Tìm theo
MAP-0004
Thuốc Gốc
Small Molecule
MAP-0004 is a proprietary orally inhaled version of dihydroergotamine, or DHE, intended to treat migraine. Study showed that MAP-0004 provided pain relief as early as within ten minutes of dosing, and that this relief was sustained through at least 24 hours. The study also demonstrated efficacy trends in treating nausea, photophobia and phonophobia. Based on these results, as well as independent research that concludes that patients prefer migraine therapies providing fast onset, pain relief, sustained pain relief and safety, the company believes that MAP-0004 has the potential to be a first-line therapy for migraine patients.
Dược Lực Học : MAP-0004 is indicated for the acute treatment of migraine headaches with or without aura and the acute treatment of cluster headache episodes. MAP-0004 binds with high affinity to 5-HT1Da and 5-HT1Db receptors. It also binds with high affinity to serotonin 5-HT1A, 5-HT2A, and 5-HT2C receptors, noradrenaline a2A, a2B and a receptors, and dopamine D2L and D3 receptors. The therapeutic activity of MAP-0004 in migraine is generally attributed to the agonist effect at 5-HT1D receptors.
Cơ Chế Tác Dụng : MAP-0004 is a proprietary orally inhaled version of dihydroergotamine, or DHE, intended to treat migraine. Study showed that MAP-0004 provided pain relief as early as within ten minutes of dosing, and that this relief was sustained through at least 24 hours. The study also demonstrated efficacy trends in treating nausea, photophobia and phonophobia. Based on these results, as well as independent research that concludes that patients prefer migraine therapies providing fast onset, pain relief, sustained pain relief and safety, the company believes that MAP-0004 has the potential to be a first-line therapy for migraine patients. Two theories have been proposed to explain the efficacy of MAP-0004 in migraine: 1) activation of 5-HT1D receptors located on intracranial blood vessels, including those on arterio-venous anastomoses, leads to vasoconstriction, which correlates with the relief of migraine headache and 2) activation of 5-HT1D receptors on sensory nerve endings of the trigeminal system results in the inhibition of pro-inflammatory neuropeptide release.
Chỉ Định : Investigated for use/treatment in migraine and cluster headaches.
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB05743
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