| Primary information |
|---|
| ThPP ID | Th1084 |
| Therapeutic Peptide/Protein Name | Becaplermin |
| Sequence | SLGSLTIAEPAMIAECKTRTEVFEISRRLIDRTNANFLVWPPCVEVQRCS view full sequnce in fasta |
| Functional Classification | Ib |
| Molecular Weight | 12294.4 |
| Chemical Formula | C532H892N162O153S9 |
| Isoelectric Point | 9.38 |
| Hydrophobicity | -0.16 |
| Melting Point (℃) | N.A. |
| Half Life | N.A. |
| Description | Recombinant 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/Disease | For topical treatment of skin ulcers (from diabetes) |
| 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). |
| Toxicity | N.A. |
| Metabolism | N.A. |
| Absorption | N.A. |
| Volume of Distribution | N.A. |
| Clearance | N.A. |
| Categories | Angiogenesis Inducing Agents |
| Patents Number | CA1340846 |
| Date of Issue | 08/12/03 |
| Date of Expiry | 16/12/19 |
| Drug Interaction | N.A. |
| Target | T-cell surface glycoprotein CD1a,Major histocompatibility complex class I-related gene protein,Integrin alpha-L,T-lymphocyte activation antigen CD86,Low affinity immunoglobulin gamma Fc region receptor II-b,T-cell surface glycoprotein CD4,Integrin beta-1,Integrin alpha-V,Integrin beta-3 |
| Information of corresponding available drug in the market |
|---|
| Brand Name | REGRANEX |
| Company | OMJ Pharmaceuticals, Inc. San German, Puerto Rico |
| Brand Discription | REGRANEX Gel contains becaplermin, a recombinant human platelet-derived growth factor for topical administration. 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. REGRANEX Gel is a non-sterile, low bioburden, preserved, sodium carboxymethylcellulose-based (CMC) topical gel, containing the active ingredient becaplermin and the following inactive ingredients: carboxymethylcellulose sodium, glacial acetic acid, l-lysine hydrochloride, m-cresol, methylparaben, propylparaben, sodium acetate trihydrate, sodium chloride, and water for injection. Each gram of REGRANEX Gel contains 100 mcg of becaplermin. |
| Prescribed for | for 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 Name | N.A. |
| Formulation | 0.01 % clear to straw-colored gel |
| Physcial Appearnce | Gel: 0.01 %; clear, colorless to straw-colored gel |
| Route of Administration | For topical use; not for oral, ophthalmic or intra |
| Recommended Dosage | Gel to be applied will vary depending upon the size of the ulcer area. |
| Contraindication | A 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 Effects | hives; difficulty breathing; swelling of your face, lips, tongue, or throat. |
| Useful Link | http://www.rxlist.com/regranex-side-effects-drug-center.htm |
| PubMed ID | 23962308, 21173589, 20941855, 20486728, 20479444, 19837327, 18251718 |
| 3-D Structure | Th1084 (View) or (Download) |