Becaplermin

Explore a selection of our essential drug information below, or:

Unlock enhanced features & extensive drug insights, including detailed interaction data & regulatory status. Create a free account.

SUBSCRIBERECOMMENDED FOR PHARMA

Explore the full scope of our drug knowledge tailored for pharmaceutical research needs in our data library. Learn more.

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

Unlock the secrets to drugging the undruggable

Discover how groundbreaking research is turning "undruggable" targets into therapeutic opportunities.

Download eBook

Unlock the secrets to drugging the undruggable

Download eBook

Pharmacology

Indication

For topical treatment of skin ulcers (from diabetes)

Reduce drug development failure rates

Build, train, & validate machine-learning models
with evidence-based and structured datasets.

See how

Build, train, & validate predictive machine-learning models with structured datasets.

See how

Associated Conditions

Indication Type	Indication	Combined Product Details	Approval Level	Age Group	Patient Characteristics	Dose Form
Treatment of	Skin ulcers		••••••••••••

Contraindications & Blackbox Warnings

Prevent Adverse Drug Events Today

Tap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.

Learn more

Avoid life-threatening adverse drug events with our Clinical API

Learn more

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).

Target	Actions	Organism
APlatelet-derived growth factor receptor beta	Not Available	Humans
UPlatelet-derived growth factor receptor alpha	Not Available	Humans
UAlpha-2-macroglobulin	Not Available	Humans

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

Improve decision support & research outcomes

With structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!

See the data

Improve decision support & research outcomes with our structured adverse effects data.

See a data sample

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

Drug product information from 10+ global regions

Our datasets provide approved product information including:
dosage, form, labeller, route of administration, and marketing period.

Access now

Access drug product information from over 10 global regions.

Access now

Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Regranex	Gel	100 ug/1g	Topical	Smith & Nephew, Inc.	2011-11-01	Not applicable
Regranex	Gel	0.01 %	Cutaneous	Janssen Cilag International Nv	2016-09-08	2012-07-16
Regranex	Gel	100 ug/1g	Topical	Healthpoint	2011-11-01	2016-01-31
Regranex	Gel	100 ug/1g	Topical	Ortho-McNeil-Janssen Pharmaceuticals, Inc.	1998-02-01	2013-01-31
Regranex (becaplermin) 0.01%	Gel	100 mcg / g	Topical	Janssen Pharmaceuticals	1999-02-01	2011-07-27

Chemical Identifiers

UNII: 1B56C968OA
CAS number: 165101-51-9

References

General References

Link [Link]

External Links

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 Clinical Trial & Rare Diseases Add-on Data Package Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package

Phase	Status	Purpose	Conditions	Count	Start Date	Why Stopped	100+ additional columns
Unlock 175K+ rows when you subscribe.View sample data
3	Completed	Treatment	Diabetic Foot Ulcers (DFUs)	1	somestatus	stop reason	just information to hide
3	Completed	Treatment	Hypertensive Leg Ulcer / Martorell's ulcer / Necrotic Angiodermatitis	1	somestatus	stop reason	just information to hide
3	Terminated	Treatment	Diabetic Neuropathies / Foot, Diabetic / Skin Ulcer / Ulcus Cruris	1	somestatus	stop reason	just information to hide
3	Unknown Status	Treatment	Diabetic Foot Ulcers (DFUs) / Venous Ulcers	1	somestatus	stop reason	just information to hide
2	Completed	Treatment	Lateral Epicondylitis	1	somestatus	stop reason	just information to hide

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Janssen-Ortho Inc.
McNeil Laboratories
OMJ Pharmaceuticals
Ortho Mcneil Janssen Pharmaceutical Inc.
Ortho-McNeil-Janssen Pharmaceuticals Inc.

Dosage Forms

Form	Route	Strength
Gel	Cutaneous	0.01 %
Gel	Topical	100 ug/1g
Gel	Topical	100 mcg / g
Gel	Topical	0.01 g

Prices

Unit description	Cost	Unit
Regranex 0.01% Gel 15 gm Tube	723.82USD	tube
Regranex 0.01% gel	46.4USD	g

DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)	Region
CA1340846	No	1999-12-07	2015-12-15

Properties

State

Liquid

Experimental Properties

Property	Value	Source
hydrophobicity	-0.160	Not Available
isoelectric point	9.38	Not Available

Targets

Build, predict & validate machine-learning models

Use our structured and evidence-based datasets to unlock new
insights and accelerate drug research.

Learn more

Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.

Learn more

Details1. Platelet-derived growth factor receptor beta

Kind: Protein
Organism: Humans
Pharmacological action: Yes

General Function: Tyrosine-protein kinase that acts as a 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 pericytes and smooth muscle cells to endothelial cells. Plays a role in the migration of vascular smooth muscle cells and the formation of neointima at vascular injury sites. Required for normal development of the cardiovascular system. Required for normal recruitment of pericytes (mesangial cells) in the kidney glomerulus, and for normal formation of a branched network of capillaries in kidney glomeruli. Promotes rearrangement of the actin cytoskeleton and the formation of membrane ruffles. Binding of its cognate ligands - homodimeric PDGFB, heterodimers formed by PDGFA and PDGFB or homodimeric PDGFD -leads to the activation of several signaling cascades; the response depends on the nature of the bound ligand and is modulated by the formation of heterodimers between PDGFRA and PDGFRB. Phosphorylates PLCG1, PIK3R1, PTPN11, RASA1/GAP, CBL, SHC1 and NCK1. Activation of PLCG1 leads to the production of the cellular signaling molecules diacylglycerol and inositol 1,4,5-trisphosphate, mobilization of cytosolic Ca(2+) and the activation of protein kinase C. Phosphorylation of PIK3R1, the regulatory subunit of phosphatidylinositol 3-kinase, leads to the activation of the AKT1 signaling pathway. Phosphorylation of SHC1, or of the C-terminus of PTPN11, creates a binding site for GRB2, resulting in the activation of HRAS, RAF1 and down-stream MAP kinases, including MAPK1/ERK2 and/or MAPK3/ERK1. Promotes phosphorylation and activation of SRC family kinases. Promotes phosphorylation of PDCD6IP/ALIX and STAM. Receptor signaling is down-regulated by protein phosphatases that dephosphorylate the receptor and its down-stream effectors, and by rapid internalization of the activated receptor
Specific Function: Atp binding
Gene Name: PDGFRB
Uniprot ID: P09619
Uniprot Name: Platelet-derived growth factor receptor beta
Molecular Weight: 123966.895 Da

References

Papanas N, Maltezos E: Becaplermin gel in the treatment of diabetic neuropathic foot ulcers. Clin Interv Aging. 2008;3(2):233-40. [Article]

Details2. Platelet-derived growth factor receptor alpha

Kind: Protein
Organism: Humans
Pharmacological action: Unknown

General 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 normal skeleton development and cephalic closure during embryonic development. Required for normal development of the mucosa lining the gastrointestinal tract, and for recruitment of mesenchymal cells and normal development of intestinal villi. Plays a role in cell migration and chemotaxis in wound healing. Plays a role in platelet activation, secretion of agonists from platelet granules, and in thrombin-induced platelet aggregation. Binding of its cognate ligands - homodimeric PDGFA, homodimeric PDGFB, heterodimers formed by PDGFA and PDGFB or homodimeric PDGFC -leads to the activation of several signaling cascades; the response depends on the nature of the bound ligand and is modulated by the formation of heterodimers between PDGFRA and PDGFRB. Phosphorylates PIK3R1, PLCG1, and PTPN11. Activation of PLCG1 leads to the production of the cellular signaling molecules diacylglycerol and inositol 1,4,5-trisphosphate, mobilization of cytosolic Ca(2+) and the activation of protein kinase C. Phosphorylates PIK3R1, the regulatory subunit of phosphatidylinositol 3-kinase, and thereby mediates activation of the AKT1 signaling pathway. Mediates activation of HRAS and of the MAP kinases MAPK1/ERK2 and/or MAPK3/ERK1. Promotes activation of STAT family members STAT1, STAT3 and STAT5A and/or STAT5B. Receptor signaling is down-regulated by protein phosphatases that dephosphorylate the receptor and its down-stream effectors, and by rapid internalization of the activated receptor
Specific Function: Atp binding
Gene Name: PDGFRA
Uniprot ID: P16234
Uniprot Name: Platelet-derived growth factor receptor alpha
Molecular Weight: 122668.46 Da

References

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]
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]
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]
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]
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]

Details3. Alpha-2-macroglobulin

Kind: Protein
Organism: Humans
Pharmacological action: Unknown

General 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 substrates (activity against high molecular weight substrates is greatly reduced). Following cleavage in the bait region, a thioester bond is hydrolyzed and mediates the covalent binding of the protein to the proteinase
Specific Function: Brain-derived neurotrophic factor binding
Gene Name: A2M
Uniprot ID: P01023
Uniprot Name: Alpha-2-macroglobulin
Molecular Weight: 163289.945 Da

References

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]
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 August 02, 2024 07:21

Becaplermin

Identification

Pharmacology

Interactions

Products

Categories

Chemical Identifiers

References

Clinical Trials

Clinical Trial & Rare Diseases Add-on Data Package

Pharmacoeconomics

Properties

Targets

References

References

References