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Identification
NamePalifermin
Accession NumberDB00039  (BIOD00042, BTD00042)
Typebiotech
Groupsapproved
Description

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

Protein structureDb00039
Protein chemical formulaC721H1142N202O204S9
Protein average weight16192.7000
Sequences
>Palifermin sequence
SYDYMEGGDIRVRRLFCRTQWYLRIDKRGKVKGTQEMKNNYNIMEIRTVAVGIVAIKGVE
SEFYLAMNKEGKLYAKKECNEDCNFKELILENHYNTYASAKWTHNGGEMFVALNQKGIPV
RGKKTKKEQKTAHFLPMAIT
Download FASTA Format
Synonyms
SynonymLanguageCode
FGF-7Not AvailableNot Available
Fibroblast growth factor- 7Not AvailableNot Available
HBGF-7Not AvailableNot Available
Keratinocyte growth factor precursorNot AvailableNot Available
KGFNot AvailableNot Available
SaltsNot Available
Brand names
NameCompany
KepivanceAmgen Inc
Brand mixturesNot Available
Categories
CAS number162394-19-6
Taxonomy
KingdomOrganic Compounds
SuperclassOrganic Acids
ClassCarboxylic Acids and Derivatives
SubclassAmino Acids, Peptides, and Analogues
Direct parentPeptides
Alternative parentsNot Available
SubstituentsNot Available
Classification descriptionNot Available
Pharmacology
IndicationFor treatment of oral mucositis associated with chemotherapy and radiation therapy.
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.
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
Metabolism
Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Powder, for solutionIntravenous
Prices
Unit descriptionCostUnit
Kepivance 6.25 mg vial1650.0USDvial
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
References
Synthesis ReferenceNot Available
General ReferenceNot Available
External Links
ResourceLink
UniProtP21781
GenbankM60828
PharmGKBPA164744014
Drug Product Database2274221
RxListhttp://www.rxlist.com/cgi/generic/kepivance.htm
Drugs.comhttp://www.drugs.com/cdi/palifermin.html
WikipediaPalifermin
ATC CodesV03AF08
AHFS Codes
  • 84:16.00
PDB Entries
FDA labelshow(113 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
BendamustineIncreases toxicity of bendamustine. Should not be administered within a 24 hour time period of antineoplastic agent administration.
PralatrexateIncreases the toxicity of pralatrexate. Avoid concomitant therapy or do not use palifermin within 24 hours after administration of pralatrexate.
Food InteractionsNot Available

Targets

1. Fibroblast growth factor receptor 2

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: binder

Components

Name UniProt ID Details
Fibroblast growth factor receptor 2 P21802 Details

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
  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
  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
  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
  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
  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
  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
  8. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed

2. Neuropilin-1

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Neuropilin-1 O14786 Details

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
  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
  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

3. Fibroblast growth factor receptor 1

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Fibroblast growth factor receptor 1 P11362 Details

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
  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
  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
  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
  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

4. Fibroblast growth factor receptor 4

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Fibroblast growth factor receptor 4 P22455 Details

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
  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
  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
  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
  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

5. Fibroblast growth factor receptor 3

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Fibroblast growth factor receptor 3 P22607 Details

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
  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
  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
  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
  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

6. Basement membrane-specific heparan sulfate proteoglycan core protein

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Basement membrane-specific heparan sulfate proteoglycan core protein P98160 Details

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
  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
  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
  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

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Drug created on June 13, 2005 07:24 / Updated on January 24, 2014 11:40