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Identification
NameBecaplermin
Accession NumberDB00102  (BTD00053, BIOD00053)
TypeBiotech
GroupsApproved, Investigational
Description

Becaplermin is produced by recombinant DNA technology by insertion of the gene for the B chain of platelet derived growth factor (PDGF) into the yeast, Saccharomyces cerevisiae. Becaplermin has a molecular weight of approximately 25 KD and is a homodimer composed of two identical polypeptide chains that are bound together by disulfide bonds.

Protein structureDb00102
Related Articles
Protein chemical formulaC532H892N162O153S9
Protein average weight12294.4 Da
Sequences
>DB00102 sequence
SLGSLTIAEPAMIAECKTRTEVFEISRRLIDRTNANFLVWPPCVEVQRCSGCCNNRNVQC
RPTQVQLRPVQVRKIEIVRKKPIFKKATVTLEDHLACKCETVAAARPVT
Download FASTA Format
Synonyms
c-sis
PDGF B-chain
PDGF-2
PDGF-BB
PDGFB
Platelet-derived growth factor B chain precursor
Platelet-derived growth factor beta polypeptide
SH-POLYPEPTIDE-59
External Identifiers
  • RWJ-60235
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Regranexgel100 ug/gtopicalHEALTHPOINT, LTD2011-11-012016-01-31Us
Regranexgel100 ug/gtopicalSmith & Nephew, Inc.2011-11-012016-04-05Us
Regranex (becaplermin) 0.01%gel100 mcgtopicalJanssen Inc1999-02-012011-07-27Canada
Generic Prescription ProductsNot Available
Over the Counter ProductsNot Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNII1B56C968OA
CAS number165101-51-9
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
Pharmacology
IndicationFor topical treatment of skin ulcers (from diabetes)
PharmacodynamicsUsed for the topical treatment of skin ulcers, Regranex has a biological activity similar to that of endogenous platelet-derived growth factor, which includes promoting the chemotactic recruitment and proliferation of cells involved in wound repair and enhancing the formation of granulation tissue.
Mechanism of actionBinds to the beta platelet-derived growth factor (PDGF) receptor, a tyrosine kinase receptor. PDGF is known to exist as a dimer, and activates its signaling pathway by a ligand induced receptor dimerization and autophosphorylation. PDGF receptors also contain many auto-phosphorylation sites, which serve to mediate binding of SH2 sites and subsequently signal corresponding pathways. There are five different isoforms of PDGF that activate through two different receptors (alpha and beta).
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Absorptionvery little systemic absorption. 15% of patients experienced complete healing within 8 weeks, while for 25% of patients, it was at 10 weeks.
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
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
Geltopical100 ug/g
Geltopical100 mcg
Prices
Unit descriptionCostUnit
Regranex 0.01% Gel 15 gm Tube723.82USD tube
Regranex 0.01% gel46.4USD g
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA1340846 No1999-12-072015-12-15Canada
Properties
StateLiquid
Experimental Properties
PropertyValueSource
hydrophobicity-0.160Not Available
isoelectric point9.38Not Available
References
Synthesis ReferenceNot Available
General References
  1. Link [Link]
  2. Link [Link]
External Links
ATC CodesA01AD08D03AX06
AHFS Codes
  • 84:16.00
PDB Entries
FDA labelDownload (248 KB)
MSDSNot Available
Interactions
Drug InteractionsNo interactions found.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
General Function:
Vascular endothelial growth factor binding
Specific Function:
Tyrosine-protein kinase that acts as cell-surface receptor for homodimeric PDGFB and PDGFD and for heterodimers formed by PDGFA and PDGFB, and plays an essential role in the regulation of embryonic development, cell proliferation, survival, differentiation, chemotaxis and migration. Plays an essential role in blood vessel development by promoting proliferation, migration and recruitment of peri...
Gene Name:
PDGFRB
Uniprot ID:
P09619
Molecular Weight:
123966.895 Da
References
  1. Papanas N, Maltezos E: Becaplermin gel in the treatment of diabetic neuropathic foot ulcers. Clin Interv Aging. 2008;3(2):233-40. [PubMed:18686746 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Vascular endothelial growth factor-activated receptor activity
Specific Function:
Tyrosine-protein kinase that acts as a cell-surface receptor for PDGFA, PDGFB and PDGFC and plays an essential role in the regulation of embryonic development, cell proliferation, survival and chemotaxis. Depending on the context, promotes or inhibits cell proliferation and cell migration. Plays an important role in the differentiation of bone marrow-derived mesenchymal stem cells. Required for...
Gene Name:
PDGFRA
Uniprot ID:
P16234
Molecular Weight:
122668.46 Da
References
  1. Abdiu A, Walz TM, Nishikawa BK, Wingren S, Larsson SE, Wasteson A: Human malignant fibrous histiocytomas in vitro: growth characteristics and their association with expression of mRNA for platelet-derived growth factor, transforming growth factor-alpha and their receptors. Eur J Cancer. 1998 Dec;34(13):2094-100. [PubMed:10070317 ]
  2. Ebert M, Yokoyama M, Friess H, Kobrin MS, Buchler MW, Korc M: Induction of platelet-derived growth factor A and B chains and over-expression of their receptors in human pancreatic cancer. Int J Cancer. 1995 Sep 4;62(5):529-35. [PubMed:7665222 ]
  3. Miller-Kasprzak E, Niemir ZI, Czekalski S: [Structure and function of PDGF-R-alpha and its expression in normal kidney and kidney diseases]. Przegl Lek. 2002;59(10):826-31. [PubMed:12632922 ]
  4. Heidaran MA, Pierce JH, Lombardi D, Ruggiero M, Gutkind JS, Matsui T, Aaronson SA: Deletion or substitution within the alpha platelet-derived growth factor receptor kinase insert domain: effects on functional coupling with intracellular signaling pathways. Mol Cell Biol. 1991 Jan;11(1):134-42. [PubMed:1702511 ]
  5. Yu J, Liu XW, Kim HR: Platelet-derived growth factor (PDGF) receptor-alpha-activated c-Jun NH2-terminal kinase-1 is critical for PDGF-induced p21WAF1/CIP1 promoter activity independent of p53. J Biol Chem. 2003 Dec 5;278(49):49582-8. Epub 2003 Sep 23. [PubMed:14506245 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Tumor necrosis factor binding
Specific Function:
Is able to inhibit all four classes of proteinases by a unique 'trapping' mechanism. This protein has a peptide stretch, called the 'bait region' which contains specific cleavage sites for different proteinases. When a proteinase cleaves the bait region, a conformational change is induced in the protein which traps the proteinase. The entrapped enzyme remains active against low molecular weight...
Gene Name:
A2M
Uniprot ID:
P01023
Molecular Weight:
163289.945 Da
References
  1. Lizonova A, Bizik J, Grofova M, Vaheri A: Coexpression of tumor-associated alpha 2-macroglobulin and growth factors in human melanoma cell lines. J Cell Biochem. 1990 Aug;43(4):315-25. [PubMed:1697862 ]
  2. Bonner JC, Osornio-Vargas AR: Differential binding and regulation of platelet-derived growth factor A and B chain isoforms by alpha 2-macroglobulin. J Biol Chem. 1995 Jul 7;270(27):16236-42. [PubMed:7541796 ]
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Drug created on June 13, 2005 07:24 / Updated on April 25, 2016 11:14