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
- 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.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Management of Oral mucositis •••••••••••• •••••••••• ••••••• ••••••••• ••••••••••••• •••• •••• •••••••• •••••••••••••• •••••••••••• ••••••••• Prophylaxis of Oral mucositis •••••••••••• •••••••••• ••••••• ••••••••• ••••••••••••• •••• •••• •••••••• •••••••••••••• •••••••••••• ••••••••• - Contraindications & Blackbox Warnings
- Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API
- 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
Target Actions Organism AFibroblast growth factor receptor 2 agonistbinderHumans UFibroblast growth factor receptor 1 agonistHumans UBasement membrane-specific heparan sulfate proteoglycan core protein ligandHumans - 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
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.
- Toxicity
Not Available
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" 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 Integrate drug-drug
interactions in your softwareAldesleukin The therapeutic efficacy of Palifermin can be decreased when used in combination with Aldesleukin. Alemtuzumab The therapeutic efficacy of Palifermin can be decreased when used in combination with Alemtuzumab. Altretamine The therapeutic efficacy of Palifermin can be decreased when used in combination with Altretamine. Amsacrine The therapeutic efficacy of Palifermin can be decreased when used in combination with Amsacrine. Ardeparin The serum concentration of Palifermin can be increased when it is combined with Ardeparin. - Food Interactions
- No interactions found.
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Kepivance Powder, for solution 6.25 mg / vial Intravenous SWEDISH ORPHAN BIOVITRUM AB (PUBL) 2006-03-14 2016-01-30 Canada Kepivance Injection, powder, lyophilized, for solution 5.16 mg/1.2mL Intravenous SWEDISH ORPHAN BIOVITRUM AB (PUBL) 2023-08-04 Not applicable US Kepivance Injection, powder, lyophilized, for solution 6.25 mg/1.2mL Intravenous SWEDISH ORPHAN BIOVITRUM AB (PUBL) 2009-12-15 2023-04-30 US Kepivance Injection 6.25 mg/1mL Intravenous Amgen 2004-12-15 2009-12-15 US
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
- 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]
- 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]
- 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]
- FDA Approved Drug Product: Kepivance (Palifermin) Intravenous Injection [Link]
- External Links
- UniProt
- P21781
- Genbank
- M60828
- PubChem Substance
- 46506691
- 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 Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Completed Prevention Multiple Myeloma (MM) / Non-Hodgkin's Lymphoma (NHL) / Non-Hodgkin's Lymphomas 1 3 Active Not Recruiting Treatment Leukemias / Mucositis / Oral Complications 1 3 Completed Supportive Care Cancer / Leukemias / Lymphoma 1 3 Completed Supportive Care Multiple Myeloma (MM) 1 3 Completed Treatment Head And Neck Cancer 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Amgen Inc.
- Baxter International Inc.
- BioVitrum AB
- Dosage Forms
Form Route Strength Injection Intravenous 6.25 mg/1mL Injection, powder, for solution Intravenous Injection, powder, lyophilized, for solution Intravenous 5.16 mg/1.2mL Injection, powder, lyophilized, for solution Intravenous 6.25 mg/1.2mL Powder, for solution Intravenous 6.25 mg / vial - Prices
Unit description Cost Unit Kepivance 6.25 mg vial 1650.0USD vial DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Liquid
- Experimental Properties
Property Value Source hydrophobicity -0.650 Not Available isoelectric point 9.47 Not Available
Targets
![](https://go.drugbank.com/assets/locked/DrugTargets2-682eb846d210ae4bf33ca03febccfb57bb1c61318e699b729e5df4dfab2c5b67.png)
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- AgonistBinder
- 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
- 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]
- 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]
- 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]
- 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]
- 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]
- 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]
- 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]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- 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]
- 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
- 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]
- 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]
- 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]
- 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]
- 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]
- 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
- 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]
- 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]
- 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]
- 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]
- 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 at June 13, 2005 13:24 / Updated at January 02, 2024 23:41