Taspoglutide

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Taspoglutide
Clinical data
Legal status ?
Routes subcutaneous
Pharmacokinetic data
Bioavailability N/A
Identifiers
CAS number 275371-94-3 N
ATC code None
UNII 2PHK27IP3B YesY
Chemical data
Formula C152H232N40O45 
Mol. mass 3339.75 g/mol
 N (what is this?)  (verify)

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

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
Oral anti-diabetic drugs and Insulin analogs (A10)
Insulin
Sensitizers
TZDs/"glitazones" (PPAR)
Dual PPAR agonists
Secretagogues
Meglitinides/"glinides"
  • Fasiglifam†
Analogs/other insulins
Other
Amylin analog
SGLT2 inhibitors
Other

M: END

anat/phys/devp/horm

noco (d)/cong/tumr, sysi/epon

proc, drug (A10/H1/H2/H3/H5)


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