| Primary information |
|---|
| ThPP ID | Th1161 |
| Therapeutic Peptide/Protein Name | Albiglutide |
| Sequence | HGEGTFTSDVSSYLEGQAAKEFIAWLVKGRHGEGTFTSDVSSYLEGQAAK view full sequnce in fasta |
| Functional Classification | Ib |
| Molecular Weight | 72972 |
| Chemical Formula | C3232H5032N864O979S43 |
| Isoelectric Point | NA |
| Hydrophobicity | NA |
| Melting Point (℃) | NA |
| Half Life | 4-7 days. |
| Description | Albiglutide is a glucagon-like peptide-1 agonist (GLP-1) biologic drug indicated in the treatment of type 2 diabetes. It is marketed under the brands Eperzan and Tanzeum by GSK (GlaxoSmithKline). It is a dipeptidyl peptidase-4-resistant glucagon-like peptide-1 dimer fused to human albumin. Albiglutide was approved on April 15, 2014 by the FDA. |
| Indication/Disease | Indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. |
| Pharmacodynamics | It lowers fasting glucose and reduces postprandial glucose excursions in patients with type 2 diabetes mellitus. The majority of the observed reduction in fasting plasma glucose occurs after a single dose, consistent with the pharmacokinetic profile of albiglutide. |
| Mechanism of Action | Albiglutide is an agonist of the GLP-1 (glucagon-like peptide 1) receptor and augments glucose-dependent insulin secretion. Albiglutide also slows gastric emptying. |
| Toxicity | RISK OF THYROID C-CELL TUMORS -Albiglutide is contraindicated in patients with a personal or family history of MTC or in patients with Multiple Endocrine Neoplasia syndrome type 2 (MEN2). Routine serum calcitonin or thyroid ultrasound monitoring is of uncertain value in patients treated with Albiglutide.O675 |
| Metabolism | Biotransformation studies have not been performed. Because albiglutide is an albumin fusion protein, it likely follows a metabolic pathway similar to native human serum albumin, which is catabolized primarily in the vascular endothelium. |
| Absorption | Maximum concentrations of albiglutide were reached at 3 to 5 days post-dosing following a single 30mg dose. The mean peak concentration (Cmax) and mean area under the time-concentration curve (AUC) of albiglutide were 1.74 mcg/mL and 465 mcg.h/mL, respectively. |
| Volume of Distribution | 13 L |
| Clearance | 69 mL/h |
| Categories | Drugs used in diabetes; alimentary tract and metabolism; blood glucose lowering drugs, excl. insulins. |
| Patents Number | |
| Date of Issue | |
| Date of Expiry | |
| Drug Interaction | Acetylsalicylic acid may increase the hypoglycemic activities of Albiglutide; Albiglutide may increase the hypoglycemic activities of Chlorpropamide; Dihydrotestosterone may increase the hypoglycemic activities of Albiglutide; Albiglutide may increase the hypoglycemic activities of Insulin Regular; Albiglutide may increase the hypoglycemic activities of Insulin Lispro; The therapeutic efficacy of Albiglutide can be decreased when used in combination with Leuprolide; Lipoic Acid may increase the hypoglycemic activities of Albiglutide; Oxandrolone may increase the hypoglycemic activities of Albiglutide; Paroxetine may increase the hypoglycemic activities of Albiglutide; Pegvisomant may increase the hypoglycemic activities of Albiglutide. |
| Target | Glucagon-like peptide 1 receptor |
| Information of corresponding available drug in the market |
|---|
| Brand Name | Tanzeum |
| Company | Glaxo Smith Kline Llc |
| Brand Discription | N.A. |
| Prescribed for | A GLP-1 receptor agonist indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus |
| Chemical Name | N.A. |
| Formulation | 30 mg/.5mL |
| Physcial Appearnce | injection, powder, lyophilized, for solution |
| Route of Administration | Subcutaneous |
| Recommended Dosage | The recommended dosage of TANZEUM is 30 mg once weekly given as a subcutaneous injection in the abdomen, thigh, or upper arm region. The dosage may be increased to 50 mg once weekly if the glycemic response is inadequate. |
| Contraindication | Contraindicated in patients with a personal or family history of medullary thyroid carcinoma (MTC) or in patients with Multiple Endocrine Neoplasia syndrome type 2 (MEN 2); in patients with a prior serious hypersensitivity reaction to albiglutide or to any of the product components |
| Side Effects | Risk of Thyroid C-cell Tumors; Acute Pancreatitis; Hypoglycemia with Concomitant Use of Insulin Secretagogues or Insulin ; Hypersensitivity Reactions; Renal Impairment. |
| Useful Link | http://www.rxlist.com/tanzeum-drug/clinical-pharmacology.htm ; https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/125431s000lbl.pdf |
| PubMed ID | 20383346, 25477585, 25083125, 19455266, 24421551, 19455266 |
| 3-D Structure | Th1161 (View) or (Download) |