Linagliptin was originally discovered at Boehringer Ingelheim as
an orally active dipeptidyl peptidase-IV (DPP-4) inhibitor. Eli Lilly
and Boehringer Ingelheim co-developed and launched linagliptin
for type II diabetes as an adjunct to diet and exercise for the
improvement of adult glycemic control. Linagliptin has a superior
DPP-4 IC50 value of 1 nM, compared with 19 nM for sitagliptin,
24 nM for alogliptin, 50 nM for saxagliptin and 62 nM for vildagliptin. In addition, linagliptin exhibited prolonged pharmacodynamic
activity with long-lasting DPP-4 inhibition in several
preclinical species. Linagliptin showed good efficacy in phase II
clinical trials with doses as low as 5 mg and no signs of hypoglycemia
with doses as high as 600 mg. The prolonged pharmacological
effect of DPP-4 activity and the good safety/tolerability profile
provided the basis for linagliptin’s approval.
화학적 성질
White to Off-White Solid
용도
Biological Activity Chemical Information Tech Support & FAQs
Biological Activity
Deferasirox(Exjade) is a rationally-designed oral iron chelator. Its main use is to reduce chronic iron overload in patients who are receiving long-term blood transfusions
정의
ChEBI: A member of the class of triazoles, deferasirox is 1,2,4-triazole substituted by a 4-carboxyphenyl group at position 1 and by 2-hydroxyphenyl groups at positions 3 and 5. An orally active iron chelator, it is used to manage chronic iron overload in patient
receiving long-term blood transfusions.
