Palifermin

Identification

Name
Palifermin
Accession Number
DB00039
Description

Palifermin is a recombinant human keratinocyte growth factor (KGF). It is 140 residues long, and is produced using E. coli.

Type
Biotech
Groups
Approved
Biologic Classification
Protein Based Therapies
Other protein based therapies
Protein Structure
Db00039
Protein Chemical Formula
C721H1142N202O204S9
Protein Average Weight
16192.7 Da
Sequences
>Palifermin sequence
MSYDYMEGGDIRVRRLFCRTQWYLRIDKRGKVKGTQEMKNNYNIMEIRTVAVGIVAIKGV
ESEFYLAMNKEGKLYAKKECNEDCNFKELILENHYNTYASAKWTHNGGEMFVALNQKGIP
VRGKKTKKEQKTAHFLPMAIT
Download FASTA Format
Synonyms
  • 24-163 fibroblast growth factor 7 (human)
  • Palifermina

Pharmacology

Indication

For treatment of oral mucositis associated with chemotherapy and radiation therapy.

Associated Conditions
Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
Learn More
Pharmacodynamics

Used in the prevention or treatment of oral mucoscitis (mouth ulcers arising from chemotherapy), Kepivance binds to the human keratinocyte growth factor (KGF) receptor on buccal cell surfaces. Kepivance acts as both a cell growth and survival factor by stimulating epithelial cell proliferation, differentiation, and migration around the tongue and mouth. The KGF receptor is found on many tissues particularly around the tongue, esophagus, salivary gland and other gastro-intestinal tract organs.

Mechanism of action

Kepivance binds to the human keratinocyte growth factor (KGF) receptor found on buccal cell surfaces. The binding activates a Ras-MapK (Map kinase) signaling pathway which leads to the transcriptional activation of many proteins important for cell growth and survival.

TargetActionsOrganism
AFibroblast growth factor receptor 2
binder
Humans
UNeuropilin-1Not AvailableHumans
UFibroblast growth factor receptor 1Not AvailableHumans
UFibroblast growth factor receptor 4Not AvailableHumans
UFibroblast growth factor receptor 3Not AvailableHumans
UBasement membrane-specific heparan sulfate proteoglycan core proteinNot AvailableHumans
Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half-life

Elimination half-life: 4.5 hours (range: 3.3-5.7 hours)

Clearance
Not Available
Adverse Effects
Learn about our commercial Adverse Effects data.
Learn More
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
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
AldesleukinThe therapeutic efficacy of Palifermin can be decreased when used in combination with Aldesleukin.
AlemtuzumabThe therapeutic efficacy of Palifermin can be decreased when used in combination with Alemtuzumab.
AltretamineThe therapeutic efficacy of Palifermin can be decreased when used in combination with Altretamine.
AmsacrineThe therapeutic efficacy of Palifermin can be decreased when used in combination with Amsacrine.
ArdeparinThe serum concentration of Palifermin can be increased when it is combined with Ardeparin.
Arsenic trioxideThe therapeutic efficacy of Palifermin can be decreased when used in combination with Arsenic trioxide.
AzacitidineThe therapeutic efficacy of Palifermin can be decreased when used in combination with Azacitidine.
BelinostatThe therapeutic efficacy of Palifermin can be decreased when used in combination with Belinostat.
BemiparinThe serum concentration of Palifermin can be increased when it is combined with Bemiparin.
BendamustineThe therapeutic efficacy of Palifermin can be decreased when used in combination with Bendamustine.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions
Not Available

Products

Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
KepivanceInjection, powder, lyophilized, for solution6.25 mg/1.2mLIntravenousSWEDISH ORPHAN BIOVITRUM AB (PUBL)2009-12-15Not applicableUs
KepivanceInjection6.25 mg/1mLIntravenousAmgen2004-12-152009-12-15Us
KepivancePowder, for solution6.25 mgIntravenousSWEDISH ORPHAN BIOVITRUM AB (PUBL)2006-03-142016-01-30Canada
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

    Learn more

Categories

ATC Codes
V03AF08 — Palifermin
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
Not Available
Kingdom
Organic Compounds
Super Class
Organic Acids
Class
Carboxylic Acids and Derivatives
Sub Class
Amino Acids, Peptides, and Analogues
Direct Parent
Peptides
Alternative Parents
Not Available
Substituents
Not Available
Molecular Framework
Not Available
External Descriptors
Not Available

Chemical Identifiers

UNII
QMS40680K6
CAS number
162394-19-6

References

General References
Not Available
UniProt
P21781
Genbank
M60828
PubChem Substance
46506691
RxNav
196319
ChEMBL
CHEMBL1201821
Therapeutic Targets Database
DAP001026
PharmGKB
PA164744014
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Palifermin
FDA label
Download (113 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedPreventionMultiple Myeloma (MM) / Non-Hodgkin's Lymphoma (NHL)1
3CompletedSupportive CareLeukemias / Malignancies / Malignant Lymphomas1
3CompletedSupportive CareMultiple Myeloma (MM)1
3CompletedTreatmentHead and Neck Carcinoma1
3CompletedTreatmentHead and Neck Carcinoma / Mucositis / Squamous Cell Carcinoma (SCC) / Stomatitis / Tumors, Solid1
3RecruitingTreatmentLeukemias / Mucositis / Oral Complications1
3TerminatedSupportive CareHead and Neck Carcinoma / Mucositis / Pain / Radiation Toxicity1
3Unknown StatusPreventionMucositis1
2Active Not RecruitingTreatmentAcute Myeloid Leukemia (AML) / Advanced Myelodysplastic Syndromes1
2CompletedPreventionOral Mucositis / Sarcomas1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Amgen Inc.
  • Baxter International Inc.
  • BioVitrum AB
Dosage Forms
FormRouteStrength
InjectionIntravenous6.25 mg/1mL
Injection, powder, lyophilized, for solutionIntravenous6.25 mg/1.2mL
Powder, for solutionIntravenous6.25 mg
Prices
Unit descriptionCostUnit
Kepivance 6.25 mg vial1650.0USD vial
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Liquid
Experimental Properties
PropertyValueSource
hydrophobicity-0.650Not Available
isoelectric point9.47Not Available

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Binder
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. Beaven AW, Shea TC: Recombinant human keratinocyte growth factor palifermin reduces oral mucositis and improves patient outcomes after stem cell transplant. Drugs Today (Barc). 2007 Jul;43(7):461-73. [PubMed:17728847]
  2. Radtke ML, Kolesar JM: Palifermin (Kepivance) for the treatment of oral mucositis in patients with hematologic malignancies requiring hematopoietic stem cell support. J Oncol Pharm Pract. 2005 Sep;11(3):121-5. [PubMed:16390600]
  3. Huang YW, Wang LS, Chang HL, Ye W, Shu S, Sugimoto Y, Lin YC: Effect of keratinocyte growth factor on cell viability in primary cultured human prostate cancer stromal cells. J Steroid Biochem Mol Biol. 2006 Jul;100(1-3):24-33. Epub 2006 Jul 18. [PubMed:16854582]
  4. Patrie KM, Kudla AJ, Olwin BB, Chiu IM: Conservation of ligand specificity between the mammalian and amphibian fibroblast growth factor receptors. J Biol Chem. 1995 Dec 1;270(48):29018-24. [PubMed:7499435]
  5. Cardoso WV, Itoh A, Nogawa H, Mason I, Brody JS: FGF-1 and FGF-7 induce distinct patterns of growth and differentiation in embryonic lung epithelium. Dev Dyn. 1997 Mar;208(3):398-405. [PubMed:9056643]
  6. Berman B, Ostrovsky O, Shlissel M, Lang T, Regan D, Vlodavsky I, Ishai-Michaeli R, Ron D: Similarities and differences between the effects of heparin and glypican-1 on the bioactivity of acidic fibroblast growth factor and the keratinocyte growth factor. J Biol Chem. 1999 Dec 17;274(51):36132-8. [PubMed:10593896]
  7. Zhu X, Lee K, Asa SL, Ezzat S: Epigenetic silencing through DNA and histone methylation of fibroblast growth factor receptor 2 in neoplastic pituitary cells. Am J Pathol. 2007 May;170(5):1618-28. [PubMed:17456767]
  8. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Vascular endothelial growth factor-activated receptor activity
Specific Function
The membrane-bound isoform 1 is a receptor involved in the development of the cardiovascular system, in angiogenesis, in the formation of certain neuronal circuits and in organogenesis outside the ...
Gene Name
NRP1
Uniprot ID
O14786
Uniprot Name
Neuropilin-1
Molecular Weight
103133.62 Da
References
  1. Beer HD, Vindevoghel L, Gait MJ, Revest JM, Duan DR, Mason I, Dickson C, Werner S: Fibroblast growth factor (FGF) receptor 1-IIIb is a naturally occurring functional receptor for FGFs that is preferentially expressed in the skin and the brain. J Biol Chem. 2000 May 26;275(21):16091-7. [PubMed:10821861]
  2. Friedl A, Chang Z, Tierney A, Rapraeger AC: Differential binding of fibroblast growth factor-2 and -7 to basement membrane heparan sulfate: comparison of normal and abnormal human tissues. Am J Pathol. 1997 Apr;150(4):1443-55. [PubMed:9094999]
  3. Wang F, Lu W, McKeehan K, Mohamedali K, Gabriel JL, Kan M, McKeehan WL: Common and specific determinants for fibroblast growth factors in the ectodomain of the receptor kinase complex. Biochemistry. 1999 Jan 5;38(1):160-71. [PubMed:9890894]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
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. Ostrovsky O, Berman B, Gallagher J, Mulloy B, Fernig DG, Delehedde M, Ron D: Differential effects of heparin saccharides on the formation of specific fibroblast growth factor (FGF) and FGF receptor complexes. J Biol Chem. 2002 Jan 25;277(4):2444-53. Epub 2001 Nov 19. [PubMed:11714710]
  2. Sher I, Lang T, Lubinsky-Mink S, Kuhn J, Adir N, Chatterjee S, Schomburg D, Ron D: Identification of residues important both for primary receptor binding and specificity in fibroblast growth factor-7. J Biol Chem. 2000 Nov 10;275(45):34881-6. [PubMed:10950949]
  3. Matsubara A, Yasumoto H, Usui T: Hormone Refractory Prostate Cancer and Fibroblast Growth Factor Receptor. Breast Cancer. 1999 Oct 25;6(4):320-324. [PubMed:11091737]
  4. Lu W, Luo Y, Kan M, McKeehan WL: Fibroblast growth factor-10. A second candidate stromal to epithelial cell andromedin in prostate. J Biol Chem. 1999 Apr 30;274(18):12827-34. [PubMed:10212269]
  5. Wang F, Lu W, McKeehan K, Mohamedali K, Gabriel JL, Kan M, McKeehan WL: Common and specific determinants for fibroblast growth factors in the ectodomain of the receptor kinase complex. Biochemistry. 1999 Jan 5;38(1):160-71. [PubMed:9890894]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
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. Imagawa W, Cunha GR, Young P, Nandi S: Keratinocyte growth factor and acidic fibroblast growth factor are mitogens for primary cultures of mammary epithelium. Biochem Biophys Res Commun. 1994 Nov 15;204(3):1165-9. [PubMed:7526860]
  2. Sher I, Lang T, Lubinsky-Mink S, Kuhn J, Adir N, Chatterjee S, Schomburg D, Ron D: Identification of residues important both for primary receptor binding and specificity in fibroblast growth factor-7. J Biol Chem. 2000 Nov 10;275(45):34881-6. [PubMed:10950949]
  3. Sannes PL, Khosla J, Li CM, Pagan I: Sulfation of extracellular matrices modifies growth factor effects on type II cells on laminin substrata. Am J Physiol. 1998 Oct;275(4 Pt 1):L701-8. [PubMed:9755102]
  4. Luo Y, Lu W, Mohamedali KA, Jang JH, Jones RB, Gabriel JL, Kan M, McKeehan WL: The glycine box: a determinant of specificity for fibroblast growth factor. Biochemistry. 1998 Nov 24;37(47):16506-15. [PubMed:9843417]
  5. Yamanaka T, Sakamoto A, Tanaka Y, Zhang Y, Hayashido Y, Toratani S, Akagawa Y, Okamoto T: Isolation and serum-free culture of epithelial cells derived from epithelial rests of Malassez in human periodontal ligament. In Vitro Cell Dev Biol Anim. 2000 Sep;36(8):548-53. [PubMed:11149756]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
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. Cancilla B, Davies A, Cauchi JA, Risbridger GP, Bertram JF: Fibroblast growth factor receptors and their ligands in the adult rat kidney. Kidney Int. 2001 Jul;60(1):147-55. [PubMed:11422746]
  2. Yamanaka T, Sakamoto A, Tanaka Y, Zhang Y, Hayashido Y, Toratani S, Akagawa Y, Okamoto T: Isolation and serum-free culture of epithelial cells derived from epithelial rests of Malassez in human periodontal ligament. In Vitro Cell Dev Biol Anim. 2000 Sep;36(8):548-53. [PubMed:11149756]
  3. Beer HD, Vindevoghel L, Gait MJ, Revest JM, Duan DR, Mason I, Dickson C, Werner S: Fibroblast growth factor (FGF) receptor 1-IIIb is a naturally occurring functional receptor for FGFs that is preferentially expressed in the skin and the brain. J Biol Chem. 2000 May 26;275(21):16091-7. [PubMed:10821861]
  4. Launay C, Fromentoux V, Thery C, Shi DL, Boucaut JC: Comparative analysis of the tissue distribution of three fibroblast growth factor receptor mRNAs during amphibian morphogenesis. Differentiation. 1994 Dec;58(2):101-11. [PubMed:7890137]
  5. Mummery CL, van Rooyen M, Bracke M, van den Eijnden-van Raaij J, van Zoelen EJ, Alitalo K: Fibroblast growth factor-mediated growth regulation and receptor expression in embryonal carcinoma and embryonic stem cells and human germ cell tumours. Biochem Biophys Res Commun. 1993 Feb 26;191(1):188-95. [PubMed:7680555]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Protein c-terminus binding
Specific Function
Integral component of basement membranes. Component of the glomerular basement membrane (GBM), responsible for the fixed negative electrostatic membrane charge, and which provides a barrier which i...
Gene Name
HSPG2
Uniprot ID
P98160
Uniprot Name
Basement membrane-specific heparan sulfate proteoglycan core protein
Molecular Weight
468826.45 Da
References
  1. Berman B, Ostrovsky O, Shlissel M, Lang T, Regan D, Vlodavsky I, Ishai-Michaeli R, Ron D: Similarities and differences between the effects of heparin and glypican-1 on the bioactivity of acidic fibroblast growth factor and the keratinocyte growth factor. J Biol Chem. 1999 Dec 17;274(51):36132-8. [PubMed:10593896]
  2. Sharma B, Handler M, Eichstetter I, Whitelock JM, Nugent MA, Iozzo RV: Antisense targeting of perlecan blocks tumor growth and angiogenesis in vivo. J Clin Invest. 1998 Oct 15;102(8):1599-608. [PubMed:9788974]
  3. Iwabuchi T, Goetinck PF: Syndecan-4 dependent FGF stimulation of mouse vibrissae growth. Mech Dev. 2006 Nov;123(11):831-41. Epub 2006 Aug 12. [PubMed:16989989]
  4. Asada N, Tanaka Y, Hayashido Y, Toratani S, Kan M, Kitamoto M, Nakanishi T, Kajiyama G, Chayama K, Okamoto T: Expression of fibroblast growth factor receptor genes in human hepatoma-derived cell lines. In Vitro Cell Dev Biol Anim. 2003 Jul-Aug;39(7):321-8. [PubMed:14753849]

Drug created on June 13, 2005 07:24 / Updated on June 12, 2020 10:51

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