Becaplermin

Identification

Summary

Becaplermin is a recombinant form of human platelet-derived growth factor used to treat ulcers due to diabetic neuropathy in the lower extremities when there is adequate blood supply to the area.

Brand Names
Regranex
Generic Name
Becaplermin
DrugBank Accession Number
DB00102
Background

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.

Type
Biotech
Groups
Approved, Investigational
Biologic Classification
Protein Based Therapies
Other protein based therapies
Protein Structure
Protein Chemical Formula
C532H892N162O153S9
Protein Average Weight
12294.4 Da
Sequences
>DB00102 sequence
SLGSLTIAEPAMIAECKTRTEVFEISRRLIDRTNANFLVWPPCVEVQRCSGCCNNRNVQC
RPTQVQLRPVQVRKIEIVRKKPIFKKATVTLEDHLACKCETVAAARPVT
Download FASTA Format
Synonyms
  • Becaplermin
  • PDGF-2
  • PDGF-BB
  • PDGFB
  • Platelet-derived growth factor BB, recombinant
  • Platelet-derived growth factor beta polypeptide
  • Recombinant platelet-derived growth factor BB
  • rhPDGF-BB
  • rPDGF-BB
  • SH-POLYPEPTIDE-59
External IDs
  • GEM 21S
  • GEM-21S
  • RWJ 60235
  • RWJ-60235

Pharmacology

Indication

For topical treatment of skin ulcers (from diabetes)

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Treatment ofSkin ulcers••••••••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

Used 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 action

Binds 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).

TargetActionsOrganism
APlatelet-derived growth factor receptor betaNot AvailableHumans
UPlatelet-derived growth factor receptor alphaNot AvailableHumans
UAlpha-2-macroglobulinNot AvailableHumans
Absorption

very little systemic absorption. 15% of patients experienced complete healing within 8 weeks, while for 25% of patients, it was at 10 weeks.

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism
Not Available
Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects
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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.
No interactions found.
Food Interactions
No interactions found.

Products

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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
RegranexGel0.01 %CutaneousJanssen Cilag International Nv2016-09-082012-08-15EU flag
RegranexGel100 ug/1gTopicalHealthpoint2011-11-012016-01-31US flag
RegranexGel100 ug/1gTopicalOrtho-McNeil-Janssen Pharmaceuticals, Inc.1998-02-012013-01-31US flag
RegranexGel100 ug/1gTopicalSmith & Nephew, Inc.2011-11-01Not applicableUS flag
Regranex (becaplermin) 0.01%Gel100 mcg / gTopicalJanssen Pharmaceuticals1999-02-012011-07-27Canada flag

Categories

ATC Codes
D03AX06 — BecaplerminA01AD08 — Becaplermin
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
1B56C968OA
CAS number
165101-51-9

References

General References
  1. Link [Link]
UniProt
P01127
Genbank
K01401
PubChem Substance
46508246
RxNav
115238
ChEMBL
CHEMBL1201556
Therapeutic Targets Database
DAP000028
PharmGKB
PA164749511
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Becaplermin
FDA label
Download (248 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3CompletedTreatmentDiabetic Foot Ulcers (DFUs)1
3CompletedTreatmentHypertensive Leg Ulcer / Martorell's ulcer / Necrotic Angiodermatitis1
3TerminatedTreatmentDiabetic Neuropathies / Foot, Diabetic / Skin Ulcer / Ulcus Cruris1
3Unknown StatusTreatmentDiabetic Foot Ulcers (DFUs) / Venous Ulcers1
2CompletedTreatmentLateral Epicondylitis1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Janssen-Ortho Inc.
  • McNeil Laboratories
  • OMJ Pharmaceuticals
  • Ortho Mcneil Janssen Pharmaceutical Inc.
  • Ortho-McNeil-Janssen Pharmaceuticals Inc.
Dosage Forms
FormRouteStrength
GelCutaneous0.01 %
GelTopical100 ug/1g
GelTopical100 mcg / g
GelTopical0.01 g
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)Region
CA1340846No1999-12-072015-12-15Canada flag

Properties

State
Liquid
Experimental Properties
PropertyValueSource
hydrophobicity-0.160Not Available
isoelectric point9.38Not Available

Targets

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Kind
Protein
Organism
Humans
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...
Gene Name
PDGFRB
Uniprot ID
P09619
Uniprot Name
Platelet-derived growth factor receptor beta
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. [Article]
Kind
Protein
Organism
Humans
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 chem...
Gene Name
PDGFRA
Uniprot ID
P16234
Uniprot Name
Platelet-derived growth factor receptor alpha
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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
Kind
Protein
Organism
Humans
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 differen...
Gene Name
A2M
Uniprot ID
P01023
Uniprot Name
Alpha-2-macroglobulin
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. [Article]
  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. [Article]

Drug created at June 13, 2005 13:24 / Updated at January 02, 2024 23:41