Detailed description page of ThPDB2

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Th1084 details
Primary information
ID10470
Therapeutic IDTh1084
Protein NameBecaplermin
Sequence>Th1084_Becaplermin SLGSLTIAEPAMIAECKTRTEVFEISRRLIDRTNANFLVWPPCVEVQRCSGCCNNRNVQCRPTQVQLRPVQVRKIEIVRKKPIFKKATVTLEDHLACKCETVAAARPVT
Molecular Weight12294.4
Chemical FormulaC532H892N162O153S9
Isoelectric Point9.38
Hydrophobicity-0.16
Melting pointNA
Half-lifeNA
DescriptionRecombinant platelet derived growth factor (PDGF), the gene for B chain, produced in yeast by cloning and expression of, Saccharomyces cerevisiae. Molecular weight ~25 KD is the homodimer composed of two identical polypeptide chains linked by disulfide bonds.
Indication/DiseaseFor 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).
ToxicityNA
MetabolismNA
Absorptionvery little systemic absorption. 15% of patients experienced complete healing within 8 weeks, while for 25% of patients, it was at 10 weeks.
NA
ClearanceNA
CategoriesAcids,Acids, Noncarboxylic,Alimentary Tract and Metabolism,Amino Acids, Peptides, and Proteins,Angiogenesis Inducing Agents,Angiogenesis Modulating Agents,Anions,Biological Factors,Blood Proteins,Cicatrizants,Dermatologicals,DNA-Binding Proteins,Electrolytes,Growth Substances,Hematologic Agents,Human Platelet-derived Growth Factor,Intercellular Signaling Peptides and Proteins,Ions,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
Patents NumberCA1340846
Date of Issue7-Dec-1999
Date of Expiry7-Oct-2005
Drug InteractionNA
TargetPlatelet-derived growth factor receptor beta,Platelet-derived growth factor receptor alpha,Alpha-2-macroglobulin
Brand NameREGRANEX
CompanyOMJ Pharmaceuticals, Inc. San German, Puerto Rico
Brand DescriptionOMJ Pharmaceuticals, Inc. San German, Puerto Rico
Prescribed Forfor the treatment of lower extremity diabetic neuropathic ulcers that extend into the subcutaneous tissue or beyond and have an adequate blood supply, when used as an adjunct to, and not a substitute for, good ulcer care practices including initial sharp debridement, pressure relief and infection control.
Chemical NameNA
Formulation0.01 % clear to straw-colored gel
Physical Appearance Gel: 0.01 %; clear, colorless to straw-colored gel
Route of AdministrationFor topical use; not for oral, ophthalmic or intra
Recommended DosageGel to be applied will vary depending upon the size of the ulcer area.
ContraindicationA very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.
Side Effectshives; difficulty breathing; swelling of your face, lips, tongue, or throat.
Useful Link 1Link
Useful Link 2NA
RemarksNA