的临床表征研究et al. (2020), the IC50 value was 1.0 nM.
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
分子量
87708.905 Da
References
  1. Liu PCC, Koblish H, Wu L, Bowman K, Diamond S, DiMatteo D, Zhang Y, Hansbury M, Rupar M, Wen X, Collier P, Feldman P, Klabe R, Burke KA, Soloviev M, Gardiner C, He X, Volgina A, Covington M, Ruggeri B, Wynn R, Burn TC, Scherle P, Yeleswaram S, Yao W, Huber R, Hollis G: INCB054828 (pemigatinib), a potent and selective inhibitor of fibroblast growth factor receptors 1, 2, and 3, displays activity against genetically defined tumor models. PLoS One. 2020 Apr 21;15(4):e0231877. doi: 10.1371/journal.pone.0231877. eCollection 2020. [Article]
Details 4.Fibroblast growth factor receptor 4
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Curator comments
在刘的临床表征研究et al. (2020), the IC50 value was 30 nM, at a concentration approximately 100 times higher than those that inhibit FGFR1, 2, and 3.
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
分子量
87953.535 Da
References
  1. Liu PCC, Koblish H, Wu L, Bowman K, Diamond S, DiMatteo D, Zhang Y, Hansbury M, Rupar M, Wen X, Collier P, Feldman P, Klabe R, Burke KA, Soloviev M, Gardiner C, He X, Volgina A, Covington M, Ruggeri B, Wynn R, Burn TC, Scherle P, Yeleswaram S, Yao W, Huber R, Hollis G: INCB054828 (pemigatinib), a potent and selective inhibitor of fibroblast growth factor receptors 1, 2, and 3, displays activity against genetically defined tumor models. PLoS One. 2020 Apr 21;15(4):e0231877. doi: 10.1371/journal.pone.0231877. eCollection 2020. [Article]
  2. FDA Approved Drug Products: PEMAZYRE (pemigatinib) tablets, for oral use [Link]

Enzymes

Details 1.Cytochrome P450 3A4
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
分子量
57342.67 Da
References
  1. FDA Approved Drug Products: PEMAZYRE (pemigatinib) tablets, for oral use [Link]

Transporters

Details 1.P-glycoprotein 1
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
Inhibitor
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
分子量
141477.255 Da
References
  1. FDA Approved Drug Products: PEMAZYRE (pemigatinib) tablets, for oral use [Link]
Details 2.ATP-binding cassette sub-family G member 2
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
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
分子量
72313.47 Da
References
  1. FDA Approved Drug Products: PEMAZYRE (pemigatinib) tablets, for oral use [Link]
Details 3.溶质载体家庭22个成员2
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Inhibitor
Curator comments
The FDA label states that pemigatinib may increase serum creatinine by interfering with OCT2- and MATE1-mediated renal tubular secretion of creatinine; however, this may not affect glomerular function.
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
溶质载体家庭22个成员2
分子量
62579.99 Da
References
  1. FDA Approved Drug Products: PEMAZYRE (pemigatinib) tablets, for oral use [Link]
Details 4.Multidrug and toxin extrusion protein 1
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Inhibitor
Curator comments
The FDA label states that pemigatinib may increase serum creatinine by interfering with OCT2- and MATE1-mediated renal tubular secretion of creatinine; however, this may not affect glomerular function.
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
分子量
61921.585 Da
References
  1. FDA Approved Drug Products: PEMAZYRE (pemigatinib) tablets, for oral use [Link]

Drug created at May 20, 2019 14:50 / Updated at April 28, 2023 03:25