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Your Position: Home > Licensing > BHE202217

5-HT1F agonist

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  • Project profile
    Project name: 5-HT1F agonist
    Indications: Migraine
    Research phase: Phase I
    Cooperation demands: License-out or co-development
  • Highlights

    1. Completely new mechanism of action:



    Completely new mechanism of action


    (1) Activation of the 5-HT1F receptor could inhibit the release of CGRP, thus preventing vasodilation.


    (2) Activation of the Aδ5-HT1F receptor could hyperpolarize the Aδnerve fibers and inhibit nerve transmission, thus preventing pain signaling.


    (3) It has no effect on 5-HT1B/1D receptor and is safer for patients with cardiovascular disease, could benefit for patients with the low response to triptans (40%).


    2. Pre-clinical research:


    (1) Better activity and high selectivity (in vitro): the affinity of 5-HT1F is stronger than that of lasmiditan in vitro, and EC50 is equivalent to that of lasmiditan. High selectivity target 5-HT1F (the affinity with 1A, 1B, 2A, and 2C is much lower than that with 1F).


    (2) Better results shown in animal models (in vivo): (1) The pharmacodynamics of migraine model in rats induced by electrical stimulation of trigeminal ganglion showed that the compound could significantly inhibit dural protein extravasation and c-fos expression in trigeminal caudate nucleus. (2) Efficacy studies on CGRP release induced by KCl showed that the compound could significantly inhibit the release of CGRP in dura and trigeminal caudate nucleus. (3) Efficacy of capsaicin-induced migraine in rats showed that the compound could significantly inhibit middle meningeal artery vascular dilatation. (4) In addition, efficacy studies on the tension of rabbit saphenous vein ring showed that the compound had no obvious effect on the contraction of rabbit saphenous vein ring.


    3. Bright Market Prospects:


    (1) The incidence of migraine in European and American countries is 10%–15%, and the incidence of migraine in China is about 9.3%.


    (2) Global migraine medicine sales increased significantly in recent years, with foreign markets 2020 sales of $4.503 billion, up 27%. According to analysts, the migraine drug market is expected to grow significantly in the next few years to more than $11 billion.

  • Project Introduction

    1. Asset type: 5-HT1F agonist

    2. Indication: Migraine

    3. Research phase: Phase 1

    4. Cooperation demands:   License-out or co-development

    5. Research progress:

    1. Clinical Phase 1 is ongoing

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