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Identification
NamePalifermin
Accession NumberDB00039  (BTD00042, BIOD00042)
TypeBiotech
GroupsApproved
DescriptionPalifermin is a recombinant human keratinocyte growth factor (KGF). It is 140 residues long, and is produced using E. coli.
Protein structureDb00039
Related Articles
Protein chemical formulaC721H1142N202O204S9
Protein average weight16192.7 Da
Sequences
>Palifermin sequence
SYDYMEGGDIRVRRLFCRTQWYLRIDKRGKVKGTQEMKNNYNIMEIRTVAVGIVAIKGVE
SEFYLAMNKEGKLYAKKECNEDCNFKELILENHYNTYASAKWTHNGGEMFVALNQKGIPV
RGKKTKKEQKTAHFLPMAIT
Download FASTA Format
Synonyms
FGF-7
Fibroblast growth factor- 7
HBGF-7
Keratinocyte growth factor precursor
KGF
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
KepivancePowder, for solution6.25 mgIntravenousSWEDISH ORPHAN BIOVITRUM AB (PUBL)2006-03-142016-01-30Canada
KepivanceInjection, powder, lyophilized, for solution6.25 mg/1.2mLIntravenousSWEDISH ORPHAN BIOVITRUM AB (PUBL)2009-12-15Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIQMS40680K6
CAS number162394-19-6
Pharmacology
IndicationFor treatment of oral mucositis associated with chemotherapy and radiation therapy.
Structured Indications
PharmacodynamicsUsed 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 actionKepivance 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.
TargetKindPharmacological actionActionsOrganismUniProt ID
Fibroblast growth factor receptor 2Proteinyes
binder
HumanP21802 details
Neuropilin-1ProteinunknownNot AvailableHumanO14786 details
Fibroblast growth factor receptor 1ProteinunknownNot AvailableHumanP11362 details
Fibroblast growth factor receptor 4ProteinunknownNot AvailableHumanP22455 details
Fibroblast growth factor receptor 3ProteinunknownNot AvailableHumanP22607 details
Basement membrane-specific heparan sulfate proteoglycan core proteinProteinunknownNot AvailableHumanP98160 details
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half lifeElimination half-life: 4.5 hours (range: 3.3-5.7 hours)
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
ArdeparinThe serum concentration of Palifermin can be increased when it is combined with Ardeparin.Approved, Withdrawn
BemiparinThe serum concentration of Palifermin can be increased when it is combined with Bemiparin.Approved
CertoparinThe serum concentration of Palifermin can be increased when it is combined with Certoparin.Approved
DalteparinThe serum concentration of Palifermin can be increased when it is combined with Dalteparin.Approved
EnoxaparinThe serum concentration of Palifermin can be increased when it is combined with Enoxaparin.Approved
HeparinThe serum concentration of Palifermin can be increased when it is combined with Heparin.Approved, Investigational
NadroparinThe serum concentration of Palifermin can be increased when it is combined with Nadroparin.Approved
ParnaparinThe serum concentration of Palifermin can be increased when it is combined with Parnaparin.Approved
ReviparinThe serum concentration of Palifermin can be increased when it is combined with Reviparin.Approved
TinzaparinThe serum concentration of Palifermin can be increased when it is combined with Tinzaparin.Approved
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesV03AF08
AHFS Codes
  • 84:16.00
PDB Entries
FDA labelDownload (113 KB)
MSDSNot Available
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
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.
PatentsNot Available
Properties
StateLiquid
Experimental Properties
PropertyValueSource
hydrophobicity-0.650Not Available
isoelectric point9.47Not Available
Taxonomy
DescriptionNot Available
KingdomOrganic Compounds
Super ClassOrganic Acids
ClassCarboxylic Acids and Derivatives
Sub ClassAmino Acids, Peptides, and Analogues
Direct ParentPeptides
Alternative ParentsNot Available
SubstituentsNot Available
Molecular FrameworkNot Available
External DescriptorsNot Available

Targets

Kind
Protein
Organism
Human
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 apoptosis, and in the regulation of embryonic development. Required for normal embryonic patterning, trophoblast function, limb bud development, lung morphogenesis, osteogenesis and skin development. Plays an...
Gene Name:
FGFR2
Uniprot ID:
P21802
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
Human
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 nervous system. It mediates the chemorepulsant activity of semaphorins. It binds to semaphorin 3A, The PLGF-2 isoform of PGF, The VEGF-165 isoform of VEGF and VEGF-B. Coexpression with KDR results in ...
Gene Name:
NRP1
Uniprot ID:
O14786
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
Human
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 and migration. Required for normal mesoderm patterning and correct axial organization during embryonic development, normal skeletogenesis and normal development of the gonadotropin-releasing hormone (...
Gene Name:
FGFR1
Uniprot ID:
P11362
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
Human
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 of lipid metabolism, bile acid biosynthesis, glucose uptake, vitamin D metabolism and phosphate homeostasis. Required for normal down-regulation of the expression of CYP7A1, the rate-limiting enzyme in...
Gene Name:
FGFR4
Uniprot ID:
P22455
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
Human
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 essential role in the regulation of chondrocyte differentiation, proliferation and apoptosis, and is required for normal skeleton development. Regulates both osteogenesis and postnatal bone mineraliz...
Gene Name:
FGFR3
Uniprot ID:
P22607
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
Human
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 is both size- and charge-selective. It serves as an attachment substrate for cells. Plays essential roles in vascularization. Critical for normal heart development and for regulating the vascular respo...
Gene Name:
HSPG2
Uniprot ID:
P98160
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 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23