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]
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| Routes of administration | subcutaneous |
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| Pharmacokinetic data | |
| Bioavailability | N/A |
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| Chemical and physical data | |
| Formula | C152H232N40O45 |
| Molar mass | 3339.763 g·mol−1 |
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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[update] 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.