Half-life prolongation of therapeutic proteins by conjugation to ATIII-binding pentasaccharides: A first-in-human study of CarboCarrier® insulin

British Journal of Clinical Pharmacology

Volumn 75, Issue 5, 2013, Pages 1221-1230

  Miltenburg, André M M ^a   Prohn, Marita ^b   van Kuijk, Jacqueline H M ^c   Tiessen, Renger G ^d   de Kort, Martin ^e   Berg, Rob J W ^a  

^a Merck Sharp and Dohme   (Netherlands)

^b PK PD   (Netherlands)

^c Statistical Department   (Netherlands)

^d PRA Health Sciences   (Netherlands)

^e Organon BioSciences   (Netherlands)

Author keywords

CarboCarrier ; Diabetes; Insulin

Indexed keywords

C PEPTIDE; CARBOCARRIER; GLUCOSE; INSULIN; ISOPHANE INSULIN; PLACEBO; SCH 900948; UNCLASSIFIED DRUG;

ADULT; AREA UNDER THE CURVE; ARTICLE; ATTENTION; BACKACHE; CONTROLLED STUDY; DIABETIC PATIENT; DIET RESTRICTION; DIZZINESS; DOSE RESPONSE; DRUG CLEARANCE; DRUG CONJUGATION; DRUG ELIMINATION; DRUG EXPOSURE; DRUG FATALITY; DRUG HALF LIFE; DRUG SAFETY; DRUG TOLERABILITY; FEMALE; FOOD INTAKE; GLUCOSE BLOOD LEVEL; HEADACHE; HUMAN; HUMAN EXPERIMENT; HUNGER; HYPOGLYCEMIA; MALE; MAXIMUM PLASMA CONCENTRATION; NAUSEA; NON INSULIN DEPENDENT DIABETES MELLITUS; NORMAL HUMAN; PRIORITY JOURNAL; PROTEIN BLOOD LEVEL; RANDOMIZED CONTROLLED TRIAL; SIDE EFFECT; SINGLE DRUG DOSE; SOMNOLENCE; TIME TO MAXIMUM PLASMA CONCENTRATION;

ADOLESCENT; ADULT; AGED; AREA UNDER CURVE; BIOLOGICAL AVAILABILITY; BLOOD GLUCOSE; C-PEPTIDE; DIABETES MELLITUS, TYPE 2; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG CARRIERS; FEMALE; GLYCOPROTEINS; HALF-LIFE; HEMOGLOBIN A, GLYCOSYLATED; HUMANS; HYPOGLYCEMIC AGENTS; INJECTIONS, SUBCUTANEOUS; INSULIN; INSULIN, LONG-ACTING; MALE; MIDDLE AGED; OLIGOSACCHARIDES; YOUNG ADULT;

EID: 84876052188     PISSN: 03065251     EISSN: 13652125     Source Type: Journal    
DOI: 10.1111/j.1365-2125.2012.04460.x     Document Type: Article

References (11)

1. Beals JM, Shanafelt AB. Enhancing exposure of protein therapeutics. Drug Discov Today Techn 2006; 3: 87-94.
2. De Kort M, Gianotten B, Wisse JAJ, Bos ES, Eppink MHM, Mattaar E, Vogel GMT, Dokter WHA, Honing M, Vonsovic S, Smit M-J, Wijkmans JCHM, van Boeckel CAA. Conjugation of ATIII-binding pentasaccharides to extend the half-life of proteins: long-acting insulin. Chem Med Chem 2008; 3: 1189-1193.
3. Pickup JC, Renard E. Long-acting insulin analogs vs. Insulin pump therapy for the treatment of type 1 and type 2 diabetes. Diabetes Care 2008; 31: (Suppl 2): S140-S145.
4. Hirsch IB. Insulin analogues. N Engl J Med 2005; 352: 174-183.
5. Wang F, Carabino JM, Vergara CM. Insulin glargine: a systematic review of a long-acting insulin analogue. Clin Ther 2003; 25: 1541-1577.
6. Home P, Kurtzhals P. Insulin detemir: from concept to clinical experience. Expert Opin Pharmacother 2006; 7: 325-343.
7. Heise T, Pieber TR. Towards peakless, reproducible and long-acting insulins. An assessment of the basal analogues based on isoglycaemic clamp studies. Diabetes Obes Metab 2007; 9: 648-659.
8. Zinman B, Fulcher G, Rao PV, Thomas N, Endahl LA, Johansen T, Lindh R, Lewin A, Rosenstack J, Pinget M, Mathieu C. Insulin degludec, an ultra-long-acting basal insulin, once a day or three times a week versus insulin glargine once a day in patients with type 2 diabetes: a 16-week, randomised, open-label, phase 2 trial. Lancet 2011; 377: 924-931.
9. Veyrat-Follet C, Vivier N, Trellu M, Dubruc C, Sanderink GJ. The pharmacokinetics of idraparinux, a long-acting indirect factor Xa inhibitor: population pharmacokinetic analysis from Phase III clinical trials. J Thromb Haemost 2009; 7: 559-565.
10. Watanabe M, Hayasaki H, Tamayama T, Shimada M. Histologic distribution of insulin and glucagon receptors. Braz J Med Biol Res 1998; 31: 243-256.
11. Bos ES, de Kort M, Smit MJ, van Boeckel CAA. PCT. Pat. Appl. WO/2006/082184, 2006, 95.