| Primary information |
|---|
| ThPP ID | Th1120 |
| Therapeutic Peptide/Protein Name | Teriparatide |
| Sequence | Parathyroid hormone precursor - Homo sapiens (1-34 view full sequnce in fasta |
| Functional Classification | Ib |
| Molecular Weight | 4117.715 |
| Chemical Formula | C181H291N55O51S2 |
| Isoelectric Point | N.A. |
| Hydrophobicity | N.A. |
| Melting Point (℃) | N.A. |
| Half Life | N.A. |
| Description | Recombinant, human parathyroid hormone (PTH). It is a potent anabolic agent used to treat osteoporosis. It is manufactured and marketed by Eli Lilly and Company. |
| Indication/Disease | For the treatment of osteoporosis in men and postmenopausal women who are at high risk for having a fracture. Also used to increase bone mass in men with primary or hypogonadal osteoporosis who are at high risk for fracture. |
| Pharmacodynamics | Clinical trials indicate that teriparatide increases predominantly trabecular bone in the lumbar spine and femoral neck; it has less significant effects at cortical sites. The combination of teriparatide with antiresorptive agents is not more effective than teriparatide monotherapy. The most common adverse effects associated with teriparatide include injection-site pain, nausea, headaches, leg cramps, and dizziness. After a maximum of two years of teriparatide therapy, the drug should be discontinued and antiresorptive therapy begun to maintain bone mineral density. |
| Mechanism of Action | Teriparatide is the portion of human parathyroid hormone (PTH),amino acid sequence 1 through 34 of the complete molecule which contains amino acid sequence 1 to 84. Endogenous PTH is the primary regulator of calcium and phosphate metabolism in bone and kidney. Daily injections of teriparatide stimulate new bone formation leading to increased bone mineral density. |
| Toxicity | Effects of overexposure may include headaches, dizziness, dizziness, decreased blood pressured, decreased fetal survival, leg cramps, changes in clinical chemistry including increased in blood levels of calcium, decreased serum phosphorous, and increased urinary calcium and phosphorus. |
| Metabolism | Hepatic |
| Absorption | Bioavailability is 95% following subcutaneous injection. |
| Volume of Distribution | 0.12 L/kg |
| Clearance | 62 L/hr [Women] 94 L/hr [Men] |
| Categories | Bone Density Conservation Agents |
| Patents Number | US6977077 |
| Date of Issue | 20/08/03 |
| Date of Expiry | 20/08/23 |
| Drug Interaction | N.A. |
| Target | Parathyroid hormone/parathyroid hormone-related peptide receptor |
| Information of corresponding available drug in the market |
|---|
| Brand Name | Forteo |
| Company | Eli Lilly and Company |
| Brand Discription | FORTEO (teriparatide [rDNA origin] injection) contains recombinant human parathyroid hormone (1-34), and is also called rhPTH (1-34). It has an identical sequence to the 34 N-terminal amino acids (the biologically active region) of the 84-amino acid human parathyroid hormone. Teriparatide has a molecular weight of 4117.8 daltons. Teriparatide (rDNA origin) is manufactured using a strain of Escherichia coli modified by recombinant DNA technology |
| Prescribed for | Treatment of Postmenopausal Women with Osteoporosis at High Risk for Fracture, Increase of Bone Mass in Men with Primary or Hypogonadal Osteoporosis at High Risk for Fracture, Treatment of Men and Women with Glucocorticoid-Induced Osteoporosis at High Risk for Fracture. |
| Chemical Name | N.A. |
| Formulation | Each prefilled delivery device is filled with 2.7 mL to deliver 2.4 mL. Each mL contains 250 mcg teriparatide (corrected for acetate, chloride, and water content), 0.41 mg glacial acetic acid, 0.1 mg sodium acetate (anhydrous), 45.4 mg mannitol, 3 mg Metacresol, and Water for Injection. In addition, hydrochloric acid solution 10% and/or sodium hydroxide solution 10% may have been added to adjust the product to pH 4. Each cartridge, pre-assembled into a delivery device, delivers 20 mcg of teriparatide per dose each day for up to 28 days. |
| Physcial Appearnce | Sterile, colorless, clear, isotonic solution in a glass cartridge which is pre-assembled into a disposable delivery device (pen) for subcutaneous injection |
| Route of Administration | Subcutaneous |
| Recommended Dosage | Treatment of Postmenopausal Women with Osteoporosis at High Risk for Fracture. The recommended dose is 20 mcg subcutaneously once a day. Increase of Bone Mass in Men with Primary or Hypogonadal Osteoporosis at High Risk for Fracture. he recommended dose is 20 mcg subcutaneously once a day. |
| Contraindication | Hypersensitivity to teriparatide or to any of its excipients. Reactions have included angioedema and anaphylaxis |
| Side Effects | N.A. |
| Useful Link | http://en.wikipedia.org/wiki/Teriparatide, http://www.forteo.com/, http://www.rxlist.com/forteo-drug.htm, |
| PubMed ID | 25649182, 25639838, 25598280, 25567777, 25567774, 16872263 |
| 3-D Structure | Th1120 (View) or (Download) |