stumble on Albiglutide Class: Incretin Mimetics Chemical Name: Albugon, a recombinant human glucagon-like peptide 1-albumin protein Molecular Formula: C 3232 H 5032 N 864 O 979 S 41 CAS Number: 782500-75-8 Brands: Tanzeum Overview Side Effects Dosage Professional Interactions More Pregnancy Warnings User Reviews Support Group Q & A Warning(s) Risk of Thyroid C-Cell Tumors GLP-1 receptor agonists such as albiglutide cause dose-dependent and treatment-duration-dependent thyroid C-cell tumors at clinically relevant exposures in both genders of rats and mice. 1 11 13 Unknown whether albiglutide causes thyroid C-cell tumors, including medullary thyroid carcinoma (MTC), in humans, as relevance to humans could not be ruled out by clinical or nonclinical studies. 1 11 13 Contraindicated in patients with a personal or family history of MTC and in patients with multiple endocrine neoplasia syndrome type 2 (MEN 2). 1 13 REMS: FDA approved a REMS for albiglutide to ensure that the benefits outweigh the risk. The REMS may apply to one or more preparations of albiglutide and consists of the following: communication plan. See the FDA REMS page () or the ASHP REMS Resource Center (). Introduction Antidiabetic agent; glucagon-like peptide-1 (GLP-1) agonist (incretin mimetic) fused to recombinant human albumin. 1 10 17 18 19 Slideshow It's In The Genes - Record Your Family Health History Uses for Albiglutide Diabetes Mellitus Used as an adjunct to diet and exercise to improve glycemic control in patients with type 2 diabetes mellitus. 1 10 Used alone or as add-on therapy with metformin, the combination of metformin and a sulfonylurea, a thiazolidinedione with or without metformin, and insulin glargine with or without oral antidiabetic agents. 1 10 Not recommended as first-line therapy for patients inadequately controlled on diet and exercise alone because of potential thyroid C-cell tumor risk and risk of acute pancreatitis. 1 13 Safety and efficacy not established in patients with a history of pancreatitis; consider other antidiabetic agents. 1 Not recommended for use in patients with severe GI disease, including severe gastroparesis. 1 Safety and efficacy in combination with prandial insulin not established. 1 Not indicated for use in patients with type 1 diabetes mellitus or diabetic ketoacidosis. 1 Albiglutide Dosage and Administration General Perform regular monitoring (e.g., blood glucose determinations, HbA 1c ) to determine therapeutic response. 1 Administration Administer by sub-Q injection using a prefilled injection pen. 1 If a dose is missed, administer it as soon as possible within 3 days after the missed dose, followed by resumption of the regular weekly schedule. 1 If it has been more than 3 days since the missed dose, skip the dose and resume the regular schedule with the next scheduled dose. 1 Administer albiglutide and insulin as separate injections in patients receiving both medications; do not mix insulin and albiglutide. 1 May inject albiglutide and insulin in the same body regions; do not administer injections adjacent to each other. 1 Sub-Q Administration Administer by sub-Q injection once weekly, on the same day each week, at any time of day without regard to meals. 1 If changing the day of weekly administration, allow at least 4 days to elapse between doses. 1 Administer into abdomen, thigh, or upper arm; rotate sites. 1 Reconstitution Reconstitute prefilled injection cartridge pens according to manufacturer's instructions prior to use. 1 12 If stored in the refrigerator, allow pen to sit at room temperature for 15 minutes before reconstitution. 1 To reconstitute albiglutide lyophilized powder, hold the clear cartridge upright displaying the number 1 in the window, then twist the cartridge several times in the direction of the arrow (clockwise) until the number 2 is displayed. 1 12 Gently rock the pen side to side (like a windshield wiper) 5 times to mix, and allow pen to stand for 15 minutes (30-mg pen) or 30 minutes (50-mg pen) to dissolve completely. 1 12 Do not shake pen. 1 12 After 15 or 30 minutes, gently rock pen side to side 5 additional times to ensure complete mixing. 1 12 Alternative instructions for healthcare professionals allowing for faster reconstitution provided in the manufacturer's labeling. 1 Attach manufacturer-supplied needle and prime by twisting the pen as directed until the number 3 is displayed in the cartridge window. 1 12 Reconstituted solution should be clear and yellow, and contains 30 or 50 mg of albiglutide per 0.5 mL. 1 12 Use within 8 hours of reconstitution prior to attaching the needle; after the needle is attached and primed, use immediately to prevent solution drying and clogging the needle. 1 12 Dosage Adults Diabetes Mellitus Sub-Q 30 mg once weekly. 1 May increase dosage to 50 mg once weekly if glycemic response is inadequate. 1 Special Populations No special population dosage recommendations. 1 Use caution when initiating albiglutide or escalating dosage in patients with renal impairment. 1 (See Renal Impairment under Cautions.) Cautions for Albiglutide Contraindications Personal or family history of MTC. 1 MEN 2. 1 Prior serious hypersensitivity to albiglutide or any component in the formulation. 1 Warnings/Precautions Warnings Risk of Thyroid C-Cell Tumors Dose-dependent and treatment-duration-dependent thyroid C-cell tumors found in rats and mice receiving GLP-1 receptor agonists at clinically relevant exposures. 1 11 13 Unknown whether albiglutide causes thyroid C-cell tumors, including MTC, in humans; relevance to humans could not be ruled out by clinical or nonclinical studies. 1 13 Uncertain value of routine monitoring of serum calcitonin (biological marker of MTC); if serum calcitonin is elevated, refer patient to endocrinologist for further evaluation. 1 Unknown whether monitoring serum calcitonin concentrations or thyroid ultrasound examinations mitigates risk of thyroid C-cell tumors. 1 Sensitivity Reactions Hypersensitivity Reactions Serious hypersensitivity reactions (dyspnea, pruritus, rash) reported. 1 Discontinue albiglutide if hypersensitivity reaction occurs and treat patient promptly according to standard of care until manifestations resolve. 1 Other Warnings and Precautions Pancreatitis and Pancreatic Precancerous Changes Acute pancreatitis reported during clinical trials. 1 FDA has been evaluating unpublished findings suggesting an increased risk of pancreatitis and precancerous pancreatic cell changes in patients with type 2 diabetes mellitus receiving incretin mimetics (exenatide, liraglutide, sitagliptin, saxagliptin, alogliptin, linagliptin). 14 15 16 FDA will notify healthcare professionals of its conclusions and recommendations when the review is complete or when the agency has additional information to report. 14 15 FDA has recommended that clinicians continue to follow the recommendations in the prescribing information for incretin mimetics. 14 15 Manufacturer states that if pancreatitis is suspected, promptly discontinue albiglutide and initiate appropriate management. 1 If pancreatitis is confirmed, do not restart albiglutide. 1 Efficacy and safety not established in patients with a history of pancreatitis; consider other antidiabetic agents in such patients. 1 Use with Drugs Known to Cause Hypoglycemia Patients receiving albiglutide in combination with an insulin secretagogue (e.g., a sulfonylurea) or insulin have an increased risk of hypoglycemia. 1 3 4 5 6 7 8 9 10 A lower dosage of the concomitant insulin secretagogue or insulin may be required to reduce this risk. 1 Renal Effects Acute renal failure and worsening of chronic renal failure (sometimes requiring hemodialysis) reported with GLP-1 receptor agonists during postmarketing experience. 1 Some patients did not have known underlying renal disease. 1 Most events occurred in patients experiencing nausea, vomiting, diarrhea, or dehydration. 1 The frequency of GI effects increased as renal function declined. 1 Because such adverse GI effects may worsen renal function, use caution when initiating albiglutide or escalating dosage in patients with renal impairment. 1 11 Macrovascular Outcomes Evidence of macrovascular risk reduction with albiglutide or any other antidiabetic agent has not been conclusively demonstrated in controlled clinical trials. 1 Specific Populations Pregnancy Category C. 1 Lactation Not known whether albiglutide distributed into milk in humans. 1 Discontinue nursing or the drug, taking into account the importance of the drug to the woman. 1 Pediatric Use Safety and efficacy not established in pediatric patients younger than 18 years of age. 1 Geriatric Use No substantial differences in safety and efficacy relative to younger adults, but increased sensitivity cannot be ruled out. 1 Hepatic Impairment Limited experience in patients with hepatic impairment; unlikely to affect albiglutide elimination. 1 12 Renal Impairment Systemic exposure increased in patients with severe renal impairment; use caution when initiating albiglutide or escalating dosage in patients with renal impairment. 1 (See Special Populations under Dosage and Administration and Renal Effects under Cautions.) Common Adverse Effects Upper respiratory tract infection, 1 10 diarrhea, 1 10 nausea, 1 10 injection site reaction, 1 cough, 1 back pain, 1 10 arthralgia, 1 sinusitis, 1 influenza. 1 10 Interactions for Albiglutide Low potential for pharmacokinetic interactions related to CYP metabolism. 1 Orally Administered Drugs Possible altered rate and extent of absorption of concomitantly administered oral drugs; use caution with concomitantly administered oral drugs. 1 Specific Drugs Drug Interaction Comments Digoxin No change in peak plasma concentration or overall AUC 1 20 No dosage adjustment necessary 1 Hormonal contraceptives, oral No change in peak plasma concentration or overall AUC of ethinyl estradiol and levonorgestrel 1 No dosage adjustment necessary 1 10 Simvastatin Decreased AUC and increased peak plasma concentration of simvastatin; increased AUC and peak plasma concentration of simvastatin acid (active metabolite) 1 Clinical relevance not known; no dosage adjustment necessary 1 Warfarin No change in peak plasma concentration or overall AUC of R - or S -warfarin; no change in INR 1 No dosage adjustment necessary 1 Albiglutide Pharmacokinetics Absorption Bioavailability Peak plasma albiglutide concentration achieved in 3 5 days. 1 17 Distribution Plasma Protein Binding Not studied; albiglutide is an albumin fusion molecule. 1 Elimination Metabolism Metabolized principally in a manner similar to that of endogenous albumin (in vascular endothelium). 1 Resistant to degradation by dipeptidyl peptidase-4 (DPP-4). 1 10 Half-life 5 days after sub-Q administration. 1 Stability Storage Parenteral Powder for Injection 2 8 C in original carton; do not freeze. 1 After dispensing, may be stored at room temperature up to 30 C for up to 4 weeks. 1 Use reconstituted solution within 8 hours prior to attaching the needle or immediately after attaching needle. 1 Actions Two long-acting human glucagon-like peptide-1 (GLP-1) receptor agonist molecules fused in tandem to recombinant human albumin; resistant to degradation by dipeptidyl peptidase-4 (DPP-4) due to a glycine substitution of the alanine at position 8. 1 10 17 18 19 Increases insulin release in the presence of elevated glucose concentrations. 1 10 17 Suppresses glucose-dependent glucagon secretion but does not impair normal glucagon response to hypoglycemia. 1 10 17 Delays gastric emptying, reducing the rate at which postprandial glucose appears in the circulation; increases satiety and decreases food intake. 1 10 17 19 Advice to Patients Importance of patients reading the medication guide prior to initiating therapy and each time the prescription is refilled. 1 11 Importance of informing patients that albiglutide causes benign and malignant thyroid C-cell tumors in mice and rats and that relevance of this finding to humans is unknown. 1 Patients should report symptoms of thyroid tumors (e.g., a lump in the neck, hoarseness, dysphagia, dyspnea) to their clinician. 1 11 Importance of informing patients of the possibility of acute pancreatitis, which may be severe or fatal, with albiglutide therapy. 1 Importance of patients informing clinicians if they have a history of pancreatitis. 1 Importance of informing patients about signs and symptoms of pancreatitis, including persistent severe abdominal pain sometimes radiating to the back that may or may not be accompanied by vomiting; importance of patient discontinuing albiglutide and promptly notifying clinician if such signs or symptoms occur. 1 11 Importance of informing patients of risk of hypoglycemia, particularly if concomitant therapy with an insulin secretagogue (e.g., a sulfonylurea) or insulin is used. 1 11 Importance of reviewing signs, symptoms, and management of hypoglycemia. 1 11 Importance of informing patients of possibility of hypersensitivity reactions. 1 11 Patients should be instructed to discontinue albiglutide and promptly seek medical advice if symptoms of hypersensitivity occur. 1 11 Importance of patients reading the manufacturer's instructions for use before starting albiglutide therapy. 1 Importance of instructing patient regarding proper use, storage, and disposal of injection pen. 1 After dispensing, pens should be stored in the refrigerator, or may be stored at room temperature for up to 4 weeks; injection pens should not be frozen. 1 12 Importance of informing patients not to take an extra dose of albiglutide to make up for a missed dose. 1 If a dose is missed, patients should take the dose as soon as possible within 3 days after the missed dose; the next dose can be taken at the usual weekly time. 1 11 If it has been more than 3 days since the missed dose, the dose should be skipped and the next dose taken at the usual weekly time. 1 11 Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed. 1 11 Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses (e.g., gallstones, pancreatitis, history of alcoholism, high triglyceride concentrations). 1 11 Importance of informing patients of other important precautionary information. 1 (See Cautions.) Preparations Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details. Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations. Albiglutide Routes Dosage Forms Strengths Brand Names Manufacturer Parenteral Powder for Injection, for subcutaneous use 30 mg Tanzeum (available as prefilled single-use injection pen with sterile water for injection diluent, and needle) GlaxoSmithKline 50 mg Tanzeum (available as prefilled single-use injection pen with sterile water for injection diluent, and needle) GlaxoSmithKline AHFS DI Essentials. Copyright 2017, Selected Revisions December 7, 2015. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814. References 1. GlaxoSmithKline. Tanzeum (albiglutide) for injection for subcutaneous use prescribing information. Research Triangle Park, NC; 2014 Jun. 2. Reinhardt R, Nauck MA, Stewart M, et al. Harmony 2 results at week 52 primary endpoint: once-weekly albitlutide monotherapy for patients with type 2 diabetes mellitus inadeequately controlled with diet and exercise. Abstract. 3. Ahrén B, Johnson SL, Stewart M et al. HARMONY 3: 104-Week Randomized, Double-Blind, Placebo- and Active-Controlled Trial Assessing the Efficacy and Safety of Albiglutide Compared With Placebo, Sitagliptin, and Glimepiride in Patients With Type 2 Diabetes Taking Metformin. Diabetes Care . 2014; 37:2141-8. [PubMed 24898304] 4. Reusch J, Stewart M, Perkins C, et al. Harmony 1 results at week 52 primary endpoint: once-weekly albiglutide vs placebo in patients with type 2 diabetes mellitus not controlled in pioglitazone metformin. Abstract. 5. Stewart M, Home P, Yang F, et al.. 52-week efficacy of albiglutide vs placebo and vs pioglitazone in triple therapy (background metformin and glimepiride) in aptients with type 2 diabetes: Harmony 5 study. Abstract. 6. Pratley RE, Nauck MA, Barnett AH et al. Once-weekly albiglutide versus once-daily liraglutide in patients with type 2 diabetes inadequately controlled on oral drugs (HARMONY 7): a randomised, open-label, multicentre, non-inferiority phase 3 study. Lancet Diabetes Endocrinol . 2014; 2:289-97. [PubMed 24703047] 7. Pratley R, Stewart M, Cirkel D, et al. Harmony 4: 52-week efficacy of albiglutide vs insulin glargine in patients with type 2 diabetes mellitus. In: 73rd Scientific Sessions, American Diabetes Association, Chicago, IL, 2013 Jun 21 25. Abstract No. 54-LB. 8. Rosenstock J, Fonseca VA, Gross JL et al. Advancing Basal Insulin Replacement in Type 2 Diabetes Inadequately Controlled With Insulin Glargine Plus Oral Agents: A Comparison of Adding Albiglutide, a Weekly GLP-1 Receptor Agonist, Versus Thrice-Daily Prandial Insulin Lispro. Diabetes Care . 2014; 37:2317-25. [PubMed 24898300] 9. Leiter LA, Carr MC, Stewart M et al. Efficacy and Safety of the Once-Weekly GLP-1 Receptor Agonist Albiglutide Versus Sitagliptin in Patients With Type 2 Diabetes and Renal Impairment: A Randomized Phase III Study. Diabetes Care . 2014; :. 10. Woodward HN, Anderson SL. Once-weekly albiglutide in the management of type 2 diabetes: patient considerations. Patient Prefer Adherence . 2014; 8:789-803. [PubMed 24926194] 11. GlaxoSmithKline. Tanzeum (albiglutide) for injection for subcutaneous use medication guide. Research Triangle Park, NC; 2014 Apr. 12. GlaxoSmithKline. Tanzeum (albiglutide) for injection for subcutaneous use instructions for use. Research Triangle Park, NC; 2014 Jun. 13. US Food and Drug Administration. BLA STB-125431 Tanzeum (Albiglutide) Glucagon-like peptide-1 (GLP-1) receptor agonist risk evaluation and mitigation strategy (REMS). From FDA website. 14. US Food and Drug Administration. Drug Safety Communication: FDA investigating reports of possible increased risk of pancreatitis and pre-cancerous findings of the pancreas from incretin mimetic drugs for type 2 diabetes. Silver Spring, MD; 2013 Mar 14. From FDA website. 15. US Food and Drug Administration. Early communication: reports of possible increased risk of pancreatitis and pre-cancerous findings of the pancreas. Silver Spring, MD; 2013 Mar 14. From FDA website. 16. Singh S, Chang HY, Richards TM et al. Glucagonlike peptide 1-based therapies and risk of hospitalization for acute pancreatitis in type 2 diabetes mellitus: a population-based matched case-control study. JAMA Intern Med. 2013; 173:534-9. 17. Matthews JE, Stewart MW, De Boever EH et al. Pharmacodynamics, pharmacokinetics, safety, and tolerability of albiglutide, a long-acting glucagon-like peptide-1 mimetic, in patients with type 2 diabetes. J Clin Endocrinol Metab . 2008; 93:4810-7. [PubMed 18812476] 18. Seino Y, Inagaki N, Miyahara H et al. A randomized dose-finding study demonstrating the efficacy and tolerability of albiglutide in Japanese patients with type 2 diabetes mellitus. Curr Med Res Opin . 2014; 30:1095-106. [PubMed 24552155] 19. Baggio LL, Huang Q, Brown TJ et al. A recombinant human glucagon-like peptide (GLP)-1-albumin protein (albugon) mimics peptidergic activation of GLP-1 receptor-dependent pathways coupled with satiety, gastrointestinal motility, and glucose homeostasis. Diabetes . 2004; 53:2492-500. [PubMed 15331566] 20. Bush M, Scott R, Watanalumlerd P et al. Effects of multiple doses of albiglutide on the pharmacokinetics, pharmacodynamics, and safety of digoxin, warfarin, or a low-dose oral contraceptive. Postgrad Med . 2012; 124:55-72. [PubMed 23322139] 21. Young MA, Wald JA, Matthews JE et al. Effect of renal impairment on the pharmacokinetics, efficacy, and safety of albiglutide. Postgrad Med . 2014; 126:35-46. [PubMed 24918790] Next Interactions Print this page Add to My Med List More about albiglutide Side Effects During Pregnancy Dosage Information Drug Interactions Support Group En Español 11 Reviews Add your own review/rating Drug class: incretin mimetics Consumer resources Albiglutide Albiglutide Subcutaneous (Advanced Reading) Professional resources Albiglutide (Wolters Kluwer) Other brands: Tanzeum Related treatment guides Diabetes, Type 2} FEATURED: CAR-T Cell Therapy Overview Mechanism of Action KTE-C19 Studies KTE-C19 Cancer Targets Adverse Events Manufacturing Drug Status Rx Availability Prescription only C Pregnancy Category Risk cannot be ruled out N/A CSA Schedule Not a controlled drug Approval History Drug history at FDA Drug Class Incretin mimetics Related Drugs Diabetes, Type 2 metformin , insulin aspart , glipizide , glimepiride , Januvia , pioglitazone , Victoza , Actos , Tradjenta , Glucophage , glyburide , Janumet , Invokana , Amaryl , Welchol , Onglyza , sitagliptin , Trulicity , Jardiance , Lantus , Farxiga , Levemir , Tresiba , Glucotrol , Bydureon , More... 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