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)
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 Treatment of Skin ulcers •••••••••••• - 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 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 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.No interactions found.
- 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 Regranex Gel 100 ug/1g Topical Ortho-McNeil-Janssen Pharmaceuticals, Inc. 1998-02-01 2013-01-31 US 
Regranex Gel 100 ug/1g Topical Smith & Nephew, Inc. 2011-11-01 Not applicable US Regranex Gel 0.01 % Cutaneous Janssen Cilag International Nv 2016-09-08 2012-08-15 EU 
Regranex Gel 100 ug/1g Topical Healthpoint 2011-11-01 2016-01-31 US Regranex (becaplermin) 0.01% Gel 100 mcg / g Topical Janssen Pharmaceuticals 1999-02-01 2011-07-27 Canada 
Categories
- ATC Codes
- D03AX06 — Becaplermin
- D03AX — Other cicatrizants
- D03A — CICATRIZANTS
- D03 — PREPARATIONS FOR TREATMENT OF WOUNDS AND ULCERS
- D — DERMATOLOGICALS
- Drug Categories
- Acids
- Acids, Noncarboxylic
- Alimentary Tract and Metabolism
- Amino Acids, Peptides, and Proteins
- Angiogenesis Inducing Agents
- Angiogenesis Modulating Agents
- Biological Factors
- Blood Proteins
- Cicatrizants
- Dermatologicals
- DNA-Binding Proteins
- Growth Substances
- Hematologic Agents
- Human Platelet-derived Growth Factor
- Intercellular Signaling Peptides and Proteins
- Neoplasm Proteins
- Oncogene Proteins
- Peptides
- Phosphoric Acids
- Phosphorus Acids
- Phosphorus Compounds
- Platelet-Derived Growth Factor
- Preparations for Treatment of Wounds and Ulcers
- Proteins
- Proto-Oncogene Proteins
- Proto-Oncogene Proteins c-sis
- Stomatological Preparations
- 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
- Link [Link]
- External Links
- UniProt
- P01127
- Genbank
- K01401
- PubChem Substance
- 46508246
- 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 Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 3 Completed Treatment Diabetic Foot Ulcers (DFUs) 1 3 Completed Treatment Hypertensive Leg Ulcer / Martorell's ulcer / Necrotic Angiodermatitis 1 3 Terminated Treatment Diabetic Foot / Diabetic Neuropathies / Skin Ulcer / Ulcus Cruris 1 3 Unknown Status Treatment Diabetic Foot Ulcers (DFUs) / Venous Ulcers 1 2 Completed Treatment Lateral Epicondylitis 1
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 Canada
Properties
- State
- Liquid
- Experimental Properties
Property Value Source hydrophobicity -0.160 Not Available isoelectric point 9.38 Not 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
- 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
- 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]
- 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
- 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 January 02, 2024 23:41