Taspoglutide

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Taspoglutide
Clinical data
Routes of
administration
subcutaneous
ATC code
  • none
Pharmacokinetic data
Bioavailability N/A
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
Chemical and physical data
Formula C152H232N40O45
Molar mass 3339.75 g/mol
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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][needs update]

Chemistry[edit]

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[edit]

References[edit]

  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; et al. (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. ^ "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".
  7. ^ "Roche Halts Trials of Taspoglutide".
  8. ^ "Experimental Diabetes Drug Taspoglutide Late-Stage Trials Suspended".
  9. ^ Clinical studies of taspoglutide