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Identification
NameBecaplermin
Accession NumberDB00102  (BIOD00053, BTD00053)
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
Protein chemical formulaC532H892N162O153S9
Protein average weight12294.4000
Sequences
>DB00102 sequence
SLGSLTIAEPAMIAECKTRTEVFEISRRLIDRTNANFLVWPPCVEVQRCSGCCNNRNVQC
RPTQVQLRPVQVRKIEIVRKKPIFKKATVTLEDHLACKCETVAAARPVT
Download FASTA Format
Synonyms
SynonymLanguageCode
c-sisNot AvailableNot Available
PDGF B-chainNot AvailableNot Available
PDGF-2Not AvailableNot Available
Platelet-derived growth factor B chain precursorNot AvailableNot Available
Platelet-derived growth factor beta polypeptideNot AvailableNot Available
SaltsNot Available
Brand names
NameCompany
RegranexOMJ Pharmaceuticals
Brand mixturesNot Available
Categories
CAS number165101-51-9
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 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).
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
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
GelTopical
Prices
Unit descriptionCostUnit
Regranex 0.01% Gel 15 gm Tube723.82USDtube
Regranex 0.01% gel46.4USDg
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
CountryPatent NumberApprovedExpires (estimated)
Canada13408461999-12-072015-12-15
Properties
Stateliquid
Experimental Properties
PropertyValueSource
hydrophobicity-0.160Not Available
isoelectric point9.38Not Available
References
Synthesis ReferenceNot Available
General Reference
  1. http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-Scientific_Discussion/human/000212/WC500050140.pdf
    #Lexicomp [Internet]. Becaplermin. 2014 [cited 12 November 2014]. Available from: http://online.lexi.com.login.ezproxy.library.ualberta.ca/lco/action/doc/retrieve/docid/patch_f/6420#f
    pharmacology-and-pharmacokinetics
External Links
ResourceLink
UniProtP01127
GenbankK01401
PharmGKBPA164749511
Drug Product Database2239405
RxListhttp://www.rxlist.com/cgi/generic2/becapler.htm
Drugs.comhttp://www.drugs.com/cdi/becaplermin.html
WikipediaBecaplermin
ATC CodesA01AD08D03AX06
AHFS Codes
  • 84:16.00
PDB Entries
FDA labelshow(248 KB)
MSDSNot Available
Interactions
Drug InteractionsSearched, but no interactions found.
Food InteractionsNot Available

Targets

1. Platelet-derived growth factor receptor beta

Kind: protein

Organism: Human

Pharmacological action: yes

Components

Name UniProt ID Details
Platelet-derived growth factor receptor beta P09619 Details

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

2. Platelet-derived growth factor receptor alpha

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Platelet-derived growth factor receptor alpha P16234 Details

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
  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
  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
  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
  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

3. Alpha-2-macroglobulin

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Alpha-2-macroglobulin P01023 Details

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
  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

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Drug created on June 13, 2005 07:24 / Updated on November 11, 2014 22:47