2022
DOI: 10.1111/cts.13309
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First‐in‐human development of a pharmacodynamic biomarker for PAC1 receptor antagonists using intradermal injections of maxadilan

Abstract: Maxadilan, a potent vasodilator peptide, selectively activates the PAC 1 receptor, a promising target for migraine therapy. Therefore, maxadilan has been suggested as a tool to study the pharmacodynamics (PDs) of PAC 1 receptor antagonists. The objectives of this first‐in‐human study were to: (1) determine the safety, tolerability, dose response, and time course of the dermal blood flow (DBF) changes after intradermal (i.d.) injections of maxadilan in the human for… Show more

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Cited by 2 publications
(2 citation statements)
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“…Turning to the clinical applications of proteins from hematophagous arthropod vectors, although not a protease, a potent vasodilator peptide, named maxadilan, from the salivary glands of Lutzomyia longipalpis , the sand fly that transmits Leishmania spp., selectively and potently activate the PAC 1 receptor ( Lerner et al., 2007 ), following intradermal injection ( Marynissen et al., 2022 ). This receptor is activated in the pathophysiology of migraine.…”
Section: Maxadilan the Vasodilator From Sand Fliesmentioning
confidence: 99%
See 1 more Smart Citation
“…Turning to the clinical applications of proteins from hematophagous arthropod vectors, although not a protease, a potent vasodilator peptide, named maxadilan, from the salivary glands of Lutzomyia longipalpis , the sand fly that transmits Leishmania spp., selectively and potently activate the PAC 1 receptor ( Lerner et al., 2007 ), following intradermal injection ( Marynissen et al., 2022 ). This receptor is activated in the pathophysiology of migraine.…”
Section: Maxadilan the Vasodilator From Sand Fliesmentioning
confidence: 99%
“…This receptor is activated in the pathophysiology of migraine. Maxadilan was proposed to be used as a novel pharmacodynamic biomarker for the early clinical development of PAC 1 receptor antagonists ( Marynissen et al., 2022 ), highlighting the potential clinical use of proteins from hematophagous arthropod vectors.…”
Section: Maxadilan the Vasodilator From Sand Fliesmentioning
confidence: 99%