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Study · Animal study (in vivo) · rat · 2020

4 results

Tissue Distribution and Receptor Activation by Somapacitan, a Long Acting Growth Hormone Derivative.

Petersen M, Gandhi PS, Buchardt J, Alanentalo T, Fels JJ, Johansen NL, Helding-Kvist P, Vad K, Thygesen P

International journal of molecular sciences11 Feb 2020Cited by 7 (Europe PMC)

PMID32053994 (opens in a new tab)PMCIDPMC7072805 (opens in a new tab)DOI10.3390/ijms21041181 (opens in a new tab)PepBankPUB-32053994
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Summary

Somapacitan is a long-acting, once-weekly, albumin-binding growth hormone (GH) derivative. The reversible albumin-binding properties leads to prolonged circulation half-life. Here, we investigated and compared somapacitan with human GH on downstream receptor signaling in primary hepatocytes and hepatocellular models and using isothermal titration calorimetry to characterize receptor binding of somapacitan in the presence or absence of human serum albumin (HSA). With non-invasive fluorescence imaging we quantitatively visualize and compare the temporal distribution and examine the tissue-specific growth hormone receptor (GHR) activation at distribution sites. We found that signaling kinetics were slightly more rapid and intense for GH compared with somapacitan. Receptor binding isotherms were characterized by a high and a low affinity interaction site with or without HSA. Using in vivo optical imaging we found prolonged systemically biodistribution of somapacitan compared with GH, which correlated with plasma pharmacokinetics. Ex vivo mouse organ analysis revealed that the temporal fluorescent intensity in livers dosed with somapacitan was significantly increased compared with GH-dosed livers and correlated with the degree of downstream GHR activation. Finally, we show that fluorescent-labeled analogs distributed to the hypertrophic zone in the epiphysis of proximal tibia of hypophysectomized rats and that somapacitan and GH activate the GHR signaling in epiphyseal tissues.
CC BYText from Europe PMC. Highlighted sentences are the source of results.

Results from this study4

4 results from studies that gave the peptide. No result from this study comes from people.

  1. 01AnimalAnimal study (in vivo)Mechanism

    In hypophysectomized rats, somapacitan activated GHR signaling in epiphyseal tissues.

    In plain wordsIn rats, somapacitan activated growth hormone receptor signaling in growth-plate tissues.

    Peptide
    Somapacitan
    Outcome
    IncreaseEpiphyseal GHR signaling
    Study

    Ratn: not reported in source

    Hypophysectomized rats
    Outcome group
    Receptor activity and mechanism · Musculoskeletal
    Studied dose
    Dose not stated

    Source sentences

    Summary
    Finally, we show that fluorescent-labeled analogs distributed to the hypertrophic zone in the epiphysis of proximal tibia of hypophysectomized rats and that somapacitan and GH activate the GHR signaling in epiphyseal tissues.
  2. 02LabIn vitro (cells)Mechanism

    In hepatocyte models, somapacitan signaling was slightly slower than GH signaling.

    In plain wordsIn cells, somapacitan signaling was slightly slower than GH signaling.

    Peptide
    Somapacitan
    Outcome
    DecreaseSignaling speed
    Study

    n: not reported in source

    Primary hepatocytes and hepatocellular models
    Comparator
    Human GH
    Outcome group
    Receptor activity and mechanism · Pharmacology
    Studied dose
    Dose not stated

    Source sentences

    Summary
    We found that signaling kinetics were slightly more rapid and intense for GH compared with somapacitan.
    1 context sentence
    Summary · context
    Here, we investigated and compared somapacitan with human GH on downstream receptor signaling in primary hepatocytes and hepatocellular models and using isothermal titration calorimetry to characterize receptor binding of somapacitan in the presence or absence of human serum albumin (HSA).
  3. 03LabIn vitro (cells)Mechanism

    In hepatocyte models, somapacitan signaling was slightly less intense than GH signaling.

    In plain wordsIn cells, somapacitan signaling was slightly less intense than GH signaling.

    Peptide
    Somapacitan
    Outcome
    DecreaseSignaling intensity
    Study

    n: not reported in source

    Primary hepatocytes and hepatocellular models
    Comparator
    Human GH
    Outcome group
    Receptor activity and mechanism · Pharmacology
    Studied dose
    Dose not stated

    Source sentences

    Summary
    We found that signaling kinetics were slightly more rapid and intense for GH compared with somapacitan.
    1 context sentence
    Summary · context
    Here, we investigated and compared somapacitan with human GH on downstream receptor signaling in primary hepatocytes and hepatocellular models and using isothermal titration calorimetry to characterize receptor binding of somapacitan in the presence or absence of human serum albumin (HSA).
  4. 04LabIn vitro (cell-free)Activity measurement

    In calorimetry experiments, somapacitan receptor binding showed high- and low-affinity sites with or without human serum albumin.

    In plain wordsIn lab tests, somapacitan showed high- and low-affinity receptor binding with or without human serum albumin.

    Peptide
    Somapacitan
    Outcome
    Not applicableReceptor binding sites
    Study

    n: not reported in source

    Isothermal titration calorimetry
    Outcome group
    Receptor activity and mechanism · Pharmacology
    Studied dose
    Dose not stated

    Source sentences

    Summary
    Receptor binding isotherms were characterized by a high and a low affinity interaction site with or without HSA.
    1 context sentence
    Summary · context
    Here, we investigated and compared somapacitan with human GH on downstream receptor signaling in primary hepatocytes and hepatocellular models and using isothermal titration calorimetry to characterize receptor binding of somapacitan in the presence or absence of human serum albumin (HSA).

AI wrote and checked these results. AI can make mistakes, so check important results against the source.

Version history

PepBank keeps every version of the data on this study. Status changes from Retraction Watch, Europe PMC and Crossref are listed with their source.

  1. Version 2Current

    28 Oct 2026, 02:03 UTC

    Study results updated

  2. Version 1

    27 Oct 2026, 16:36 UTC

    First added · source update from Europe PMC

Subjects

Terms as the source lists them.

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