Cumulative clinical experience with use of insulin lispro: critical appraisal, role in therapy, and patient considerations

Figures & data

Figure 1 Structure of insulin lispro, showing the amino acid modifications that produce insulin lispro.

Modified from PDB ID: 3E7Y Timofeev VI, Baidus AN, Kislitsyn YA, Juranova IP.

Figure 2 (A) Concentration of insulin lispro reaches its peak in half of the time that human regular insulin takes to reach its peak. (B) The highest glucose infusion rate is reached in half of the time for insulin lispro compared with human regular insulin.

Reprinted with permission from Holleman MD, Hoekstrra JBL. Insulin Lispro. N Engl J Med. 1997;337:176–183.⁶⁷

Table 1 Comparison of human regular insulin and insulin lispro^2–4

		Human regular insulin (SC)	Insulin lispro (SC)
Pharmacokinetics	Maximum serum insulin level (pM)	308 ± 132	698 ± 227
	Time to peak concentration (minutes)	101 ± 40	42 ± 20
	Area under the serum insulin concentration versus time curve (nmol · min^−1·· L^−1)	72.7 ± 12.3	71.4 ± 14.6
Pharmacodynamics	Onset of action (minutes)	30–60	5–15
	Peak of action (hours)	2–3	0.5–1.5
	Duration of action (hours)	6–10	4–5
	Maximum glucose infusion rate (mmol/minute)	2.20 ± 1.01	3.10 ± 1.19
	Time to maximum glucose infusion rate (minutes)	179 ± 93	99 ± 39
	Total amount of glucose infused (mmol)	454.7 ± 167.4	450.8 ± 161.8
Receptor affinity and mitogenicity	Insulin receptor affinity (%)	100	84 ± 6
	Insulin receptor off rate (%)	100	100 ± 11
	Metabolic potency (%)	100	82 ± 3
	IGF-1 receptor potency (%)	100	156 ± 16
	Mitogenic potency (%)	100	66 ± 10

Abbreviations: IGF-1, insulin growth-like factor 1; SC, subcutaneous.

Holleman MD Hoekstrra JBL Insulin Lispro N Engl J Med 1997 337 176 183 9219705

 PubMed Web of Science ®Google Scholar

Howey DC Bowsher RR Brunelle RL Woodworth JR Lys(B28), pro(B29)-human insulin. A rapidly absorbed analogue of human insulin Diabetes 1994 43 3 396 402 8314011

 PubMed Web of Science ®Google Scholar

Kurtzhals P Schaffer L Sorensen A Correlations of receptor binding and metabolic and mitogenic potencies of insulin analogs designed for clinical use Diabetes 2000 49 6 999 1005 10866053

 PubMed Web of Science ®Google Scholar