Taspoglutide

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

Two 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 incidences of serious hypersensitivity reactions and gastrointestinal side effects.[7][8]

As of May 2013 no new trials had been registered.[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.

Chemistry

Taspoglutide was a promising Glucagon-like Peptide 1 receptor agonist and Incretin mimetic. The short duration of action was likely its demise.

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.
  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.
  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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