FDA Approved Metabolic & Weight Loss

Insulin lispro

also known as: Humalog, Admelog, Lyumjev, LY275585

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.

The first FDA-approved rapid-acting insulin analog (Humalog, Eli Lilly, approved 1996), created by swapping the positions of proline (B28) and lysine (B29) on the insulin B-chain to destabilize hexamer formation and accelerate subcutaneous absorption; Lyumjev (2020) is the same molecule with treprostinil and citrate excipients for ultra-rapid kinetics, and Admelog (Sanofi, 2017) is a follow-on biologic.

Mechanism of action

Insulin receptor agonism — drives glucose uptake into muscle and adipose tissue, suppresses hepatic gluconeogenesis, and promotes glycogen and lipid synthesis. The B28–B29 swap prevents the zinc-coordinated hexamer self-association that delays absorption of regular human insulin, accelerating onset.

Primary uses

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

Typical dosing

with meals (subcutaneous or IV)

Dosing is fully individualized — varies from <10 units/day to >100 units/day depending on insulin sensitivity and carbohydrate intake.

Regulatory status

FDA-approved 1996 as Humalog (Lilly). Admelog (Sanofi follow-on biologic) approved 2017. Lyumjev (Lilly ultra-rapid formulation with treprostinil/citrate) approved 2020.

References

  1. [fda-pi] FDA. Humalog (insulin lispro) prescribing information. Eli Lilly, updated 2024.
  2. [fda-pi] FDA. Lyumjev (insulin lispro-aabc) prescribing information. Eli Lilly, 2020.
  3. [pubmed] Howey DC, et al. "[Lys(B28), Pro(B29)]-human insulin: a rapidly absorbed analogue of human insulin." Diabetes, 1994;43:396-402.

Related peptides

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.

Insulin glulisine

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.

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.

Semaglutide

A once-weekly GLP-1 receptor agonist FDA-approved for type 2 diabetes and chronic weight management.
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.