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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

Petrelintide — pharmacology

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

Document identifier
CEI-MN-016/2
Series
Compound monograph
Version
3.2
Published
20 Jul 2024
Last reviewed
20 Apr 2025
Next review
20 Apr 2027
Identifier
10.71829/cei.mono.16
Certainty
Low
Cycle
2024 Q3

§2Pharmacology

§2.1Molecular targets

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

TargetInteractionNote
Amylin receptors (AMY1–AMY3)AgonistSelectivity profile against the calcitonin receptor reported but not independently verified
Calcitonin receptor (CTR)AgonistRelative activity not published

§2.2Mechanism of action

Amylin receptor agonism at the area postrema promoting meal-related satiation, with a formulation and half-life supporting weekly dosing. The therapeutic hypothesis is tolerability advantage rather than efficacy advantage.[1,2]

§2.3Pharmacokinetics

Terminal half-life
reported as supporting weekly dosing
Time to maximum concentration
not published
Volume of distribution
not published
Plasma protein binding
high
Clearance
not published
Bioavailability
not published

Not published.

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. Lau DCW, Erichsen L, Francisco AM, Satylganova A, le Roux CW, McGowan B, Pedersen SD, Pietiläinen KH, Rubino DM, Batterham RL. Once-weekly cagrilintide for weight management in people with overweight and obesity: a multicentre, randomised, double-blind, placebo-controlled and active-controlled, dose-finding phase 2 trial. The Lancet 2021;398(10317):2160–2172. doi:10.1016/S0140-6736(21)01751-7 · PMID 34798060
  2. Hollander PA, Levy P, Fineman MS, Maggs DG, Shen LZ, Strobel SA, Weyer C, Kolterman OG. Pramlintide as an adjunct to insulin therapy improves long-term glycemic and weight control in patients with type 2 diabetes: a 1-year randomized controlled trial. Diabetes Care 2003;26(3):784–790. doi:10.2337/diacare.26.3.784 · PMID 12610038

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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