Skip to main content

New Drug Approvals 2014 - Pt. X - Albiglutide (Eperzan™ or Tanzeum™)

By


Wikipedia: Albiglutide
ChEMBL: CHEMBL2107841

On April 15th the FDA approved Tanzeum (albiglutide) subcutaneous injection to improve glycemic control, along with diet and exercise, in adults with type 2 diabetes.

Type II diabetes

Type II diabetes is a metabolic disorder that is characterized by high blood sugar (hyperglycemia) due to insulin resistance or relative lack of insulin. The disease affects millions of patient world-wide and can lead to long-term complications if the blood levels are not lowered in the patients: heart diseases, strokes and kidney failure.

Albiglutide

The drug is a dipeptidyl peptidase-4-resistant glucagon-like peptide-1 dimer fused to human albumin.
Schematic representation of the albiglutide (EMA)

Mode of action

Traditionally, a decrease in the glucose blood level of affected patients is triggered using insulin injections. One alternative mechanism consists at indirectly stimulating insulin release using a glucagon-like peptide-1 (GLP-1) or an analogue of the corresponding receptor.
GLP-1 receptor agonists are of particular interest, as they naturally stop simulating insulin release when plasma glucose concentration is in the fasting range, and hence preventing hypoglycemia in the patient too.
The natural half-life of GLP-1 is less than 2 minutes in the human blood, the peptide is rapidly degraded by an enzyme called dipeptidyl peptidase-4. On the other hand, albiglutide half-life ranges between four to seven days (resistance to dipeptidyl peptidase-4), a considerably longer time than endogenous peptide and than the others GLP-1 analogous drugs (exenatide and liraglutide). This property allows to reduce the number of injections in diabetic patient to biweekly or weekly instead of daily, hence considerably increasing treatment overheads.

Clinical trials

A series of eight clinical trials involving over 2,000 patients with type II diabetes demonstrated the safety and effectiveness of the drug. Patients reported improved HbA1c level (hemoglobin A1c or glycosylated hemoglobin, a measure of blood sugar control). The most common side-effects observed were diarrhea, nausea, and injection site reactions.

Indication and warnings

Albiglutide can be used as a stand-alone as well as in combination therapy (with metformin, glimepiride, pioglitazone, or insulin for instance). The drug is not suited to treat type I diabetes and not indicated for patients with increased ketones in their blood or urine. Albiglutide should be used only when diet and exercise therapies are not successful.
The drug has an FDA boxed warning, as cases of tumors of the thyroid gland have been observed in rodent studies with some other GLP-1 receptor agonists. The FDA further required post-marketing studies regarding dose, efficacy and safety in pediatric patients and for cardiovascular outcomes in patients with high baseline risk of cardiovascular disease.

Tradenames

The drug was invented by Human Genome Sciences and was developed in collaboration with GSK. Albiglutide is marketed as Eperzan in Europe and Tanzeum in the USA.
Labels:

Comments

Post a Comment

Popular posts from this blog

New SureChEMBL announcement

By
(Generated with DALL-E 3 ∙ 30 October 2023 at 1:48 pm) We have some very exciting news to report: the new SureChEMBL is now available! Hooray! What is SureChEMBL, you may ask. Good question! In our portfolio of chemical biology services, alongside our established database of bioactivity data for drug-like molecules ChEMBL , our dictionary of annotated small molecule entities ChEBI , and our compound cross-referencing system UniChem , we also deliver a database of annotated patents! Almost 10 years ago , EMBL-EBI acquired the SureChem system of chemically annotated patents and made this freely accessible in the public domain as SureChEMBL. Since then, our team has continued to maintain and deliver SureChEMBL. However, this has become increasingly challenging due to the complexities of the underlying codebase. We were awarded a Wellcome Trust grant in 2021 to completely overhaul SureChEMBL, with a new UI, backend infrastructure, and new f
Post a Comment
Read more

Legacy SureChEMBL retirement

By
Dear SureChEMBL users, About six months ago, we introduced the new version of SureChEMBL . It brought significant improvements in terms of performance and stability, and it also allows us to implement new functionalities. After the survey at the beginning of the year, we prioritised what should be delivered first. You should see the materialisation of our work in the coming months. As originally announced when the new SureChEMBL was introduced, the plan was to shut down the old system permanently to focus all our resources on the new SureChEMBL. This time has come, so expect www.surechembl-legacy.org to be unreachable in the coming days with no turning back! Consequently, and in parallel, the new SureChEMBL will lose its Beta status, and we will stop referring to it as the new version. This does not mean we are reducing our efforts to improve our system; on the contrary, this removes a distraction! If you have any feedback, you can contact us directly at surechembl-help@ebi.ac.uk . W
Post a Comment
Read more

ChEMBL & SureChEMBL anniversary symposium

By
  In 2024 we celebrate the 15th anniversary of the first public release of the ChEMBL database as well as the 10th anniversary of SureChEMBL. To recognise this important landmark we are organising a two-day symposium to celebrate the work achieved by ChEMBL and SureChEMBL, and look forward to its future.   Save the date for the ChEMBL 15 Year Symposium October 1-2, 2024     Day one will consist of four workshops, a basic ChEMBL drug design workshop; an advanced ChEMBL workshop (EUbOPEN community workshop); a ChEMBL data deposition workshop; and a SureChEMBL workshop. Day two will consist of a series of talks from invited speakers, a few poster flash talks, a local nature walk, as well as celebratory cake. During the breaks, the poster session will be a great opportunity to catch up with other users and collaborators of the ChEMBL resources and chat to colleagues, co-workers and others to find out more about how the database is being used. Lunch and refreshments will be pro
Post a Comment
Read more

ChEMBL 34 is out!

By
We are delighted to announce the release of ChEMBL 34, which includes a full update to drug and clinical candidate drug data. This version of the database, prepared on 28/03/2024 contains:         2,431,025 compounds (of which 2,409,270 have mol files)         3,106,257 compound records (non-unique compounds)         20,772,701 activities         1,644,390 assays         15,598 targets         89,892 documents Data can be downloaded from the ChEMBL FTP site:  https://ftp.ebi.ac.uk/pub/databases/chembl/ChEMBLdb/releases/chembl_34/ Please see ChEMBL_34 release notes for full details of all changes in this release:  https://ftp.ebi.ac.uk/pub/databases/chembl/ChEMBLdb/releases/chembl_34/chembl_34_release_notes.txt New Data Sources European Medicines Agency (src_id = 66): European Medicines Agency's data correspond to EMA drugs prior to 20 January 2023 (excluding vaccines). 71 out of the 882 newly added EMA drugs are only authorised by EMA, rather than from other regulatory bodies e.g.
Post a Comment
Read more

A python client for accessing ChEMBL web services

By
Motivation The CheMBL Web Services provide simple reliable programmatic access to the data stored in ChEMBL database. RESTful API approaches are quite easy to master in most languages but still require writing a few lines of code. Additionally, it can be a challenging task to write a nontrivial application using REST without any examples. These factors were the motivation for us to write a small client library for accessing web services from Python. Why Python? We choose this language because Python has become extremely popular (and still growing in use) in scientific applications; there are several Open Source chemical toolkits available in this language, and so the wealth of ChEMBL resources and functionality of those toolkits can be easily combined. Moreover, Python is a very web-friendly language and we wanted to show how easy complex resource acquisition can be expressed in Python. Reinventing the wheel? There are already some libraries providing access to ChEMBL d
1 comment
Read more