Taspoglutide

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]

Taspoglutide
Clinical data
Routes of
administration		subcutaneous
ATC code
  • none
Pharmacokinetic data
BioavailabilityN/A
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
Chemical and physical data
FormulaC152H232N40O45
Molar mass3339.763 g·mol−1
 ☒NcheckY (what is this?)  (verify)

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]

As of May 2022 no new trials have been registered since 2010.[9]

Chemistry

Taspoglutide is the peptide with the sequence H2N-His-2-methyl-Ala-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-2-methyl-Ala-Arg-CONH2.

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.
  2. "Roche Moves Investigational Diabetes Drug, Taspoglutide, Into Phase III Clinical Trials". June 2008. Archived from the original on 3 March 2016. Retrieved 13 January 2009.
  3. Baggio LL, Drucker DJ (2008). "Glucagon-like Peptide-1 Analogs Other Than Exenatide".
  4. "Ipsen's Partner Roche Announces That Taspoglutide Meets Its Primary Endpoint in the First Phase III Clinical Trial". October 2009. Archived from the original on 1 March 2010. Retrieved 12 February 2010.
  5. "Roche Reports Positive Data from Five Phase III Trials of Type 2 Diabetes Therapy". February 2010.
  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.
  8. "Experimental Diabetes Drug Taspoglutide Late-Stage Trials Suspended". 13 September 2010.
  9. Clinical studies of taspoglutide


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