Taspoglutide

Taspoglutide

Clinical data
Routes of administration	subcutaneous
ATC code	none
Pharmacokinetic data
Bioavailability	N/A
Identifiers
CAS Number	275371-94-3
ChemSpider	none
UNII	2PHK27IP3B
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]

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

• Glucagon-like peptide-1 analogs:

exenatide (Byetta)

liraglutide (Victoza)

albiglutide

• DPP4 inhibitors
• Incretin

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; 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