Palifermin

Identification

Summary

Palifermin is a form of recombinant human keratinocyte growth factor used to prevent and treat oral mucositis following radiation or chemotherapy.

Brand Names
Kepivance
Generic Name
Palifermin
DrugBank Accession Number
DB00039
Background

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

Palifermin was granted FDA approval on 15 December 2004.4

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)
  • Palifermin
  • Palifermina

Pharmacology

Indication

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

Pharmacology
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Drug Discovery
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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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

Palifermin has been shown to protect oral and intestinal epithelia from the effects of radiation and chemotherapy, though the exact mechanism is not well understood.1 As a recombinant keratinocyte growth factor (KGF), palifermin may promote cell proliferation, reducing the severity of oral mucositis in patients in the relevant treatment groups.1 Agonism of fibroblast growth factor 2 may be predominantly responsible for this effect.2 The endogenous form if palifermin is expressed in the kidney of rats.3

TargetActionsOrganism
AFibroblast growth factor receptor 2
agonist
binder
Humans
UFibroblast growth factor receptor 1
agonist
Humans
UBasement membrane-specific heparan sulfate proteoglycan core protein
ligand
Humans
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
Medicalerrors
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Toxicity

Not Available

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.
Interactions
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Food Interactions
No interactions found.

Products

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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
KepivancePowder, for solution6.25 mg / vialIntravenousSWEDISH ORPHAN BIOVITRUM AB (PUBL)2006-03-142016-01-30Canada flag
KepivanceInjection, powder, lyophilized, for solution6.25 mg/1.2mLIntravenousSWEDISH ORPHAN BIOVITRUM AB (PUBL)2009-12-15Not applicableUS flag
KepivanceInjection6.25 mg/1mLIntravenousAmgen2004-12-152009-12-15US flag

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
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
QMS40680K6
CAS number
162394-19-6

References

General References
  1. Barasch A, Epstein J, Tilashalski K: Palifermin for management of treatment-induced oral mucositis in cancer patients. Biologics. 2009;3:111-6. doi: 10.2147/btt.2009.2871. Epub 2009 Jul 13. [Article]
  2. Ornitz DM, Xu J, Colvin JS, McEwen DG, MacArthur CA, Coulier F, Gao G, Goldfarb M: Receptor specificity of the fibroblast growth factor family. J Biol Chem. 1996 Jun 21;271(25):15292-7. [Article]
  3. 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. [Article]
  4. FDA Approved Drug Product: Kepivance (Palifermin) Intravenous Injection [Link]
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 RecruitingTreatmentLeukemias / Multiple Myeloma (MM) / Myelodysplastic Syndrome / Non-Hodgkin's Lymphoma (NHL)1
2CompletedPreventionOral Mucositis / Sarcomas1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Amgen Inc.
  • Baxter International Inc.
  • BioVitrum AB
Dosage Forms
FormRouteStrength
InjectionIntravenous6.25 mg/1mL
Injection, powder, for solutionIntravenous
Injection, powder, lyophilized, for solutionIntravenous6.25 mg/1.2mL
Powder, for solutionIntravenous6.25 mg / vial
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

Drugtargets
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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  8. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
  9. Ornitz DM, Xu J, Colvin JS, McEwen DG, MacArthur CA, Coulier F, Gao G, Goldfarb M: Receptor specificity of the fibroblast growth factor family. J Biol Chem. 1996 Jun 21;271(25):15292-7. [Article]
  10. FDA Approved Drug Product: Kepivance (Palifermin) Intravenous Injection [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Agonist
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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  6. Ornitz DM, Xu J, Colvin JS, McEwen DG, MacArthur CA, Coulier F, Gao G, Goldfarb M: Receptor specificity of the fibroblast growth factor family. J Biol Chem. 1996 Jun 21;271(25):15292-7. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  5. 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. [Article]

Drug created on June 13, 2005 13:24 / Updated on May 06, 2021 01:18