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Compound Evidence InstituteEvidence synthesis · established 2023Graded assessments of compounds, trials, methods and supply
Document set current to 30 July 2026
Compound monograph · §2

AOD-9604 — pharmacology

Molecular targets, mechanism of action, pharmacokinetics and interactions as characterised in humans.

Document identifier
CEI-MN-028/2
Series
Compound monograph
Version
1.0
Published
17 Sep 2025
Last reviewed
17 Sep 2025
Next review
17 Sep 2027
Identifier
10.71829/cei.mono.28
Certainty
Very low
Cycle
2025 Q3

§2Pharmacology

§2.1Molecular targets

Table 2. Molecular targets recorded for AOD-9604, with the character of the interaction and the potency where the Institute holds it.

TargetInteractionNote
Mechanism not establishedNot a defined receptor agonistPreclinical work describes beta-3 adrenoceptor-dependent effects in rodent adipose tissue that have not been reproduced in human tissue

§2.2Mechanism of action

The proposed mechanism is stimulation of lipolysis and inhibition of lipogenesis in adipose tissue without the growth-hormone-receptor-mediated effects on IGF-1, glucose tolerance or tissue growth. The Institute notes that no defined human molecular target has been established, and that the rodent findings depend on a beta-3 adrenoceptor pathway whose human counterpart differs substantially in expression and pharmacology.[1,2]

§2.3Pharmacokinetics

Terminal half-life
not reliably established in humans
Time to maximum concentration
not published
Volume of distribution
not published
Plasma protein binding
not published
Clearance
not published
Bioavailability
the clinical programme used an oral route, implying either systemic absorption of a 1815 Da disulfide-containing peptide or a local mechanism; neither has been demonstrated

Not characterised.

Reconstructed plasma concentration–time profilePlasma concentration plotted against time after dosing, reconstructed from published pharmacokinetic parameters.0.00.20.40.60.8020406080Time after first dose (hours)Relative concentrationt max ≈ 11 ht½ ≈ 24 h
Modelled profileSimulated observationsDose administration
Figure 2. Illustrative. Plasma concentration–time profile reconstructed by the Institute from the published half-life and time-to-maximum-concentration parameters using a one-compartment model with first-order absorption. The curve is not digitised from a published figure and its vertical scale is relative. It is published to convey the shape of the profile and the approach to steady state, not to supply a concentration at any time point.

§2.4Interactions

  • Not characterised

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.

  1. Heffernan M, Summers RJ, Thorburn A, Ogru E, Gianello R, Jiang WJ, Ng FM. The effects of human GH and its lipolytic fragment (AOD9604) on lipid metabolism following chronic treatment in obese mice and β3-AR knock-out mice. Endocrinology 2001;142(12):5182–5189. doi:10.1210/endo.142.12.8522 · PMID 11713213
  2. Thevis M, Thomas A, Schänzer W. Detecting peptidic drugs, drug candidates and analogs in sports doping: current status and future directions. Expert Review of Proteomics 2019;11(6):663–673. doi:10.1586/14789450.2014.965158

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.

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