Chemistry:Taspoglutide

From HandWiki

Taspoglutide is a former experimental drug, a glucagon-like peptide-1 agonist (GLP-1 agonist), that was under investigation for treatment of type 2 diabetes and being codeveloped by Ipsen and Roche.[1] [2]

Initially, phase II trials reported it was effective and well tolerated.[3]

Of the eight planned phase III clinical trials of weekly taspoglutide (four against exenatide, sitagliptin, insulin glargine, and pioglitazone), at least five were active in 2009.[4] Preliminary results in early 2010 were favourable.[5] (At least one of the eight planned phase III trials had not started recruiting by end 2009.[6])

In September 2010 Roche halted Phase III clinical trials due to instances of serious hypersensitivity reactions and gastrointestinal side effects.[7][8][9]

As of May 2022 no new trials have been registered since 2010.[10]

Chemistry

Taspoglutide is the peptide with the sequence His-Aib-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys-Glu-Phe-Ile-Ala-Trp-Leu-Val-Lys-Aib-Arg-NH2, where Aib is 2-aminoisobutyric acid (2-methylalanine).

In other words, it is the 8-(2-methylalanine)-35-(2-methylalanine)-36-L-argininamide derivative of the amino acid sequence 7–36 of human glucagon-like peptide I.

See also

References

  1. "Ipsen: Roche Moves Investigational Diabetes Drug, Taspoglutide, into Phase III Clinical Trials". Business Wire. June 2008. http://findarticles.com/p/articles/mi_m0EIN/is_2008_June_10/ai_n25492242. 
  2. "Roche Moves Investigational Diabetes Drug, Taspoglutide, Into Phase III Clinical Trials". June 2008. http://www.bio-medicine.org/medicine-technology-1/Roche-Moves-Investigational-Diabetes-Drug--Taspoglutide--Into-Phase-III-Clinical-Trials-2379-1/. 
  3. "Glucagon-like Peptide-1 Analogs Other Than Exenatide". 2008. http://www.medscape.com/viewarticle/578304. 
  4. "Ipsen's Partner Roche Announces That Taspoglutide Meets Its Primary Endpoint in the First Phase III Clinical Trial". October 2009. http://www.medicalnewstoday.com/articles/169171.php. 
  5. "Roche Reports Positive Data from Five Phase III Trials of Type 2 Diabetes Therapy". February 2010. http://www.genengnews.com/news/bnitem.aspx?name=75286047. 
  6. Clinical trial number NCT01051011 for "A Study to Compare Taspoglutide and Insulin Glargine in Insulin-Naïve Patients With Type 2 Diabetes Mellitus Inadequately Controlled on Metformin and Sulfonylurea Combination Therapy" at ClinicalTrials.gov
  7. "Roche Halts Trials of Taspoglutide". 13 September 2010. http://www.medpagetoday.com/Endocrinology/Diabetes/22139. 
  8. "Retatrutide | Peptides". 13 September 2010. https://peptidescostarica.net/retatrutide-costa-rica/. 
  9. "Experimental Diabetes Drug Taspoglutide Late-Stage Trials Suspended". 13 September 2010. http://www.medicalnewstoday.com/articles/200893.php. 
  10. Clinical studies of taspoglutide