Insulin glulisine

also known as: Apidra, HMR1964

Sanofi's rapid-acting insulin analog (Apidra, 2004) — the third rapid-acting analog approved, differentiated by being zinc-free in formulation, which gives it slightly faster monomeric onset than lispro or aspart.

A rapid-acting insulin analog (Apidra, Sanofi, FDA-approved 2004) with two B-chain substitutions — asparagine-B3 → lysine and lysine-B29 → glutamate — that together with a zinc-free polysorbate-20-stabilized formulation produce an absorption profile slightly faster than lispro or aspart, particularly in patients with higher BMI.

Mechanism of action

Insulin receptor agonism. The zinc-free formulation means the drug is already predominantly monomeric in the vial, so SC absorption is not limited by hexamer dissociation. The B3 and B29 charge changes stabilize the monomer against self-association even without zinc.

Primary uses

Type 1 diabetes mellitus (mealtime bolus)
Type 2 diabetes mellitus requiring prandial insulin
Insulin pump therapy (CSII)

Typical dosing

with meals (subcutaneous or IV)

Fully individualized.

Regulatory status

FDA-approved 2004 as Apidra (Sanofi).

References

[fda-pi] FDA. Apidra (insulin glulisine) prescribing information. Sanofi, updated 2023.
[pubmed] Becker RH. "Insulin glulisine complementing basal insulins: a review of structure and activity." Diabetes Technol Ther, 2007;9:109-121.

Related peptides

Insulin lispro

The first FDA-approved rapid-acting insulin analog (Humalog, Lilly, 1996) — the B28–B29 position swap prevents hexamer self-association, producing faster subcutaneous absorption than regular human insulin.

Insulin aspart

Novo Nordisk's rapid-acting insulin analog (NovoLog / NovoRapid, approved 2000) — the B28 proline → aspartate substitution destabilizes hexamer formation, and the ultra-rapid Fiasp formulation (2017) adds niacinamide and L-arginine for even faster absorption.

Regular human insulin

The original recombinant human insulin (Humulin R, 1982) — unmodified native sequence, short-acting kinetics driven by hexamer self-association; U-500 concentration for severely insulin-resistant patients.

Disclaimer

This entry is for educational purposes only and does not constitute medical advice. Dosing information reflects published regulatory or research data and is not a recommendation. Many compounds described here are not approved for human use in the United States. Consult a licensed medical professional before considering any peptide therapy.