IGF-1 LR3 — pharmacology
Molecular targets, mechanism of action, pharmacokinetics and interactions as characterised in humans.
§2Pharmacology
§2.1Molecular targets
Table 2. Molecular targets recorded for IGF-1 LR3, with the character of the interaction and the potency where the Institute holds it.
| Target | Interaction | Note |
|---|---|---|
| IGF-1 receptor (IGF1R) | Agonist | Retains high affinity |
| Insulin receptor | Weak agonist | Cross-reactivity is the basis of the hypoglycaemia risk |
| IGF-binding proteins 1–6 | Markedly reduced binding | The design feature that extends half-life and simultaneously removes a physiological buffering mechanism |
§2.2Mechanism of action
IGF-1 receptor agonism with greatly reduced binding-protein sequestration. The consequence is a sustained, unbuffered IGF-1 receptor signal. Because the IGF-binding proteins normally constrain free IGF-1 to a small fraction of total, removing that constraint changes the pharmacology qualitatively rather than merely quantitatively, and the Institute regards the safety implications as under-appreciated.[1,2]
§2.3Pharmacokinetics
- Terminal half-life
- reported as substantially longer than native IGF-1, whose free half-life is approximately 10 minutes
- Time to maximum concentration
- not published
- Volume of distribution
- not published
- Plasma protein binding
- markedly reduced
- Clearance
- not published
- Bioavailability
- not published
Not characterised in humans for this analogue.
§2.4Interactions
- Insulin and secretagogues — additive hypoglycaemia risk
References cited on this page
References are numbered in order of first citation in this document. Each superscript in the text links to its entry below.
- International Council for Harmonisation of Technical Requirements for Pharmaceuticals for Human Use. ICH Q6B Specifications: Test Procedures and Acceptance Criteria for Biotechnological/Biological Products. ICH Harmonised Tripartite Guideline 1999;Step 4 version. identifier not held by the Institute
- United States Pharmacopeial Convention. General Chapter ⟨85⟩ Bacterial Endotoxins Test. United States Pharmacopeia — National Formulary (USP–NF) 2024;USP 2024 Issue 1. identifier not held by the Institute
Identifiers are reproduced only where the Institute holds them. Where a digital object identifier or PubMed identifier is not shown, the Institute has recorded the journal and year and has not constructed an identifier.