Abstract
Insulin degludec is, like insulin detemir, a product of coupling of Des-B30 threonine insulin to fatty acid side chains. After injection, degludec self associates, precipitating in subcutaneous tissue. There is a continuous and highly predictable slow dissociation of insulin monomers from this depot; insulin levels rise immediately reaching tmax at 10-12 hours, followed by a slow decline with a t1/2 of 17-21 hours, roughly double the duration of action of insulin glargine. An important property of degludec not shared by glargine is miscibility with rapid-acting insulin. Although the effect of coadministered insulin aspart is somewhat blunted by coformulation with degludec, a preparation of 70% degludec and 30% aspart has predictable pharmacodynamics. Daily administration of degludec has glucose-lowering benefits not different from those of glargine, with purportedly less hypoglycemia. Although degludec is approved and marketed in Europe under the brand name Tresiba®, the U.S. Food and Drug Administration, in a surprising development, challenged the assertion of lower tendency to hypoglycemia with degludec, and, more importantly, raised concerns that degludec may have a higher cardiovascular risk than glargine. Only a long-term study in a large patient population can resolve these questions. However, release of degludec for marketing to appropriate patients should proceed while awaiting the results of such a study.
| Original language | English |
|---|---|
| Pages (from-to) | 387-397 |
| Number of pages | 11 |
| Journal | Drugs of Today |
| Volume | 49 |
| Issue number | 6 |
| DOIs | |
| State | Published - Jun 2013 |
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All Science Journal Classification (ASJC) codes
- Pharmacology
- Pharmacology (medical)
Cite this
Insulin degludec : A long-acting modern insulin analogue with a predictable pharmacokinetic/ pharmacodynamic profile. / Rendell, Marc.
In: Drugs of Today, Vol. 49, No. 6, 06.2013, p. 387-397.Research output: Contribution to journal › Review article
}
TY - JOUR
T1 - Insulin degludec
T2 - A long-acting modern insulin analogue with a predictable pharmacokinetic/ pharmacodynamic profile
AU - Rendell, Marc
PY - 2013/6
Y1 - 2013/6
N2 - Insulin degludec is, like insulin detemir, a product of coupling of Des-B30 threonine insulin to fatty acid side chains. After injection, degludec self associates, precipitating in subcutaneous tissue. There is a continuous and highly predictable slow dissociation of insulin monomers from this depot; insulin levels rise immediately reaching tmax at 10-12 hours, followed by a slow decline with a t1/2 of 17-21 hours, roughly double the duration of action of insulin glargine. An important property of degludec not shared by glargine is miscibility with rapid-acting insulin. Although the effect of coadministered insulin aspart is somewhat blunted by coformulation with degludec, a preparation of 70% degludec and 30% aspart has predictable pharmacodynamics. Daily administration of degludec has glucose-lowering benefits not different from those of glargine, with purportedly less hypoglycemia. Although degludec is approved and marketed in Europe under the brand name Tresiba®, the U.S. Food and Drug Administration, in a surprising development, challenged the assertion of lower tendency to hypoglycemia with degludec, and, more importantly, raised concerns that degludec may have a higher cardiovascular risk than glargine. Only a long-term study in a large patient population can resolve these questions. However, release of degludec for marketing to appropriate patients should proceed while awaiting the results of such a study.
AB - Insulin degludec is, like insulin detemir, a product of coupling of Des-B30 threonine insulin to fatty acid side chains. After injection, degludec self associates, precipitating in subcutaneous tissue. There is a continuous and highly predictable slow dissociation of insulin monomers from this depot; insulin levels rise immediately reaching tmax at 10-12 hours, followed by a slow decline with a t1/2 of 17-21 hours, roughly double the duration of action of insulin glargine. An important property of degludec not shared by glargine is miscibility with rapid-acting insulin. Although the effect of coadministered insulin aspart is somewhat blunted by coformulation with degludec, a preparation of 70% degludec and 30% aspart has predictable pharmacodynamics. Daily administration of degludec has glucose-lowering benefits not different from those of glargine, with purportedly less hypoglycemia. Although degludec is approved and marketed in Europe under the brand name Tresiba®, the U.S. Food and Drug Administration, in a surprising development, challenged the assertion of lower tendency to hypoglycemia with degludec, and, more importantly, raised concerns that degludec may have a higher cardiovascular risk than glargine. Only a long-term study in a large patient population can resolve these questions. However, release of degludec for marketing to appropriate patients should proceed while awaiting the results of such a study.
UR - http://www.scopus.com/inward/record.url?scp=84880009335&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84880009335&partnerID=8YFLogxK
U2 - 10.1358/dot.2013.49.6.1976051
DO - 10.1358/dot.2013.49.6.1976051
M3 - Review article
C2 - 23807942
AN - SCOPUS:84880009335
VL - 49
SP - 387
EP - 397
JO - Drugs of Today
JF - Drugs of Today
SN - 0025-7656
IS - 6
ER -