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sumatriptan

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Description

Sumatriptan: A serotonin agonist that acts selectively at 5HT1 receptors. It is used in the treatment of MIGRAINE DISORDERS. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

sumatriptan : A sulfonamide that consists of N,N-dimethyltryptamine bearing an additional (N-methylsulfamoyl)methyl substituent at position 5. Selective agonist for a vascular 5-HT1 receptor subtype (probably a member of the 5-HT1D family). Used (in the form of its succinate salt) for the acute treatment of migraine with or without aura in adults. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID5358
CHEMBL ID128
CHEBI ID10650
SCHEMBL ID1482
MeSH IDM0027392

Synonyms (112)

Synonym
BIDD:GT0248
1-[3-(2-dimethylaminoethyl)-1h-indol-5-yl]-n-methyl-methanesulfonamide
(3-[2-(dimethylamino)ethyl]-1h-indol-5-yl)-n-methylmethanesulfonamide
CHEBI:10650 ,
sumax
3-(2-(dimethylamino)ethyl)-n-methyl-1h-indole-5-methanesulfonamide
sumatran
1-{3-[2-(dimethylamino)ethyl]-1h-indol-5-yl}-n-methylmethanesulfonamide
sumatriptanum
BRD-K50938287-001-01-7
gtpl54
tosymra (nasal spray)
imigran
imitrex
sumatriptanum [inn-latin]
brn 6930870
gr 43175
gr-43175
gr 43175x
1h-indole-5-methanesulfonamide, 3-(2-(dimethylamino)ethyl)-n-methyl-
BSPBIO_002304
3-[2-(dimethylamino)ethyl]-n-methylindole-5-methanesulfonamide
MLS001304742
MLS001195659
smr000596517
C07319
sumatriptan
103628-46-2
DB00669
imigran (tn)
sumatriptan (jan/usp/inn)
D00451
imitrex (tn)
NCGC00095838-01
SPECTRUM1505372
NCGC00095838-02
dfn-11 (sumatriptan injection)
dfn-11
CHEMBL128 ,
n02cc01
L000584
bdbm50005835
1-[3-(2-dimethylaminoethyl)-1h-indol-5-yl]-n-methylmethanesulfonamide
dtxsid4023628 ,
dtxcid303628
cas-103628-46-2
tox21_111528
HMS2231B21
zecuity
avp 825
8r78f6l9vo ,
avp-825
avp825
hsdb 7742
sumatriptan [usp:inn:ban]
unii-8r78f6l9vo
FT-0674779
FT-0631027
NCGC00095838-03
sumatriptan [usp monograph]
sumatriptan [usp-rs]
sumatriptan [orange book]
3-[2-(dimethylamino)ethyl]-n-methy-1h-indole-5-methanesulfonamide
tosymra
sumatriptan [who-dd]
sumatriptan [hsdb]
sumatriptan [jan]
sumatriptan [mart.]
sumatriptan [mi]
sumatriptan [inn]
sumatriptan [vandf]
AKOS015894924
HMS3369A05
SCHEMBL1482
tox21_111528_1
NCGC00095838-04
AB00698285-13
AB00698285-12
(3-[2-(dimethylamino)ethyl]-1h-indol-5-yl)-n-methylmethanesulfonamide #
3-[2-(dimethylamino)ethyl]-n-methyl-1h-indole-5-methanesulfonamide
3-[2-(dimethylamino)ethyl]-n-methyl-1h-indole-5-methanesulphonamide
3-[2-(dimethylamino)ethyl]-n-methyl-1h-indole -5-methanesulphonamide
1-(3-(2-(dimethylamino)ethyl)-1h-indol-5-yl)-n-methylmethanesulfonamide
AB00698285_14
AB00698285_15
STL451003
J-001014
CCG-230331
imigran recovery
1h-indole-5-methanesulfonamide, 3-[2-(dimethylamino)ethyl]-n-methyl-
SBI-0206837.P001
{3-[2-(dimethylamino)ethyl]-1h-indol-5-yl}-n-methylmethanesulfonamide
Q416978
1-[3-[2-(dimethylamino)ethyl]-1h-indol-5-yl]-n-methylmethanesulfonamide
BCP02237
AMY17769
C90357
sumatriptansuccinate
BS164424
sumatriptan- bio-x
EN300-123008
HY-B0121B
CS-0009565
sumatriptanum (inn-latin)
1-(3-(2-dimethylaminoethyl)-1h-indol-5-yl)-n-methyl-methanesulfonamide
sumatriptan (usp:inn:ban)
(3-(2-(dimethylamino)ethyl)-1h-indol-5-yl)-n-methylmethanesulfonamide
sumatriptan (usp monograph)
sumatriptan (mart.)
3-(2-(dimethylamino)ethyl)-n-methy-1h-indole-5-methanesulfonamide
3-(2-(dimethylamino)ethyl)-n-methylindole-5-methanesulfonamide
sumatriptan (usp-rs)

Research Excerpts

Overview

Sumatriptan is a serotonin receptor agonist and the most commonly used triptan for the acute treatment of migraine. It acts as a synergist of the NTG vasodilating action.

ExcerptReferenceRelevance
"Sumatriptan is a specific 5-Hydroxytryptamine 1B/1D receptor agonist and has neuroprotective effects in various neuropsychiatric disorders."( Neuroprotective effect of sumatriptan in pentylenetetrazole-induced seizure is mediated through N-methyl-D-aspartate/nitric oxide and cAMP response element-binding protein signaling pathway.
Abdollahi, A; Alotaibi, G; Dehpour, AR; Ghazi-Khansari, M; Imran Khan, M; Mumtaz, F; Rashki, A; Shadboorestan, A, 2022
)
1.74
"Sumatriptan (ST) is a commonly prescribed drug for treating migraine. "( Harnessing Intranasal Delivery Systems of Sumatriptan for the Treatment of Migraine.
Akhtari, J; Asadi, P; Assadpour, S; Sahebkar, A; Shiran, MR, 2022
)
2.43
"Sumatriptan acts as a synergist of the NTG vasodilating action."( Duality in response of intracranial vessels to nitroglycerin revealed in rats by imaging photoplethysmography.
Iurkova, PM; Kamshilin, AA; Nippolainen, E; Potapenko, AV; Sokolov, AY; Volynsky, MA; Zaytsev, VV, 2023
)
1.63
"Sumatriptan is a 5-hydroxytryptamine 1B/1D (5HT1B/1D) agonist used as a treatment for migraine headaches."( Inhibition of ovalbumin-induced allergic rhinitis by sumatriptan through the nitric oxide pathway in mice.
Alaeddini, M; Dabiri, S; Dehpour, AR; Etemad-Moghadam, S; Hemmati, S; Rahimi, N, 2019
)
1.48
"Sumatriptan is a serotonin receptor agonist and the most commonly used triptan for the acute treatment of migraine."( Evaluation of the Pharmacokinetic Interaction of Ubrogepant Coadministered With Sumatriptan and of the Safety of Ubrogepant With Triptans.
Boinpally, R; Butler, M; Jakate, A; Lu, K; McGeeney, D; Periclou, A, 2020
)
1.51
"Sumatriptan, which is an anti-migraine agent is a specific agonist for 5-hydroxytryptamine 1B, 1D (5HT1B, 1D) receptors."( The protective effects of sumatriptan on vincristine - induced peripheral neuropathy in a rat model.
Abdollahi, A; Afshari, K; Dehpour, AR; Hadian, MR; Khalilzadeh, M; Momeny, M; Norouzi-Javidan, A; Panahi, G; Rahimi, N; Rashidian, A; Shakiba, S, 2018
)
1.5
"Sumatriptan TDS is a useful addition to the treatment options available to migraine patients."( Sumatriptan iontophoretic transdermal system: a review of its use in patients with acute migraine.
Garnock-Jones, KP, 2013
)
2.55
"Sumatriptan is an abortive medication for migraine attacks, belonging to the triptan family."( Sumatriptan (all routes of administration) for acute migraine attacks in adults - overview of Cochrane reviews.
Derry, CJ; Derry, S; Moore, RA, 2014
)
2.57
"Sumatriptan is an effective abortive treatment for acute migraine attacks, but is associated with increased adverse events relative to placebo. "( Sumatriptan (all routes of administration) for acute migraine attacks in adults - overview of Cochrane reviews.
Derry, CJ; Derry, S; Moore, RA, 2014
)
3.29
"Sumatriptan is a tryptamine derivative that acts at 5-HT(1B/1D) receptors and is used for the treatment of migraines."( Multidrug toxicity involving sumatriptan.
Bosy, TZ; Hughes, RL; Knittel, JL; Levine, B; Vorce, SP,
)
1.14
"Sumatriptan (Imigran) is a potent and highly selective 5-HT1 receptor agonist often used in treating acute migraine. "( Effects of sumatriptan nasal spray (Imigran) on isolated rat's tracheal smooth muscle.
Chang, YN; Cheng, LH; Chiu, FS; Chu, YH; Liu, SC; Wang, HW; Wu, PC, 2015
)
2.25
"Sumatriptan succinate is a drug of choice for migraine."( Application of design of experiment for polyox and xanthan gum coated floating pulsatile delivery of sumatriptan succinate in migraine treatment.
Jagdale, SC; Pawar, CR, 2014
)
1.34
"Sumatriptan is a 5-HT1B/1D receptor agonist used for the treatment of cluster headaches and migraine which might cause memory impairment as a potential side effect."( Protective Effects of Lithium on Sumatriptan-Induced Memory Impairment in Mice.
Behestani, S; Dehpour, AR; Javadi-Paydar, M; Nikoui, V; Salehi, M, 2016
)
1.44
"Sumatriptan is a useful alternative treatment for postcraniotomy headache."( Sumatriptan improves postoperative quality of recovery and reduces postcraniotomy headache after cranial nerve decompression.
Bailey, T; Li, L; Manninen, PH; Tymianski, M; Venkatraghavan, L, 2016
)
2.6
"Sumatriptan is a 5-HT-1B/D receptor agonist considered to activate receptors involved in the pathophysiology specific to migraine."( Pharmacological synergy: the next frontier on therapeutic advancement for migraine.
Blumenfeld, A; Cady, R; Gennings, C, 2012
)
1.1
"Sumatriptan is an agent effective in treatment of migraine and cluster headache."( Sumatriptan inhibits TRPV1 channels in trigeminal neurons.
Cheng, X; Disney, KE; Evans, MS; Jeffry, JA; Premkumar, LS, 2012
)
2.54
"Sumatriptan is an abortive medication for migraine attacks, belonging to the triptan family."( Sumatriptan (oral route of administration) for acute migraine attacks in adults.
Derry, CJ; Derry, S; Moore, RA, 2012
)
2.54
"Sumatriptan is an abortive medication for migraine attacks, belonging to the triptan family."( Sumatriptan (intranasal route of administration) for acute migraine attacks in adults.
Derry, CJ; Derry, S; Moore, RA, 2012
)
2.54
"Sumatriptan is an abortive medication for migraine attacks, belonging to the triptan family."( Sumatriptan (rectal route of administration) for acute migraine attacks in adults.
Derry, CJ; Derry, S; Moore, RA, 2012
)
2.54
"Sumatriptan is an abortive medication for migraine attacks, belonging to the triptan family."( Sumatriptan (subcutaneous route of administration) for acute migraine attacks in adults.
Derry, CJ; Derry, S; Moore, RA, 2012
)
2.54
"This sumatriptan auto-injector is a single-use system for the rapid subcutaneous delivery of 6 mg of sumatriptan succinate in the acute management of migraine pain. "( An open-label trial of a sumatriptan auto-injector for migraine in patients currently treated with subcutaneous sumatriptan.
Landy, SH; Ramos, E; Schweizer, E; Tepper, SJ; Wein, T, 2013
)
1.21
"Sumatriptan is a potent serotonin 5HT(1B/1D) agonist widely used in the treatment of migraine; the effectiveness of the intranasal formulation (20mg) has been well established in several clinical studies."( Clinical pharmacokinetics of intranasal sumatriptan.
Barrow, A; Fuseau, E; Ibbotson, T; Moore, KH; Petricoul, O, 2002
)
1.3
"Sumatriptan is a potent and selective vascular 5-HT1 receptor agonist effective for the treatment of migraine. "( Pharmacokinetics of sumatriptan nasal spray in adolescents.
Christensen, ML; Fuseau, E; Jabbour, JT; Mottern, RK, 2003
)
2.09
"Sumatriptan is a serotonin1D agonist."( Pharmacological challenge with a serotonin 1D agonist in alcohol dependence.
Hugo, CJ; Maritz, JS; Pienaar, W; Stein, DJ; Vythilingum, B, 2005
)
1.05
"Oral sumatriptan (100 mg) is an effective and well tolerated acute treatment for patients who report menstrually related migraine."( Managing migraine headaches experienced by patients who self-report with menstrually related migraine: a prospective, placebo-controlled study with oral sumatriptan.
Aurora, SK; Dowson, AJ; Massiou, H, 2005
)
0.98
"Sumatriptan is a selective agonist of 5HT1 (1B/1D) receptors, which has proved to be effective and safe for the acute treatment of migraine attacks. "( Pharmacokinetics of sumatriptan in non-respondent and in adverse drug reaction reporting migraine patients.
Bertolini, A; Coccia, CP; Ferrari, A; Leone, S; Pinetti, D; Sternieri, E, 2005
)
2.09
"Sumatriptan is a 5-HT 1,2-serotonin blocker."( [Particular features of the impact of certain vegetotropic drugs on the excitability of cholinergic structures, contractile myocardial function and electromotive stomach activity].
Lychkova, AE, 2005
)
1.05
"Sumatriptan is a serotonin 5-HT(1B/1D) receptor agonist that is used for the acute treatment of migraine attacks. "( Sumatriptan fast-disintegrating/rapid-release tablets.
Keating, GM; Moen, MD, 2006
)
3.22
"Sumatriptan is a potent and selective 5-HT(1B) and 5-HT(1D )agonist used in the symptomatic treatment of migraine; it shows poor oral bioavailability ascribed, in part, to its low lipophilicity. "( Unanticipated acyloxymethylation of sumatriptan indole nitrogen atom and its implications in prodrug design.
Guedes, RC; Iley, J; Lopes, F; Moreira, R; Rodrigues, T, 2008
)
2.06
"Sumatriptan is a potent and selective agonist at a vascular serotonin1 (5-hydroxytryptamine1; 5-HT1) receptor subtype (similar to 5-HT1D) and is used in acute treatment of migraine and cluster headache. "( Sumatriptan. A reappraisal of its pharmacology and therapeutic efficacy in the acute treatment of migraine and cluster headache.
McTavish, D; Plosker, GL, 1994
)
3.17
"Sumatriptan is a potent and selective serotonin1D receptor agonist, which can be administered orally and via the subcutaneous or intranasal route."( Acute treatment of migraine attacks.
Ferrari, MD; Haan, J, 1995
)
1.01
"Sumatriptan is a new product with a higher acquisition cost than DHE."( A literature review comparing the economic, clinical, and humanistic attributes of dihydroergotamine and sumatriptan.
Kozma, CM; Lawrence, BJ; Mauch, RP; Reeder, CE,
)
1.07
"Sumatriptan is a potent vasoconstrictor of intracranial arteries."( The mode of action of sumatriptan is vascular? A debate.
Goadsby, PJ; Humphrey, PP, 1994
)
1.32
"Sumatriptan is a highly cleared compound that is eliminated from the body primarily by metabolism to the pharmacologically inactive indoleacetic acid analogue."( Single dose pharmacokinetics of sumatriptan in healthy volunteers.
Fowler, PA; Hussey, EK; Lacey, LF, 1995
)
1.3
"Sumatriptan is a novel serotonin 1 (5-hydroxytryptamine 1; 5-HT1)-like agonist which has been shown to be effective in the treatment of acute migraine. "( Sumatriptan clinical pharmacokinetics.
Scott, AK, 1994
)
3.17
"Sumatriptan is a new 5HT1-like agonist that has proved a novel and effective treatment for migraine. "( Disposition of sumatriptan in laboratory animals and humans.
Andrew, PD; Bradbury, A; Dixon, CM; Oxford, J; Saynor, DA; Tarbit, MH,
)
1.93
"Sumatriptan is a very effective agent that has joined the ranks of other effective abortive migraine treatments, such as ergotamine, dihydroergotamine, and nonsteroidal anti-inflammatory agents, as well as narcotic analgesics."( Migraine: a pharmacologic review with newer options and delivery modalities.
Baumel, B, 1994
)
1.01
"Sumatriptan is a new anti-migraine drug which has been shown in clinical studies to be efficacious in up to 80% of attacks treated."( [Sumatriptan in the treatment of migraine in general practice].
Midelfart, E; Winnem, M, 1994
)
1.92
"Sumatriptan is a selective agonist of 5-hydroxytryptamine receptors, recommended for the acute treatment of migraine. "( The use of sumatriptan in the treatment of migraine.
Gross, M,
)
1.96
"Sumatriptan (GR43175) is a selective 5-hydroxytryptamine (5HT1) receptor agonist effective in the acute treatment of migraine. "( Effect of subcutaneous sumatriptan, a selective 5HT1 agonist, on the systemic, pulmonary, and coronary circulation.
Bhargava, B; Gemmill, JD; Hillis, WS; Hogg, KJ; MacIntyre, PD, 1993
)
2.04
"Sumatriptan is a selective 5-HT1-like agonist, which is effective in the treatment of migraine and cluster headache. "( Sumatriptan in the acute treatment of migraine.
Lloyd, K; Pilgrim, AJ; Tansey, MJ, 1993
)
3.17
"Sumatriptan is a new serotonin receptor agonist that is useful in the treatment of migraine headache. "( Sumatriptan: a new serotonin agonist for the treatment of migraine headache.
Susman, JL, 1993
)
3.17
"Sumatriptan is a potent and selective agonist at the vascular 5HT1 receptor which mediates constriction of certain large cranial blood vessels and/or inhibits the release of vasoactive neuropeptides from perivascular trigeminal axons in the dura mater following activation of the trigeminovascular system. "( Migraine and cluster headache--their management with sumatriptan: a critical review of the current clinical experience.
Diener, HC; Pfaffenrath, V; Schoenen, J; Steiner, TJ; Wilkinson, M, 1995
)
1.98
"Sumatriptan is a novel drug for migraine headache pain, which, on the basis of its mechanism of action, may have therapeutic potential in other pain states. "( Dual effect of the serotonin agonist, sumatriptan, on peripheral neurogenic inflammation.
Levine, JD; Peroutka, SJ; Pierce, PA; Xie, GX,
)
1.85
"Sumatriptan is a selective 5-hydroxytryptamine1d (5-HT1d)-receptor agonist, highly effective in the short-term treatment of migraine headaches. "( Cerebral and ocular hemodynamic effects of sumatriptan in the nitroglycerin headache model.
Eichler, HG; Findl, O; Graselli, U; Krejcy, K; Schmetterer, L; Singer, EA; Wolzt, M, 1996
)
2
"1 Sumatriptan is a potent and selective 5-HT1 receptor agonist marketed for the treatment of migraine by both oral and subcutaneous routes. "( The preclinical toxicological evaluation of sumatriptan.
Hartley, K; Jackson, MR; Owen, K; Parkinson, MM; Tucker, ML; Tweats, DJ, 1995
)
1.27
"Oral sumatriptan is an effective acute treatment for migraine in adults, but its efficacy in children is still undetermined. "( Sumatriptan for migraine attacks in children: a randomized placebo-controlled study. Do children with migraine respond to oral sumatriptan differently from adults?
Hämäläinen, ML; Hoppu, K; Santavuori, P, 1997
)
2.25
"Sumatriptan is a selective agonist at serotonin 5-HT1-like receptors, including 5-HT1B/1D subtypes. "( Sumatriptan. An updated review of its use in migraine.
Markham, A; Perry, CM, 1998
)
3.19
"Sumatriptan is a 5-HT1 receptor agonist which has found widespread use in the treatment of migraine."( Validation of a liquid chromatographic tandem mass spectrometric method for the determination of sumatriptan in human biological fluids.
Barrow, A; Cheng, KN; Redrup, MJ; Williams, PN, 1998
)
1.24
"Sumatriptan is an antimigraine agent, which interacts most potently with 5HT1D receptors."( Treatment of severe, drug resistant obsessive compulsive disorder with the 5HT1D agonist sumatriptan.
Cohen, R; Sasson, Y; Stern, L; Zohar, J, 1998
)
1.24
"Sumatriptan is a 5-HT1B/1D-receptor agonist which also has affinity for 5-HT1F-receptors. "( Vasoconstriction in human isolated middle meningeal arteries: determining the contribution of 5-HT1B- and 5-HT1F-receptor activation.
Beer, MS; Heald, MA; Hill, RG; Longmore, J; Maskell, L; Pickard, JD; Razzaque, Z, 1999
)
1.75
"Sumatriptan is an effective and well tolerated agent in the treatment of migraine."( Sumatriptan. A pharmacoeconomic review of its use in migraine.
Coukell, AJ; Lamb, HM, 1997
)
2.46
"Sumatriptan is a highly effective treatment for migraine in adults but its efficacy in children has not been determined. "( Intranasal sumatriptan for the acute treatment of migraine in children.
Ueberall, MA; Wenzel, D, 1999
)
2.14
"Sumatriptan is a specific migraine treatment which has recently become among the most widely prescribed acute migraine therapies."( Acute treatment of migraine attacks: efficacy and safety of a nonsteroidal anti-inflammatory drug, diclofenac-potassium, in comparison to oral sumatriptan and placebo. The Diclofenac-K/Sumatriptan Migraine Study Group.
, 1999
)
1.23
"Sumatriptan is a novel drug for the treatment of acute migraine attacks. "( [The efficacy of subcutaneous sumatriptan for the treatment of migraine attack].
Stepień, A, 1999
)
2.03
"Sumatriptan nasal spray is a single-dose device that delivers 5 mg, 10 mg, or 20 mg of sumatriptan (dosage availability dependent upon country) in a 0.1 ml aqueous solution to one nostril. "( Sumatriptan nasal spray in the acute treatment of migraine: a review of clinical studies.
Dahlöf, C, 1999
)
3.19
"Sumatriptan is a 5HT1D agonist used in the treatment of migraine. "( Lack of pharmacokinetic interaction between sumatriptan and naproxen.
Rambhau, D; Rao, BR; Rao, YM; Srinivasu, P, 2000
)
2.01
"Oral sumatriptan, which is a well tolerated, effective acute treatment for migraine, and is selectively available in different countries in 100 mg, 50 mg, and 25 mg tablets. "( Defining optimal dosing for sumatriptan tablets in the acute treatment of migraine.
Mathew, NT; Salonen, R, 1999
)
1.11
"Sumatriptan is an acute treatment for migraine which is often used by women in their child-bearing years, and who become unexpectedly pregnant. "( Pregnancy and perinatal outcomes in migraineurs using sumatriptan: a prospective study.
Davis, RL; Ephross, SA; Fox, AW; Gutterman, DL; O'Quinn, S; Williams, V, 1999
)
1.99
"Sumatriptan is a selective 5-HT(1B/D) receptor agonist which does not cross the blood-brain barrier."( Sumatriptan reduces exercise capacity in healthy males: a peripheral effect of 5-hydroxytryptamine agonism?
Cahill, H; Hillis, WS; Hills, WS; Knipe, S; MacIntyre, PD; McCann, GP; Muir, DF, 2000
)
2.47
"Sumatriptan is a 5-HT1B/D receptor agonist of documented efficacy in relieving migraine and associated symptoms such as nausea and vomiting. "( Gastric motor effects of triptans: open questions and future perspectives.
Cipolla, G; Crema, F; De Ponti, F; Frigo, G; Moro, E; Sacco, S, 2001
)
1.75
"Sumatriptan is a serotonin agonist that has been studied for the acute treatment of migraine and cluster headache. "( Sumatriptan: a selective 5-hydroxytryptamine receptor agonist for the acute treatment of migraine.
Fullerton, T; Gengo, FM, 1992
)
3.17
"Sumatriptan is a novel, highly effective drug against migraine and cluster headache attacks. "( Clinical effects and mechanism of action of sumatriptan in migraine.
Ferrari, MD; Saxena, PR, 1992
)
1.99
"Sumatriptan is a 5-HT1D agonist of therapeutic use in migraine and cluster headaches. "( Psychoactivity and abuse potential of sumatriptan.
Busch, M; Jasinski, DR; Preston, KL; Sullivan, JT; Testa, MP, 1992
)
2
"1. Sumatriptan (GR43175) is a selective 5-HT1-receptor agonist effective in the acute treatment of migraine. "( The effect of i.v. sumatriptan, a selective 5-HT1-receptor agonist on central haemodynamics and the coronary circulation.
Bhargava, B; Gemmill, JD; Hillis, WS; Hogg, KJ; Macintyre, PD, 1992
)
1.23
"Sumatriptan is an agonist of 5-HT1 -like receptors and exerts a selective vasoconstricting effect on the arteries of the head, particularly in the rami of the carotid artery."( [Sumatriptan and its use in treatment of migraine and cluster headaches].
Prusiński, A, 1992
)
1.92
"Sumatriptan is a highly selective 5 HT1 receptor subtype agonist. "( [Sumatriptan--future development, alternative features and potential new indications].
Arnold, WS, 1992
)
2.64
"Sumatriptan is a serotonin1 (5-HT1) receptor agonist, which is effective in the acute treatment of migraine headache. "( Sumatriptan. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in the acute treatment of migraine and cluster headache.
Clissold, SP; Dechant, KL, 1992
)
3.17
"Sumatriptan is a highly selective 5-HT1-like receptor agonist which selectively constricts cranial blood vessels (including those in the dura mater)."( Rationale for the use of 5-HT1-like agonists in the treatment of migraine.
Connor, HE; Feniuk, W; Humphrey, PP; Perren, MJ; Whalley, ET, 1991
)
1
"Sumatriptan is an effective and well-tolerated treatment for acute attacks of cluster headache."( Treatment of acute cluster headache with sumatriptan.
, 1991
)
1.99
"Sumatriptan succinate is a novel compound currently in development for the acute treatment of migraine. "( Development and validation of a liquid chromatographic-mass spectrometric assay for the determination of sumatriptan in plasma.
Lant, MS; Oxford, J, 1989
)
1.93

Effects

Sumatriptan has a weak coronary constrictor effect. It has a large apparent volume of distribution (170 l) and an elimination half-life of 2 h.

Sumatriptan (Imitrex) has been used in the treatment of migraine and other vascular headaches since 1993 in the United States. Only sum atriptan nasal spray has been approved for thetreatment of acute migraine with or without aura in adolescents aged 12-17 years in Europe.

ExcerptReferenceRelevance
"Sumatriptan has a large apparent volume of distribution (170 l) and an elimination half-life of 2 h."( Single dose pharmacokinetics of sumatriptan in healthy volunteers.
Fowler, PA; Hussey, EK; Lacey, LF, 1995
)
1.3
"Sumatriptan has a weak coronary constrictor effect."( [The migraine remedy sumatriptan (Imigran) and coronary heart disease].
Landmark, K; Nguyen, KN, 1995
)
1.33
"Sumatriptan has a low oral bioavailability (14%) and all the newer triptans have an improved oral bioavailability and for one, risatriptan, the rate of absorption is faster."( Triptans in migraine: a comparative review of pharmacology, pharmacokinetics and efficacy.
De Vries, P; Saxena, PR; Tfelt-Hansen, P, 2000
)
1.03
"Sumatriptan has a rapid onset of action and a large volume of distribution."( Sumatriptan: a new drug for vascular headache.
Hsu, VD, 1992
)
2.45
"Sumatriptan has a much more selective pharmacological profile than ergot preparations which are also used in the acute treatment of migraine."( Rationale for the use of 5-HT1-like agonists in the treatment of migraine.
Connor, HE; Feniuk, W; Humphrey, PP; Perren, MJ; Whalley, ET, 1991
)
1
"Sumatriptan has been among the top choices in the management of migraine headaches. "( Biphasic effect of sumatriptan on PTZ-induced seizures in mice: Modulation by 5-HT1B/D receptors and NOS/NO pathway.
Aghamollaii, V; Ahmadi, M; Amiri, S; Dehpour, AR; Ghasemi, K; Gooshe, M; Rohani, MM; Tafakhori, A, 2018
)
2.25
"SC sumatriptan has high efficacy and a rapid onset of action compared with other available triptans and formulations presumably because of its short Tmax, high Cmax, and avoidance of enteral absorption."( A review of needle-free sumatriptan injection for rapid control of migraine.
Farr, SJ; Freitag, FG; Rothrock, JF; Smith, EF, 2013
)
1.21
"Sumatriptan succinate has oral bioavailability of 15% and undergoes hepatic metabolism, hence it is suitable for nasal administration."( Development of in situ gel for nasal delivery: design, optimization, in vitro and in vivo evaluation.
Chaudhari, PD; Galgatte, UC; Kumbhar, AB, 2014
)
1.12
"Sumatriptan succinate has bitter taste, low oral bioavailability, and shorter half-life."( Application of design of experiment for polyox and xanthan gum coated floating pulsatile delivery of sumatriptan succinate in migraine treatment.
Jagdale, SC; Pawar, CR, 2014
)
1.34
"Sumatriptan has been used for the acute treatment of migraine attacks. "( Sumatriptan, an Antimigraine Drug, Inhibits Pentylenetetrazol-induced Seizures in NMRI Mice.
Jand, A; Palizvan, MR, 2017
)
3.34
"Oral sumatriptan has been shown to be an effective drug for the treatment of a single acute attack of migraine. "( WITHDRAWN: Oral sumatriptan for acute migraine.
Gray, RN; McCrory, DC, 2012
)
1.24
"Sumatriptan has failed to show superiority over more standard and cheaper treatment such as aspirin or aspirin plus metoclopramide."( Sumatriptan: a review of its pharmacokinetics, pharmacodynamics and efficacy in the acute treatment of migraine.
Hougaard, A; Tfelt-Hansen, P, 2013
)
2.55
"Sumatriptan has direct scavenging activity on free radicals and NO. "( Sumatriptan scavenges superoxide, hydroxyl, and nitric oxide radicals: in vitro electron spin resonance study.
Ikeda, Y; Jimbo, H; Satoh, K; Shimazu, M, 2002
)
3.2
"With sumatriptan, this finding has proven to be a consequence of the form in which the drug was administered rather than the inherent properties of the drug."( Sumatriptan nasal spray for migraine: a review of studies in patients aged 17 years and younger.
Hämäläinen, M; Jones, M; Loftus, J; Saiers, J, 2002
)
2.21
"Oral sumatriptan has been shown to be an effective drug for the treatment of a single acute attack of migraine. "( Oral sumatriptan for acute migraine.
Gray, RN; McCrory, DC, 2003
)
1.35
"Sumatriptan tablets have been developed in a fast-disintegrating, rapid-release formulation designed to facilitate tablet disintegration and drug dispersion and to potentially mitigate the effects of gastric stasis that can accompany migraine."( Efficacy and tolerability of sumatriptan tablets in a fast-disintegrating, rapid-release formulation for the acute treatment of migraine: results of a multicenter, randomized, placebo-controlled study.
Ahmad, F; Boswell, D; Carpay, J; Kinrade, F; Schoenen, J, 2004
)
2.06
"Sumatriptan has been developed as a new tablet formulation to enhance the rate of systemic drug delivery by improving tablet disintegration and drug dispersion relative to those of conventional tablets."( Pharmacokinetic profile of a new form of sumatriptan tablets in healthy volunteers.
Boswell, D; Bullman, J; Dow, A; Lewis, A; Sidhu, J; Summers, SJ; Walls, C, 2004
)
1.31
"Sumatriptan has been used in the treatment of migraine and other vascular headaches since 1993 in the United States. "( Oral sumatriptan-induced myocardial infarction.
Hack, JB, 2004
)
2.28
"Sumatriptan (Imitrex) has been available for the longest time within the class, is most flexible in form and has been given successfully to the most number of patients."( Sumatriptan: a decade of use and experience in the treatment of migraine.
Bigal, ME; Rapoport, AM; Sheftell, FD; Tepper, SJ, 2004
)
2.49
"Sumatriptan has been instrumental in defining a biological basis for migraine."( Sumatriptan: update and review.
Cady, R; Schreiber, C, 2006
)
2.5
"Only sumatriptan nasal spray has been approved for the treatment of acute migraine with or without aura in adolescents aged 12-17 years in Europe."( Sumatriptan nasal spray in the acute treatment of migraine in adolescents and children.
Brouwer, OF; Callenbach, PM; Gooskens, RH; Linssen, WH; Mulder, PG; Pels, LP; van der Zwan, JL, 2007
)
2.24
"Sumatriptan has a large apparent volume of distribution (170 l) and an elimination half-life of 2 h."( Single dose pharmacokinetics of sumatriptan in healthy volunteers.
Fowler, PA; Hussey, EK; Lacey, LF, 1995
)
1.3
"Sumatriptan has a weak coronary constrictor effect."( [The migraine remedy sumatriptan (Imigran) and coronary heart disease].
Landmark, K; Nguyen, KN, 1995
)
1.33
"Oral sumatriptan (100 mg) has been evaluated against ergotamine, 2 mg, plus caffeine, 200 mg (as Cafergot); and against aspirin, 900 mg, plus metoclopramide, 10 mg."( Sumatriptan in the acute treatment of migraine.
Lloyd, K; Pilgrim, AJ; Tansey, MJ, 1993
)
2.18
"Sumatriptan has shown to be effective in the treatment of an acute migraine- and cluster-headache. "( [Sumatriptan--side effects and problems in routine clinical practice].
Aull, S; Marterer, A; Schnider, P; Wessely, P; Wöber, C, 1995
)
2.64
"Sumatriptan has both vascular and neurogenic effects, both of which may be necessary for a good clinical outcome."( [Drug treatment of migraine attacks. Pharmacological considerations].
Salvesen, R, 1996
)
1.02
"Sumatriptan has been shown to be most effective in migraine attacks, but with transient, slight side effects and high rebound attack rates. "( Sumatriptan treatment of acute migraine attacks in a Saudi population.
al Deeb, S; al Kawi, Z; Bohlega, S; Cheung, P; Yaqub, B, 1997
)
3.18
"Sumatriptan has been used successfully in the acute treatment of migraine since 1991. "( [Evaluation of efficacy and tolerance sumatriptan at a dose of 50 mg in treatment of migraine attack].
Król, F; Prusiński, A, 1998
)
2.01
"Thus sumatriptan has become the de facto gold standard and will be thus employed here."( The scientific basis of medication choice in symptomatic migraine treatment.
Goadsby, PJ, 1999
)
0.76
"Oral sumatriptan 50 mg has been found to have good efficacy and tolerability in the acute treatment of migraine but has been less well studied than the 100 mg dose."( A double-blind placebo-controlled study assessing the efficacy and tolerability of 50 mg sumatriptan tablets in the acute treatment of migraine. Sumatriptan Tablets S2CM07 Study Group.
Ashford, EA; Brautaset, NJ; Hassani, H; Reunanen, M; Saiers, J; Savani, N; Szirmai, I, 1999
)
1.04
"Sumatriptan has been used successfully in patients with postdural puncture headache, however, its use has not been investigated in a controlled fashion."( Sumatriptan in patients with postdural puncture headache.
Connelly, NR; Gibson, CS; Parker, RK; Rahimi, A, 2000
)
2.47
"Sumatriptan has also been reported to be effective for the treatment of postdural puncture headache, postictal headache, and headache related to intravenous immunoglobulin infusion."( Sumatriptan for headache caused by head and neck cancer.
Manfredi, PL; Payne, R; Shenoy, S, 2000
)
2.47
"Sumatriptan has a low oral bioavailability (14%) and all the newer triptans have an improved oral bioavailability and for one, risatriptan, the rate of absorption is faster."( Triptans in migraine: a comparative review of pharmacology, pharmacokinetics and efficacy.
De Vries, P; Saxena, PR; Tfelt-Hansen, P, 2000
)
1.03
"Sumatriptan has been used effectively to treat adult patients with migraine headaches, but its efficacy in children has not been established."( Efficacy of sumatriptan in the treatment of migraine: a review of the literature.
McAlhany, A, 2001
)
1.41
"Sumatriptan has a rapid onset of action and a large volume of distribution."( Sumatriptan: a new drug for vascular headache.
Hsu, VD, 1992
)
2.45
"Sumatriptan has a much more selective pharmacological profile than ergot preparations which are also used in the acute treatment of migraine."( Rationale for the use of 5-HT1-like agonists in the treatment of migraine.
Connor, HE; Feniuk, W; Humphrey, PP; Perren, MJ; Whalley, ET, 1991
)
1

Actions

Sumatriptan can inhibit the electrophysiological activity of ASICs in the trigeminal ganglion (TG) neurons. The drug was found to suppress the CPH attacks as well as indomethacin.

ExcerptReferenceRelevance
"Sumatriptan failed to produce either of these effects due to a poor brain penetration."( 5-HT1D receptor agonist properties of novel 2-[5-[[(trifluoromethyl)sulfonyl]oxy]indolyl]ethylamines and their use as synthetic intermediates.
Barf, TA; de Boer, P; Ennis, MD; Ghazal, NB; McGuire, JC; Peroutka, SJ; Smith, MW; Swensson, K; Wikström, H, 1996
)
1.02
"Sumatriptan can inhibit the electrophysiological activity of ASICs in the trigeminal ganglion (TG) neurons."( Sumatriptan inhibits the electrophysiological activity of ASICs in rat trigeminal ganglion neurons.
Guo, L; Hong, L; Li, R; Liu, A; Ming, P; Zhao, L, 2018
)
2.64
"Sumatriptan in lower concentration increases skin flap survival by means of activation of 5-hydroxytryptamine 1b/1d receptors. "( Sumatriptan Increases Skin Flap Survival through Activation of 5-Hydroxytryptamine 1b/1d Receptors in Rats: The Mediating Role of the Nitric Oxide Pathway.
Abbaszadeh-Kasbi, A; Afshari, K; Amirlak, B; Dehdashtian, A; Dehpour, AR; Haddadi, NS; Jazaeri, F; Sheikhi, M; Tavangar, SM; Zarifeh Jazaeri, S, 2019
)
3.4
"Sumatriptan can cause myocardial ischaemia and myocardial infarction."( Amplification of sumatriptan-induced contractions with phenylephrine, histamine and KCl in the isolated human mesenteric artery: in-vitro evidence for sumatriptan-induced mesenteric ischaemia.
Gul, H; Yildiz, O, 2002
)
1.38
"The sumatriptan-induced increase of growth hormone concentrations was significantly (P < 0.05) blunted in patients with active cluster headache."( Abnormal 5-HT1D receptor function in cluster headache: a neuroendocrine study with sumatriptan.
Arvat, E; Del Rizzo, P; Ferrero, M; Gianotti, L; Limone, P; Lo Giudice, R; Pinessi, L; Rainero, I; Rivoiro, C; Valfrè, W, 2003
)
1.02
"The Sumatriptan-induced increase in GH responses to GHRH was dependent on the stimulus tested."( Role of the serotonin receptor subtype 5-HT1D on basal and stimulated growth hormone secretion.
Bento, A; Dieguez, C; Mota, A; Peñalva, A; Pombo, M, 1995
)
0.77
"Both sumatriptan and 5-HT inhibit adenylate cyclase activity at doses which correlate with the mitogenic effect."( 5-HT1D receptor type is involved in stimulation of cell proliferation by serotonin in human small cell lung carcinoma.
Bondiolotti, G; Cattaneo, MG; Palazzi, E; Vicentini, LM, 1994
)
0.74
"Sumatriptan appears to cause peripheral venoconstriction only at high doses locally applied (in the hand vein), by acting on 5HT2 receptors."( Amplifying effect of sumatriptan on noradrenaline venoconstriction in migraine patients.
Anselmi, B; Curradi, C; Franchi, G; Panconesi, A; Tarquini, B, 1993
)
1.33
"Sumatriptan was found to suppress the CPH attacks as well as indomethacin."( Intracranial hypertension and sumatriptan efficacy in a case of chronic paroxysmal hemicrania which became bilateral. (The mechanism of indomethacin in CPH).
Hannerz, J; Jogestrand, T, 1993
)
1.3
"Sumatriptan failed to produce a significant reduction in sensory and total pain scores at 60 minutes following treatment, however the result was statistically significant for the affective pain score (P < .05)."( A double-blind, placebo-controlled, crossover, study to evaluate the efficacy of subcutaneous sumatriptan in the treatment of atypical facial pain.
al Balawi, S; Feinmann, C; Tariq, M, 1996
)
1.23
"Sumatriptan blunted the increase in blood flow following stimulation of the trigeminal ganglion."( Trigeminal ganglion elicited increases in nucleus trigeminal caudalis blood flow: a novel migraine model.
McCall, RB, 1997
)
1.02
"Sumatriptan did not cause relaxation."( Sumatriptan contracts large coronary arteries of beagle dogs through 5-HT1-like receptors.
Kaumann, AJ; Parsons, AA; Raval, P; Stutchbury, C, 1992
)
2.45

Treatment

Sumatriptan/naproxen treatment resulted in significantly higher medication satisfaction scores on the efficacy, functionality, and total efficacy subscales compared with placebo in all attacks. Sum atriptan treatment during the aura preempted the development of headache in 34/38 (89%) attacks.

ExcerptReferenceRelevance
"Sumatriptan treatment significantly reduced the mechanical hypersensitivity induced by IS stimulations and decreased the BBB disruption and VEGF expression."( Recurrent Headache Increases Blood-Brain Barrier Permeability and VEGF Expression in Rats.
Chen, L; Mi, X; Qin, G; Ran, L, 2018
)
1.2
"Sumatriptan/naproxen treatment resulted in significantly higher medication satisfaction scores on the efficacy, functionality, and total efficacy subscales compared with placebo in all attacks in both studies."( Consistency of return to normal function, productivity, and satisfaction following migraine attacks treated with sumatriptan/naproxen sodium combination.
Cady, RK; Landy, SH; Nelsen, A; Runken, MC; White, J, 2014
)
1.33
"Sumatriptan treatment during the aura preempted the development of headache in 34/38 (89%) attacks. "( Revisiting the efficacy of sumatriptan therapy during the aura phase of migraine.
Aurora, SK; Barrodale, PM; Burstein, R; Jakubowski, M; McDonald, SA, 2009
)
2.09
"Sumatriptan pre-treatment significantly delayed solid but not liquid gastric emptying (t1/2 respectively 159 +/- 11 vs. "( Influence of delaying gastric emptying on meal-related symptoms in healthy subjects.
Coulie, B; Janssens, J; Tack, J; Verbeke, K, 2006
)
1.78
"More sumatriptan-treated patients were completely pain free compared with placebo-treated patients at both 2 h (24% versus 12%) and 4 h (48% versus 18)."( Oral sumatriptan compared with placebo in the acute treatment of migraine.
Byrne, M; Nappi, G; Roncolato, M; Sicuteri, F; Zerbini, O, 1994
)
1.26
"Sumatriptan also treated nausea and photophobia more effectively in menstrual-migraine patients than did placebo."( Treatment of menstruation-associated migraine headache with subcutaneous sumatriptan.
Solbach, MP; Waymer, RS, 1993
)
1.24
"Sumatriptan-treated patients used rescue medication for 19% of their attacks, compared to 59% for comparator drugs (p = 0.001)."( Comparison of subcutaneous sumatriptan with usual acute treatments for migraine. French Sumatriptan Study Group.
Bertin, L; Boureau, F; Chazot, G; d'Allens, H; Emile, J, 1995
)
1.31
"More sumatriptan-treated patients than placebo-treated patients reported adverse events (29% versus 16%) but the difference was not statistically significant."( [Evaluation of the efficacy of oral sumatriptan in the management of migraine attacks. Clinical results].
Albano, O; Bassi, A; Cassiano, MA; Centonze, V; Di Bari, M; Fabbri, L; Polito, MB, 1995
)
1.02
"Sumatriptan is an acute treatment for migraine which is often used by women in their child-bearing years, and who become unexpectedly pregnant. "( Pregnancy and perinatal outcomes in migraineurs using sumatriptan: a prospective study.
Davis, RL; Ephross, SA; Fox, AW; Gutterman, DL; O'Quinn, S; Williams, V, 1999
)
1.99
"Sumatriptan treatment tended to reduce median productivity loss 2 hours after injection compared with placebo (25.2 vs 29.9 minutes, respectively; P = .14)."( Effectiveness of sumatriptan in reducing productivity loss due to migraine: results of a randomized, double-blind, placebo-controlled clinical trial.
Batenhorst, AS; Cady, RK; Henry, D; O'Quinn, SO; Putnam, DG; Schulman, EA; Watson, CB, 2000
)
1.37
"Sumatriptan treatment had beneficial effects on aspects of health state and mood during the postictal period."( Effects of medication use on health state in postictal migraineurs.
de Geus, EJ; Linssen, WH; Mulder, EJ; Passchier, J, 2001
)
1.03
"Sumatriptan treatment was associated with a 3-fold increase in payments for services for painful respiration and other chest pain."( Cost savings in migraine associated with less chest pain on new triptan therapy.
Barr, CE; Goldfarb, SD; Rowland, CR; Torigoe, Y; Wang, E; Wang, JT, 2002
)
1.04
"Pre-treatment with sumatriptan attenuated PACAP38-induced headache without affecting PACAP38-induced arterial dilation."( Investigation of sumatriptan and ketorolac trometamol in the human experimental model of headache.
Al-Karagholi, MA; Amin, FM; Arngrim, N; Ashina, M; Ghanizada, H; Larsson, HBW; Metcalf-Clausen, M; Mørch-Rasmussen, M, 2020
)
1.22
"Pre-treatment with sumatriptan decreased 5-hydroxytryptamine (5HT) level by 53%, and significantly decreased calcitonin gene-related peptide (CGRP) levels, lipid pereoxidation, neutrophil infiltration, and level of pro-inflammatory markers in the serum."( Involvement of 5-HT1B/1D receptors in the inflammatory response and oxidative stress in intestinal ischemia/reperfusion in rats.
Abdollahi, A; Dehpour, AR; Gharishvandi, F; Mohammad Jafari, R; Pasalar, P; Shafaroodi, H, 2020
)
0.88
"Pre-treatment with sumatriptan prevents cilostazol induced headache from developing. "( Pre-treatment with sumatriptan for cilostazol induced headache in healthy volunteers.
Falkenberg, K; Olesen, J, 2018
)
1.14
"Treatment with sumatriptan significantly increased the endothelial nitric oxide synthase (eNOS) expression consequences nitric oxide metabolites' level in I/R rats."( Sumatriptan protects against myocardial ischaemia-reperfusion injury by inhibition of inflammation in rat model.
Azizi, Y; Dehpour, AR; Dehpour, S; Faghir-Ghanesefat, H; Ghahremani, MH; Keshavarz-Bahaghighat, H; Rahimi, N; Sepand, MR; Sheibani, M, 2019
)
2.3
"Treatment with sumatriptan during migraine attacks appeared to be associated with a decrease in 5-HT1B receptor binding, a finding that is most likely associated with the binding of sumatriptan to central 5-HT1B receptors, but the contribution of ongoing cerebral serotonin release to the lower binding cannot be excluded; the migraine attack-associated decrease in binding could indicate that migraine attacks are associated with increases in endogenous serotonin."( Association Between Sumatriptan Treatment During a Migraine Attack and Central 5-HT1B Receptor Binding.
Ashina, M; Deen, M; Dyssegaard, A; Hansen, HD; Hougaard, A; Knudsen, GM; Schain, M, 2019
)
1.19
"Treatment with sumatriptan-naproxen may provide relief of menstrual symptoms and migraine in female migraineurs with dysmenorrhea. "( Relief of menstrual symptoms and migraine with a single-tablet formulation of sumatriptan and naproxen sodium.
Ballard, J; Derosier, FJ; Diamond, MP; Krishen, A; Lener, SE; Mannix, LK; Martin, VT; McDonald, SA, 2014
)
0.98
"Treatment with sumatriptan repressed NGF- and MAPK-stimulated CGRP promoter activity."( Stimulation of the calcitonin gene-related peptide enhancer by mitogen-activated protein kinases and repression by an antimigraine drug in trigeminal ganglia neurons.
Durham, PL; Russo, AF, 2003
)
0.66
"Pretreatment with sumatriptan increased both pressures and volumes needed to induce first perception and discomfort."( Role of tension receptors in dyspeptic patients with hypersensitivity to gastric distention.
Caenepeel, P; Corsetti, M; Janssens, J; Tack, J, 2004
)
0.65
"Treatment with sumatriptan/naproxen sodium allowed significantly more subjects to return to normal or mildly impaired functioning more quickly, and sumatriptan/naproxen sodium patients were significantly more satisfied with their treatment compared with other treatment groups. "( Two double-blind, multicenter, randomized, placebo-controlled, single-dose studies of sumatriptan/naproxen sodium in the acute treatment of migraine: function, productivity, and satisfaction outcomes.
Ames, MH; Burch, SP; DeRossett, SE; Landy, S; McDonald, SA; Rapoport, A; Rothrock, J, 2007
)
0.92
"Treatment with sumatriptan was well tolerated."( High efficacy and low frequency of headache recurrence after oral sumatriptan. The Oral Sumatriptan Italian Study Group.
Bamfi, F; Fabbri, L; Pini, LA; Sternieri, E; Zerbini, O,
)
0.71
"Pretreatment with Sumatriptan did not modify the GH response to clonidine or pyridostigmine, as assessed by the peak GH response and the area under the curve."( Role of the serotonin receptor subtype 5-HT1D on basal and stimulated growth hormone secretion.
Bento, A; Dieguez, C; Mota, A; Peñalva, A; Pombo, M, 1995
)
0.61
"Treatment with sumatriptan during the migraine attack was accompanied by a significant increase in the duration of ES2 (p < or = 0.05), but no significant changes in the durations of the late suppression periods were observed under any other conditions."( Exteroceptive suppression of temporalis muscle activity during migraine attack and migraine interval before and after treatment with sumatriptan.
Dworschak, M; Ensink, FB; Göbel, H; Heuss, D; Krapat, S; Soyka, D, 1994
)
0.83
"Treatment with sumatriptan has been well tolerated with only minor, transient, acute side effects reported."( Sumatriptan in the treatment of migraine.
Ferrari, MD, 1993
)
2.07
"Treatment with sumatriptan was associated with significant (P < .05) improvements relative to baseline in three of the Short Form-36 Health Survey quality-of-life dimensions (Bodily Pain, General Health Perceptions, and Social Functioning) and three of the Migraine-Specific Quality of Life Questionnaire dimensions (Role Function-Restrictive, Role Function-Preventive, and Emotional Function). "( Improvements in health-related quality of life with sumatriptan treatment for migraine.
Cady, RK; Grice, RB; Gutterman, DL; Jhingran, P; Miller, D; Rubino, J, 1996
)
0.9
"Oral treatment with sumatriptan 100 mg tid over a 7-day period was not associated with an increased or altered adverse event profile from that previously reported."( Preemptive oral treatment with sumatriptan during a cluster period.
Cole, J; Krabbe, A; Micieli, G; Monstad, I; Pilgrim, A; Prusinski, A; Shevlin, P,
)
0.73
"Treatment with sumatriptan was efficient in 89.5% of the attacks."( [18 months long-term analysis of effectiveness, safety and tolerance of sumatriptan s.c. in acute therapy of migraine attacks].
Christiani, K; Dworschak, M; Göbel, H; Heinze, A; Heuss, D; Lindner, V; Stolze, H, 1996
)
0.87
"Treatment with sumatriptan reduced the numbers of Fos-positive cells found in laminae I and IIo of the TNC and C2 (6, 13 cells and 9 cells, respectively) after mechanical stimulation."( Sumatriptan can inhibit trigeminal afferents by an exclusively neural mechanism.
Goadsby, PJ; Hoskin, KL; Kaube, H, 1996
)
2.08
"Treatment with sumatriptan was effective in 88% of the attacks and 57% of the patients were pain-free within 15 min after injection; 42% of the patients became painfree within 15 min after at least 90% of their attacks."( [Acute therapy of episodic and chronic cluster headache with sumatriptan s.c. Results of a one-year long-term study].
Göbel, H; Heinze, A; Lindner, V; Pfaffenrath, V; Ribbat, M; Stolze, H, 1998
)
0.88
"Pretreatment with sumatriptan (n = 9) produced a highly significant reduction in the ratio of extravasation within the dura to 1.10 +/- 0.06 (P = 0.002) and in the retina to 0.96 +/- 0.06 (P = 0.001), as did the neurokinin-1 receptor antagonist RP 67580 (n = 12) in the dura (1.04 +/- 0.11, P = 0.002) and retina (1.08 +/- 0.06, P = 0.001)."( Retinal plasma extravasation in animals but not in humans: implications for the pathophysiology of migraine.
Diener, HC; Effert, R; Goadsby, PJ; Hargreaves, RJ; Knorr, M; May, A; Shepheard, SL; Wessing, A, 1998
)
0.62
"Pretreatment with sumatriptan is able to restore impaired accommodation and to improve early satiety in patients with functional dyspepsia."( The physiology and the pathophysiology of the gastric accommodation reflex in man.
Tack, J, 2000
)
0.63
"Pretreatment with sumatriptan (720 nmol kg-1 x 2, i.v.) did not block c-fos expression in trigeminal nucleus caudalis following formalin application to the nasal mucosa.6."( CP-93,129, sumatriptan, dihydroergotamine block c-fos expression within rat trigeminal nucleus caudalis caused by chemical stimulation of the meninges.
Boccalini, P; Moskowitz, MA; Nozaki, K, 1992
)
1

Toxicity

The incidence and nature of adverse events in the asthmatic patient subgroup who received sumatriptan was similar to that in the complete clinical trial population. Diclofenac-potassium seemed to be as well tolerated as placebo.

ExcerptReferenceRelevance
" Adverse events were dose related; the most common types were injection site reactions and tingling."( Dose ranging efficacy and safety of subcutaneous sumatriptan in the acute treatment of migraine. US Sumatriptan Research Group.
Couch, J; Dexter, J; Flamenbaum, W; Goldstein, J; Mathew, NT; Rapoport, A; Saper, J; Sheftell, F; Silberstein, S; Solomon, S, 1992
)
0.54
" Safety monitoring involved collection of all adverse events, regardless of their relationship to treatment, and included routine laboratory screening tests and some special investigations."( The safety and tolerability of sumatriptan: an overview.
Brown, EG; Endersby, CA; Smith, RN; Talbot, JC, 1991
)
0.57
" The incidence and nature of adverse events in this study were similar to that seen in previous studies."( The efficacy and safety of subcutaneous sumatriptan in the acute treatment of menstrual migraine. The Sumatriptan Menstrual Migraine Study Group.
Bonellie, G; Facchinetti, F; Kangasniemi, P; Pascual, J; Shuaib, A, 1995
)
0.56
" Because sumatriptan does not appear to cross the blood-brain barrier and has a short half-life, it was deemed relatively safe to prescribe sumatriptan with antidepressant treatments."( The safety of concomitant use of sumatriptan and antidepressant treatments.
Bergeron, R; Blier, P, 1995
)
0.99
" The majority of adverse events (defined as any medical event irrespective of possible causal relationship to treatment) were mild to moderate in intensity, transient and resolved spontaneously."( The clinical profile of sumatriptan: safety and tolerability.
Lloyd, K, 1994
)
0.6
" The incidence and nature of adverse events in the asthmatic patient subgroup who received sumatriptan was similar to that in the complete clinical trial population."( The safety of sumatriptan in asthmatic migraineurs.
Lloyd, DK; Pilgrim, AJ, 1993
)
0.87
"The study tried to investigate the efficacy, adverse events and possible risk factors of sumatriptan in daily clinical practice."( [Sumatriptan--side effects and problems in routine clinical practice].
Aull, S; Marterer, A; Schnider, P; Wessely, P; Wöber, C, 1995
)
1.42
" Adverse events were reported by 69% of the patients which was more frequent than in most clinic studies described."( [Sumatriptan--side effects and problems in routine clinical practice].
Aull, S; Marterer, A; Schnider, P; Wessely, P; Wöber, C, 1995
)
1.2
" The risk as to severe adverse events, especially cardial adverse events, exists if contraindications for sumatriptan are not considered."( [Sumatriptan--side effects and problems in routine clinical practice].
Aull, S; Marterer, A; Schnider, P; Wessely, P; Wöber, C, 1995
)
1.42
"9% of the patients withdrew from the study because of adverse events and because they felt the treatment was not effective."( [18 months long-term analysis of effectiveness, safety and tolerance of sumatriptan s.c. in acute therapy of migraine attacks].
Christiani, K; Dworschak, M; Göbel, H; Heinze, A; Heuss, D; Lindner, V; Stolze, H, 1996
)
0.53
" They are almost always benign, but can be mistaken for a serious adverse event by the patient."( The site of common side effects of sumatriptan.
Lipton, RB; Newman, LC; Solomon, S, 1997
)
0.57
" The suppositories were generally well tolerated; transient asthenia, drowsiness, and headache were the most frequently reported adverse events, and these were not dose-related."( Safety, tolerability, and pharmacokinetics of sumatriptan suppositories following single and multiple doses in healthy volunteers.
Aubert, B; Fowler, PA; Hussey, EK; Kunka, RL; Pakes, GE; Richard, I; Shaw, S; Warner, P, 1997
)
0.56
" Adverse events were mild and consisted mainly of bitter taste at the back of the throat and events typical of sumatriptan administered by other routes (headache, lightheadedness and tingling)."( Safety, tolerability, and pharmacokinetics of sumatriptan in healthy subjects following ascending single intranasal doses and multiple intranasal doses.
Duquesnoy, C; Fuseau, E; Hussey, EK; Moore, KH; Pakes, GE; Shaw, S, 1997
)
0.77
" For 6 hours after treatment, a continuous electrocardiogram (ECG) was performed, and headache severity, adverse events, and vital signs were recorded."( Monitoring of acute migraine attacks: placebo response and safety data.
Cutler, NR; Ford, NF; Fulmor, IE; Jhee, SS; Salazar, DE; Sramek, JJ, 1998
)
0.3
" The incidence of adverse events with 25-mg and 50-mg sumatriptan tablets was similar to the incidence with placebo and lower than the incidence with 100-mg sumatriptan tablets."( Efficacy and safety of sumatriptan tablets (25 mg, 50 mg, and 100 mg) in the acute treatment of migraine: defining the optimum doses of oral sumatriptan.
Cunin, G; Pfaffenrath, V; Prendergast, S; Sjonell, G, 1998
)
0.86
"To evaluate the efficacy, speed of onset, and adverse events of 6 mg subcutaneous, 100 mg oral, and 20 mg intranasal sumatriptan in the treatment of migraine attacks."( Efficacy and adverse events of subcutaneous, oral, and intranasal sumatriptan used for migraine treatment: a systematic review based on number needed to treat.
Tfelt-Hansen, P, 1998
)
0.75
"Numbers needed to treat (NNT) were calculated for relief of headache and for adverse events (when data were available)."( Efficacy and adverse events of subcutaneous, oral, and intranasal sumatriptan used for migraine treatment: a systematic review based on number needed to treat.
Tfelt-Hansen, P, 1998
)
0.54
"Subcutaneous sumatriptan in a dose of 6 mg is significantly more efficacious than 100 mg of oral sumatriptan, but causes more adverse events than oral sumatriptan."( Efficacy and adverse events of subcutaneous, oral, and intranasal sumatriptan used for migraine treatment: a systematic review based on number needed to treat.
Tfelt-Hansen, P, 1998
)
0.91
" Forty-five patients (88%) reported at least one adverse event and 23 (45%) experienced pressure, tightness, and/or pain in the chest, neck, and/or throat after administration of avitriptan."( Safety trial with the 5HT1B/1D agonist avitriptan (BMS-180048) in patients with migraine who have experienced pressure, tightness, and/or pain in the chest, neck, and/or throat following sumatriptan.
Dahlöf, CG; Falk, L; Lewis, CP; Risenfors, M, 1998
)
0.49
" However, while effective, it has low oral bioavailability and some problematic adverse effects."( Acute treatment of migraine attacks: efficacy and safety of a nonsteroidal anti-inflammatory drug, diclofenac-potassium, in comparison to oral sumatriptan and placebo. The Diclofenac-K/Sumatriptan Migraine Study Group.
, 1999
)
0.5
" Diclofenac-potassium seemed to be as well tolerated as placebo, with fewer adverse events reported than after sumatriptan treatment and with more patients assessing the overall tolerability of diclofenac-potassium better than that of sumatriptan."( Acute treatment of migraine attacks: efficacy and safety of a nonsteroidal anti-inflammatory drug, diclofenac-potassium, in comparison to oral sumatriptan and placebo. The Diclofenac-K/Sumatriptan Migraine Study Group.
, 1999
)
0.72
" Sumatriptan is more effective, but resulted in more adverse events."( Efficacy and safety of intravenous acetylsalicylic acid lysinate compared to subcutaneous sumatriptan and parenteral placebo in the acute treatment of migraine. A double-blind, double-dummy, randomized, multicenter, parallel group study. The ASASUMAMIG St
Diener, HC, 1999
)
1.43
"9% of the patients withdrew from the study because of insufficient efficacy or adverse events."( Open-labeled long-term study of the efficacy, safety, and tolerability of subcutaneous sumatriptan in acute migraine treatment.
Göbel, H; Heinze, A; Heinze-Kuhn, K; Lindner, V; Stolze, H, 1999
)
0.53
" The results show that the overall incidence of adverse events among patients receiving sumatriptan injections for the treatment of cluster headache is low."( Sumatriptan overuse in episodic cluster headache: lack of adverse events, rebound syndromes, drug dependence and tachyphylaxis.
Albano, O; Bassi, A; Cassiano, MA; Causarano, V; Centonze, A; Centonze, V; Dalfino, L; Fabbri, L,
)
1.8
"8 mg group is due to the termination of this trial arm after the incidence of a serious adverse event and a subsequent protocol amendment."( The efficacy and safety of sc alniditan vs. sc sumatriptan in the acute treatment of migraine: a randomized, double-blind, placebo-controlled trial.
Dahlöf, C; de Beukelaar, F; Diener, HC; Ferrari, MD; Mathew, N; Olesen, J; Tfelt-Hansen, P, 2001
)
0.57
" Safety and tolerability were assessed through the collection of adverse events, monitoring of heart rate and blood pressure performance of 12-lead electrocardiogram, hematology screen, and blood chemistry studies."( Tolerability and safety of frovatriptan with short- and long-term use for treatment of migraine and in comparison with sumatriptan.
Géraud, G; Keywood, C; Spierings, EL, 2002
)
0.52
" The incidence of adverse events was higher in the frovatriptan-treated patients than in the patients who took placebo (47% versus 34%) and the spectrum of adverse events was similar."( Tolerability and safety of frovatriptan with short- and long-term use for treatment of migraine and in comparison with sumatriptan.
Géraud, G; Keywood, C; Spierings, EL, 2002
)
0.52
" Frovatriptan treatment produced an adverse events profile similar to that of placebo, and in a direct comparison study was better tolerated than sumatriptan 100 mg."( Tolerability and safety of frovatriptan with short- and long-term use for treatment of migraine and in comparison with sumatriptan.
Géraud, G; Keywood, C; Spierings, EL, 2002
)
0.72
"To determine the level of concern among migraineurs about migraine prescription medication tolerability and adverse effects and the impact of these concerns on their self-management of migraine."( Migraine medication attributes important for patient compliance: concerns about side effects may delay treatment.
Gallagher, RM; Kunkel, R, 2003
)
0.32
" Of those meeting the criteria, pain relief and speed of onset were important product attributes for 75% to 77% of sufferers, and the absence of adverse effects was important to over 40%."( Migraine medication attributes important for patient compliance: concerns about side effects may delay treatment.
Gallagher, RM; Kunkel, R, 2003
)
0.32
"Adverse effects are an important factor in migraine management, and concern about adverse effects significantly affected patient compliance."( Migraine medication attributes important for patient compliance: concerns about side effects may delay treatment.
Gallagher, RM; Kunkel, R, 2003
)
0.32
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32
" Safety evaluations included adverse events and laboratory tests."( Twelve-month tolerability and safety of sumatriptan-naproxen sodium for the treatment of acute migraine.
Alexander, WJ; Cady, RK; Frishberg, BM; Kori, SH; Lener, SE; Ruoff, GE; Winner, P; Zhang, Y, 2007
)
0.61
" The most common treatment-related adverse events were nausea, muscle tightness, and dizziness."( Twelve-month tolerability and safety of sumatriptan-naproxen sodium for the treatment of acute migraine.
Alexander, WJ; Cady, RK; Frishberg, BM; Kori, SH; Lener, SE; Ruoff, GE; Winner, P; Zhang, Y, 2007
)
0.61
" The adverse events did not differ from those expected for the individual components alone, and no new or unexpected findings occurred."( Twelve-month tolerability and safety of sumatriptan-naproxen sodium for the treatment of acute migraine.
Alexander, WJ; Cady, RK; Frishberg, BM; Kori, SH; Lener, SE; Ruoff, GE; Winner, P; Zhang, Y, 2007
)
0.61
" Safety was evaluated based on the frequency of reported adverse events, and treatment with eASA was associated with lower incidence of adverse events than was with sumatriptan."( Efficacy and safety of 1,000 mg effervescent aspirin: individual patient data meta-analysis of three trials in migraine headache and migraine accompanying symptoms.
Diener, HC; Lampl, C; Voelker, M, 2007
)
0.54
" In addition, the incidence of adverse events with 2 sumatriptan/naproxen sodium tablets administered 2 hours apart was lower than that with the single dose."( Distinct pharmacokinetic profile and safety of a fixed-dose tablet of sumatriptan and naproxen sodium for the acute treatment of migraine.
Haberer, LJ; Lener, SE; McDonald, SA; Taylor, DR; Walls, CM, 2010
)
0.84
" In AT1, which was previously published in part, group differences in adverse events (AEs) were analyzed using the Fisher exact test, and response rates were compared using logistic regression."( Safety and tolerability of frovatriptan in the acute treatment of migraine and prevention of menstrual migraine: Results of a new analysis of data from five previously published studies.
Campbell, JC; Hu, X; MacGregor, EA; Pawsey, SP, 2010
)
0.36
" Information regarding safety of triptans while breastfeeding is limited but also reassuring, as the minimal amounts excreted into the milk are insufficient to cause any adverse effects on the breastfeeding infant."( Safety of triptans for migraine headaches during pregnancy and breastfeeding.
Bozzo, P; Duong, S; Einarson, A; Nordeng, H, 2010
)
0.36
" An understanding of structure-activity relationships (SARs) of chemicals can make a significant contribution to the identification of potential toxic effects early in the drug development process and aid in avoiding such problems."( Developing structure-activity relationships for the prediction of hepatotoxicity.
Fisk, L; Greene, N; Naven, RT; Note, RR; Patel, ML; Pelletier, DJ, 2010
)
0.36
" Adverse events were reported by 80%, 56%, and 60% of BGG492, sumatriptan, and placebo subjects, respectively."( Randomized, multicenter trial to assess the efficacy, safety and tolerability of a single dose of a novel AMPA receptor antagonist BGG492 for the treatment of acute migraine attacks.
Brand, R; Campos, V; Diener, HC; Evers, S; Göbel, H; Gomez-Mancilla, B; Hariry, S; Johns, D; Jürgens, TP; Kalkman, HO; Pezous, N; Sommer, C; Sommer, M; Straube, A, 2014
)
0.64
" Expert commentary: A new formulation of a low-dose sumatriptan intranasal powder administered via a novel breath-powered delivery device appears to be a safe and efficacious option for the acute management of a migraine ideally suited for this situation."( The efficacy and safety of sumatriptan intranasal powder in adults with acute migraine.
Freitag, FG; Shumate, DA, 2016
)
0.98
" Safety was evaluated by monitoring of adverse events in addition to laboratory and clinical assessments."( A Phase I, Open-Label, Single-Dose Safety, Pharmacokinetic, and Tolerability Study of the Sumatriptan Iontophoretic Transdermal System in Adolescent Migraine Patients.
Aycardi, E; Bigal, ME; Chitra, R; Gutman, D; Hellriegel, E; Kansagra, S; Kidron, OS; Knebel, H; Kunta, J; Linder, S; Ma, Y; Pierce, M; Spiegelstein, O; Winner, PK, 2016
)
0.66
" All adverse events were mild or moderate, with application-site paresthesia being the most common (32%)."( A Phase I, Open-Label, Single-Dose Safety, Pharmacokinetic, and Tolerability Study of the Sumatriptan Iontophoretic Transdermal System in Adolescent Migraine Patients.
Aycardi, E; Bigal, ME; Chitra, R; Gutman, D; Hellriegel, E; Kansagra, S; Kidron, OS; Knebel, H; Kunta, J; Linder, S; Ma, Y; Pierce, M; Spiegelstein, O; Winner, PK, 2016
)
0.66
" The objective of this study was to evaluate the safety and tolerability of DFN-02 (10 mg) in the acute treatment of episodic migraine with and without aura over a 6-month period based on the incidence of treatment-emergent adverse events and the evaluation of results of clinical laboratory tests, vital signs, physical examination, and electrocardiograms."( A multicenter, open-label, long-term safety and tolerability study of DFN-02, an intranasal spray of sumatriptan 10 mg plus permeation enhancer DDM, for the acute treatment of episodic migraine.
Allenby, K; Brand-Schieber, E; Cady, RK; Munjal, S; Rapoport, AM; Spierings, ELH, 2017
)
0.67
" Adverse events were those expected for triptans, as well as for nasally administered compounds."( A multicenter, open-label, long-term safety and tolerability study of DFN-02, an intranasal spray of sumatriptan 10 mg plus permeation enhancer DDM, for the acute treatment of episodic migraine.
Allenby, K; Brand-Schieber, E; Cady, RK; Munjal, S; Rapoport, AM; Spierings, ELH, 2017
)
0.67
" AVP-825 was well tolerated in controlled trials, with the most common adverse events localized at the administration-site (abnormal taste, nasal discomfort); these were mostly mild, leading to only one discontinuation."( A review of clinical safety data for sumatriptan nasal powder administered by a breath powered exhalation delivery system in the acute treatment of migraine.
Silberstein, SD, 2018
)
0.75
"6% (89/219) of subjects reported treatment-emergent adverse events (TEAE), the most common of which were associated with the injection site: swelling (12."( Efficacy and safety of DFN-11 (sumatriptan injection, 3 mg) in adults with episodic migraine: an 8-week open-label extension study.
Brand-Schieber, E; Landy, S; Munjal, S; Rapoport, AM, 2018
)
0.77
"DFN-11 was effective, tolerable, and safe in the acute treatment of 4 migraine attacks over 8 weeks, with consistent responses on pain and associated symptoms."( Efficacy and safety of DFN-11 (sumatriptan injection, 3 mg) in adults with episodic migraine: an 8-week open-label extension study.
Brand-Schieber, E; Landy, S; Munjal, S; Rapoport, AM, 2018
)
0.77
"4% (16/119) who received placebo experienced at least 1 treatment-emergent adverse event (TEAE), the most common of which were injection site swelling (7."( Efficacy and safety of DFN-11 (sumatriptan injection, 3 mg) in adults with episodic migraine: a multicenter, randomized, double-blind, placebo-controlled study.
Brand-Schieber, E; Landy, S; Munjal, S; Rapoport, AM, 2018
)
0.77
" As of 2018, the FDA Adverse Event Reporting System public dashboard lists a total of 2889 reports of safety problems with the patch, 904 of which were classified as serious."( Safety Problems With a Transdermal Patch for Migraine: Lessons From the Development, Approval, and Marketing Process.
Burch, RC; Loder, EW; Rayhill, M, 2018
)
0.48
" Approval was based on 1 clinical trial and 2 open label studies in which reporting of adverse events was suboptimal."( Safety Problems With a Transdermal Patch for Migraine: Lessons From the Development, Approval, and Marketing Process.
Burch, RC; Loder, EW; Rayhill, M, 2018
)
0.48
" Treatment-emergent adverse events were evaluated up to 30 days after the last dose in the Phase 1 and Phase 3 studies."( Evaluation of the Pharmacokinetic Interaction of Ubrogepant Coadministered With Sumatriptan and of the Safety of Ubrogepant With Triptans.
Boinpally, R; Butler, M; Jakate, A; Lu, K; McGeeney, D; Periclou, A, 2020
)
0.79
" No treatment-emergent adverse events were reported with the coadministration of ubrogepant 100 mg and sumatriptan 100 mg in the Phase 1 study."( Evaluation of the Pharmacokinetic Interaction of Ubrogepant Coadministered With Sumatriptan and of the Safety of Ubrogepant With Triptans.
Boinpally, R; Butler, M; Jakate, A; Lu, K; McGeeney, D; Periclou, A, 2020
)
1
"We aimed at evaluating adverse drug reactions during the post-marketing phase with erenumab as the suspected/interacting drug in Eudravigilance, with the final goal of investigating the consistency of the disproportionality signals (DS) for erenumab in Eudravigilance and the American Food and Drug Administration Adverse Event Reporting System (FDA FAERS) and undetected DS from Eudravigilance."( Post-marketing safety surveillance of erenumab: new insight from Eudravigilance.
Liang, D; Sessa, M, 2022
)
0.72
" The three system organ classes with the highest proportion of adverse events were general disorders and administration site conditions (16."( Post-marketing safety surveillance of erenumab: new insight from Eudravigilance.
Liang, D; Sessa, M, 2022
)
0.72

Pharmacokinetics

There were slight alterations in ubrogepant pharmacokinetic parameters when coadministered with sumatriptan. Such changes are expected to have minimal clinical relevance. For all doses, the tmax of sum atriptan occurred within 2.5 h after dosing. Headache recurrence and lack of headache relief do not appear to be explained by pharmacokinetics or pharmacodynamic differences between patients.

ExcerptReferenceRelevance
" There were no significant differences between treatments in relation to Cmax (82."( Lack of effect of flunarizine on the pharmacokinetics and pharmacodynamics of sumatriptan in healthy volunteers.
De Schepper, PJ; Depré, M; Durham, JM; Fowler, PA; Lacey, LF; Van Hecken, AM, 1992
)
0.51
" Pharmacokinetic and pharmacodynamic variables were similar in all groups studied and were not altered by the presence of food, alcohol, dihydroergotamine or prophylactic migraine treatments."( The clinical pharmacology, pharmacokinetics and metabolism of sumatriptan.
Baber, NS; Fowler, PA; Keene, ON; Lacey, LF; Tanner, RJ; Thomas, M, 1991
)
0.52
" There were no statistically significant differences for butorphanol between the 2 treatments on any of the following pharmacokinetic parameters: Cmax, tmax, AUC, t1/2, CL/f, and Vz/f."( Lack of pharmacokinetic interaction between butorphanol tartrate nasal spray and sumatriptan succinate.
Barbhaiya, RH; Lee, JS; Shyu, WC; Srinivas, NR; Upmalis, D, 1995
)
0.52
" Single-dose pharmacokinetic studies reflect the way that sumatriptan will be used in routine practice, but relatively few studies have been published."( Sumatriptan clinical pharmacokinetics.
Scott, AK, 1994
)
1.98
" We studied whether pharmacokinetic or pharmacodynamic differences may explain these different clinical effects."( Pharmacokinetic and pharmacodynamic profiles of sumatriptan in migraine patients with headache recurrence or no response.
Burggraaf, J; Cohen, AF; Ferrari, MD; Fowler, PA; Muller, LM; Schoemaker, RC; Visser, WH, 1996
)
0.55
"We compared the pharmacokinetic profiles of subcutaneous sumatriptan in 14 patients who consistently had headache relief without headache recurrence, in 12 patients who had headache recurrence in every attack, and in six patients who did not have headache relief after sumatriptan."( Pharmacokinetic and pharmacodynamic profiles of sumatriptan in migraine patients with headache recurrence or no response.
Burggraaf, J; Cohen, AF; Ferrari, MD; Fowler, PA; Muller, LM; Schoemaker, RC; Visser, WH, 1996
)
0.79
"Despite sufficient power of the study, no important differences in pharmacokinetic and pharmacodynamic profiles between the three patient groups were detected."( Pharmacokinetic and pharmacodynamic profiles of sumatriptan in migraine patients with headache recurrence or no response.
Burggraaf, J; Cohen, AF; Ferrari, MD; Fowler, PA; Muller, LM; Schoemaker, RC; Visser, WH, 1996
)
0.55
"Headache recurrence and lack of headache relief after sumatriptan do not appear to be explained by pharmacokinetic or pharmacodynamic differences between patients, which may be an important finding for the development of novel antimigraine drugs."( Pharmacokinetic and pharmacodynamic profiles of sumatriptan in migraine patients with headache recurrence or no response.
Burggraaf, J; Cohen, AF; Ferrari, MD; Fowler, PA; Muller, LM; Schoemaker, RC; Visser, WH, 1996
)
0.8
"We investigated the hypothesis that distributions of continuous pharmacokinetic variables are positively skewed in nature and that logarithmic transformation of these variables restores normality."( Common noncompartmental pharmacokinetic variables: are they normally or log-normally distributed?
Bye, A; Keene, ON; Lacey, LF; Pritchard, JF, 1997
)
0.3
" Pharmacokinetic parameters evaluated after administration of single intravenous and oral doses were very similar and the ANOVA analysis did not show any statistically significant differences for t1/2, Cmax, V or AUC (normalised)."( A method using a liquid chromatographic-electrospray-mass spectrometric assay for the determination of antimigraine compounds: preliminary pharmacokinetics of MDL 74,721, sumatriptan and naratriptan, in rabbit.
David, M; Duléry, BD; Huebert, ND; Petty, MA; Schoun, J, 1997
)
0.49
" The elimination half-life (t1/2), approximately 2 h, was unaffected by the magnitude of dose."( Safety, tolerability, and pharmacokinetics of sumatriptan in healthy subjects following ascending single intranasal doses and multiple intranasal doses.
Duquesnoy, C; Fuseau, E; Hussey, EK; Moore, KH; Pakes, GE; Shaw, S, 1997
)
0.56
"Allometric scaling is an empirical examination of the relationships between the pharmacokinetic parameters and size (usually body weight), but it can also involve brain weight for metabolized drug."( Mixed effect modeling of sumatriptan pharmacokinetics during drug development. I: Interspecies allometric scaling.
Bye, A; Cosson, VF; Efthymiopoulos, C; Fuseau, E, 1997
)
0.6
" There were no statistical differences between the non-parenteral routes for tmax or Cmax/AUCinfinity."( Comparative clinical pharmacokinetics of single doses of sumatriptan following subcutaneous, oral, rectal and intranasal administration.
Duquesnoy, C; Fuseau, E; Mamet, JP; Sumner, D, 1998
)
0.55
" Many novel antimigraine compounds are in clinical development, yet full characterization of each one's pharmacodynamic behavior is a formidable task due to the difficulty in studying a migraineur during an attack."( The pharmacodynamics of sumatriptan in nitroglycerin-induced headache.
Forrest, A; Fullerton, T; Gengo, FM; Komorowski-Swiatek, D, 1999
)
0.61
" The pharmacokinetic parameters were calculated by using model-independent methods."( Lack of pharmacokinetic interaction between sumatriptan and naproxen.
Rambhau, D; Rao, BR; Rao, YM; Srinivasu, P, 2000
)
0.57
" Pharmacokinetic parameters were calculated using noncompartmental methods."( Chronopharmacokinetics of sumatriptan in healthy human subjects.
Boinpally, RR; Devaraj, R; Poondru, S; Yamasani, MR, 2000
)
0.61
" As expected for a class of compounds developed for affinity at a specific receptor, there are minor pharmacodynamic differences between the triptans."( Triptans in migraine: a comparative review of pharmacology, pharmacokinetics and efficacy.
De Vries, P; Saxena, PR; Tfelt-Hansen, P, 2000
)
0.31
"In the 24 evaluable subjects (12 men, 12 women) included in the pharmacokinetic analysis, mean sumatriptan AUC(infinity) and Cmax values after administration of combination treatment were 9% and 14% higher, respectively, than the corresponding values after administration of sumatriptan alone."( The pharmacokinetics of sumatriptan when administered with clarithromycin in healthy volunteers.
Bye, C; Gray, P; Leese, PT; McNeal, S; Moore, KH; O'Quinn, S; Sale, M, 2002
)
0.84
" However, the possibility of a pharmacokinetic interaction and the safety of this regime have not been examined."( A pharmacokinetic interaction study between butorphanol and sumatriptan nasal sprays in healthy subjects: importance of the timing of butorphanol administration.
Boulton, DW; Nichola, PS; Shyu, WC; Vachharajani, NN, 2002
)
0.56
" The elimination phase half-life is approximately 2 hours, consistent with administration by other routes."( Clinical pharmacokinetics of intranasal sumatriptan.
Barrow, A; Fuseau, E; Ibbotson, T; Moore, KH; Petricoul, O, 2002
)
0.58
" A total of 16 subjects (10 males and 6 females) had pharmacokinetic data that could be analyzed, 2 withdrew from the study 30 and 60 minutes after dosing following the loss of venous access for blood sampling, and a bioanalysis failure resulted in loss of data from 3 subjects."( Pharmacokinetics of sumatriptan nasal spray in adolescents.
Christensen, ML; Fuseau, E; Jabbour, JT; Mottern, RK, 2003
)
0.64
" A comparison is also presented between several methods based on animal pharmacokinetic data, using the same set of proprietary compounds, and it lends further support for the use of this method, as opposed to methods that require the gathering of pharmacokinetic data in laboratory animals."( Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
Gao, F; Lombardo, F; Obach, RS; Shalaeva, MY, 2004
)
0.32
" Pharmacokinetic analysis included both noncompartmental and population modeling methods."( Pharmacokinetics of sumatriptan nasal spray in children.
Christensen, ML; Fuseau, E; Jabbour, JT; Mottern, RK, 2004
)
0.65
" Potential explanations for differences among triptans in the incidence of CNS side-effects may relate to pharmacological and pharmacokinetic differences, including receptor binding, lipophilicity, and the presence of active metabolites."( Triptans and CNS side-effects: pharmacokinetic and metabolic mechanisms.
Dodick, DW; Martin, V, 2004
)
0.32
"This randomized, open-label, 4-way crossover study (n = 32) was conducted to determine whether the new formulation of sumatriptan 50 and 100 mg is bioequivalent to sumatriptan conventional tablets and to compare the pharmacokinetic profiles of the new formulation and the conventional tablet during the early (0-2 h) postdose interval in healthy volunteers."( Pharmacokinetic profile of a new form of sumatriptan tablets in healthy volunteers.
Boswell, D; Bullman, J; Dow, A; Lewis, A; Sidhu, J; Summers, SJ; Walls, C, 2004
)
0.8
" Pharmacokinetic parameters measured early (0-2 h) after dosing reveal slightly faster absorption, on average, of the new sumatriptan formulation than sumatriptan conventional tablets although high intersubject variability was observed."( Pharmacokinetic profile of a new form of sumatriptan tablets in healthy volunteers.
Boswell, D; Bullman, J; Dow, A; Lewis, A; Sidhu, J; Summers, SJ; Walls, C, 2004
)
0.8
" The pharmacokinetics of topiramate are characterised by linear pharmacokinetics over the dose range 100-800 mg, low oral clearance (22-36 mL/min), which, in monotherapy, is predominantly through renal excretion (renal clearance 10-20 mL/min), and a long half-life (19-25 hours), which is reduced when coadministered with inducing AEDs such as phenytoin, phenobarbital and carbamazepine."( Pharmacokinetic interactions of topiramate.
Bialer, M; Curtin, C; Doose, DR; Murthy, B; Schwabe, S; Twyman, RE; Wang, SS, 2004
)
0.32
" The analysis was based on phase I pharmacokinetic naratriptan data, sumatriptan pharmacodynamic data, and naratriptan preclinical (animal) potency information, together with general knowledge as to how migraine affects oral absorption."( Uncertainty analysis in pharmacokinetics and pharmacodynamics: application to naratriptan.
Aarons, L; Gueorguieva, I; Nestorov, IA; Rowland, M, 2005
)
0.56
"A previously developed pharmacokinetic (PK)/pharmacodynamic (PD) model for naratriptan disposition and effect was used."( Uncertainty analysis in pharmacokinetics and pharmacodynamics: application to naratriptan.
Aarons, L; Gueorguieva, I; Nestorov, IA; Rowland, M, 2005
)
0.33
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35
"(1) To determine whether sumatriptan can be absorbed across the oral mucosa, and, if so; then (2) to describe its pharmacokinetics; and (3) to investigate whether there are pharmacodynamic correlates of such pharmacokinetics in patients experiencing migraine attacks."( Rapid oral transmucosal absorption of sumatriptan, and pharmacodynamics in acute migraine.
Bergstrom, D; Cabana, B; Dilone, E; Fox, AW; Nedumpara, M,
)
0.71
" The first, in normal volunteers, compared the pharmacokinetic performance of a lingual spray (LS) formulation of sumatriptan (2 dose sizes, one of which in both the fed and fasted state) with an orthodox 50-mg sumatriptan tablet."( Rapid oral transmucosal absorption of sumatriptan, and pharmacodynamics in acute migraine.
Bergstrom, D; Cabana, B; Dilone, E; Fox, AW; Nedumpara, M,
)
0.61
" sumatriptan on pharmacokinetic grounds."( Subcutaneous sumatriptan pharmacokinetics: delimiting the monoamine oxidase inhibitor effect.
Fox, AW, 2010
)
1.64
"Summary pharmacokinetic data were taken from the literature and from GlaxoSmithKline (GSK) study C92-050."( Subcutaneous sumatriptan pharmacokinetics: delimiting the monoamine oxidase inhibitor effect.
Fox, AW, 2010
)
0.73
"There are no pharmacokinetic grounds to deter co-administration of an MAOI-A and subcutaneous sumatriptan."( Subcutaneous sumatriptan pharmacokinetics: delimiting the monoamine oxidase inhibitor effect.
Fox, AW, 2010
)
0.95
"To describe the pharmacokinetic and safety profiles of sumatriptan 85 mg formulated with RT Technology (RT) and naproxen sodium 500 mg in a fixed-dose combination tablet (sumatriptan/naproxen sodium) that targets both serotonergic dysmodulation and inflammation in migraine."( Distinct pharmacokinetic profile and safety of a fixed-dose tablet of sumatriptan and naproxen sodium for the acute treatment of migraine.
Haberer, LJ; Lener, SE; McDonald, SA; Taylor, DR; Walls, CM, 2010
)
0.84
" The pharmacokinetics of 2 sumatriptan/naproxen sodium tablets administered 2 hours apart were consistent with the pharmacokinetic predictions from a single dose of the combination tablet."( Distinct pharmacokinetic profile and safety of a fixed-dose tablet of sumatriptan and naproxen sodium for the acute treatment of migraine.
Haberer, LJ; Lener, SE; McDonald, SA; Taylor, DR; Walls, CM, 2010
)
0.89
"The combination tablet of sumatriptan/naproxen sodium has unique pharmacokinetic properties."( Distinct pharmacokinetic profile and safety of a fixed-dose tablet of sumatriptan and naproxen sodium for the acute treatment of migraine.
Haberer, LJ; Lener, SE; McDonald, SA; Taylor, DR; Walls, CM, 2010
)
0.89
" Blood samples for pharmacokinetic assessment were collected up to 14 hours after the administration of the first dose."( Pharmacokinetics and tolerability of sumatriptan after single-dose administration of a fixed-dose combination tablet of sumatriptan/naproxen sodium 85/500 mg followed two hours later by subcutaneous sumatriptan 4- or 6-mg injection: a randomized, open-lab
Berges, A; Lener, SE; McDonald, SA; Walls, C, 2010
)
0.63
" With S/N + S4, sumatriptan Cmax and AUC(0-14) did not exceed those with S100 + S100."( Pharmacokinetics and tolerability of sumatriptan after single-dose administration of a fixed-dose combination tablet of sumatriptan/naproxen sodium 85/500 mg followed two hours later by subcutaneous sumatriptan 4- or 6-mg injection: a randomized, open-lab
Berges, A; Lener, SE; McDonald, SA; Walls, C, 2010
)
0.98
" Pharmacologically, pharmacokinetic parameters, in particular bioavailability, T(max) and C(max) are responsible for the wide efficacy of the compound and the limited adverse effect (AE) profile."( Sumatriptan succinate : pharmacokinetics of different formulations in clinical practice.
Casolla, B; Lionetto, L; Martelletti, P; Negro, A; Simmaco, M, 2012
)
1.82
" This method was successfully applied to a pharmacokinetic study conducted with 10 healthy volunteers."( Rapid determination of sumatriptan in human plasma by ultra performance liquid chromatography-tandem mass spectrometry and its application to clinical pharmacokinetic study.
Bae, MH; Lee, HW; Lee, J; Lim, MS; Park, J; Park, SM; Seo, JJ; Seong, SJ; Yoon, YR, 2013
)
0.7
"The purpose of this study was to directly compare the pharmacokinetic (PK) profile of 22-mg sumatriptan powder delivered intranasally with a novel Breath Powered™ device (11 mg in each nostril) vs a 20-mg sumatriptan liquid nasal spray, a 100-mg oral tablet, and a 6-mg subcutaneous injection."( Improved pharmacokinetics of sumatriptan with Breath Powered™ nasal delivery of sumatriptan powder.
Carothers, J; Djupesland, PG; Mahmoud, RA; Messina, J; Obaidi, M; Offman, E, 2013
)
0.9
" However, the many formulations available are characterized by differences in the pharmacokinetic profile that could affect therapy effectiveness."( Pharmacokinetics and safety of a new aspirin formulation for the acute treatment of primary headaches.
D'Alonzo, L; Lecchi, M; Martelletti, P; Negro, A, 2014
)
0.4
"Limited pharmacokinetic sampling strategy may be useful for predicting the area under the curve (AUC) for triptans and may have clinical utility as a prospective tool for prediction."( Intranasal Pharmacokinetic Data for Triptans Such as Sumatriptan and Zolmitriptan Can Render Area Under the Curve (AUC) Predictions for the Oral Route: Strategy Development and Application.
Srinivas, NR; Syed, M, 2016
)
0.68
" The validated method was successfully applied to a pharmacokinetic study with simultaneous administration of naproxen sodium and sumatriptan succinate tablet formulations in healthy volunteers."( Development and validation of an LC-ESI-MS/MS method for the simultaneous quantification of naproxen and sumatriptan in human plasma: application to a pharmacokinetic study.
Bellorio, KB; Brêtas, CM; Brêtas, JM; César, IC; Mundim, IM; Pianetti, GA; Teixeira, Lde S, 2016
)
0.85
" Blood samples for pharmacokinetic profiling of sumatriptan were obtained prior to dosing and at predetermined time points covering the 12 hours postonset of treatment."( A Phase I, Open-Label, Single-Dose Safety, Pharmacokinetic, and Tolerability Study of the Sumatriptan Iontophoretic Transdermal System in Adolescent Migraine Patients.
Aycardi, E; Bigal, ME; Chitra, R; Gutman, D; Hellriegel, E; Kansagra, S; Kidron, OS; Knebel, H; Kunta, J; Linder, S; Ma, Y; Pierce, M; Spiegelstein, O; Winner, PK, 2016
)
0.91
" Cmax , tmax , AUC0-∞ , and t½ values were all similar between male and female patients and between younger (12-14 years) and older (15-17 years) adolescents."( A Phase I, Open-Label, Single-Dose Safety, Pharmacokinetic, and Tolerability Study of the Sumatriptan Iontophoretic Transdermal System in Adolescent Migraine Patients.
Aycardi, E; Bigal, ME; Chitra, R; Gutman, D; Hellriegel, E; Kansagra, S; Kidron, OS; Knebel, H; Kunta, J; Linder, S; Ma, Y; Pierce, M; Spiegelstein, O; Winner, PK, 2016
)
0.66
"To evaluate the potential for pharmacokinetic interaction and the safety and tolerability when ubrogepant and sumatriptan are coadministered in a Phase 1 study in healthy participants, and to inform the safety and tolerability of ubrogepant alone and in combination with triptans in Phase 3 trials in participants with migraine."( Evaluation of the Pharmacokinetic Interaction of Ubrogepant Coadministered With Sumatriptan and of the Safety of Ubrogepant With Triptans.
Boinpally, R; Butler, M; Jakate, A; Lu, K; McGeeney, D; Periclou, A, 2020
)
1
"The Phase 1 study was a single-center, open-label, randomized, 3-way crossover, single-dose, pharmacokinetic interaction study, where participants received each of 3 oral treatments with a 7-day washout period between treatments: single dose of ubrogepant 100 mg, single dose of sumatriptan 100 mg, and ubrogepant 100 mg plus sumatriptan 100 mg."( Evaluation of the Pharmacokinetic Interaction of Ubrogepant Coadministered With Sumatriptan and of the Safety of Ubrogepant With Triptans.
Boinpally, R; Butler, M; Jakate, A; Lu, K; McGeeney, D; Periclou, A, 2020
)
0.96
"Although there were slight alterations in ubrogepant pharmacokinetic parameters when coadministered with sumatriptan, such changes are expected to have minimal clinical relevance, especially because no changes were seen in sumatriptan area under the curve and maximum plasma concentration when coadministered with ubrogepant."( Evaluation of the Pharmacokinetic Interaction of Ubrogepant Coadministered With Sumatriptan and of the Safety of Ubrogepant With Triptans.
Boinpally, R; Butler, M; Jakate, A; Lu, K; McGeeney, D; Periclou, A, 2020
)
1
" Pharmacokinetic evaluations were also performed during an in-vivo study on Sprague-Dawley rats and neuropharmacokinetic parameters such as drug targeting efficiency (DTE) and direct transport percentage (DTP) were calculated."( Nose-to-brain delivery of sumatriptan-loaded nanostructured lipid carriers: preparation, optimization, characterization and pharmacokinetic evaluation.
Azadi, A; Heidari, R; Masjedi, M; Mohammadi-Samani, S, 2020
)
0.86

Compound-Compound Interactions

The extent of absorption of sumatriptan was similar after oral administration alone and in combination with clarithromycin dosed to steady state. Nonsteroidal anti-inflammatory drugs (NSAID) such as tolfenamic acid and naproxen sodium have demonstrated efficacy in reducing recurrence observed with the single use of this drug.

ExcerptReferenceRelevance
" Drug-drug interactions are further implicated through this study."( Cerebral blood flow effects of sumatriptan in drug combinations in the baboon model.
Dormehl, IC; Hugo, N; Oliver, DW, 1995
)
0.58
" This study analyzed the ability of ergotamine, dihydroergotamine, and 5-HT and sumatriptan to interact with the four known human 5-HT1 receptor subtypes."( Wolff Award presentation 1993. Anti-migraine drug interactions with cloned human 5-hydroxytryptamine1 receptor subtypes.
Havlik, S; Oksenberg, D; Peroutka, SJ,
)
0.36
" This article details those medications that may interact significantly with the SSRIs, and provides clinical guidelines for minimising the likelihood of such complications."( Drug interactions of clinical significance with selective serotonin reuptake inhibitors.
Mitchell, PB, 1997
)
0.3
" Nonsteroidal anti-inflammatory drugs (NSAID) such as tolfenamic acid and naproxen sodium combined with sumatriptan have demonstrated efficacy in reducing recurrence observed with the single use of this drug."( Dexamethasone decreases migraine recurrence observed after treatment with a triptan combined with a nonsteroidal anti-inflammatory drug.
Barbosa, JS; Krymchantowski, AV, 2001
)
0.53
"The extent of absorption of sumatriptan was similar after oral administration alone and in combination with clarithromycin dosed to steady state."( The pharmacokinetics of sumatriptan when administered with clarithromycin in healthy volunteers.
Bye, C; Gray, P; Leese, PT; McNeal, S; Moore, KH; O'Quinn, S; Sale, M, 2002
)
0.92
" The efficacy of indomethacin, alone and combined with prochlorperazine and caffeine, in abolishing peripheral and central sensitization in in vivo models of hyperalgesia is a further explanation of the clinical efficacy of IndoProCaf in the treatment of migraine."( Indomethacin, alone and combined with prochlorperazine and caffeine, but not sumatriptan, abolishes peripheral and central sensitization in in vivo models of migraine.
Galeotti, N; Ghelardini, C; Grazioli, I; Uslenghi, C, 2004
)
0.55
"The authors present a 14-year-old girl with 18q- syndrome combined with cyclic vomiting syndrome."( Successful treatment with sumatriptan in a case with cyclic vomiting syndrome combined with 18q- syndrome.
Haginoya, K; Hirose, M; Kakisaka, Y; Munakata, M; Sato, I; Sato, T; Tsuchiya, S; Uematsu, M; Wakusawa, K, 2009
)
0.65
" These data suggest a mechanism of medication overuse headache by which migraine medications combined with repeated episodes of pain may amplify the consequences of nociceptor activation and increase the probability of future migraine attacks as well as risk of medication overuse headache."( Sustained exposure to acute migraine medications combined with repeated noxious stimulation dysregulates descending pain modulatory circuits: Relevance to medication overuse headache.
Dodick, DW; Nation, KM; Navratilova, E; Porreca, F, 2019
)
0.51
"To evaluate the potential for pharmacokinetic interaction and the safety and tolerability when ubrogepant and sumatriptan are coadministered in a Phase 1 study in healthy participants, and to inform the safety and tolerability of ubrogepant alone and in combination with triptans in Phase 3 trials in participants with migraine."( Evaluation of the Pharmacokinetic Interaction of Ubrogepant Coadministered With Sumatriptan and of the Safety of Ubrogepant With Triptans.
Boinpally, R; Butler, M; Jakate, A; Lu, K; McGeeney, D; Periclou, A, 2020
)
1

Bioavailability

Sumatriptan succinate has oral bioavailability of 15% and undergoes hepatic metabolism, hence it is suitable for nasal administration. Compared to sum atriptan, the second-generation triptans have a higher oral bio availability and longer plasma half-life.

ExcerptReferenceRelevance
" Its subcutaneous bioavailability approaches 100%, and its mean terminal half-life is two hours."( Sumatriptan: a new drug for vascular headache.
Hsu, VD, 1992
)
1.73
" Bioavailability was nearly 100% after subcutaneous administration and averaged 14% after oral administration."( The clinical pharmacology, pharmacokinetics and metabolism of sumatriptan.
Baber, NS; Fowler, PA; Keene, ON; Lacey, LF; Tanner, RJ; Thomas, M, 1991
)
0.52
" The bioavailability is greater than 54% in dog, but lower in rat."( The kinetics of 14C-GR43175 in rat and dog.
Dallas, FA; Dixon, CM; McCulloch, RJ; Saynor, DA, 1989
)
0.28
" The drug was rapidly absorbed after oral dosing and had a mean absolute bioavailability of 14% due at least in part to first-pass metabolism."( Early studies with the novel 5-HT 1-like agonist GR43175 in healthy volunteers.
Andrew, P; Dallas, FA; Fowler, PA; Lacey, LF; Thomas, M, 1989
)
0.28
"Sumatriptan exhibits low oral bioavailability partly due to presystemic metabolism, which may vary with regional differences in metabolic activity throughout the gastrointestinal tract."( Sumatriptan absorption from different regions of the human gastrointestinal tract.
Brouwer, KL; Davis, IM; Donn, KH; Dukes, GE; Heizer, WD; Hussey, EK; Powell, JR; Warner, PE, 1995
)
3.18
" The objective of this work was to identify potent and selective 5-HT1D receptor agonists with high oral bioavailability and low central nervous system penetration."( Synthesis and serotonergic activity of N,N-dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethylamine and analogues: potent agonists for 5-HT1D receptors.
Baker, R; Beer, MS; Davey, WB; Guiblin, AR; Jelley, RA; Reeve, AJ; Routledge, H; Sternfeld, F; Street, LJ; Watt, AP, 1995
)
0.29
" The mean subcutaneous bioavailability is 96% compared to 14% for the oral tablet."( Single dose pharmacokinetics of sumatriptan in healthy volunteers.
Fowler, PA; Hussey, EK; Lacey, LF, 1995
)
0.57
" Bioavailability is high (96%) following subcutaneous injection, but low (14%) following oral administration because of first-pass metabolism."( Sumatriptan clinical pharmacokinetics.
Scott, AK, 1994
)
1.73
" Both 8d,k were found to be well absorbed in the rat with oral bioavailabilities of 66% and 62%, respectively."( Synthesis and biological activity of 3-[2-(dimethylamino)ethyl]-5-[(1,1-dioxo-5-methyl-1,2,5-thiadiazolidin- 2-yl)-methyl]-1H-indole and analogues: agonists for the 5-HT1D receptor.
Baker, R; Beer, MS; Castro, JL; Guiblin, AR; Hargreaves, RJ; Hobbs, SC; Jenkins, MR; Russell, MG; Scholey, K; Stanton, JA, 1994
)
0.29
" dose both probably due to extensive and rapid metabolism of the parent drugs as suggested by the low values for bioavailability (range 13."( A method using a liquid chromatographic-electrospray-mass spectrometric assay for the determination of antimigraine compounds: preliminary pharmacokinetics of MDL 74,721, sumatriptan and naratriptan, in rabbit.
David, M; Duléry, BD; Huebert, ND; Petty, MA; Schoun, J, 1997
)
0.49
" In conscious rats and dogs, naratriptan has high oral bioavailability (71% and 95%, respectively)."( Naratriptan: biological profile in animal models relevant to migraine.
Beattie, DT; Connor, HE; Feniuk, W; Humphrey, PP; North, PC; Oxford, AW; Saynor, DA, 1997
)
0.3
" The overall bioavailability of sumatriptan was 40-50%."( off absorption, pharmacodynamics, metabolism and excretion of 14C-sumatriptan following intranasal administration to the beagle dog.
Barrow, A; Dixon, CM; Perren, MJ; Saynor, DA; Smith, I; Stowe, R, 1997
)
0.82
" A higher lipophilicity explains (except for alniditan) their greater oral bioavailability and better central nervous system penetration."( Acute migraine therapy: the newer drugs.
Schoenen, J, 1997
)
0.3
"To cater to the special situation of much reduced oral bioavailability which occurs in severe migraine attacks with pronounced nausea and vomiting, sumatriptan can also be used in a subcutaneous form that can be self-administered."( Practicability and acceptance of subcutaneous self-administration of the selective serotonin agonist sumatriptan.
Baar, H; Beckmann-Reinhold, A; Beiküfner, HD; Böhme, K; Göbel, H, 1998
)
0.72
" Usual absorption parameters were described and the rate of absorption was assessed using deconvolution technics."( Comparative clinical pharmacokinetics of single doses of sumatriptan following subcutaneous, oral, rectal and intranasal administration.
Duquesnoy, C; Fuseau, E; Mamet, JP; Sumner, D, 1998
)
0.55
"Zolmitriptan (previously known as 311C90) is a serotoninergic 5-HT1B/D agonist with high oral bioavailability with a double, central and peripheral, action mechanism."( [Clinical efficacy of zolmitriptan in migraine].
Leira, R; Noya, M, 1998
)
0.3
" The optimum compound was 1-(3-[5-(1,2, 4-triazol-4-yl)-1H-indol-3-yl]propyl)-4-(2-(3-fluorophenyl)ethyl)p ipe razine (7f) which has excellent selectivity for h5-HT1D receptors over other 5-HT receptor subtypes and good oral bioavailability in three species."( 3-(Piperazinylpropyl)indoles: selective, orally bioavailable h5-HT1D receptor agonists as potential antimigraine agents.
Beer, MS; Chambers, MS; Goodacre, S; Hobbs, SC; Hunt, P; Jelley, RA; MacLeod, AM; Matassa, VG; Rathbone, D; Reeve, AJ; Stanton, JA; Sternfeld, F; Street, LJ; Watt, AP, 1999
)
0.3
" However, while effective, it has low oral bioavailability and some problematic adverse effects."( Acute treatment of migraine attacks: efficacy and safety of a nonsteroidal anti-inflammatory drug, diclofenac-potassium, in comparison to oral sumatriptan and placebo. The Diclofenac-K/Sumatriptan Migraine Study Group.
, 1999
)
0.5
" L-772,405 also shows very good selectivity over a range of other serotonin and nonserotonin receptors and has excellent bioavailability following subcutaneous administration in rats."( 3-[3-(Piperidin-1-yl)propyl]indoles as highly selective h5-HT(1D) receptor agonists.
Beer, MS; Broughton, HB; Castro, JL; Hitzel, L; Matassa, VG; Pengilley, RR; Russell, MG; Sohal, B; Stanton, JA; van Niel, MB; Watt, AP, 1999
)
0.3
"The quantitative structure-bioavailability relationship of 232 structurally diverse drugs was studied to evaluate the feasibility of constructing a predictive model for the human oral bioavailability of prospective new medicinal agents."( QSAR model for drug human oral bioavailability.
Topliss, JG; Yoshida, F, 2000
)
0.31
" 23% bioavailability following oral drug administration."( The effect of SB-236057-A, a selective 5-HT1B receptor inverse agonist, on in vivo extracellular 5-HT levels in the freely-moving guinea-pig.
Austin, NE; Gaster, LM; Hagan, JJ; Hatcher, P; Jeffrey, P; Middlemiss, DN; Roberts, C; Routledge, C; Wyman, P, 2000
)
0.31
" In early clinical trials, rizatriptan was shown to have good bioavailability and favorable effects on quality of life."( Rizatriptan versus usual care in long-term treatment of migraine.
Silberstein, SD, 2000
)
0.31
" Zolmitriptan introduced in 1994 is an agonists of 5-HT 1B/1D receptor, is active both peripherally and centrally, is well absorbed from the digestive tract and has a good bioavailability index /40%/."( [Emergency treatment of migraine attacks with particular reference to agonists of 5-HT1B/1D receptor].
Prusiński, A, 1999
)
0.3
" Sumatriptan has a low oral bioavailability (14%) and all the newer triptans have an improved oral bioavailability and for one, risatriptan, the rate of absorption is faster."( Triptans in migraine: a comparative review of pharmacology, pharmacokinetics and efficacy.
De Vries, P; Saxena, PR; Tfelt-Hansen, P, 2000
)
1.22
" Eletriptan has a rapid and complete oral absorption and a good oral bioavailability in migraineurs."( Pharmacology and efficacy of eletriptan for the treatment of migraine attacks.
Diener, HC; McHarg, A, 2000
)
0.31
" A qualitative model for pharmacokinetic properties was then used to guide the synthesis toward molecules likely to have oral bioavailability in humans."( Discovery of 4-[3-(trans-3-dimethylaminocyclobutyl)-1H-indol-5-ylmethyl]-(4S)-oxazolidin-2-one (4991W93), a 5HT(1B/1D) receptor partial agonist and a potent inhibitor of electrically induced plasma extravasation.
Barrett, V; Brockwell, M; Cambridge, D; Farrant, DR; Foster, C; Giles, H; Glen, RC; Hill, AP; Hobbs, H; Honey, A; Jandu, KS; Martin, GR; Salmon, J; Selwood, DL; Smith, D; Woollard, P, 2001
)
0.31
"Rizatriptan is a potent, oral, 5-HT1B/1D agonist with more rapid absorption and higher bioavailability than oral sumatriptan."( Oral rizatriptan versus oral sumatriptan: a direct comparative study in the acute treatment of migraine. Rizatriptan 030 Study Group.
Block, GA; Giacovazzo, M; Malbecq, W; Paz, J; Reines, SA; Rodriguez, F; Teall, J; Tfelt-Hansen, P; Visser, WH,
)
0.63
" Compared to sumatriptan, the second-generation triptans have a higher oral bioavailability and longer plasma half-life."( An introduction to migraine: from ancient treatment to functional pharmacology and antimigraine therapy.
Centurión, D; De Vries, P; Saxena, PR; Valdivia, LF; Villalón, CM, 2002
)
0.68
"5 h) and rizatriptan has greater bioavailability than sumatriptan (45% versus 15%)."( Rizatriptan: pharmacological differences from sumatriptan and clinical results.
Lines, CR; McCarroll, KA; Visser, WH, 2001
)
0.82
"The potential advantages of eletriptan lie firstly in its lipophilicity reflected as an increased rate of absorption and Tmax compared to sumatriptan."( Eletriptan: pharmacological differences and clinical results.
Giffin, N, 2001
)
0.51
" In adults, intranasal sumatriptan is well absorbed and tolerated."( Pharmacokinetics of sumatriptan nasal spray in adolescents.
Christensen, ML; Fuseau, E; Jabbour, JT; Mottern, RK, 2003
)
0.95
" This compound demonstrated favorable in vitro metabolic stability in human and rat liver microsomes and was found to be orally bioavailable in rats (F(po)=51%)."( Design, synthesis and biological activity of novel dimethyl-[2-[6-substituted-indol-1-yl]-ethyl]-amine as potent, selective, and orally-bioavailable 5-HT(1D) agonists.
Arora, J; Demschyshyn, L; Draper, S; Edwards, L; Harrison, S; Isaac, M; Labrie, P; MacLean, N; Maddaford, S; Naismith, A; O'Brien, A; Papac, D; Slassi, M; Tehim, A; Wang, H; Wilson, J; Xin, T, 2003
)
0.32
"Onset of effect is related to rate of absorption of sumatriptan."( Onset of effect of 5-HT1B/1D agonists: a model with pharmacokinetic validation.
Fox, AW, 2004
)
0.57
" Also, some nasal preparations have significant adverse effects or are not well absorbed and therefore do not work consistently; others are more challenging to administer as a result of their delivery apparatus."( Intranasal medications for the treatment of migraine and cluster headache.
Bigal, ME; Rapoport, AM; Sheftell, FD; Tepper, SJ, 2004
)
0.32
" Compared to sumatriptan, the second-generation triptans have a higher oral bioavailability and longer plasma half-life."( Migraine: pathophysiology, pharmacology, treatment and future trends.
Centurión, D; de Vries, P; Saxena, PR; Valdivia, LF; Villalón, CM, 2003
)
0.69
" Pharmacokinetic parameters and bioavailability of sumatriptan did not seem to be correlated either to the lack of efficacy or the appearance of side effects."( Pharmacokinetics of sumatriptan in non-respondent and in adverse drug reaction reporting migraine patients.
Bertolini, A; Coccia, CP; Ferrari, A; Leone, S; Pinetti, D; Sternieri, E, 2005
)
0.9
" Based on a population pharmacokinetic model, mean concentration-time profiles were generated by varying the absorption rate constant and lag time."( Relevance of absorption rate and lag time to the onset of action in migraine.
Danhof, M; Della Pasqua, OE; Maas, HJ; Spruit, MA, 2008
)
0.35
"Model-based predictions suggest that increases in the absorption rate of the currently marketed oral formulation of sumatriptan result in a gain in the pain-free response that is both clinically and statistically relevant."( Relevance of absorption rate and lag time to the onset of action in migraine.
Danhof, M; Della Pasqua, OE; Maas, HJ; Spruit, MA, 2008
)
0.56
"Sumatriptan is a potent and selective 5-HT(1B) and 5-HT(1D )agonist used in the symptomatic treatment of migraine; it shows poor oral bioavailability ascribed, in part, to its low lipophilicity."( Unanticipated acyloxymethylation of sumatriptan indole nitrogen atom and its implications in prodrug design.
Guedes, RC; Iley, J; Lopes, F; Moreira, R; Rodrigues, T, 2008
)
2.06
"The absolute bioavailability of subcutaneous (s."( Subcutaneous sumatriptan pharmacokinetics: delimiting the monoamine oxidase inhibitor effect.
Fox, AW, 2010
)
0.73
"Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall elimination (Fg), and fraction escaping hepatic elimination (Fh)."( Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
Chang, G; El-Kattan, A; Miller, HR; Obach, RS; Rotter, C; Steyn, SJ; Troutman, MD; Varma, MV, 2010
)
0.36
" In addition, food had no significant effect on the bioavailability of naproxen or sumatriptan after administration of sumatriptan/naproxen sodium but slightly delayed the time to peak plasma concentration of sumatriptan by approximately 40 minutes."( Distinct pharmacokinetic profile and safety of a fixed-dose tablet of sumatriptan and naproxen sodium for the acute treatment of migraine.
Haberer, LJ; Lener, SE; McDonald, SA; Taylor, DR; Walls, CM, 2010
)
0.82
" For oral formulations, these limitations include difficulty in taking an oral medication due to the nausea and vomiting that often accompany migraine, and inconsistent absorption, whereas nasal and subcutaneous formulations may be associated with low bioavailability and an undesirable rate of adverse events, respectively."( Transdermal delivery of sumatriptan for the treatment of acute migraine.
Pierce, MW, 2010
)
0.67
" Migraine-associated gastroparesis can impair absorption and reduce bioavailability of oral migraine medications and thereby reduce and delay therapeutic efficacy."( Twelve-month tolerability and efficacy study of NP101, the sumatriptan iontophoretic transdermal system.
Goldstein, J; Pierce, MW; Pugach, N; Silberstein, S; Singer, R; Smith, TR, 2012
)
0.62
" The new drug formulations that are the most similar to the pharmacokinetics parameters of the subcutaneous one are promising because they both improve pharmacokinetic bioavailability bypassing the first-pass metabolism and increase patient compliance."( Sumatriptan succinate : pharmacokinetics of different formulations in clinical practice.
Casolla, B; Lionetto, L; Martelletti, P; Negro, A; Simmaco, M, 2012
)
1.82
" BMS-742413 has good intranasal bioavailability in the rabbit and shows a robust, dose-dependent inhibition of CGRP-induced increases in marmoset facial blood flow."( Discovery of (R)-N-(3-(7-methyl-1H-indazol-5-yl)-1-(4-(1-methylpiperidin-4-yl)-1-oxopropan-2-yl)-4-(2-oxo-1,2-dihydroquinolin-3-yl)piperidine-1-carboxamide (BMS-742413): a potent human CGRP antagonist with superior safety profile for the treatment of migr
Cantor, GH; Chaturvedula, PV; Conway, CM; Davis, C; Denton, R; Dubowchik, GM; Keavy, D; Macci, R; Macor, JE; Mathias, N; Mercer, SE; Moench, P; Pin, SS; Schartman, R; Signor, L; Thalody, G; Whiterock, V; Xu, C, 2013
)
0.39
"An open-label, cross-over, comparative bioavailability study was conducted in 20 healthy subjects at a single center in the USA."( Improved pharmacokinetics of sumatriptan with Breath Powered™ nasal delivery of sumatriptan powder.
Carothers, J; Djupesland, PG; Mahmoud, RA; Messina, J; Obaidi, M; Offman, E, 2013
)
0.68
" Sumatriptan succinate has oral bioavailability of 15% and undergoes hepatic metabolism, hence it is suitable for nasal administration."( Development of in situ gel for nasal delivery: design, optimization, in vitro and in vivo evaluation.
Chaudhari, PD; Galgatte, UC; Kumbhar, AB, 2014
)
1.31
"The objective of the investigation was to develop a mucoadhesive in situ gel to improve the bioavailability of the sumatriptan succinate."( Development of in situ gel for nasal delivery: design, optimization, in vitro and in vivo evaluation.
Chaudhari, PD; Galgatte, UC; Kumbhar, AB, 2014
)
0.61
"5% poloxamer 188 group, with absolute bioavailability 29."( Non-ionic surfactants as novel intranasal absorption enhancers: in vitro and in vivo characterization.
Ding, J; Li, J; Li, Y; Mao, S; Zhang, X, 2016
)
0.43
" Intranasal sumatriptan is well absorbed and is generally effective in relieving headache."( Effects of sumatriptan nasal spray (Imigran) on isolated rat's tracheal smooth muscle.
Chang, YN; Cheng, LH; Chiu, FS; Chu, YH; Liu, SC; Wang, HW; Wu, PC, 2015
)
1.19
"Sumatriptan succinate (SS) is a 5-HT1 receptor agonist used in the treatment of migraine having poor bioavailability (15%) due to its extensive first-pass effect."( Sumatriptan succinate sublingual fast dissolving thin films: formulation and in vitro/in vivo evaluation.
Abou Ghaly, MH; Amin, MM; El Nabarawi, MA; Tayel, SA, 2016
)
3.32
" Absorption of SS delivered by MNs was similar to that observed after subcutaneous injection and was associated with high bioavailability (ca."( Improvement of transdermal delivery of sumatriptan succinate using a novel self-dissolving microneedle array fabricated from sodium hyaluronate in rats.
Kamiyama, F; Katsumi, H; Kusamori, K; Quan, YS; Sakane, T; Wu, D; Yamamoto, A, 2015
)
0.69
" The intestinal absorption rate for each drug was acquired by deconvolution, using historical intravenous data as reference, and used with the intestinal surface area and the dose remaining in the lumen to estimate the Peff."( Human in vivo regional intestinal permeability: quantitation using site-specific drug absorption data.
Dahlgren, D; Lennernäs, H; Roos, C; Sjögren, E, 2015
)
0.42
"The low bioavailability of the anti-migraine drug sumatriptan is partially caused by first-pass hepatic metabolism."( OCT1 mediates hepatic uptake of sumatriptan and loss-of-function OCT1 polymorphisms affect sumatriptan pharmacokinetics.
Abu Abed, M; Brockmöller, J; Dos Santos Pereira, JN; Faltraco, F; Knoch, T; Kuron, D; Matthaei, J; Prukop, T; Tzvetkov, MV, 2016
)
0.97
"Available formulations of sumatriptan succinate (SS) have low bioavailability or are associated with site reactions."( Permeation of sumatriptan succinate across human skin using multiple types of self-dissolving microneedle arrays fabricated from sodium hyaluronate.
Kamiyama, F; Katsumi, H; Kusamori, K; Quan, YS; Sakane, T; Wu, D; Yamamoto, A, 2016
)
1.1
"Sumatriptan succinate (SS) is a selective serotonin receptor agonist used for the treatment of migraine attacks, suffering from extensive first-pass metabolism and low oral bioavailability (∼14%)."( Comparative Study Between Different Ready-Made Orally Disintegrating Platforms for the Formulation of Sumatriptan Succinate Sublingual Tablets.
AbouGhaly, MH; Amin, MM; El Nabarawi, MA; Tayel, SA, 2017
)
2.11
" Rapid rate of absorption is suggested to be important for optimal efficacy."( A multicenter, open-label, long-term safety and tolerability study of DFN-02, an intranasal spray of sumatriptan 10 mg plus permeation enhancer DDM, for the acute treatment of episodic migraine.
Allenby, K; Brand-Schieber, E; Cady, RK; Munjal, S; Rapoport, AM; Spierings, ELH, 2017
)
0.67
"Nanoformulations in the past few decades have gained tremendous attention owing to their affirmative applications in increasing the bioavailability of poorly soluble drugs."( Preparation and Characterization of Micelles.
Jain, RD; Patravale, VB; Upadhaya, PG, 2019
)
0.51
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
" SUT bioavailability is low (15%) when it is taken orally owing to its gastric breakdown and bloodstream before reaching the target arteries."( Development and Evaluation of in-situ Nasal Gel Formulations of Nanosized Transferosomal Sumatriptan: Design, Optimization, in vitro and in vivo Evaluation.
Ali Hasan, O; El Sisi, AM; Eleraky, NE; Omar, MM, 2019
)
0.74
"The aim of the study was to enhance SUT bioavailability through developing an intranasal transferosomal mucoadhesive gel."( Development and Evaluation of in-situ Nasal Gel Formulations of Nanosized Transferosomal Sumatriptan: Design, Optimization, in vitro and in vivo Evaluation.
Ali Hasan, O; El Sisi, AM; Eleraky, NE; Omar, MM, 2019
)
0.74
"Based on enhancing the bioavailability and sustaining the drug release, it can be concluded that the in-situ gel of SUT-loaded nano-transferosomes were developed as a promising non-invasive drug delivery system for treating migraine."( Development and Evaluation of in-situ Nasal Gel Formulations of Nanosized Transferosomal Sumatriptan: Design, Optimization, in vitro and in vivo Evaluation.
Ali Hasan, O; El Sisi, AM; Eleraky, NE; Omar, MM, 2019
)
0.74
" The bioavailability of conventional nasal liquids is low due to the deposition of a large fraction of the delivered dose of a drug in the nasal cavity."( Harnessing Intranasal Delivery Systems of Sumatriptan for the Treatment of Migraine.
Akhtari, J; Asadi, P; Assadpour, S; Sahebkar, A; Shiran, MR, 2022
)
0.99
" Sumatriptan belongs to a BCS class III, which exhibits poor oral bioavailability and several side-effects."( Intranasal drug delivery of sumatriptan succinate-loaded polymeric solid lipid nanoparticles for brain targeting.
Dewangan, HK; Shah, K; Yadav, RK, 2022
)
1.93
" In vivo pharmacokinetic study demonstrated improved brain bioavailability of SUT-NEsG as compared to orally administered sumatriptan solution (SUT-SL)."( Quality by design for sumatriptan loaded nano-ethosomal mucoadhesive gel for the therapeutic management of nitroglycerin induced migraine.
Alharbi, HM; Almari, AH; Batool, S; Din, FU; Fatease, AA; Lahiq, AA; Shafique, U; Sohail, S, 2023
)
1.43

Dosage Studied

Sumatriptan tablets provided significantly more effective pain relief compared with placebo as early as 20 minutes after dosing. Pre-incubation with L-NNA abolished the sumatriptAn-induced dilation and significantly shifted the dose-response of the constriction curve to the left.

ExcerptRelevanceReference
" In the published clinical trials of the oral and subcutaneous dosage forms to date, sumatriptan was effective in reducing headache severity from moderate/severe to mild/absent in approximately 70-80 percent of patients treated with active drug, compared with only 20-30 percent in the placebo groups, and 48 percent in the oral ergotamine tartrate/caffeine (Cafergot)-treated group."( Sumatriptan: a selective 5-hydroxytryptamine receptor agonist for the acute treatment of migraine.
Fullerton, T; Gengo, FM, 1992
)
1.95
" Based on this study, a simple, rapid and sensitive voltammetric method was developed for the determination of the drug in a tablet dosage form."( Differential pulse voltammetric determination of sumatriptan succinate (1:1) in a tablet dosage form.
Fernandez Alvarez, JM; Hua, C; Munden, R; Sagar, K; Smyth, MR, 1992
)
0.54
"The results of the very first large-scale placebo-controlled dose-response trial with the novel selective 5-hydroxytryptamine1-like (5HT1-like) receptor agonist sumatriptan are presented."( Treatment of migraine attacks with subcutaneous sumatriptan: first placebo-controlled study. The Subcutaneous Sumatriptan International Study Group.
Bayliss, EM; Ferrari, MD; Ludlow, S; Pilgrim, AJ; Visser, WH, 1992
)
0.74
" Headache relief rates showed an approximate dose-response relationship and at 1 hour were as follows: placebo, 24%; 1 mg, 43%; 2 mg, 57%; 3 mg, 57%; 4 mg, 50%; 6 mg, 73%; and 8 mg, 80%."( Dose ranging efficacy and safety of subcutaneous sumatriptan in the acute treatment of migraine. US Sumatriptan Research Group.
Couch, J; Dexter, J; Flamenbaum, W; Goldstein, J; Mathew, NT; Rapoport, A; Saper, J; Sheftell, F; Silberstein, S; Solomon, S, 1992
)
0.54
" In contrast, morphine (the positive control) produced expected dose-response relationships on measures of reinforcing and physiologic effects."( Psychoactivity and abuse potential of sumatriptan.
Busch, M; Jasinski, DR; Preston, KL; Sullivan, JT; Testa, MP, 1992
)
0.55
"The role of serotonin in the pathogenesis of migraine is discussed, and the chemistry, pharmacology, pharmacokinetics, efficacy, adverse effects, and dosage and administration of sumatriptan are reviewed."( Sumatriptan: a new drug for vascular headache.
Hsu, VD, 1992
)
1.92
" No findings of toxicological significance were observed in rats and dogs after chronic dosing for 1 year or more."( Preclinical studies on the anti-migraine drug, sumatriptan.
Feniuk, W; Humphrey, PP; Jackson, MR; Marriott, AS; Tanner, RJ; Tucker, ML, 1991
)
0.54
" The effect of twice-daily dosing with propranolol on the pharmacokinetics and pharmacodynamics of a single oral dose of sumatriptan was investigated in 10 healthy male subjects."( Lack of an interaction between propranolol and sumatriptan.
Breckenridge, AM; Fowler, PA; Lacey, LF; Scott, AK; Walley, T, 1991
)
0.75
" Rats and dogs were dosed intravenously (iv) and orally (po) with 1 mg 14C-GR43175 base (as succinate salt)/kg bodyweight."( The kinetics of 14C-GR43175 in rat and dog.
Dallas, FA; Dixon, CM; McCulloch, RJ; Saynor, DA, 1989
)
0.28
" The drug was rapidly absorbed after oral dosing and had a mean absolute bioavailability of 14% due at least in part to first-pass metabolism."( Early studies with the novel 5-HT 1-like agonist GR43175 in healthy volunteers.
Andrew, P; Dallas, FA; Fowler, PA; Lacey, LF; Thomas, M, 1989
)
0.28
" Dosing should be individualized according to the needs of the patient."( Oral sumatriptan for the acute treatment of migraine: evaluation of three dosage strengths.
Clements, B; Cutler, N; Davis, R; Mushet, GR; Whitcher, L, 1995
)
0.81
" Moreover, the products are currently marketed in different dosage forms--intramuscular for DHE and subcutaneous for sumatriptan."( A literature review comparing the economic, clinical, and humanistic attributes of dihydroergotamine and sumatriptan.
Kozma, CM; Lawrence, BJ; Mauch, RP; Reeder, CE,
)
0.55
" Following oral dosing up to 400 mg, the pharmacokinetics are also linear, with the exception of rate of absorption, as indicated by a dose dependent increase in time to peak concentration."( Single dose pharmacokinetics of sumatriptan in healthy volunteers.
Fowler, PA; Hussey, EK; Lacey, LF, 1995
)
0.57
"Although sumatriptan has proven effective in treating migraine symptoms, there have been no studies comparing this drug with non-steroid anti-inflammatory drugs (NSAIDs) and ergotamine compounds under ideal dosage and delivery conditions."( [Clinical experience with sumatriptan ++ in the treatment of migraine symptoms].
Pascual, J,
)
0.85
" Patients whose headache was completely resolved 90 minutes after subcutaneous dosing received either oral sumatriptan or placebo at the onset of recurrent headache."( Oral sumatriptan in the treatment of recurrent headache.
Cady, RK; Crummett, D; Littlejohn, TW; Rubino, J, 1994
)
1.02
" New medications, such as sumatriptan, and new dosage forms of older medications, including dihydroergotamine, NSAIDs, and phenothiazines are available to treat acute attacks."( Therapeutic advances in migraine.
Solomon, GD, 1993
)
0.59
" The recommended dosage of sumatriptan at the onset of migraine symptoms is 100 mg orally or 6 mg subcutaneously."( Migraine and cluster headache--their management with sumatriptan: a critical review of the current clinical experience.
Diener, HC; Pfaffenrath, V; Schoenen, J; Steiner, TJ; Wilkinson, M, 1995
)
0.84
" The patients described had a high frequency of attacks (more than two per day); therefore, far higher dosage of the drug was taken than commonly used in cluster headache."( Use of high sumatriptan dosages during episodic cluster headache: three clinical cases.
Albano, O; Attolini, E; Bassi, A; Cassiano, MA; Cavazzuti, L; Centonze, V; Polito, BM; Ricchhetti, G; Sabbà, C, 1996
)
0.67
" Clinical disability scores 120 minutes after dosing showed that 75% and 85% of sumatriptan-treated patients, compared with 30% and 42% of placebo-treated patients, were normal or only mildly impaired (a statistically significant difference)."( Efficacy and tolerability of subcutaneous sumatriptan administered using the IMITREX STATdose System.
Baker, CC; Cady, RK; Clements, B; Davis, R; Gutterman, DL; Mushet, GR,
)
0.62
"The proportion of patients whose conditions improved from severe or moderate headache immediately before dosing to mild or no headache at 2 hours after drug administration (ie, headache relief)."( Rizatriptan vs sumatriptan in the acute treatment of migraine. A placebo-controlled, dose-ranging study. Dutch/US Rizatriptan Study Group.
Ferrari, MD; Jiang, K; Lines, CR; Reines, SA; Terwindt, GM; Visser, WH, 1996
)
0.65
"2 mumol/kg), GR-127,935 right-shifted the dose-response curve of sumatriptan."( The 5-HT1D receptor antagonist GR-127,935 prevents inhibitory effects of sumatriptan but not CP-122,288 and 5-CT on neurogenic plasma extravasation within guinea pig dura mater.
Cutrer, FM; Moskowitz, MA; Waeber, C; Yu, XJ, 1997
)
0.77
" The two dosing periods were separated by 3 to 14 days."( Safety, tolerability, and pharmacokinetics of sumatriptan in healthy subjects following ascending single intranasal doses and multiple intranasal doses.
Duquesnoy, C; Fuseau, E; Hussey, EK; Moore, KH; Pakes, GE; Shaw, S, 1997
)
0.56
"9 h after intravenous or intranasal dosage respectively."( off absorption, pharmacodynamics, metabolism and excretion of 14C-sumatriptan following intranasal administration to the beagle dog.
Barrow, A; Dixon, CM; Perren, MJ; Saynor, DA; Smith, I; Stowe, R, 1997
)
0.53
"5 mg dose was on the shoulder of the dose-response curve (2-h headache response rate 64%), showing similar efficacy to the 5 mg dose (67%)."( Zolmitriptan (Zomig, 311C90), a novel dual central and peripheral 5HT1B/1D agonist: an overview of efficacy.
Sawyer, J; Schoenen, J, 1997
)
0.3
" These findings suggest that the leftward shift of the dose-response curve for 5-HT, which plays an important role in the pathogenesis of coronary spasm, is mediated by activation of 5-HT1Dbeta receptor."( 5-HT1Dbeta receptor mediates the supersensitivity of isolated coronary artery to serotonin in variant angina.
Akita, H; Hirata, K; Ishida, T; Kanazawa, K; Kawashima, S; Sakoda, T; Yokoyama, M, 1998
)
0.3
"5 mg or 25 mg) or placebo at home for the treatment of a moderate or severe migraine attack and those who experienced headache recurrence within 24 hours of dosing had the option to repeat the dose."( Sumatriptan suppositories for the acute treatment of migraine. S2B351 Study Group.
Cochran, A; Hobbs, S; Tepper, SJ; Woessner, M,
)
1.57
"Mean productivity loss 2 hours after dosing and across the work shift; percentages of patients returning to normal work performance within 2 hours after dosing and across the work shift; percentages of patients experiencing headache relief (reduction of moderate or severe predose pain to mild or no pain) 1 and 2 hours after dosing."( Sumatriptan injection reduces productivity loss during a migraine attack: results of a double-blind, placebo-controlled trial.
Cady, RC; Jhingran, P; O'Quinn, S; Pait, DG; Ryan, R, 1998
)
1.74
"001) greater percentages of patients in the sumatriptan group compared with the placebo group returned to normal work performance by 2 hours after dosing (sumatriptan, 52%; placebo, 9%) and across the work shift (sumatriptan, 66%; placebo, 18%)."( Sumatriptan injection reduces productivity loss during a migraine attack: results of a double-blind, placebo-controlled trial.
Cady, RC; Jhingran, P; O'Quinn, S; Pait, DG; Ryan, R, 1998
)
2
" For their second treatment, patients were evaluated on their response to sumatriptan, number of 25-mg tablets taken, and dosage prescribed for future migraines."( Dosing of oral sumatriptan: a review of our first 104 patients.
Becker, J; Frizelis, K; Kunkel, RS; Solomon, GD, 1998
)
0.88
" The majority of patients required more than one 25-mg tablet for a migraine attack, reflecting both inadequacy of dosing for some migraines and recurrence of headache, yet 40% of patients continued on treatment with 25-mg tablets."( Dosing of oral sumatriptan: a review of our first 104 patients.
Becker, J; Frizelis, K; Kunkel, RS; Solomon, GD, 1998
)
0.65
"With an onset of headache relief as early as 15 min postdose compared with placebo, sumatriptan nasal spray is an important treatment option for patients who seek rapid headache relief and/or a convenient dosing form, whose migraine-associated nausea and vomiting render the use of an oral medication impractical, and those who prefer not to use an injectable form of migraine medication."( Consistency of response to sumatriptan nasal spray across patient subgroups and migraine types.
Ashford, E; Saiers, J; Salonen, R; Woessner, M, 1998
)
0.82
" For each migraine, patients recorded pain severity scores before and after taking sumatriptan and the time between dosing and onset of meaningful relief."( Sumatriptan treatment for migraine in a health maintenance organization: economic, humanistic, and clinical outcomes.
Batenhorst, A; Beall, D; Beck, A; Clements, B; Cohen, JA; Miller, DW; Pait, DG; Rawlings, J, 1999
)
1.97
" Secondary analyses showed that diclofenac-potassium provided significant pain relief from 60 min after dosing and for all remaining endpoints in the 8-h observation period."( Acute treatment of migraine attacks: efficacy and safety of a nonsteroidal anti-inflammatory drug, diclofenac-potassium, in comparison to oral sumatriptan and placebo. The Diclofenac-K/Sumatriptan Migraine Study Group.
, 1999
)
0.5
" dosing and 68."( Mixed effect modeling of sumatriptan pharmacokinetics during drug development: II. From healthy subjects to phase 2 dose ranging in patients.
Cosson, VF; Fuseau, E, 1999
)
0.61
" The results of this study suggest that no alteration in the sumatriptan dosage will be necessary for migraine patients taking naproxen prophylactic therapy."( Lack of pharmacokinetic interaction between sumatriptan and naproxen.
Rambhau, D; Rao, BR; Rao, YM; Srinivasu, P, 2000
)
0.81
" Allowed to select dosing themselves, patients tend to migrate to the 100 mg dose."( Defining optimal dosing for sumatriptan tablets in the acute treatment of migraine.
Mathew, NT; Salonen, R, 1999
)
0.6
" Overall, the mean percentages of attacks per patient in which headache relief had been obtained 4 h after dosing were 71%, 71%, and 80% for the 25 mg, 50 mg, and 100 mg doses, respectively."( Patient-selected dosing in a six-month open-label study evaluating oral sumatriptan in the acute treatment of migraine. Sumatriptan Tablets S2CM10 Study Group.
Ashford, EA; Dowson, AJ; Flöter, T; Hassani, H; Prendergast, S; Roberts, GW; Szczudlik, A, 1999
)
0.54
" Fewer patients required rescue medication in the active groups (1% 100 mg to 13% 6 mg) compared with placebo (17%), and more patients were able to work and function normally two hours after dosing (41%, 100 mg; 20%, placebo)."( A dose-defining study of sumatriptan suppositories in the acute treatment of migraine.
Bertin, L; Brion, N; Färkkilä, M; Göbel, H; Wessely, P, 1999
)
0.61
" As additional triptans and new dosage formulations are developed and approved, it is anticipated that the treatment of migraine headaches in children may change significantly in the next several years."( Childhood migraine.
Turk, WR, 2000
)
0.31
" Each dose of sumatriptan (5 mg, 10 mg, and 20 mg) was superior to placebo with respect to the cumulative percentages of patients first reporting headache relief within 2 hours of dosing (Kaplan-Meier)."( A randomized, double-blind, placebo-controlled study of sumatriptan nasal spray in the treatment of acute migraine in adolescents.
Asgharnejad, M; Austin, R; Laurenza, A; Nett, R; Peykamian, M; Rothner, AD; Saper, J; Winner, P, 2000
)
0.91
" Therefore, it is quite possible that both drugs produce adverse immunological effects in vivo in cases of high dosage or obstruction of elimination."( [Effect of migraine medications on monocyte chemotaxis] .
Krumholz, W; Menges, T; Ogal, H; Szalay, G, 2000
)
0.31
" Pre-incubation with L-NNA abolished the sumatriptan-induced dilation and significantly shifted the dose-response of the constriction curve to the left."( Sumatriptan elicits both constriction and dilation in human and bovine brain intracortical arterioles.
Elhusseiny, A; Hamel, E, 2001
)
2.02
" Headache response 2 hours after dosing was reported by 76% of patients taking the 10-mg dose and 72% of those taking the 20-mg dose."( One-year tolerability and efficacy of sumatriptan nasal spray in adolescents with migraine: results of a multicenter, open-label study.
Asgharnejad, M; Austin, R; Laurenza, A; Nett, R; Peykamian, M; Rothner, AD; Winner, P, 2000
)
0.58
" Headache recurrence, defined as return of moderate or severe headache within 24 hours of dosing and following a headache response at two hours after initial dosing, occurred in 33% of the patients following 100 mg sumatriptan and in 28%, 34% and 32% after 20 mg, 40 mg and 80 mg eletriptan."( Pharmacology and efficacy of eletriptan for the treatment of migraine attacks.
Diener, HC; McHarg, A, 2000
)
0.49
" However, sumatriptan injection was perceived as the most effective dosing form by the greatest proportion of patients."( Sumatriptan injection and tablets in clinical practice: results of a survey of 707 migraineurs.
Dahlöf, CG; Saiers, J,
)
1.98
" The serious cardiovascular incidents after consuming sumatriptan have been associated mostly with the subcutaneous dosage form of this drug and with patients with underlying cardiovascular risk factors."( Fatal cardiac arrhythmia after oral sumatriptan.
Laine, K; Mäntynen, J; Raasakka, T; Saukko, P,
)
0.65
" For each attack, patients rated headache severity, presence of associated symptoms, and functional disability prior to dosing and at intervals through 4 hours thereafter."( Crossover comparison of rizatriptan 5 mg and 10 mg versus sumatriptan 25 mg and 50 mg in migraine. Rizatriptan Protocol 046 Study Group.
Block, GA; Getson, A; Goldstein, J; Jiang, K; Lines, C; Norman, B; Ryan, R,
)
0.38
"This study was designed to test the hypothesis that the encapsulation methods used to mask active drug may delay absorption of sumatriptan from dosing to 2 hours after dosing (the traditional end point in clinical trials of migraine treatment), an effect that may be enhanced by migraine-associated gastric stasis."( Effect of encapsulation on absorption of sumatriptan tablets: data from healthy volunteers and patients during a migraine.
Coates, P; Fuseau, E; Leibowitz, M; McNeal, S; Metz, A; O'Quinn, S; Pereira, A; Petricoul, O; Purdon, H; Sabin, A; Salonen, R; Thein, S, 2001
)
0.78
" Absorption was assessed by calculating the area under the plasma concentration-time curve from dosing to 2 hours after dosing (AUC2) and the times to first measurable plasma concentration, 10 ng/mL, 20 ng/mL, and maximum plasma concentration."( Effect of encapsulation on absorption of sumatriptan tablets: data from healthy volunteers and patients during a migraine.
Coates, P; Fuseau, E; Leibowitz, M; McNeal, S; Metz, A; O'Quinn, S; Pereira, A; Petricoul, O; Purdon, H; Sabin, A; Salonen, R; Thein, S, 2001
)
0.58
" It produces a dextral shift of the 5-HT dose-response curves for the binding of GTPgamma[35S] to human 5-HT(1B) (pK(b)=9."( In vitro activity of LY393558, an inhibitor of the 5-hydroxytryptamine transporter with 5-HT(1B/1D/2) receptor antagonist properties.
Boot, JR; Carney, SL; Cohen, ML; Colvin, EM; Conway, RG; Hardy, CH; Lucaites, VL; Nelson, DL; Pullar, IA; Schenck, KW; Tomlinson, R; Wedley, S, 2001
)
0.31
" However, plasma concentrations increased from the first minute after intranasal dosing suggesting that sumatriptan and naratriptan are absorbed into the general systemic circulation from the nasal cavity in rats in a first-order fashion with no lag time."( Intranasal absorption of sumatriptan and naratriptan: no evidence of local transfer from the nasal cavities to the brain arterial blood in male rats.
Deprez, S; Einer-Jensen, N; Larsen, L; Schwartz, S; Starns, E, 2001
)
0.83
"This study sought to determine the effect of coadministration of clarithromycin dosed to steady state on the pharmacokinetics of a single dose of sumatriptan."( The pharmacokinetics of sumatriptan when administered with clarithromycin in healthy volunteers.
Bye, C; Gray, P; Leese, PT; McNeal, S; Moore, KH; O'Quinn, S; Sale, M, 2002
)
0.82
"The extent of absorption of sumatriptan was similar after oral administration alone and in combination with clarithromycin dosed to steady state."( The pharmacokinetics of sumatriptan when administered with clarithromycin in healthy volunteers.
Bye, C; Gray, P; Leese, PT; McNeal, S; Moore, KH; O'Quinn, S; Sale, M, 2002
)
0.92
" Studies of frovatriptan in isolated human arteries demonstrated a lower threshold for constriction of cerebral than coronary vasculature and a bell-shaped dose-response curve was apparent in the coronary arteries."( Pharmacology of the selective 5-HT(1B/1D) agonist frovatriptan.
Comer, MB, 2002
)
0.31
"In direct head-to-head comparative clinical trials, oral rizatriptan 10 mg enabled more migraine sufferers to function normally at 2 h after dosing than oral sumatriptan, naratriptan, and zolmitriptan."( Restoring migraine sufferers' ability to function normally: a comparison of rizatriptan and other triptans in randomized trials.
Bussone, G; D'Amico, D; Gerth, W; Lines, CR; McCarroll, KA, 2002
)
0.51
" A total of 16 subjects (10 males and 6 females) had pharmacokinetic data that could be analyzed, 2 withdrew from the study 30 and 60 minutes after dosing following the loss of venous access for blood sampling, and a bioanalysis failure resulted in loss of data from 3 subjects."( Pharmacokinetics of sumatriptan nasal spray in adolescents.
Christensen, ML; Fuseau, E; Jabbour, JT; Mottern, RK, 2003
)
0.64
" On the cost side of the equation, reflecting the health-care system perspective of the analysis, drug costs for initial dosing, second dosing for nonresponse, and recurrence and rescue medication were taken into account."( A cost-effectiveness analysis of eletriptan 40 and 80 mg versus sumatriptan 50 and 100 mg in the acute treatment of migraine.
Carter, D; DPhil, M; Drummond, M; Hettiarachchi, J; Pang, F; Parpia, T; Wells, N,
)
0.37
" The suggested methods were successfully applied for determining sumatriptan succinate in bulk powder, laboratory-prepared mixtures and pharmaceutical dosage forms (Imigran tablet) with good accuracy and precision."( Stability-indicating methods for the determination of sumatriptan succinate.
Abo-Talib, NF; Bebawy, LI; Moustafa, AA, 2003
)
0.81
" Trials comparing different doses of sumatriptan or dosing regimens were also included."( Oral sumatriptan for acute migraine.
Gray, RN; McCrory, DC, 2003
)
1.11
"To determine the cost-effectiveness of the triptans, a meta-analysis was conducted of the efficacy data from 27 oral triptan trials, using the endpoint of "pain-free" status within 2 hours after initial dosing as the indicator of efficacy."( Meta-analysis of oral triptan therapy for migraine: number needed to treat and relative cost to achieve relief within 2 hours.
Adelman, JU; Belsey, J,
)
0.13
" After the perivascular preinjection of 1 nmol/l L-668,169 or 1 nmol/l L-733,060 (NK1 receptor antagonists), the SP dose-response curve was shifted to the right."( Effects of neuropeptides on the sumatriptan-disturbed circulation in the optic nerve head of rabbits.
Cunha-Vaz, JG; Gaspar, MN; Macedo, TR; Ribeiro, CA, 2004
)
0.61
" Patients recorded details of the treated migraine on a diary card and rated pain severity immediately before dosing and 30 minutes, 45 minutes, 1 hour, and 2 hours after dosing using a 4-point scale (from 0 = none to 3 = severe)."( Efficacy and tolerability of sumatriptan tablets in a fast-disintegrating, rapid-release formulation for the acute treatment of migraine: results of a multicenter, randomized, placebo-controlled study.
Ahmad, F; Boswell, D; Carpay, J; Kinrade, F; Schoenen, J, 2004
)
0.61
" The dosing scheme based on age and weight resulted in maximal concentrations (C(max)) and systemic exposure (AUC) that were comparable to those observed in adolescents and adults treated with 20 mg."( Pharmacokinetics of sumatriptan nasal spray in children.
Christensen, ML; Fuseau, E; Jabbour, JT; Mottern, RK, 2004
)
0.65
" These findings suggest that effect of NTG on nNOS at a high dosage may involve the cycloxygenase pathway and that activation of the peripheral 5-HT1B/D receptors is not able to modify this effect."( Nitroglycerin-induced nNOS increase in rat trigeminal nucleus caudalis is inhibited by systemic administration of lysine acetylsalicylate but not of sumatriptan.
Pardutz, A; Schoenen, J; Szatmári, E; Vecsei, L, 2004
)
0.52
" Pharmacokinetic parameters measured early (0-2 h) after dosing reveal slightly faster absorption, on average, of the new sumatriptan formulation than sumatriptan conventional tablets although high intersubject variability was observed."( Pharmacokinetic profile of a new form of sumatriptan tablets in healthy volunteers.
Boswell, D; Bullman, J; Dow, A; Lewis, A; Sidhu, J; Summers, SJ; Walls, C, 2004
)
0.8
" During concomitant treatment with topiramate and carbamazepine or phenytoin, the (oral) clearance of topiramate increases 2-fold and its half-life becomes shorter by approximately 50%, which may require topiramate dosage adjustment when phenytoin or carbamazepine therapy is added or discontinued."( Pharmacokinetic interactions of topiramate.
Bialer, M; Curtin, C; Doose, DR; Murthy, B; Schwabe, S; Twyman, RE; Wang, SS, 2004
)
0.32
" In the early treatment group significantly more patients were pain free at all times measured during two hours after dosing than in the late treatment group."( Early treatment of a migraine attack while pain is still mild increases the efficacy of sumatriptan.
Banik, N; Moeckesch, B; Schellenberg, R; Scholpp, J, 2004
)
0.55
" Across all migraines with evaluable efficacy data (n=4334), headache relief was reported in 43% of migraines at 1 hour and in 59% at 2 hours after dosing with sumatriptan nasal spray 20 mg."( Long-term tolerability of sumatriptan nasal spray in adolescent patients with migraine.
Jabbour, JT; Natarajan, S; Richardson, MS; Webster, CJ,
)
0.63
"When compared at 2 and 24 hours, aggressive (20 mg dosed up to four times) IV metoclopramide and 6 mg of subcutaneous sumatriptan relieved migraine headache pain comparably."( A trial of metoclopramide vs sumatriptan for the emergency department treatment of migraines.
Bijur, PE; Corbo, J; Esses, D; Friedman, BW; Gallagher, EJ; Lipton, RB; Solorzano, C, 2005
)
0.83
" Using a personal digital assistant, patients recorded the time of dosing and the time at which pain severity reached none or mild (ie, pain relief) or none (ie, pain free) in real time so that the time to onset of relief could be measured as a continuous variable."( Two replicate randomized, double-blind, placebo-controlled trials of the time to onset of pain relief in the acute treatment of migraine with a fast-disintegrating/rapid-release formulation of sumatriptan tablets.
Agosti, R; Barrett, PS; Brandes, JL; Dahlöf, CG; Jones, MW; Sheftell, FD, 2005
)
0.52
"A novel model-based meta-analysis was used to quantify the dose-response relationship of sumatriptan and eletriptan for the proportion of patients that achieve migraine pain relief up to 4 h after treatment."( Therapeutic benefit of eletriptan compared to sumatriptan for the acute relief of migraine pain--results of a model-based meta-analysis that accounts for encapsulation.
Alderman, J; Cox, E; Mandema, JW, 2005
)
0.81
"This was a retrospective cohort study conducted in a managed care organization for patients aged 18 years or older who had picked up at least one outpatient prescription for any sumatriptan dosage form at the pharmacy between January 2002 and June 2002."( Assessment of clinical, service, and cost outcomes of a conversion program of sumatriptan to rizatriptan ODT in primary care patients with migraine headaches.
Billups, SJ; Carroll, N; Delate, T; Gershovich, OE; Hoffman, CK, 2006
)
0.75
" Disease dynamics must be considered to evaluate treatment response adequately and optimise the dosing regimen in migraine."( A model-based approach to treatment comparison in acute migraine.
Danhof, M; Della Pasqua, O; Maas, HJ, 2006
)
0.33
"Sumatriptan-naproxen sodium was more effective than placebo for headache relief at 2 hours after dosing (study 1, 65% vs 28%; P<."( Sumatriptan-naproxen for acute treatment of migraine: a randomized trial.
Adelman, JU; Alexander, WJ; Barrett, PS; Brandes, JL; Kudrow, D; Lener, SE; O'Carroll, CP; O'Donnell, FJ; Spruill, SE; Stark, SR, 2007
)
3.23
"In this double-blind, double-dummy, randomised, parallel group, multicentre study, the efficacy of dosing and re-dosing of a fixed combination of indomethacin, prochlorperazine and caffeine (Indoprocaf) was compared with encapsulated sumatriptan in the acute treatment of two migraine attacks."( Efficacy of dosing and re-dosing of two oral fixed combinations of indomethacin, prochlorperazine and caffeine compared with oral sumatriptan in the acute treatment of multiple migraine attacks: a double-blind, double-dummy, randomised, parallel group, mu
Cerbo, R; Del Bene, E; Ferrari, A; Genco, S; Grazioli, I; Martelletti, P; Nappi, G; Pinessi, L; Sandrini, G; Sarchielli, P; Tamburro, P; Uslenghi, C; Zanchin, G, 2007
)
0.73
"The study demonstrated that the efficacy of the initial dosing of Indoprocaf was not higher than that of sumatriptan, but that the strategy to use the lowest effective dose as soon as the headache occurred, followed by a second dose if the headache has not relieved or to treat a relapse, was very effective, especially with Indoprocaf."( Efficacy of dosing and re-dosing of two oral fixed combinations of indomethacin, prochlorperazine and caffeine compared with oral sumatriptan in the acute treatment of multiple migraine attacks: a double-blind, double-dummy, randomised, parallel group, mu
Cerbo, R; Del Bene, E; Ferrari, A; Genco, S; Grazioli, I; Martelletti, P; Nappi, G; Pinessi, L; Sandrini, G; Sarchielli, P; Tamburro, P; Uslenghi, C; Zanchin, G, 2007
)
0.76
" In an oral formulation, which is the patients' preferred dosing route, sumatriptan FDT/RRT may therefore constitute an advance in the management of acute migraine attacks."( Sumatriptan fast-disintegrating/rapid-release tablets in the acute treatment of migraine.
Barbanti, P; Cruccu, G; Le Pera, D, 2007
)
2.01
"The slow rate and low extent of absorption of the drug during the first 2 h after dosing observed in patients of group B could explain their unsatisfactory response to oral sumatriptan."( Interindividual variability of oral sumatriptan pharmacokinetics and of clinical response in migraine patients.
Bertolini, A; Coccia, C; Ferrari, A; Pinetti, D; Sternieri, E, 2008
)
0.81
" Although at discharge the patient was advised to permanently avoid triptans, she continued the use of oral sumatriptan at low dosage (25-50 mg) without any problems."( Acute myocardial infarction with sumatriptan: a case report and review of the literature.
Chalaupka, FD, 2009
)
0.85
"The complete RCT model involved three submodels: i) the input-output submodel for the prediction of events (using the sigmoid dose-response relationship as the basic model), ii) the execution submodel for deviations from a randomized, controlled two-arm parallel trial related to either patient-specific or investigator-specific elements or both: placebo or nocebo effect, errors of measurement, effect of concomitant therapy, regression to the mean phenomenon, blinding process, loss to follow-up and randomization process, iii) the covariate distribution submodel."( Revisiting the level of evidence in randomized controlled clinical trials: A simulation approach.
Bajard, A; Boissel, JP; Chabaud, S; Nony, P; Pérol, D, 2009
)
0.35
" The adverse-event profile of the sumatriptan/naproxen sodium combination tablet did not appear to differ from that of the individual components of the same or similar dosage strengths administered alone or in combination."( Distinct pharmacokinetic profile and safety of a fixed-dose tablet of sumatriptan and naproxen sodium for the acute treatment of migraine.
Haberer, LJ; Lener, SE; McDonald, SA; Taylor, DR; Walls, CM, 2010
)
0.87
" Hence, this method demonstrated to be adequate for in vitro studies of NAP and SUMA in the combinational dosage form, since there is no official monograph, collaborating to the official codes."( In vitro dissolution profile comparison of an anti-migraine combinational drug in dosage form.
Bhojraj, S; Hiremath, VB; Kaliaperumal, K; Nanjan, MJ, 2010
)
0.36
" CGRP 8-37 had no significant effects on blood pressure dose-response profiles and individual dose blood pressure responses to any of the vasomodulators tested."( Effect of calcitonin gene-related peptide receptor antagonism on the systemic blood pressure responses to mechanistically diverse vasomodulators in conscious rats.
Detwiler, TJ; Kane, SA; Lynch, JJ; Regan, CP, 2010
)
0.36
" For each drug, 6 healthy male volunteers were dosed with 100 μg (14)C-labelled compound."( Comparative pharmacokinetics between a microdose and therapeutic dose for clarithromycin, sumatriptan, propafenone, paracetamol (acetaminophen), and phenobarbital in human volunteers.
Alder, J; Bjerrum, OJ; Brian Houston, J; Garner, C; Gesson, C; Grynkiewicz, G; Jochemsen, R; Lappin, G; Oosterhuis, B; Rowland, M; Shishikura, Y; Weaver, RJ, 2011
)
0.59
" Patients were treated with sumatriptan-naproxen using a very early intervention paradigm in 4 test migraines over 12 weeks where dosage occurred within 30 minutes of symptom onset."( Sumatriptan-naproxen migraine efficacy in allodynic patients: early intervention.
Hoagland, NA; Hoagland, R; Landy, S, 2012
)
2.12
" Trials comparing different doses of sumatriptan or dosing regimens were also included."( WITHDRAWN: Oral sumatriptan for acute migraine.
Gray, RN; McCrory, DC, 2012
)
1
"There were insufficient data to evaluate other doses of oral diclofenac, or to compare different formulations or different dosing regimens; only one study compared oral diclofenac with an active comparator (oral sumatriptan 100 mg)."( Diclofenac with or without an antiemetic for acute migraine headaches in adults.
Derry, S; Moore, RA; Rabbie, R, 2012
)
0.57
" Subjects reporting headache pain 2 hours after dosing were randomly assigned into a 12-week double-blind phase, treating 1 moderate-to-severe migraine (attack 2) with placebo (n = 145), suma/nap 10/60 mg (n = 96), 30/180 mg (n = 97), or 85/500 mg (n = 152)."( Randomized trial of sumatriptan and naproxen sodium combination in adolescent migraine.
Derosier, FJ; Goodman, DK; Granberry, WK; Hershey, AD; Jimenez, TB; Lewis, D; Linder, SL; Pearlman, E; Rothner, AD; Runken, MC; Winner, PK, 2012
)
0.7
" Special clinical trials of the timing of dosage and sumatriptan in combination with other triptans as well as non-triptan drugs are also included."( Sumatriptan: a review of its pharmacokinetics, pharmacodynamics and efficacy in the acute treatment of migraine.
Hougaard, A; Tfelt-Hansen, P, 2013
)
2.08
"There were insufficient data to evaluate other doses of oral diclofenac, or to compare different formulations or different dosing regimens; only one study compared oral diclofenac with an active comparator (oral sumatriptan 100 mg)."( Diclofenac with or without an antiemetic for acute migraine headaches in adults.
Derry, S; Moore, RA; Rabbie, R, 2013
)
0.58
" Frequent dosing of SumaRT/Nap or naproxen sodium was well tolerated in this study."( Treatment of chronic migraine: a 3-month comparator study of naproxen sodium vs SumaRT/Nap.
Beach, ME; Cady, R; Dexter, K; Freitag, F; Manley, HR; Nett, R, 2014
)
0.4
" Patients recorded details of the treated migraine on a diary card and rated pain severity immediately before dosing and 30 minutes, 1 hour, 2 hours, and 4 hours after dosing using a 4-point scale (0 = none to 3 = severe)."( Promethazine plus sumatriptan in the treatment of migraine: a randomized clinical trial.
Amini, A; Asadollahi, S; Forouzanfar, MM; Heidari, K; Shahrami, A; Vafaee, R, 2014
)
0.74
" Furthermore, in vitro release studies revealed 90% release of drug from developed dosage form within 10 min, thus suggesting rapid drug dissolution followed by faster onset of action, which forms a strong rationale for development of ODTs of sumatriptan succinate."( Freeze drying: exploring potential in development of orodispersible tablets of sumatriptan succinate.
Desai, P; Gugulothu, D; Pandharipande, P; Patravale, V, 2015
)
0.83
" As the migraine follows circadian rhythm in which headache is more painful at the awakening time, the dosage form should be given during night time to release drug when pain get worsen."( Development and optimization of press coated floating pulsatile drug delivery of sumatriptan succinate.
Jagdale, SC; Pawar, CR, 2014
)
0.63
" This needs administration of dosage form at night time to release drug after lag period when pain gets worse."( Application of design of experiment for polyox and xanthan gum coated floating pulsatile delivery of sumatriptan succinate in migraine treatment.
Jagdale, SC; Pawar, CR, 2014
)
0.62
" Blood samples for pharmacokinetic profiling of sumatriptan were obtained prior to dosing and at predetermined time points covering the 12 hours postonset of treatment."( A Phase I, Open-Label, Single-Dose Safety, Pharmacokinetic, and Tolerability Study of the Sumatriptan Iontophoretic Transdermal System in Adolescent Migraine Patients.
Aycardi, E; Bigal, ME; Chitra, R; Gutman, D; Hellriegel, E; Kansagra, S; Kidron, OS; Knebel, H; Kunta, J; Linder, S; Ma, Y; Pierce, M; Spiegelstein, O; Winner, PK, 2016
)
0.91
" Initially dosing with MSM while pain was mild was associated with the lowest daily disability [medication × pain at dosing F (4, 6336."( Acute migraine medication adherence, migraine disability and patient satisfaction: A naturalistic daily diary study.
Nicholson, RA; Robbins, MS; Seng, EK, 2017
)
0.46
" Results from the primary endpoint (SPID-30, defined as the sum of pain intensity differences from dosing to 30 minutes), key secondary efficacy endpoints and safety assessments have been reported in the primary publication (Tepper et al."( Early Onset of Efficacy and Consistency of Response Across Multiple Migraine Attacks From the Randomized COMPASS Study: AVP-825 Breath Powered
Halker, R; Mahmoud, RA; McAllister, PJ; Siffert, J; Silberstein, S; Tepper, SJ; Winner, PK, 2017
)
0.46
" Patients recorded ordinal migraine pain intensity and migraine-related disability before dosing (predose), and at 10, 15, 30, 45, 60, 90 and 120 minutes."( Faster Improvement in Migraine Pain Intensity and Migraine-Related Disability at Early Time Points with AVP-825 (Sumatriptan Nasal Powder Delivery System) versus Oral Sumatriptan: A Comparative Randomized Clinical Trial Across Multiple Attacks from the CO
Buse, DC; Lipton, RB; McGinley, JS; Shulman, KJ; Wirth, RJ, 2017
)
0.67
"The present study involved segmental testing of hair in two clinical cases with known dosage histories."( Segmental Hair Analysis-Interpretation of the Time of Drug Intake in Two Patients Undergoing Drug Treatment.
Johansen, SS; Linnet, K; Nielsen, MKK; Wang, X, 2019
)
0.51
" Cluster headache is not optimally treated and few clinical trials are available to model therapy, especially dosing and administration."( Cluster Headache: Opportunities for Pharmacists to Improve Care.
Clark, AS; Smith, TR; Wenzel, R, 2022
)
0.72
" Classical oral dosage forms are not frequently workable in migraine because of the associated nausea/vomiting, and no effective fixed dose combination is available."( Development of Optimized Sumatriptan-Prochlorperazine Combined Orodispersible Films Without Disintegrant: in vitro, ex vivo and in vivo Characterization.
Anwer, UU; Bukhari, NI; Hafiz, MA; Hussain, A; Javed, S; Rasool, F; Raza, SA; Shah, PA; Shamim, R, 2022
)
1.02
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
serotonergic agonistAn agent that has an affinity for serotonin receptors and is able to mimic the effects of serotonin by stimulating the physiologic activity at the cell receptors. Serotonin agonists are used as antidepressants, anxiolytics, and in the treatment of migraine disorders.
vasoconstrictor agentDrug used to cause constriction of the blood vessels.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (2)

ClassDescription
sulfonamideAn amide of a sulfonic acid RS(=O)2NR'2.
tryptaminesTryptamine and its substitution derivatives.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (48)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Beta-lactamaseEscherichia coli K-12Potency44.66840.044717.8581100.0000AID485294
AR proteinHomo sapiens (human)Potency11.88320.000221.22318,912.5098AID1259243
EWS/FLI fusion proteinHomo sapiens (human)Potency0.00330.001310.157742.8575AID1259255
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency0.23910.000214.376460.0339AID720691
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency0.00240.057821.109761.2679AID1159526
chromobox protein homolog 1Homo sapiens (human)Potency79.43280.006026.168889.1251AID540317
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
5-hydroxytryptamine receptor 3EHomo sapiens (human)IC50 (µMol)2.50550.00042.08059.0000AID5956; AID5997
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
5-hydroxytryptamine receptor 3BHomo sapiens (human)IC50 (µMol)2.50550.00041.95059.0000AID5956; AID5997
Bile salt export pumpHomo sapiens (human)IC50 (µMol)134.00000.11007.190310.0000AID1443980; AID1473738
5-hydroxytryptamine receptor 1AHomo sapiens (human)IC50 (µMol)0.44970.00010.666410.0000AID3912; AID3975
5-hydroxytryptamine receptor 1AHomo sapiens (human)Ki0.35740.00010.532610.0000AID3809; AID3829; AID3834; AID3835; AID3849; AID3850; AID3858; AID3860
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)Ki1.00000.00020.667710.0000AID5729
Carboxypeptidase MHomo sapiens (human)IC50 (µMol)0.02000.02000.02000.0200AID4863
D(2) dopamine receptorHomo sapiens (human)Ki0.21800.00000.651810.0000AID63225
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)IC50 (µMol)10.00000.00040.908610.0000AID5606
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)0.64000.00021.874210.0000AID3731
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC50 (µMol)0.72200.00031.38338.4000AID3731; AID625190
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki0.45900.00010.739610.0000AID625190
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)0.64000.00021.270410.0000AID3731
5-hydroxytryptamine receptor 1DHomo sapiens (human)IC50 (µMol)0.30910.00050.28702.4000AID4292; AID4595; AID4596; AID4597; AID4600; AID4601; AID4640; AID4642
5-hydroxytryptamine receptor 1DHomo sapiens (human)Ki0.00770.00010.808710.0000AID404703; AID4549; AID4615; AID4617; AID4622; AID4626; AID4627; AID4629; AID4632; AID4899; AID4900; AID4908
5-hydroxytryptamine receptor 1BHomo sapiens (human)IC50 (µMol)0.01310.00050.39756.5000AID4270; AID4510; AID4511; AID4512; AID4514; AID4515; AID4516
5-hydroxytryptamine receptor 1BHomo sapiens (human)Ki0.01880.00010.54859.2100AID404702; AID4245; AID4248; AID4252; AID4255; AID4256; AID4258; AID4260; AID4569; AID4919; AID4924; AID4929; AID4931
5-hydroxytryptamine receptor 2AHomo sapiens (human)IC50 (µMol)8.97160.00010.88018.8500AID5366; AID5404
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki0.68800.00000.385510.0000AID5201; AID5398
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC50 (µMol)5.98350.00011.03029.0000AID5636; AID5691; AID5956
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)IC50 (µMol)0.80400.00051.48357.8000AID625190
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)Ki0.45900.00031.29679.2440AID625190
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)IC50 (µMol)0.06100.00311.73607.8000AID4873
5-hydroxytryptamine receptor 1EHomo sapiens (human)IC50 (µMol)5.50005.50005.50005.5000AID4970
5-hydroxytryptamine receptor 1FHomo sapiens (human)IC50 (µMol)1.00000.08781.94393.8000AID4977
5-hydroxytryptamine receptor 1FHomo sapiens (human)Ki0.02570.00161.786510.0000AID4983
5-hydroxytryptamine receptor 7Homo sapiens (human)Ki1.00000.00030.380610.0000AID1546005
Alpha-1A adrenergic receptorHomo sapiens (human)IC50 (µMol)10.00000.00020.56145.4000AID5636
5-hydroxytryptamine receptor 3ARattus norvegicus (Norway rat)Ki1.00000.00020.484110.0000AID5878
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)0.64000.00001.819410.0000AID3731
5-hydroxytryptamine receptor 3AHomo sapiens (human)IC50 (µMol)3.33850.00011.07899.0000AID5956; AID5997; AID6025; AID6358
5-hydroxytryptamine receptor 5AHomo sapiens (human)IC50 (µMol)0.50120.50120.50120.5012AID3978
5-hydroxytryptamine receptor 1BOryctolagus cuniculus (rabbit)Ki0.00120.00090.04640.1370AID404703
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki0.21800.00000.437510.0000AID63082
5-hydroxytryptamine receptor 1DSus scrofa (pig)IC50 (µMol)0.02000.00030.64963.7153AID4858; AID4863; AID4864
5-hydroxytryptamine receptor 1AMus musculus (house mouse)IC50 (µMol)0.45000.00210.35812.0000AID4460
5-hydroxytryptamine receptor 3DHomo sapiens (human)IC50 (µMol)2.50550.00042.08059.0000AID5956; AID5997
5-hydroxytryptamine receptor 3CHomo sapiens (human)IC50 (µMol)2.50550.00042.08059.0000AID5956; AID5997
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
Multidrug and toxin extrusion protein 1Homo sapiens (human)IC50 (µMol)6.70000.01002.765610.0000AID721754
5-hydroxytryptamine receptor 3BRattus norvegicus (Norway rat)Ki1.00000.00020.502310.0000AID5878
5-hydroxytryptamine receptor 1BGorilla gorilla gorilla (western lowland gorilla)Ki0.00640.00642.89075.7750AID4484
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Voltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)EC50 (µMol)0.01200.00080.00640.0120AID4575
5-hydroxytryptamine receptor 1AHomo sapiens (human)Kd0.39810.00010.95285.0119AID438555
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)EC50 (µMol)1.30000.00543.251020.9400AID3709
5-hydroxytryptamine receptor 1DHomo sapiens (human)EC50 (µMol)0.01170.00080.00600.0160AID4571; AID4572; AID4574; AID4575; AID4577; AID4578; AID4581
5-hydroxytryptamine receptor 1BHomo sapiens (human)EC50 (µMol)0.05760.01160.13880.4300AID4495; AID4496
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)EC50 (µMol)0.09700.00130.03880.0970AID4872
5-hydroxytryptamine receptor 1FHomo sapiens (human)EC50 (µMol)0.03500.03500.03500.0350AID4974
Voltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)EC50 (µMol)0.01200.00080.00640.0120AID4575
Voltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)EC50 (µMol)0.01200.00080.00640.0120AID4575
Voltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)EC50 (µMol)0.01200.00080.00640.0120AID4575
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Solute carrier family 22 member 1 Homo sapiens (human)Km55.00000.47704.03089.0000AID1526737
5-hydroxytryptamine receptor 1DHomo sapiens (human)ED500.31700.06800.19250.3170AID4583
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (307)

Processvia Protein(s)Taxonomy
serotonin receptor signaling pathway5-hydroxytryptamine receptor 3EHomo sapiens (human)
monoatomic ion transmembrane transport5-hydroxytryptamine receptor 3EHomo sapiens (human)
excitatory postsynaptic potential5-hydroxytryptamine receptor 3EHomo sapiens (human)
inorganic cation transmembrane transport5-hydroxytryptamine receptor 3EHomo sapiens (human)
regulation of membrane potential5-hydroxytryptamine receptor 3EHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 3EHomo sapiens (human)
xenobiotic metabolic processSolute carrier family 22 member 1 Homo sapiens (human)
neurotransmitter transportSolute carrier family 22 member 1 Homo sapiens (human)
serotonin transportSolute carrier family 22 member 1 Homo sapiens (human)
establishment or maintenance of transmembrane electrochemical gradientSolute carrier family 22 member 1 Homo sapiens (human)
organic cation transportSolute carrier family 22 member 1 Homo sapiens (human)
quaternary ammonium group transportSolute carrier family 22 member 1 Homo sapiens (human)
prostaglandin transportSolute carrier family 22 member 1 Homo sapiens (human)
monoamine transportSolute carrier family 22 member 1 Homo sapiens (human)
putrescine transportSolute carrier family 22 member 1 Homo sapiens (human)
spermidine transportSolute carrier family 22 member 1 Homo sapiens (human)
acetylcholine transportSolute carrier family 22 member 1 Homo sapiens (human)
dopamine transportSolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine transportSolute carrier family 22 member 1 Homo sapiens (human)
thiamine transportSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transportSolute carrier family 22 member 1 Homo sapiens (human)
epinephrine transportSolute carrier family 22 member 1 Homo sapiens (human)
serotonin uptakeSolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine uptakeSolute carrier family 22 member 1 Homo sapiens (human)
thiamine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
metanephric proximal tubule developmentSolute carrier family 22 member 1 Homo sapiens (human)
purine-containing compound transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
dopamine uptakeSolute carrier family 22 member 1 Homo sapiens (human)
monoatomic cation transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
transport across blood-brain barrierSolute carrier family 22 member 1 Homo sapiens (human)
(R)-carnitine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
acyl carnitine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
spermidine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
cellular detoxificationSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transport across blood-brain barrierSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
visual perceptionVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
detection of light stimulus involved in visual perceptionVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 3BHomo sapiens (human)
monoatomic ion transmembrane transport5-hydroxytryptamine receptor 3BHomo sapiens (human)
excitatory postsynaptic potential5-hydroxytryptamine receptor 3BHomo sapiens (human)
inorganic cation transmembrane transport5-hydroxytryptamine receptor 3BHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 3BHomo sapiens (human)
regulation of membrane potential5-hydroxytryptamine receptor 3BHomo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
behavioral fear response5-hydroxytryptamine receptor 1AHomo sapiens (human)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
gamma-aminobutyric acid signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of serotonin secretion5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of vasoconstriction5-hydroxytryptamine receptor 1AHomo sapiens (human)
exploration behavior5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of dopamine metabolic process5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin metabolic process5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of hormone secretion5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 1AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 1AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 1AHomo sapiens (human)
anatomical structure morphogenesisCarboxypeptidase MHomo sapiens (human)
peptide metabolic processCarboxypeptidase MHomo sapiens (human)
protein processingCarboxypeptidase MHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
temperature homeostasisD(2) dopamine receptorHomo sapiens (human)
response to hypoxiaD(2) dopamine receptorHomo sapiens (human)
negative regulation of protein phosphorylationD(2) dopamine receptorHomo sapiens (human)
response to amphetamineD(2) dopamine receptorHomo sapiens (human)
nervous system process involved in regulation of systemic arterial blood pressureD(2) dopamine receptorHomo sapiens (human)
regulation of heart rateD(2) dopamine receptorHomo sapiens (human)
regulation of sodium ion transportD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor internalizationD(2) dopamine receptorHomo sapiens (human)
positive regulation of neuroblast proliferationD(2) dopamine receptorHomo sapiens (human)
positive regulation of receptor internalizationD(2) dopamine receptorHomo sapiens (human)
autophagyD(2) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
neuron-neuron synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
neuroblast proliferationD(2) dopamine receptorHomo sapiens (human)
axonogenesisD(2) dopamine receptorHomo sapiens (human)
synapse assemblyD(2) dopamine receptorHomo sapiens (human)
sensory perception of smellD(2) dopamine receptorHomo sapiens (human)
long-term memoryD(2) dopamine receptorHomo sapiens (human)
grooming behaviorD(2) dopamine receptorHomo sapiens (human)
locomotory behaviorD(2) dopamine receptorHomo sapiens (human)
adult walking behaviorD(2) dopamine receptorHomo sapiens (human)
protein localizationD(2) dopamine receptorHomo sapiens (human)
negative regulation of cell population proliferationD(2) dopamine receptorHomo sapiens (human)
associative learningD(2) dopamine receptorHomo sapiens (human)
visual learningD(2) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(2) dopamine receptorHomo sapiens (human)
response to light stimulusD(2) dopamine receptorHomo sapiens (human)
response to toxic substanceD(2) dopamine receptorHomo sapiens (human)
response to iron ionD(2) dopamine receptorHomo sapiens (human)
response to inactivityD(2) dopamine receptorHomo sapiens (human)
Wnt signaling pathwayD(2) dopamine receptorHomo sapiens (human)
striatum developmentD(2) dopamine receptorHomo sapiens (human)
orbitofrontal cortex developmentD(2) dopamine receptorHomo sapiens (human)
cerebral cortex GABAergic interneuron migrationD(2) dopamine receptorHomo sapiens (human)
adenohypophysis developmentD(2) dopamine receptorHomo sapiens (human)
negative regulation of cell migrationD(2) dopamine receptorHomo sapiens (human)
peristalsisD(2) dopamine receptorHomo sapiens (human)
auditory behaviorD(2) dopamine receptorHomo sapiens (human)
regulation of synaptic transmission, GABAergicD(2) dopamine receptorHomo sapiens (human)
positive regulation of cytokinesisD(2) dopamine receptorHomo sapiens (human)
circadian regulation of gene expressionD(2) dopamine receptorHomo sapiens (human)
negative regulation of dopamine secretionD(2) dopamine receptorHomo sapiens (human)
response to histamineD(2) dopamine receptorHomo sapiens (human)
response to nicotineD(2) dopamine receptorHomo sapiens (human)
positive regulation of urine volumeD(2) dopamine receptorHomo sapiens (human)
positive regulation of renal sodium excretionD(2) dopamine receptorHomo sapiens (human)
positive regulation of multicellular organism growthD(2) dopamine receptorHomo sapiens (human)
response to cocaineD(2) dopamine receptorHomo sapiens (human)
negative regulation of circadian sleep/wake cycle, sleepD(2) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(2) dopamine receptorHomo sapiens (human)
drinking behaviorD(2) dopamine receptorHomo sapiens (human)
regulation of potassium ion transportD(2) dopamine receptorHomo sapiens (human)
response to morphineD(2) dopamine receptorHomo sapiens (human)
pigmentationD(2) dopamine receptorHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transductionD(2) dopamine receptorHomo sapiens (human)
positive regulation of G protein-coupled receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
negative regulation of blood pressureD(2) dopamine receptorHomo sapiens (human)
negative regulation of innate immune responseD(2) dopamine receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IID(2) dopamine receptorHomo sapiens (human)
negative regulation of insulin secretionD(2) dopamine receptorHomo sapiens (human)
acid secretionD(2) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(2) dopamine receptorHomo sapiens (human)
behavioral response to ethanolD(2) dopamine receptorHomo sapiens (human)
regulation of long-term neuronal synaptic plasticityD(2) dopamine receptorHomo sapiens (human)
response to axon injuryD(2) dopamine receptorHomo sapiens (human)
branching morphogenesis of a nerveD(2) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(2) dopamine receptorHomo sapiens (human)
epithelial cell proliferationD(2) dopamine receptorHomo sapiens (human)
negative regulation of epithelial cell proliferationD(2) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(2) dopamine receptorHomo sapiens (human)
release of sequestered calcium ion into cytosolD(2) dopamine receptorHomo sapiens (human)
dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
positive regulation of dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
regulation of synapse structural plasticityD(2) dopamine receptorHomo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionD(2) dopamine receptorHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergicD(2) dopamine receptorHomo sapiens (human)
excitatory postsynaptic potentialD(2) dopamine receptorHomo sapiens (human)
positive regulation of growth hormone secretionD(2) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(2) dopamine receptorHomo sapiens (human)
negative regulation of dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeD(2) dopamine receptorHomo sapiens (human)
regulation of locomotion involved in locomotory behaviorD(2) dopamine receptorHomo sapiens (human)
postsynaptic modulation of chemical synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
negative regulation of cellular response to hypoxiaD(2) dopamine receptorHomo sapiens (human)
positive regulation of glial cell-derived neurotrophic factor productionD(2) dopamine receptorHomo sapiens (human)
positive regulation of long-term synaptic potentiationD(2) dopamine receptorHomo sapiens (human)
hyaloid vascular plexus regressionD(2) dopamine receptorHomo sapiens (human)
negative regulation of neuron migrationD(2) dopamine receptorHomo sapiens (human)
negative regulation of cytosolic calcium ion concentrationD(2) dopamine receptorHomo sapiens (human)
regulation of dopamine secretionD(2) dopamine receptorHomo sapiens (human)
negative regulation of adenylate cyclase activityD(2) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(2) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(2) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1DHomo sapiens (human)
intestine smooth muscle contraction5-hydroxytryptamine receptor 1DHomo sapiens (human)
regulation of locomotion5-hydroxytryptamine receptor 1DHomo sapiens (human)
vasoconstriction5-hydroxytryptamine receptor 1DHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 1DHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 1DHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 1DHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway5-hydroxytryptamine receptor 1DHomo sapiens (human)
G protein-coupled receptor internalization5-hydroxytryptamine receptor 1BHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1BHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway5-hydroxytryptamine receptor 1BHomo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1BHomo sapiens (human)
negative regulation of gamma-aminobutyric acid secretion5-hydroxytryptamine receptor 1BHomo sapiens (human)
regulation of dopamine secretion5-hydroxytryptamine receptor 1BHomo sapiens (human)
negative regulation of serotonin secretion5-hydroxytryptamine receptor 1BHomo sapiens (human)
negative regulation of synaptic transmission, GABAergic5-hydroxytryptamine receptor 1BHomo sapiens (human)
response to cocaine5-hydroxytryptamine receptor 1BHomo sapiens (human)
vasoconstriction5-hydroxytryptamine receptor 1BHomo sapiens (human)
drinking behavior5-hydroxytryptamine receptor 1BHomo sapiens (human)
response to ethanol5-hydroxytryptamine receptor 1BHomo sapiens (human)
bone remodeling5-hydroxytryptamine receptor 1BHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 1BHomo sapiens (human)
response to mineralocorticoid5-hydroxytryptamine receptor 1BHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergic5-hydroxytryptamine receptor 1BHomo sapiens (human)
cellular response to alkaloid5-hydroxytryptamine receptor 1BHomo sapiens (human)
cellular response to xenobiotic stimulus5-hydroxytryptamine receptor 1BHomo sapiens (human)
cellular response to temperature stimulus5-hydroxytryptamine receptor 1BHomo sapiens (human)
presynaptic modulation of chemical synaptic transmission5-hydroxytryptamine receptor 1BHomo sapiens (human)
regulation of presynaptic cytosolic calcium ion concentration5-hydroxytryptamine receptor 1BHomo sapiens (human)
positive regulation of vascular associated smooth muscle cell proliferation5-hydroxytryptamine receptor 1BHomo sapiens (human)
regulation of synaptic vesicle exocytosis5-hydroxytryptamine receptor 1BHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 1BHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 1BHomo sapiens (human)
temperature homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytokine production involved in immune response5-hydroxytryptamine receptor 2AHomo sapiens (human)
glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
activation of phospholipase C activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytosolic calcium ion concentration5-hydroxytryptamine receptor 2AHomo sapiens (human)
memory5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 2AHomo sapiens (human)
response to xenobiotic stimulus5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
regulation of dopamine secretion5-hydroxytryptamine receptor 2AHomo sapiens (human)
artery smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
urinary bladder smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of heat generation5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of potassium ion transport5-hydroxytryptamine receptor 2AHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of neuron apoptotic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein localization to cytoskeleton5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of vasoconstriction5-hydroxytryptamine receptor 2AHomo sapiens (human)
symbiont entry into host cell5-hydroxytryptamine receptor 2AHomo sapiens (human)
sensitization5-hydroxytryptamine receptor 2AHomo sapiens (human)
behavioral response to cocaine5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of inflammatory response5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylation5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of temperature stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of mechanical stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergic5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic modulation of chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of execution phase of apoptosis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of platelet aggregation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of DNA biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2AHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
behavioral fear response5-hydroxytryptamine receptor 2CHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
locomotory behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
feeding behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2CHomo sapiens (human)
cGMP-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of nervous system process5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of appetite5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of corticotropin-releasing hormone secretion5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of calcium-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2CHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1EHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1EHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway5-hydroxytryptamine receptor 1EHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 1EHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 1EHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1FHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 1FHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 1FHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway5-hydroxytryptamine receptor 1FHomo sapiens (human)
smooth muscle contraction5-hydroxytryptamine receptor 7Homo sapiens (human)
circadian rhythm5-hydroxytryptamine receptor 7Homo sapiens (human)
blood circulation5-hydroxytryptamine receptor 7Homo sapiens (human)
vasoconstriction5-hydroxytryptamine receptor 7Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 7Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 7Homo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 7Homo sapiens (human)
MAPK cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of heart rate involved in baroreceptor response to increased systemic arterial blood pressureAlpha-1A adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine vasoconstriction involved in regulation of systemic arterial blood pressureAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of heart rate by epinephrine-norepinephrineAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of the force of heart contraction by epinephrine-norepinephrineAlpha-1A adrenergic receptorHomo sapiens (human)
apoptotic processAlpha-1A adrenergic receptorHomo sapiens (human)
smooth muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
signal transductionAlpha-1A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
activation of phospholipase C activityAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1A adrenergic receptorHomo sapiens (human)
adult heart developmentAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of cell population proliferationAlpha-1A adrenergic receptorHomo sapiens (human)
response to xenobiotic stimulusAlpha-1A adrenergic receptorHomo sapiens (human)
response to hormoneAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of autophagyAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cardiac muscle hypertrophyAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of synaptic transmission, GABAergicAlpha-1A adrenergic receptorHomo sapiens (human)
intracellular signal transductionAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of action potentialAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of vasoconstrictionAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of smooth muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
calcium ion transport into cytosolAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cardiac muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
cell growth involved in cardiac muscle cell developmentAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of protein kinase C signalingAlpha-1A adrenergic receptorHomo sapiens (human)
pilomotor reflexAlpha-1A adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1A adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1A adrenergic receptorHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 3AHomo sapiens (human)
monoatomic ion transmembrane transport5-hydroxytryptamine receptor 3AHomo sapiens (human)
excitatory postsynaptic potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
inorganic cation transmembrane transport5-hydroxytryptamine receptor 3AHomo sapiens (human)
regulation of presynaptic membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 3AHomo sapiens (human)
regulation of membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 5AHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 5AHomo sapiens (human)
hippocampus development5-hydroxytryptamine receptor 5AHomo sapiens (human)
response to estradiol5-hydroxytryptamine receptor 5AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 5AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 5AHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway5-hydroxytryptamine receptor 5AHomo sapiens (human)
calcium ion transportVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
sensory perception of soundVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
positive regulation of adenylate cyclase activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
positive regulation of calcium ion transportVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
regulation of atrial cardiac muscle cell membrane repolarizationVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
calcium ion importVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
calcium ion transmembrane transportVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
cardiac muscle cell action potential involved in contractionVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
membrane depolarization during cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
membrane depolarization during SA node cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
regulation of heart rate by cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
regulation of potassium ion transmembrane transporter activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
regulation of potassium ion transmembrane transportVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
skeletal system developmentVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
extraocular skeletal muscle developmentVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
calcium ion transportVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
muscle contractionVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
striated muscle contractionVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
endoplasmic reticulum organizationVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
myoblast fusionVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
neuromuscular junction developmentVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
skeletal muscle adaptationVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
positive regulation of muscle contractionVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
skeletal muscle fiber developmentVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
release of sequestered calcium ion into cytosolVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
calcium ion transmembrane transportVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
cellular response to caffeineVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
immune system developmentVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
heart developmentVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
regulation of cardiac muscle contraction by regulation of the release of sequestered calcium ionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
embryonic forelimb morphogenesisVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
camera-type eye developmentVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
positive regulation of adenylate cyclase activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
positive regulation of muscle contractionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion transport into cytosolVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion transmembrane transport via high voltage-gated calcium channelVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion transmembrane transportVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
cardiac muscle cell action potential involved in contractionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membrane depolarization during cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membrane depolarization during AV node cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
cell communication by electrical coupling involved in cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
regulation of heart rate by cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
regulation of ventricular cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membrane depolarization during atrial cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 3DHomo sapiens (human)
monoatomic ion transmembrane transport5-hydroxytryptamine receptor 3DHomo sapiens (human)
excitatory postsynaptic potential5-hydroxytryptamine receptor 3DHomo sapiens (human)
inorganic cation transmembrane transport5-hydroxytryptamine receptor 3DHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 3DHomo sapiens (human)
regulation of membrane potential5-hydroxytryptamine receptor 3DHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 3CHomo sapiens (human)
monoatomic ion transmembrane transport5-hydroxytryptamine receptor 3CHomo sapiens (human)
excitatory postsynaptic potential5-hydroxytryptamine receptor 3CHomo sapiens (human)
inorganic cation transmembrane transport5-hydroxytryptamine receptor 3CHomo sapiens (human)
regulation of membrane potential5-hydroxytryptamine receptor 3CHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 3CHomo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
organic cation transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
putrescine transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
xenobiotic transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
thiamine transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
amino acid import across plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-arginine import across plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-alpha-amino acid transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
proton transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-arginine transmembrane transportMultidrug and toxin extrusion protein 1Homo sapiens (human)
xenobiotic detoxification by transmembrane export across the plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (82)

Processvia Protein(s)Taxonomy
serotonin-gated monoatomic cation channel activity5-hydroxytryptamine receptor 3EHomo sapiens (human)
excitatory extracellular ligand-gated monoatomic ion channel activity5-hydroxytryptamine receptor 3EHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential5-hydroxytryptamine receptor 3EHomo sapiens (human)
acetylcholine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
neurotransmitter transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
dopamine:sodium symporter activitySolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine:sodium symporter activitySolute carrier family 22 member 1 Homo sapiens (human)
protein bindingSolute carrier family 22 member 1 Homo sapiens (human)
monoamine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
secondary active organic cation transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
organic cation transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
pyrimidine nucleoside transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
thiamine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
putrescine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
spermidine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
quaternary ammonium group transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
toxin transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
identical protein bindingSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
(R)-carnitine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
metal ion bindingVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
serotonin-gated monoatomic cation channel activity5-hydroxytryptamine receptor 3BHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential5-hydroxytryptamine receptor 3BHomo sapiens (human)
excitatory extracellular ligand-gated monoatomic ion channel activity5-hydroxytryptamine receptor 3BHomo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 1AHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 1AHomo sapiens (human)
receptor-receptor interaction5-hydroxytryptamine receptor 1AHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 1AHomo sapiens (human)
carboxypeptidase activityCarboxypeptidase MHomo sapiens (human)
zinc ion bindingCarboxypeptidase MHomo sapiens (human)
metallocarboxypeptidase activityCarboxypeptidase MHomo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(2) dopamine receptorHomo sapiens (human)
G-protein alpha-subunit bindingD(2) dopamine receptorHomo sapiens (human)
protein bindingD(2) dopamine receptorHomo sapiens (human)
heterotrimeric G-protein bindingD(2) dopamine receptorHomo sapiens (human)
dopamine bindingD(2) dopamine receptorHomo sapiens (human)
ionotropic glutamate receptor bindingD(2) dopamine receptorHomo sapiens (human)
identical protein bindingD(2) dopamine receptorHomo sapiens (human)
heterocyclic compound bindingD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(2) dopamine receptorHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 1DHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 1DHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 1BHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 1BHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 1BHomo sapiens (human)
voltage-gated calcium channel activity involved in regulation of presynaptic cytosolic calcium levels5-hydroxytryptamine receptor 1BHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 1BHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
virus receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein tyrosine kinase activator activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein-containing complex binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled receptor activity5-hydroxytryptamine receptor 1EHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 1EHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 1EHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 1EHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 1EHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 1FHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 1FHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 1FHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 7Homo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 7Homo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 7Homo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-1A adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1A adrenergic receptorHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 3AHomo sapiens (human)
serotonin-gated monoatomic cation channel activity5-hydroxytryptamine receptor 3AHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 3AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 3AHomo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
excitatory extracellular ligand-gated monoatomic ion channel activity5-hydroxytryptamine receptor 3AHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 5AHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 5AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 5AHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
protein bindingVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
ankyrin bindingVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
metal ion bindingVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
alpha-actinin bindingVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
voltage-gated calcium channel activity involved in cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
voltage-gated calcium channel activity involved SA node cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
protein bindingVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
calmodulin bindingVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
small molecule bindingVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
metal ion bindingVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
molecular function activator activityVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activity involved in cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
protein bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calmodulin bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
metal ion bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
alpha-actinin bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activity involved in cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activity involved in AV node cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 3DHomo sapiens (human)
serotonin-gated monoatomic cation channel activity5-hydroxytryptamine receptor 3DHomo sapiens (human)
excitatory extracellular ligand-gated monoatomic ion channel activity5-hydroxytryptamine receptor 3DHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential5-hydroxytryptamine receptor 3DHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 3CHomo sapiens (human)
serotonin-gated monoatomic cation channel activity5-hydroxytryptamine receptor 3CHomo sapiens (human)
excitatory extracellular ligand-gated monoatomic ion channel activity5-hydroxytryptamine receptor 3CHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential5-hydroxytryptamine receptor 3CHomo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
protein bindingMultidrug and toxin extrusion protein 1Homo sapiens (human)
organic cation transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-amino acid transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
thiamine transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
antiporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
putrescine transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
L-arginine transmembrane transporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
polyspecific organic cation:proton antiporter activityMultidrug and toxin extrusion protein 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (72)

Processvia Protein(s)Taxonomy
plasma membrane5-hydroxytryptamine receptor 3EHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 3EHomo sapiens (human)
serotonin-activated cation-selective channel complex5-hydroxytryptamine receptor 3EHomo sapiens (human)
neuron projection5-hydroxytryptamine receptor 3EHomo sapiens (human)
transmembrane transporter complex5-hydroxytryptamine receptor 3EHomo sapiens (human)
synapse5-hydroxytryptamine receptor 3EHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3EHomo sapiens (human)
plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
basal plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
membraneSolute carrier family 22 member 1 Homo sapiens (human)
basolateral plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
apical plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
lateral plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
presynapseSolute carrier family 22 member 1 Homo sapiens (human)
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
photoreceptor outer segmentVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
membraneVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
perikaryonVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3BHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 3BHomo sapiens (human)
serotonin-activated cation-selective channel complex5-hydroxytryptamine receptor 3BHomo sapiens (human)
cell surface5-hydroxytryptamine receptor 3BHomo sapiens (human)
transmembrane transporter complex5-hydroxytryptamine receptor 3BHomo sapiens (human)
synapse5-hydroxytryptamine receptor 3BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3BHomo sapiens (human)
neuron projection5-hydroxytryptamine receptor 3BHomo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1AHomo sapiens (human)
synapse5-hydroxytryptamine receptor 1AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1AHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 1AHomo sapiens (human)
extracellular regionCarboxypeptidase MHomo sapiens (human)
plasma membraneCarboxypeptidase MHomo sapiens (human)
cell surfaceCarboxypeptidase MHomo sapiens (human)
extracellular exosomeCarboxypeptidase MHomo sapiens (human)
side of membraneCarboxypeptidase MHomo sapiens (human)
extracellular spaceCarboxypeptidase MHomo sapiens (human)
Golgi membraneD(2) dopamine receptorHomo sapiens (human)
acrosomal vesicleD(2) dopamine receptorHomo sapiens (human)
plasma membraneD(2) dopamine receptorHomo sapiens (human)
ciliumD(2) dopamine receptorHomo sapiens (human)
lateral plasma membraneD(2) dopamine receptorHomo sapiens (human)
endocytic vesicleD(2) dopamine receptorHomo sapiens (human)
axonD(2) dopamine receptorHomo sapiens (human)
dendriteD(2) dopamine receptorHomo sapiens (human)
synaptic vesicle membraneD(2) dopamine receptorHomo sapiens (human)
sperm flagellumD(2) dopamine receptorHomo sapiens (human)
dendritic spineD(2) dopamine receptorHomo sapiens (human)
perikaryonD(2) dopamine receptorHomo sapiens (human)
axon terminusD(2) dopamine receptorHomo sapiens (human)
postsynaptic membraneD(2) dopamine receptorHomo sapiens (human)
ciliary membraneD(2) dopamine receptorHomo sapiens (human)
non-motile ciliumD(2) dopamine receptorHomo sapiens (human)
dopaminergic synapseD(2) dopamine receptorHomo sapiens (human)
GABA-ergic synapseD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor complexD(2) dopamine receptorHomo sapiens (human)
glutamatergic synapseD(2) dopamine receptorHomo sapiens (human)
presynaptic membraneD(2) dopamine receptorHomo sapiens (human)
plasma membraneD(2) dopamine receptorHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1DHomo sapiens (human)
synapse5-hydroxytryptamine receptor 1DHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1DHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 1DHomo sapiens (human)
endoplasmic reticulum5-hydroxytryptamine receptor 1BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1BHomo sapiens (human)
presynaptic membrane5-hydroxytryptamine receptor 1BHomo sapiens (human)
calyx of Held5-hydroxytryptamine receptor 1BHomo sapiens (human)
serotonergic synapse5-hydroxytryptamine receptor 1BHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 1BHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 1BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1BHomo sapiens (human)
neurofilament5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
caveola5-hydroxytryptamine receptor 2AHomo sapiens (human)
axon5-hydroxytryptamine receptor 2AHomo sapiens (human)
cytoplasmic vesicle5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
neuronal cell body5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendritic shaft5-hydroxytryptamine receptor 2AHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
cell body fiber5-hydroxytryptamine receptor 2AHomo sapiens (human)
glutamatergic synapse5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
synapse5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2CHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2CHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1EHomo sapiens (human)
synapse5-hydroxytryptamine receptor 1EHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1EHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 1EHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1FHomo sapiens (human)
synapse5-hydroxytryptamine receptor 1FHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1FHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 1FHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 7Homo sapiens (human)
trans-Golgi network membrane5-hydroxytryptamine receptor 7Homo sapiens (human)
synapse5-hydroxytryptamine receptor 7Homo sapiens (human)
dendrite5-hydroxytryptamine receptor 7Homo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 7Homo sapiens (human)
nucleusAlpha-1A adrenergic receptorHomo sapiens (human)
nucleoplasmAlpha-1A adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-1A adrenergic receptorHomo sapiens (human)
cytosolAlpha-1A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1A adrenergic receptorHomo sapiens (human)
caveolaAlpha-1A adrenergic receptorHomo sapiens (human)
nuclear membraneAlpha-1A adrenergic receptorHomo sapiens (human)
intracellular membrane-bounded organelleAlpha-1A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1A adrenergic receptorHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3AHomo sapiens (human)
cleavage furrow5-hydroxytryptamine receptor 3AHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 3AHomo sapiens (human)
serotonin-activated cation-selective channel complex5-hydroxytryptamine receptor 3AHomo sapiens (human)
synapse5-hydroxytryptamine receptor 3AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3AHomo sapiens (human)
transmembrane transporter complex5-hydroxytryptamine receptor 3AHomo sapiens (human)
neuron projection5-hydroxytryptamine receptor 3AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 5AHomo sapiens (human)
perikaryon5-hydroxytryptamine receptor 5AHomo sapiens (human)
postsynaptic specialization membrane5-hydroxytryptamine receptor 5AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 5AHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 5AHomo sapiens (human)
plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
Z discVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
L-type voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
cytoplasmVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
sarcoplasmic reticulumVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
T-tubuleVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
I bandVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
L-type voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
cytoplasmVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
postsynaptic densityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
Z discVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
dendriteVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
perikaryonVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
postsynaptic density membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
L-type voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3DHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 3DHomo sapiens (human)
serotonin-activated cation-selective channel complex5-hydroxytryptamine receptor 3DHomo sapiens (human)
synapse5-hydroxytryptamine receptor 3DHomo sapiens (human)
transmembrane transporter complex5-hydroxytryptamine receptor 3DHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3DHomo sapiens (human)
neuron projection5-hydroxytryptamine receptor 3DHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3CHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 3CHomo sapiens (human)
serotonin-activated cation-selective channel complex5-hydroxytryptamine receptor 3CHomo sapiens (human)
synapse5-hydroxytryptamine receptor 3CHomo sapiens (human)
transmembrane transporter complex5-hydroxytryptamine receptor 3CHomo sapiens (human)
neuron projection5-hydroxytryptamine receptor 3CHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3CHomo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
basolateral plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
apical plasma membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
membraneMultidrug and toxin extrusion protein 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (359)

Assay IDTitleYearJournalArticle
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1345154Rat 5-HT6 receptor (5-Hydroxytryptamine receptors)1998Journal of neurochemistry, Nov, Volume: 71, Issue:5
Identification of residues in transmembrane regions III and VI that contribute to the ligand binding site of the serotonin 5-HT6 receptor.
AID1346739Human 5-HT1F receptor (5-Hydroxytryptamine receptors)2005Naunyn-Schmiedeberg's archives of pharmacology, Mar, Volume: 371, Issue:3
[3H]LY334370, a novel radioligand for the 5-HT1F receptor. I. In vitro characterization of binding properties.
AID1345615Human 5-HT1A receptor (5-Hydroxytryptamine receptors)1999European journal of pharmacology, Mar-05, Volume: 368, Issue:2-3
Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors.
AID1346739Human 5-HT1F receptor (5-Hydroxytryptamine receptors)1993Proceedings of the National Academy of Sciences of the United States of America, Jan-15, Volume: 90, Issue:2
Cloning of another human serotonin receptor (5-HT1F): a fifth 5-HT1 receptor subtype coupled to the inhibition of adenylate cyclase.
AID1346739Human 5-HT1F receptor (5-Hydroxytryptamine receptors)1993Proceedings of the National Academy of Sciences of the United States of America, Mar-15, Volume: 90, Issue:6
Molecular cloning and functional expression of 5-HT1E-like rat and human 5-hydroxytryptamine receptor genes.
AID1345068Human 5-HT5A receptor (5-Hydroxytryptamine receptors)2001European journal of pharmacology, Apr-27, Volume: 418, Issue:3
Human 5-HT(5) receptors: the 5-HT(5A) receptor is functional but the 5-HT(5B) receptor was lost during mammalian evolution.
AID1346603Human 5-ht1e receptor (5-Hydroxytryptamine receptors)2004European journal of pharmacology, Jan-26, Volume: 484, Issue:2-3
Molecular cloning and pharmacological characterization of the guinea pig 5-HT1E receptor.
AID1346264Human 5-HT1B receptor (5-Hydroxytryptamine receptors)1996Journal of neurochemistry, Nov, Volume: 67, Issue:5
Two amino acid differences in the sixth transmembrane domain are partially responsible for the pharmacological differences between the 5-HT1D beta and 5-HT1E 5-hydroxytryptamine receptors.
AID624233Agonists at Human 5-Hydroxytryptamine receptor 5-HT1F1993Proceedings of the National Academy of Sciences of the United States of America, Mar-15, Volume: 90, Issue:6
Molecular cloning and functional expression of 5-HT1E-like rat and human 5-hydroxytryptamine receptor genes.
AID1346739Human 5-HT1F receptor (5-Hydroxytryptamine receptors)
AID624212Agonists at Human 5-Hydroxytryptamine receptor 5-ht5a2001European journal of pharmacology, Apr-27, Volume: 418, Issue:3
Human 5-HT(5) receptors: the 5-HT(5A) receptor is functional but the 5-HT(5B) receptor was lost during mammalian evolution.
AID1346603Human 5-ht1e receptor (5-Hydroxytryptamine receptors)1992Proceedings of the National Academy of Sciences of the United States of America, Jun-15, Volume: 89, Issue:12
Molecular cloning of a serotonin receptor from human brain (5HT1E): a fifth 5HT1-like subtype.
AID1345068Human 5-HT5A receptor (5-Hydroxytryptamine receptors)1994FEBS letters, Dec-05, Volume: 355, Issue:3
Cloning and characterisation of the human 5-HT5A serotonin receptor.
AID1346528Human 5-HT1D receptor (5-Hydroxytryptamine receptors)1996Molecular pharmacology, Dec, Volume: 50, Issue:6
Alniditan, a new 5-hydroxytryptamine1D agonist and migraine-abortive agent: ligand-binding properties of human 5-hydroxytryptamine1D alpha, human 5-hydroxytryptamine1D beta, and calf 5-hydroxytryptamine1D receptors investigated with [3H]5-hydroxytryptamin
AID1346603Human 5-ht1e receptor (5-Hydroxytryptamine receptors)1999European journal of pharmacology, Mar-05, Volume: 368, Issue:2-3
Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors.
AID1345061Mouse 5-HT5A receptor (5-Hydroxytryptamine receptors)2001European journal of pharmacology, Apr-27, Volume: 418, Issue:3
Human 5-HT(5) receptors: the 5-HT(5A) receptor is functional but the 5-HT(5B) receptor was lost during mammalian evolution.
AID1346264Human 5-HT1B receptor (5-Hydroxytryptamine receptors)2000Molecular pharmacology, Nov, Volume: 58, Issue:5
Inverse agonism and constitutive activity as functional correlates of serotonin h5-HT(1B) receptor/G-protein stoichiometry.
AID1345170Human 5-HT6 receptor (5-Hydroxytryptamine receptors)1996Journal of neurochemistry, Jan, Volume: 66, Issue:1
Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor.
AID1345061Mouse 5-HT5A receptor (5-Hydroxytryptamine receptors)1993Molecular pharmacology, Mar, Volume: 43, Issue:3
Mouse 5-hydroxytryptamine5A and 5-hydroxytryptamine5B receptors define a new family of serotonin receptors: cloning, functional expression, and chromosomal localization.
AID1345235Rat 5-HT7 receptor (5-Hydroxytryptamine receptors)1993Proceedings of the National Academy of Sciences of the United States of America, Sep-15, Volume: 90, Issue:18
Molecular cloning, characterization, and localization of a high-affinity serotonin receptor (5-HT7) activating cAMP formation.
AID1345291Human 5-HT7 receptor (5-Hydroxytryptamine receptors)1997British journal of pharmacology, Sep, Volume: 122, Issue:1
Cloning, expression and pharmacology of a truncated splice variant of the human 5-HT7 receptor (h5-HT7b).
AID1346264Human 5-HT1B receptor (5-Hydroxytryptamine receptors)1999European journal of pharmacology, Sep-10, Volume: 380, Issue:2-3
Identification of an amino acid residue important for binding of methiothepin and sumatriptan to the human 5-HT(1B) receptor.
AID1346264Human 5-HT1B receptor (5-Hydroxytryptamine receptors)1992Proceedings of the National Academy of Sciences of the United States of America, Apr-15, Volume: 89, Issue:8
Human serotonin 1D receptor is encoded by a subfamily of two distinct genes: 5-HT1D alpha and 5-HT1D beta.
AID624230Agonists at Human 5-Hydroxytryptamine receptor 5-ht1e1996Journal of neurochemistry, Nov, Volume: 67, Issue:5
Two amino acid differences in the sixth transmembrane domain are partially responsible for the pharmacological differences between the 5-HT1D beta and 5-HT1E 5-hydroxytryptamine receptors.
AID624230Agonists at Human 5-Hydroxytryptamine receptor 5-ht1e2004European journal of pharmacology, Jan-26, Volume: 484, Issue:2-3
Molecular cloning and pharmacological characterization of the guinea pig 5-HT1E receptor.
AID1346528Human 5-HT1D receptor (5-Hydroxytryptamine receptors)1992Proceedings of the National Academy of Sciences of the United States of America, Apr-15, Volume: 89, Issue:8
Human serotonin 1D receptor is encoded by a subfamily of two distinct genes: 5-HT1D alpha and 5-HT1D beta.
AID624233Agonists at Human 5-Hydroxytryptamine receptor 5-HT1F
AID1346264Human 5-HT1B receptor (5-Hydroxytryptamine receptors)2000Synapse (New York, N.Y.), Feb, Volume: 35, Issue:2
Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT(1B), 5-HT(1D) and dopamine D(2) and D(3) receptors. Significance for the modulation of frontocortical monoaminergic tr
AID624210Agonists at Human 5-Hydroxytryptamine receptor 5-HT1A1999European journal of pharmacology, Mar-05, Volume: 368, Issue:2-3
Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors.
AID624233Agonists at Human 5-Hydroxytryptamine receptor 5-HT1F1993Proceedings of the National Academy of Sciences of the United States of America, Jan-15, Volume: 90, Issue:2
Cloning of another human serotonin receptor (5-HT1F): a fifth 5-HT1 receptor subtype coupled to the inhibition of adenylate cyclase.
AID1345291Human 5-HT7 receptor (5-Hydroxytryptamine receptors)1993The Journal of biological chemistry, Nov-05, Volume: 268, Issue:31
Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase.
AID1346603Human 5-ht1e receptor (5-Hydroxytryptamine receptors)1993Proceedings of the National Academy of Sciences of the United States of America, Jan-15, Volume: 90, Issue:2
Cloning of another human serotonin receptor (5-HT1F): a fifth 5-HT1 receptor subtype coupled to the inhibition of adenylate cyclase.
AID1346528Human 5-HT1D receptor (5-Hydroxytryptamine receptors)1999European journal of pharmacology, Mar-05, Volume: 368, Issue:2-3
Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors.
AID624212Agonists at Human 5-Hydroxytryptamine receptor 5-ht5a1994FEBS letters, Dec-05, Volume: 355, Issue:3
Cloning and characterisation of the human 5-HT5A serotonin receptor.
AID1346264Human 5-HT1B receptor (5-Hydroxytryptamine receptors)1996Molecular pharmacology, Dec, Volume: 50, Issue:6
Alniditan, a new 5-hydroxytryptamine1D agonist and migraine-abortive agent: ligand-binding properties of human 5-hydroxytryptamine1D alpha, human 5-hydroxytryptamine1D beta, and calf 5-hydroxytryptamine1D receptors investigated with [3H]5-hydroxytryptamin
AID1346739Human 5-HT1F receptor (5-Hydroxytryptamine receptors)1999European journal of pharmacology, Mar-05, Volume: 368, Issue:2-3
Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors.
AID1346264Human 5-HT1B receptor (5-Hydroxytryptamine receptors)1999European journal of pharmacology, Mar-05, Volume: 368, Issue:2-3
Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors.
AID624233Agonists at Human 5-Hydroxytryptamine receptor 5-HT1F1999European journal of pharmacology, Mar-05, Volume: 368, Issue:2-3
Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors.
AID624230Agonists at Human 5-Hydroxytryptamine receptor 5-ht1e1999European journal of pharmacology, Mar-05, Volume: 368, Issue:2-3
Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors.
AID624230Agonists at Human 5-Hydroxytryptamine receptor 5-ht1e1993Proceedings of the National Academy of Sciences of the United States of America, Jan-15, Volume: 90, Issue:2
Cloning of another human serotonin receptor (5-HT1F): a fifth 5-HT1 receptor subtype coupled to the inhibition of adenylate cyclase.
AID1346528Human 5-HT1D receptor (5-Hydroxytryptamine receptors)2000Synapse (New York, N.Y.), Feb, Volume: 35, Issue:2
Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT(1B), 5-HT(1D) and dopamine D(2) and D(3) receptors. Significance for the modulation of frontocortical monoaminergic tr
AID1346603Human 5-ht1e receptor (5-Hydroxytryptamine receptors)1996Journal of neurochemistry, Nov, Volume: 67, Issue:5
Two amino acid differences in the sixth transmembrane domain are partially responsible for the pharmacological differences between the 5-HT1D beta and 5-HT1E 5-hydroxytryptamine receptors.
AID624230Agonists at Human 5-Hydroxytryptamine receptor 5-ht1e1992Proceedings of the National Academy of Sciences of the United States of America, Jun-15, Volume: 89, Issue:12
Molecular cloning of a serotonin receptor from human brain (5HT1E): a fifth 5HT1-like subtype.
AID1345235Rat 5-HT7 receptor (5-Hydroxytryptamine receptors)1993The Journal of biological chemistry, Aug-25, Volume: 268, Issue:24
Molecular cloning and expression of a 5-hydroxytryptamine7 serotonin receptor subtype.
AID624233Agonists at Human 5-Hydroxytryptamine receptor 5-HT1F2005Naunyn-Schmiedeberg's archives of pharmacology, Mar, Volume: 371, Issue:3
[3H]LY334370, a novel radioligand for the 5-HT1F receptor. I. In vitro characterization of binding properties.
AID1346528Human 5-HT1D receptor (5-Hydroxytryptamine receptors)1991Molecular pharmacology, Aug, Volume: 40, Issue:2
Primary structure and functional characterization of a human 5-HT1D-type serotonin receptor.
AID165752The compound was tested for functional activity by measuring the contraction of saphenous vein from New Zealand white rabbit1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Synthesis and serotonergic activity of arylpiperazide derivatives of serotonin: potent agonists for 5-HT1D receptors.
AID3835Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1A receptor in CHO-K1 cells1996Journal of medicinal chemistry, Dec-06, Volume: 39, Issue:25
Serotonin dimers: application of the bivalent ligand approach to the design of new potent and selective 5-HT(1B/1D) agonists.
AID224186In vitro evaluation in rabbit basilar artery for maximal response1993Journal of medicinal chemistry, Jun-25, Volume: 36, Issue:13
(+/-) 3-Amino-6-carboxamido-1,2,3,4-tetrahydrocarbazole: a conformationally restricted analogue of 5-carboxamidotryptamine with selectivity for the serotonin 5-HT1D receptor.
AID1864493Substrate activity at human OCT3 overexpressed in HEK293 cells assessed as uptake ratio incubated for 2 mins by LC-MS/MS analysis2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Substrates and Inhibitors of the Organic Cation Transporter 3 and Comparison with OCT1 and OCT2.
AID3829Binding affinity was measured on 5-hydroxytryptamine 1A receptor in AK cells transfected with human 5-HT1A gene labeled with [3H]-8-OH-DPAT1994Journal of medicinal chemistry, Sep-02, Volume: 37, Issue:18
5-(Nonyloxy)tryptamine: a novel high-affinity 5-HT1D beta serotonin receptor agonist.
AID4919Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.1996Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24
5-HT1D receptor agonist properties of novel 2-[5-[[(trifluoromethyl)sulfonyl]oxy]indolyl]ethylamines and their use as synthetic intermediates.
AID4867The compound was tested for intrinsic activity against 5-HT1D receptor1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Computer-aided design and synthesis of 5-substituted tryptamines and their pharmacology at the 5-HT1D receptor: discovery of compounds with potential anti-migraine properties.
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID5729Binding affinity was measured on 5-hydroxytryptamine 2C receptor in J1 cells transfected with rat 5-HT2C gene labeled with [3H]mesulergine1994Journal of medicinal chemistry, Sep-02, Volume: 37, Issue:18
5-(Nonyloxy)tryptamine: a novel high-affinity 5-HT1D beta serotonin receptor agonist.
AID6025Binding activity radioligand.1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
Synthesis and serotonergic activity of N,N-dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethylamine and analogues: potent agonists for 5-HT1D receptors.
AID3849In vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT radioligand1998Bioorganic & medicinal chemistry letters, Mar-17, Volume: 8, Issue:6
Dimerization of sumatriptan as an efficient way to design a potent, centrally and orally active 5-HT1B agonist.
AID63225The compound was tested for CNS binding affinity towards Dopamine receptor D2 from cloned Human membranes.1998Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13
Isochroman-6-carboxamides as highly selective 5-HT1D agonists: potential new treatment for migraine without cardiovascular side effects.
AID1221960Apparent permeability from apical to basolateral side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY3359792011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID4512Compound was evaluated for the affinity at 5-hydroxytryptamine 1B receptor1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.
AID395324Lipophilicity, log D at pH 7.4 by liquid chromatography2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID4873Binding affinity was measured against serotonin 5-hydroxytryptamine 1D receptor1994Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
5-[(3-nitropyrid-2-yl)amino]indoles: novel serotonin agonists with selectivity for the 5-HT1D receptor. Variation of the C3 substituent on the indole template leads to increased 5-HT1D receptor selectivity.
AID409602Inhibition of human aquaporin 4 M23 isoform expressed in Xenopus laevis oocytes2009Bioorganic & medicinal chemistry, Jan-01, Volume: 17, Issue:1
Identification of aquaporin 4 inhibitors using in vitro and in silico methods.
AID4626In vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1D receptor using [3H]5-CT radioligand1998Bioorganic & medicinal chemistry letters, Mar-17, Volume: 8, Issue:6
Dimerization of sumatriptan as an efficient way to design a potent, centrally and orally active 5-HT1B agonist.
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID4698Binding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HT1994Journal of medicinal chemistry, Sep-02, Volume: 37, Issue:18
5-(Nonyloxy)tryptamine: a novel high-affinity 5-HT1D beta serotonin receptor agonist.
AID1771268Toxicity in NewZealand rabbit Saphenous vein rings assessed as induction of vasoconstriction at 1 to 100 uM2021European journal of medicinal chemistry, Dec-05, Volume: 225Design, synthesis and biological evaluation of pyridinylmethylenepiperidine derivatives as potent 5-HT
AID4269Selectivity ratio against cloned human 5-hydroxytryptamine 1B receptor to that of human 5-hydroxytryptamine 1D receptor2003Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20
(R)-3-(N-methylpyrrolidin-2-ylmethyl)-5-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives as high affinity h5-HT1B/1D ligands.
AID4617Binding affinity towards cloned human 5-hydroxytryptamine 1D receptor2003Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20
(R)-3-(N-methylpyrrolidin-2-ylmethyl)-5-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives as high affinity h5-HT1B/1D ligands.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID4581Measurement of agonist induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with 5-hydroxytryptamine 1D receptor.1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
3-[2-(Pyrrolidin-1-yl)ethyl]indoles and 3-[3-(piperidin-1-yl)propyl]indoles: agonists for the h5-HT1D receptor with high selectivity over the h5-HT1B subtype.
AID444054Oral bioavailability in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID4865Binding affinity for 5-hydroxytryptamine 1D receptor in piglet caudate using [3H]5-HT1993Journal of medicinal chemistry, Jun-25, Volume: 36, Issue:13
(+/-) 3-Amino-6-carboxamido-1,2,3,4-tetrahydrocarbazole: a conformationally restricted analogue of 5-carboxamidotryptamine with selectivity for the serotonin 5-HT1D receptor.
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID231640Binding affinity ratio of cloned human 5-HT1B to that of human 5-HT1D2000Bioorganic & medicinal chemistry letters, Aug-07, Volume: 10, Issue:15
5-Alkyltryptamine derivatives as highly selective and potent 5-HT1D receptor agonists.
AID26362Ionization constant (pKa)2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID63680The compound was tested for CNS binding affinity towards Dopamine receptor D4 from cloned Human membranes; Inactive1998Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13
Isochroman-6-carboxamides as highly selective 5-HT1D agonists: potential new treatment for migraine without cardiovascular side effects.
AID4549The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1D receptor from cloned gorilla membranes expressed in cultured HEK 293 cells1998Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13
Isochroman-6-carboxamides as highly selective 5-HT1D agonists: potential new treatment for migraine without cardiovascular side effects.
AID234526Selectivity of compound towards human 5-HT1D receptor over human 5-HT1B receptor1999Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4
3-(Piperazinylpropyl)indoles: selective, orally bioavailable h5-HT1D receptor agonists as potential antimigraine agents.
AID409603Inhibition of human aquaporin 4 M23 isoform expressed in Xenopus laevis oocytes at 20 uM2009Bioorganic & medicinal chemistry, Jan-01, Volume: 17, Issue:1
Identification of aquaporin 4 inhibitors using in vitro and in silico methods.
AID4779Compound was tested for 5-hydroxytryptamine 1D like receptor-mediated vascular effect in rabbit saphenous vein (RSV)1998Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13
Benzylimidazolines as h5-HT1B/1D serotonin receptor ligands: a structure-affinity investigation.
AID4588Maximum stimulation of [35S]GTP-gamma-S, binding expressed relative to the maximal effect produced by 5-hydroxytryptamine 1D receptor.1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.
AID5609Displacement of [3H]DOB binding to 5-hydroxytryptamine 2A receptor from rat cortex homogenate1994Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
Synthesis and biological activity of 3-[2-(dimethylamino)ethyl]-5-[(1,1-dioxo-5-methyl-1,2,5-thiadiazolidin- 2-yl)-methyl]-1H-indole and analogues: agonists for the 5-HT1D receptor.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID4600Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1D receptor stably expressed in CHO cells1999Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4
Synthesis and serotonergic activity of 3-[2-(pyrrolidin-1-yl)ethyl]indoles: potent agonists for the h5-HT1D receptor with high selectivity over the h5-HT1B receptor.
AID234875Binding activity radioligand.1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
Synthesis and serotonergic activity of N,N-dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethylamine and analogues: potent agonists for 5-HT1D receptors.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID235510Selectivity value is the ratio between EC50 values of 5-HT1A and 5-HT1D receptors1994Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
5-[(3-nitropyrid-2-yl)amino]indoles: novel serotonin agonists with selectivity for the 5-HT1D receptor. Variation of the C3 substituent on the indole template leads to increased 5-HT1D receptor selectivity.
AID29811Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID4572Ability to inhibit forskolin-stimulated adenylate cyclase activity in Chinese hamster ovary (CHO) stable cell lines expressing human 5-hydroxytryptamine 1D receptor2003Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
Design, synthesis and biological activity of novel dimethyl-[2-[6-substituted-indol-1-yl]-ethyl]-amine as potent, selective, and orally-bioavailable 5-HT(1D) agonists.
AID4258Binding affinity towards cloned human 5-hydroxytryptamine 1B receptor2000Bioorganic & medicinal chemistry letters, Aug-07, Volume: 10, Issue:15
5-Alkyltryptamine derivatives as highly selective and potent 5-HT1D receptor agonists.
AID592681Apparent permeability across human Caco2 cell membrane after 2 hrs by LC-MS/MS analysis2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
QSAR-based permeability model for drug-like compounds.
AID673054Cardiovascular toxicity in human coronary arteries assessed as induction of vasoconstriction after 30 mins relative to serotonin2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
The synthesis and SAR of calcitonin gene-related peptide (CGRP) receptor antagonists derived from tyrosine surrogates. Part 1.
AID539464Solubility of the compound in 0.1 M phosphate buffer at 600 uM at pH 7.4 after 24 hrs by LC/MS/MS analysis2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Experimental solubility profiling of marketed CNS drugs, exploring solubility limit of CNS discovery candidate.
AID588208Literature-mined public compounds from Lowe et al phospholipidosis modelling dataset2010Molecular pharmaceutics, Oct-04, Volume: 7, Issue:5
Predicting phospholipidosis using machine learning.
AID234716Relative efficacy in stimulation of [35S]GTP-gamma-S, binding in CHO cells compared to 5-HT1999Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4
3-(Piperazinylpropyl)indoles: selective, orally bioavailable h5-HT1D receptor agonists as potential antimigraine agents.
AID771317Cellular uptake in human HEK293 cells assessed as human OCT1-mediated drug transport at 2.5 uM after 4 mins by LC-MS/MS analysis2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Identification of novel substrates and structure-activity relationship of cellular uptake mediated by human organic cation transporters 1 and 2.
AID624626Ratio of apparent permeability from basolateral to apical side over apical to basolateral side determined in MDR1-MDCKII cells2001The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2
Rational use of in vitro P-glycoprotein assays in drug discovery.
AID5997Binding activity radioligand.1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
Synthesis and serotonergic activity of N,N-dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethylamine and analogues: potent agonists for 5-HT1D receptors.
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID3912Binding activity radioligand.1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
Synthesis and serotonergic activity of N,N-dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethylamine and analogues: potent agonists for 5-HT1D receptors.
AID229104efficacy relative to 5-HT1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
3-[2-(Pyrrolidin-1-yl)ethyl]indoles and 3-[3-(piperidin-1-yl)propyl]indoles: agonists for the h5-HT1D receptor with high selectivity over the h5-HT1B subtype.
AID624628Drug-stimulated Pgp ATPase activity ratio determined in MDR1-Sf9 cell membranes with test compound at a concentration of 20uM2001The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2
Rational use of in vitro P-glycoprotein assays in drug discovery.
AID28233Fraction ionized (pH 7.4)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID1333949Decrease in plasma protein extravasation in fasted Harlan Sprague-Dawley rat model of migraine compound administered via oral gavage 1 hr prior to electrical stimulation of trigeminal ganglion measured after 15 mins by FITC-BSA based fluorescence assay2017Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
Discovery of dual positive allosteric modulators (PAMs) of the metabotropic glutamate 2 receptor and CysLT1 antagonists for treating migraine headache.
AID404704Displacement of [3H]5-hydroxytryptamine from rhesus monkey cloned 5HT1F receptor expressed in African green monkey COS7 cells by liquid scintillation counting2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Designing selective, high affinity ligands of 5-HT1D receptor by covalent dimerization of 5-HT1F ligands derived from 4-fluoro-N-[3-(1-methyl-4-piperidinyl)-1H-indol-5-yl]benzamide.
AID4591Intrinsic activity for 5-hydroxytryptamine 1D receptor1999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
N-Methyl-5-tert-butyltryptamine: A novel, highly potent 5-HT1D receptor agonist.
AID1221956Apparent permeability from apical to basolateral side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID5081Binding affinity for 5-hydroxytryptamine 2 receptor in rat cortex using [3H]- ketanserin1993Journal of medicinal chemistry, Jun-25, Volume: 36, Issue:13
(+/-) 3-Amino-6-carboxamido-1,2,3,4-tetrahydrocarbazole: a conformationally restricted analogue of 5-carboxamidotryptamine with selectivity for the serotonin 5-HT1D receptor.
AID4642Binding affinity in CHO-K1 cells transfected with human 5-hydroxytryptamine 1D receptor2001Journal of medicinal chemistry, Mar-01, Volume: 44, Issue:5
Discovery of 4-[3-(trans-3-dimethylaminocyclobutyl)-1H-indol-5-ylmethyl]-(4S)-oxazolidin-2-one (4991W93), a 5HT(1B/1D) receptor partial agonist and a potent inhibitor of electrically induced plasma extravasation.
AID1918193Dissociation constant, pKa of the compound2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
Identification of Organic Anion Transporter 2 Inhibitors: Screening, Structure-Based Analysis, and Clinical Drug Interaction Risk Assessment.
AID4750Binding affinity for 5-hydroxytryptamine 1C receptor in piglet choroid plexus using [3H]5-HT1993Journal of medicinal chemistry, Jun-25, Volume: 36, Issue:13
(+/-) 3-Amino-6-carboxamido-1,2,3,4-tetrahydrocarbazole: a conformationally restricted analogue of 5-carboxamidotryptamine with selectivity for the serotonin 5-HT1D receptor.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID4256In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor1999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
N-Methyl-5-tert-butyltryptamine: A novel, highly potent 5-HT1D receptor agonist.
AID342466Inhibition of AQP4 expressed in rat FRT cells assessed as osmotic water permeability at 10 uM by stopped-flow light scattering method2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Lack of aquaporin-4 water transport inhibition by antiepileptics and arylsulfonamides.
AID4583Compound was evaluated for its agonistic activity on 5-hydroxytryptamine 1D receptor1994Journal of medicinal chemistry, Sep-02, Volume: 37, Issue:18
5-(Nonyloxy)tryptamine: a novel high-affinity 5-HT1D beta serotonin receptor agonist.
AID233219Relative binding to serotonin 5-HT 1B and 5-HT 1D receptors1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1221962Efflux ratio of permeability from apical to basolateral side over basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY3359792011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID5452The compound was tested for binding affinity against 5-HT2A receptor1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Computer-aided design and synthesis of 5-substituted tryptamines and their pharmacology at the 5-HT1D receptor: discovery of compounds with potential anti-migraine properties.
AID4970Compound was evaluated for the affinity at 5-hydroxytryptamine 1E receptor1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.
AID4929Binding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HT1994Journal of medicinal chemistry, Sep-02, Volume: 37, Issue:18
5-(Nonyloxy)tryptamine: a novel high-affinity 5-HT1D beta serotonin receptor agonist.
AID395327Dissociation constant, pKa by capillary electrophoresis2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID4899Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor alpha expressed in CHO-K1 cells.1996Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24
5-HT1D receptor agonist properties of novel 2-[5-[[(trifluoromethyl)sulfonyl]oxy]indolyl]ethylamines and their use as synthetic intermediates.
AID342472Inhibition of AQP4 in mouse erythrocytes assessed as inhibition of osmotic water permeability at 100 uM after 15 mins by stopped-flow light scattering method2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Lack of aquaporin-4 water transport inhibition by antiepileptics and arylsulfonamides.
AID679753TP_TRANSPORTER: increase in Calcein-AM intracellular accumulation (Calcein-AM: ? uM, Sumatriptan: 100 uM) in MDR1-expressing MDCKII cells2002The Journal of pharmacology and experimental therapeutics, Dec, Volume: 303, Issue:3
Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs.
AID224012The compound was tested for its antagonist activity using rabbit saphenous vein (RSV) preparation2000Bioorganic & medicinal chemistry letters, Aug-07, Volume: 10, Issue:15
5-Alkyltryptamine derivatives as highly selective and potent 5-HT1D receptor agonists.
AID166850Binding affinity towards rabbit saphenous vein2001Journal of medicinal chemistry, Mar-01, Volume: 44, Issue:5
Discovery of 4-[3-(trans-3-dimethylaminocyclobutyl)-1H-indol-5-ylmethyl]-(4S)-oxazolidin-2-one (4991W93), a 5HT(1B/1D) receptor partial agonist and a potent inhibitor of electrically induced plasma extravasation.
AID4869The compound was tested for binding affinity against 5-HT1D receptor1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Computer-aided design and synthesis of 5-substituted tryptamines and their pharmacology at the 5-HT1D receptor: discovery of compounds with potential anti-migraine properties.
AID4574Compound was evaluated for the stimulation of [35S]GTP-gamma-S, binding in CHO cells expressing the 5-hydroxytryptamine 1D receptor.1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.
AID165751Maximum vein contraction obtained relative to 5-hydroxytryptamine1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Synthesis and serotonergic activity of arylpiperazide derivatives of serotonin: potent agonists for 5-HT1D receptors.
AID5691Binding activity radioligand.1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
Synthesis and serotonergic activity of N,N-dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethylamine and analogues: potent agonists for 5-HT1D receptors.
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID91481Binding constant against human serum albumin (HSA)2001Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25
Cheminformatic models to predict binding affinities to human serum albumin.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID624629Inhibition of Pgp expressed in MDR1-MDCKII cells measured by calcein-AM assay2001The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2
Rational use of in vitro P-glycoprotein assays in drug discovery.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID395326Fraction unbound in rat brain2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID234285Selectivity is the binding affinity towards human 5-HT1B receptor to that of human 5-HT1F receptor2001Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
N-[3-(2-Dimethylaminoethyl)-2-methyl-1H- indol-5-yl]-4-fluorobenzamide: a potent, selective, and orally active 5-HT(1F) receptor agonist potentially useful for migraine therapy.
AID4571Ability to inhibit forskolin-stimulated adenylate cyclase in a cell line expressing human 5-hydroxytryptamine 1D receptor1999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
N-Methyl-5-tert-butyltryptamine: A novel, highly potent 5-HT1D receptor agonist.
AID342469Inhibition of AQP4 expressed in rat FRT cells assessed as transepithelial osmotic water permeability at 100 uM by dye dilution method2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Lack of aquaporin-4 water transport inhibition by antiepileptics and arylsulfonamides.
AID438555Binding affinity to 5HT1A receptor2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Physical binding pocket induction for affinity prediction.
AID781328pKa (acid-base dissociation constant) as determined by Luan ref: Pharm. Res. 20052014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID4908Binding affinity to recombinant human 5-hydroxytryptamine 1D receptor alpha1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Synthesis and serotonergic activity of arylpiperazide derivatives of serotonin: potent agonists for 5-HT1D receptors.
AID234525Selectivity of compound for human 5-HT1D receptor over human 5-HT1B receptor1999Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4
Synthesis and serotonergic activity of 3-[2-(pyrrolidin-1-yl)ethyl]indoles: potent agonists for the h5-HT1D receptor with high selectivity over the h5-HT1B receptor.
AID4597Compound was evaluated for the affinity at 5-hydroxytryptamine 1D receptor1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.
AID342470Inhibition of AQP4 in wild type mouse brain gilial cells assessed as osmotic water permeability at 10 to 100 uM after 15 mins by calcein quenching assay2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Lack of aquaporin-4 water transport inhibition by antiepileptics and arylsulfonamides.
AID1221965Transporter substrate index of efflux ratio in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY3359792011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID4596Binding affinity by displacement to human cloned 5-hydroxytryptamine 1D receptor in CHO cells by [3H]5-HT displacement.1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
3-[2-(Pyrrolidin-1-yl)ethyl]indoles and 3-[3-(piperidin-1-yl)propyl]indoles: agonists for the h5-HT1D receptor with high selectivity over the h5-HT1B subtype.
AID721753Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells at 20 uM after 1.5 mins by fluorescence assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling.
AID3860Binding affinity for cloned human 5-hydroxytryptamine 1A receptor1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Synthesis and serotonergic activity of arylpiperazide derivatives of serotonin: potent agonists for 5-HT1D receptors.
AID234715Relative efficacy of compound in stimulation of [35S]GTP gamma-S binding in CHO cells compared to 5-HT1999Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4
Synthesis and serotonergic activity of 3-[2-(pyrrolidin-1-yl)ethyl]indoles: potent agonists for the h5-HT1D receptor with high selectivity over the h5-HT1B receptor.
AID248822Compound was tested for serotonergic activity on dual protein extravasation induced by electrical stimulation in guinea-pigs (3-7 nM/kg)2004Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18
2-(Anilino)imidazolines and 2-(benzyl)imidazoline derivatives as h5-HT1D serotonin receptor ligands.
AID4622Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1D receptor in CHO-K1 cells1996Journal of medicinal chemistry, Dec-06, Volume: 39, Issue:25
Serotonin dimers: application of the bivalent ligand approach to the design of new potent and selective 5-HT(1B/1D) agonists.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1180756Antimigraine activity in migraine patient assessed as pain relief incidence at 100 mg after 2 hrs (Rvb = 51.2%)2014Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
Calcitonin gene-related peptide receptor antagonists: new therapeutic agents for migraine.
AID5636Binding activity radioligand.1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
Synthesis and serotonergic activity of N,N-dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethylamine and analogues: potent agonists for 5-HT1D receptors.
AID4270Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor2001Journal of medicinal chemistry, Mar-01, Volume: 44, Issue:5
Discovery of 4-[3-(trans-3-dimethylaminocyclobutyl)-1H-indol-5-ylmethyl]-(4S)-oxazolidin-2-one (4991W93), a 5HT(1B/1D) receptor partial agonist and a potent inhibitor of electrically induced plasma extravasation.
AID5956Compound was evaluated for the affinity at 5-hydroxytryptamine 2C receptor1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.
AID1221963Transporter substrate index ratio of permeability from apical to basolateral side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY3359792011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID673053Cardiovascular toxicity in human coronary arteries assessed as induction of vasoconstriction after 30 mins2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
The synthesis and SAR of calcitonin gene-related peptide (CGRP) receptor antagonists derived from tyrosine surrogates. Part 1.
AID234286Selectivity is the binding affinity towards human 5-HT1D receptor to that of human 5-HT1F receptor2001Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
N-[3-(2-Dimethylaminoethyl)-2-methyl-1H- indol-5-yl]-4-fluorobenzamide: a potent, selective, and orally active 5-HT(1F) receptor agonist potentially useful for migraine therapy.
AID4292Compound was tested for the displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1D receptor stably expressed in CHO cells.1999Journal of medicinal chemistry, Dec-02, Volume: 42, Issue:24
3-[3-(Piperidin-1-yl)propyl]indoles as highly selective h5-HT(1D) receptor agonists.
AID4900Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor alpha measured as the reduction of forskolin-stimulated cAMP.1996Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24
5-HT1D receptor agonist properties of novel 2-[5-[[(trifluoromethyl)sulfonyl]oxy]indolyl]ethylamines and their use as synthetic intermediates.
AID681116TP_TRANSPORTER: transepithelial transport (basal to apical) in MDR1-expressing MDCKII cells2002The Journal of pharmacology and experimental therapeutics, Dec, Volume: 303, Issue:3
Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs.
AID232942Binding selectivity for 5-HT 1D receptor1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
3-[2-(Pyrrolidin-1-yl)ethyl]indoles and 3-[3-(piperidin-1-yl)propyl]indoles: agonists for the h5-HT1D receptor with high selectivity over the h5-HT1B subtype.
AID4632Binding affinity for human 5-hydroxytryptamine 1D receptor2000Bioorganic & medicinal chemistry letters, May-01, Volume: 10, Issue:9
5-Thienyltryptamine derivatives as serotonin 5-HT1B/1D receptor agonists: potential treatments for migraine.
AID4516Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.1999Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4
3-(Piperazinylpropyl)indoles: selective, orally bioavailable h5-HT1D receptor agonists as potential antimigraine agents.
AID444053Renal clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID4872Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1D receptor1994Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
5-[(3-nitropyrid-2-yl)amino]indoles: novel serotonin agonists with selectivity for the 5-HT1D receptor. Variation of the C3 substituent on the indole template leads to increased 5-HT1D receptor selectivity.
AID444050Fraction unbound in human plasma2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID4577Stimulation of [35S]GTP-gamma-S, binding in CHO cells expressing the 5-hydroxytryptamine 1D receptor1999Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4
Synthesis and serotonergic activity of 3-[2-(pyrrolidin-1-yl)ethyl]indoles: potent agonists for the h5-HT1D receptor with high selectivity over the h5-HT1B receptor.
AID4496Effective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell lines1998Bioorganic & medicinal chemistry letters, Mar-17, Volume: 8, Issue:6
Dimerization of sumatriptan as an efficient way to design a potent, centrally and orally active 5-HT1B agonist.
AID4484The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells1998Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13
Isochroman-6-carboxamides as highly selective 5-HT1D agonists: potential new treatment for migraine without cardiovascular side effects.
AID4510Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID444058Volume of distribution at steady state in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID166996Ability to contract saphenous vein of New Zealand white rabbit1994Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
Synthesis and biological activity of 3-[2-(dimethylamino)ethyl]-5-[(1,1-dioxo-5-methyl-1,2,5-thiadiazolidin- 2-yl)-methyl]-1H-indole and analogues: agonists for the 5-HT1D receptor.
AID771314Cellular uptake in human HEK293 cells assessed as human OCT2-mediated drug transport at 2.5 uM after 4 mins by LC-MS/MS analysis relative to passive uptake2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Identification of novel substrates and structure-activity relationship of cellular uptake mediated by human organic cation transporters 1 and 2.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID5201Binding affinity was measured on 5-hydroxytryptamine 2A receptor in GF6 cells transfected with human 5-HT2A gene labeled with [3H]ketanserin1994Journal of medicinal chemistry, Sep-02, Volume: 37, Issue:18
5-(Nonyloxy)tryptamine: a novel high-affinity 5-HT1D beta serotonin receptor agonist.
AID235511Selectivity value is the ratio between IC50 values of 5-HT1A and 5-HT1D receptors1994Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
5-[(3-nitropyrid-2-yl)amino]indoles: novel serotonin agonists with selectivity for the 5-HT1D receptor. Variation of the C3 substituent on the indole template leads to increased 5-HT1D receptor selectivity.
AID218766In vitro evaluation in the dog saphenous vein for maximal response1993Journal of medicinal chemistry, Jun-25, Volume: 36, Issue:13
(+/-) 3-Amino-6-carboxamido-1,2,3,4-tetrahydrocarbazole: a conformationally restricted analogue of 5-carboxamidotryptamine with selectivity for the serotonin 5-HT1D receptor.
AID29656Oral bioavailability in human2001Journal of medicinal chemistry, Mar-01, Volume: 44, Issue:5
Discovery of 4-[3-(trans-3-dimethylaminocyclobutyl)-1H-indol-5-ylmethyl]-(4S)-oxazolidin-2-one (4991W93), a 5HT(1B/1D) receptor partial agonist and a potent inhibitor of electrically induced plasma extravasation.
AID3709Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor1994Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
5-[(3-nitropyrid-2-yl)amino]indoles: novel serotonin agonists with selectivity for the 5-HT1D receptor. Variation of the C3 substituent on the indole template leads to increased 5-HT1D receptor selectivity.
AID4863Displacement of [3H]5-HT binding to 5-hydroxytryptamine 1D receptor from pig caudate membrane1994Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
Synthesis and biological activity of 3-[2-(dimethylamino)ethyl]-5-[(1,1-dioxo-5-methyl-1,2,5-thiadiazolidin- 2-yl)-methyl]-1H-indole and analogues: agonists for the 5-HT1D receptor.
AID1221958Efflux ratio of permeability from apical to basolateral side over basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID3809In vitro affinity at human cloned 5-hydroxytryptamine 1A receptor by [3H]8-OH-DPAT displacement.1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
Binding of O-alkyl derivatives of serotonin at human 5-HT1D beta receptors.
AID754786Vasoconstriction of human coronary artery2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Discovery of (R)-N-(3-(7-methyl-1H-indazol-5-yl)-1-(4-(1-methylpiperidin-4-yl)-1-oxopropan-2-yl)-4-(2-oxo-1,2-dihydroquinolin-3-yl)piperidine-1-carboxamide (BMS-742413): a potent human CGRP antagonist with superior safety profile for the treatment of migr
AID588220Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset2008Toxicology mechanisms and methods, , Volume: 18, Issue:2-3
Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.
AID444052Hepatic clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID26280Partition coefficient at pH 7.41994Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
Synthesis and biological activity of 3-[2-(dimethylamino)ethyl]-5-[(1,1-dioxo-5-methyl-1,2,5-thiadiazolidin- 2-yl)-methyl]-1H-indole and analogues: agonists for the 5-HT1D receptor.
AID234284Selectivity is the binding affinity towards human 5-HT1A receptor to that of human 5-HT1F receptor2001Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
N-[3-(2-Dimethylaminoethyl)-2-methyl-1H- indol-5-yl]-4-fluorobenzamide: a potent, selective, and orally active 5-HT(1F) receptor agonist potentially useful for migraine therapy.
AID588209Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset2010Chemical research in toxicology, Jul-19, Volume: 23, Issue:7
Developing structure-activity relationships for the prediction of hepatotoxicity.
AID404703Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1D receptor expressed in CHOK1 cells by liquid scintillation counting2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Designing selective, high affinity ligands of 5-HT1D receptor by covalent dimerization of 5-HT1F ligands derived from 4-fluoro-N-[3-(1-methyl-4-piperidinyl)-1H-indol-5-yl]benzamide.
AID29925Volume of distribution in man (IV dose)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID76310The level of 5-HT (prefrontal cortex) measured by means of HPCL with electrochemical detection methods at 25 (umol/kg, sc)1996Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24
5-HT1D receptor agonist properties of novel 2-[5-[[(trifluoromethyl)sulfonyl]oxy]indolyl]ethylamines and their use as synthetic intermediates.
AID721754Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID4977Compound was evaluated for the affinity at 5-hydroxytryptamine 1F receptor1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.
AID1221961Apparent permeability from basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY3359792011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID8002Observed volume of distribution2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID4569The compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Synthesis and serotonergic activity of arylpiperazide derivatives of serotonin: potent agonists for 5-HT1D receptors.
AID588210Human drug-induced liver injury (DILI) modelling dataset from Ekins et al2010Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 38, Issue:12
A predictive ligand-based Bayesian model for human drug-induced liver injury.
AID1864500Substrate activity at human OCT1 overexpressed in HEK293 cells at 2.5 uM incubated for 2 mins by LC-MS/MS analysis2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Substrates and Inhibitors of the Organic Cation Transporter 3 and Comparison with OCT1 and OCT2.
AID4245Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor2004Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3
3-(2-pyrrolidin-1-ylethyl)-5-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives as high affinity human 5-HT(1B/1D) ligands.
AID4511Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
3-[2-(Pyrrolidin-1-yl)ethyl]indoles and 3-[3-(piperidin-1-yl)propyl]indoles: agonists for the h5-HT1D receptor with high selectivity over the h5-HT1B subtype.
AID3731Binding affinity was measured against serotonin 5-hydroxytryptamine 1A receptor1994Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
5-[(3-nitropyrid-2-yl)amino]indoles: novel serotonin agonists with selectivity for the 5-HT1D receptor. Variation of the C3 substituent on the indole template leads to increased 5-HT1D receptor selectivity.
AID1864507Substrate activity at OCT1 (unknown origin) assessed as uptake ratio2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Substrates and Inhibitors of the Organic Cation Transporter 3 and Comparison with OCT1 and OCT2.
AID4931Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells.1996Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24
5-HT1D receptor agonist properties of novel 2-[5-[[(trifluoromethyl)sulfonyl]oxy]indolyl]ethylamines and their use as synthetic intermediates.
AID76293The level of 5-HIAA (hypothalamus) measured by means of HPCL with electrochemical detection methods at 25 (umol/kg, sc)1996Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24
5-HT1D receptor agonist properties of novel 2-[5-[[(trifluoromethyl)sulfonyl]oxy]indolyl]ethylamines and their use as synthetic intermediates.
AID624622Apparent permeability (Papp) from apical to basolateral side determined in MDR1-MDCKII cells2001The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2
Rational use of in vitro P-glycoprotein assays in drug discovery.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID5398The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 2A receptor from cloned Human membranes1998Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13
Isochroman-6-carboxamides as highly selective 5-HT1D agonists: potential new treatment for migraine without cardiovascular side effects.
AID4252Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells1996Journal of medicinal chemistry, Dec-06, Volume: 39, Issue:25
Serotonin dimers: application of the bivalent ligand approach to the design of new potent and selective 5-HT(1B/1D) agonists.
AID26304Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID4248Binding affinity towards cloned human 5-hydroxytryptamine 1B receptor2003Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20
(R)-3-(N-methylpyrrolidin-2-ylmethyl)-5-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives as high affinity h5-HT1B/1D ligands.
AID26301Partition coefficient (logD7.4)1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
Synthesis and serotonergic activity of 5-(oxadiazolyl)tryptamines: potent agonists for 5-HT1D receptors.
AID4864Displacement of radioligand [3H]5-HT binding to 5-hydroxytryptamine 1D receptor in pig caudate membrane1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
Synthesis and serotonergic activity of 5-(oxadiazolyl)tryptamines: potent agonists for 5-HT1D receptors.
AID233923Ratio of IC50 for h5-HT1B to h5-HT1D receptors1999Journal of medicinal chemistry, Dec-02, Volume: 42, Issue:24
3-[3-(Piperidin-1-yl)propyl]indoles as highly selective h5-HT(1D) receptor agonists.
AID771316Cellular uptake in human HEK293 cells assessed as human OCT2-mediated drug transport at 2.5 uM after 4 mins by LC-MS/MS analysis2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Identification of novel substrates and structure-activity relationship of cellular uptake mediated by human organic cation transporters 1 and 2.
AID342468Inhibition of AQP4 expressed in rat FRT cells assessed as osmotic water permeability at 100 uM after 60 mins by stopped-flow light scattering method2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Lack of aquaporin-4 water transport inhibition by antiepileptics and arylsulfonamides.
AID4514Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.1999Journal of medicinal chemistry, Dec-02, Volume: 42, Issue:24
3-[3-(Piperidin-1-yl)propyl]indoles as highly selective h5-HT(1D) receptor agonists.
AID444057Fraction escaping hepatic elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID5366Compound was evaluated for the affinity at 5-hydroxytryptamine 2A receptor1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.
AID29337Ionisation constant (pKa)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID4575Agonist-induced [35S]- GTPgammaS binding in CHO cells stably transfected with 5-hydroxytryptamine 1D receptor1999Journal of medicinal chemistry, Dec-02, Volume: 42, Issue:24
3-[3-(Piperidin-1-yl)propyl]indoles as highly selective h5-HT(1D) receptor agonists.
AID1221957Apparent permeability from basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1443980Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch2010Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2
Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
AID4627In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1D receptor1999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
N-Methyl-5-tert-butyltryptamine: A novel, highly potent 5-HT1D receptor agonist.
AID7783Unbound fraction (plasma)2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID4260Binding affinity for human 5-hydroxytryptamine 1B receptor2000Bioorganic & medicinal chemistry letters, May-01, Volume: 10, Issue:9
5-Thienyltryptamine derivatives as serotonin 5-HT1B/1D receptor agonists: potential treatments for migraine.
AID444056Fraction escaping gut-wall elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID4578Stimulation of [35S]GTP-gamma-S, binding in CHO cells expressing the 5-hydroxytryptamine 1D receptor1999Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4
3-(Piperazinylpropyl)indoles: selective, orally bioavailable h5-HT1D receptor agonists as potential antimigraine agents.
AID3858The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1A receptor from cloned Human membranes.1998Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13
Isochroman-6-carboxamides as highly selective 5-HT1D agonists: potential new treatment for migraine without cardiovascular side effects.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID22293Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID3980Binding affinity for 5-hydroxytryptamine 1A receptor in piglet hippocampus using [3H]8-OH-DPAT1993Journal of medicinal chemistry, Jun-25, Volume: 36, Issue:13
(+/-) 3-Amino-6-carboxamido-1,2,3,4-tetrahydrocarbazole: a conformationally restricted analogue of 5-carboxamidotryptamine with selectivity for the serotonin 5-HT1D receptor.
AID4460Compound was evaluated for the affinity at 5-hydroxytryptamine 1A receptor1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.
AID395325Lipophilicity, log P by microemulsion electrokinetic chromatography2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID4595Displacement of [3H]5-HT from human 5-hydroxytryptamine 1D receptor expressed in CHO cells1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.
AID1918194Lipophilicity, log D of the compound2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
Identification of Organic Anion Transporter 2 Inhibitors: Screening, Structure-Based Analysis, and Clinical Drug Interaction Risk Assessment.
AID76303The level of 5-HT (hypothalamus) measured by means of HPCL with electrochemical detection methods at 25 (umol/kg, sc)1996Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24
5-HT1D receptor agonist properties of novel 2-[5-[[(trifluoromethyl)sulfonyl]oxy]indolyl]ethylamines and their use as synthetic intermediates.
AID28235Unbound fraction (plasma)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID771315Cellular uptake in human HEK293 cells assessed as human OCT1-mediated drug transport at 2.5 uM after 4 mins by LC-MS/MS analysis relative to passive uptake2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Identification of novel substrates and structure-activity relationship of cellular uptake mediated by human organic cation transporters 1 and 2.
AID1526737Substrate activity at human OCT1 expressed in HEK293 cells assessed as increase in compound uptake by measuring Km incubated for 2 mins by LC-MS/MS analysis based Michaelis-Menten plot analysis relative to control empty vector transfected cells2019Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1.
AID1864506Substrate activity at human OCT2 overexpressed in HEK293 cells assessed as uptake ratio incubated for 2 mins by LC-MS/MS analysis2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Substrates and Inhibitors of the Organic Cation Transporter 3 and Comparison with OCT1 and OCT2.
AID230346Ratio of receptor binding affinities of 5-hydroxytryptamine 1D receptor alpha vs 5-hydroxytryptamine 1D receptor beta1996Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24
5-HT1D receptor agonist properties of novel 2-[5-[[(trifluoromethyl)sulfonyl]oxy]indolyl]ethylamines and their use as synthetic intermediates.
AID4858Binding activity radioligand.1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
Synthesis and serotonergic activity of N,N-dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethylamine and analogues: potent agonists for 5-HT1D receptors.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID3834Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1A receptor expressed in CHO-K1 cells.1996Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24
5-HT1D receptor agonist properties of novel 2-[5-[[(trifluoromethyl)sulfonyl]oxy]indolyl]ethylamines and their use as synthetic intermediates.
AID218767Intrinsic activity was measured as maximum contraction relative to 5-HT in dog saphenous vein1993Journal of medicinal chemistry, Jun-25, Volume: 36, Issue:13
(+/-) 3-Amino-6-carboxamido-1,2,3,4-tetrahydrocarbazole: a conformationally restricted analogue of 5-carboxamidotryptamine with selectivity for the serotonin 5-HT1D receptor.
AID4255In vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligand1998Bioorganic & medicinal chemistry letters, Mar-17, Volume: 8, Issue:6
Dimerization of sumatriptan as an efficient way to design a potent, centrally and orally active 5-HT1B agonist.
AID4924Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
Binding of O-alkyl derivatives of serotonin at human 5-HT1D beta receptors.
AID231294Relative binding affinity for 5-HT1B and 5-HT1D receptor2000Bioorganic & medicinal chemistry letters, May-01, Volume: 10, Issue:9
5-Thienyltryptamine derivatives as serotonin 5-HT1B/1D receptor agonists: potential treatments for migraine.
AID5404Binding activity radioligand.1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
Synthesis and serotonergic activity of N,N-dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethylamine and analogues: potent agonists for 5-HT1D receptors.
AID74051Ability to inhibit [125I]- albumin extravasation into dura following electrical stimulation of trigeminal ganglion of Guinea pig2001Journal of medicinal chemistry, Mar-01, Volume: 44, Issue:5
Discovery of 4-[3-(trans-3-dimethylaminocyclobutyl)-1H-indol-5-ylmethyl]-(4S)-oxazolidin-2-one (4991W93), a 5HT(1B/1D) receptor partial agonist and a potent inhibitor of electrically induced plasma extravasation.
AID165754Functional activity was determined by the contraction of New Zealand white rabbit saphenous vein.1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
Synthesis and serotonergic activity of N,N-dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethylamine and analogues: potent agonists for 5-HT1D receptors.
AID4515Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells1999Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4
Synthesis and serotonergic activity of 3-[2-(pyrrolidin-1-yl)ethyl]indoles: potent agonists for the h5-HT1D receptor with high selectivity over the h5-HT1B receptor.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID76288Effect of 25 (umol/kg, sc) compound on guinea pig rectal temperature (Hypothermia)1996Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24
5-HT1D receptor agonist properties of novel 2-[5-[[(trifluoromethyl)sulfonyl]oxy]indolyl]ethylamines and their use as synthetic intermediates.
AID3850In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1A receptor1999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
N-Methyl-5-tert-butyltryptamine: A novel, highly potent 5-HT1D receptor agonist.
AID4291Compound was tested for maximum stimulation of [35S]GTP-gamma-S, binding expressed relative to the maximal effect produced by 5-HT.1999Journal of medicinal chemistry, Dec-02, Volume: 42, Issue:24
3-[3-(Piperidin-1-yl)propyl]indoles as highly selective h5-HT(1D) receptor agonists.
AID4974In vitro effective concentration for inhibition of skolin-stimulated adenylate cyclase in cell line expressing human 5-hydroxytryptamine 1F receptor2001Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
N-[3-(2-Dimethylaminoethyl)-2-methyl-1H- indol-5-yl]-4-fluorobenzamide: a potent, selective, and orally active 5-HT(1F) receptor agonist potentially useful for migraine therapy.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID4975In vitro agonist potency against human 5-hydroxytryptamine 1F receptor2001Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
N-[3-(2-Dimethylaminoethyl)-2-methyl-1H- indol-5-yl]-4-fluorobenzamide: a potent, selective, and orally active 5-HT(1F) receptor agonist potentially useful for migraine therapy.
AID444055Fraction absorbed in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID19424Partition coefficient (logD7.4)2001Journal of medicinal chemistry, Jul-19, Volume: 44, Issue:15
ElogD(oct): a tool for lipophilicity determination in drug discovery. 2. Basic and neutral compounds.
AID5606Binding activity radioligand.1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
Synthesis and serotonergic activity of N,N-dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethylamine and analogues: potent agonists for 5-HT1D receptors.
AID77859The compound (25umol/kg, sc) was tested for hypothermic response for 60 mins in Guinea pig1998Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13
Isochroman-6-carboxamides as highly selective 5-HT1D agonists: potential new treatment for migraine without cardiovascular side effects.
AID63082Binding affinity for rat dopamine D2 receptor expressed in CHO-K1 cells1996Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24
5-HT1D receptor agonist properties of novel 2-[5-[[(trifluoromethyl)sulfonyl]oxy]indolyl]ethylamines and their use as synthetic intermediates.
AID4495Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells1996Journal of medicinal chemistry, Dec-06, Volume: 39, Issue:25
Serotonin dimers: application of the bivalent ligand approach to the design of new potent and selective 5-HT(1B/1D) agonists.
AID404707Selectivity for human 5HT1D receptor over human 5HT1B receptor2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Designing selective, high affinity ligands of 5-HT1D receptor by covalent dimerization of 5-HT1F ligands derived from 4-fluoro-N-[3-(1-methyl-4-piperidinyl)-1H-indol-5-yl]benzamide.
AID5878Binding affinity was measured on 5-hydroxytryptamine 3 receptor in NG-108 cells labeled with [3H]GR-656301994Journal of medicinal chemistry, Sep-02, Volume: 37, Issue:18
5-(Nonyloxy)tryptamine: a novel high-affinity 5-HT1D beta serotonin receptor agonist.
AID42945-hydroxytryptamine 1B receptor agonist potency determined in rabbit saphenous vein contraction model1998Bioorganic & medicinal chemistry letters, Mar-17, Volume: 8, Issue:6
Dimerization of sumatriptan as an efficient way to design a potent, centrally and orally active 5-HT1B agonist.
AID4601Displacement of [3H]5-HT binding from human 5-hydroxytryptamine 1D receptor expressed in CHO cells1999Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4
3-(Piperazinylpropyl)indoles: selective, orally bioavailable h5-HT1D receptor agonists as potential antimigraine agents.
AID29423HPLC capacity factor (k')2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID28236Unbound fraction (tissues)2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID404708Selectivity for human 5HT1D receptor over human 5HT1F receptor2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Designing selective, high affinity ligands of 5-HT1D receptor by covalent dimerization of 5-HT1F ligands derived from 4-fluoro-N-[3-(1-methyl-4-piperidinyl)-1H-indol-5-yl]benzamide.
AID4629Binding affinity for human 5-hydroxytryptamine 1D receptor2000Bioorganic & medicinal chemistry letters, Aug-07, Volume: 10, Issue:15
5-Alkyltryptamine derivatives as highly selective and potent 5-HT1D receptor agonists.
AID4640Binding activity radioligand.1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
Synthesis and serotonergic activity of N,N-dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethylamine and analogues: potent agonists for 5-HT1D receptors.
AID6281Displacement of [3H]-Q-ICS 205-930 binding to 5-hydroxytryptamine 3 receptor from rat cortex homogenate1994Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
Synthesis and biological activity of 3-[2-(dimethylamino)ethyl]-5-[(1,1-dioxo-5-methyl-1,2,5-thiadiazolidin- 2-yl)-methyl]-1H-indole and analogues: agonists for the 5-HT1D receptor.
AID19418Partition coefficient (logD7.4)1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
Synthesis and serotonergic activity of N,N-dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethylamine and analogues: potent agonists for 5-HT1D receptors.
AID1221964Transporter substrate index ratio of permeability from basolateral to apical side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY3359792011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID4615Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1D receptor2004Bioorganic & medicinal chemistry letters, Feb-09, Volume: 14, Issue:3
3-(2-pyrrolidin-1-ylethyl)-5-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives as high affinity human 5-HT(1B/1D) ligands.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1221982Fraction absorbed in human2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1546005Displacement of [3H]5-HT from recombinant human 5-HT7 receptor expressed in African green monkey COS7 cells2019European journal of medicinal chemistry, Dec-01, Volume: 183Structure-activity relationships of serotonin 5-HT
AID76298The level of 5-HIAA (prefrontal cortex) measured by means of HPCL with electrochemical detection methods at 25 (umol/kg, sc)1996Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24
5-HT1D receptor agonist properties of novel 2-[5-[[(trifluoromethyl)sulfonyl]oxy]indolyl]ethylamines and their use as synthetic intermediates.
AID476929Human intestinal absorption in po dosed human2010European journal of medicinal chemistry, Mar, Volume: 45, Issue:3
Neural computational prediction of oral drug absorption based on CODES 2D descriptors.
AID3978Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex1994Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
Synthesis and biological activity of 3-[2-(dimethylamino)ethyl]-5-[(1,1-dioxo-5-methyl-1,2,5-thiadiazolidin- 2-yl)-methyl]-1H-indole and analogues: agonists for the 5-HT1D receptor.
AID6358Compound was evaluated for the affinity at 5-hydroxytryptamine 3 receptor1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.
AID3975Binding activity radioligand.1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
Synthesis and serotonergic activity of N,N-dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethylamine and analogues: potent agonists for 5-HT1D receptors.
AID1180753Antimigraine activity in migraine patient assessed as pain freedom incidence at 100 mg after 2 hrs (Rvb = 15.3%)2014Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
Calcitonin gene-related peptide receptor antagonists: new therapeutic agents for migraine.
AID4983Binding affinity towards human 5-hydroxytryptamine 1F receptor was determined2001Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
N-[3-(2-Dimethylaminoethyl)-2-methyl-1H- indol-5-yl]-4-fluorobenzamide: a potent, selective, and orally active 5-HT(1F) receptor agonist potentially useful for migraine therapy.
AID624623Apparent permeability (Papp) from basolateral to apical side determined in MDR1-MDCKII cells2001The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2
Rational use of in vitro P-glycoprotein assays in drug discovery.
AID342471Inhibition of AQP4 in wild type mouse brain gilial cells assessed as reduction of osmotic equilibrium rate at 10 to 100 uM after 15 mins by calcein quenching assay relative to water permeability2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Lack of aquaporin-4 water transport inhibition by antiepileptics and arylsulfonamides.
AID404702Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Designing selective, high affinity ligands of 5-HT1D receptor by covalent dimerization of 5-HT1F ligands derived from 4-fluoro-N-[3-(1-methyl-4-piperidinyl)-1H-indol-5-yl]benzamide.
AID444051Total clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID224187Intrinsic activity was measured as maximum contraction relative to 5-HT in rabbit basilar artery1993Journal of medicinal chemistry, Jun-25, Volume: 36, Issue:13
(+/-) 3-Amino-6-carboxamido-1,2,3,4-tetrahydrocarbazole: a conformationally restricted analogue of 5-carboxamidotryptamine with selectivity for the serotonin 5-HT1D receptor.
AID342467Inhibition of AQP4 expressed in rat FRT cells assessed as osmotic water permeability at 100 uM after 15 mins by stopped-flow light scattering method2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Lack of aquaporin-4 water transport inhibition by antiepileptics and arylsulfonamides.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (2,271)

TimeframeStudies, This Drug (%)All Drugs %
pre-199029 (1.28)18.7374
1990's896 (39.45)18.2507
2000's805 (35.45)29.6817
2010's435 (19.15)24.3611
2020's106 (4.67)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 84.63

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index84.63 (24.57)
Research Supply Index7.96 (2.92)
Research Growth Index6.40 (4.65)
Search Engine Demand Index220.21 (26.88)
Search Engine Supply Index2.90 (0.95)

This Compound (84.63)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials461 (19.17%)5.53%
Reviews435 (18.09%)6.00%
Case Studies233 (9.69%)4.05%
Observational2 (0.08%)0.25%
Other1,274 (52.97%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (109)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Imigran STATdose - Japan Clinical Experience Study for Self-injection [NCT00356603]Phase 375 participants (Actual)Interventional2006-06-20Completed
A Study to Assess the Efficacy and Safety of Oral CL-H1T in the Treatment of Acute Migraine Pain, With or Without Aura, and the Prevention of Migraine Associated Nausea and Vomiting. [NCT03877718]Phase 2475 participants (Actual)Interventional2019-02-01Completed
Investigation of PACAP38-induced Headache and Rosacea-like Symptoms in Patients With Rosacea [NCT03878784]38 participants (Actual)Interventional2018-11-12Completed
A Multicenter, Randomized, Double-Blind, Placebo-Controlled Efficacy and Safety Study of DFN-02 in Episodic Migraine With or Without Aura [NCT02856802]Phase 2107 participants (Actual)Interventional2016-07-11Completed
A Randomized, Placebo-Controlled, Parallel-Groups, Outpatient Study to Compare the Efficacy and Safety of MK0462 5 mg p.o. and Sumatriptan 50 mg p.o. for the Acute Treatment of Migraine [NCT00897104]Phase 3933 participants (Actual)Interventional1995-08-31Completed
A Randomized, Double-Blind, Four-Period, Crossover Study to Evaluate the Cardiovascular Effect of Single Oral Doses of Lasmiditan When Coadministered With Single Oral Doses of Sumatriptan in Healthy Subjects [NCT03310411]Phase 140 participants (Actual)Interventional2017-10-17Completed
Impact of Migraine on Work Productivity in Patients Treated With a Combination Product Containing Sumatriptan and Naproxen Sodium or Triptan Monotherapy [NCT01381497]1 participants (Actual)Observational2010-03-31Completed
Sumatriptan as Treatment for Moderate to Severe Post-Traumatic Headache [NCT01854385]Phase 240 participants (Actual)Interventional2013-06-30Completed
The Role of Inflammation and Vasodilatation in PACAP38-induced Headache Using MRI on Healthy Subjects [NCT03585894]34 participants (Actual)Interventional2018-08-01Completed
Drug Use Investigation for IMIGRAN Tablet [NCT01376141]3,571 participants (Actual)Observational2001-09-30Completed
A Combination Product of Sumatriptan and Naproxen Sodium Versus Single-entity Oral Triptans: An Analysis of Real World Data [NCT01381523]1 participants (Actual)Observational2010-11-30Completed
A Randomized, Placebo-Controlled, Parallel-Groups, Outpatient Study to Examine the Safety, Tolerability, and Efficacy of Single Oral Doses of MK0462 5 mg, MK0462 10 mg, and Sumatriptan 100 mg for Acute Treatment of Migraine [NCT00898677]Phase 31,268 participants (Actual)Interventional1995-09-30Completed
Investigation of PACAP38 Induced Headache, Migraine and Flushing in Patients With Migraine [NCT03881644]37 participants (Actual)Interventional2018-07-17Completed
A Randomized, Double-blind, Placebo-controlled, Parallel-group Study to Evaluate the Efficacy and Tolerability of TREXIMA* (Sumatriptan Succinate/Naproxen Sodium) for a Single Moderate or Severe Headache in Adults Diagnosed With Probable Migraine Without [NCT00387881]Phase 3679 participants (Actual)Interventional2006-09-30Completed
The Effect of Sumatriptan and Placebo on Cilostazol Induced Headache. Development of a Pragmatic Migraine Model [NCT02486276]30 participants (Actual)Interventional2015-06-30Completed
The Effect of Sumatriptan and Placebo on Isosorbide-5-mononitrate Induced Headache. Development of a Pragmatic Migraine Model [NCT02485340]30 participants (Actual)Interventional2015-04-30Completed
A Multi-centre, Randomized, Double-blind, Parallel Group, Active and Placebo Controlled, Proof of Concept Study in Patients With Acute Migraine to Assess the Efficacy, Safety and Tolerability of Single Oral Doses of BGG492 [NCT00892203]Phase 275 participants (Actual)Interventional2009-04-30Completed
Pharmacokinetics and Safety of Commonly Used Drugs in Lactating Women and Breastfed Infants [NCT03511118]1,600 participants (Anticipated)Observational2018-10-04Recruiting
Phase 1, Randomized, Parallel-Group, Double-Blind, Placebo-Controlled, Single-Dose Study to Evaluate the Effect on Blood Pressure of AMG 334 Given Concomitantly With Subcutaneous Sumatriptan (Imitrex™) in Healthy Subjects [NCT02741310]Phase 134 participants (Actual)Interventional2016-02-22Completed
Evaluation of CGRP, Estrogen, Cortisol, VIP, α-Amylase, PGE2, PGI2 and ß-Endorphin Levels in Saliva of Menstrual Migraine Patients Before and After Treatment With Treximet™ [NCT01329562]Phase 441 participants (Actual)Interventional2011-05-31Completed
A Phase I, Open-Label, Two-Part Study of the Effect of Multiple-Dose Evobrutinib on Transporter Substrates Digoxin, Metformin, Rosuvastatin, and Sumatriptan Pharmacokinetics in Healthy Participants [NCT05064488]Phase 140 participants (Actual)Interventional2021-10-04Completed
A Phase I, Single Center, Open Label, Randomized, Single-Dose, Three-Way Crossover Study to Compare the Pharmacokinetics and Bioavailability of Two NP101 (Sumatriptan Iontophoretic Transdermal Patch) With an Oral Formulation of Imitrex in Healthy Voluntee [NCT01381796]Phase 163 participants (Actual)Interventional2009-12-31Completed
A Randomized, Double-Blind, Three Period, Cross-Over Study to Evaluate the Effect of Single Oral Doses of Lasmiditan When Coadministered With Single Oral Doses of Sumatriptan (Imitrex) in Healthy Male and Female Subjects [NCT03076970]Phase 142 participants (Actual)Interventional2017-03-21Completed
Effect of Sumatriptan on Levcromakalim-Induced Symptoms in Individuals With Migraine: A Randomized Double-Blind Two-Way Crossover Study [NCT05211050]20 participants (Anticipated)Interventional2022-02-15Recruiting
Open Label, Randomized, Two Way Crossover, Comparative Evaluation of Relative Bioavailabilities of Two Formulations of Sumatriptan Succinate Tablets 100 mg (Dr. Reddy's Laboratories Limited, India)With the Reference Formulation Imitrex Tablets 100 mg (Gla [NCT01269281]Phase 150 participants (Actual)Interventional2005-07-31Completed
A Single Center Randomized Open-Label Two Arm Crossover Study of Subject Productivity Improvement and Satisfaction With Migraine Treatment Using Treximet vs Usual Triptan [NCT01086358]Phase 460 participants (Actual)Interventional2009-09-30Completed
A Phase 1, Open Label, Single-Dose Safety, Pharmacokinetic, and Tolerability Study of Zecuity® in Adolescent Subjects With a History of Acute Migraine [NCT02684409]Phase 137 participants (Actual)Interventional2013-08-31Completed
Effect of Sumatriptan on the Postoperative Quality of Recovery After Elective Minimally Invasive Craniotomy [NCT01632657]40 participants (Actual)Interventional2012-06-30Completed
Single-Dose Food In Vivo Bioequivalence Study of Sumatriptan Succinate Tablets (100 mg; Mylan) to Imitrex® Tablets (100 mg; GlaxoSmithKline) in Healthy Volunteers [NCT00650247]Phase 157 participants (Actual)Interventional2004-11-30Completed
The Effect of Sumatriptan and Placebo on CGRP Induced Headache [NCT03542357]30 participants (Actual)Interventional2018-02-15Completed
Prospective Analgesic Compound Efficacy (PACE) Study [NCT02403687]300 participants (Actual)Observational [Patient Registry]2015-06-30Completed
A Single-Center, Open-label, Single-Arm Study to Evaluate the Effects of Repeat Doses of Subcutaneously Delivered Sumatriptan Via the Intraject System of Local Injection Site Signs in Healthy Adult Subjects. [NCT00620425]Phase 118 participants (Actual)Interventional2007-12-31Completed
Effects of Genetic Polymorphisms in the Organic Cation Transporter OCT1 on Cellular Uptake and Metabolism of Antidepressants and Other Organic Cationic Drugs [NCT02054299]Phase 148 participants (Actual)Interventional2013-04-30Completed
Mirtazapine vs Sumatriptan in the Treatment of Postdural Puncture Headache Following Obstetric Surgery Under Spinal Anesthesia: A Randomized Controlled Trial [NCT05108688]Phase 4210 participants (Anticipated)Interventional2021-11-15Recruiting
A Parallel Two Arm, Double Blinded Placebo Study, Examining the Efficacy of Sumatriptan With Naprosyn in the Treatment of Migraine With Aura [NCT00893594]30 participants (Anticipated)Interventional2010-10-31Recruiting
A Phase I, Open Label, Single-Dose, Four-Way Crossover Study Comparing the Pharmacokinetics of NP101 (Sumatriptan Iontophoretic Transdermal Patch) With an Oral Formulation of Imitrex® (50mg) in Migraine Subjects During an Acute Migraine Attack and During [NCT00723983]Phase 123 participants (Actual)Interventional2008-11-30Completed
A Randomized Clinical Trial to Compare Naproxen and Sumatriptan for Headache Patients Discharged From the Emergency Department (ED) [NCT00449787]Phase 4401 participants (Actual)Interventional2007-03-31Completed
Influence of Ubrogepant and Sumatriptan on the Dermal Blood Flow Response After a Histamine Skin Prick as Well as After the Topical Application of Cinnamaldehyde and Capsaicin [NCT05654298]20 participants (Actual)Interventional2022-03-15Completed
Is Theophylline More Effective Than Sumatriptan in the Treatment of Post-dural Puncture Headache: A Randomized Clinical Trial [NCT04257851]Phase 460 participants (Actual)Interventional2020-02-15Completed
The Sumatriptan and Naratriptan Pregnancy Registry [NCT01059604]868 participants (Actual)Observational [Patient Registry]2001-12-31Completed
Study TXA107977, a Long-Term Safety Study of a Combination Product Containing Sumatriptan Succinate and Naproxen Sodium for the Treatment of Migraine in Adolescents [NCT00488514]Phase 3656 participants (Actual)Interventional2007-07-13Completed
Evaluation of a Behavioral Program for Migraineurs in the Emergency Department. [NCT02643719]0 participants (Actual)Interventional2015-12-31Withdrawn(stopped due to Study team missed continuing review and study lapsed with out recruiting any subjects.)
TXA107979: A Randomized, Multicenter, Placebo-Controlled, Parallel Group Study to Evaluate the Efficacy and Safety of a Combination Product Containing Sumatriptan and Naproxen Sodium for the Acute Treatment of Migraine in Adolescents [NCT00843024]Phase 3589 participants (Actual)Interventional2008-12-31Completed
The Efficacy and Tolerability of NP101, a Sumatriptan Iontophoretic Transdermal Patch, in the Treatment of Acute Migraine: A Randomized, Double-Blind, Placebo-Controlled Study [NCT00724815]Phase 3530 participants (Actual)Interventional2009-01-31Completed
A Phase 3, Multicenter, Randomized, Double-blind, Placebo-controlled Study to Assess the Safety and Efficacy of ONZETRA® Xsail® (Sumatriptan Nasal Powder) for the Acute Treatment of Episodic Migraine With or Without Aura in Adolescents [NCT03338920]Phase 3159 participants (Actual)Interventional2017-11-02Terminated(stopped due to eDiary data collected not sufficient to utilize in the analysis of protocol endpoints)
Assessment of the Effect of Sumatriptan and Naproxen Sodium Combination Tablet, Sumatriptan Tablet, and Naproxen Sodium Tablet Treatment on Blood Pressure When Administered Intermittently for Six Months for the Acute Treatment of Migraine Attacks, With or [NCT00792636]Phase 4407 participants (Actual)Interventional2008-11-30Completed
A Phase 2 Study of the Safety and Effectiveness of a Single Oral Dose of NXN 188 for the Treatment of Moderate to Severe Migraine Headache With Aura [NCT00920686]Phase 2239 participants (Actual)Interventional2009-06-30Completed
A Phase I, Single Center, Open Label, Single-Dose, Five-Period Study to Compare the Pharmacokinetics of NP101 (Sumatriptan Iontophoretic Transdermal Patch) in Healthy Volunteers [NCT00720018]Phase 14 participants (Actual)Interventional2008-06-30Completed
Treximet in the Treatment of Chronic Migraine [NCT01090050]Phase 456 participants (Actual)Interventional2010-09-30Completed
A Phase I, Single Center, Open Label, Randomized, Single-Dose, Five-Way Crossover Study to Compare the Pharmacokinetics of NP101 (Sumatriptan Iontophoretic Transdermal Patch) With Three Formulations of Imitrex® in Healthy Volunteers [NCT00546650]Phase 125 participants (Actual)Interventional2007-11-30Completed
A Study of Combination Product (Sumatriptan Succinate and Naproxen Sodium) in Migraine Subjects Who Report Poor Response or Intolerance to Short Acting Triptans (Study 2 of 2) [NCT00382993]Phase 3169 participants (Actual)Interventional2006-12-31Completed
Comparison of Treximet and Imitrex as They Affect the Levels of Inflammatory Markers When the Patient is Actively Having a Migraine Headache. [NCT01916395]30 participants (Actual)Observational2009-12-31Completed
An Open Label, Bioequivalence Study of Sumatriptan Succinate 100 mg Tablets (Containing 140 mg of Sumatriptan Succinate Equivalent to 100 mg Sumatriptan) Under Fed Conditions [NCT00872274]32 participants (Actual)Interventional2008-07-31Completed
An Open-label, Randomized, 3-period Crossover Study to Evaluate Sumatriptan Pharmacokinetics for a TREXIMA™ (Sumatriptan Succinate / Naproxen Sodium) Tablet Followed by IMITREX® (Sumatriptan Succinate) Injection 4mg Administered Using the IMITREX STATdose [NCT00875784]Phase 130 participants (Actual)Interventional2008-05-06Completed
Effects of Serotonin Receptor Agonism on Blood Glucose Lowering: Proof of Concept in Humans [NCT04690270]Early Phase 112 participants (Anticipated)Interventional2021-01-04Not yet recruiting
A Study of Combination Product (Sumatriptan Succinate and Naproxen Sodium) in Migraine Subjects Who Report Poor Response or Intolerance to Short Acting Triptans (Study 1 of 2) [NCT00383162]Phase 3173 participants (Actual)Interventional2006-11-30Completed
A Randomized, Double-blind, Multi-center, Placebo-controlled, Cross-over Study to Determine the Consistency of Response for Trexima (Sumatriptan 85mg/Naproxen Sodium 500mg) Administered During the Mild Pain Phase for the Acute Treatment of Multiple Migrai [NCT00240630]Phase 3646 participants (Actual)Interventional2005-10-31Completed
A Multicentre, Double Blind, Double Dummy, Parallel Group, Placebo Controlled, Study of Two Dose Levels of Oral Eletriptan and Two Dose Levels Oral Sumatriptan Given for the Acute Treatment of Migraine(With and Without Aura). [NCT01986088]Phase 31,008 participants (Actual)Interventional1996-11-30Completed
A Multicenter, Double-blind, Placebo Controlled, Parallel Group, Study of Two Dose Levels of Oral Eletriptan and Two Dose Levels of of Oral Sumatriptan Given for the Acute Treatment of Migraine [NCT01986270]Phase 31,141 participants (Actual)Interventional1996-12-31Completed
A Randomized, Multicenter, Placebo-Controlled, Parallel Group Study to Evaluate the Efficacy and Safety of Oral Sumatriptan for the Acute Treatment of Migraine in Children and Adolescents [NCT00963937]Phase 3178 participants (Actual)Interventional2009-09-28Completed
Ictal and Interictal Inflammatory Markers in Migraine [NCT01138150]Phase 436 participants (Actual)Interventional2009-09-30Completed
An Open Label, Single Dose, Randomised, Parallel Group Pharmacokinetic Study to Evaluate a Combination Product Containing Naproxen Sodium and Sumatriptan in Adolescent Subjects With Migraine and Healthy Adult Subjects Administered at Three Doses. [NCT00989625]Phase 150 participants (Actual)Interventional2008-11-04Completed
A Multicenter, Randomized, Double-Blind, Placebo-Controlled Crossover Trial to Evaluate the Efficacy and Tolerability of Rizatriptan 10 mg for the Treatment of Acute Migraine in Sumatriptan Non-Responders [NCT00894556]Phase 3109 participants (Actual)Interventional2009-06-10Completed
A Two-Way Crossover, Open-Label, Single-Dose, Fasting Bioequivalence Study of Sumatriptan Succinate 100 mg Tablets Versus Imitrex® 100 mg Tablets in Normal Healthy Non-Smoking Male and Female Subjects [NCT00847405]Phase 128 participants (Actual)Interventional2003-03-31Completed
Single-Dose Fasting In Vivo Bioequivalence Study of Sumatriptan Succinate Tablets (100 mg; Mylan) to Imitrex® Tablets (100 mg; GlaxoSmithKline) in Healthy Volunteers [NCT00648466]Phase 155 participants (Actual)Interventional2004-11-30Completed
"An Open-label Study to Evaluate Completeness of Response Following Treatment With Treximet™ for Migraine" [NCT00893737]Phase 4147 participants (Actual)Interventional2009-06-30Completed
A Randomized, Double-blind, Single Migraine Attack, Placebo -Controlled, Patallel-group Multicenter Study to Evaluate the Efficacy and Tolerability or Trexima (Sumatriptan Succinate/Naproxen Sodium) Tablets vs Placebo When Administered During the Mild Pai [NCT00329459]Phase 3320 participants (Actual)Interventional2006-05-31Completed
An Evaluation of Treximet in the Treatment of Acute Migraine Headache: A Placebo-Controlled, Double-Blind, Crossover Study, Assessing Cognitive Function. [NCT00837044]30 participants (Anticipated)Interventional2009-02-28Recruiting
An Open Label, Bioequivalence Study of Sumatriptan Succinate 100 mg Tablets (Containing 140 mg of Sumatriptan Succinate Equivalent to 100 mg Sumatriptan) Under Fasting Conditions [NCT00872924]32 participants (Actual)Interventional2008-07-31Completed
A Random Controlled Trial a Comprehensive Migraine Intervention at the Time of Discharge From the Emergency Department After Treatment for Acute Migraine [NCT01071317]Phase 450 participants (Actual)Interventional2010-02-28Completed
Evaluation of the Efficacy of Treximet for Prevention of Post Traumatic Headache Associated With Cognitive Dysfunction [NCT01053507]Phase 423 participants (Actual)Interventional2010-05-31Terminated(stopped due to Enrollment rate was slower than anticipated.)
An Open-Label Phase 1 Study to Establish the Pharmacokinetics and Safety of Sumatriptan Succinate Administered Via the Sofusa™ DoseConnect™ System at Escalating Doses Compared to Oral Imitrex® Single 100 mg Dose in Healthy Subjects [NCT03229798]Phase 119 participants (Actual)Interventional2018-01-17Completed
An Open-Label, Repeat Dose Study Of The Safety Of Combo Formulation In The Treatment Of Multiple Episodes Of Acute Migraine Over 12 Months [NCT00442221]Phase 3500 participants Interventional2004-05-31Completed
TreximetTM in the Prevention and Modification of Disease Progression in Migraine [NCT01300546]Phase 440 participants (Actual)Interventional2010-12-31Completed
A Multi-center, Randomized, Double-blind, Parallel-group Single-dose, Placebo-controlled Study Comparing the Efficacy and Safety of Acetaminophen, Aspirin and Caffeine With Sumatriptan in the Acute Treatment of Migraine. [NCT01248468]Phase 4752 participants (Actual)Interventional2010-11-30Completed
A Randomized, Open Label, Crossover, Bioavailability Study to Compare Omexa Sumatriptan Transmucosal Sublingual Tablet Versus Commercial Imitrex® Sumatriptan Oral Tablet in Healthy Volunteers [NCT02954276]Phase 113 participants (Actual)Interventional2016-03-31Active, not recruiting
Cerebral Pharmacodynamic Effects of 5-HT1B Receptor Stimulation [NCT02932488]Phase 117 participants (Actual)Interventional2016-09-30Terminated(stopped due to Pilot study with sumatriptan found no significant changes in the primary outcome parameter (change in CBF))
A Double-Blind, Multicenter, Randomized, Placebo-Controlled Single Dose Study to Evaluate the Safety and Efficacy Opf Trexima in the Acute Treatment of Migraine Headaches [NCT00433732]Phase 31,400 participants Interventional2004-08-31Completed
A Double-Blind Multicenter, Randomized, Placebo-Controlled Single Dose Study to Evaluate the Safety and Efficacy of Trexima in the Acute Treatment of Migrane Headaches [NCT00434083]Phase 31,200 participants Interventional2004-07-31Completed
An Open Label, Single Dose, Parallel Group Study to Evaluate Absorption and Transit Characteristics of TREXIMA and RELPAX in Patients Inside and Outside of an Acute Migraine Attack. [NCT00385008]Phase 320 participants (Actual)Interventional2006-09-13Completed
A Randomized, Double-Blind, Placebo-Controlled, Parallel-Group Study Evaluating the Efficacy and Safety of a Single 20 mg Dose of Sumatriptan Powder Delivered Intranasally With the Bi-directional Device in Adults With Acute Migraine With or Without Aura [NCT01462812]Phase 3223 participants (Actual)Interventional2011-01-31Completed
A Phase 3 Open-Label Study to Assess Subcutaneous Self-Injection With Sumatriptan Succinate Using an Auto-injector During a Single Migraine Attack [NCT00510419]Phase 373 participants (Actual)Interventional2007-07-31Completed
Randomized, Double-Blind, Crossover, Comparator Pilot Study of DFN-11 Injection (Strength A vs. Strength B) for Rapidly Escalating Migraine [NCT02571049]Phase 224 participants (Actual)Interventional2015-09-30Completed
A Randomized, Two-Way, Single-Dose, Open-Label Study to Evaluate the Bioequivalence of a Test Tablet Formulation of Sumatriptan Succinate, (100mg), Compared to and Equivalent Dose of a Commercially Available Reference Drug Product (Imitrex®, GlaxoSmithKli [NCT00846885]Phase 128 participants (Actual)Interventional2004-08-31Completed
Neuropeptides in the Humane Intra- og Extracerebral Circulation - in Relation to Sumatriptan in Healthy Volunteers. [NCT00399633]16 participants (Actual)Interventional2007-01-31Completed
4mg StatDose Imitrex for Acute Treatment of Cluster Headache [NCT00399243]Phase 420 participants (Anticipated)Interventional2006-11-30Recruiting
Pretreatment With Sumatriptan on Cilostazol Induced Headache in Healthy Volunteers. Development of a Pragmatic Migraine Model [NCT03156920]30 participants (Actual)Interventional2017-05-23Completed
A Double-Blind, Randomized, Placebo-Controlled, 3-Period, Single Dose Crossover Study to Evaluate the Safety, Tolerability, and Blood Pressure Effect of an Oral Dose of Sumatriptan Alone and in Combination With MK0974 in Migraine Patients [NCT00701389]Phase 124 participants (Actual)Interventional2007-11-20Completed
A Randomized, Open-Label, Single-Dose, Four-way Crossover Study to Evaluate the Pharmacokinetics and Bioequivalence of Sumatriptan Delivered Via the Intraject System Versus IMITREX STATdose at Three Injection Sites in Healthy Adults [NCT00614029]Phase 154 participants (Actual)Interventional2006-12-31Completed
A Safety, Tolerability, and Efficacy Study of LY2590443 in the Treatment of Acute Migraine Headache [NCT00804973]Phase 2120 participants (Actual)Interventional2008-11-30Terminated(stopped due to Due to efficacy results of interim analysis)
Phase IIb: Double-Blind, Randomized, Placebo Controlled, Dose-ranging Trial of BMS-927711 for the Acute Treatment of Migraine [NCT01430442]Phase 21,026 participants (Actual)Interventional2011-10-31Completed
A Randomized, Double-blind, Multi-center, Placebo-controlled, Cross-over Study to Determine the Consistency of Response for Trexima* (Sumatriptan 85mg/Naproxen Sodium 500mg) Administered During the Mild Pain Phase for the Acute Treatment of Multiple Migra [NCT00240617]Phase 3623 participants (Actual)Interventional2005-10-31Completed
A Randomized, Double-blind, Single Migraine Attack, Placebo-controlled, Parallel-group Multicenter Study to Evaluate the Efficacy and Tolerability of Trexima (Sumatriptan Succinate.Naproxen Sodium) Tablets vs Placebo When Administered During the Mild Pain [NCT00329355]Phase 3351 participants (Actual)Interventional2006-05-31Completed
An Open-Label, Single-Dose, Randomized, Crossover Study to Compare the Bioavailability of the Intranasal Administration of 20 mg OPTINOSE SUMATRIPTAN With 20 mg IMITREX® (Sumatriptan) Nasal Spray, 100 mg IMITREX® (Sumatriptan) Oral Tablet and 6 mg IMITREX [NCT01507610]Phase 120 participants (Actual)Interventional2012-01-31Completed
Efficacy and Safety of Oral Sumatriptan Plus Oral Promethazine in Migraine Treatment: a Randomized, Double Blind Clinical Trial [NCT01814189]Phase 3350 participants (Actual)Interventional2013-01-31Completed
Treximet ™ Pharmacy Budget Impact Model Database Validation Study [NCT01332500]61,737 participants (Actual)Observational2009-07-31Completed
Study of Effects of Metoclopramide Versus Sumatriptan on Migraine Headache [NCT01791400]Phase 2124 participants (Actual)Interventional2009-07-31Completed
Open-label, 6 Month Crossover Study Evaluating Migraine Patient Satisfaction Comparing Treximet to 2 Aleve and 100mg Imitrex Taken Concomitantly [NCT01450995]Phase 450 participants (Actual)Interventional2009-12-31Completed
A Multicenter, Randomized, Double-blind, Placebo-controlled Clinical Trial of the Efficacy and Safety of Sumatriptan Naproxen Sodium Succinate Tablets for the Treatment of Acute Migraine Attacks. [NCT04948164]Phase 3240 participants (Anticipated)Interventional2018-08-01Recruiting
A PHASE 1, FIXED-SEQUENCE, OPEN LABEL STUDY TO EVALUATE THE EFFECT OF PF-06651600 ON PHARMACOKINETICS OF SINGLE DOSE SUMATRIPTAN IN HEALTHY PARTICIPANTS [NCT04355845]Phase 110 participants (Actual)Interventional2020-06-15Completed
A Single Dose, Placebo-Controlled, Ascending Dose Study to Determine the Safety, Tolerability and Pharmacokinetics of ALD403, a Humanized Anti-Calcitonin Gene-Related Peptide Monoclonal Antibody Administered by Intravenous Infusion and Subcutaneous Inject [NCT01579383]Phase 1104 participants (Actual)Interventional2012-04-30Completed
The Effect of Sumatriptan and Placebo Injection on Cilostazol Induced Headache [NCT03422796]30 participants (Actual)Interventional2017-11-01Completed
A Randomized, Double-Blind, Double-Dummy, Active-Controlled, Cross-Over Study Evaluating the Efficacy and Safety of 20 mg Sumatriptan Powder Delivered Intranasally With the Bi-directional Device Compared With 100 mg Sumatriptan Tablets in Adults With Acut [NCT01667679]Phase 3275 participants (Actual)Interventional2012-08-31Completed
Randomized, Double-Blind, and Placebo-Controlled Study to Assess a Single Dose of Low-Dose Naltrexone and Acetaminophen Combination Versus Sumatriptan in the Acute Treatment of Migraine With Nausea [NCT03185143]Phase 2/Phase 336 participants (Actual)Interventional2017-06-27Completed
A Multicenter, Open-label Evaluation of Treatment Satisfaction, Tolerability, Safety and Preference for Sumavel DosePro for Treatment of Migraine in Subjects Currently Treated With Triptans [NCT01016834]Phase 4246 participants (Actual)Interventional2009-11-30Completed
A Randomized, Double-Blind, Placebo-Controlled, Single Ascending Dose Phase 1 Study to Determine the Safety, Tolerability, and Pharmacokinetics of ALD1910, a Humanized Anti-Pituitary Adenylate Cyclase Activating Peptide (PACAP) Monoclonal Antibody [NCT04197349]Phase 196 participants (Actual)Interventional2019-09-24Completed
A Multi-Center, Open-Label, Single-dose, Single-Arm Study to Evaluate the Usability of Subcutaneously Administered Sumatriptan Delivered Via the Intraject® System in Adult Patients During Acute Migraine Attack [NCT00530517]Phase 254 participants (Actual)Interventional2007-09-30Completed
Multi-Center, Double-Blind, Placebo Controlled Pilot Study of VVD-101 for the Treatment of Delayed Alcohol-Induced Headaches [NCT02176655]Phase 231 participants (Actual)Interventional2014-07-31Completed
Comparison of Ketorolac Nasal Spray to Sumatriptan Nasal Spray and Placebo for Acute Treatment of Migraine (The KSPN Migraine Study) [NCT01807234]Phase 472 participants (Actual)Interventional2013-02-28Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00356603 (3) [back to overview]Percentage of Participants With Headache Relief at 60 Minutes Post Dose(Migraine) or 30 Minutes Post Dose(Cluster Headache)
NCT00356603 (3) [back to overview]Percentage of Participants With Investigator/Sub Investigator-rated Successful Self-injection Rate
NCT00356603 (3) [back to overview]Number of Participants With Subject-rated Acceptability of the Sumatriptan 3mg Kit Product
NCT00382993 (19) [back to overview]Complete Pain/Symptom-Free Assessed at Baseline, 2, 4, and 8 Hours Post-dose
NCT00382993 (19) [back to overview]Migraine Headache Pain Free at 0.5, 1, 4, and 8 Hours Post-Dose
NCT00382993 (19) [back to overview]Migraine-Associated Nausea Assessed at Baseline, 2, 4, and 8 Hours Post-dose
NCT00382993 (19) [back to overview]Migraine-Associated Phonophobia Assessed at Baseline, 2, 4, and 8 Hours Post-dose
NCT00382993 (19) [back to overview]Migraine-Associated Photophobia Assessed at Baseline, 2, 4, and 8 Hours Post-dose
NCT00382993 (19) [back to overview]Migraine-Associated Sinus Pain Assessed at Baseline, 2, 4, and 8 Hours Post-dose
NCT00382993 (19) [back to overview]Migraine-Free Assessment at 2, 4, and 8 Hours Post-dose
NCT00382993 (19) [back to overview]Recurrence of Any Migraine Headache Pain
NCT00382993 (19) [back to overview]Sustained Freedom From Migraine-Associated Neck Pain
NCT00382993 (19) [back to overview]Sustained Freedom From Migraine-Associated Phonophobia
NCT00382993 (19) [back to overview]Sustained Freedom From Migraine-Associated Photophobia
NCT00382993 (19) [back to overview]Sustained Freedom From Migraine-Associated Nausea
NCT00382993 (19) [back to overview]Sustained Freedom From Migraine Pain Between 2-24 Hours Post-dose
NCT00382993 (19) [back to overview]Sustained Freedom From Migraine
NCT00382993 (19) [back to overview]Sustained Complete Pain/Symptom-Free
NCT00382993 (19) [back to overview]Rescue Medication Use During 0 - 24 Hours Post-Dose
NCT00382993 (19) [back to overview]Migraine Headache Pain Free at 2 Hours Post-Dose
NCT00382993 (19) [back to overview]Migraine-Associated Neck Pain Assessed at Baseline, 2, 4, and 8 Hours Post-dose
NCT00382993 (19) [back to overview]Sustained Freedom From Migraine-Associated Sinus Pain
NCT00383162 (19) [back to overview]Sustained Freedom From Migraine-Associated Nausea
NCT00383162 (19) [back to overview]Sustained Freedom From Migraine Pain Between 2-24 Hours Post-dose
NCT00383162 (19) [back to overview]Sustained Freedom From Migraine
NCT00383162 (19) [back to overview]Sustained Complete Pain/Symptom-Free
NCT00383162 (19) [back to overview]Rescue Medication Used up to 24 Hours Post-dose
NCT00383162 (19) [back to overview]Pain-Free Assessment at 2 Hours Post-dose
NCT00383162 (19) [back to overview]Recurrence of Any Migraine Headache Pain
NCT00383162 (19) [back to overview]Pain-Free Assessment at 1/2, 1, 4, 8 Hours Post-dose
NCT00383162 (19) [back to overview]Migraine-Free Assessment at 2, 4, and 8 Hours Post-dose
NCT00383162 (19) [back to overview]Migraine-Associated Sinus Pain Assessed at Baseline, 2, 4, and 8 Hours Post-dose
NCT00383162 (19) [back to overview]Migraine-Associated Photophobia Assessed at Baseline, 2, 4, and 8 Hours Post-dose
NCT00383162 (19) [back to overview]Migraine-Associated Phonophobia Assessed at Baseline, 2, 4, and 8 Hours Post-dose
NCT00383162 (19) [back to overview]Migraine-Associated Neck Pain Assessed at Baseline, 2, 4, and 8 Hours Post-dose
NCT00383162 (19) [back to overview]Migraine-Associated Nausea Assessed at Baseline, 2, 4, and 8 Hours Post-dose
NCT00383162 (19) [back to overview]Complete Pain/Symptom-Free Assessed at Baseline, 2, 4, and 8 Hours Post-dose
NCT00383162 (19) [back to overview]Sustained Freedom From Migraine-Associated Sinus Pain
NCT00383162 (19) [back to overview]Sustained Freedom From Migraine-Associated Photophobia
NCT00383162 (19) [back to overview]Sustained Freedom From Migraine-Associated Phonophobia
NCT00383162 (19) [back to overview]Sustained Freedom From Migraine-Associated Neck Pain
NCT00385008 (15) [back to overview]Time to First Appearance of Sumatriptan, Naproxen and Eletriptan at the Proximal Small Intestine
NCT00385008 (15) [back to overview]Cmax for Eletriptan
NCT00385008 (15) [back to overview]Maximum Observed Drug Concentration (Cmax) for Sumatriptan and Naproxen
NCT00385008 (15) [back to overview]Mean Area Under the Drug Concentration Time Curve (AUC) From Time of Dosing Through 2 Hour Post-dose [AUC (0-2)], Through 24 Hour [AUC (0-24)] and AUC From Time of Dosing Extrapolated to Infinity [AUC (0-inf)] for Sumatriptan and Naproxen
NCT00385008 (15) [back to overview]Time of Maximal Drug Concentration (Tmax) for Sumatriptan and Naproxen
NCT00385008 (15) [back to overview]Small Intestine Transit and Residence (Time to 50% Through Intestine) of the Radioactive Markers Representing Sumatriptan, Naproxen and Eletriptan
NCT00385008 (15) [back to overview]Small Intestine Transit and Residence (Time to 50% Through Intestine) of the Radioactive Markers Representing Sumatriptan, Naproxen and Eletriptan
NCT00385008 (15) [back to overview]Number of Participants With Any Adverse Events (AEs) and Serious Adverse Events (SAEs)
NCT00385008 (15) [back to overview]Tmax for Eletriptan
NCT00385008 (15) [back to overview]Mean AUC (0-inf) and AUC (0-2) for Eletriptan
NCT00385008 (15) [back to overview]Time to First Appearance of Sumatriptan, Naproxen and Eletriptan at the Proximal Small Intestine
NCT00385008 (15) [back to overview]Time to Complete Dispersion of the Sumatriptan and Naproxen Portions of the TREXIMA Tablet and of the Relpax Tablet
NCT00385008 (15) [back to overview]Time to Complete Dispersion of the Sumatriptan and Naproxen Portions of the TREXIMA Tablet and of the Relpax Tablet
NCT00385008 (15) [back to overview]Time to 10%, 50%, 90% and Complete Gastric Empting of the Radioactive Markers Representing Sumatriptan, Naproxen and Eletriptan
NCT00385008 (15) [back to overview]Time to 10%, 50%, 90% and Complete Gastric Empting of the Radioactive Markers Representing Sumatriptan, Naproxen and Eletriptan
NCT00387881 (9) [back to overview]Sustained Headache Relief 2-24 Hours After Treatment
NCT00387881 (9) [back to overview]Freedom From Headache Pain at 0.5, 1, and 4 Hours After Treatment
NCT00387881 (9) [back to overview]Headache Relief at 4, 2, 1 and 0.5 Hours After Treatment
NCT00387881 (9) [back to overview]Incidence of Headache Associated: Neck Pain, Sinus Pain, Photophobia, Phonophobia, Nausea at Time Intervals of 4 and 2 Hours After Treatment
NCT00387881 (9) [back to overview]Intermediate Sustained Pain-Free: Post-dose at Intervals of 2-4 Hours and 1-2 Hours
NCT00387881 (9) [back to overview]Subjects Who Used Rescue Medication From 0 - 24 Hours After Treatment
NCT00387881 (9) [back to overview]Pain-Free at 2 Hours Post-dose and Sustained Pain-Free From 2-24 Hours Post-dose.
NCT00387881 (9) [back to overview]Medication Satisfaction: Mean Patient Perception of Migraine (PPMQ-R) Subscale Score
NCT00387881 (9) [back to overview]Intermediate Sustained Pain Relief: Post-dose at Intervals of 2-4 Hours and 1-2 Hours After Treatment
NCT00449787 (3) [back to overview]Headache-related Functional Disability
NCT00449787 (3) [back to overview]Numerical Rating Scale
NCT00449787 (3) [back to overview]Patient Satisfaction
NCT00488514 (27) [back to overview]Number of Treated Migraine Attacks With Photophobia, Phonophobia, Nausea, Neck Pain, Sinus Pain, and Vomiting
NCT00488514 (27) [back to overview]Number of Treated Migraine Attacks
NCT00488514 (27) [back to overview]Number of Participants With Hematocrit and Hemoglobin Values of Interest That Shifted From Normal at Baseline to Abnormal at the End of Study Visit
NCT00488514 (27) [back to overview]Number of Participants With the Indicated Drug-related Adverse Events
NCT00488514 (27) [back to overview]Number of Tablets Taken, After Which at Least One Adverse Event Occurred Within 3 or 5 Days of Dosing With That Combination Tablet
NCT00488514 (27) [back to overview]Mean Body Mass Index (BMI) for All Study Participants at the Indicated Time Points
NCT00488514 (27) [back to overview]Number of Total Migraines Headaches and Migraines Treated With the Combination Tablet
NCT00488514 (27) [back to overview]Number of Treated Attacks Classified as Migraine Pain-Free (MPF) Within 24 Hours of Dosing With the Combination Tablet
NCT00488514 (27) [back to overview]Number of Treated Attacks Classified as Migraine Pain-Free (MPF) Within 4 Hours of Dosing With a Combination Tablet
NCT00488514 (27) [back to overview]Average Number of Headaches, Migraine Attacks, and Treated Migraine Attacks Per Month
NCT00488514 (27) [back to overview]Mean Blood Pressure for All Study Participants at the Indicated Time Points
NCT00488514 (27) [back to overview]Number of Treated Attacks Classified as Migraine Pain-Free Within 4 Hours That Were Also Pain Free Within 2 Hours of Dosing With the Combination Tablet
NCT00488514 (27) [back to overview]Mean Change From Baseline in the Migraine Specific Quality of Life (QOL) Questionnaire for Adolescents (MSQ-A) Score at Months 3, 6, 9, and 12
NCT00488514 (27) [back to overview]Mean Heart Rate for All Study Participants at the Indicated Time Points
NCT00488514 (27) [back to overview]Mean Height for All Study Participants at the Indicated Time Points
NCT00488514 (27) [back to overview]Mean Weight for All Study Participants at the Indicated Time Points
NCT00488514 (27) [back to overview]Number of Migraine Attacks Rated With the Indicated Pain Severity
NCT00488514 (27) [back to overview]Number of Participants Categorized by Response to Each of the 3 Global Satisfaction Questions From the Patient Perception Migraine Questionaire-Revised (PPMQ-R) at Month 12
NCT00488514 (27) [back to overview]Number of Participants Categorized by Response to Each of the 3 Global Satisfaction Questions From the Patient Perception Migraine Questionnaire-Revised (PPMQ-R) at the Screening Visit
NCT00488514 (27) [back to overview]Number of Participants With Abnormal Electrocardiogram Findings at Screening and at the Final Visit as Assessed by the Investigator
NCT00488514 (27) [back to overview]Number of Participants With Alanine Aminotransferase (ALT), Aspartate Aminotransferase (AST), Creatinine, Potassium, and Blood Urea Nitrogen (BUN) Values of Interest That Shifted From Normal at Baseline to Abnormal at the End of Study Visit
NCT00488514 (27) [back to overview]Number of Participants With Any Adverse Event Categorized by Participant Age
NCT00488514 (27) [back to overview]Number of Participants With Any Adverse Event Categorized by Participant Gender
NCT00488514 (27) [back to overview]Number of Participants With Any Adverse Event Categorized by Participant Race
NCT00488514 (27) [back to overview]Number of Participants With Any Adverse Event Categorized by Severity
NCT00488514 (27) [back to overview]Number of Participants With Any Adverse Event Categorized Over Time
NCT00488514 (27) [back to overview]Number of Participants With Any Adverse Event That Occurred Within 3 or 5 Days of the First Dose of the Combination Tablet
NCT00620425 (1) [back to overview]The Number of Injections With Local Site Reactions (Bleeding, Swelling, Bruising and Erythema).
NCT00701389 (4) [back to overview]Number of Participants Who Experienced an Adverse Event During the Study
NCT00701389 (4) [back to overview]Number of Participants Who Were Discontinued From Any Study Period Due to an Adverse Event
NCT00701389 (4) [back to overview]Time-weighted Mean Arterial Pressure (Sumatriptan With Telcagepant Versus Sumatriptan Alone)
NCT00701389 (4) [back to overview]Time-weighted Mean Arterial Pressure (Telcagepant Versus Placebo)
NCT00724815 (4) [back to overview]Nausea Free at Two Hours
NCT00724815 (4) [back to overview]Pain Free at Two Hours
NCT00724815 (4) [back to overview]Phonophobia Free at Two Hours
NCT00724815 (4) [back to overview]Photophobia Free at Two Hours
NCT00792636 (15) [back to overview]Number of Participants With a Consecutive 2-day Average Diastolic Blood Pressure of >=90 mmHg
NCT00792636 (15) [back to overview]Number of Participants With a Consecutive 2-day Average Systolic Blood Pressure of >=140 mmHg During the Study
NCT00792636 (15) [back to overview]Number of Participants With an Increase of >=3 mmHg From the Baseline Diastolic Blood Pressure for the Average of Any Given Two-day Consecutive Collection of Blood Pressure Measurements
NCT00792636 (15) [back to overview]Time to the First Day With an Average Systolic Blood Pressure Increase of >=5 mmHg From the Baseline Systolic Blood Pressure
NCT00792636 (15) [back to overview]Time to the First Day With an Average Diastolic Blood Pressure Increase of >=3 mmHg From the Baseline Diastolic Blood Pressure
NCT00792636 (15) [back to overview]Number of Participants Withdrawn From the Study Due to Blood Pressure Changes
NCT00792636 (15) [back to overview]Number of Participants With an Increase of >=5 mmHg From the Baseline Systolic Blood Pressure for the Average of Any Given Two-day Consecutive Collection of Blood Pressure Measurements
NCT00792636 (15) [back to overview]Treatment Difference in Systolic and Diastolic Blood Pressure Mean Changes From Baseline at 6 Months Between Sumatriptan/Naproxen and Sumatriptan
NCT00792636 (15) [back to overview]Mean Change From Baseline in Systolic and Diastolic Blood Pressure at Month 6 for Sumatriptan/Naproxen for the ITT Subpopulation of Participants Treating With <30 Total Doses, 30-60 Total Doses, >=30, 60-90 Total Doses, and >90 Total Doses
NCT00792636 (15) [back to overview]Treatment Difference in Systolic and Diastolic Blood Pressure Mean Changes From Baseline at 6 Months Between Sumatriptan/Naproxen and Naproxen
NCT00792636 (15) [back to overview]Mean Change From Baseline in Systolic and Diastolic Blood Pressure at Month 6 for Sumatriptan/Naproxen for the ITT Subpopulation of Participants Treating, on Average, With <6, 6-10, >=6, 10-14, and >14 Doses Per Month
NCT00792636 (15) [back to overview]Mean Change From Baseline in Systolic and Diastolic Blood Pressure at Month 6 for Sumatriptan/Naproxen
NCT00792636 (15) [back to overview]Mean Change From Baseline in Systolic and Diastolic Blood Pressure at Month 6 for Sumatriptan/Naproxen for the ITT Subpopulation of Participants Treating, on Average, <4 Migraines, 4-6 Migraines, >=4 Migraines, and >6 Migraines Per Month
NCT00792636 (15) [back to overview]Mean Change From Baseline in Systolic and Diastolic Blood Pressure at Month 6 for Sumatriptan/Naproxen for the ITT Subpopulation of Participants Treating, on Average, <1.3 Times Per Migraine, 1.3-1.7 Times Per Migraine, and >1.7 Times Per Migraine
NCT00792636 (15) [back to overview]Mean Change From Baseline in Systolic and Diastolic Blood Pressure at Month 6 for Sumatriptan and Naproxen
NCT00804973 (10) [back to overview]Number of Participants With Recurrent Migraine Headache Within 24 or 48 Hours
NCT00804973 (10) [back to overview]Number of Participants With Photophobia
NCT00804973 (10) [back to overview]Number of Participants With Pain Relief Response
NCT00804973 (10) [back to overview]Number of Participants With Pain Free Response
NCT00804973 (10) [back to overview]Number of Participants With Nausea
NCT00804973 (10) [back to overview]Number of Participants With Headache Pain Free Response
NCT00804973 (10) [back to overview]Number of Participants With Phonophobia
NCT00804973 (10) [back to overview]Number of Participants With Vomiting
NCT00804973 (10) [back to overview]Number of Participants With Sustained Pain Relief Response
NCT00804973 (10) [back to overview]Number of Participants With Sustained Pain Free Response
NCT00843024 (17) [back to overview]Number of Participants Sustained Pain-free From 2-24 Hours
NCT00843024 (17) [back to overview]Number of Participants Sustained Phonophobia-free From 2-24 Hours
NCT00843024 (17) [back to overview]Mean Body Mass Index of Participants at Baseline Categorized by Age Group
NCT00843024 (17) [back to overview]Mean Age of Participants at Baseline Categorized by Age Group
NCT00843024 (17) [back to overview]Number of Participants Photophobia-free at 2 Hours Post-dose
NCT00843024 (17) [back to overview]Number of Female and Male Participants Categorized by Age Group
NCT00843024 (17) [back to overview]Number of Participants Nausea-free at 2 Hours Post-dose
NCT00843024 (17) [back to overview]Number of Participants of the Indicated Race Categorized by Age Group
NCT00843024 (17) [back to overview]Number of Participants Randomized to Double-blind Treatment in the Indicated Age Categories at Baseline
NCT00843024 (17) [back to overview]Number of Participants Sustained Nausea-free From 2-24 Hours
NCT00843024 (17) [back to overview]Mean Weight of Participants at Baseline Categorized by Age Group
NCT00843024 (17) [back to overview]Number of Participants Pain-free at 1 Hour Post-dose
NCT00843024 (17) [back to overview]Number of Participants Who Used Rescue Medication From 2 to 24 Hours Post Dose
NCT00843024 (17) [back to overview]Number of Participants Who Were Pain Free at 2 Hours Post-dose
NCT00843024 (17) [back to overview]Number of Participants Who Used Their First Dose of Rescue Medication Through the Indicated Time Points
NCT00843024 (17) [back to overview]Number of Participants Sustained Photophobia-free From 2-24 Hours
NCT00843024 (17) [back to overview]Number of Participants Phonophobia-free at 2 Hours Post-dose
NCT00846885 (3) [back to overview]Cmax (Maximum Observed Concentration of Drug Substance in Plasma)
NCT00846885 (3) [back to overview]AUC0-t (Area Under the Concentration-time Curve From Time Zero to Time of Last Measurable Concentration)
NCT00846885 (3) [back to overview]AUC0-inf (Area Under the Concentration-time Curve From Time Zero to Infinity)
NCT00847405 (3) [back to overview]AUC0-t (Area Under the Concentration-time Curve From Time Zero to Time of Last Measurable Concentration)
NCT00847405 (3) [back to overview]AUC0-inf (Area Under the Concentration-time Curve From Time Zero to Infinity)
NCT00847405 (3) [back to overview]Cmax (Maximum Observed Concentration of Drug Substance in Plasma)
NCT00893737 (3) [back to overview]Change in Scores From Completeness of Response Survey (CORS)
NCT00893737 (3) [back to overview]Paired T-test Indicating Greater Subject Satisfaction With Treximet Over Usual Pre-study Triptan as Determined by the Revised Patient Perception of Migraine Questionnaire (PPMQ-R)
NCT00893737 (3) [back to overview]Percent of Participants Reporting Treximet Provides Therapeutic Advantage Over Usual Pre-study Triptan
NCT00894556 (2) [back to overview]Pain Relief (PR)
NCT00894556 (2) [back to overview]Pain Freedom (PF)
NCT00897104 (7) [back to overview]Presence or Absence of Associated Symptoms (Photophobia, Phonophobia, Nausea, and Vomiting) at 2 Hours After Treatment
NCT00897104 (7) [back to overview]Pain Relief at 2 Hours After Treatment
NCT00897104 (7) [back to overview]Pain Free at 2 Hours After Treatment
NCT00897104 (7) [back to overview]Participants Who Used Escape Medication 2 Hours After the Treatment Dose
NCT00897104 (7) [back to overview]Time to Relief Within 2 Hours After Treatment
NCT00897104 (7) [back to overview]Lack of Functional Disability at 2 Hours After Treatment as Measured by the Level of Impairment in Daily Activities
NCT00897104 (7) [back to overview]Duration of Relief (Time to Recurrence From the Time of First Recorded Pain Relief [Grade = 0 or 1])
NCT00898677 (5) [back to overview]Functional Status at 2 Hours After Dose
NCT00898677 (5) [back to overview]Nausea at 2 Hours After Dose
NCT00898677 (5) [back to overview]Pain Relief at 2 Hours After Dose
NCT00898677 (5) [back to overview]Time to Relief Within 2 Hours After Dose
NCT00898677 (5) [back to overview]Pain Free at 2 Hours After Dose
NCT00920686 (5) [back to overview]24 Hours Post Administration - Incidence of Complete Headache Relief, Photophobia, Phonophobia and Nausea
NCT00920686 (5) [back to overview]Time (Hours) to First Use of Rescue Medication
NCT00920686 (5) [back to overview]2 Hours Post Administration - Incidence of Complete Headache Relief, Photophobia, Phonophobia and Nausea
NCT00920686 (5) [back to overview]Headache Relief and Recurrence (Observed Cases)
NCT00920686 (5) [back to overview]4 Hours Post Administration - Incidence of Complete Headache Relief, Photophobia, Phonophobia and Nausea
NCT00963937 (8) [back to overview]Percentage of Participants Who Used Rescue Medication Between the Time of Dosing and 240 Minutes Post-Treatment
NCT00963937 (8) [back to overview]Percentage of Participants Who Reported Pain Relief at 120 Minutes Post-Treatment
NCT00963937 (8) [back to overview]Percentage of Participants Who Were Nausea Free at 30, 60, 120, and 240 Minutes Post-Treatment
NCT00963937 (8) [back to overview]Percentage of Participants Who Were Photophobia Free at 30, 60, 120, and 240 Minutes Post-Treatment
NCT00963937 (8) [back to overview]Percentage of Participants Who Were Phonophobia Free at 30, 60, 120, and 240 Minutes Post-Treatment
NCT00963937 (8) [back to overview]Percentage of Participants Who Were Pain Free at 30, 60, 120, and 240 Minutes Post-Treatment
NCT00963937 (8) [back to overview]Percentage of Participants Who Were Free of Vomiting at 30, 60, 120, and 240 Minutes Post-Treatment
NCT00963937 (8) [back to overview]Percentage of Participants Who Reported Pain Relief at 30, 60, 120, and 240 Minutes Post-Treatment
NCT01016834 (3) [back to overview]Treatment Preference
NCT01016834 (3) [back to overview]Overall Satisfaction
NCT01016834 (3) [back to overview]Treatment Confidence
NCT01053507 (5) [back to overview]Change in Number of Associated Headache Symptoms
NCT01053507 (5) [back to overview]Headache Impact Test-6 (HIT-6) Score
NCT01053507 (5) [back to overview]Mental Efficiency Workload Test (MEWT) Performance Index
NCT01053507 (5) [back to overview]Migraine Specific Quality of Life Questionnaire (MSQ)
NCT01053507 (5) [back to overview]Headache Days
NCT01071317 (4) [back to overview]Number of Participants Who Returned to the Emergency Department for Management of Headache
NCT01071317 (4) [back to overview]Number of Participants Who Report They Are Comfortable With Disease Management, as Measured by a Three-item Likert Scale
NCT01071317 (4) [back to overview]Migraine Functional Impairment as Measured by Score on the Headache Impact Test 6 (HIT6) Scale
NCT01071317 (4) [back to overview]Number of Participants Who Report Satisfaction With Treatment, as Measured by a Three Item Likert Scale
NCT01086358 (4) [back to overview]Lost Activity Time
NCT01086358 (4) [back to overview]Workplace Productivity and Activity Impairment Scale (WPAI).
NCT01086358 (4) [back to overview]Lost Workplace Productivity
NCT01086358 (4) [back to overview]Favorable Response on Migraine-ACT
NCT01090050 (8) [back to overview]Migraine Headache Days With Greater Than 50% Reduction
NCT01090050 (8) [back to overview]Migraine Headache Duration From Onset to Pain Free
NCT01090050 (8) [back to overview]Migraine Headache Duration From Time of Treatment to Pain Free
NCT01090050 (8) [back to overview]Percent Change of Doses of Study Medication
NCT01090050 (8) [back to overview]Percent Change of Migraine Headache Days in All Treatment Periods Compared to Baseline
NCT01090050 (8) [back to overview]Percent Change of Migraine Headache Days Compared to Baseline
NCT01090050 (8) [back to overview]Migraine Disability Assessment(MIDAS)Questionnaire Total Score
NCT01090050 (8) [back to overview]Compliance With Lifestyle Changes
NCT01138150 (8) [back to overview]Change in the Total Serum Adiponectin (T-ADP)
NCT01138150 (8) [back to overview]High Molecular Weight (HMW)-Adiponectin (ADP)
NCT01138150 (8) [back to overview]High Molecular Weight (HMW): T-ADP
NCT01138150 (8) [back to overview]Leptin
NCT01138150 (8) [back to overview]Low Molecular Weight (LMW)-ADP
NCT01138150 (8) [back to overview]Low Molecular Weight (LMW):Total (T)-ADP
NCT01138150 (8) [back to overview]Middle Molecular Weight (MMW)-ADP
NCT01138150 (8) [back to overview]Resistin
NCT01248468 (4) [back to overview]Percent of Subjects Who Are Free of Nausea at 2 Hours.
NCT01248468 (4) [back to overview]Percent of Subjects Who Are Free of Phonophobia at 2 Hours.
NCT01248468 (4) [back to overview]Percent of Subjects Who Are Free of Photophobia at 2 Hours.
NCT01248468 (4) [back to overview]Percent of Subjects Who Are Pain Free at 2 Hours.
NCT01300546 (12) [back to overview]Migraine Attacks With 50% Reduction
NCT01300546 (12) [back to overview]Compliance With Lifestyle Changes
NCT01300546 (12) [back to overview]Percent Change of Headache Days Compared to Baseline
NCT01300546 (12) [back to overview]Doses of Study Medication
NCT01300546 (12) [back to overview]Migraine Attacks
NCT01300546 (12) [back to overview]Headache Days With Greater Than 50% Reduction
NCT01300546 (12) [back to overview]Migraine Disability Assessment Test (MIDAS)
NCT01300546 (12) [back to overview]Migraine Duration From Onset to Pain Free
NCT01300546 (12) [back to overview]Percent Change in Headache Days All Treatment Periods Compared to Baseline
NCT01300546 (12) [back to overview]Percent Change of Doses of Study Medication
NCT01300546 (12) [back to overview]Migraine Severity
NCT01300546 (12) [back to overview]Migraine Duration From Time of Treatment to Pain Free
NCT01329562 (18) [back to overview]CGRP Measured at Menstrual Migraine Headache Onset, Migraine Headache Free, and 24 Hours Migraine Headache Free in Responders vs Non-Responders
NCT01329562 (18) [back to overview]CGRP Measured at Menstrual Headache Onset, Migraine Headache Free, and 24 Hours Migraine Headache Free.
NCT01329562 (18) [back to overview]CGRP Measured at Baseline, Menstrual Migraine Headache Onset, and 2 Hours Post-Treatment in Responders vs Non-Responders
NCT01329562 (18) [back to overview]CGRP Measured at Baseline, Menstrual Migraine Headache Onset, and 2 Hours Post Treatment
NCT01329562 (18) [back to overview]Biomarkers Measured at Menstrual Migraine Headache Onset, Migraine Headache Free, and 24 Hours Migraine Headache Free.
NCT01329562 (18) [back to overview]Biomarkers Measured at Menstrual Migraine Headache Onset, Migraine Headache Free, and 24 Hours Migraine Headache Free in Responders vs Non-Responders
NCT01329562 (18) [back to overview]Biomarkers Measured at Baseline, Menstrual Migraine Headache Onset, and 2 Hours Post Treatment
NCT01329562 (18) [back to overview]Time to Pain-Free in Responders vs Non-Responders
NCT01329562 (18) [back to overview]Migraine Recurrence
NCT01329562 (18) [back to overview]Biomarkers Measured at Baseline, Menstrual Migraine Onset, and 2 Hours Post Treatment in Responders vs Non-Responders
NCT01329562 (18) [back to overview]Migraine Recurrence Responders vs Non-Responders
NCT01329562 (18) [back to overview]α-Amylase Measured at Menstrual Headache Onset, Migraine Headache Free, and 24 Hours Migraine Headache Free.
NCT01329562 (18) [back to overview]α-Amylase Measured at Baseline, Menstrual Migraine Headache Onset, and 2 Hours Post Treatment in Responders vs Non-Responders
NCT01329562 (18) [back to overview]α-Amylase Measured at Baseline, Menstrual Migraine Headache Onset, and 2 Hours Post Treatment
NCT01329562 (18) [back to overview]Correlation of Mean Estrogen Levels in Saliva and Urine Estradiol at Mid-Luteal and at Menstrual Migraine Headache Free in Responders vs Non-Responders
NCT01329562 (18) [back to overview]α-Amylase Measured at Menstrual Migraine Headache Onset, Migraine Headache Free, and 24 Hours Migraine Headache Free in Responders vs Non-Responders
NCT01329562 (18) [back to overview]Time to Pain Free
NCT01329562 (18) [back to overview]Correlation of Mean Estrogen Levels in Saliva and Urine Estradiol at Mid Luteal and at Menstrual Migraine Headache Free.
NCT01332500 (6) [back to overview]Mean Number of Triptan Tablets Per Participant in 6-month Follow-up Period: Treatment-switch Analysis
NCT01332500 (6) [back to overview]Mean Health Plan Cost Per Participant for Migraine-related Medications in 6-month Follow-up Period: Treatment-naïve Analysis
NCT01332500 (6) [back to overview]Mean Health Plan Cost Per Participant for Migraine-related Medications in 6-month Follow-up Period: Treatment-switch Analysis
NCT01332500 (6) [back to overview]Mean Number of Triptan Tablets Per Participant in 6-month Follow-up Period: Treatment-naïve Analysis
NCT01332500 (6) [back to overview]Mean Total Cost (Health Plan Plus Participant Copay Costs) Per Participant for Migraine-related Medications in 6-month Follow-up Period: Treatment-naïve Analysis
NCT01332500 (6) [back to overview]Mean Total Cost (Health Plan Plus Participant Copay Costs) Per Participant for Migraine-related Medications in 6-month Follow-up Period: Treatment-switch Analysis
NCT01430442 (5) [back to overview]Number of Participants Achieving Sustained Pain Freedom From 2 to 48 Hours Post Dose
NCT01430442 (5) [back to overview]Number of Participants With Total Migraine Freedom at 2 Hours Post Dose
NCT01430442 (5) [back to overview]Number of Pain Free Participants (Pain Freedom) at 2 Hours Post-dose
NCT01430442 (5) [back to overview]Number of Participants Achieving Sustained Pain Freedom From 2 to 24 Hours Post Dose
NCT01430442 (5) [back to overview]Number of Participants With Adverse Events (AEs), Serious Adverse Events (SAEs), and Discontinuation Due to Adverse Events
NCT01462812 (1) [back to overview]Headache Relief
NCT01667679 (27) [back to overview]Change From Baseline in Albumin and Total Protein at Visit 3 (up to Week 12) and Visit 4 (up to Week 24)
NCT01667679 (27) [back to overview]Change From Baseline in Alkaline Phosphatase (ALP) and Alanine Aminotransferase (ALT) at Visit 3 (up to Week 12) and Visit 4 (up to Week 24)
NCT01667679 (27) [back to overview]Change From Baseline in Aspartate Aminotransferase (AST) and Gamma Glutamyl Transferase (GGT) at Visit 3 (up to Week 12) and Visit 4 (up to Week 24)
NCT01667679 (27) [back to overview]Change From Baseline in Creatinine at Visit 3 (up to Week 12) and Visit 4 (up to Week 24)
NCT01667679 (27) [back to overview]Change From Baseline in Hematocrit at Visit 3 (up to 12 Weeks) and Visit 4 (up to 24 Weeks)
NCT01667679 (27) [back to overview]Change From Baseline in Hemoglobin at Visit 3 (up to 12 Weeks) and Visit 4 (up to 24 Weeks)
NCT01667679 (27) [back to overview]Change From Baseline in Pulse at Visit 3 (up to Week 12) and Visit 4 (up to Week 24)
NCT01667679 (27) [back to overview]Change From Baseline in Red Blood Cell Count at Visit 3 (up to Week 12) and Visit 4 (up to Week 24)
NCT01667679 (27) [back to overview]Change From Baseline in Sodium, Potassium, Chloride, Calcium, and Glucose at Visit 3 (up to Week 12) and Visit 4 (up to Week 24)
NCT01667679 (27) [back to overview]Change From Baseline in Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP) at Visit 3 (up to Week 12) and Visit 4 (up to Week 24)
NCT01667679 (27) [back to overview]Change From Baseline in Total Bilirubin at Visit 3 (up to Week 12) and Visit 4 (up to Week 24)
NCT01667679 (27) [back to overview]Change From Baseline in Urea at Visit 3 (up to Week 12) and Visit 4 (up to Week 24)
NCT01667679 (27) [back to overview]Change From Baseline in Urinalysis Values by Dipstick Method at Visit 3 (up to Week 12) and Visit 4 (up to Week 24)
NCT01667679 (27) [back to overview]Change From Baseline in White Blood Cell Count, Basinophils, Monocytes, Neutrophils, Lymphocytes, Eosinophils, and Platelets at Visit 3 (up to Week 12) and Visit 4 (up to Week 24)
NCT01667679 (27) [back to overview]Mean Change From Baseline in Clinical Disability Score at 10, 15, 30, 45, 60, 90, and 120 Minutes Post-dose
NCT01667679 (27) [back to overview]Mean Change in Headache Severity From Baseline to 10, 15, 30, 45, 60, 90, and 120 Minutes Post-dose
NCT01667679 (27) [back to overview]Mean Sum of Migraine Pain Intensity Differences (SPID)-30 for Headaches With a Baseline Intensity of Mild and Moderate/Severe
NCT01667679 (27) [back to overview]Number of Participants With Any Treatment-emergent Non-serious and Serious Adverse Event
NCT01667679 (27) [back to overview]Number of Participants With the Indicated 12-lead Electrocardiogram (ECG) Findings at Baseline, Visit 3 (up to Week 12), and Visit 4 (up to Week 24)
NCT01667679 (27) [back to overview]Number of Participants With the Indicated Concomitant Medications
NCT01667679 (27) [back to overview]Number of Participants With the Indicated Physical Examination Abnormalities at Baseline, Visit 3 (up to Week 12), and Visit 4 (up to Week 24)
NCT01667679 (27) [back to overview]Percentage of Attacks in Which Pain Freedom Was Achieved
NCT01667679 (27) [back to overview]Percentage of Attacks in Which Pain Reduction Was Achieved
NCT01667679 (27) [back to overview]Percentage of Attacks in Which Pain Relief Was Achieved
NCT01667679 (27) [back to overview]Number of Participants With the Indicated Amounts of Protein, Glucose, Ketones, Blood, and White Blood Cells (WBCs) in Urine at Baseline, Visit 3 (up to Week 12), and Visit 4 (up to Week 24)
NCT01667679 (27) [back to overview]Mean Sum of Migraine Pain Intensity Differences (SPID)-30
NCT01667679 (27) [back to overview]Median Time to Pain Freedom
NCT01807234 (10) [back to overview]Pain Freedom
NCT01807234 (10) [back to overview]Absence of Photophobia
NCT01807234 (10) [back to overview]Absence of Nausea
NCT01807234 (10) [back to overview]Absence of Allodynia
NCT01807234 (10) [back to overview]2- Hour Pain Relief
NCT01807234 (10) [back to overview]Time to Pain Relief
NCT01807234 (10) [back to overview]Absence of Phonophobia
NCT01807234 (10) [back to overview]Self-assessment of Disability: Percentage of Participants With Moderate or Severe Disability
NCT01807234 (10) [back to overview]Sustained Pain Freedom (SPF)
NCT01807234 (10) [back to overview]Sustained Pain Relief (SPR)
NCT01854385 (4) [back to overview]Change in Headache Relief
NCT01854385 (4) [back to overview]Adverse Events
NCT01854385 (4) [back to overview]Headache Diary Compliance
NCT01854385 (4) [back to overview]Sumatriptan Compliance
NCT02176655 (11) [back to overview]Number of Headaches Relieved
NCT02176655 (11) [back to overview]Headache Severity at Treatment, 30 Minutes and 1 Hour Post Treatment
NCT02176655 (11) [back to overview]Comparing Acute Hangover Scale Individual Symptoms With Headache Severity 2 Hours Post Treatment
NCT02176655 (11) [back to overview]Acute Hangover Scale Compared to Pain Severity 2 Hours Post Treatment
NCT02176655 (11) [back to overview]Satisfaction
NCT02176655 (11) [back to overview]Number of Participants With Consistent Response to VVD-101
NCT02176655 (11) [back to overview]Number of Headaches With Sustained Pain Freedom at Twenty Four Hours Post Treatment
NCT02176655 (11) [back to overview]Number of Headaches Relieved to Complete Pain Freedom at Two Hours Post Treatment
NCT02176655 (11) [back to overview]Number of Drinks Consumed Compared to Pain Severity 2 Hours Post Treatment
NCT02176655 (11) [back to overview]Meaningful Headache Relief
NCT02176655 (11) [back to overview]Headache Severity 2 Hours Post Treatment
NCT02571049 (1) [back to overview]The Percentage of Subjects Reporting Pain Freedom at 60 Minutes Post-treatment
NCT02741310 (6) [back to overview]Area Under the Concentration-time Curve From Time 0 to 6 Hours for Sumatriptan
NCT02741310 (6) [back to overview]Time-weighted Averages of Mean Arterial Pressure
NCT02741310 (6) [back to overview]Number of Participants With Adverse Events
NCT02741310 (6) [back to overview]Number of Participants Who Developed Anti-erenumab Antibodies
NCT02741310 (6) [back to overview]Maximum Observed Plasma Concentration (Cmax) of Sumatriptan
NCT02741310 (6) [back to overview]Area Under the Concentration-time Curve From Time 0 to Infinity for Sumatriptan
NCT02856802 (3) [back to overview]Number of Participants With Absence of Most Bothersome Symptom (MBS) Among Nausea, Photophobia and Phonophobia at 2 Hours (DB1)
NCT02856802 (3) [back to overview]Number of Participants With Headache Pain Freedom at 2 Hours Postdose in the Double-blind Treatment Period 2 (DB2)
NCT02856802 (3) [back to overview]Number of Participants Free From Headache Pain at 2 Hours After the First Dose of Study Medication Taken for a Migraine Attack With Moderate to Severe Headache Pain During the Double-blind Treatment Period 1 (DB1).
NCT03076970 (16) [back to overview]Pharmacodynamics- Change From Pre-dose to 24 Hours in ECGs: QTcB - Bazett's Correction Formula
NCT03076970 (16) [back to overview]Pharmacodynamics- Change From Pre-dose to 24 Hours in ECGs: QTcF - Fridericia's Correction Formula
NCT03076970 (16) [back to overview]Pharmacodynamics- Change From Pre-dose to 24 Hours in ECGs: Summary (Mean) PR Duration
NCT03076970 (16) [back to overview]Pharmacodynamics- Change From Pre-dose to 24 Hours in ECGs: Summary (Mean) QRS Duration
NCT03076970 (16) [back to overview]Pharmacodynamics- Change From Pre-dose to 24 Hours in ECGs: Summary (Mean) QT Duration
NCT03076970 (16) [back to overview]Pharmacodynamics- Change From Pre-dose to 24 Hours in ECGs: Summary (Mean) RR Duration
NCT03076970 (16) [back to overview]Pharmacodynamics- Change From Pre-dose to 24 Hours in Vital Signs: Diastolic Blood Pressure
NCT03076970 (16) [back to overview]Pharmacodynamics- Change From Pre-dose to 24 Hours in Vital Signs: Pulse Rate
NCT03076970 (16) [back to overview]Pharmacodynamics- Change From Pre-dose to 24 Hours in Vital Signs: Respiratory Rate
NCT03076970 (16) [back to overview]Pharmacodynamics- Change From Pre-dose to 24 Hours in Vital Signs: Systolic Blood Pressure
NCT03076970 (16) [back to overview]Pharmacokinetics - AUC0-t
NCT03076970 (16) [back to overview]Pharmacokinetics - Cmax
NCT03076970 (16) [back to overview]Pharmacokinetics - Tmax
NCT03076970 (16) [back to overview]Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)
NCT03076970 (16) [back to overview]Pharmacodynamics- Change From Pre-dose to 24 Hours in Vital Signs: Temperature
NCT03076970 (16) [back to overview]Pharmacodynamics- Change From Pre-dose to 24 Hours in ECGs: Heart Rate
NCT03310411 (3) [back to overview]Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0 ∞]) of Lasmiditan and Sumatriptan
NCT03310411 (3) [back to overview]Pharmacodynamics (PD): Change From Baseline in Mean 24-hour Systolic Blood Pressure (SBP)
NCT03310411 (3) [back to overview]Pharmacokinetics (PK): Maximum Observed Concentration (Cmax) of Lasmiditan and Sumatriptan
NCT03338920 (1) [back to overview]Number of Participants Who Were Headache Pain Free at 120 Minutes After Treatment

Percentage of Participants With Headache Relief at 60 Minutes Post Dose(Migraine) or 30 Minutes Post Dose(Cluster Headache)

Headache relief rate was the percentage of participants who showed effectiveness 60 minutes post dose (migraine) or 30 minutes post dose (cluster headache). Data for participants with percentage effectiveness along with 95% confidence interval has been presented. (NCT00356603)
Timeframe: 30 minutes or 60 Minutes after each administration

InterventionPercentage of participants (Number)
Migraine93.9
Cluster Headache93.9
Migraine + Cluster Headache93.9

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Percentage of Participants With Investigator/Sub Investigator-rated Successful Self-injection Rate

The investigator/sub investigator-rated successful self-injection rate was the percentage of participants who were able to use the kit as directed by the investigator/ sub investigator. The response was given as yes or no. Data for percentage of participants who were actually able to use the kit as directed has been presented. (NCT00356603)
Timeframe: Up to 2 months

InterventionPercentage of participants (Number)
Migraine100
Cluster Headache100
Migraine + Cluster Headache100

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Number of Participants With Subject-rated Acceptability of the Sumatriptan 3mg Kit Product

"The subject-rated acceptability of sumatriptan succinate injection 3 mg kit product had three questions, question 1 was Was the kit product easy to use?, question 2 was Do you want to use the kit product in the future? and question 3 was Do you consider that the kit product is necessary for the treatment of your illness?. The responses were given as yes or no. Data for number of participants who responded to the three questions as yes or no has been presented." (NCT00356603)
Timeframe: Up to 2 months

,,
InterventionParticipants (Count of Participants)
Question 1: YesQuestion 1: NoQuestion 2: YesQuestion 2: NoQuestion 3: YesQuestion 3: No
Cluster Headache330312294
Migraine321312312
Migraine + Cluster Headache651624606

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Complete Pain/Symptom-Free Assessed at Baseline, 2, 4, and 8 Hours Post-dose

"Number of participants who were completely symptom-free (migraine-free plus neck and sinus pain-free) at time of assessment. Complete pain/symptom-free was defined as migraine-free, neck pain-free, and sinus pain free." (NCT00382993)
Timeframe: Baseline, 2, 4, and 8 hours post-dose

,
InterventionParticipants (Number)
Complete Pain/Symptom-BaselineComplete Pain/Symptom-2 Hours Post-DoseComplete Pain/Symptom-4 Hours Post-DoseComplete Pain/Symptom-8 Hours Post-Dose
Placebo132121114106
Sumatriptan/Naproxen Sodium134947058

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Migraine Headache Pain Free at 0.5, 1, 4, and 8 Hours Post-Dose

Participants rated their pain severity using a four point scale where 0=no pain, 1=mild pain, 2=moderate pain, and 3=severe pain. Pain-free was a rating of 0 (no pain) at the specified time. (NCT00382993)
Timeframe: 0.5, 1, 4, and 8 Hours Post-Dose

,
InterventionParticipants (Number)
Pain Free at 0.5 Hour Post-DosePain Free at 1 Hour Post-DosePain Free at 4 Hours Post-DosePain Free at 8 Hours Post-Dose
Placebo3122332
Sumatriptan/Naproxen Sodium3338388

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Migraine-Associated Nausea Assessed at Baseline, 2, 4, and 8 Hours Post-dose

Number of participants who had nausea at the time of assessment. Resolution of an associated symptom was defined as a migraine headache symptom that was present at the time of treatment that was not present post-dose. Symptom resolution was defined only among subjects who treated while their symptom was present. (NCT00382993)
Timeframe: Baseline, 2, 4, and 8 hours

,
InterventionParticipants (Number)
Migraine Associated Nausea at BaselineMigraine Associated Nausea 2 Hours Post-DoseMigraine Associated Nausea 4 Hours Post-DoseMigraine Associated Nausea 8 Hours Post-Dose
Placebo40433527
Sumatriptan/Naproxen Sodium48331814

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Migraine-Associated Phonophobia Assessed at Baseline, 2, 4, and 8 Hours Post-dose

Number of participants who had phonophobia (sensitivity to noise) at the time of assessment. (NCT00382993)
Timeframe: Baseline, 2, 4, and 8 hours post-dose

,
InterventionParticipants (Number)
Migraine Assoc Phonophobia-BaselineMigraine Assoc Phonophobia 2 Hours Post-DoseMigraine Assoc Phonophobia 4 Hours Post-DoseMigraine Assoc Phonophobia 8 Hours Post-Dose
Placebo75685642
Sumatriptan/Naproxen Sodium80422720

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Migraine-Associated Photophobia Assessed at Baseline, 2, 4, and 8 Hours Post-dose

Number of participants who had photophobia (sensitivity to light) at the time of assessment. (NCT00382993)
Timeframe: Baseline, 2, 4, and 8 hours post-dose

,
InterventionParticipants (Number)
Migraine Assoc Photophobia-BaselineMigraine Assoc Photophobia 2 Hours Post-DoseMigraine Assoc Photophobia 4 Hours Post-DoseMigraine Assoc Photophobia 8 Hours Post-Dose
Placebo100846951
Sumatriptan/Naproxen Sodium101483125

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Migraine-Associated Sinus Pain Assessed at Baseline, 2, 4, and 8 Hours Post-dose

Number of participants who had sinus pain at the time of assessment. (NCT00382993)
Timeframe: Baseline, 2, 4, and 8 hours post-dose

,
InterventionParticipants (Number)
Migraine-Assoc Sinus Pain at BaselineMigraine-Assoc Sinus Pain at 2 Hours Post-DoseMigraine-Assoc Sinus Pain at 4 Hours Post-DoseMigraine-Assoc Sinus Pain at 8 Hours Post-Dose
Placebo47403627
Sumatriptan/Naproxen Sodium56412720

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Migraine-Free Assessment at 2, 4, and 8 Hours Post-dose

Migraine-free was defined as pain-free with no traditional migraine-associated symptoms (i.e.,photophobia, phonophobia, nausea and vomiting) at the time of the assessment. (NCT00382993)
Timeframe: 2, 4 , and 8 hours post-dose

,
InterventionParticipants (Number)
Migraine-Free at 2 Hours Post-DoseMigraine-Free at 4 Hours Post-DoseMigraine-Free at 8 Hours Post-Dose
Placebo152030
Sumatriptan/Naproxen Sodium467683

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Recurrence of Any Migraine Headache Pain

Recurrence is defined as the return of any migraine headache pain during the specified post-dose period, following a pain-free response at 2 hours. (NCT00382993)
Timeframe: 24 hours and 48 hours

,
InterventionParticipants (Number)
Recurrence by 24 hours post-doseRecurrence by 48 hours post-dose
Placebo56
Sumatriptan/Naproxen Sodium1313

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Sustained Freedom From Migraine-Associated Neck Pain

Sustained Freedom from Migraine-Associated Neck Pain was defined as the absence of neck pain from 2 to 24 hours post-dose. (NCT00382993)
Timeframe: 2 - 24 hours post-dose

InterventionParticipants (Number)
Placebo29
Sumatriptan/Naproxen Sodium65

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Sustained Freedom From Migraine-Associated Phonophobia

Sustained Freedom from Migraine-Associated Phonophobia was defined as the absence of phonophobia (sensitivity to noise) from 2 to 24 hours post-dose. (NCT00382993)
Timeframe: 2 - 24 hours post-dose

InterventionParticipants (Number)
Placebo30
Sumatriptan/Naproxen Sodium68

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Sustained Freedom From Migraine-Associated Photophobia

Sustained Freedom from Migraine-Associated Photophobia was defined as the absence of photophobia (sensitivity to light) from 2 to 24 hours post-dose. (NCT00382993)
Timeframe: 2 - 24 hours post-dose

InterventionParticipants (Number)
Placebo23
Sumatriptan/Naproxen Sodium65

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Sustained Freedom From Migraine-Associated Nausea

Sustained Freedom from Migraine-Associated Nausea was defined as the absence of nausea from 2 to 24 hours post-dose. (NCT00382993)
Timeframe: 2 - 24 hours post-dose

InterventionParticipants (Number)
Placebo38
Sumatriptan/Naproxen Sodium79

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Sustained Freedom From Migraine Pain Between 2-24 Hours Post-dose

Sustained freedom from migraine pain was defined as having no pain at 2 hours post-dose without the use of rescue medication; and without the recurrence of any pain or the use of any rescue medication 2 to 24 hours post-dose. (NCT00382993)
Timeframe: 2 - 24 Hours Post-Dose

InterventionParticipants (Number)
Placebo10
Sumatriptan/Naproxen Sodium41

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Sustained Freedom From Migraine

Migraine-free was defined as pain-free with no traditional migraine-associated symptoms (i.e.,photophobia, phonophobia, nausea). Sustained migraine-free was defined as migraine-free at 2 hours and sustained from 2 to 24 hours post dose without the use of rescue medication. (NCT00382993)
Timeframe: 2 - 24 hours post-dose

InterventionParticipants (Number)
Placebo8
Sumatriptan/Naproxen Sodium34

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Sustained Complete Pain/Symptom-Free

Sustained Complete Pain/Symptom-Free was defined as completely symptom-free (migraine-free plus neck and sinus pain-free) at 2 hours and sustained from 2 to 24 hours without the use of rescue medication. (NCT00382993)
Timeframe: 2 - 24 hours post-dose

InterventionParticipants (Number)
Placebo7
Sumatriptan/Naproxen Sodium30

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Rescue Medication Use During 0 - 24 Hours Post-Dose

A rescue medication was defined as an additional medication taken for the treatment of migraine headache pain symptoms associated with the attack. Allowed were a single dose of either: sumatriptan (50mg or 100mg), OR naproxen sodium (max 550mg), OR, an over-the-counter pain-reliever (per label). (NCT00382993)
Timeframe: 0-24 Hours Post-Dose

InterventionParticipants (Number)
Placebo72
Sumatriptan/Naproxen Sodium29

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Migraine Headache Pain Free at 2 Hours Post-Dose

Participants rated their pain severity using a four point scale where 0=no pain, 1=mild pain, 2=moderate pain, and 3=severe pain. Pain-free was a rating of 0 (no pain) at the specified time. (NCT00382993)
Timeframe: 2 Hours Post-Dose

InterventionParticipants (Number)
Placebo19
Sumatriptan/Naproxen Sodium59

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Migraine-Associated Neck Pain Assessed at Baseline, 2, 4, and 8 Hours Post-dose

Number of Participants with neck pain at the time of assessment. (NCT00382993)
Timeframe: Baseline, 2, 4, and 8 hours post-dose

,
InterventionParticipants (Number)
Migraine-Assoc Neck Pain at BaselineMigraine-Assoc Neck Pain at 2 Hours Post-DoseMigraine-Assoc Neck Pain at 4 Hours Post-DoseMigraine-Assoc Neck Pain at 8 Hours Post-Dose
Placebo81716551
Sumatriptan/Naproxen Sodium75523829

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Sustained Freedom From Migraine-Associated Sinus Pain

Sustained Freedom from Migraine-Associated Sinus Pain was defined as the absence of sinus pain from 2 to 24 hours post-dose. (NCT00382993)
Timeframe: 2 - 24 hours post-dose

InterventionParticipants (Number)
Placebo44
Sumatriptan/Naproxen Sodium75

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Sustained Freedom From Migraine-Associated Nausea

Sustained Freedom from Migraine-Associated Nausea was defined as the absence of nausea from 2 to 24 hours post-dose. (NCT00383162)
Timeframe: 2 - 24 hours post-dose

InterventionParticipants (Number)
Placebo38
Sumatriptan-Naproxen Sodium70

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Sustained Freedom From Migraine Pain Between 2-24 Hours Post-dose

Sustained freedom from migraine pain was defined as having no pain at 2 hours post-dose without the use of rescue medication; and without the recurrence of any pain or the use of any rescue medication 2 to 24 hours post-dose. (NCT00383162)
Timeframe: 2 - 24 hours post-dose

InterventionParticipants (Number)
Placebo10
Sumatriptan-Naproxen Sodium36

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Sustained Freedom From Migraine

Migraine-free was defined as pain-free with no traditional migraine-associated symptoms (i.e.,photophobia, phonophobia, nausea). Sustained migraine-free was defined as migraine-free at 2 hours and sustained from 2 to 24 hours post dose without the use of rescue medication. (NCT00383162)
Timeframe: 2 - 24 hours post-dose

InterventionParticipants (Number)
Placebo11
Sumatriptan-Naproxen Sodium32

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Sustained Complete Pain/Symptom-Free

Sustained Complete Pain/Symptom-Free was defined as completely symptom-free (migraine-free plus neck and sinus pain-free) at 2 hours and sustained from 2 to 24 hours without the use of rescue medication. (NCT00383162)
Timeframe: 2 - 24 hours post-dose

InterventionParticipants (Number)
Placebo9
Sumatriptan-Naproxen Sodium30

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Rescue Medication Used up to 24 Hours Post-dose

A rescue medication was defined as an additional medication taken for the treatment of migraine headache pain symptoms associated with the attack. Allowed were a single dose of either: sumatriptan (50mg or 100mg), OR naproxen sodium (max 550mg), OR, an over-the-counter pain-reliever (per label). (NCT00383162)
Timeframe: Dosing to 24 hours post-dose

InterventionParticipants (Number)
Placebo84
Sumatriptan-Naproxen Sodium40

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Pain-Free Assessment at 2 Hours Post-dose

Participants rated their pain severity using a four point scale where 0=no pain, 1=mild pain, 2=moderate pain, and 3=severe pain. Pain-free was a rating of 0 (no pain) at the specified time. (NCT00383162)
Timeframe: 2 hours post-dose

InterventionParticipants (Number)
Placebo23
Sumatriptan-Naproxen Sodium54

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Recurrence of Any Migraine Headache Pain

Recurrence is defined as the return of any migraine headache pain during the specified post-dose period, following a pain-free response at 2 hours. (NCT00383162)
Timeframe: 24 hours and 48 hours

,
InterventionParticipants (Number)
Recurrence by 24 hours post-doseRecurrence by 48 hours post-dose
Placebo1213
Sumatriptan-Naproxen Sodium1111

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Pain-Free Assessment at 1/2, 1, 4, 8 Hours Post-dose

Participants rated their pain severity using a four point scale where 0=no pain, 1=mild pain, 2=moderate pain, and 3=severe pain. Pain-free was a rating of 0 (no pain) at the specified time. (NCT00383162)
Timeframe: 1/2, 1, 4, and 8 hours post-dose

,
InterventionParticipants (Number)
1/2 hour post-dose1 hour post-dose4 hours post-dose8 hours post-dose
Placebo2133032
Sumatriptan-Naproxen Sodium6268088

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Migraine-Free Assessment at 2, 4, and 8 Hours Post-dose

Migraine-free was defined as pain-free with no traditional migraine-associated symptoms (i.e.,photophobia, phonophobia, nausea and vomiting) at the time of the assessment. (NCT00383162)
Timeframe: 2, 4 , and 8 hours post-dose

,
InterventionParticipants (Number)
2 hours post-dose4 hours post-dose8 hours post-dose
Placebo193029
Sumatriptan-Naproxen Sodium477280

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Migraine-Associated Sinus Pain Assessed at Baseline, 2, 4, and 8 Hours Post-dose

Number of participants who had sinus pain at the time of assessment. (NCT00383162)
Timeframe: Baseline, 2, 4, and 8 hours post-dose

,
InterventionParticipants (Number)
Baseline2 hours post-dose4 hours post-dose8 hours post-dose
Placebo58523935
Sumatriptan-Naproxen Sodium61312019

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Migraine-Associated Photophobia Assessed at Baseline, 2, 4, and 8 Hours Post-dose

Number of participants who had photophobia (sensitivity to light) at the time of assessment. (NCT00383162)
Timeframe: Baseline, 2, 4, and 8 hours post-dose

,
InterventionParticipants (Number)
Baseline2 hours post-dose4 hours post-dose8 hours post-dose
Placebo98866548
Sumatriptan-Naproxen Sodium95573327

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Migraine-Associated Phonophobia Assessed at Baseline, 2, 4, and 8 Hours Post-dose

Number of participants who had phonophobia (sensitivity to noise) at the time of assessment. (NCT00383162)
Timeframe: Baseline, 2, 4, and 8 hours post-dose

,
InterventionParticipants (Number)
Baseline2 hours post-dose4 hours post-dose8 hours post-dose
Placebo82735644
Sumatriptan-Naproxen Sodium86473124

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Migraine-Associated Neck Pain Assessed at Baseline, 2, 4, and 8 Hours Post-dose

Number of Participants with neck pain at the time of assessment. (NCT00383162)
Timeframe: Baseline, 2, 4, and 8 hours post-dose

,
InterventionParticipants (Number)
Baseline2 hours post-dose4 hours post-dose8 hours post-dose
Placebo65544637
Sumatriptan-Naproxen Sodium82544031

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Migraine-Associated Nausea Assessed at Baseline, 2, 4, and 8 Hours Post-dose

Number of participants who had nausea at the time of assessment. Resolution of an associated symptom was defined as a migraine headache symptom that was present at the time of treatment that was not present post-dose. Symptom resolution was defined only among subjects who treated while their symptom was present. (NCT00383162)
Timeframe: Baseline, 2, 4, and 8 hours

,
InterventionParticipants (Number)
Baseline2 hours post-dose4 hours post-dose8 hours post-dose
Placebo45422924
Sumatriptan-Naproxen Sodium48392014

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Complete Pain/Symptom-Free Assessed at Baseline, 2, 4, and 8 Hours Post-dose

"Number of participants who were completely symptom-free (migraine-free plus neck and sinus pain-free) at time of assessment.Complete pain/symptom-free was defined as migraine-free, neck pain-free, and sinus pain free." (NCT00383162)
Timeframe: Baseline, 2, 4, and 8 hours post-dose

,
InterventionParticipants (Number)
Baseline2 hours post-dose4 hours post-dose8 hours post-dose
Placebo133117107106
Sumatriptan-Naproxen Sodium136927362

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Sustained Freedom From Migraine-Associated Sinus Pain

Sustained Freedom from Migraine-Associated Sinus Pain was defined as the absence of sinus pain from 2 to 24 hours post-dose. (NCT00383162)
Timeframe: 2 - 24 hours post-dose

InterventionParticipants (Number)
Placebo34
Sumatriptan-Naproxen Sodium76

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Sustained Freedom From Migraine-Associated Photophobia

Sustained Freedom from Migraine-Associated Photophobia was defined as the absence of photophobia (sensitivity to light) from 2 to 24 hours post-dose. (NCT00383162)
Timeframe: 2 - 24 hours post-dose

InterventionParticipants (Number)
Placebo23
Sumatriptan-Naproxen Sodium59

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Sustained Freedom From Migraine-Associated Phonophobia

Sustained Freedom from Migraine-Associated Phonophobia was defined as the absence of phonophobia (sensitivity to noise) from 2 to 24 hours post-dose. (NCT00383162)
Timeframe: 2 - 24 hours post-dose

InterventionParticipants (Number)
Placebo31
Sumatriptan-Naproxen Sodium66

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Sustained Freedom From Migraine-Associated Neck Pain

Sustained Freedom from Migraine-Associated Neck Pain was defined as the absence of neck pain from 2 to 24 hours post-dose. (NCT00383162)
Timeframe: 2 - 24 hours post-dose

InterventionParticipants (Number)
Placebo33
Sumatriptan-Naproxen Sodium63

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Time to First Appearance of Sumatriptan, Naproxen and Eletriptan at the Proximal Small Intestine

Scintigraphic images were analyzed in a time-lapse format and regions of interest were to be drawn to include the stomach and small intestine. Images were recorded in a supine position and a series of 3 to 60 consecutive anterior scintigraphic images, each 1 minute in duration, were recorded using a clinical grade gamma camera. After this initial continuous imaging sequence, additional images were recorded to coincide with PK blood sampling times as necessary to monitor the tablet disintegration and transit time through the intestines. Prior to ingesting the radiolabeled dosage forms, two external markers (2-3 microcuries of indium-111 or technetium-99m) were placed on each participant to facilitate consistent positioning underneath the gamma camera. The first marker was placed on the right side of the participant's chest (approximately at the fifth intercostal rib) and a second marker was placed on the hip bone (approximately the left anterior superior ileac spine). (NCT00385008)
Timeframe: Day 1 of each treatment administered (For 30 days)

Interventionhr (Median)
Sumatriptan, Non-migraineSumatriptan, MigraineNaproxen, Non-migraineNaproxen, Migraine
TREXIMA (Sumatriptan 85 mg + Naproxen 500 mg)4.3654.3504.5104.350

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Cmax for Eletriptan

Following Relpax administration, 8 mL blood sample was collected at pre-dose and then at 5, 10 , 15, 20, 25, 30, 35, 40, 45, 50, 55, 60, and 75 minutes. Then at 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 5.5, 6 hour and at 8, 10, 12 hour post-dose for each treatment administered. All available plasma supernatant was withdrawn from the precipitated blood fraction. (NCT00385008)
Timeframe: Pre-dose and then at 5 minute intervals through 60 minutes, at 75 minutes, every 30 minutes from 90 minutes through 6 hours, and at 8, 10, 12 hours post-dose for each treatment administered.

Interventionng/mL (Geometric Mean)
Non-migraineMigraine
Relpax (Eletriptan 40 mg)80.24691.323

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Maximum Observed Drug Concentration (Cmax) for Sumatriptan and Naproxen

Following TREXIMA administration, 6 mL blood sample was collected at pre-dose and then at 5, 10 , 15, 20, 25, 30, 35, 40, 45, 50, 55, 60, and 75 minutes. Then at 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 5.5, 6 hour and at 8, 10, 12, 24, 48, 72 hour post-dose for each treatment administered. All available plasma supernatant was withdrawn from the precipitated blood fraction. (NCT00385008)
Timeframe: Pre-dose and then at 5 minute intervals through 60 minutes, at 75 minutes, every 30 minutes from 90 minutes through 6 hours, and at 8, 10, 12, 24, 48 and 72 hours post-dose for each treatment administered.

Interventionnanograms per milliliter (ng/mL) (Geometric Mean)
Sumatriptan, Non-migraineSumatriptan, MigraineNaproxen, Non-migraineNaproxen, Migraine
TREXIMA (Sumatriptan 85 mg + Naproxen 500 mg)49.90045.67646.3456.36

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Mean Area Under the Drug Concentration Time Curve (AUC) From Time of Dosing Through 2 Hour Post-dose [AUC (0-2)], Through 24 Hour [AUC (0-24)] and AUC From Time of Dosing Extrapolated to Infinity [AUC (0-inf)] for Sumatriptan and Naproxen

Following TREXIMA administration, 6 mL blood sample was collected at pre-dose and then at 5, 10 , 15, 20, 25, 30, 35, 40, 45, 50, 55, 60, and 75 minutes. Then at 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 5.5, 6 hour and at 8, 10, 12, 24, 48, 72 hour post-dose for each treatment administered. All available plasma supernatant was withdrawn from the precipitated blood fraction. (NCT00385008)
Timeframe: Pre-dose and then at 5 minute intervals through 60 minutes, at 75 minutes, every 30 minutes from 90 minutes through 6 hours, and at 8, 10, 12, 24, 48 and 72 hours post-dose for each treatment administered.

Interventionmicrogram*hr per mL (µg*hr/mL) (Geometric Mean)
AUC (0-24), Sumatriptan, Non-migraineAUC (0-24), Sumatriptan, MigraineAUC (0-inf), Sumatriptan, Non-migraineAUC (0-inf), Sumatriptan, MigraineAUC (0-2), Sumatriptan, Non-migraineAUC (0-2), Sumatriptan, MigraineAUC (0-24), Naproxen, Non-migraineAUC (0-24), Naproxen, MigraineAUC (0-inf), Naproxen, Non-migraineAUC (0-inf), Naproxen, MigraineAUC (0-2), Naproxen, Non-migraineAUC (0-2), Naproxen, Migraine
TREXIMA (Sumatriptan 85 mg + Naproxen 500 mg)231.526165.707231.999158.03665.15654.884570.54627.06901.13978.3923.1624.38

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Time of Maximal Drug Concentration (Tmax) for Sumatriptan and Naproxen

Following TREXIMA administration, 6 mL blood sample was collected at pre-dose and then at 5, 10 , 15, 20, 25, 30, 35, 40, 45, 50, 55, 60, and 75 minutes. Then at 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 5.5, 6 hour and at 8, 10, 12, 24, 48, 72 hour post-dose for each treatment administered. All available plasma supernatant was withdrawn from the precipitated blood fraction. (NCT00385008)
Timeframe: Pre-dose and then at 5 minute intervals through 60 minutes, at 75 minutes, every 30 minutes from 90 minutes through 6 hours, and at 8, 10, 12, 24, 48 and 72 hours post-dose for each treatment administered.

Interventionhr (Median)
Sumatriptan, Non-migraineSumatriptan, MigraineNaproxen, Non-migraineNaproxen, Migraine
TREXIMA (Sumatriptan 85 mg + Naproxen 500 mg)2.0001.5004.504.00

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Small Intestine Transit and Residence (Time to 50% Through Intestine) of the Radioactive Markers Representing Sumatriptan, Naproxen and Eletriptan

Scintigraphic images were analyzed in a time-lapse format and regions of interest were to be drawn to include the stomach and small intestine. Images were recorded in a supine position and a series of 3 to 60 consecutive anterior scintigraphic images, each 1 minute in duration, were recorded using a clinical grade gamma camera. After this initial continuous imaging sequence, additional images were recorded to coincide with PK blood sampling times as necessary to monitor the tablet disintegration and transit time through the intestines. Prior to ingesting the radiolabeled dosage forms, two external markers (2-3 microcuries of indium-111 or technetium-99m) were placed on each participant to facilitate consistent positioning underneath the gamma camera. The first marker was placed on the right side of the participant's chest (approximately at the fifth intercostal rib) and a second marker was placed on the hip bone (approximately the left anterior superior ileac spine). (NCT00385008)
Timeframe: Day 1 of each treatment administered (For 30 days)

Interventionhr (Median)
Sumatriptan, Non-MigraineSumatriptan, MigraineNaproxen, Non-MigraineNaproxen, Migraine
TREXIMA (Sumatriptan 85 mg + Naproxen 500 mg)2.8952.9902.5502.230

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Small Intestine Transit and Residence (Time to 50% Through Intestine) of the Radioactive Markers Representing Sumatriptan, Naproxen and Eletriptan

Scintigraphic images were analyzed in a time-lapse format and regions of interest were to be drawn to include the stomach and small intestine. Images were recorded in a supine position and a series of 3 to 60 consecutive anterior scintigraphic images, each 1 minute in duration, were recorded using a clinical grade gamma camera. After this initial continuous imaging sequence, additional images were recorded to coincide with PK blood sampling times as necessary to monitor the tablet disintegration and transit time through the intestines. Prior to ingesting the radiolabeled dosage forms, two external markers (2-3 microcuries of indium-111 or technetium-99m) were placed on each participant to facilitate consistent positioning underneath the gamma camera. The first marker was placed on the right side of the participant's chest (approximately at the fifth intercostal rib) and a second marker was placed on the hip bone (approximately the left anterior superior ileac spine). (NCT00385008)
Timeframe: Day 1 of each treatment administered (For 30 days)

Interventionhr (Median)
Eletriptan, Non-MigraineEletriptan, Migraine
Relpax (Eletriptan 40 mg)4.3354.140

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Number of Participants With Any Adverse Events (AEs) and Serious Adverse Events (SAEs)

AE is any untoward medical occurrence in a clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. SAE is any untoward event resulting in death, life threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, congenital anomaly/birth defect or any other situation according to medical or scientific judgment. (NCT00385008)
Timeframe: Up to Day 30

,
InterventionParticipants (Count of Participants)
Any AEsAny SAEs
Relpax (Eletriptan 40 mg)30
TREXIMA (Sumatriptan 85 mg + Naproxen 500 mg)80

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Tmax for Eletriptan

Following Relpax administration, 8 mL blood sample was collected at pre-dose and then at 5, 10 , 15, 20, 25, 30, 35, 40, 45, 50, 55, 60, and 75 minutes. Then at 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 5.5, 6 hour and at 8, 10, 12 hour post-dose for each treatment administered. All available plasma supernatant was withdrawn from the precipitated blood fraction. (NCT00385008)
Timeframe: Pre-dose and then at 5 minute intervals through 60 minutes, at 75 minutes, every 30 minutes from 90 minutes through 6 hours, and at 8, 10, 12 hours post-dose for each treatment administered.

Interventionhr (Median)
Non-migraineMigraine
Relpax (Eletriptan 40 mg)2.5002.000

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Mean AUC (0-inf) and AUC (0-2) for Eletriptan

Following Relpax administration, 8 mL blood sample was collected at pre-dose and then at 5, 10 , 15, 20, 25, 30, 35, 40, 45, 50, 55, 60, and 75 minutes. Then at 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 5.5, 6 hour and at 8, 10, 12 hour post-dose for each treatment administered. All available plasma supernatant was withdrawn from the precipitated blood fraction. (NCT00385008)
Timeframe: Pre-dose and then at 5 minute intervals through 60 minutes, at 75 minutes, every 30 minutes from 90 minutes through 6 hours, and at 8, 10, 12 hours post-dose for each treatment administered.

Interventionµg*hr/mL (Geometric Mean)
AUC (0-inf), Non-migraineAUC (0-inf), MigraineAUC (0-2), Non-migraineAUC (0-2), Migraine
Relpax (Eletriptan 40 mg)540.669570.86070.24978.092

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Time to First Appearance of Sumatriptan, Naproxen and Eletriptan at the Proximal Small Intestine

Scintigraphic images were analyzed in a time-lapse format and regions of interest were to be drawn to include the stomach and small intestine. Images were recorded in a supine position and a series of 3 to 60 consecutive anterior scintigraphic images, each 1 minute in duration, were recorded using a clinical grade gamma camera. After this initial continuous imaging sequence, additional images were recorded to coincide with PK blood sampling times as necessary to monitor the tablet disintegration and transit time through the intestines. Prior to ingesting the radiolabeled dosage forms, two external markers (2-3 microcuries of indium-111 or technetium-99m) were placed on each participant to facilitate consistent positioning underneath the gamma camera. The first marker was placed on the right side of the participant's chest (approximately at the fifth intercostal rib) and a second marker was placed on the hip bone (approximately the left anterior superior ileac spine). (NCT00385008)
Timeframe: Day 1 of each treatment administered (For 30 days)

Interventionhr (Median)
Eletriptan, Non-migraineEletriptan, Migraine
Relpax (Eletriptan 40 mg)5.5305.810

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Time to Complete Dispersion of the Sumatriptan and Naproxen Portions of the TREXIMA Tablet and of the Relpax Tablet

Scintigraphic images were analyzed in a time-lapse format and regions of interest were to be drawn to include the stomach and small intestine. Images were recorded in a supine position and a series of 3 to 60 consecutive anterior scintigraphic images, each 1 minute in duration, were recorded using a clinical grade gamma camera. After this initial continuous imaging sequence, additional images were recorded to coincide with PK blood sampling times as necessary to monitor the tablet disintegration and transit time through the intestines. Prior to ingesting the radiolabeled dosage forms, two external markers (2-3 microcuries of indium-111 or technetium-99m) were placed on each participant to facilitate consistent positioning underneath the gamma camera. The first marker was placed on the right side of the participant's chest (approximately at the fifth intercostal rib) and a second marker was placed on the hip bone (approximately the left anterior superior ileac spine). (NCT00385008)
Timeframe: Day 1 of each treatment administered (For 30 days)

Interventionhr (Median)
Sumatriptan, Non-migraineSumatriptan, MigraineNaproxen, Non-migraineNaproxen, Migraine
TREXIMA (Sumatriptan 85 mg + Naproxen 500 mg)0.0500.0501.1251.250

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Time to Complete Dispersion of the Sumatriptan and Naproxen Portions of the TREXIMA Tablet and of the Relpax Tablet

Scintigraphic images were analyzed in a time-lapse format and regions of interest were to be drawn to include the stomach and small intestine. Images were recorded in a supine position and a series of 3 to 60 consecutive anterior scintigraphic images, each 1 minute in duration, were recorded using a clinical grade gamma camera. After this initial continuous imaging sequence, additional images were recorded to coincide with PK blood sampling times as necessary to monitor the tablet disintegration and transit time through the intestines. Prior to ingesting the radiolabeled dosage forms, two external markers (2-3 microcuries of indium-111 or technetium-99m) were placed on each participant to facilitate consistent positioning underneath the gamma camera. The first marker was placed on the right side of the participant's chest (approximately at the fifth intercostal rib) and a second marker was placed on the hip bone (approximately the left anterior superior ileac spine). (NCT00385008)
Timeframe: Day 1 of each treatment administered (For 30 days)

Interventionhr (Median)
Eletriptan, Non-migraineEletriptan, Migraine
Relpax (Eletriptan 40 mg)0.6000.670

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Time to 10%, 50%, 90% and Complete Gastric Empting of the Radioactive Markers Representing Sumatriptan, Naproxen and Eletriptan

Scintigraphic images were analyzed in a time-lapse format and regions of interest were drawn to include the stomach and small intestine. Images were recorded in a supine position and a series of 3 to 60 consecutive anterior scintigraphic images, each 1 minute in duration, were recorded using a clinical grade gamma camera. After this initial continuous imaging sequence, additional images were recorded to coincide with pharmacokinetic (PK) blood sampling times as necessary to monitor the tablet disintegration and transit time through the intestines. Prior to ingesting the radiolabeled dosage forms, two external markers (2-3 microcuries of indium-111 or technetium-99m) were placed on each participant to facilitate consistent positioning underneath the gamma camera. The first marker was placed on the right side of the participant's chest (approximately at the fifth intercostal rib) and a second marker was placed on the hip bone (approximately the left anterior superior ileac spine). (NCT00385008)
Timeframe: Day 1 of each treatment administration (For 30 days)

Interventionhours (hr) (Median)
10% gastric emptying, Eletriptan, Non-migraine10% gastric emptying, Eletriptan, Migraine50% gastric emptying, Eletriptan, Non-migraine50% gastric emptying, Eletriptan, Migraine90% gastric emptying, Eletriptan, Non-migraine90% gastric emptying, Eletriptan, MigraineComplete gastric emptying, Eletriptan,Non-migraineComplete gastric emptying, Eletriptan, Migraine
Relpax (Eletriptan 40 mg)0.4000.4100.5900.8902.5902.4903.7653.510

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Time to 10%, 50%, 90% and Complete Gastric Empting of the Radioactive Markers Representing Sumatriptan, Naproxen and Eletriptan

Scintigraphic images were analyzed in a time-lapse format and regions of interest were drawn to include the stomach and small intestine. Images were recorded in a supine position and a series of 3 to 60 consecutive anterior scintigraphic images, each 1 minute in duration, were recorded using a clinical grade gamma camera. After this initial continuous imaging sequence, additional images were recorded to coincide with pharmacokinetic (PK) blood sampling times as necessary to monitor the tablet disintegration and transit time through the intestines. Prior to ingesting the radiolabeled dosage forms, two external markers (2-3 microcuries of indium-111 or technetium-99m) were placed on each participant to facilitate consistent positioning underneath the gamma camera. The first marker was placed on the right side of the participant's chest (approximately at the fifth intercostal rib) and a second marker was placed on the hip bone (approximately the left anterior superior ileac spine). (NCT00385008)
Timeframe: Day 1 of each treatment administration (For 30 days)

Interventionhours (hr) (Median)
10% gastric emptying, Sumatriptan, Non-migraine10% gastric emptying, Sumatriptan, Migraine10% gastric emptying, Naproxen, Non-migraine10% gastric emptying, Naproxen, Migraine50% gastric emptying, Sumatriptan, Non-migraine50% gastric emptying, Sumatriptan, Migraine50% gastric emptying, Naproxen, Non-migraine50% gastric emptying, Naproxen, Migraine90% gastric emptying, Sumatriptan, Non-migraine90% gastric emptying, Sumatriptan, Migraine90% gastric emptying, Naproxen, Non-migraine90% gastric emptying, Naproxen, MigraineComplete gastric emptying,Sumatriptan,Non-migraineComplete gastric emptying, Sumatriptan, MigraineComplete gastric emptying, Naproxen, Non-migraineComplete gastric emptying, Naproxen, Migraine
TREXIMA (Sumatriptan 85 mg + Naproxen 500 mg)0.1000.1301.1951.3000.6751.0702.2602.3103.0203.4404.2904.0104.5054.0004.7604.500

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Sustained Headache Relief 2-24 Hours After Treatment

Sustained pain relief was defined as having pain relief (mild or no pain) at 2 hours w/o any moderate or severe pain during 2-24 hour period post-treatment, without rescue medication. (NCT00387881)
Timeframe: 2-24 hours after treatment

InterventionParticipants (Number)
Placebo77
Sumatriptan/Naproxen110

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Freedom From Headache Pain at 0.5, 1, and 4 Hours After Treatment

Pain-Free is defined as post-treatment headache pain severity of none in subjects who have not used rescue medication prior to or at the time of the assessment. (NCT00387881)
Timeframe: 0.5, 1, and 4 hours after Treatment

,
InterventionParticipants (Number)
Pain-free at 4 hoursPain-free at 1 hourPain-free at 0.5 hour
Placebo60166
Sumatriptan/Naproxen105235

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Headache Relief at 4, 2, 1 and 0.5 Hours After Treatment

Pain relief was defined as reduction of headache pain from a baseline severity of moderate or severe to none or mild at the given time. (NCT00387881)
Timeframe: 0.5, 1, 2, and 4 hours after treatment

,
InterventionParticipants (Number)
Headache relief at 4 hoursHeadache relief at 2 hoursHeadache relief at 1 hourHeadache relief at 0.5 hour
Placebo1081137339
Sumatriptan/Naproxen1531248541

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Incidence of Headache Associated: Neck Pain, Sinus Pain, Photophobia, Phonophobia, Nausea at Time Intervals of 4 and 2 Hours After Treatment

Neck pain, sinus pain, photophobia, phonophobia and nausea are considered headache-associated symptoms.(Headache-associated=Headache-Assoc.) (NCT00387881)
Timeframe: 2 and 4 hours after treatment

,
InterventionParticipants (Number)
Headache-Assoc. Neck Pain at 4 hoursHeadache-Assoc. Neck Pain at 2 hoursHeadache-Assoc. Sinus Pain at 4 hoursHeadache-Assoc. Sinus Pain at 2 hoursHeadache-Assoc. Photophobia at 4 hoursHeadache-Assoc. Photophobia at 2 hoursHeadache-Assoc. Phonophobia at 4 hoursHeadache-Assoc. Phonophobia at 2 hoursHeadache-Assoc. Nausea at 4 hoursHeadache-Assoc. Nausea at 2 hours
Placebo93688849876083538237
Sumatriptan/Naproxen63594936604659545136

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Intermediate Sustained Pain-Free: Post-dose at Intervals of 2-4 Hours and 1-2 Hours

Intermediate sustained pain free was defined as achieving headache pain-free (moderate or severe pain to no pain) prior to the specified timepoint (1 or 2 hours) and maintaining it to the specified timepoint (2-4 hours).(Intermediate=Intermed.) (NCT00387881)
Timeframe: 1-2 and 2-4 hours after treatment

,
InterventionParticipants (Number)
Intermed. Sustained Pain-free, 2-4 hrs post-doseIntermed. Sustained Pain-free, 1-2 hrs post-dose
Placebo2211
Sumatriptan/Naproxen6123

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Subjects Who Used Rescue Medication From 0 - 24 Hours After Treatment

Rescue medication defined as additional medication (i.e. sumatriptan/naproxen sodium as open-label rescue or other medication as permitted per protocol), taken by subject for the treatment of headache pain or other symptoms associated with the headache attack. (NCT00387881)
Timeframe: 0 - 24 hours after treatment

InterventionParticipants (Number)
Placebo101
Sumatriptan/Naproxen61

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Pain-Free at 2 Hours Post-dose and Sustained Pain-Free From 2-24 Hours Post-dose.

Pain-free was defined as a headache severity of no pain (grade 0) at 2 hours post-treatment in subjects who have not used rescue medication prior to or at the time of the assessment. Sustained pain-free response was defined as pain-free at 2 hours post-treatment through 24 hours post-treatment without rescue medicine. (NCT00387881)
Timeframe: 2 hours through 24 hours after Treatment

,
InterventionParticipants (Number)
Pain-Free (2 hours)Sustained Pain-Free (2-24 hours)
Placebo2520
Sumatriptan/Naproxen6454

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Medication Satisfaction: Mean Patient Perception of Migraine (PPMQ-R) Subscale Score

Patient Perception of Migraine Questionnaire-Revised(PPMQ-R) evaluates subject satisfaction with treatment 24 hours post-dose using validated questions. Questions are analyzed on 4 subscale scores (efficacy, functionality, ease-of-use, and tolerability) and total score. Scores range from 0-100, with the higher scores indicating better satisfaction. (NCT00387881)
Timeframe: 0 - 24 hours after treatment

,
InterventionScore in scale (Mean)
Efficacy Adjusted MeanFunctionality Adjusted MeanEase-of-Use Adjusted MeanBothersome-of-Side Effects Adjusted MeanTotal Score adjusted Mean
Placebo5356849464
Sumatriptan/Naproxen6770889175

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Intermediate Sustained Pain Relief: Post-dose at Intervals of 2-4 Hours and 1-2 Hours After Treatment

Intermediate sustained pain relief was defined as achieving headache pain relief (from moderate or severe pain at baseline to mild or no pain) prior to the specified timepoint (1 or 2 hours) and maintaining it to the specified timepoint (2-4 hours). (Intermediate=Intermed.) (NCT00387881)
Timeframe: 1-2, and 2- 4 hours after treatment

,
InterventionParticipants (Number)
Intermed. Sustained Pain Relief, 2-4 hrs post-doseIntermed. Sustained Pain Relief, 1-2 hrs post-dose
Placebo9267
Sumatriptan/Naproxen11884

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Numerical Rating Scale

"Within 48 hours of ED discharge, participants were allowed to take the investigational medication. At the moment they took the investigational medication, they were asked to record a number from 0 to 10, which represented their headache. 0 signified no pain and 10 signified the worse pain imaginable.~Two hours later, participants were asked again to record their pain on a scale from 0 to 10. The outcome is the change in pain between baseline and two hours and will be a number between 0 and 10. Greater numbes signify greater relief" (NCT00449787)
Timeframe: Baseline, two hours

Interventionunits on a scale (Mean)
Sumatriptan4.1
Naproxen4.3

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Patient Satisfaction

"At the 48 hour assessment, patients were asked, The next time you go to an emergency room with a headache, do you want to receive the same medication. This outcome tabulates the number of affirmative responses." (NCT00449787)
Timeframe: 48 hours after ER discharge

Interventionparticipants (Number)
Sumatriptan69
Naproxen68

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Number of Treated Migraine Attacks With Photophobia, Phonophobia, Nausea, Neck Pain, Sinus Pain, and Vomiting

The number of treated migraine attacks with the reported migraine-associated symptoms of photophobia, phonophobia, nausea, neck pain, sinus pain, and vomiting were counted. Photophobia: sensitivity to light; phonophobia: sensitivity to sound. (NCT00488514)
Timeframe: Baseline through End of Study (up to Month 12)

,,
Interventiontreated migraine attacks (Number)
PhotophobiaPhonophobiaNauseaNeck painSinus painVomiting
12 Month Completer Population40643725217321721424375
6 Month Completer Population56085221312030502052555
ITT Population65286063369035402428682

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Number of Treated Migraine Attacks

The number of migraine attacks eligible for evaluation, not associated with rescue medication use, or prohibited medications, was summarized. Rescue medication was additional medication taken within 24 hours of Combination Tablet. Prohibited medications: ergot, opioid, barbiturate, 5-HT1 agonist, long-acting non-steroidal anti-inflammatory drug (NSAID), short-acting NSAID-containing compound, analgesic, anti-emetic, monoamine oxidase inhibitors, St. John's Wort, angiotensin-converting enzyme inhibitor, Angiotensin II receptor blockers, anti-coagulant, anti-platelet. (NCT00488514)
Timeframe: Baseline through End of Study (up to Month 12)

Interventiontreated migraine attacks (Number)
All MigrainesMigraines Without Rescue MedicationMigraines Without Rescue or Prohibited Medication
85 mg Sumatriptan/500 mg Naproxen Sodium851777917657

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Number of Participants With Hematocrit and Hemoglobin Values of Interest That Shifted From Normal at Baseline to Abnormal at the End of Study Visit

"A shift from normal to low, for example, indicates that a value was normal at baseline but low at the end of study visit. The value ranges were determined by the central laboratory. Reference ranges: hemoglobin, 12-17 years old (y): 120-160 grams (g)/L; hematocrit (expressed as the percentage of blood occupied by red blood cells), 12-17 y: 0.360-0.490." (NCT00488514)
Timeframe: Baseline through End of Study (up to Month 12)

,,
Interventionparticipants (Number)
Hemoglobin, normal to high, n=318,176, 546Hemoglobin, normal to low, n=318,176, 546Hematocrit, normal to high, n=318,176, 546Hematocrit, normal to low, n=318,176, 546
12 Month Completer Population06010
6 Month Completer Population610217
Safety Population920429

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Number of Tablets Taken, After Which at Least One Adverse Event Occurred Within 3 or 5 Days of Dosing With That Combination Tablet

The number of events that occurred within 3 or 5 days of dosing with the combination tablet on a per tablet basis. A total of 8413, 5876, and 9989 tablets were taken by the 6 Month Completer, 12 Month Completer, and the Safety Populations, respectively. (NCT00488514)
Timeframe: Baseline through End of Study (up to Month 12)

,,
Interventiontablets (Number)
Number of tablets with an AE within 3 daysNumber of tablets with an AE within 5 days
12 Month Completer Population667706
6 Month Completer Population917970
Safety Population11161178

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Mean Body Mass Index (BMI) for All Study Participants at the Indicated Time Points

BMI = (Weight in kilograms)/(height in centimeters/100)^2 (NCT00488514)
Timeframe: Screening and Months 3, 6, 9, and 12

,,
Interventionkilograms per meters squared (Mean)
Screening, n=285, 337, 622Month 3, n=270, 306, 576Month 6, n=223, 248, 471Month 9, n= 197, 220, 417Month 12, n=178, 198, 376
12-14 Years22.0122.0922.5422.5822.81
12-17 Years22.9722.9523.1723.2023.33
15-17 Years23.7723.7123.7423.7423.79

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Number of Total Migraines Headaches and Migraines Treated With the Combination Tablet

The total number of migraine headaches and the number of migraine headaches treated with the Combination Tablet during the study were summarized. (NCT00488514)
Timeframe: Baseline through End of Study (up to Month 12)

,,
Interventionmigraine attacks (Number)
Total MigrainesTreated Migraines
12 Month Completer Population58515234
6 Month Completer Population82907318
ITT Population99378517

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Number of Treated Attacks Classified as Migraine Pain-Free (MPF) Within 24 Hours of Dosing With the Combination Tablet

The number of migraine attacks eligible for evaluation, not associated with rescue medication use, and not associated with either rescue medication use or prohibited medications were counted. Migraine Pain Free was defined as the migraine attack ending <= 24 hours after the participant was dosed with the Combination Tablet. (NCT00488514)
Timeframe: Baseline through End of Study (up to Month 12)

Interventiontreated migraine attacks (Number)
All MigrainesMigraines Without Rescue MedicationMigraines Without Rescue or Prohibited Medication
85 mg Sumatriptan/500 mg Naproxen Sodium640061426052

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Number of Treated Attacks Classified as Migraine Pain-Free (MPF) Within 4 Hours of Dosing With a Combination Tablet

The number of migraine attacks eligible for evaluation, not associated with rescue medication use, and not associated with either rescue medication use or prohibited medications were counted. Migraine Pain Free was defined as the migraine attack ending <= 4 hours after the participant was dosed with the Combination Tablet. (NCT00488514)
Timeframe: Baseline through End of Study (up to Month 12)

Interventiontreated migraine attacks (Number)
All MigrainesMigraines Without Rescue MedicationMigraines Without Rescue or Prohibited Medication
85 mg Sumatriptan/500 mg Naproxen Sodium507650205017

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Average Number of Headaches, Migraine Attacks, and Treated Migraine Attacks Per Month

The average number of headaches (non-migraine and migraine attacks), migraine attacks, and treated migraine attacks per month was calculated for each participant, based on their time in the study. The outcome measure represents the average of the mean number of the headaches, migraine headaches, and treated migraines per month of the study participants in the 6 Month, 12 Month, and ITT Populations. A treated attack is defined as a migraine treated with the Combination Tablet. (NCT00488514)
Timeframe: Baseline through End of Study (up to Month 12)

,,
Interventionevents (Mean)
HeadachesMigrainesTreated migraine attacks
12 Month Completer Population3.92.62.4
6 Month Completer Population3.32.21.9
ITT Population3.01.81.5

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Mean Blood Pressure for All Study Participants at the Indicated Time Points

At each visit, a participant's blood pressure was taken three times. The average of the three readings was then calculated for each participant at each visit (mean blood pressure). The outcome measure represents the average of the mean blood pressure of all of the study participants. SBP, systolic blood pressure; DBP, diastolic blood pressure. (NCT00488514)
Timeframe: Screening and Months 3, 6, 9, and 12

,,
Interventionmillimeters of mercury (mmHg) (Mean)
SBP, Screening, n=285, 337, 622SBP, Month 3, n=270, 308, 578SBP, Month 6, n=224, 249, 473SBP, Month 9, n=198, 221, 419SBP, Month 12, n=178, 198, 376DBP, Screening, n=285, 337, 622DBP, Month 3, n=270, 308, 578DBP, Month 6, n=224, 249, 473DBP, Month 9, n=198, 221, 419DBP, Month 12, n=178, 198, 376
12-14 Years107.4107.2109.2109.6111.066.265.766.165.666.6
12-17 Years108.9109.3110.6111.2111.567.767.167.367.368.3
15-17 Years110.2111.1112.0112.7112.169.068.468.468.969.9

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Number of Treated Attacks Classified as Migraine Pain-Free Within 4 Hours That Were Also Pain Free Within 2 Hours of Dosing With the Combination Tablet

The number of migraine attacks eligible for evaluation, not associated with rescue medication use, and not associated with either rescue medication use or prohibited medications were counted. Migraine Pain Free was defined as the migraine attack ending <= 4 hours after the participant was dosed with the Combination Tablet. (NCT00488514)
Timeframe: Baseline through End of Study (up to Month 12)

Interventiontreated migraine attacks (Number)
All MigrainesMigraines Without Rescue MedicationMigraines Without Rescue or Prohibited Medication
85 mg Sumatriptan/500 mg Naproxen Sodium362335983596

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Mean Change From Baseline in the Migraine Specific Quality of Life (QOL) Questionnaire for Adolescents (MSQ-A) Score at Months 3, 6, 9, and 12

The MSQ-A consists of 14 items measuring how migraines affect QOL: Role Function (RF)-Restrictive (items 1-7) and RF-Preventative (items 8-11), examining the degree to which performance of daily activities is limited or interrupted, respectively, by migraine; RF-Emotional (items 12-14, examining frustration/helplessness due to migraine). Dimensions (dim.) are scored independently. The 14 items are reverse coded onto a 1-6 scale; dim. are then created by summing specific item scores and transforming raw total score onto a 0-100 scale. For each dim., higher scores indicate better health status. (NCT00488514)
Timeframe: Baseline and Months 3, 6, 9, and 12

,
Interventionpoints on a scale (Mean)
Role restrictive, Month 3, n=457, 160Role restrictive, Month 6, n=366, 160Role restrictive, Month 9, n=315, 148Role restrictive, Month 12, n=291, 153Role preventative, Month 3, n=457, 160Role preventative, Month 6, n=366, 160Role preventative, Month 9, n=315, 148Role preventative, Month 12, n=291, 153Role emotional , Month 3, n=457, 160Role emotional, Month 6, n=366, 160Role emotional, Month 9, n=315, 148Role emotional, Month 12, n=291, 153
12 Month Completer Population9.08.29.011.59.68.38.28.47.97.29.07.1
ITT Population10.110.513.715.77.96.89.49.87.16.610.511.4

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Mean Heart Rate for All Study Participants at the Indicated Time Points

A sitting heart rate was measured once for each participant at each visit. (NCT00488514)
Timeframe: Screening and Months 3, 6, 9, and 12

,,
Interventionbeats per minute (Mean)
Screening, n=284, 336, 620Month 3, n=266, 305, 571Month 6, n=221, 247, 468Month 9, n=198, 221, 419Month 12, n=178, 198, 376
12-14 Years75.876.977.576.976.8
12-17 Years7.4376.276.476.175.7
15-17 Years73.075.675.475.474.7

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Mean Height for All Study Participants at the Indicated Time Points

(NCT00488514)
Timeframe: Screening and Months 3, 6, 9, and 12

,,
Interventioncentimeters (Mean)
Screening, n=285, 337, 622Month 3, n=271, 308, 579Month 6, n=224, 249, 473Month 9, n=198, 221, 419Month 12, n=178, 198, 376
12-14 Years160.2161.3162.6163.8165.3
12-17 Years163.9164.5165.1165.8166.7
15-17 Years167.0167.3167.3167.6167.9

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Mean Weight for All Study Participants at the Indicated Time Points

(NCT00488514)
Timeframe: Screening and Months 3, 6, 9, and 12

,,
Interventionkilograms (Mean)
Screening, n=285, 337, 622Month 3, n=270, 306, 576Month 6, n=223, 248, 471Month 9, n=197, 220, 417Month 12, n=178, 198, 376
12-14 Years57.0258.0160.2061.2462.92
12-17 Years62.1962.5863.5764.2365.25
15-17 Years66.5766.6166.6166.9067.35

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Number of Migraine Attacks Rated With the Indicated Pain Severity

The number of migraine attacks treated at the mild, moderate, or severe intensity were counted. Pain severity was assessed by participants based on a scale of 0-3: 0=no pain, 1=mild, 2= moderate, 3=severe. (NCT00488514)
Timeframe: Baseline through End of Study (up to Month 12)

,,
Interventiontreated migraine attacks (Number)
No painMildModerateSevere
12 Month Completer Population0100925351686
6 Month Completer Population0137335552385
ITT Population0161941322759

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Number of Participants Categorized by Response to Each of the 3 Global Satisfaction Questions From the Patient Perception Migraine Questionaire-Revised (PPMQ-R) at Month 12

"The PPMQ-R is a fully validated 32-item questionnaire assessing participant satisfaction with acute migraine medication and includes 3 questions that assess satisfaction with respect to efficacy, side effects, and overall satisfaction (i.e., How effective the medication is overall, side effects of the medication, overall satisfaction with the medication). Each item is rated on a 7-point scale ranging from very satisfied (1) to very dissatisfied (7)." (NCT00488514)
Timeframe: End of Study/Month 12

,,
Interventionparticipants (Number)
Overall Efficacy, Very SatisfiedOverall Efficacy, SatisfiedOverall Efficacy, Somewhat SatisfiedOverall Efficacy, NeutralOverall Efficacy, Somewhat DissatisfiedOverall Efficacy, DissatisfiedOverall Efficacy, Very DissatisfiedSide Effects, Very SatisfiedSide Effects, SatisfiedSide Effects, Somewhat SatisfiedSide Effects, NeutralSide Effects, Somewhat DissatisfiedSide Effects, DissatisfiedSide Effects, Very DissatisfiedOverall Treatment Satisfaction, Very SatisfiedOverall Treatment Satisfaction, SatisfiedOverall Treatment Satisfaction, Somewhat SatisfiedOverall Treatment Satisfaction, NeutralTreatment Satisfaction, Somewhat DissatisfiedOverall Treatment Satisfaction, DissatisfiedOverall Treatment Satisfaction, Very Dissatisfied
12 Month Completer Population48461231004240146332514762301
6 Month Completer Population5963165100495121107426461105301
ITT Population66752072105561241112537176136311

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Number of Participants Categorized by Response to Each of the 3 Global Satisfaction Questions From the Patient Perception Migraine Questionnaire-Revised (PPMQ-R) at the Screening Visit

"The PPMQ-R is a fully validated 32-item questionnaire assessing participant satisfaction with acute migraine medication and includes 3 questions that assess satisfaction with respect to efficacy, side effects, and overall satisfaction (i.e., How effective the medication is overall, side effects of the medication, overall satisfaction with the medication). Each item is rated on a 7-point scale ranging from very satisfied (1) to very dissatisfied (7)." (NCT00488514)
Timeframe: Screening

,,
Interventionparticipants (Number)
Overall Efficacy, Very SatisfiedOverall Efficacy, SatisfiedOverall Efficacy, Somewhat SatisfiedOverall Efficacy, NeutralOverall Efficacy, Somewhat DissatisfiedOverall Efficacy, DissatisfiedOverall Efficacy, Very DissatisfiedSide Effects, Very SatisfiedSide Effects, SatisfiedSide Effects, Somewhat SatisfiedSide Effects, NeutralSide Effects, Somewhat DissatisfiedSide Effects, DissatisfiedSide Effects, Very DissatisfiedOverall Treatment Satisfaction, Very SatisfiedOverall Treatment Satisfaction, SatisfiedOverall Treatment Satisfaction, Somewhat SatisfiedOverall Treatment Satisfaction, NeutralTreatment Satisfaction, Somewhat DissatisfiedOverall Treatment Satisfaction, DissatisfiedOverall Treatment Satisfaction, Very Dissatisfied
12 Month Completer Population1154721512825050263662411705616993
6 Month Completer Population22102113302322489874569136730113943513238
ITT Population3616319267494312135166771272918115019216467314315

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Number of Participants With Abnormal Electrocardiogram Findings at Screening and at the Final Visit as Assessed by the Investigator

The number of participants with an electrocardiogram (ECG) status of normal, abnormal, clinically significant (CS), or not clinically significant (NCS), as determined by the Investigator, was reported. Specific definitions of ECG categorizations were not provided; investigators were expected to apply reasonable standards of clinical judgment. Normal, all ECG parameters within accepted normal ranges; abnormal, ECG finding(s) outside of normal ranges; CS, ECG with a CS abnormality that meets exclusion criteria; NCS, ECG with an abnormality not CS or meeting exclusion criteria per investigator. (NCT00488514)
Timeframe: Screening and Final Visit (up to Month 12)

,,
Interventionparticipants (Number)
Screening, normal, n=284, 337, 621Screening, abnormal, NCS, n=284, 337, 621Screening, abnormal, CS, n=284, 337, 621Final Visit, Normal, n=248, 294, 542Final Visit, abnormal, NCS, n=248, 294, 542Final Visit, abnormal, CS, n=248, 294, 542
12-14 Years224600196520
12-17 Years49412704161260
15-17 Years270670220740

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Number of Participants With Alanine Aminotransferase (ALT), Aspartate Aminotransferase (AST), Creatinine, Potassium, and Blood Urea Nitrogen (BUN) Values of Interest That Shifted From Normal at Baseline to Abnormal at the End of Study Visit

"A shift from normal to low, for example, indicates that a value was normal at baseline but low at the end of study visit. The value ranges were determined by the central laboratory. Reference ranges: ALT, 12 years old (y): 0-45 Units/liter (U/L), >13 y: 0-48 U/L; AST, 12 y: 0-42 U/L, >13 y 0-42 U/L; creatinine, 12 y: 27-88 micromoles/liter (UMOL/L), >13 y: 44-124 UMOL/L; potassium, 12 y: 3.5-5.5 millimoles/liter (MMOL/L), >13 y: 3.5-5.3 MMOL/L; BUN, 12-17 y: 24-101 milligrams (mg)/deciliter (dL)." (NCT00488514)
Timeframe: Baseline through End of Study (up to Month 12)

,,
Interventionparticipants (Number)
ALT, normal to high, n=330, 179, 565ALT, normal to low, n=330, 179, 565AST, normal to high, n=329, 179, 562AST, normal to low, n=329, 179, 562Creatinine, normal to high, n=330, 179, 565Creatinine, normal to low, n=330, 179, 565Potassium, normal to high, n=329, 179, 562Potassium, normal to low, n=329, 179, 562BUN, normal to high, n=330, 179, 565BUN, normal to low, n=330, 179, 565
12 Month Completer Population1010010200
6 Month Completer Population2010021302
Safety Population3030024619

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Number of Participants With Any Adverse Event Categorized by Participant Age

The number of participants with any adverse event by age group (12-14 and 15-17 years) is recorded. (NCT00488514)
Timeframe: Baseline through End of Study (up to Month 12)

,,
Interventionparticipants (Number)
Ages 12-14Ages 15-17
12 Month Completer Population5773
6 Month Completer Population104135
Safety Population175218

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Number of Participants With Any Adverse Event Categorized by Participant Gender

The number of participants with adverse events by gender is recorded. (NCT00488514)
Timeframe: Baseline through End of Study (up to Month 12)

Interventionparticipants (Number)
FemaleMale
85 mg Sumatriptan/500 mg Naproxen Sodium238155

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Number of Participants With Any Adverse Event Categorized by Participant Race

"The number of participants with any adverse event was categorized by race. The category Other captures : American Indian or Alaskan Native; Asian, Native Hawaiian, or Other Pacific Islander; African American/African Heritage and Asian; African American/African Heritage and White; and American Indian or Alaskan Native and White." (NCT00488514)
Timeframe: Baseline through End of Study (up to Month 12)

Interventionparticipants (Number)
CaucasianAfrican AmericanOther
85 mg Sumatriptan/500 mg Naproxen Sodium3443514

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Number of Participants With Any Adverse Event Categorized by Severity

The number of participants with at least one mild (an event that is easily tolerated by the participant, causing minimal discomfort and not interfering with everyday activities), moderate (an event that is sufficiently discomforting to interfere with normal everyday activities), or severe adverse event (an event that prevents normal everyday activities) was recorded. (NCT00488514)
Timeframe: Baseline through End of Study (up to Month 12)

,,
Interventionparticipants (Number)
MildModerateSevere
12 Month Completer Population437214
6 Month Completer Population7414024
Safety Population12722044

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Number of Participants With Any Adverse Event Categorized Over Time

The number of participants with an adverse event occurring in either the first six months of the study (months 0-6; <=194 days) or the second six months of the study (months 6-12; =>194 days until end of study) was recorded. (NCT00488514)
Timeframe: Baseline through End of Study (up to Month 12)

,,
Interventionparticipants (Number)
First six months of studySecond six months of study
12 Month Completer Population11285
6 Month Completer Population208143
Safety Population348191

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Number of Participants With Any Adverse Event That Occurred Within 3 or 5 Days of the First Dose of the Combination Tablet

The number of participants with adverse events that occurred within 3 or 5 days of their first dose of the Combination Tablet was recorded. (NCT00488514)
Timeframe: Baseline through End of Study (up to Month 12)

,,
Interventionparticipants (Number)
Within 3 daysWithin 5 days
12 Month Completer Population3535
6 Month Completer Population6666
Safety Population128130

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The Number of Injections With Local Site Reactions (Bleeding, Swelling, Bruising and Erythema).

Each of the 18 participants were injected three times (for a total of 54 injections)with Sumavel DosePro, and followed over three days. (NCT00620425)
Timeframe: -15 min, immediately Post-dose, and 1, 4, 8, 24, 48 and 72 hrs post-dose

,,,,,,,
Interventioninjections (Number)
Injections with Bleeding presentInjections with Bruising presentInjections with Swelling presentInjections with Erythema present
1 hr Post-dose001839
24 hr Post-dose04013
4 hr Post-dose01037
48 hr Post-dose01002
72 hr Post-dose0100
8 hr Post-dose03018
All Participants at -15 Min Pre-dose0000
All Participants Immediately Post-dose510399

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Number of Participants Who Experienced an Adverse Event During the Study

Participants were assessed throughout the study for adverse events. An adverse event was defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the product, whether or not considered related to the use of the product. Any worsening (i.e., any clinically significant adverse change in frequency and/or intensity) of a preexisting condition which was temporally associated with the use of the product, was also an adverse event. (NCT00701389)
Timeframe: up to 14 days after last dose of study drug (up to 10 weeks)

InterventionParticipants (Number)
100 mg Sumatriptan/600 mg Telcagepant9
100 mg Sumatriptan/Telcagepant Placebo12
Sumatriptan Placebo/600 mg Telcagepant8
Sumatriptan Placebo/Telcagepant Placebo10

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Number of Participants Who Were Discontinued From Any Study Period Due to an Adverse Event

Participants were assessed throughout the study for adverse events. An adverse event was defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the product, whether or not considered related to the use of the product. Any worsening (i.e., any clinically significant adverse change in frequency and/or intensity) of a preexisting condition which was temporally associated with the use of the product, was also an adverse event. The number of participants who were discontinued from the study due to adverse event was summarized. (NCT00701389)
Timeframe: up to 10 weeks

InterventionParticipants (Number)
100 mg Sumatriptan/600 mg Telcagepant0
100 mg Sumatriptan/Telcagepant Placebo0
Sumatriptan Placebo/600 mg Telcagepant0
Sumatriptan Placebo/Telcagepant Placebo0

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Time-weighted Mean Arterial Pressure (Sumatriptan With Telcagepant Versus Sumatriptan Alone)

In each treatment period (1 through 4), duplicate readings of semi-recumbent blood pressure (BP) were completed using an automated blood pressure machine at predose, 30, 60, 90, 120, 150, 180, and 360 minutes postdose. Mean arterial pressure (MAP) was calculated as follows: MAP = Diastolic Blood Pressure (DBP) + (0.33 * Pulse Pressure [PP]) where PP = Systolic Blood Pressure [SBP] minus DBP. Only mean arterial pressure measurements up to and including 150 minutes postdose (including the predose measurement) were used to calculate the time-weighted averages. Time-weighted averages for each participant were obtained by calculating the area under the measurement-time curve of mean arterial pressure divided by the time period over which measurements were made (i.e. 150 minutes). (NCT00701389)
Timeframe: Predose up to 150 minutes postdose of each treatment period (up to 10 weeks)

InterventionmmHg (Least Squares Mean)
100 mg Sumatriptan/600 mg Telcagepant89.0
100 mg Sumatriptan/Telcagepant Placebo87.5

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Time-weighted Mean Arterial Pressure (Telcagepant Versus Placebo)

In each treatment period (1 through 4), duplicate readings of semi-recumbent blood pressure (BP) were completed using an automated blood pressure machine at predose, 30, 60, 90, 120, 150, 180, and 360 minutes postdose. Mean arterial pressure (MAP) was calculated as follows: MAP = Diastolic Blood Pressure (DBP) + (0.33 * Pulse Pressure [PP]) where PP = Systolic Blood Pressure [SBP] minus DBP. Only mean arterial pressure measurements up to and including 150 minutes postdose (including the predose measurement) were used to calculate the time-weighted averages. Time-weighted averages for each participant were obtained by calculating the area under the measurement-time curve of mean arterial pressure divided by the time period over which measurements were made (i.e. 150 minutes). (NCT00701389)
Timeframe: Predose up to 150 minutes postdose of each treatment period (up to 10 weeks)

InterventionmmHg (Least Squares Mean)
Sumatriptan Placebo/600 mg Telcagepant84.7
Sumatriptan Placebo/Telcagepant Placebo83.5

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Nausea Free at Two Hours

Number of subjects who were nausea free and who had not received any rescue medication before their two-hour assessment. (NCT00724815)
Timeframe: 2 hours post patch activation

Interventionparticipants (Number)
NP101 Patch189
Placebo Patch144

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Pain Free at Two Hours

Subjects whose headache severity score equaled zero (0) two hours post patch activation and who had not received any rescue medication before their two-hour assessment. (NCT00724815)
Timeframe: 2 hours post patch activation

Interventionparticipants (Number)
NP101 Patch40
Placebo Patch21

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Phonophobia Free at Two Hours

Subjects who were phonophobia free and who had not received any rescue medication before their two-hour assessment. (NCT00724815)
Timeframe: 2 hours post patch activation

Interventionparticipants (Number)
NP101 Patch125
Placebo Patch89

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Photophobia Free at Two Hours

Subjects who were photophobia free and who had not received any rescue medication before their two-hour assessment. (NCT00724815)
Timeframe: 2 hours post patch activation

Interventionparticipants (Number)
NP101 Patch116
Placebo Patch83

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Number of Participants With a Consecutive 2-day Average Diastolic Blood Pressure of >=90 mmHg

The number of participants with any valid two-day consecutive average diastolic blood pressure measurement of >=90 mmHg was calculated. Valid blood pressure measurements were defined as follows: must be taken at least 24 hours following last dose of investigational product used to treat an individual migraine, must be taken no later than 96 hours after last dose of investigational product used to treat an individual migraine, must be taken prior to the onset of a subsequent individual migraine. (NCT00792636)
Timeframe: Baseline to End of Study (6-month study duration)

Interventionparticipants (Number)
Sumatriptan/Naproxen10
Sumatriptan11
Naproxen11

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Number of Participants With a Consecutive 2-day Average Systolic Blood Pressure of >=140 mmHg During the Study

The number of participants with any valid two-day consecutive average systolic blood pressure measurement of >=140 mmHg was calculated. Valid blood pressure measurements were defined as follows: must be taken at least 24 hours following last dose of investigational product used to treat an individual migraine, must be taken no later than 96 hours after last dose of investigational product used to treat an individual migraine, must be taken prior to the onset of a subsequent individual migraine. (NCT00792636)
Timeframe: Baseline to End of Study (6-month study duration)

Interventionparticipants (Number)
Sumatriptan/Naproxen2
Sumatriptan2
Naproxen3

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Number of Participants With an Increase of >=3 mmHg From the Baseline Diastolic Blood Pressure for the Average of Any Given Two-day Consecutive Collection of Blood Pressure Measurements

The number of participants with an increase of >=3 mmHg from the baseline diastolic blood pressure for the average of any given two-day consecutive collection of valid blood pressure measurements during the study were summarized. Valid blood pressure measurements were defined as follows: must be taken at least 24 hours following last dose of investigational product used to treat an individual migraine, must be taken no later than 96 hours after last dose of investigational product used to treat an individual migraine, must be taken prior to the onset of a subsequent individual migraine. (NCT00792636)
Timeframe: Baseline to End of Study (6-month study duration)

Interventionparticipants (Number)
Sumatriptan/Naproxen72
Sumatriptan65
Naproxen77

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Time to the First Day With an Average Systolic Blood Pressure Increase of >=5 mmHg From the Baseline Systolic Blood Pressure

Kaplan-Meier curves for the distribution of time to the first day with an average diastolic BP increase of >=3 mmHg from the baseline diastolic BP during each calendar day were calculated and graphed for each treatment group. Only valid BP measurements were included and were defined as follows: must be taken at least 24 hours following last dose of investigational product used to treat an individual migraine, must be taken no later than 96 hours after last dose of investigational product used to treat an individual migraine, must be taken prior to the onset of a subsequent individual migraine. (NCT00792636)
Timeframe: Baseline to End of Study (6-month study duration)

Interventiondays (Median)
Sumatriptan/Naproxen42.5
Sumatriptan32.5
Naproxen18.5

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Time to the First Day With an Average Diastolic Blood Pressure Increase of >=3 mmHg From the Baseline Diastolic Blood Pressure

Kaplan-Meier curves for the distribution of time to the first day with an average diastolic BP increase of >=3 mmHg from the baseline diastolic BP during each calendar day were calculated and graphed for each treatment group. Only valid BP measurements were included and were defined as follows: must be taken at least 24 hours following last dose of investigational product used to treat an individual migraine, must be taken no later than 96 hours after last dose of investigational product used to treat an individual migraine, must be taken prior to the onset of a subsequent individual migraine. (NCT00792636)
Timeframe: Baseline to End of Study (6-month study duration)

Interventiondays (Median)
Sumatriptan/Naproxen51
Sumatriptan50.5
Naproxen26

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Number of Participants Withdrawn From the Study Due to Blood Pressure Changes

The number of participants withdrawn from the study due to protocol-defined blood pressure changes were summarized for each treatment group. Defined blood pressure changes included (1) monthly average BP ≥140 mmHg systolic or >=90 mmHg diastolic and confirmed in clinic, (2) monthly average BP increase of >=30 mmHg systolic or >=20 mmHg from in-clinic screening and confirmed in clinic, and (3) systolic >=140 mmHg or diastolic >=90 mmHg on consecutive clinic visits >=2 weeks apart. (NCT00792636)
Timeframe: Baseline to End of Study (6-month study duration)

Interventionparticipants (Number)
Sumatriptan/Naproxen1
Sumatriptan0
Naproxen0

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Number of Participants With an Increase of >=5 mmHg From the Baseline Systolic Blood Pressure for the Average of Any Given Two-day Consecutive Collection of Blood Pressure Measurements

The number of participants with an increase of >=5 mmHg from the baseline systolic blood pressure for the average of any given two-day consecutive collection of valid blood pressure measurements during the study were summarized. Valid blood pressure measurements were defined as follows: must be taken at least 24 hours following last dose of investigational product used to treat an individual migraine, must be taken no later than 96 hours after last dose of investigational product used to treat an individual migraine, must be taken prior to the onset of a subsequent individual migraine. (NCT00792636)
Timeframe: Baseline to End of Study (6-month study duration)

Interventionparticipants (Number)
Sumatriptan/Naproxen53
Sumatriptan57
Naproxen63

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Treatment Difference in Systolic and Diastolic Blood Pressure Mean Changes From Baseline at 6 Months Between Sumatriptan/Naproxen and Sumatriptan

The calculation of baseline and post-baseline mean BP (either systolic or diastolic) for each month (30-day period) is the average of all valid Telephonic Self-Measured Blood Pressure (T-SMBP) measurements. T-SMBP technology is a method that allows the participant to self-measure BP outside the clinic using a BP monitor and transfer the data from their home to a central server. Change from baseline was calculated as the Month 6 value minus the Baseline value. Least squares mean and confidence intervals were based on mixed model repeated measures analysis (MMRM). (NCT00792636)
Timeframe: Baseline and Month 6

,
InterventionmmHg (Mean)
Systolic, Baseline, n=120, 109Systolic, Month 6, n=48, 42Systolic, Change from Baseline, n=47, 41Diastolic, Baseline, n=120, 109Diastolic, Month 6, n=48, 42Diastolic, Change from Baseline, n=47, 41
Sumatriptan110.8109.4-2.875.773.9-1.6
Sumatriptan/Naproxen111.7107.1-2.976.073.0-2.1

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Mean Change From Baseline in Systolic and Diastolic Blood Pressure at Month 6 for Sumatriptan/Naproxen for the ITT Subpopulation of Participants Treating With <30 Total Doses, 30-60 Total Doses, >=30, 60-90 Total Doses, and >90 Total Doses

The calculation of baseline and post-baseline mean BP (either systolic or diastolic) for each month (30-day period) is the average of all valid T-SMBP measurements. The subgrouping of the ITT population was created and examined to demonstrate the robustness of the results for the primary analysis. Descriptive statistics were calculated for baseline, month 6, and change from baseline to month 6. LSMeans and corresponding confidence intervals (CIs) were based on MMRM analysis. LSMeans and CIs were not calculated for the 60-90 and the >90 total dose groups due to lack of convergence. (NCT00792636)
Timeframe: Baseline and Month 6

InterventionmmHg (Least Squares Mean)
Systolic, <30 total dosesSystolic, 30-60 total dosesSystolic, >=30 total dosesDiastolic, <30 total dosesDiastolic, 30-60 total dosesDiastolic, >=30 total doses
Sumatriptan/Naproxen-1.2-3.4-3.7-0.6-3.3-3.6

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Treatment Difference in Systolic and Diastolic Blood Pressure Mean Changes From Baseline at 6 Months Between Sumatriptan/Naproxen and Naproxen

The calculation of baseline and post-baseline mean BP (either systolic or diastolic) for each month (30-day period) is the average of all valid Telephonic Self-Measured Blood Pressure (T-SMBP) measurements. T-SMBP technology is a method that allows the participant to self-measure BP outside the clinic using a BP monitor and transfer the data from their home to a central server. Change from baseline was calculated as the Month 6 value minus the Baseline value. Least squares mean and confidence intervals were based on mixed model repeated measures analysis (MMRM). (NCT00792636)
Timeframe: Baseline and Month 6

,
InterventionmmHg (Mean)
Systolic, Baseline, n=120, 115Systolic, Month 6, n=48, 37Systolic, Change from Baseline, n=47, 36Diastolic, Baseline, n=120, 115Diastolic, Month 6, n=48, 37Diastolic, Change from Baseline, n=47, 36
Naproxen110.1108.2-1.874.774.3-0.6
Sumatriptan/Naproxen111.7107.1-2.976.073.0-2.1

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Mean Change From Baseline in Systolic and Diastolic Blood Pressure at Month 6 for Sumatriptan/Naproxen for the ITT Subpopulation of Participants Treating, on Average, With <6, 6-10, >=6, 10-14, and >14 Doses Per Month

The calculation of baseline and post-baseline mean BP (either systolic or diastolic) for each month (30-day period) is the average of all valid T-SMBP measurements. The subgrouping of the ITT population was created and examined to demonstrate the robustness of the results for the primary analysis. Descriptive statistics were calculated for baseline, month 6, and change from baseline to month 6. LSMeans and corresponding confidence intervals (CIs) were based on MMRM analysis. LSMeans and CIs were not calculated for the 10-14 and the >14 doses/month groups due to lack of convergence. (NCT00792636)
Timeframe: Baseline and Month 6

InterventionmmHg (Least Squares Mean)
Systolic,<6 doses per monthSystolic, 6-10 doses per monthSystolic, >=6 doses per monthDiastolic,<6 doses per monthDiastolic, 6-10 doses per monthDiastolic, >=6 doses per month
Sumatriptan/Naproxen-1.6-4.6-4.3-1.0-3.7-3.5

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Mean Change From Baseline in Systolic and Diastolic Blood Pressure at Month 6 for Sumatriptan/Naproxen

The calculation of baseline and post-baseline mean blood pressure (BP) (either systolic or diastolic) for each month (30-day period) is the average of all valid Telephonic Self-Measured Blood Pressure (T-SMBP) measurements. T-SMBP technology is a method that allows the participant to self-measure BP outside the clinic using a BP monitor and transfer the data from their home to a central server. Change from baseline was calculated as the Month 6 value minus the Baseline value. Least squares mean and confidence intervals were based on mixed model repeated measures analysis (MMRM). (NCT00792636)
Timeframe: Baseline and Month 6

Interventionmillimeters of mercury (mmHg) (Mean)
Systolic, Baseline, n=120Systolic, Month 6, n=48Systolic, Change from Baseline, n=47Diastolic, Baseline, n=120Diastolic, Month 6, n=48Diastolic, Change from Baseline, n=47
Sumatriptan/Naproxen111.7107.1-2.976.073.0-2.1

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Mean Change From Baseline in Systolic and Diastolic Blood Pressure at Month 6 for Sumatriptan/Naproxen for the ITT Subpopulation of Participants Treating, on Average, <4 Migraines, 4-6 Migraines, >=4 Migraines, and >6 Migraines Per Month

The calculation of baseline and post-baseline mean BP (either systolic or diastolic) for each month (30-day period) is the average of all valid T-SMBP measurements. The subgrouping of the ITT population was created and examined to demonstrate the robustness of the results for the primary analysis.Descriptive statistics were calculated for baseline, month 6, and change from baseline to month 6. LSMeans and corresponding confidence intervals were based on MMRM analysis. LSMeans and corresponding confidence intervals were not calculated for > 6 migraines/month group due to lack of convergence. (NCT00792636)
Timeframe: Baseline and Month 6

InterventionmmHg (Least Squares Mean)
Systolic, <4 migraines per monthSystolic, 4-6 migraines per monthSystolic, >=4 migraines per monthDiastolic, <4 migraines per monthDiastolic, 4-6 migraines per monthDiastolic, >=4 migraines per month
Sumatriptan/Naproxen-2.0-3.3-3.7-1.2-5.3-4.1

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Mean Change From Baseline in Systolic and Diastolic Blood Pressure at Month 6 for Sumatriptan/Naproxen for the ITT Subpopulation of Participants Treating, on Average, <1.3 Times Per Migraine, 1.3-1.7 Times Per Migraine, and >1.7 Times Per Migraine

The calculation of baseline and post-baseline mean BP (either systolic or diastolic) for each month (30-day period) is the average of all valid T-SMBP measurements. The subgrouping of the ITT population was created and examined to demonstrate the robustness of the results for the primary analysis.Descriptive statistics were calculated for baseline, month 6, and change from baseline to month 6. LSMeans and corresponding confidence intervals were based on MMRM analysis. (NCT00792636)
Timeframe: Baseline and Month 6

InterventionmmHg (Least Squares Mean)
Systolic, <1.3 doses per migraineSystolic, 1.3-1.7 doses per migraineSystolic, >1.7 doses per migraineDiastolic, <1.3 doses per migraineDiastolic, 1.3-1.7 doses per migrainesDiastolic, >1.7 doses per migraine
Sumatriptan/Naproxen-0.3-2.7-3.8-0.4-0.9-3.2

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Mean Change From Baseline in Systolic and Diastolic Blood Pressure at Month 6 for Sumatriptan and Naproxen

The calculation of baseline and post-baseline mean BP (either systolic or diastolic) for each month (30-day period) is the average of all valid Telephonic Self-Measured Blood Pressure (T-SMBP) measurements. T-SMBP technology is a method that allows the participant to self-measure BP outside the clinic using a BP monitor and transfer the data from their home to a central server. Change from baseline was calculated as the Month 6 value minus the Baseline value. Least squares mean and confidence intervals were based on mixed model repeated measures analysis (MMRM). (NCT00792636)
Timeframe: Baseline and Month 6

,
InterventionmmHg (Mean)
Systolic, Baseline, n=109, 115Systolic, Month 6, n=42, 37Systolic, Change from Baseline, n=41, 36Diastolic, Baseline, n=109, 115Diastolic, Month 6, n=42, 37Diastolic, Change from Baseline, n=41, 36
Naproxen110.1108.2-1.874.774.3-0.6
Sumatriptan110.8109.4-2.875.773.9-1.6

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Number of Participants With Recurrent Migraine Headache Within 24 or 48 Hours

The time to headache recurrence is presented as the number of participants experiencing at least 1 recurring headache within 24 or 48 hours of receiving study drug. (NCT00804973)
Timeframe: Up to 24 and 48 hours after study drug administration

,,
InterventionParticipants (Count of Participants)
24 Hours Post-dose48 Hours Post-dose
LY259044326
Placebo46
Sumatriptan24

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Number of Participants With Photophobia

The number of participants reporting photophobia as a migraine symptom (NCT00804973)
Timeframe: Pre-dose, 30 minutes, 1 hour, 1.5 hours, 2 hours, 3 hours, and 4 hours after study drug administration.

,,
InterventionParticipants (Count of Participants)
Pre-Dose30 Minutes Post-dose1 Hour Post-dose1.5 Hours Post-dose2 Hours Post-dose3 Hours Post-dose4 Hours Post-dose
LY25904433833312522126
Placebo3836312724106
Sumatriptan373128231994

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Number of Participants With Pain Relief Response

"Participants were required to assess the presence of a headache and grade the intensity of the headache as severe, moderate, mild, or none. Pain relief response was defined as the number of participants with a migraine pain intensity score of none." (NCT00804973)
Timeframe: 30 minutes, 1 hour, 1.5 hours, 2 hours, 3 hours, and 4 hours after study drug administration.

,,
InterventionParticipants (Count of Participants)
30 Minutes Post-dose1 Hour Post-dose1.5 Hours Post-dose2 Hours Post-dose3 Hours Post-dose4 Hours Post-dose
LY259044371117223438
Placebo41218243534
Sumatriptan81425313539

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Number of Participants With Pain Free Response

"Participants were required to assess the presence of a headache and grade the intensity of the headache as severe, moderate, mild, or none. Pain free response was defined as the number of participants with a migraine pain intensity score of none." (NCT00804973)
Timeframe: 30 minutes, 1 hour, 1.5 hours, 3 hours, and 4 hours after study drug administration

,,
InterventionParticipants (Count of Participants)
30 Minutes Post-dose1 Hour Post-dose1.5 Hours Post-dose3 Hours Post-dose4 Hours Post-dose
LY25904437131425
Placebo4251324
Sumatriptan85101930

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Number of Participants With Nausea

The number of participants reporting nausea as a migraine symptom (NCT00804973)
Timeframe: Pre-dose, 30 minutes, 1 hour, 1.5 hours, 2 hours, 3 hours, and 4 hours after study drug administration.

,,
InterventionParticipants (Count of Participants)
Pre-Dose30 Minutes Post-dose1 Hour Post-dose1.5 Hours Post-dose2 Hours Post-dose3 Hours Post-dose4 Hours Post-dose
LY25904431813138864
Placebo2519128632
Sumatriptan16191310874

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Number of Participants With Headache Pain Free Response

"Participants were required to assess the presence of a headache and grade the intensity of the headache as severe, moderate, mild, or none. Headache pain free response was defined as the number of participants with a migraine pain intensity score of none." (NCT00804973)
Timeframe: 2 hours after study drug administration

InterventionParticipants (Count of Participants)
LY25904436
Sumatriptan12
Placebo6

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Number of Participants With Phonophobia

The number of participants reporting phonophobia as a migraine symptom (NCT00804973)
Timeframe: Pre-dose, 30 minutes, 1 hour, 1.5 hours, 2 hours, 3 hours, and 4 hours after study drug administration.

,,
InterventionParticipants (Count of Participants)
Pre-Dose30 Minutes Post-dose1 Hour Post-dose1.5 Hours Post-dose2 Hours Post-dose3 Hours Post-dose4 Hours Post-dose
LY2590443282419151164
Placebo312622161253
Sumatriptan332520181331

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Number of Participants With Vomiting

The number of participants reporting vomiting as a migraine symptom (NCT00804973)
Timeframe: Pre-dose, 30 minutes, 1 hour, 1.5 hours, 2 hours, 3 hours, and 4 hours after study drug administration.

,,
InterventionParticipants (Count of Participants)
Pre-Dose30 Minutes Post-dose1 Hour Post-dose1.5 Hours Post-dose2 Hours Post-dose3 Hours Post-dose4 Hours Post-dose
LY25904431011100
Placebo2100000
Sumatriptan1211000

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Number of Participants With Sustained Pain Relief Response

"Participants were required to assess the presence of a headache and grade the intensity of the headache as severe, moderate, mild, or none. Sustained pain relief response was defined as the number of participants with no return of a moderate or severe headache after pain went down to mild or none at 2 hours." (NCT00804973)
Timeframe: 24 and 48 hours after study drug administration

,,
InterventionParticipants (Count of Participants)
Pain Relief at 24 Hrs Post-dosePain Relief at 48 Hrs Post-dose
LY25904431919
Placebo2423
Sumatriptan2827

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Number of Participants With Sustained Pain Free Response

"Participants were required to assess the presence of a headache and grade the intensity of the headache as severe, moderate, mild, or none. Sustained pain free response was defined as the number of participants with no return of a mild, moderate or severe headache after pain intensity went down to none at 2 hours." (NCT00804973)
Timeframe: 24 and 48 hours after study drug administration

,,
InterventionParticipants (Count of Participants)
Pain Free at 24 Hours Post-dosePain Free at 48 Hours Post-dose
LY259044355
Placebo66
Sumatriptan119

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Number of Participants Sustained Pain-free From 2-24 Hours

Participants with sustained pain-freedom were defined as those with pain-freedom at 2 hours post-dose that was maintained up to 24 hours post-treatment without the use of rescue medication. (NCT00843024)
Timeframe: 2 to 24 hours after single dose of double-blind treatment (Randomization through Week 13)

,,,
Interventionparticipants (Number)
Total Population, n=142, 96, 97, 15012-14 years, n=70, 43, 46, 6515-17 years, n=72, 53, 51, 85
Placebo13103
Sumatriptan 10 mg/ Naproxen 60 mg23149
Sumatriptan 30 mg/ Naproxen 180 mg241212
Sumatriptan 85 mg/ Naproxen 500 mg351718

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Number of Participants Sustained Phonophobia-free From 2-24 Hours

Participants with sustained freedom from phonophobia were those with an absence of phonophobia (sensitivity to sound) from 2 to 24 hours post-dose without the use of rescue medication. (NCT00843024)
Timeframe: 2 to 24 hours after single dose of double-blind treatment (Randomization through Week 13)

,,,
Interventionparticipants (Number)
Total Population, n=144, 96, 96, 15112-14 years, n=71, 43, 46, 6515-17 years, n=73, 53, 50, 86
Placebo472720
Sumatriptan 10 mg/ Naproxen 60 mg482424
Sumatriptan 30 mg/ Naproxen 180 mg513120
Sumatriptan 85 mg/ Naproxen 500 mg793643

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Mean Body Mass Index of Participants at Baseline Categorized by Age Group

The mean body mass index of participants at baseline was calculated for all participants in the 12 to 14 year and 15 to 17 year age groups. Body mass index is calculated as: weight (kilograms [kg]) divided by height (meters [m]^2). (NCT00843024)
Timeframe: Baseline

InterventionKilograms per meters squared (kg/m^2) (Mean)
12 to 14 Years Age Group22.6
15 to 17 Years Age Group24.6

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Mean Age of Participants at Baseline Categorized by Age Group

The mean age of participants at baseline was calculated for all participants in the 12 to 14 year and 15 to 17 year age groups. (NCT00843024)
Timeframe: Baseline

InterventionYears (Mean)
12 to 14 Years Age Group13.1
15 to 17 Years Age Group16.1

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Number of Participants Photophobia-free at 2 Hours Post-dose

The number of participants who did not have photophobia (sensitivity to light) at 2 hours post dose was analyzed. (NCT00843024)
Timeframe: 2 hours after single dose of double-blind treatment (Randomization through Week 13)

,,,
Interventionparticipants (Number)
Total Population, n=144, 96, 96, 15112-14 years, n=71, 43, 46, 6515-17 years, n=73, 53, 50, 86
Placebo593326
Sumatriptan 10 mg/ Naproxen 60 mg572928
Sumatriptan 30 mg/ Naproxen 180 mg472423
Sumatriptan 85 mg/ Naproxen 500 mg894148

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Number of Female and Male Participants Categorized by Age Group

The gender of participants at baseline was reported for all participants in the 12 to 14 year and 15 to 17 year age groups. (NCT00843024)
Timeframe: Baseline

,
InterventionParticipants (Number)
FemaleMale
12 to 14 Years Age Group114111
15 to 17 Years Age Group17392

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Number of Participants Nausea-free at 2 Hours Post-dose

The number of participants who did not have nausea at 2 hours post dose was analzyed. (NCT00843024)
Timeframe: 2 hours after single dose of double-blind treatment (Randomization through Week 13)

,,,
Interventionparticipants (Number)
Total Population, n=144, 95, 96, 15112-14 years, n=71, 43, 46, 6515-17 years, n=73, 52, 50, 86
Placebo1015546
Sumatriptan 10 mg/ Naproxen 60 mg783642
Sumatriptan 30 mg/ Naproxen 180 mg743836
Sumatriptan 85 mg/ Naproxen 500 mg1064759

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Number of Participants of the Indicated Race Categorized by Age Group

The race of participants at baseline was reported for all participants in the 12 to 14 year and 15 to 17 year age groups. (NCT00843024)
Timeframe: Baseline

,
InterventionParticipants (Number)
African American/African HeritageAmerican Indian or Alaska NativeAsianNative Hawaiian or other Pacific IslanderWhiteAfrican American/African Heritage and WhiteAmerican Indian or Alaska Native and WhiteAsian and Native Hawaiian/other Pacific IslanderAsian and WhiteNative Hawaiian/ other Pacific Islander and WhiteMissing
12 to 14 Years Age Group31121181240201
15 to 17 Years Age Group32020216441321

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Number of Participants Randomized to Double-blind Treatment in the Indicated Age Categories at Baseline

The number of participants receiving double-blind treatment were reported according to age. (NCT00843024)
Timeframe: Baseline

,,,
InterventionParticipants (Number)
12-14 years15-17 years
Placebo7174
Sumatriptan 10 mg/ Naproxen 60 mg4353
Sumatriptan 30 mg/ Naproxen 180 mg4651
Sumatriptan 85 mg/ Naproxen 500 mg6587

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Number of Participants Sustained Nausea-free From 2-24 Hours

Participants with sustained freedom from nausea were those with an absence of nausea from 2 to 24 hours post-dose without the use of rescue medication. (NCT00843024)
Timeframe: 2 to 24 hours after single dose of double-blind treatment (Randomization through Week 13)

,,,
Interventionparticipants (Number)
Total Population, n=144, 95, 96, 15112-14 years, n=71, 43, 46, 6515-17 years, n=73, 52, 50, 86
Placebo683929
Sumatriptan 10 mg/ Naproxen 60 mg673136
Sumatriptan 30 mg/ Naproxen 180 mg643331
Sumatriptan 85 mg/ Naproxen 500 mg944351

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Mean Weight of Participants at Baseline Categorized by Age Group

The mean weight of participants at baseline was calculated for all participants in the 12 to 14 year and 15 to 17 year age groups. (NCT00843024)
Timeframe: Baseline

InterventionKilograms (kg) (Mean)
12 to 14 Years Age Group58.7
15 to 17 Years Age Group69.6

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Number of Participants Pain-free at 1 Hour Post-dose

Participants with a pain-free response at 1 hour post-dose were considered as those who had a reduction in migraine headache pain from moderate (a score of 2) or severe (a score of 3) at baseline to none (a score of 0) post-treatment, without the use of rescue medication prior to or at 1 hour post dose. (NCT00843024)
Timeframe: 1 hour after single dose of double-blind treatment (Randomization through Week 13)

,,,
Interventionparticipants (Number)
Total Population, n=142, 96, 97, 15012-14 years, n=70, 43, 46, 6515-17 years, n=72, 53, 51, 85
Placebo642
Sumatriptan 10 mg/ Naproxen 60 mg972
Sumatriptan 30 mg/ Naproxen 180 mg624
Sumatriptan 85 mg/ Naproxen 500 mg1147

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Number of Participants Who Used Rescue Medication From 2 to 24 Hours Post Dose

Rescue medication was defined as an additional medication taken by participants for the treatment of migraine pain or associated symptoms within 24 hours of dosing with investigational product. Permitted rescue medications included oral naproxen sodium (maximum 15 mg/kg), oral over-the-counter pain reliever, and anti-emetics. This outcome measure included only participants who rescued from 2 to 24 hours post-dose, inclusive. (NCT00843024)
Timeframe: 2 to 24 hours after single dose of double-blind treatment (Randomization through Week 13)

,,,
Interventionparticipants (Number)
Total Population, n=145, 96, 97, 15212-14 years, n=71, 43, 46, 6515-17 years, n=74, 53, 51, 87
Placebo472126
Sumatriptan 10 mg/ Naproxen 60 mg1459
Sumatriptan 30 mg/ Naproxen 180 mg16610
Sumatriptan 85 mg/ Naproxen 500 mg211011

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Number of Participants Who Were Pain Free at 2 Hours Post-dose

Participants were evaluated (self-assessment) for pain intensity by using a 4-point rating scale: 0=none, 1=mild, 2=moderate, and 3=severe. Participants with pain-free response were considered as those who had a reduction in migraine headache pain from moderate (score=2) or severe (score=3) at baseline to none (score=0) post-treatment, without the use of rescue medication (additional medication taken by participants for the treatment of migraine pain or associated symptoms) prior to or at 2 hours post-dose. (NCT00843024)
Timeframe: 2 hours after single dose of double-blind treatment (Randomization through Week 13)

,,,
Interventionparticipants (Number)
Total Population, n=142, 96, 97, 15012-14 years, n=70, 43, 46, 6515-17 years, n=72, 53, 51, 85
Placebo14104
Sumatriptan 10 mg/ Naproxen 60 mg281810
Sumatriptan 30 mg/ Naproxen 180 mg261313
Sumatriptan 85 mg/ Naproxen 500 mg361719

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Number of Participants Who Used Their First Dose of Rescue Medication Through the Indicated Time Points

Rescue medication was defined as an additional medication taken by participants for the treatment of migraine pain or associated symptoms within 24 hours of dosing with double-blind treatment. In addition to participants who rescued from 2 to 24 hours post-dose, inclusive, this outcome measure also included nine protocol violators who rescued < 2 hours post-treatment. (NCT00843024)
Timeframe: Dosing to 24 hours after single dose of double-blind treatment (Randomization through Week 13)

,,,
Interventionparticipants (Number)
Total Population, 1 hour, n=145, 96, 96, 152Total Population, 2 hours, n=145, 96, 96, 152Total Population, 3 hours, n=145, 96, 96, 152Total Population, 4 hours, n=145, 96, 96, 152Total Population, 8 hours, n=145, 96, 96, 152Total Population, 12 hours, n=145, 96, 96, 152Total Population, 18 hours, n=145, 96, 96, 152Total Population, 24 hours, n=145, 96, 96, 15212-14 years, 1 hour, n=71, 43, 46, 6512-14 years, 2 hours, n=71, 43, 46, 6512-14 years, 3 hours, n=71, 43, 46, 6512-14 years, 4 hours, n=71, 43, 46, 6512-14 years, 8 hours, n=71, 43, 46, 6512-14 years, 12 hours, n=71, 43, 46, 6512-14 years, 18 hours, n=71, 43, 46, 6512-14 years, 24 hours, n=71, 43, 46, 6515-17 years, 1 hour, n=74, 53, 50, 8715-17 years, 2 hours, n=74, 53, 50, 8715-17 years, 3 hours, n=74, 53, 50, 8715-17 years, 4 hours, n=74, 53, 50, 8715-17 years, 8 hours, n=74, 53, 50, 8715-17 years, 12 hours, n=74, 53, 50, 8715-17 years, 18 hours, n=74, 53, 50, 8715-17 years, 24 hours, n=74, 53, 50, 87
Placebo2102934454850521411142010212216182025282930
Sumatriptan 10 mg/ Naproxen 60 mg006691113140011444500555799
Sumatriptan 30 mg/ Naproxen 180 mg0611131515151701244446059911111111
Sumatriptan 85 mg/ Naproxen 500 mg23151620202223017810101010228810101213

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Number of Participants Sustained Photophobia-free From 2-24 Hours

Participants with sustained freedom from photophobia were those with an absence of photophobia (sensitivity to light) from 2 to 24 hours post-dose without the use of rescue medication. (NCT00843024)
Timeframe: 2 to 24 hours after single dose of double-blind treatment (Randomization through Week 13)

,,,
Interventionparticipants (Number)
Total Population, n=144, 96, 96, 15112-14 years, n=71, 43, 46, 6515-17 years, n=73, 53, 50, 86
Placebo442519
Sumatriptan 10 mg/ Naproxen 60 mg482127
Sumatriptan 30 mg/ Naproxen 180 mg432122
Sumatriptan 85 mg/ Naproxen 500 mg753540

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Number of Participants Phonophobia-free at 2 Hours Post-dose

The number of participants who did not have phonophobia (sensitivity to sound) at 2 hours post dose was analzyed. (NCT00843024)
Timeframe: 2 hours after single dose of double-blind treatment (Randomization through Week 13)

,,,
Interventionparticipants (Number)
Total Population, n=144, 96, 96, 15112-14 years, n=71, 43, 46, 6515-17 years, n=73, 53, 50, 86
Placebo603426
Sumatriptan 10 mg/ Naproxen 60 mg593247
Sumatriptan 30 mg/ Naproxen 180 mg553322
Sumatriptan 85 mg/ Naproxen 500 mg904149

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Cmax (Maximum Observed Concentration of Drug Substance in Plasma)

Bioequivalence based on Cmax. (NCT00846885)
Timeframe: Blood samples collected over a 12 hour period.

Interventionng/mL (Mean)
Test (Sumatriptan)80.334
Reference (Imitrex®)71.483

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AUC0-t (Area Under the Concentration-time Curve From Time Zero to Time of Last Measurable Concentration)

Bioequivalence based on AUC0-t. (NCT00846885)
Timeframe: Blood samples collected over a 12 hour period.

Interventionng*h/mL (Mean)
Test (Sumatriptan)305.374
Reference (Imitrex®)288.099

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AUC0-inf (Area Under the Concentration-time Curve From Time Zero to Infinity)

Bioequivalence based on AUC0-inf. (NCT00846885)
Timeframe: Blood samples collected over a 12 hour period.

Interventionng*h/mL (Mean)
Test (Sumatriptan)314.996
Reference (Imitrex®)298.953

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AUC0-t (Area Under the Concentration-time Curve From Time Zero to Time of Last Measurable Concentration)

Bioequivalence based on AUC0-t. (NCT00847405)
Timeframe: Blood samples collected over a 12 hour period.

Interventionng*h/mL (Mean)
Test (Sumatriptan)258.76
Reference (Imitrex®)252.26

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AUC0-inf (Area Under the Concentration-time Curve From Time Zero to Infinity)

Bioequivalence based on AUC0-inf. (NCT00847405)
Timeframe: Blood samples collected over a 12 hour period.

Interventionng*h/mL (Mean)
Test (Sumatriptan)268.5
Reference (Imitrex®)260.47

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Cmax (Maximum Observed Concentration of Drug Substance in Plasma)

Bioequivalence based on Cmax. (NCT00847405)
Timeframe: Blood samples collected over a 12 hour period.

Interventionng/mL (Mean)
Test (Sumatriptan)57.26
Reference (Imitrex®)56.66

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Change in Scores From Completeness of Response Survey (CORS)

"CORS scores for Pain (0-4), Associated Symptoms (0-4), Limbic/Affective Symptoms (0-5), and Speed of Return to Functionality (1-5), represent outcome measures that are relevant to patients. Higher scores represent better treatment efficacy.~The analysis compares CORS scores for usual triptan (pre-study) versus (vs.) Treximet (study medication)." (NCT00893737)
Timeframe: Visit 1 (screening) and Visit 2 (study completion following 2-month treatment period)

InterventionUnits on a scale (Mean)
Pain ScoreAssociated Symptoms ScoreLimbic Symptoms ScoreFunctionality Score
Treximet0.170.070.030.10

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Paired T-test Indicating Greater Subject Satisfaction With Treximet Over Usual Pre-study Triptan as Determined by the Revised Patient Perception of Migraine Questionnaire (PPMQ-R)

Scores calculated for (1) Efficacy (2) Functionality (3) Ease of use (4) Cost. Higher score represents better treatment satisfaction. (NCT00893737)
Timeframe: Visit 1 (screening) and Visit 2 (study completion following 2-month treatment period)

InterventionUnits on a scale (Mean)
EfficacyFunctionalityEase of UseCost
Treximet8.6113.862.767.28

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Percent of Participants Reporting Treximet Provides Therapeutic Advantage Over Usual Pre-study Triptan

CORS completed at Visit 1 regarding participant pre-study triptan and at Visit 2 regarding Treximet taken in study. Areas of therapeutic advantage evaluated: How often does 1 dose completely relieve (1) headache pain (2) neck/shoulder pain (3) nausea (4) light sensitivity (5) sound sensitivity (6) irritability. How quickly can/do you (1) concentrate or think clearly (2) resume normal activities (3) function normally (4) feel completely normal. How confident are you that (1) one dose will completely relieve migraine within 2 hours (2) once relieved, migraine will not return within 24 hours. (NCT00893737)
Timeframe: Visit 1 (screening) and Visit 2 (study completion following 2-month treatment period)

InterventionPercent of Participants (Number)
How often 1 dose relieves headache painHow often 1 dose relieves neck/shoulder painHow often 1 dose relieves nauseaHow often 1 dose relieves light sensitivityHow often 1 dose relieves sound sensitivityHow often 1 dose relieves irritabilityHow quickly can you concentrate or think clearlyHow quickly can you resume normal activitiesHow quickly can you function normallyHow quickly do you feel completely normalConfidence 1 dose will relieve migraine in 2 hoursConfidence migraine will not return in 24 hours
Treximet425243424536313232363338

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Pain Relief (PR)

Pain severity was rated by the participants in a paper diary. Pain severity rating scale: 0 (no pain), 1 (mild pain), 2 (moderate pain), or 3 (severe pain). Pain relief (PR) is defined as a reduction in headache severity from Grade 3/2 at baseline to Grade 1/0 post dose. (NCT00894556)
Timeframe: 2 hours post dose

,
Interventionattacks (Number)
Resulting in PR at 2 hours post doseNot resulting in PR at 2 hours post dose
Placebo2178
Rizatriptan102100

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Pain Freedom (PF)

Headache pain severity, relative to the administration of study medication, was rated by the participants in a paper diary. Pain severity rating scale: 0 (no pain), 1 (mild pain), 2 (moderate pain), or 3 (severe pain). Pain freedom (PF) is defined as a reduction in headache severity from Grade 3/2 at baseline to Grade 0 (no pain) post dose. (NCT00894556)
Timeframe: 2 hours post dose

,
Interventionattacks (Number)
Resulting in PF at 2 hours post doseNot resulting in PF at 2 hours post dose
Placebo1287
Rizatriptan46156

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Presence or Absence of Associated Symptoms (Photophobia, Phonophobia, Nausea, and Vomiting) at 2 Hours After Treatment

Participants who recorded the presence or absence of the associated symptoms photophobia, phonophobia, nausea, and vomiting at 2 hours after treatment. (NCT00897104)
Timeframe: 2 hours after treatment

,,
InterventionParticipants (Number)
2-hour PhotophobiaNo 2-hour Photophobia2-hour PhonophobiaNo 2-hour Phonophobia2-hour NauseaNo 2-hour NauseaNot Analyzed for Nausea2-hour VomitingNo 2-hour VomitingNot Analyzed for Vomiting
Placebo66144733483026677
Rizatriptan 5 mg1611891262241052432123308
Sumatriptan 5 mg15320112522913122121233012

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Pain Relief at 2 Hours After Treatment

Participants reporting pain relief defined as a reduction of headache severity from grades 2 or 3 (moderate or severe pain) at baseline to grades 0 or 1 (no headache or mild pain) at 2 hours after treatment (NCT00897104)
Timeframe: 2 hours after treatment

,,
InterventionParticipants (Number)
2-hour pain reliefNo 2-hour pain relief
Placebo1862
Rizatriptan 5 mg223129
Sumatriptan 5 mg238118

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Pain Free at 2 Hours After Treatment

Participants pain free (defined as a reduction of headache severity to grade 0 [no pain]) at 2 hours after treatment. Each participant rated headache severity on a 4-grade scale (0 = no headache; 1 = mild pain; 2 = moderate pain; 3 = severe pain). (NCT00897104)
Timeframe: 2 hours after treatment

,,
InterventionParticipants (Number)
2-hour pain freedomNo 2-hour pain freedom
Placebo278
Rizatriptan 5 mg95257
Sumatriptan 5 mg113243

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Participants Who Used Escape Medication 2 Hours After the Treatment Dose

Escape medication is defined as rescue medication for participants who experienced lack of efficacy from the study medication. (NCT00897104)
Timeframe: 2 hours after treatment

,,
InterventionParticipants (Number)
Used Escape MedicationDid not Use Escape Medication
Placebo3347
Rizatriptan 5 mg73282
Sumatriptan 5 mg55302

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Time to Relief Within 2 Hours After Treatment

Participants reporting time to relief (defined as the first time that a participant reported grade 0 or 1 in headache severity within 2 hours after treatment (for the comparison of rizatriptan 5 mg and sumatriptan 50 mg). (NCT00897104)
Timeframe: within 2 hours after treatment

,,
InterventionParticipants (Number)
First pain relief within 2 hrsPain relief did not occur within 2 hrs
Placebo2456
Rizatriptan 5 mg231121
Sumatriptan 5 mg247109

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Lack of Functional Disability at 2 Hours After Treatment as Measured by the Level of Impairment in Daily Activities

Participants with no functional disability measured by the level of impairment to daily activities at 2 hours after treatment. Each participant rated functional disability on a 4-grade scale (0 =normal; 1 = daily activities mildly impaired; 2 = daily activities severely impaired; 3 =unable to carry out daily activities, required bed rest). (NCT00897104)
Timeframe: 2 hours after treatment

,,
InterventionParticipants (Number)
NormalMildly ImpairedSeverely ImpairedRequired Bed Rest
Placebo4281830
Rizatriptan 5 mg1081523852
Sumatriptan 5 mg1161484249

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Duration of Relief (Time to Recurrence From the Time of First Recorded Pain Relief [Grade = 0 or 1])

Duration of relief or the time to recurrence from the time of first recorded pain relief (grade = 0 or 1) was calculated for responders who had a headache recurrence (NCT00897104)
Timeframe: 24 hours

InterventionHours (Mean)
Rizatriptan 5 mg11.07
Sumatriptan 5 mg11.58
Placebo14.38

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Functional Status at 2 Hours After Dose

Patients with no functional disability measured by the level of impairment to daily activities at 2 hours after treatment. Each patient rated functional disability on a 4-grade scale (0 = no functional disability; 1 = daily activities mildly impaired; 2 = daily activities severely impaired; 3 = unable to carry out daily activities, requires bed rest). (NCT00898677)
Timeframe: 2 hours after dose

,,,
InterventionParticipants (Number)
No functional disabilityMildly impairedSeverely impairedRequired bed rest
Placebo31593336
Rizatriptan 10 mg1601236042
Rizatriptan 5 mg52622723
Sumatriptan 100 mg1261426752

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Nausea at 2 Hours After Dose

Patients who recorded the presence or absence of nausea 2 hours after dose (NCT00898677)
Timeframe: 2 hours after dose

,,,
Interventionparticipants (Number)
2-hour NauseaNo 2-hour Nausea
Placebo6891
Rizatriptan 10 mg95290
Rizatriptan 5 mg37127
Sumatriptan 100 mg128259

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Pain Relief at 2 Hours After Dose

Patients reporting pain relief defined as a reduction of headache severity from grades 2 or 3 (moderate or severe pain) at baseline to grades 0 or 1 (no headache or mild pain) at 2 hours after treatment (NCT00898677)
Timeframe: 2 hours after dose

,,,
InterventionParticipants (Number)
2-hour pain reliefNo 2-hour pain relief
Placebo6495
Rizatriptan 10 mg258127
Rizatriptan 5 mg9965
Sumatriptan 100 mg239148

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Time to Relief Within 2 Hours After Dose

Patients reporting time to relief defined as the first time point at which a patient reported headache severity grade 1 or 0 (mild pain or no headache) within 2 hours after dose (NCT00898677)
Timeframe: within 2 hours after dose

,,,
InterventionParticipants (Number)
First pain relief within 2 hrsPain relief did not occur within 2 hrs
Placebo7287
Rizatriptan 10 mg265120
Rizatriptan 5 mg10262
Sumatriptan 100 mg247140

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Pain Free at 2 Hours After Dose

Patients pain free (defined as a reduction of headache severity to grade 0 [no pain]) at 2 hours after treatment. Each patient rated headache severity on a 4-point scale (0 = no headache; 1 = mild pain; 2 = moderate pain; 3 = severe pain). (NCT00898677)
Timeframe: 2 hours after dose

,,,
InterventionParticipants (Number)
2-hour Pain freedomNo 2-hour pain freedom
Placebo15139
Rizatriptan 10 mg155230
Rizatriptan 5 mg41123
Sumatriptan 100 mg127260

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24 Hours Post Administration - Incidence of Complete Headache Relief, Photophobia, Phonophobia and Nausea

"Complete headache relief is defined as reduction of headache severity from moderate or severe to absent.~Presence of Photophobia and Phonophobia measured on a 2-point scale: 0 = absent; 1 = present~Nausea was measured on a 4-point scale: 0 = no nausea; 1 = mild nausea; 2 = moderate nausea; 3 = severe nausea" (NCT00920686)
Timeframe: 24 hours

,,
InterventionParticipants (Number)
Complete Headache Relief-Observed CasesPhotophobia-Shift from Baseline (present-absent)Phonophobia-Shift from Baseline (present-absent)Nausea Score-Improvement from BaselineOverall Eval-Study Medication-(Good/Excellent)
NXN-188 600 mg3549414030
Placebo3751473924
Sumatriptan Succinate3848384435

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Time (Hours) to First Use of Rescue Medication

(NCT00920686)
Timeframe: 24 hours

Interventionhours (Median)
PlaceboNA
NXN-188NA
Sumatriptan SuccinateNA

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2 Hours Post Administration - Incidence of Complete Headache Relief, Photophobia, Phonophobia and Nausea

"Complete headache relief is defined as reduction of headache severity from moderate or severe to absent.~Presence of Photophobia and Phonophobia measured on a 2-point scale: 0 = absent; 1 = present~Nausea was measured on a 4-point scale: 0 = no nausea; 1 = mild nausea; 2 = moderate nausea; 3 = severe nausea" (NCT00920686)
Timeframe: 2 hours

,,
InterventionParticipants (Number)
Complete Headache Relief-Observed CasesPhotophobia-Shift from Baseline (present-absent)Phonophobia-Shift from Baseline (present-absent)Nausea Score-Improvement from Baseline
NXN-188 600 mg6143017
Placebo12161818
Sumatriptan Succinate 100 mg12302223

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Headache Relief and Recurrence (Observed Cases)

"Headache relief is defined as a ≥ 1-point reduction from baseline in Headache Severity Score. The Headache Severity Score is a four-point scale: 0=no pain; 1 = mild pain; 2 = moderate pain; and 3 = severe pain.~Headache recurrence is defined as any subject that experiences headache relief within 4 hours, who did not use rescue medication, and who experienced a worsening of their headache to moderate or severe within 24 hours following study drug administration." (NCT00920686)
Timeframe: 2, 4 and up to 24 hours

,,
Interventionpercentage of participants (Number)
Headache Relief - 2 hoursHeadache Relief - 4 hoursHeadache Recurrence
NXN-188 600 mg62.081.111.1
Placebo59.673.55.6
Sumatriptan Succinate 100 mg69.181.813.9

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4 Hours Post Administration - Incidence of Complete Headache Relief, Photophobia, Phonophobia and Nausea

"Complete headache relief is defined as reduction of headache severity from moderate or severe to absent.~Presence of Photophobia and Phonophobia measured on a 2-point scale: 0 = absent; 1 = present~Nausea was measured on a 4-point scale: 0 = no nausea; 1 = mild nausea; 2 = moderate nausea; 3 = severe nausea" (NCT00920686)
Timeframe: 4 hours

,,
InterventionParticipants (Number)
Complete Headache Relief-Observed CasesPhotophobia-Shift from Baseline (present-absent)Phonophobia-Shift from Baseline (present-absent)Nausea Score-Improvement from Baseline
NXN-188 600 mg19292526
Placebo21312523
Sumatriptan Succinate 100 mg22302129

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Percentage of Participants Who Used Rescue Medication Between the Time of Dosing and 240 Minutes Post-Treatment

Rescue medication included one of the following: a single oral dose of a nonsteroidal anti-inflammatory drug (NSAID) or acetaminophen, not to exceed the maximum recommended single dose; and anti-emetics (a drug to prevent vomiting). (NCT00963937)
Timeframe: within 240 minutes post-treatment (Randomization through Final Visit [Week 6])

Interventionpercentage of participants (Number)
Placebo12.9
Sumatriptan 25 mg12.1
Sumatriptan 50 mg14.6
Sumatriptan Pooled13.5

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Percentage of Participants Who Reported Pain Relief at 120 Minutes Post-Treatment

Pain relief was defined as at least a 2-grade reduction in pain intensity on a 5-grade scale in participants who had not used headache rescue medication before assessment. A pain intensity score of 5 was assigned for all subsequent assessments if a participant took rescue medication (a single oral dose for the treatment of migraine pain or associated symptoms). The 5-grade scale is a participant's self-rating scale to assess the pain intensity of a migraine with the following scores: 1 = none, 2 = mild, 3 = mild to moderate, 4 = moderate to severe, and 5 = severe. (NCT00963937)
Timeframe: 120 minutes post-treatment (Randomization through Final Visit [Week 6])

Interventionpercentage of participants (Number)
Placebo38.6
Sumatriptan Pooled31.1

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Percentage of Participants Who Were Nausea Free at 30, 60, 120, and 240 Minutes Post-Treatment

"Nausea is one of the associated symptoms of a migraine. A participant was assessed as nausea free when the symptom was recorded as absent at each time point in his or her patient diary. Nausea was recorded as present for all subsequent assessments if a participant took rescue medication." (NCT00963937)
Timeframe: 30, 60, 120, and 240 minutes post-treatment (Randomization through Final Visit [Week 6])

,,,
Interventionpercentage of participants (Number)
30 minutes post-treatment60 minutes post-treatment120 minutes post-treatment240 minutes post-treatment
Placebo47.666.781.081.0
Sumatriptan 25 mg40.040.070.070.0
Sumatriptan 50 mg12.512.550.050.0
Sumatriptan Pooled27.827.861.161.1

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Percentage of Participants Who Were Photophobia Free at 30, 60, 120, and 240 Minutes Post-Treatment

"Photophobia (sensitivity to light) is one of the associated symptoms of a migraine. A participant was assessed as photophobia free when the symptom was recorded as absent at each time point in his or her patient diary. Photophobia was recorded as present for all subsequent assessments if a participant took rescue medication." (NCT00963937)
Timeframe: 30, 60, 120, and 240 minutes post-treatment (Randomization through Final Visit [Week 6])

,,,
Interventionpercentage of participants (Number)
30 minutes post-treatment60 minutes post-treatment120 minutes post-treatment240 minutes post-treatment
Placebo16.744.452.869.4
Sumatriptan 25 mg13.326.760.080.0
Sumatriptan 50 mg15.438.546.269.2
Sumatriptan Pooled14.332.153.675.0

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Percentage of Participants Who Were Phonophobia Free at 30, 60, 120, and 240 Minutes Post-Treatment

"Phonophobia (sensitivity to sound) is one of the associated symptoms of a migraine. A participant was assessed as phonophobia free when the symptom was recorded as absent at each time point in his or her patient diary. Phonophobia was recorded as present for all subsequent assessments if a participant took rescue medication." (NCT00963937)
Timeframe: 30, 60, 120, and 240 minutes post-treatment (Randomization through Final Visit [Week 6])

,,,
Interventionpercentage of participants (Number)
30 minutes post-treatment60 minutes post-treatment120 minutes post-treatment240 minutes post-treatment
Placebo22.745.563.672.7
Sumatriptan 25 mg50.057.164.378.6
Sumatriptan 50 mg12.525.043.868.8
Sumatriptan Pooled30.040.053.373.3

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Percentage of Participants Who Were Pain Free at 30, 60, 120, and 240 Minutes Post-Treatment

Pain free was defined as a post-treatment pain intensity score of 1 on a 5-grade scale in participants who had not used headache rescue medication before assessment. A pain intensity score of 5 was assigned for all subsequent assessments if a participant took a rescue medication. The 5-grade scale is a participant's self-rating scale to assess the pain intensity of a migraine with the following scores: 1 = none, 2 =mild, 3=mild to moderate, 4=moderate to severe, and 5=severe. (NCT00963937)
Timeframe: 30, 60, 120, and 240 minutes post-treatment (Randomization through Final Visit [Week 6])

,,,
Interventionpercentage of participants (Number)
30 minutes post-treatment60 minutes post-treatment120 minutes post-treatment240 minutes post-treatment
Placebo2.912.928.647.1
Sumatriptan 25 mg03.024.263.6
Sumatriptan 50 mg2.42.419.539.0
Sumatriptan Pooled1.42.721.650.0

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Percentage of Participants Who Were Free of Vomiting at 30, 60, 120, and 240 Minutes Post-Treatment

"Vomiting is one of the associated symptoms of a migraine. A participant was assessed as being free of vomiting when the symptom was recorded as absent at each time point in his or her patient diary. Vomiting was recorded as present for all subsequent assessments if a participant took a rescue medication." (NCT00963937)
Timeframe: 30, 60, 120, and 240 minutes post-treatment (Randomization through Final Visit [Week 6])

,
Interventionpercentage of participants (Number)
30 minutes post-treatment60 minutes post-treatment120 minutes post-treatment240 minutes post-treatment
Sumatriptan 25 mg00100.0100.0
Sumatriptan Pooled00100.0100.0

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Percentage of Participants Who Reported Pain Relief at 30, 60, 120, and 240 Minutes Post-Treatment

Pain relief was defined as at least a 2-grade reduction in pain intensity on a 5-grade scale in participants who had not used headache rescue medication before assessment. A pain intensity score of 5 was assigned for all subsequent assessments if a participant took rescue medication (a single oral dose for the treatment of migraine pain or associated symptoms). The 5-grade scale is a participant's self-rating scale to assess the pain intensity of a migraine with the following scores: 1 = none, 2 = mild, 3 = mild to moderate, 4 = moderate to severe, and 5 = severe. (NCT00963937)
Timeframe: 30, 60, 120, and 240 minutes post-treatment (Randomization through Final Visit [Week 6])

,,,
Interventionpercentage of participants (Number)
30 minutes post-treatment60 minutes post-treatment120 minutes post-treatment240 minutes post-treatment
Placebo4.318.638.651.4
Sumatriptan 25 mg09.133.366.7
Sumatriptan 50 mg9.87.329.361.0
Sumatriptan Pooled5.48.131.163.5

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Treatment Preference

Number of subjects preferring Sumavel DosePro compared to their pre-study migraine treatment (Prefer Sumavel DosePro vs. No Preference or Prefer Other Treatment). (NCT01016834)
Timeframe: After 4 migraines or 60 days

Interventionparticipants (Number)
Sumavel DosePro74

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Overall Satisfaction

"Change from baseline in overall subject satisfaction with migraine treatments. Patient Perception of Migraine Questionnaire-Revised, question 3c Overall satisfaction was the measure. Baseline measured subjects satisfaction with past migraine treatments. End of study measured subject's satisfaction with migraine treatment by Sumavel DosePro. PPMQ-R scale (1-7 scale; 1=very satisfied)is transformed to a 0-100 scale (100=very satisfied)" (NCT01016834)
Timeframe: After 4 migraines or 60 days

InterventionScale of 0-100; 100= very satisfied (Mean)
Sumavel DosePro73.7

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Treatment Confidence

Number of subjects who indicated they were confident or very confident in treating repeated migraine attacks with Sumavel DosePro at end of treatment. (NCT01016834)
Timeframe: After 4 migraines or 60 days

Interventionparticipants (Number)
Sumavel DosePro136

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Change in Number of Associated Headache Symptoms

Change in number of associated headache symptoms at Day 0 vs. Day 30 in Treximet arm vs. Placebo arm. Associated headache symptoms measured included number of incidences of: sleeplessness, difficulty thinking, and bodily pain. (NCT01053507)
Timeframe: Day 0, Day 30

,
Interventionchange in number of symptoms (Mean)
Change in SleeplessnessChange in Difficulty ThinkingChange in Bodily Pain
Placebo-2.300.00-3.80
Treximet2.430.14-1.71

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Headache Impact Test-6 (HIT-6) Score

The Headache Impact Test-6 (HIT-6) scale measures the impact of headache symptoms on subject's life. Possible scores range from 36 to 78. Score of 48 or less indicates headache has little impact on life. Score of 60-78 indicative of very severe impact. (NCT01053507)
Timeframe: Day 0, Day 30

,
Interventionunits on a scale (Mean)
Day 0Day 30
Placebo61.9161.91
Treximet59.4358.57

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Mental Efficiency Workload Test (MEWT) Performance Index

The Mental Efficiency Workload Test (MEWT) performance index is a scale with minimum and maximum values of 1 to 10, 1 indicates the poorest level and 10 indicates the best level of cognitive functioning. (NCT01053507)
Timeframe: Day 0, Day 30

,
Interventionunits on a scale (Mean)
Day 0Day 30
Placebo3.43.11
Treximet3.103.17

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Migraine Specific Quality of Life Questionnaire (MSQ)

The Migraine-Specific Quality of Life Questionnaire (MSQ) is a scale that measures the impact of migraine across three aspects: role function-restrictive (RR), role function-preventive (RP), and emotional function (EF). Possible scores on each subscale range from a 0 to 100 scale such that higher scores indicate better quality of life. (NCT01053507)
Timeframe: Day 0, Day 30

,
Interventionunits on a scale (Mean)
Day 0 - Role Function-Restrictive ScoreDay 30 - Role Function-Restrictive ScoreDay 0 - Role Function-Preventive ScoreDay 30 - Role Function-Preventive ScoreDay 0 - Emotional Function ScoreDay 30 - Emotional Function Score
Placebo45.7150.3968.6469.5550.9157.58
Treximet6059.5979.29806065.03

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Headache Days

Change in number of headache days at Day 0 vs. Day 30 in Treximet arm vs. Placebo arm. (NCT01053507)
Timeframe: Day 0, Day 30

Interventiondays (Mean)
Treximet-3.00
Placebo-0.30

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Number of Participants Who Returned to the Emergency Department for Management of Headache

We report the number of patient who returned to the emergency department for management of headache (NCT01071317)
Timeframe: 1 month after study enrollment

InterventionParticipants (Count of Participants)
Comprehensive Care1
Typical Care3

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Number of Participants Who Report They Are Comfortable With Disease Management, as Measured by a Three-item Likert Scale

Participants were asked to describe themselves as very comfortable, somewhat comfortable, or uncomfortable. Reported here are those who were very comfortable (NCT01071317)
Timeframe: 1 month after study enrollment

InterventionParticipants (Count of Participants)
Comprehensive Care10
Typical Care6

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Migraine Functional Impairment as Measured by Score on the Headache Impact Test 6 (HIT6) Scale

This is a standardized instrument commonly used in migraine research. Participants answer 6 Likert questions about the impact of migraine on their daily life. A score of 36, the lowest possible score, indicates minimal functional impairment. A score of 78, the highest possible score, indicates substantial functional impairment (NCT01071317)
Timeframe: 1 month after study enrollment

Interventionunits on a scale (Mean)
Comprehensive Care59
Typical Care56

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Number of Participants Who Report Satisfaction With Treatment, as Measured by a Three Item Likert Scale

Participants could report that they were completely satisfied, mostly satisfied or unsatisfied. Reported here are the number who were unsatisfied. (NCT01071317)
Timeframe: 1 month after study enrollment

InterventionParticipants (Count of Participants)
Comprehensive Care4
Typical Care4

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Lost Activity Time

This outcome measure was lost activity time as measured by a variant of the Work Productivity and Activity Impairment Scale (WPAI) at 6 months.The primary efficacy dataset included the 37 patients that completed both phases of the study and uses the last observed headache. The primary efficacy dataset included the 37 patients that completed both phases of the study and uses the last observed headache. The unit of analysis is hours lost. The higher the score the greater impact on productivity. The range depends on the length of the attack, but in the sample among all observed attacks, lost work productivity ranged from 0-10.5 hours, while lost non-workplace activity time ranged from 0 to 8.95 hours. The total lost productivity is the sum of lost work productivity and lost non-workplace activity time. (NCT01086358)
Timeframe: 6 Months

Interventionhours (Mean)
Arm 1 - Triptan1.89
Arm 2 - Sumatriptan/Naproxen Sodium (Treximet) Arm1.22

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Workplace Productivity and Activity Impairment Scale (WPAI).

The primary outcome measure was lost productivity (workplace productivity + non-workplace activity time) as measured by a variant of the Work Productivity and Activity Impairment Scale (WPAI) at 6 months. The primary efficacy dataset included the 37 patients that completed both phases of the study and uses the last observed headache. The unit of analysis is hours lost. The higher the score the greater impact on productivity. The range depends on the length of the attack, but in the sample among all observed attacks, lost work productivity ranged from 0-10.5 hours, while lost non-workplace activity time ranged from 0 to 8.95 hours. The total lost productivity is the sum of lost work productivity and lost non-workplace activity time. (NCT01086358)
Timeframe: 6 months

Interventionhours (Mean)
Arm 1 - Triptan4.15
Arm 2 - Sumatriptan/Naproxen Sodium (Treximet) Arm2.44

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Lost Workplace Productivity

This outcome measure was lost workplace productivity as measured by a variant of the Work Productivity and Activity Impairment Scale (WPAI) at 6 months.The primary efficacy dataset included the 37 patients that completed both phases of the study and uses the last observed headache. The primary efficacy dataset included the 37 patients that completed both phases of the study and uses the last observed headache. The unit of analysis is hours lost. The higher the score the greater impact on productivity. The range depends on the length of the attack, but in the sample among all observed attacks, lost work productivity ranged from 0-10.5 hours, while lost non-workplace activity time ranged from 0 to 8.95 hours. The total lost productivity is the sum of lost work productivity and lost non-workplace activity time. (NCT01086358)
Timeframe: 6 months

Interventionhours (Mean)
Arm 1 - Triptan2.25
Arm 2 - Sumatriptan/Naproxen Sodium (Treximet) Arm1.23

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Favorable Response on Migraine-ACT

The Migraine-ACT is a 4-item scale with yes/no responses. A score of 3 or more is considered favorable. The primary efficacy dataset included the 37 patients that completed both phases of the study and uses the last observed headache. The Migraine-ACT is reported as a binary measure (3 or more positive responses). The outcome presented included the percentage with a score of 3 or more, and the Odds ratio comparing the two treatments. (NCT01086358)
Timeframe: 6 months

Interventionpercentage of favorable responses (Mean)
Arm 1 - Triptan46
Arm 2 - Sumatriptan/Naproxen Sodium (Treximet) Arm71

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Migraine Headache Days With Greater Than 50% Reduction

Number of subjects with at least 50% reduction in number of migraine headache days reported in Baseline vs. Treatment Period months 1(days 31-60), 2(days 61-90), and 3(days 91-120)in the Sumatriptan/Naproxen Sodium arm vs. Naproxen Sodium arm. (NCT01090050)
Timeframe: Baseline Period collected at Day 31, Treatment Period Months 1, 2, and 3 collected at Days 61, 92, and 121 respectively.

,
Interventionparticipants (Number)
Baseline to Treatment Period Month 1Baseline to Treatment Period Month 2Baseline to Treatment Period Month 3
Naproxen Sodium434
Sumatriptan/Naproxen Sodium303

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Migraine Headache Duration From Onset to Pain Free

"Comparing mean migraine duration from onset to pain free from Baseline Period (Days 1-30), to each of the Treatment Period Months 1(days 31-60), 2(days 61-90), and 3(days 91-120) in Sumatriptan/Naproxen Sodium arm vs. Naproxen Sodium arm. Percent change was calculated by determining percent change in each subject, from each Treatment Period month compared to Baseline. The following formula was used for each treatment period month calculation.~e.g. Percent change=[(mean migraine duration from onset to pain free during Treatment Period Month 3(days 91-120)-mean migraine duration from onset to pain free during Baseline(days 1-30)/mean duration from onset to pain free during Baseline(days 1-30)]*100%)" (NCT01090050)
Timeframe: Baseline Period collected at Day 31, Treatment Period Months 1, 2, and 3 collected at Days 61, 91, and 121 respectively.

,
Interventionpercent hours of migraine duration (Mean)
Baseline to Treatment Period Month 1Baseline to Treatment Period Month 2Baseline to Treatment Period Month 3
Naproxen Sodium26.3728.9119.65
Sumatriptan/Naproxen Sodium167.83176.18151.49

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Migraine Headache Duration From Time of Treatment to Pain Free

"Comparing mean migraine duration from time of treatment to pain free from Baseline Period (Days 1-30), to each of the Treatment Period Months 1(days 31-60), 2(days 61-90), and 3(days 91-120) in Sumatriptan/Naproxen Sodium arm vs. Naproxen Sodium arm. Percent change was calculated by determining percent change in each subject, from each Treatment Period month compared to Baseline. The following formula was used for each treatment period month calculation.~e.g. Percent change=[(mean migraine duration from time of treatment to pain free during Treatment Period Month 3(days 91-120)-mean migraine duration from time of treatment to pain free during Baseline(days 1-30)/mean duration from time of treatment to pain free during Baseline(days 1-30)]*100%)" (NCT01090050)
Timeframe: Baseline Period collected at Day 31, Treatment Period Months 1, 2, and 3 collected at Days 61, 91, and 121 respectively.

,
Interventionpercent hours of migraine duration (Mean)
Baseline to Treatment Period Month 1Baseline to Treatment Period Month 2Baseline to Treatment Period Month 3
Naproxen Sodium24.5828.4523.15
Sumatriptan/Naproxen Sodium176.70175.78151.12

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Percent Change of Doses of Study Medication

"Comparing the number of doses of study medication taken during Baseline Period(days 1-30) of triptans(Group A) and non-steroidal anti-inflammatory drugs(NSAIDS)(Group B)to the number of doses of study medication taken during Treatment Period Months 1(days 31-60), 2(days 61-90), and 3(days 91-120)in the Sumatriptan/Naproxen Sodium arm vs. Naproxen Sodium arm.~e.g.Percent change=[(number of doses of study medication during Treatment Period Month 3(days 91-120)-number of doses of study medication during Baseline(days 1-30)/number of doses of study medication during Baseline(days 1-30)]*100%)." (NCT01090050)
Timeframe: Baseline Period collected at Day 31, Treatment Period Months 1, 2, and 3 collected at Days 61, 92, and 121 respectively.

,
Interventionpercent doses of study medication (Mean)
Baseline to Treatment Period Month 1Baseline to Treatment Period Month 2Baseline to Treatment Period Month 3
Naproxen Sodium825.6239.8135.6
Sumatriptan/Naproxen Sodium173.840.140.0

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Percent Change of Migraine Headache Days in All Treatment Periods Compared to Baseline

"Comparing number of migraine headache days from Baseline to Treatment Period Months 1, 2, and 3 in the Sumatriptan/Naproxen Sodium arm vs. Naproxen Sodium arm.~Comparing the number of migraine headache days reported from Baseline Period days 1-30 to number of migraine headache days reported in Treatment Period days Months 1(days 31-60), 2(days 61-90),and 3(days 91-120)in the Sumatriptan/Naproxen Sodium arm versus (vs.) Naproxen Sodium arm. Each treatment period month percent change was individually compared to Baseline. The following formula was used for each treatment period calculation.~e.g. percent change=[(total headache days during Treatment Period Month 3(days 91-120)-total headache days during Baseline(days 1-30)/total headache days during Baseline(days 1-30)]*100%)" (NCT01090050)
Timeframe: Baseline Period (days 1-30) collected at Day 31, Treatment Period Months 1, 2, and 3 collected at Days 61, 91, and 121, respectively.

,
Interventionpercent migraine headache days per month (Mean)
Baseline to Treatment Period Month 1Baseline to Treatment Period Month 2Baseline to Treatment Period Month 3
Naproxen Sodium-61.55-45.42-56.37
Sumatriptan/Naproxen Sodium-26.22-2.96-8.06

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Percent Change of Migraine Headache Days Compared to Baseline

Comparing the number of migraine headache days during Baseline Period days 1-30 to number of migraine headache days reported in Treatment Period days 91-120 in the Sumatriptan/Naproxen Sodium arm versus (vs.) Naproxen Sodium arm. Percent change=[(total headache days during Treatment Period Month 3(days 91-120)-total headache days during Baseline(days 1-30)/total headache days during Baseline(days 1-30)]*100%) (NCT01090050)
Timeframe: Day 121 (following 30 day Baseline Period and Treatment Period days 91-120.

Interventionpercent migraine headache days per month (Mean)
Sumatriptan/Naproxen Sodium-8.06
Naproxen Sodium-56.37

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Migraine Disability Assessment(MIDAS)Questionnaire Total Score

"Change in Migraine Disability Assessment (MIDAS) total score (effect migraine headaches have on subjects daily function) from Baseline (Day 31) to 3 months after Baseline to end of Treatment Period Month 3(Day 121) following final dose of study medication in the Sumatriptan/Naproxen Sodium arm vs. the Naproxen Sodium arm.~Total score of disability ranges:~0 to 5, MIDAS Grade I, Little or no disability~6 to 10, MIDAS Grade II, Mild disability~11 to 20, MIDAS Grade III, Moderate disability~21+, MIDAS Grade IV, Severe disability Score ranges from 0-450. No subscales are present." (NCT01090050)
Timeframe: Baseline MIDAS collected at Day 31, Post final dose study at Day 121.

,
Interventionscores on a scale (Mean)
Day 31Day 121
Naproxen Sodium81.216.4
Sumatriptan/Naproxen Sodium76.656.3

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Compliance With Lifestyle Changes

Self-assessed grade of compliance with lifestyle modification changes (where A=1, B=2, C=3, D=4, and F=5) in the Sumatriptan/Naproxen Sodium arm vs. Naproxen Sodium arm. Lower scores indicate a better outcome. Higher scores indicate a worse outcome. (NCT01090050)
Timeframe: Day 121

InterventionUnits on a scale (Mean)
Sumatriptan/Naproxen Sodium2.00
Naproxen Sodium2.40

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Change in the Total Serum Adiponectin (T-ADP)

Change in total serum adiponectin after treatment in responders and non responders (NCT01138150)
Timeframe: 30 minutes after treatment, 60 minutes after treatment, 120 minutes after treatment

Interventionug/mL (Mean)
Treatment Responders 30 Minutes After Treatment-0.96
Treatment Non-Responders 30 Minutes After Treatment0.25
Treatment Responders 60 Minutes After Treatment-0.97
Treatment Non-Responders 60 Minutes After Treatment0.29
Treatment Responders 120 Minutes After Treatment-0.98
Treatment Non-Responders0.24

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High Molecular Weight (HMW)-Adiponectin (ADP)

serum HMW-ADP levels after treatment in responders and non responders (NCT01138150)
Timeframe: 30 minutes after treatment, 60 minutes after treatment, 120 minutes after treatment

Interventionug/mL (Mean)
Treatment Responders 120 Minutes After Treatment-0.24
Treatment Non Responders 120 Minutes After Treatment-0.08
Treatment Responders 30 Minutes After Treatment-0.23
Treatment Non-Responders 30 Minutes After Treatment-0.14
Treatment Non-Responders 60 Minutes After Treatment-0.24
Treatment Responders 60 Minutes After Treatment-0.21

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High Molecular Weight (HMW): T-ADP

serum HMW:T-ADP levels after treatment in responders and non responders (NCT01138150)
Timeframe: 30 minutes, 60 minutes, 120 minutes after treatment

Interventionratio (Mean)
Treatment Responders 120 Minutes After Treatment-0.04
Treatment Non Responders 120 Minutes After Treatment0.01
Treatment Responders 30 Minutes After Treatment-0.02
Treatment Non-Responders 30 Minutes After Treatment0.01
Treatment Non-Responders 60 Minutes After Treatment0.01
Treatment Responders 60 Minutes After Treatment-0.02

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Leptin

serum leptin levels after treatment in responders and non responders (NCT01138150)
Timeframe: 30 minutes after treatment, 60 minutes after treatment, 120 minutes after treatment

Interventionug/mL (Mean)
Treatment Responders 120 Minutes After Treatment0.71
Treatment Non Responders 120 Minutes After Treatment0.89
Treatment Responders 30 Minutes After Treatment0.28
Treatment Non-Responders 30 Minutes After Treatment0.84
Treatment Non-Responders 60 Minutes After Treatment1.00
Treatment Responders 60 Minutes After Treatment0.02

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Low Molecular Weight (LMW)-ADP

serum LMW-ADP levels after treatment in responders and non responders (NCT01138150)
Timeframe: 30 minutes after treatment, 60 minutes after treatment, 120 minutes after treatment

Interventionug/mL (Mean)
Treatment Responders 120 Minutes After Treatment0.32
Treatment Non Responders 120 Minutes After Treatment-0.43
Treatment Responders 30 Minutes After Treatment0.15
Treatment Non-Responders 30 Minutes After Treatment-0.25
Treatment Non-Responders 60 Minutes After Treatment-0.45
Treatment Responders 60 Minutes After Treatment0.11

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Low Molecular Weight (LMW):Total (T)-ADP

serum LMW:T-ADP levels after treatment in responders and non responders (NCT01138150)
Timeframe: 30 minutes after treatment, 60 minutes after treatment, 120 minutes after treatment

Interventionratio (Mean)
Treatment Responders 120 Minutes After Treatment0.04
Treatment Non Responders 120 Minutes After Treatment-0.04
Treatment Responders 30 Minutes After Treatment-0.01
Treatment Non-Responders 30 Minutes After Treatment0.02
Treatment Non-Responders 60 Minutes After Treatment-0.04
Treatment Responders 60 Minutes After Treatment0.01

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Middle Molecular Weight (MMW)-ADP

serum MMW-ADP levels after treatment in responders and non responders (NCT01138150)
Timeframe: 30 minutes after treatment, 60 minutes after treatment, 120 minutes after treatment

Interventionug/mL (Mean)
Treatment Responders 120 Minutes After Treatment-0.02
Treatment Non Responders 120 Minutes After Treatment0.02
Treatment Responders 30 Minutes After Treatment-0.03
Treatment Non-Responders 30 Minutes After Treatment-0.02
Treatment Non-Responders 60 Minutes After Treatment0.16
Treatment Responders 60 Minutes After Treatment-0.03

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Resistin

serum resistin levels after treatment in responders and non responders (NCT01138150)
Timeframe: 30 minutes after treatment, 60 minutes after treatment, 120 minutes after treatment

Interventionug/mL (Mean)
Treatment Responders 120 Minutes After Treatment-0.95
Treatment Non Responders 120 Minutes After Treatment-0.97
Treatment Responders 30 Minutes After Treatment-1
Treatment Non-Responders 30 Minutes After Treatment-0.88
Treatment Non-Responders 60 Minutes After Treatment-1.36
Treatment Responders 60 Minutes After Treatment-0.79

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Percent of Subjects Who Are Free of Nausea at 2 Hours.

Subjects assessed severity of relevant symptom on a 4 point scale (0=none, …, 3=severe) at set time points after dosing through 4 hours. Subjects who indicated severity of relevant symptom=none at 2 hours were considered relevant symptom free at 2 hours (NCT01248468)
Timeframe: 2 hours

Interventionpercent of participants (Number)
Aspirin, Acetaminophen, and Caffeine70.6
Sumatriptan (100 mg)72.2
Placebo66.4

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Percent of Subjects Who Are Free of Phonophobia at 2 Hours.

Subjects assessed severity of relevant symptom on a 4 point scale (0=none, …, 3=severe) at set time points after dosing through 4 hours. Subjects who indicated severity of relevant symptom=none at 2 hours were considered relevant symptom free at 2 hours (NCT01248468)
Timeframe: 2 hours

InterventionPercent of participants (Number)
Aspirin, Acetaminophen, and Caffeine53.4
Sumatriptan (100 mg)60.9
Placebo46.2

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Percent of Subjects Who Are Free of Photophobia at 2 Hours.

Subjects assessed severity of relevant symptom on a 4 point scale (0=none, …, 3=severe) at set time points after dosing through 4 hours. Subjects who indicated severity of relevant symptom=none at 2 hours were considered relevant symptom free at 2 hours (NCT01248468)
Timeframe: 2 hours

InterventionPercent of participants (Number)
Aspirin, Acetaminophen, and Caffeine48.6
Sumatriptan (100 mg)52.3
Placebo40.8

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Percent of Subjects Who Are Pain Free at 2 Hours.

Subjects assessed severity of pain on a 4 point scale (0=none, …, 3=severe) at set time points after dosing through 4 hours. Subjects who indicated severity of pain=none at 2 hours were considered pain free at 2 hours (NCT01248468)
Timeframe: 2 hours

InterventionPercent of participants (Number)
Aspirin, Acetaminophen, and Caffeine34.7
Sumatriptan (100 mg)44.9
Placebo26.4

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Migraine Attacks With 50% Reduction

Number of subjects with at least a 50% reduction in number of migraine attacks reported in Baseline versus Treatment period Months 1, 2, and 3 in Sumatriptan/Naproxen Sodium arm vs. Naproxen Sodium arm (NCT01300546)
Timeframe: Baseline Period collected at Day 31, Treatment Period Months 1, 2, and 3 collected at Days 61, 91, and 121.

,
Interventionparticipants (Number)
Baseline to Treatment Period Month 1Baseline to Treatment Period Month 2Baseline to Treatment Period Month 3
Naproxen Sodium106
Sumatriptan/Naproxen Sodium324

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Compliance With Lifestyle Changes

Self-assessed grade of compliance with lifestyle modification changes (where A=1, B=2, C=3, D=4, and F=5; lower scores represent better outcomes) in Sumatriptan/Naproxen Sodium arm vs. Naproxen Sodium arm. (NCT01300546)
Timeframe: Day 121

Interventionscores on a scale (Mean)
Sumatriptan/Naproxen Sodium2.33
Naproxen Sodium2.43

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Percent Change of Headache Days Compared to Baseline

Comparing the number of migraine headache days during Baseline Period Days 1-30 to number or migraine headache days reported in Treatment Period Days 91-120 in Sumatriptan/Naproxen Sodium arm vs. Naproxen Sodium arm. Percent change=[ (total headache days during Treatment Period Month 3 (Days 91-120)-total headache days during Baseline (Days 1-30)/total headache days during Baseline (Days 1-30)]*100%). (NCT01300546)
Timeframe: Day 121 (following 30 day Baseline Period and Treatment Period Days 91-120)

Interventionpercent change of headache days (Mean)
Sumatriptan/Naproxen Sodium-13.50
Naproxen Sodium-36.50

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Doses of Study Medication

Total number of doses of study medication reported taken per participant in Treatment Period Months 1, 2, and 3 in Sumatriptan/Naproxen Sodium arm vs. Naproxen Sodium arm. (NCT01300546)
Timeframe: Treatment Period Months 1, 2, and 3 collected at Days 61, 91, and 121.

,
Interventiondoses of study medication (Mean)
Treatment Period Month 1Treatment Period Month 2Treatment Period Month 3
Naproxen Sodium9.368.868.50
Sumatriptan/Naproxen Sodium11.0010.2810.28

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Migraine Attacks

Comparing the number of migraine attacks reported from Baseline to the number of migraine attacks reported in Treatment Period Months 1(Days 31-60), 2(Days 61-90), and 3(Days 91-120) in Sumatriptan/Naproxen Sodium arm vs. Naproxen Sodium arm. Each treatment month percent change was individually compared to Baseline. The following formula was used for each treatment period calculation. e.g.,Percent change=[ (total migraine attacks days during Treatment Period Month 3 (Days 91-120)-total migraine attacks during Baseline (Days 1-30)/total migraine attacks during Baseline (Days 1-30)]*100%). (NCT01300546)
Timeframe: Baseline Period collected at Day 31, Treatment Period Months 1, 2, and 3 collected at Days 61, 91, and 121.

,
Interventionpercent change of migraine attacks (Mean)
Baseline to Treatment Period Month 1Baseline to Treatment Period Month 2Baseline to Treatment Period Month 3
Naproxen Sodium-12.23-9.03-39.12
Sumatriptan/Naproxen Sodium-4.35-2.88-8.63

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Headache Days With Greater Than 50% Reduction

Number of subjects with at least a 50% reduction in number of headache days reported in Baseline versus Treatment period Months 1, 2, and 3 in Sumatriptan/Naproxen Sodium arm vs. Naproxen Sodium arm. (NCT01300546)
Timeframe: Baseline Period collected at Day 31, Treatment Period Months 1, 2, and 3 collected at Days 61, 91, and 121.

,
Interventionparticipants (Number)
Baseline to Treatment Period Month 1Baseline to Treatment Period Month 2Baseline to Treatment Period Month 3
Naproxen Sodium336
Sumatriptan/Naproxen Sodium123

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Migraine Disability Assessment Test (MIDAS)

"Change in MIDAS total score from end of Baseline (Day 31) to end Treatment Period month 3 (Day 121) in the Sumatriptan/Naproxen Sodium arm vs. Naproxen Sodium arm.~Total score of disability ranges:~0 to 5, MIDAS Grade I, Little or no disability~6 to 10, MIDAS Grade II, Mild disability~11 to 20, MIDAS Grade III, Moderate disability~21+, MIDAS Grade IV, Severe disability No subscales are present." (NCT01300546)
Timeframe: Baseline MIDAS collected at Day 31, Post final dose study medication MIDAS collected at Day 121.

,
Interventionscores on a scale (Mean)
Baseline Day 31Day 121
Naproxen Sodium22.624.1
Sumatriptan/Naproxen Sodium28.727.9

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Migraine Duration From Onset to Pain Free

Comparing mean migraine duration from onset to painfree from Baseline(Days 1-30) to each month: Treatment Period Months 1 (Days 31-60), 2(Days 61-90), and 3(Days 91-120) in Sumatriptan/Naproxen Sodium arm vs. Naproxen Sodium arm. Percent change was calculated by determining percent change in each subject, from Treatment Period Month 3 and Baseline, then comparing the average change between each arm. The following formula was used for each treatment period calculation. e.g.,Percent change=[(mean duration from onset to painfree during Treatment Period Month 3 (Days 91-120)- mean duration from onset to painfree during Baseline (Days 1-30)/mean duration from onset to painfree during Baseline (Days 1-30)]*100%). (NCT01300546)
Timeframe: Baseline Period collected at Day 31, Treatment Period Months 1, 2, and 3 collected at Days 61, 91, and 121.

,
Interventionpercent change of migraine duration (Mean)
Baseline to Treatment Period Month 1Baseline to Treatment Period Month 2Baseline to Treatment Period Month 3
Naproxen Sodium-14.92-26.3570.84
Sumatriptan/Naproxen Sodium72.0435.8661.96

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Percent Change in Headache Days All Treatment Periods Compared to Baseline

Comparing the number of migraine headache days during Baseline Period Days 1-30 to number or migraine headache days reported in Treatment Period Month 1 (Days 31-60), Treatment Period Month 2 (Days 61-90), and Treatment Period Month 3 (Days 91-120) in Sumatriptan/Naproxen Sodium arm vs. Naproxen Sodium arm. e.g., Percent change=[ (total headache days during Treatment Period Month 3 (Days 91-120)-total headache days during Baseline (Days 1-30)/total headache days during Baseline (Days 1-30)]*100%). (NCT01300546)
Timeframe: Baseline Period collected at Day 31, Treatment Period Months 1, 2, and 3 collected at Days 61, 91, and 121.

,
Interventionpercent change of migraine headache days (Mean)
Baseline to Treatment Period Month 1Baseline to Treatment Period Month 2Baseline to Treatment Period Month 3
Naproxen Sodium-26.86-21.44-36.50
Sumatriptan/Naproxen Sodium-1.70-4.39-13.50

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Percent Change of Doses of Study Medication

% change in number of doses during Baseline of triptans (Group A) and non-steroidal anti-inflammatory drugs(NSAIDs) (Group B) vs. doses during Treatment Period Months 1, 2, and 3 of study medication in the Sumatriptan/Naproxen Sodium arm vs. Naproxen Sodium arm. e.g.,Percent change=[(number of doses during Treatment Period Month 3 (Days 91-120)- number of doses during Baseline (Days 1-30)/number of doses during Baseline (Days 1-30)]*100%). The total number of subjects used in this analysis is different than the total number of subjects as the analysis is only looking at those subjects that were taking one of the study medications during Baseline. (NCT01300546)
Timeframe: Treatment Period Months 1, 2, and 3 collected at Days 61, 91, and 121.

,
Interventionpercent change of study medication (Mean)
Baseline to Treatment Period Month 1Baseline to Treatment Period Month 2Baseline to Treatment Period Month 3
Naproxen Sodium160.876.4112.7
Sumatriptan/Naproxen Sodium130.8114.996.1

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Migraine Severity

Comparing migraine severity 2 hours after treatment from Baseline(Days 1-30) to migraine severity reported 2 hours after treatment in Treatment Period Months 1 (Days 31-60), 2(Days 61-90), and 3(Days 91-120) in Sumatriptan/Naproxen Sodium arm vs. Naproxen Sodium arm. Percent change was calculated by determining percent change in each subject, from Treatment Period Month 3 and Baseline, then comparing the average change between each arm. The following formula was used for each treatment period calculation. e.g.,Percent change=[ (mean migraine severity during Treatment Period Month 3 (Days 91-120)- mean migraine severity during Baseline (Days 1-30)/mean migraine severity during Baseline (Days 1-30)]*100%). (NCT01300546)
Timeframe: Baseline Period collected at Day 31, Treatment Period Months 1, 2, and 3 collected at Days 61, 91, and 121.

,
Interventionpercent change of migraine severity (Mean)
2 hours after treatment for Baseline to Month 12 hours after treatment for Baseline to Month 22 hours after treatment for Baseline to Month 3
Naproxen Sodium11.780.3332.62
Sumatriptan/Naproxen Sodium-17.84-36.71-55.60

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Migraine Duration From Time of Treatment to Pain Free

"% change from Baseline in mean migraine duration from time of treatment to pain free reported in Treatment Period Months 1, 2, and 3 in Sumatriptan/Naproxen Sodium arm vs. Naproxen Sodium arm.~Percent change=[(mean duration from treatment to painfree during Treatment Period Month 3 (Days 91-120)- mean duration from treatment to painfree during Baseline (Days 1-30)/mean duration from treatment to painfree during Baseline (Days 1-30)]*100%)." (NCT01300546)
Timeframe: Baseline Period collected at Day 31, Treatment Period Months 1, 2, and 3 collected at Days 61, 91, and 121.

,
Interventionpercent change of migraine duration (Mean)
Baseline to Treatment Period Month 1Baseline to Treatment Period Month 2Baseline to Treatment Period Month 3
Naproxen Sodium-14.91-25.5273.42
Sumatriptan/Naproxen Sodium150.1092.73114.10

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CGRP Measured at Menstrual Migraine Headache Onset, Migraine Headache Free, and 24 Hours Migraine Headache Free in Responders vs Non-Responders

"CGRP levels collected for 1 menstrual migraine headache at Menstrual Migraine Headache Onset, Migraine Headache Free, and 24 Hours Migraine Headache Free in Responders vs Non-Responders**.~*This endpoint was separated into 3 outcome measures as all biomarkers were not reported in the same units of measure.~**A responder is defined as those who at the time of two hours post treatment reported mild or no pain. Additionally, these subjects could not have taken a rescue medication or have a pain level increase within 24 hours post treatment.~A non-responder is one that fails to meet the responder criteria." (NCT01329562)
Timeframe: From Baseline to 24 hours post headache gone for 1 menstrual migraine.

,,
Interventionpmol/mg (Mean)
CGRP Migraine Onset (n=10,7,6)CGRP Migraine Headache Free (n=9,4,6)CGRP 24 Hours Migraine Headache Free (n=9,7,7)
Placebo22.2822.5529.37
Treximet Non-Responder33.7620.7835.87
Treximet Responder22.7449.4828.43

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CGRP Measured at Menstrual Headache Onset, Migraine Headache Free, and 24 Hours Migraine Headache Free.

"CGRP levels collected at Menstrual Migraine Headache Onset, Migraine Headache Free, and 24 Hours Migraine Headache Free in Treximet vs. Placebo arm for 1 menstrual migraine headache.~* This endpoint was separated into 3 outcome measures as all biomarkers were not reported in the same units of measure." (NCT01329562)
Timeframe: From baseline to 24 hours post headache gone for 1 menstrual migraine headache

,
Interventionpmol/mg (Mean)
CGRP Migraine Onset (n=10,7,6)CGRP Migraine Headache Free (n=9,4,6)CGRP 24 Hours Migraine Headache Free (n=9,7,7)
Placebo22.2822.5529.37
Treximet28.8232.2632.15

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CGRP Measured at Baseline, Menstrual Migraine Headache Onset, and 2 Hours Post-Treatment in Responders vs Non-Responders

"CGRP levels collected for 1 menstrual migraine headache at Baseline, Menstrual Migraine Headache Onset, and 2 Hours Post-Treatment in Responders vs Non-Responders**.~*This endpoint was separated into 3 outcome measures as all biomarkers were not reported in the same units of measure.~**A responder is defined as those who at the time of two hours post treatment reported mild or no pain. Additionally, these subjects could not have taken a rescue medication or have a pain level increase within 24 hours post treatment.~A non-responder is one that fails to meet the responder criteria." (NCT01329562)
Timeframe: From Baseline until 2 Hours post menstrual migraine treatment for 1 menstrual migraine headache.

,,
Interventionpmol/mg (Mean)
CGRP Baseline (n=10,7,7)CGRP Migraine Onset (n=10,7,6)CGRP 2 Hours Post Treatment (n=9,7,7)
Placebo18.5522.2814.92
Treximet Non-Responder17.8033.7621.67
Treximet Responder12.2722.7421.08

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CGRP Measured at Baseline, Menstrual Migraine Headache Onset, and 2 Hours Post Treatment

"CGRP levels collected at Baseline, Menstrual Migraine Headache Onset, and 2 Hours Post Treatment in Treximet vs. Placebo arms for 1 menstrual migraine headache~* This endpoint was separated into 3 outcome measures as all biomarkers were not reported in the same units of measure." (NCT01329562)
Timeframe: From Baseline until 2 hours post treatment for 1 menstrual migraine headache

,
Interventionpmol/mg (Mean)
CGRP Baseline (n=10, 14)CGRP Migraine Onset (n=10, 13)CGRP 2 Hours Post Treatment (n=9, 14)
Placebo18.5522.2814.92
Treximet15.0327.8221.38

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Biomarkers Measured at Menstrual Migraine Headache Onset, Migraine Headache Free, and 24 Hours Migraine Headache Free.

"VIP, PGE2, Cortisol, PGI2, Estradiol, and β-endorphin** levels collected at Menstrual Migraine Headache Onset, Migraine Headache Free and 24 Hours Migraine Headache Free in Treximet vs. Placebo arm for 1 menstrual migraine headache.~* This endpoint was separated into 3 outcome measures as all biomarkers were not reported in the same units of measure. CGRP and α-amylase both have their own outcome measure reported individually.~**β-endorphin levels were not assayed due to limitations on saliva sample volumes." (NCT01329562)
Timeframe: From baseline to 24 hours post headache gone for 1 menstrual migraine headache.

,
Interventionpg/mL (Mean)
VIP Migraine Onset (n=10,7,6)VIP Migraine Headache Free (n=9,4,7)VIP 24 Hours Migraine Headache Free (n=10,7,6)PGE2 Migraine Onset (n=10,7,6)PGE2 Migraine Headache Free (n=10,4,6,)PGE2 24 Hours Migraine Headache Free (n=10,7,7)Cortisol Migraine Onset (n=8,7,6)Cortisol Migraine Headache Free (n=10,3,6)Cortisol 24 Hours Migraine Headache Free(n=10,6,6)PGI2 Migraine Onset (n=10,7,6)PGI2 Migraine Headache Free (n=10,4,6)PGI2 24 Hours Migraine Headache Free (n=10,7,7)Estradiol Migraine Onset (n=9,7,6)Estradiol Migraine Headache Free (n=9,4,5,)Estradiol 24 Hours Migraine Headache Free(n=6,7,5)
Placebo1052.8964.41059.97.568.3510.461084.51490.921031.16108.23115.6397.6937.0548.8321.34
Treximet1111.31949.71353.0413.029.2713.041209.341498.921271.4158.29167.48224.5843.9339.9256.33

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Biomarkers Measured at Menstrual Migraine Headache Onset, Migraine Headache Free, and 24 Hours Migraine Headache Free in Responders vs Non-Responders

"VIP, PGE2, Cortisol, PGI2, Estradiol, and β-endorphin** levels collected for 1 menstrual migraine headache at Menstrual Migraine Headache Onset, Migraine Headache Free, and 24 Hours Migraine Headache Free in Responders vs Non-Responders***.~*This endpoint was separated into 3 outcome measures as all biomarkers were not reported in the same units of measure. CGRP and α-amylase both have their own outcome measure reported individually.~**β-endorphin levels were not assayed due to limitations on saliva sample volumes.~***A responder is defined as those who at the time of two hours post treatment reported mild or no pain. Additionally, these subjects could not have taken a rescue medication or have a pain level increase within 24 hours post treatment. A non-responder is one that fails to meet the responder criteria." (NCT01329562)
Timeframe: From Baseline for the duration of 1 menstrual migraine headache, an estimated 7 days

,,
Interventionpg/mL (Mean)
VIP Migraine Onset (n=10,7,6)VIP Migraine Headache Free (n=9,4,6)VIP 24 Hours Migraine Headache Free (n=10,7,5)PGE2 Migraine Onset (n=10,7,6)PGE2 Migraine Headache Free (n=10,4,6)PGE2 24 Hours Migraine Headache Free (n=10,7,7)Cortisol Migraine Onset (n=8,7,6)Cortisol Migraine Headache Free (n=10,3,5)Cortisol 24 Hours Migraine Headache Free(n=10,6,6)PGI2 Migraine Onset (n=10,7,6)PGI2 Migraine Headache Free (n=10,4,6)PGI2 24 Hours Migraine Headache Free (n=10,7,7)Estradiol Migraine Onset (n=9,7,6)Estradiol Migraine Headache Free (n=9,5,4)Estradiol 24 Hours Migraine Headache Free(n=6,7,6)
Placebo105.28964.41059.97.568.3510.461084.51490.921031.16108.23115.6397.6937.7548.8321.34
Treximet Non-Responder948.97643.01174.211.7210.2112.651508.972042.871621.38186.17176.37295.0742.8126.5881.38
Treximet Responder1251.141409.751480.7914.137.8713.43952.52592.35863.09134.40154.16154.1044.8956.5934.86

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Biomarkers Measured at Baseline, Menstrual Migraine Headache Onset, and 2 Hours Post Treatment

"Vasoactive Intestinal Peptide (VIP), Prostaglandin E2 (PGE2), Cortisol, Prostaglandin I2 (PGI2), Estradiol, and β-endorphin** levels collected at Baseline, Menstrual Migraine Headache Onset, and 2 Hours Post Treatment in Treximet vs. Placebo arms for 1 menstrual migraine headache * This endpoint was separated into 3 outcome measures as all biomarkers were not reported in the same units of measure. Calcitonin Gene-Related Peptide (CGRP) and α-amylase both have their own outcome measure reported individually.~**β-endorphin levels were not assayed due to limitations on saliva sample volumes." (NCT01329562)
Timeframe: From Baseline until 2 hours post treatment of 1 menstrual migraine headache

,
Interventionpg/mL (Mean)
VIP Baseline (n=10, 14)VIP Migraine Onset (n=10, 13)VIP 2 Hours Post Treatment (n=9, 13)PGE2 Baseline (n=10, 14)PGE2 Migraine Onset (n=10, 13)PGE2 2 Hours Post Treatment (n=9, 14)Cortisol Baseline (n=10, 13)Cortisol Migraine Onset (n=8, 13)Cortisol 2 Hours Post Treatment (n=8, 10)PGI2 Baseline (n=10, 14)PGI2 Migraine Onset (n=10, 13)PGI2 2 Hours Post Treatment (n=9, 14)Estradiol Baseline (n=10, 13)Estradiol Migraine Onset (n=9, 13)Estradiol 2 Hours Post Treatment (n=9,14)
Placebo763.61052.81130.449.257.568.291064.141084.852011.45109.51108.2397.5863.3741.6854.07
Treximet1149.51111.31933.7712.6513.027.991040.491209.34418.48160.27158.29201.6062.6143.9341.66

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Time to Pain-Free in Responders vs Non-Responders

"Duration of time from treatment at menstrual migraine headache onset until pain-free in Treximet vs. Placebo arms in responders* vs. non-responders for 1 menstrual migraine.~0-3 Pain Scale, with 0=No Pain, 1=Mild, 2=Moderate, and 3=Severe.~*A responder is defined as those who at the time of two hours post treatment reported mild or no pain. Additionally, these subjects could not have taken a rescue medication or have a pain level increase within 24 hours post treatment.~A non-responder is one that fails to meet the responder criteria." (NCT01329562)
Timeframe: From the onset of 1 menstrual migraine headache until pain-free.

Interventionhours (Mean)
Placebo7.64
Treximet Responder3.13
Treximet Non-Responder4.68

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Migraine Recurrence

"Number of subjects either pain free or mild at 2 hours then pain level increases within 24 hours following treatment with Treximet versus (vs.) Placebo for 1 menstrual migraine.~0-3 pain scale with 0=No Pain, 1=Mild, 2=Moderate,and 3=Severe." (NCT01329562)
Timeframe: From onset of a single menstrual migraine episode to 24 hours post menstrual migraine treatment.

Interventionparticipants (Number)
Placebo0
Treximet2

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Biomarkers Measured at Baseline, Menstrual Migraine Onset, and 2 Hours Post Treatment in Responders vs Non-Responders

"VIP, PGE2, Cortisol, PGI2, Estradiol, and β-endorphin** levels collected for 1 menstrual migraine headache at Baseline, Menstrual Migraine Headache Onset, and 2 Hours Post Treatment in Treximet vs. Placebo arms in responders vs. non-responders***.~*This endpoint was separated into 3 outcome measures as all biomarkers were not reported in the same unit of measure. CGRP and α-amylase both have their own outcome measure reported individually.~**β-endorphin levels were not assayed due to limitations on saliva sample volumes.~***A responder is defined as those who at the time of two hours post treatment reported mild or no pain. Additionally, these subjects could not have taken a rescue medication or have a pain level increase within 24 hours post treatment.~A non-responder is one that fails to meet the responder criteria." (NCT01329562)
Timeframe: From Baseline until 2 Hours post menstrual migraine treatment for 1 menstrual migraine headache.

,,
Interventionpg/mL (Mean)
VIP Baseline (n=10,7,7)VIP Migraine Onset (n=10,7,6)VIP 2 Hours Post Treatment (n=9,7,6,)PGE2 Baseline (n=10,7,7)PGE2 Migraine Onset (n=10,7,6)PGE2 2 Hours Post Treatment (n=9,7,7)Cortisol Baseline (n=10,6,7)Cortisol Migraine Onset (n=8,7,6)Cortisol 2 Hours Post Treatment (n=8,6,4)PGI2 Baseline (n=10,7,7)PGI2 Migraine Onset (n=10,7,6)PGI2 2 Hours Post Treatment (n=9,7,7)Estradiol Baseline (n=9,7,6)Estradiol Migraine Onset (n=8,7,6)Estradiol 2 Hours Post Treatment (n=8,7,7)
Placebo763.61052.81130.449.257.568.291064.141084.52011.45109.51108.2397.5863.3737.0554.07
Treximet Non-Responder885.0948.17414.011.0111.729.151254.531508.97322.72177.54186.17247.6366.6842.8146.68
Treximet Responder1414.01251.141320.1414.2914.136.83790.77952.52482.32142.99134.40155.5649.6044.8936.64

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Migraine Recurrence Responders vs Non-Responders

"Number of subjects either pain-free or mild at 2 hours then pain level increases within 24 hours following treatment in Treximet vs. Placebo arm for 1 menstrual migraine headache with Treximet vs. Placebo in responders* vs. non-responders.~0-3 Pain Scale with 0=No Pain, 1=Mild, 2=Moderate, and 3=Severe~*A responder is defined as those who at the time of two hours post treatment reported mild or no pain. Additionally, these subjects could not have taken a rescue medication or have a pain level increase within 24 hours post treatment.~A non-responder is one that fails to meet the responder criteria." (NCT01329562)
Timeframe: From the onset of 1 menstrual migraine until 24 hours post treatment.

Interventionparticipants (Number)
Placebo1
Treximet Responder2
Treximet Non-Responder0

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α-Amylase Measured at Menstrual Headache Onset, Migraine Headache Free, and 24 Hours Migraine Headache Free.

"α-Amylase levels collected at Menstrual Migraine Headache Onset, Migraine Headache Free, and 24 Hours Migraine Headache Free in Treximet vs. Placebo arm for 1 menstrual migraine headache~* This endpoint was separated into 3 outcome measures as all biomarkers were not reported in the same units of measure." (NCT01329562)
Timeframe: From baseline to 24 hours post headache gone for 1 menstrual migraine headache

,
InterventionU/L (Mean)
α-Amylase Migraine Onset (n=10,7,6)α-Amylase Migraine Headache Free (n=10,4,6)α-Amylase 24 Hours Migraine Headache Free(n=10,7,7
Placebo100956.70102908.61100354.00
Treximet98853.32101307.25102017.80

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α-Amylase Measured at Baseline, Menstrual Migraine Headache Onset, and 2 Hours Post Treatment in Responders vs Non-Responders

"α-Amylase levels collected at Baseline, Menstrual Migraine Headache Onset, and 2 Hours Post Treatment in Responders vs Non-Responders*.~*A responder is defined as those who at the time of two hours post treatment reported mild or no pain. Additionally, these subjects could not have taken a rescue medication or have a pain level increase within 24 hours post treatment.~A non-responder is one that fails to meet the responder criteria." (NCT01329562)
Timeframe: From Baseline until 2 hours post treatment of 1 menstrual migraine headache.

,,
InterventionU/L (Mean)
α-Amylase Baseline (n=10,7,7)α-Amylase Migraine Onset (n=10,7,6)α-Amylase 2 Hours Post Treatment (n=9,7,7)
Placebo109280.50100956.7102449.88
Treximet Non-Responder101250.5493456.77103662.4
Treximet Responder98002.68103478.94103527.5

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α-Amylase Measured at Baseline, Menstrual Migraine Headache Onset, and 2 Hours Post Treatment

"α-Amylase levels collected at Baseline, Menstrual Migraine Headache Onset, and 2 Hours Post Treatment in Treximet vs. Placebo arm for 1 menstrual migraine headache~* This endpoint was separated into 3 outcome measures as all biomarkers were not reported in the same units of measure." (NCT01329562)
Timeframe: From Baseline until 2 hours post treatment for 1 menstrual migraine headache

,
InterventionU/L (Mean)
α-Amylase Baseline (n=10, 14)α-Amylase Migraine Onset (n=10, 13)α-Amylase 2 Hours Post Treatment (n=9, 14)
Placebo109280.50100956.70102449.80
Treximet99626.6198853.32103594.90

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Correlation of Mean Estrogen Levels in Saliva and Urine Estradiol at Mid-Luteal and at Menstrual Migraine Headache Free in Responders vs Non-Responders

"Correlation of mean estrogen levels in saliva and urine estradiol at mid-luteal, menstrual migraine headache onset* and at migraine headache free following treatment in responders vs. non-responders**.~*Urine estradiol levels were not collected at migraine onset, therefore; correlations could not be completed for that time point.~***A responder is defined as those who at the time of two hours post treatment reported mild or no pain. Additionally, these subjects could not have taken a rescue medication or have a pain level increase within 24 hours post treatment.~A non-responder is one that fails to meet the responder criteria." (NCT01329562)
Timeframe: From mid luteal phase and for the duration of 1 menstrual migraine until headache free.

,,
Interventionpg/mL (Mean)
Urine Pre-Cycle Day 1 (n=3,2,4)Urine Pre-Cycle Day 2 (n=6,3,5)Urine Pre-Cycle Day 3 (n=8,2,5)Urine Pre-Cycle Day 4 (n=9,5,5)Urine Migraine Headache Free (n=10,7,7)Saliva Pre-Cycle Day 1 (n=1,0,4)Saliva Pre-Cycle Day 2 (n=2,2,4)Saliva Pre-Cycle Day 3 (n=8,4,7)Saliva Pre-Cycle Day 4 (n=8,5,4)Saliva Migraine Headache Free (n=8,3,4)
Placebo2442.444333.923582.923232.102398.5541.7563.4546.4755.8654.93
Treximet Non-Responder3687.073661.525629.714266.023373.4043.3347.3667.7654.2233.22
Treximet Responder1898.63875.343739.442016.992542.09NA30.8981.0531.7175.45

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α-Amylase Measured at Menstrual Migraine Headache Onset, Migraine Headache Free, and 24 Hours Migraine Headache Free in Responders vs Non-Responders

"α-Amylase levels collected for 1 menstrual migraine at Menstrual Migraine Headache Onset, Migraine Headache Free, and 24 Hours Migraine Headache Free in Responders vs Non-Responders**.~*This endpoint was separated into 3 outcome measures as all biomarkers were not reported in the same units of measure.~**A responder is defined as those who at the time of two hours post treatment reported mild or no pain. Additionally, these subjects could not have taken a rescue medication or have a pain level increase within 24 hours post treatment.~A non-responder is one that fails to meet the responder criteria." (NCT01329562)
Timeframe: From Baseline from 24 hours post migraine gone for 1 menstrual migraine.

,,
InterventionU/L (Mean)
α-amylase Migraine Onset (n=10,7,6)α-amylase Migraine Headache Free (n=9,7,7)α-amylase 24 Hours Migraine Headache Free(n=10,4,6
Placebo100956.7102908.61100354.3
Treximet Non-Responder93456.77103031.44101559.9
Treximet Responder103478.9498720.95102475.8

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Time to Pain Free

"Duration of 1 menstrual migraine from time of treatment at menstrual migraine headache onset until pain free in Treximet vs. Placebo arms.~0-3 pain scale with 0=No Pain, 1=Mild, 2=Moderate, and 3=Severe." (NCT01329562)
Timeframe: From onset of 1 menstrual migraine headache until pain free.

Interventionhours (Mean)
Placebo7.64
Treximet3.90

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Correlation of Mean Estrogen Levels in Saliva and Urine Estradiol at Mid Luteal and at Menstrual Migraine Headache Free.

"Correlation of mean estrogen levels in saliva and urine estradiol at mid luteal, menstrual migraine headache onset*, and at migraine headache free following treatment with Treximet vs. Placebo for 1 menstrual migraine headache~*Urine estradiol levels were not collected at migraine onset, therefore; correlations could not be completed for that time point." (NCT01329562)
Timeframe: From mid luteal phase and for the duration of 1 menstrual migraine headache and until headache free

,
Interventionpg/mL (Mean)
Urine Pre-Cycle Day 1 (n=3, 6)Urine Pre-Cycle Day 2 (n=6, 8)Urine Pre-Cycle Day 3 (n=8, 6)Urine Pre-Cycle Day 4 (n=9, 10)Urine Migraine Headache Free (n=11, 13Saliva Pre-Cycle Day 1 (n=1, 4)Saliva Pre-Cycle Day 2 (n=2, 6)Saliva Pre-Cycle Day 3 (n=8, 10)Saliva Pre-Cycle Day 4 (n=6, 9)Saliva Migraine Headache Free (n=8, 6)
Placebo2442.444333.923582.923232.102398.5541.7563.4546.4755.8654.93
Treximet3090.922616.645089.633141.512989.7243.3341.8773.0841.7251.32

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Mean Number of Triptan Tablets Per Participant in 6-month Follow-up Period: Treatment-switch Analysis

"The mean number of tablets per participant was computed using prescription fills dispensed in the 6-month follow-up period. Other represents APAP/isometheptene/dichlorphenazone and APAP/isometheptene/caffeine, for example. The number of tablets dispensed was obtained from the quantity dispensed field in the claims data. Triptan tablets were classified as index and non-index medication (if a different oral triptan was filled from that of the index medication); only oral triptans were considered (i.e., excluded injectable triptans)." (NCT01332500)
Timeframe: 6-months from the index date (from January 1, 2009 to May 31, 2009; index date was defined as the first switch date to oral triptan/sumatriptan-naproxen sodium prescription)

,
Interventiontablets per participant (Mean)
TriptansNon-steroidal anti-inflammatory drugsOpioidsErgotsOther
Switch - Oral Triptan24.422.987.40.11.3
Switch - Sumatriptan/Naproxen Sodium24.420.988.40.01.4

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Mean Number of Triptan Tablets Per Participant in 6-month Follow-up Period: Treatment-naïve Analysis

"The mean number of tablets per participant was computed using prescription fills dispensed in the 6-month follow-up period. Other represents acetaminophen (APAP)/isometheptene/dichlorphenazone and APAP/isometheptene/caffeine, for example. The number of tablets dispensed was obtained from the quantity dispensed field in the claims data. Triptan tablets were classified as index and non-index medication (if a different oral triptan was filled from that of the index medication); only oral triptans were considered (i.e., excluded injectable triptans)." (NCT01332500)
Timeframe: 6-months from the index date (from January 1, 2009 to May 31, 2009; the index date was defined as the first date of oral triptan/sumatriptan-naproxen sodium prescription)

,
Interventiontablets per participant (Mean)
TriptansNon-steroidal anti-inflammatory drugsOpioidsErgotsOther
Naïve - Oral Triptan18.421.580.10.11.4
Naïve - Sumatriptan/Naproxen Sodium17.719.275.80.11.5

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Number of Participants Achieving Sustained Pain Freedom From 2 to 48 Hours Post Dose

"Participants were considered to have sustained pain freedom if all of their reported pain readings in the interval are none on the four point numeric rating scale (no pain=0, mild pain=1, moderate pain=2, severe pain=3). The intervals are inclusive of the endpoints. Sustained pain freedom was analyzed with a CMH test for general association that compares the ED90 to placebo, and controls for baseline pain severity." (NCT01430442)
Timeframe: 2 hours to 48 hours post dose

InterventionParticipants (Count of Participants)
Treatment A: Rimegepant, 10 mg8
Treatment B: Rimegepant, 25 mg9
Treatment C: Rimegepant, 75 mg24
Treatment D: Rimegepant, 150 mg24
Treatment E: Rimegepant, 300 mg29
Treatment F: Rimegepant, 600 mg17
Treatment P: Rimegepant Placebo-Matching Capsules15
Treatment G: Sumatriptan 100 mg26

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Number of Participants With Total Migraine Freedom at 2 Hours Post Dose

"Total migraine freedom is defined as complete absence of migraine symptoms. A participant was positive for total migraine freedom at a particular time point if he/she reports the absence of: pain, nausea, photophobia, and phonophobia. This corresponds to reporting none on each of the four-point numeric rating scale (none =0, mild =1, moderate =2, severe =3) from baseline associated with these symptoms. Participants with baseline moderate pain or severe pain were included in the analysis." (NCT01430442)
Timeframe: Baseline, 2 hours post dose

InterventionParticipants (Count of Participants)
Treatment A: Rimegepant, 10 mg13
Treatment B: Rimegepant, 25 mg11
Treatment C: Rimegepant, 75 mg24
Treatment D: Rimegepant, 150 mg22
Treatment E: Rimegepant, 300 mg26
Treatment F: Rimegepant, 600 mg16
Treatment P: Rimegepant Placebo-Matching Capsules24
Treatment G: Sumatriptan 100 mg32

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Number of Pain Free Participants (Pain Freedom) at 2 Hours Post-dose

"Pain freedom was defined as participants reporting a value of none on the four-point numeric rating scale (none=0, mild =1, moderate =2, severe =3) from baseline. Participants with baseline moderate pain or severe pain were included in the analysis." (NCT01430442)
Timeframe: Baseline, 2 hours post-dose

InterventionParticipants (Count of Participants)
Treatment A: Rimegepant, 10 mg14
Treatment B: Rimegepant, 25 mg12
Treatment C: Rimegepant, 75 mg27
Treatment D: Rimegepant, 150 mg28
Treatment E: Rimegepant, 300 mg33
Treatment F: Rimegepant, 600 mg20
Treatment P: Rimegepant Placebo-Matching Capsules31
Treatment G: Sumatriptan 100 mg35

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Number of Participants Achieving Sustained Pain Freedom From 2 to 24 Hours Post Dose

"Participants were considered to have sustained pain freedom if all of their reported pain readings in the interval are none on the four point numeric rating scale (no pain=0, mild pain=1, moderate pain=2, severe pain=3). The intervals are inclusive of the endpoints. Sustained pain freedom was analyzed with a Cochran Mantel Haenszel (CMH) test for general association that compares the ED90 to placebo, and controls for baseline pain severity." (NCT01430442)
Timeframe: 2 hours to 24 hours post dose

InterventionParticipants (Count of Participants)
Treatment A: Rimegepant, 10 mg9
Treatment B: Rimegepant, 25 mg10
Treatment C: Rimegepant, 75 mg24
Treatment D: Rimegepant, 150 mg24
Treatment E: Rimegepant, 300 mg29
Treatment F: Rimegepant, 600 mg17
Treatment P: Rimegepant Placebo-Matching Capsules15
Treatment G: Sumatriptan 100 mg26

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Number of Participants With Adverse Events (AEs), Serious Adverse Events (SAEs), and Discontinuation Due to Adverse Events

An AE was defined as any new untoward medical occurrence or worsening of a pre-existing medical condition, unfavorable and unintended sign, symptom, or disease temporally associated with the use of study drug, whether or not related to study drug. A SAE was defined as an event which was fatal or life threatening, required or prolonged hospitalization, was significantly or permanently disabling or incapacitating, constituted a congenital anomaly or a birth defect, or suspected transmission of an infectious agent, or encompassed any other clinically significant event that could jeopardize the subject or require medical or surgical intervention to prevent one of the aforementioned outcomes. (NCT01430442)
Timeframe: AEs: from first dose to end of treatment visit (up to 7 weeks); SAE: from signing of informed consent to 30 days after the last dose (up to 11 weeks).

,,,,,,,
InterventionParticipants (Count of Participants)
AEsSAEsParticipants discontinued due to AEs
Treatment A: Rimegepant, 10 mg1500
Treatment B: Rimegepant, 25 mg1000
Treatment C: Rimegepant, 75 mg1800
Treatment D: Rimegepant, 150 mg1230
Treatment E: Rimegepant, 300 mg1800
Treatment F: Rimegepant, 600 mg1400
Treatment G: Sumatriptan 100 mg1700
Treatment P: Rimegepant Placebo-Matching Capsules2900

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Headache Relief

The primary objective for this study is to compare headache relief (defined as a reduction from moderate [Grade 2] or severe [Grade 3] pain to none [Grade 0] or mild [Grade 1] pain) at 120 minutes following a dose of 20 mg of OPTINOSE SUMATRIPTAN with placebo in the acute treatment of a single migraine attack. (NCT01462812)
Timeframe: 120 Minutes

Interventionparticipants (Number)
Matching Placebo47
Sumatriptan73

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Change From Baseline in Albumin and Total Protein at Visit 3 (up to Week 12) and Visit 4 (up to Week 24)

Change from Baseline in albumin and total protein was assessed at Visit 3 (the start of Treatment Period 2) and Visit 4 (the end-of-study visit). Change from Baseline was calculated as the post-Baseline value minus the Baseline value. The Baseline value is the last non-missing value prior to or on the start date of Treatment Period 1. (NCT01667679)
Timeframe: Baseline and Visits 3 (up to 12 weeks) and 4 (up to 24 weeks)

,
Interventiongrams per Liter (grams/L) (Mean)
albumin, Visit 3, n=108, 94albumin, Visit 4, n=123, 110total protein, Visit 3, n=108, 94total protein, Visit 4, n=122, 110
100 mg Sumatriptan+PBO (TP1)/20 mg Sumatriptan+PBO (TP2)-0.9-0.5-1.2-1.0
20 mg Sumatriptan+PBO (TP1)/100 mg Sumatriptan+PBO (TP2)-0.8-0.9-1.0-1.2

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Change From Baseline in Alkaline Phosphatase (ALP) and Alanine Aminotransferase (ALT) at Visit 3 (up to Week 12) and Visit 4 (up to Week 24)

Change from Baseline in ALP and ALT was assessed at Visit 3 (the start of Treatment Period 2) and Visit 4 (the end-of-study visit). Change from Baseline was calculated as the post-Baseline value minus the Baseline value. The Baseline value is the last non-missing value prior to or on the start date of Treatment Period 1. (NCT01667679)
Timeframe: Baseline and Visits 3 (up to 12 weeks) and 4 (up to 24 weeks)

,
InterventionInternational Units per Liter (IU/L) (Mean)
ALP, Visit 3, n=108, 94ALP, Visit 4, n=123, 110ALT, Visit 3, n=108, 94ALT, Visit 4, n=123, 110
100 mg Sumatriptan+PBO (TP1)/20 mg Sumatriptan+PBO (TP2)0.0-1.00.0-0.9
20 mg Sumatriptan+PBO (TP1)/100 mg Sumatriptan+PBO (TP2)-0.5-1.70.40.4

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Change From Baseline in Aspartate Aminotransferase (AST) and Gamma Glutamyl Transferase (GGT) at Visit 3 (up to Week 12) and Visit 4 (up to Week 24)

Change from Baseline in AST and GGT was assessed at Visit 3 (the start of Treatment Period 2) and Visit 4 (the end-of-study visit). Change from Baseline was calculated as the post-Baseline value minus the Baseline value. The Baseline value is the last non-missing value prior to or on the start date of Treatment Period 1. (NCT01667679)
Timeframe: Baseline and Visits 3 (up to 12 weeks) and 4 (up to 24 weeks)

,
InterventionInternational Units per Liter (IU/L) (Mean)
AST, Visit 3, n=108, 92AST, Visit 4, n=123, 110GGT, Visit 3, n=108, 94GGT, Visit 4, n=123, 110
100 mg Sumatriptan+PBO (TP1)/20 mg Sumatriptan+PBO (TP2)0.5-1.20.0-0.7
20 mg Sumatriptan+PBO (TP1)/100 mg Sumatriptan+PBO (TP2)-0.20.60.80.4

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Change From Baseline in Creatinine at Visit 3 (up to Week 12) and Visit 4 (up to Week 24)

Change from Baseline in creatinine was assessed at Visit 3 (the start of Treatment Period 2) and Visit 4 (the end-of-study visit). Change from Baseline was calculated as the post-Baseline value minus the Baseline value. The Baseline value is the last non-missing value prior to or on the start date of Treatment Period 1. (NCT01667679)
Timeframe: Baseline and Visits 3 (up to 12 weeks) and 4 (up to 24 weeks)

,
Interventionmicromoles per Liter (µmol/L) (Mean)
Visit 3, n=108, 94Visit 4, n=123, 110
100 mg Sumatriptan+PBO (TP1)/20 mg Sumatriptan+PBO (TP2)-0.7-0.6
20 mg Sumatriptan+PBO (TP1)/100 mg Sumatriptan+PBO (TP2)-1.9-1.3

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Change From Baseline in Hematocrit at Visit 3 (up to 12 Weeks) and Visit 4 (up to 24 Weeks)

Change from Baseline in hematocrit (proportion of total blood volume that is composed of red blood cells) was assessed at Visit 3 (the start of Treatment Period 2) and Visit 4 (the end-of-study visit). Change from Baseline was calculated as the post-Baseline value minus the Baseline value.The Baseline value is the last non-missing value prior to or on the start date of Treatment Period 1. (NCT01667679)
Timeframe: Baseline and Visits 3 (up to 12 weeks) and 4 (up to 24 weeks)

,
Interventionproportion (Mean)
Visit 3, n=108, 94Visit 4, n=124, 110
100 mg Sumatriptan+PBO (TP1)/20 mg Sumatriptan+PBO (TP2)-0.005-0.002
20 mg Sumatriptan+PBO (TP1)/100 mg Sumatriptan+PBO (TP2)-0.002-0.005

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Change From Baseline in Hemoglobin at Visit 3 (up to 12 Weeks) and Visit 4 (up to 24 Weeks)

Change from Baseline in hemoglobin was assessed at Visit 3 (the start of Treatment Period 2) and Visit 4 (the end-of-study visit). Change from Baseline was calculated as the post-Baseline value minus the Baseline value. The Baseline value is the last non-missing value prior to or on the start date of Treatment Period 1. (NCT01667679)
Timeframe: Baseline and Visits 3 (up to 12 weeks) and 4 (up to 24 weeks)

,
Interventiongrams per Liter (g/L) (Mean)
Visit 3Visit 4
100 mg Sumatriptan+PBO (TP1)/20 mg Sumatriptan+PBO (TP2)-1.3-0.8
20 mg Sumatriptan+PBO (TP1)/100 mg Sumatriptan+PBO (TP2)-1.3-2.7

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Change From Baseline in Pulse at Visit 3 (up to Week 12) and Visit 4 (up to Week 24)

Change from Baseline in pulse was assessed at Visit 3 (the start of Treatment Period 2) and Visit 4 (the end-of-study visit). Change from Baseline was calculated as the post-Baseline value minus the Baseline value. The Baseline value is the last non-missing value prior to or on the start date of Treatment Period 1. (NCT01667679)
Timeframe: Baseline and Visits 3 (up to 12 weeks) and 4 (up to 24 weeks)

,
Interventionbeats per minute (Mean)
Visit 3, n=110, 95Visit 4, n=124, 111
100 mg Sumatriptan+PBO (TP1)/20 mg Sumatriptan+PBO (TP2)0.1-0.2
20 mg Sumatriptan+PBO (TP1)/100 mg Sumatriptan+PBO (TP2)0.1-2.2

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Change From Baseline in Red Blood Cell Count at Visit 3 (up to Week 12) and Visit 4 (up to Week 24)

Change from Baseline in red blood cell count was assessed at Visit 3 (the start of Treatment Period 2) and Visit 4 (the end-of-study visit). Change from Baseline was calculated as the post-Baseline value minus the Baseline value. The Baseline value is the last non-missing value prior to or on the start date of Treatment Period 1. (NCT01667679)
Timeframe: Baseline and Visits 3 (up to 12 weeks) and 4 (up to 24 weeks)

,
Intervention10^12 cells per Liter (Mean)
Visit 3, n=109, 95Visit 4, n=124, 110
100 mg Sumatriptan+PBO (TP1)/20 mg Sumatriptan+PBO (TP2)-0.04-0.02
20 mg Sumatriptan+PBO (TP1)/100 mg Sumatriptan+PBO (TP2)-0.02-0.05

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Change From Baseline in Sodium, Potassium, Chloride, Calcium, and Glucose at Visit 3 (up to Week 12) and Visit 4 (up to Week 24)

Change from Baseline in sodium, potassium, chloride, calcium, and glucose was assessed at Visit 3 (the start of Treatment Period 2) and Visit 4 (the end-of-study visit). Change from Baseline was calculated as the post-Baseline value minus the Baseline value. The Baseline value is the last non-missing value prior to or on the start date of Treatment Period 1. (NCT01667679)
Timeframe: Baseline and Visits 3 (up to 12 weeks) and 4 (up to 24 weeks)

,
Interventionmmoles/L (Mean)
sodium, Visit 3, n=108, 94sodium, Visit 4, n=122, 110potassium, Visit 3, n=108, 94potassium, Visit 4, n=122, 110chloride, Visit 3, n=108, 94chloride, Visit 4, n=122, 110calcium, Visit 3, n=108, 94calcium, Visit 4, n=123, 110glucose, Visit 3, n=108, 94glucose, Visit 4, n=123, 110
100 mg Sumatriptan+PBO (TP1)/20 mg Sumatriptan+PBO (TP2)-0.5-0.2-0.04-0.000.00.2-0.016-0.0060.050.24
20 mg Sumatriptan+PBO (TP1)/100 mg Sumatriptan+PBO (TP2)-0.3-0.3-0.08-0.10-0.10.2-0.019-0.0110.340.20

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Change From Baseline in Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP) at Visit 3 (up to Week 12) and Visit 4 (up to Week 24)

Change from Baseline in SBP and DBP was assessed at Visit 3 (the start of Treatment Period 2) and Visit 4 (the end-of-study visit). Change from Baseline was calculated as the post-Baseline value minus the Baseline value. The Baseline value is the last non-missing value prior to or on the start date of Treatment Period 1. (NCT01667679)
Timeframe: Baseline and Visits 3 (up to 12 weeks) and 4 (up to 24 weeks)

,
Interventionmillimeters of mercury (mmHg) (Mean)
SBP, Visit 3, n=110, 95SBP, Visit 4, n=124, 111DBP, Visit 3, n=110, 95DBP, Visit 4, n=124, 111
100 mg Sumatriptan+PBO (TP1)/20 mg Sumatriptan+PBO (TP2)1.52.01.0-0.2
20 mg Sumatriptan+PBO (TP1)/100 mg Sumatriptan+PBO (TP2)0.11.6-0.20.2

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Change From Baseline in Total Bilirubin at Visit 3 (up to Week 12) and Visit 4 (up to Week 24)

Change from Baseline in total bilirubin was assessed at Visit 3 (the start of Treatment Period 2) and Visit 4 (the end-of-study visit). Change from Baseline was calculated as the post-Baseline value minus the Baseline value. The Baseline value is the last non-missing value prior to or on the start date of Treatment Period 1. (NCT01667679)
Timeframe: Baseline and Visits 3 (up to 12 weeks) and 4 (up to 24 weeks)

,
InterventionUnits per Liter (U/L) (Mean)
Visit 3, n=108, 94Visit 4, n=123, 110
100 mg Sumatriptan+PBO (TP1)/20 mg Sumatriptan+PBO (TP2)-0.20.2
20 mg Sumatriptan+PBO (TP1)/100 mg Sumatriptan+PBO (TP2)0.2-0.6

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Change From Baseline in Urea at Visit 3 (up to Week 12) and Visit 4 (up to Week 24)

Change from Baseline in urea was assessed at Visit 3 (the start of Treatment Period 2) and Visit 4 (the end-of-study visit). Change from Baseline was calculated as the post-Baseline value minus the Baseline value. The Baseline value is the last non-missing value prior to or on the start date of Treatment Period 1. (NCT01667679)
Timeframe: Baseline and Visits 3 (up to 12 weeks) and 4 (up to 24 weeks)

,
Interventionmillimoles per Liter (mmol/L) (Mean)
Visit 3, n=108, 94Visit 4, n=123, 110
100 mg Sumatriptan+PBO (TP1)/20 mg Sumatriptan+PBO (TP2)0.0790.308
20 mg Sumatriptan+PBO (TP1)/100 mg Sumatriptan+PBO (TP2)0.0700.156

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Change From Baseline in Urinalysis Values by Dipstick Method at Visit 3 (up to Week 12) and Visit 4 (up to Week 24)

Change from Baseline in urinalysis values was assessed at Visit 3 (the start of Treatment Period 2) and Visit 4 (the end-of-study visit). Change from Baseline was calculated as the post-Baseline value minus the Baseline value. The Baseline value is the last non-missing value prior to or on the start date of Treatment Period 1. (NCT01667679)
Timeframe: Baseline and Visits 3 (up to 12 weeks) and 4 (up to 24 weeks)

,
InterventionpH (Mean)
Visit 3, n=108, 95Visit 4, n=124, 109
100 mg Sumatriptan+PBO (TP1)/20 mg Sumatriptan+PBO (TP2)-0.03-0.07
20 mg Sumatriptan+PBO (TP1)/100 mg Sumatriptan+PBO (TP2)-0.040.01

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Change From Baseline in White Blood Cell Count, Basinophils, Monocytes, Neutrophils, Lymphocytes, Eosinophils, and Platelets at Visit 3 (up to Week 12) and Visit 4 (up to Week 24)

Change from Baseline in white blood cell (WBC) count, basinophils, monocytes, neutrophils, lymphocytes, eosinophils, and platelets was assessed at Visit 3 (the start of Treatment Period 2) and Visit 4 (the end-of-study visit). Change from Baseline was calculated as the post-Baseline value minus the Baseline value. The Baseline value is the last non-missing value prior to or on the start date of Treatment Period 1. (NCT01667679)
Timeframe: Baseline and Visits 3 (up to 12 weeks) and 4 (up to 24 weeks)

,
Intervention10^9 cells per Liter (Mean)
WBC Count, Visit 3, n=109, 95WBC Count, Visit 4, n=124, 110Basophils, Visit 3, n=108, 95Basophils, Visit 4, n=124, 110Monocytes, Visit 3, n=108, 95Monocytes, Visit 4, n=124, 110Neutrophils, Visit 3, n=108, 95Neutrophils, Visit 4, n=124, 110Lymphocytes, Visit 3, n=108, 95Lymphocytes, Visit 4, n=124, 110Eosinophils, Visit 3, n=108, 95Eosinophils, Visit 4, n=124, 110Platelets, Visit 3, n=109, 93Platelets, Visit 4, n=123, 110
100 mg Sumatriptan+PBO (TP1)/20 mg Sumatriptan+PBO (TP2)-0.19-0.090.000-0.001-0.022-0.026-0.134-0.057-0.038-0.0200.0060.013-8.2-7.5
20 mg Sumatriptan+PBO (TP1)/100 mg Sumatriptan+PBO (TP2)-0.10-0.050.0000.000-0.030-0.014-0.052-0.059-0.0490.012-0.0010.012-1.9-4.0

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Mean Change From Baseline in Clinical Disability Score at 10, 15, 30, 45, 60, 90, and 120 Minutes Post-dose

Participants were required to record their clinical disability score in their e-diaries immediately before intake of study medication (Baseline) and at 10, 15, 30, 45, 60, 90, and 120 minutes post-dose. Participants graded their disability on the following scale: 0, no disability, able to function normally; 1, performance of daily activities mildly impaired, can still do everything but with difficulty; 2, performance of daily activities moderately impaired, unable to do some things; 3, performance of daily activities severely impaired, cannot do all or most things, bed rest may be necessary. Mean change from Baseline was calculated as the post-Baseline value minus the Baseline value. (NCT01667679)
Timeframe: Baseline and 10, 15, 30, 45, 60, 90, and 120 minutes post-dose (up to 24 weeks)

,
Interventionscores on a scale (Least Squares Mean)
10 minutes post-dose15 minutes post-dose30 minutes post-dose45 minutes post-dose60 minutes post-dose90 minutes post-dose120 minutes post-dose
100 mg Sumatriptan Tablet-0.03-0.09-0.26-0.43-0.56-0.72-0.85
20 mg Sumatriptan Nasal Powder-0.08-0.18-0.42-0.60-0.73-0.83-0.92

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Mean Change in Headache Severity From Baseline to 10, 15, 30, 45, 60, 90, and 120 Minutes Post-dose

Participants were required to record their headache severity score in their e-diaries immediately before intake of study medication (Baseline) and at 10, 15, 30, 45, 60, 90, and 120 minutes post-dose. Participants graded their headaches on the following severity scale: 0, none; 1, mild; 2, moderate; 3, severe. Mean change from Baseline was calculated as the post-Baseline value minus the Baseline value. (NCT01667679)
Timeframe: Baseline and 10, 15, 30, 45, 60, 90, and 120 minutes post-dose (up to 24 weeks)

,
Interventionscores on a scale (Least Squares Mean)
10 minutes post-dose15 minutes post-dose30 minutes post-dose45 minutes post-dose60 minutes post-dose90 minutes post-dose120 minutes post-dose
100 mg Sumatriptan Tablet-0.09-0.18-0.38-0.60-0.79-0.98-1.15
20 mg Sumatriptan Nasal Powder-0.11-0.26-0.56-0.77-0.93-1.09-1.19

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Mean Sum of Migraine Pain Intensity Differences (SPID)-30 for Headaches With a Baseline Intensity of Mild and Moderate/Severe

"SPID-30 is defined as the sum of the pain intensity differences (measured as area under the curve) from dosing (Baseline) through 30 minutes post-dose for headaches with a Baseline intensity of mild and moderate/severe (rated on a 4-point scale: 0=none, 1=mild, 2=moderate, and 3=severe). The range of possible scores for all participants is -60 to +90. For participants with a mild headache at Baseline, the SPID range is -60 to +30. For participants with a moderate/severe headache at Baseline, the SPID range is -30 to +90. A higher number indicates a greater reduction in pain intensity. Negative values indicate worsening pain. A value of 0 indicates that there was no change in pain intensity from Baseline through 30 minutes. Results are from an ANCOVA model with treatment, period, and treatment sequence as fixed effects and participant as a random effect. The LOCF imputation method (missing values were replaced by carrying forward the preceding value) was used for this analysis." (NCT01667679)
Timeframe: Baseline and 30 minutes post-dose (up to 24 weeks)

,
Interventionscores on a scale (Least Squares Mean)
mild attacks, n=113, 109moderate/severe attacks, n=158, 168
100 mg Sumatriptan Tablet0.2410.07
20 mg Sumatriptan Nasal Powder3.9013.83

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Number of Participants With Any Treatment-emergent Non-serious and Serious Adverse Event

An adverse event is defined as any untoward medical occurrence associated with the use of an investigational product in humans, whether or not it is considered related to the investigational product. This includes any occurrence that was new in onset or aggravated in severity or frequency from the Baseline condition. (NCT01667679)
Timeframe: Baseline compared to Vist 2, 3 and 4

,
Interventionparticipants (Number)
Treatment-emergent Adverse EventTreatment-emergent Serious Adverse Event
100 mg Sumatriptan Tablet730
20 mg Sumatriptan Nasal Powder1180

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Number of Participants With the Indicated 12-lead Electrocardiogram (ECG) Findings at Baseline, Visit 3 (up to Week 12), and Visit 4 (up to Week 24)

"The Baseline value is the last non-missing value prior to or on the start date of Treatment Period 1. Clinical significance was determined by the Investigator (per clinical judgement). A categorization of normal or abnormal was made per the investigators' clinical judgment of the ECG, taking the participants' demographic characteristics and other medical conditions into account. CS = clinically significant. CNS = clinically not significant." (NCT01667679)
Timeframe: Baseline and Visits 3 (up to 12 weeks) and 4 (up to 24 weeks)

,
Interventionparticipants (Number)
Baseline, normal; n=133, 129Baseline, abnormal, CS; n=133, 129Baseline, abnormal, CNS; n=133, 129Visit 3, normal; n=110, 95Visit 3, abnormal, CS; n=110, 95Visit 3, abnormal, CNS; n=110, 95Visit 4, normal; n=124, 111Visit 4, abnormal, CS; n=124, 111Visit 4, abnormal, CNS; n=123, 111
100 mg Sumatriptan+PBO (TP1)/20 mg Sumatriptan+PBO (TP2)990307002573137
20 mg Sumatriptan+PBO (TP1)/100 mg Sumatriptan+PBO (TP2)961367903190034

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Number of Participants With the Indicated Concomitant Medications

Concomitant medications are defined as non-study medications with a start or stop date between the first dose of study medication and the end of safety follow-up, inclusive. Derm. = dermatologic; incl. - including. (NCT01667679)
Timeframe: up to 24 weeks

,
Interventionparticipants (Number)
Any concomitant medicationAgents acting on the renin-angiotensin systemOther therapeutic productsAllergensAnabolic agents for systemic useAnalgesicsAnestheticsAnti-acne preparationsAnti-Parkinson drugsAntianemic preparationsAntibacterials for systemic useAntibiotics and chemotherapeutics for derm. useAntidiarrrheals, intestinal antiinflammatoriesAntiemetics and antinauseantsAntiepilepticsAntigout preparationsAntihistamines for systemic useAntiinflammatory and antirheumatic productsAntimyotics for systemic useAntiobesity preparations, exluding diet productsAntiprotozoalsAntiseptics and disinfectantsAntithrombotic agentsAntivirals for systemic useBeta blocking agentsCalcium channel blockersCardiac therapyCorticosteroids for systemic useCorticosteroids, dermatologic preparationsCough and cold preparationsDiureticsDrugs for acid related disordersDrugs for functional gastrointestinal disordersDrugs for obstructive airways diseasesDrugs for treatment of bone diseasesDrugs used in diabetesEctoparasiticides, incl. scabacides, insecticidesGynecological antiinfectives and antisepticsImmune sera and immunoglobulinsLaxativesLipid modifying agentsMineral supplementsMuscle relaxantsNasal preparationsOpthalmologicalsOther alimentary tract and metabolism productsOther dermatological preparationsOther gynecologicalsOther nervous system drugsOtologicalsPsychoanalepticsPsycholepticsSex hormones and modulators of the genital systemThyroid therapyUnspecified herbal and traditional medicineUrologicalsVaccinesVitamins
100 mg Sumatriptan+PBO (TP1)/20 mg Sumatriptan+PBO (TP2)22614241148623201726124139143331083158181972332619021320221627651213060315916124256
20 mg Sumatriptan+PBO (TP1)/100 mg Sumatriptan+PBO (TP2)21812231143623181307115138135130182189171862252017111423201225751213157316218113157

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Number of Participants With the Indicated Physical Examination Abnormalities at Baseline, Visit 3 (up to Week 12), and Visit 4 (up to Week 24)

The Baseline value is the last non-missing value prior to or on the start date of Treatment Period 1. Clinical significance was determined by the Investigator (per clinical judgement). CS = clinically significant. CNS = clinically not significant. (NCT01667679)
Timeframe: Baseline and Visits 3 (up to 12 weeks) and 4 (up to 24 weeks)

,
Interventionparticipants (Number)
Baseline, CS; n=133, 129Baseline, CNS; n=133, 129Visit 3, CS; n=110, 95Visit 3, CNS; n=110, 95Visit 4, CS; n=124, 111Visit 4, CNS; n=124, 111
100 mg Sumatriptan+PBO (TP1)/20 mg Sumatriptan+PBO (TP2)01292930111
20 mg Sumatriptan+PBO (TP1)/100 mg Sumatriptan+PBO (TP2)113211090124

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Percentage of Attacks in Which Pain Freedom Was Achieved

Percentage of attacks in which pain freedom (defined as pain level reduced to none [Grade 0]) was achieved at 10, 15, 30, 45, 60, 90, and 120 minutes after the initial dose for all attacks. (NCT01667679)
Timeframe: Baseline and 10, 15, 30, 45, 60, 90, and 120 minutes post-dose (up to 24 weeks)

,
Interventionpercentage of attacks (Number)
10 minutes post-dose15 minutes post-dose30 minutes post-dose45 minutes post-dose60 minutes post-dose90 minutes post-dose120 minutes post-dose
100 mg Sumatriptan Tablet1.33.710.821.332.944.956.3
20 mg Sumatriptan Nasal Powder2.57.218.231.041.252.860.4

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Percentage of Attacks in Which Pain Reduction Was Achieved

Percentage of attacks in which pain reduction (defined as a decrease in pain intensity of at least one point on the following scale: 0, none; 1, mild; 2, moderate; 3, severe) was achieved at 10, 15, 30, 45, 60, 90, and 120 minutes after the initial dose for all attacks. (NCT01667679)
Timeframe: 10, 15, 30, 45, 60, 90, and 120 minutes

,
Interventionpercentage of attacks (Number)
10 minutes post-dose15 minutes post-dose30 minutes post-dose45 minutes post-dose60 minutes post-dose90 minutes post-dose120 minutes post-dose
100 mg Sumatriptan Tablet10.219.635.249.959.869.875.2
20 mg Sumatriptan Nasal Powder11.526.449.060.767.274.678.0

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Percentage of Attacks in Which Pain Relief Was Achieved

Percentage of attacks treated at a severity of moderate (Grade 2) or severe (Grade 3) in which pain relief (defined as pain level reduced to none [Grade 0] or mild [Grade 1]) was achieved at 10, 15, 30, 45, 60, 90, and 120 minutes after the initial dose for all attacks. (NCT01667679)
Timeframe: Baseline and 10, 15, 30, 45, 60, 90, and 120 minutes post-dose (up to 24 weeks)

,
Interventionpercentage of attacks (Number)
10 minutes post-dose15 minutes post-dose30 minutes post-dose45 minutes post-dose60 minutes post-dose90 minutes post-dose120 minutes post-dose
100 mg Sumatriptan Tablet11.520.938.753.962.672.076.9
20 mg Sumatriptan Nasal Powder13.827.953.865.072.177.479.6

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Number of Participants With the Indicated Amounts of Protein, Glucose, Ketones, Blood, and White Blood Cells (WBCs) in Urine at Baseline, Visit 3 (up to Week 12), and Visit 4 (up to Week 24)

"The Baseline value is the last non-missing value prior to or on the start date of Treatment Period 1. Data are based on standard reads, with 1+, 2+, and 3+ indicating increasing amounts of metabolites in urine." (NCT01667679)
Timeframe: Baseline and Visits 3 (up to 12 weeks) and 4 (up to 24 weeks)

,
Interventionparticipants (Number)
Protein, Baseline, negativeProtein, Baseline, traceProtein, Baseline, 1+Protein, Baseline, 2+Protein, Visit 3, negativeProtein, Visit 3, traceProtein, Visit 3, 1+Protein, Visit 3, 2+Protein, Visit 4, negativeProtein, Visit 4, traceProtein, Visit 4, 1+Protein, Visit 4, 2+Glucose, Baseline, negativeGlucose, Baseline, traceGlucose, Baseline, 3+Glucose, Visit 3, negativeGlucose, Visit 3, traceGlucose, Visit 3, 3+Glucose, Visit 4, negativeGlucose, Visit 4, traceGlucose, Visit 4, 1+Glucose, Visit 4, 3+Ketones, Baseline, negativeKetones, Baseline, traceKetones, Baseline, 1+Ketones, Baseline, 2+Ketones, Visit 3, negativeKetones, Visit 3, traceKetones, Visit 3, 1+Ketones, Visit 3, 2+Ketones, Visit 4, negativeKetones, Visit 4, traceKetones, Visit 4, 1+Blood, Baseline, negativeBlood, Baseline, traceBlood, Baseline, 1+Blood, Baseline, 2+Blood, Baseline, 3+Blood, Visit 3, negativeBlood, Visit 3, traceBlood, Visit 3, 1+Blood, Visit 3, 2+Blood, Visit 3, 3+Blood, Visit 4, negativeBlood, Visit 4, traceBlood, Visit 4, 1+Blood, Visit 4, 2+Blood, Visit 4, 3+WBCs, Baseline, negativeWBCs, Baseline, traceWBCs, Baseline, 1+WBCs, Baseline, 2+WBCs, Baseline, 3+WBCs, Visit 3, negativeWBCs, Visit 3, traceWBCs, Visit 3, 1+WBCs, Visit 3, 2+WBCs, Visit 3, 3+WBCs, Visit 4, negativeWBCs, Visit 4, traceWBCs, Visit 4, 1+WBCs, Visit 4, 2+WBCs, Visit 4, 3+
100 mg Sumatriptan+PBO (TP1)/20 mg Sumatriptan+PBO (TP2)10519327515509012611262194101081001217108860110180116431578642594653110181154757463857584
20 mg Sumatriptan+PBO (TP1)/100 mg Sumatriptan+PBO (TP2)1121650921141104173013210107011220111247021025101193211672539445231113145991212739084511055482

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Mean Sum of Migraine Pain Intensity Differences (SPID)-30

"SPID-30 is defined as the sum of the pain intensity differences (measured as area under the curve) from dosing (Baseline) through 30 minutes post-dose for headaches with a Baseline intensity of mild, moderate, or severe. The range of possible scores is -60 to +90. A higher number indicates a greater reduction in pain intensity. Negative values indicate worsening pain. A value of 0 indicates that there was no change in pain intensity from Baseline through 30 minutes. Results are from an analysis of covariance (ANCOVA) model with treatment, period, and treatment sequence as fixed effects and participant as a random effect. The Last Observation Carried Forward (LOCF) imputation method (missing values were replaced by carrying forward the preceding value) was used for this analysis." (NCT01667679)
Timeframe: Baseline and 30 minutes post-dose (up to 24 weeks)

Interventionscores on a scale (Least Squares Mean)
20 mg Sumatriptan Nasal Powder10.80
100 mg Sumatriptan Tablet7.41

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Median Time to Pain Freedom

Pain freedom is defined as a pain level reduced to none (Grade 0). (NCT01667679)
Timeframe: 120 minutes post-dose (up to 24 weeks)

Interventionminutes (Median)
20 mg Sumatriptan Nasal Powder91
100 mg Sumatriptan Tablet121

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Pain Freedom

1) Pain Freedom: Pain Freedom at 2 hours is defined as being free of pain. Pain was assessed using a 4-point scale (none, mild, moderate, and severe). (NCT01807234)
Timeframe: 2-hours

Interventionpercentage of patients (Number)
Ketorolac/ Placebo43.1
Sumatriptan/Placebo36.7
Ketorolac Placebo/ Sumatriptan Placebo18.4

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Absence of Photophobia

2) Defined as reduction of photophobia to none. Symptom was assessed using a 4-point scale (none, mild, moderate, and severe) (NCT01807234)
Timeframe: 2-hours

Interventionpercentage of patients (Number)
Ketorolac/ Placebo65.4
Sumatriptan/ Placebo64.0
Ketorolac Placebo/ Sumatriptan Placebo46.0

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Absence of Nausea

4) Defined as reduction of nausea to none. Symptom was assessed using a 4-point scale (none, mild, moderate, and severe) (NCT01807234)
Timeframe: 2-hours

Interventionpercentage of patients (Number)
Ketorolac/ Placebo82.7
Sumatriptan/ Placebo74.0
Ketorolac Placebo/ Sumatriptan Placebo66.0

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Absence of Allodynia

5) Absence of allodynia The presence of allodynia was assessed based on a series of 8 questions inquiring as to the presence of allodynia. Participants answering 2 or more questions positively were considered to have allodynia. (NCT01807234)
Timeframe: 2-hours

Interventionpercentage of patients (Number)
Ketorolac/ Placebo70.5
Sumatriptan/ Placebo75.5
Ketorolac Placebo/ Sumatriptan Placebo69.0

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2- Hour Pain Relief

The primary outcome was 2-hour headache relief; headache relief was defined as headache pain from moderate or severe pain to none or mild pain. Pain was assessed using a 4-point scale (none, mild, moderate, and severe) (NCT01807234)
Timeframe: 2 hours

Interventionpercentage of participants (Number)
Ketorolac/ Placebo72.5
Sumatriptan/ Placebo69.4
Ketorolac Placebo/ Sumatriptan Placebo38.8

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Time to Pain Relief

9) The time, in minutes, will be measured from the time study drug is taken to the time when significant pain relief is first observed and maintained through 2 hours with no rescue medication use at or prior to this point. (NCT01807234)
Timeframe: following each treated migraine attack

,,
Interventionpercentage of patients (Number)
10 minutes15 minutes20 minutes30 minutes1 hour
Ketorolac Placebo/ Sumatriptan Placebo12.214.322.426.532.6
Ketorolac/ Placebo15.735.343.154.958.8
Sumatriptan/ Placebo14.336.044.953.157.1

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Absence of Phonophobia

3) Defined as reduction of phonophobia to none. Symptom was assessed using a 4-point scale (none, mild, moderate, and severe) (NCT01807234)
Timeframe: 2-hours

Interventionpercentage of patients (Number)
Ketorolac/ Placebo75.0
Sumatriptan/Placebo66.0
Ketorolac Placebo/ Sumatriptan Placebo56.0

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Self-assessment of Disability: Percentage of Participants With Moderate or Severe Disability

Participants' self-assessment of disability was assessed using 4-point scales (none, mild, moderate, and severe). A binary outcome variable was created grouping none and mild vs moderate to severe. . (NCT01807234)
Timeframe: 2-hours

Interventionpercentage of patients (Number)
Ketorolac/ Placebo1.9
Sumatriptan/ Placebo8.1
Ketorolac Placebo/ Sumatriptan Placebo10.2

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Sustained Pain Freedom (SPF)

8) 24 and 48 hours sustained pain freedom (SPF); Defined as the reduction of pain to none. Pain was assessed using a 4-point scale (none, mild, moderate, and severe). (NCT01807234)
Timeframe: 24 and 48 hours

,,
Interventionpercentage of patients (Number)
24 hour sustained pain freedom48 hour sustained pain freedom
Ketorolac Placebo/ Sumatriptan Placebo12.212.2
Ketorolac/ Placebo35.333.3
Sumatriptan/ Placebo22.418.4

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Sustained Pain Relief (SPR)

7) 24 and 48 hours sustained pain relief (SPR) Defined as the reduction of pain to none or mild from moderate or severe, on a 4-point scale (none, mild, moderate, and severe). (NCT01807234)
Timeframe: 24 and 48 hours

,,
Interventionpercentage of patients (Number)
24 hour sustained pain relief48 hour sustained pain relief
Ketorolac Placebo/ Sumatriptan Placebo20.420.4
Ketorolac/ Placebo49.049.0
Sumatriptan/ Placebo40.830.6

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Change in Headache Relief

percent of headaches that had complete resolution (pain free at 2 hours) for each person, during the initial (pre-intervention) month when they used their regular treatment and during the second of the two months (intervention) when they treated headaches with sumatriptan compared using a mixed-effects regression model. Reported number is the difference in headache resolution from the pre-intervention headaches to the intervention headaches. (NCT01854385)
Timeframe: 1 month

Interventionpercentage of headaches resolved (Mean)
Sumatriptan23

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Adverse Events

The investigators will calculate the percent who stopped taking sumatriptan because of side effects, percent who experienced each adverse event. (NCT01854385)
Timeframe: 2 months

Interventionparticipants (Number)
Stopped taking sumatriptan due to side effectsRebound headachesFatigue/drowsinessDizzinessGastrointestinal symptomsNumbness/TinglingItch/rashJoint painRestlessnessSweating/flushingElevated blood pressureAnxietySore Throat
Sumatriptan0122421112111

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Headache Diary Compliance

The investigators will calculate the mean percentage of headache diary completion of intervention subjects in the final month of participation. (NCT01854385)
Timeframe: 1 month

Interventionpercentage of diary days completed (Mean)
Sumatriptan80

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Sumatriptan Compliance

Mean rate of headaches treated with sumatriptan in final month of intervention. (NCT01854385)
Timeframe: 1 month

Interventionpercentage of headaches (Mean)
Sumatriptan25

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Number of Headaches Relieved

Headache relief from before treatment, at 30 minutes, 1 hour, and 2 hours post treatment in attacks treated with VVD-101 vs. placebo. Headache relief is defined as a headache going from moderate or severe to mild or no headache or mild headache going to no headache. Headache severity was measured on a 4 point Likert scale with 0 = no pain, 1 = mild pain, 2 = moderate, 3 = severe pain. (NCT02176655)
Timeframe: Immediately Prior to Treatment to 2 Hours Post Treatment

,
InterventionHeadaches (Number)
30 Minutes Post-Treatment1 Hour Post-Treatment2 Hours Post-Treatment
Placebo121727
VVD-101102330

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Headache Severity at Treatment, 30 Minutes and 1 Hour Post Treatment

Change in headache severity from before treatment, at 30 minutes, and 1 hour post treatment in attacks treated with VVD-101 vs. placebo. Headache severity was measured on a 4 point Likert scale with 0 = no pain, 1 = mild pain, 2 = moderate, 3 = severe pain. (NCT02176655)
Timeframe: Immediately Prior to Treatment through 1 Hours Post Treatment

,
Interventionunits on a scale (Mean)
Pre-Treatment30 Mintues Post-Treatment1 Hour Post-Treatment
Placebo2.091.851.55
VVD-1012.181.781.20

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Comparing Acute Hangover Scale Individual Symptoms With Headache Severity 2 Hours Post Treatment

Comparison of headache severity 2 hours post treatment of headache treated with VVD-101 with each associated hangover symptom items on the AHS taken before treatment. Individual Hangover Symptoms Scores range from 0 [None] to 7 [Incapacitating]. The AHS scale is rated on a score of 0-63. A score of 0 indicates no symptoms and a total score of 63 indicates the maximum number of reported symptoms.Headache severity was measured on a 4 point Likert scale with 0 = no pain, 1 = mild pain, 2 = moderate, 3 = severe pain. (NCT02176655)
Timeframe: Immediately Before Treatment to 2 Hours Post Treatment

Interventionunits on a scale (Mean)
HangoverThirstyTiredHeadacheDizziness or FaintnessNauseaStomach AcheHeart RacingLoss of AppetiteHeadache Pain Severity 2 Hours Post Treatment
VVD-1013.533.53.784.231.651.751.581.101.88.85

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Acute Hangover Scale Compared to Pain Severity 2 Hours Post Treatment

Comparison of Acute Hangover Scale (AHS) score before treatment with headache pain severity 2 hours post treatment for headaches treated with VVD-101. The AHS scale is rated on a score of 0-63. A score of 0 indicates no symptoms and a total score of 63 indicates the maximum number of reported symptoms. Headache severity was measured on a 4 point Likert scale with 0 = no pain, 1 = mild pain, 2 = moderate, 3 = severe pain. (NCT02176655)
Timeframe: Immediately Before Treatment of 3 Headaches to 2 Hours Post Treatment

Interventionunits on a scale (Mean)
Acute Hangover Scale Before TreatmentHeadache Pain Severity 2 Hours Post Treatment
VVD-10122.98.85

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Satisfaction

To assess subject satisfaction with treatment results comparing VVD-101 vs. placebo. Satisfaction was measured on a 7 point Likert scale whereas 0 = extremely dissatisfied and 6 = extremely satisfied. (NCT02176655)
Timeframe: 24 Hours Post Treatment for 3 Headaches (estimated 6 months)

Interventionunits on a scale (Mean)
VVD-1013.75
Placebo2.62

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Number of Participants With Consistent Response to VVD-101

To assess the consistency of response to VVD-101 over the three active treatments of VVD-101. Consistency is defined as meeting the requirements of headache relief 2 hours post treatment for 2 out of 3 active treated headaches. Headache relief is defined as a headache going from moderate or severe to mild or no headache or mild headache going to no headache. Headache severity was measured on a 4 point Likert scale with 0 = no pain, 1 = mild pain, 2 = moderate, 3 = severe pain. (NCT02176655)
Timeframe: Response to Treatment of Three Headaches (estimated 6 months)

Interventionparticipants (Number)
VVD-1019

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Number of Headaches With Sustained Pain Freedom at Twenty Four Hours Post Treatment

Number of headaches with sustained headache pain freedom at 24 hours post treatment for VVD-101 vs. placebo. Sustained headache pain freedom is defined as no pain 2 hours post treatment and headache freedom continuing for 24 hours post treatment without rescue. Headache severity was measured on a 4 point Likert scale with 0 = no pain, 1 = mild pain, 2 = moderate, 3 = severe pain. (NCT02176655)
Timeframe: Time of Treatment to 24 Hours Post Treatment

InterventionHeadaches (Number)
VVD-10115
Placebo12

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Number of Headaches Relieved to Complete Pain Freedom at Two Hours Post Treatment

Number of headaches relieved (no head pain) at 2 hours post treatment for VVD-101 vs. placebo. Headache severity was measured on a 4 point Likert scale with 0 = no pain, 1 = mild pain, 2 = moderate, 3 = severe pain. (NCT02176655)
Timeframe: Immediately Prior to Treatment to 2 Hours Post Treatment

InterventionHeadaches (Number)
VVD-10115
Placebo13

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Number of Drinks Consumed Compared to Pain Severity 2 Hours Post Treatment

Comparison of the number of drinks consumed at one sitting with pain severity 2 hours post treatment for headaches treated with VVD-101. Headache severity was measured on a 4 point Likert scale with 0 = no pain, 1 = mild pain, 2 = moderate, 3 = severe pain. (NCT02176655)
Timeframe: Time of Last Sitting to 2 Hours Post Treatment (estimated 14 hours)

InterventionNumber of Drinks Consumed (Mean)
VVD-1014.71

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Meaningful Headache Relief

Time to meaningful headache relief for VVD-101 vs. placebo. Meaningful headache relief is defined as experiencing substantial relief as reported by the subject. (NCT02176655)
Timeframe: Time of Onset to Meaningful Headache Relief (up to 24 hours)

Interventionminutes (Mean)
VVD-101226.33
Placebo351.14

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Headache Severity 2 Hours Post Treatment

Headache severity 2 hours post treatment in sumatriptan succinate 12.5 mg and acetylsalicylic acid 325 mg (VVD-101) vs. placebo. Headache severity was measured on a 4 point Likert scale with 0 = no pain, 1 = mild pain, 2 = moderate, 3 = severe pain. (NCT02176655)
Timeframe: Immediately Prior to Treatment through 2 Hours Post Treatment

,
Interventionunits on a scale (Mean)
Pre-Treatment2 Hours Post-Treatment
Placebo2.091.17
VVD-1012.180.85

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The Percentage of Subjects Reporting Pain Freedom at 60 Minutes Post-treatment

(NCT02571049)
Timeframe: 60 minutes post-treatment

InterventionPercentage of responders (Number)
Sumatriptan 3 mg50
Sumatriptan 6 mg52.63

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Area Under the Concentration-time Curve From Time 0 to 6 Hours for Sumatriptan

"Plasma concentrations of sumatriptan were quantified using a validated high performance liquid chromatographic method with tandem mass spectrometry detection.~Area under the plasma concentration-time curve from time 0 to 6 hours post dose (AUC6hr) after the 2nd 6 mg dose of sumatriptan was estimated using the linear trapezoidal method. Sumatriptan plasma concentrations below the lower limit of quantification (LLOQ; 0.100 ng/mL) were set to 0 before data analysis.~Log-transformed AUC6hr was analyzed using a linear mixed effects model with treatment as a fixed effect and subject as a random effect.~Sumatriptan Alone data include participants from both Groups A (Parts 1 and 2) and B (Part 1 only)." (NCT02741310)
Timeframe: Day 2 and day 5 at 1 hour (prior to 2nd sumatriptan injection), 1 hour 10 minutes, 1.25, 1.5, 2, 3, 4.5, and 7 hours relative to the first 6 mg dose of sumatriptan.

Interventionhr*ng/mL (Geometric Least Squares Mean)
Sumatriptan Alone133.33
Erenumab + Sumatriptan130.59

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Time-weighted Averages of Mean Arterial Pressure

"Mean arterial pressure (MAP) is the average arterial pressure during a single cardiac cycle. MAP was calculated as diastolic blood pressure (DBP) + 0.33 * (systolic blood pressure [SBP]-DBP). Individual time-weighted average in MAP were calculated as area under the measurement-time curve from predose through 2.5 hours of MAP divided by the time period over which the measurements were made (ie, AUCmap0-2.5 hr /2.5 hours).~Data were analyzed using a linear mixed effects regression model with fixed effects for treatment and period and random effect for subject; Sumatriptan Alone data include participants from both Groups A (Parts 1 and 2) and B (Part 1 only)." (NCT02741310)
Timeframe: Days 2 and 5 from predose to 2.5 hours after sumatriptan dosing.

InterventionmmHg (Least Squares Mean)
Sumatriptan Alone87.40
Erenumab + Sumatriptan87.36

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Number of Participants With Adverse Events

"Adverse events (AEs) were graded according to the Common Terminology Criteria for Adverse Events (CTCAE) version 4.0 and according to the following:~Grade 1 = Mild AE, asymptomatic or mild symptoms; Grade 2 = Moderate, minimal, local or noninvasive intervention indicated; Grade 3 = Severe or medically significant but not immediately life-threatening; Grade 4 = Life-threatening consequences, urgent intervention indicated; Grade 5 = Death related to AE." (NCT02741310)
Timeframe: From the first dose of study drug (sumatriptan, placebo or erenumab) until 84 days after the last dose (89 days). Part 1 includes AEs from day 1 to predose on day 4 and Part 2 includes AEs from day 4 through day 89.

,,,
InterventionParticipants (Count of Participants)
Any adverse eventAdverse event ≥ grade 2Adverse event ≥ grade 3Adverse event ≥ grade 4Serious adverse eventsAE leading to discontinuation of study drugFatal adverse events
Part 1 Group A: Placebo + Sumatriptan11100020
Part 1 Group B: Placebo + Sumatriptan19000020
Part 2 Group A: Placebo + Sumatriptan9000000
Part 2 Group B: Erenumab + Sumatriptan17300000

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Number of Participants Who Developed Anti-erenumab Antibodies

"Two validated assays were used to detect the presence of anti-erenumab antibodies. All samples were first tested in an electrochemiluminescence-based bridging assay to detect antibodies capable of binding to erenumab (Binding Antibody Assay). Samples confirmed to be positive for binding antibodies were subsequently tested in a cell-based assay to determine neutralizing activity against erenumab (Neutralizing Antibody Assay). If a post-dose sample was positive for binding antibodies and demonstrated neutralizing activity at the same time point, the sample was defined as positive for neutralizing antibodies.~Binding/neutralizing antibody positive is defined as participants with an antibody positive postbaseline results and with a negative or no result at baseline." (NCT02741310)
Timeframe: Baseline and day 89

,
InterventionParticipants (Count of Participants)
Binding antibody positiveNeutralizing antibody positive
Group A: Placebo + Sumatriptan00
Group B: Erenumab + Sumatriptan11

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Maximum Observed Plasma Concentration (Cmax) of Sumatriptan

"Plasma concentrations of sumatriptan were quantified using a validated high performance liquid chromatographic method with tandem mass spectrometry detection. Sumatriptan plasma concentrations below the lower limit of quantification (LLOQ) (0.100 ng/mL) were set to 0 before data analysis.~Log-transformed maximum observed plasma concentration (Cmax) was analyzed using a linear mixed effects model with treatment as a fixed effect and subject as a random effect. Sumatriptan Alone data include participants from both Groups A (Parts 1 and 2) and B (Part 1 only)." (NCT02741310)
Timeframe: Day 2 and day 5 at predose, 1 hour (prior to 2nd sumatriptan injection), 1 hour 10 minutes, 1.25, 1.5, 2, 3, 4.5, and 7 hours relative to the first 6 mg dose of sumatriptan.

Interventionng/mL (Geometric Least Squares Mean)
Sumatriptan Alone83.50
Erenumab + Sumatriptan79.00

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Area Under the Concentration-time Curve From Time 0 to Infinity for Sumatriptan

"Plasma concentrations of sumatriptan were quantified using a validated high performance liquid chromatographic method with tandem mass spectrometry detection. The area under the plasma concentration-time curve from time 0 to infinity (AUCinf) after the 2nd 6 mg dose of sumatriptan was estimated as the sum of AUClast and Clast/λz where Clast is the last observed concentration and λz is the first-order terminal rate constant estimated via linear regression of the terminal log-linear decay phase. Sumatriptan plasma concentrations below the lower limit of quantification (LLOQ) (0.100 ng/mL) were set to 0 before data analysis.~Log-transformed AUCinf was analyzed using a linear mixed effects model with treatment as a fixed effect and subject as a random effect. Sumatriptan Alone data include participants from both Groups A (Parts 1 and 2) and B (Part 1 only)." (NCT02741310)
Timeframe: Day 2 and day 5 at 1 hour (prior to 2nd sumatriptan injection), 1 hour 10 minutes, 1.25, 1.5, 2, 3, 4.5, and 7 hours relative to the first 6 mg dose of sumatriptan.

Interventionhr*ng/mL (Geometric Least Squares Mean)
Sumatriptan Alone144.32
Erenumab + Sumatriptan144.81

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Number of Participants With Absence of Most Bothersome Symptom (MBS) Among Nausea, Photophobia and Phonophobia at 2 Hours (DB1)

Number of participants with their MBS among nausea, photophobia and phonophobia absent at 10, 15, 20, 30, 60, 90, and 120 minutes after the first dose of study medication taken for a migraine attack during DB1 treatment period are summarized by treatment group and time point for the full analysis set (FAS1). The corresponding p-values from Fisher's exact test were computed for the comparison between treatment groups. Subjects who reported a MBS predose and reported the status of the MBS at the particular postdose time point were analyzed. (NCT02856802)
Timeframe: 2 hours after study medication administration

InterventionParticipants (Count of Participants)
DFN-02 (DB1)29
Placebo (DB1)15

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Number of Participants With Headache Pain Freedom at 2 Hours Postdose in the Double-blind Treatment Period 2 (DB2)

In Double-blind Treatment Period 2 (DB2), freedom from headache pain 2 hours after the first dose of study medication taken within one hour of experiencing a migraine attack for any headache pain level, e.g., mild [Grade 1], moderate [Grade 2], or severe [Grade 3] and reduced to none [Grade 0] after study medication administration. If the subject was not able to use study medication for the first migraine after randomization, they were instructed to use the study medication for the next attack. (NCT02856802)
Timeframe: 2 hours after study medication administration

InterventionParticipants (Count of Participants)
DFN-02 (DB2)19
Placebo (DB2)17

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Number of Participants Free From Headache Pain at 2 Hours After the First Dose of Study Medication Taken for a Migraine Attack With Moderate to Severe Headache Pain During the Double-blind Treatment Period 1 (DB1).

Freedom from headache pain at 2 hours after the first dose of study medication taken within one hour after experiencing a migraine attack of moderate to severe headache pain during the DB1 treatment period, e.g., headache pain rating of moderate [Grade 2] or severe [Grade 3] predose and reduced to none [Grade 0] postdose). Mild headache pain was recorded as Grade 1. If the subject was not able to use study medication for the first migraine after randomization, they were instructed to use the study medication for the next attack. If the subject experienced insufficient relief from the first dose of study medication, they were permitted to take a second dose of study medication or rescue medication 2 or more hours after the first dose, and only after completing the 2 hours' postdose assessments. If no relief was experienced from the first dose of study medication after 2 hours only rescue medication could be administered. Maximum 2 doses of study medication per 24 hours. (NCT02856802)
Timeframe: 2 hours after study medication administration

InterventionParticipants (Count of Participants)
DFN-02 (DB1)21
Placebo (DB1)9

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Pharmacodynamics- Change From Pre-dose to 24 Hours in ECGs: QTcB - Bazett's Correction Formula

A standard, digital 12-lead ECG with a 10-second rhythm strip was used to assess cardiac function after participants have been at least 5 minutes supine. Serial ECGs collected when lasmiditan administered alone and when sumatriptan is administered alone compared to when lasmiditan and sumatriptan are administered together. (NCT03076970)
Timeframe: Pre-dose, 24 hours post-dose

Interventionmsec (Mean)
Lasmiditan 200 mg-2.7
Sumatriptan 100 mg-3.3
Combination of Lasmiditan and Sumatriptan1.6

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Pharmacodynamics- Change From Pre-dose to 24 Hours in ECGs: QTcF - Fridericia's Correction Formula

A standard, digital 12-lead ECG with a 10-second rhythm strip was used to assess cardiac function after participants have been at least 5 minutes supine. Serial ECGs collected when lasmiditan administered alone and when sumatriptan is administered alone compared to when lasmiditan and sumatriptan are administered together. (NCT03076970)
Timeframe: Pre-dose, 24 hours post-dose

Interventionmsec (Mean)
Lasmiditan 200 mg-1.8
Sumatriptan 100 mg-2.0
Combination of Lasmiditan and Sumatriptan1.3

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Pharmacodynamics- Change From Pre-dose to 24 Hours in ECGs: Summary (Mean) PR Duration

A standard, digital 12-lead ECG with a 10-second rhythm strip was used to assess cardiac function after participants have been at least 5 minutes supine. Serial ECGs collected when lasmiditan administered alone and when sumatriptan is administered alone compared to when lasmiditan and sumatriptan are administered together. (NCT03076970)
Timeframe: Pre-dose, 24 hours post-dose

Interventionmilliseconds (msec) (Mean)
Lasmiditan 200 mg-4.5
Sumatriptan 100 mg-2.5
Combination of Lasmiditan and Sumatriptan-1.6

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Pharmacodynamics- Change From Pre-dose to 24 Hours in ECGs: Summary (Mean) QRS Duration

A standard, digital 12-lead ECG with a 10-second rhythm strip was used to assess cardiac function after participants have been at least 5 minutes supine. Serial ECGs collected when lasmiditan administered alone and when sumatriptan is administered alone compared to when lasmiditan and sumatriptan are administered together. (NCT03076970)
Timeframe: Pre-dose, 24 hours post-dose

Interventionmsec (Mean)
Lasmiditan 200 mg-0.5
Sumatriptan 100 mg-1.7
Combination of Lasmiditan and Sumatriptan-0.6

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Pharmacodynamics- Change From Pre-dose to 24 Hours in ECGs: Summary (Mean) QT Duration

A standard, digital 12-lead ECG with a 10-second rhythm strip was used to assess cardiac function after participants have been at least 5 minutes supine. Serial ECGs collected when lasmiditan administered alone and when sumatriptan is administered alone compared to when lasmiditan and sumatriptan are administered together. (NCT03076970)
Timeframe: Pre-dose, 24 hours post-dose

Interventionmsec (Mean)
Lasmiditan 200 mg0.1
Sumatriptan 100 mg1.0
Combination of Lasmiditan and Sumatriptan0.6

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Pharmacodynamics- Change From Pre-dose to 24 Hours in ECGs: Summary (Mean) RR Duration

A standard, digital 12-lead ECG with a 10-second rhythm strip was used to assess cardiac function after participants have been at least 5 minutes supine. Serial ECGs collected when lasmiditan administered alone and when sumatriptan is administered alone compared to when lasmiditan and sumatriptan are administered together. (NCT03076970)
Timeframe: Pre-dose, 24 hours post-dose

Interventionmsec (Mean)
Lasmiditan 200 mg14.1
Sumatriptan 100 mg24.2
Combination of Lasmiditan and Sumatriptan-4.1

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Pharmacodynamics- Change From Pre-dose to 24 Hours in Vital Signs: Diastolic Blood Pressure

Vital signs were measured in semi-supine position after 5 minutes rest. Serial vital signs assessed when lasmiditan is administered alone and when sumatriptan is administered alone compared to when lasmiditan and sumatriptan are administered together. (NCT03076970)
Timeframe: Pre-dose, 24 hours post-dose

InterventionmmHg (Mean)
Lasmiditan 200 mg-1.3
Sumatriptan 100 mg-1.1
Combination of Lasmiditan and Sumatriptan0.6

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Pharmacodynamics- Change From Pre-dose to 24 Hours in Vital Signs: Pulse Rate

Vital signs were measured in semi-supine position after 5 minutes rest. Serial vital signs assessed when lasmiditan is administered alone and when sumatriptan is administered alone compared to when lasmiditan and sumatriptan are administered together. (NCT03076970)
Timeframe: Pre-dose, 24 hours post-dose

Interventionbeats/min (Mean)
Lasmiditan 200 mg-2.5
Sumatriptan 100 mg-1.0
Combination of Lasmiditan and Sumatriptan1.8

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Pharmacodynamics- Change From Pre-dose to 24 Hours in Vital Signs: Respiratory Rate

Vital signs were measured in semi-supine position after 5 minutes rest. Serial vital signs assessed when lasmiditan is administered alone and when sumatriptan is administered alone compared to when lasmiditan and sumatriptan are administered together. (NCT03076970)
Timeframe: Pre-dose, 24 hours post-dose

Interventionbreaths/min (Mean)
Lasmiditan 200 mg0.2
Sumatriptan 100 mg0.2
Combination of Lasmiditan and Sumatriptan0.7

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Pharmacodynamics- Change From Pre-dose to 24 Hours in Vital Signs: Systolic Blood Pressure

Vital signs were measured in semi-supine position after 5 minutes rest. Serial vital signs assessed when lasmiditan is administered alone and when sumatriptan is administered alone compared to when lasmiditan and sumatriptan are administered together. (NCT03076970)
Timeframe: Pre-dose, 24 hours post-dose

Interventionmillimeters of mercury (mmHg) (Mean)
Lasmiditan 200 mg0.6
Sumatriptan 100 mg-2.3
Combination of Lasmiditan and Sumatriptan-0.1

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Pharmacokinetics - AUC0-t

Area under the plasma concentration versus time curve from time 0 to the time t of the last quantifiable concentration, calculated by means of the mixed log-linear trapezoidal rule of lasmiditan alone compare to lasmiditan in combination with sumatriptan. (NCT03076970)
Timeframe: Pre-dose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 16, 24 and 30 hours following the dose at time 0 in each dosing period

Interventionnanogram*hour per milliliter (ng*h/mL) (Geometric Mean)
Lasmiditan Alone1730
Combination of Lasmiditan and Sumatriptan1650

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Pharmacokinetics - Cmax

Maximum plasma concentration of lasmiditan alone compared to lasmiditan in combination with sumatriptan. (NCT03076970)
Timeframe: Pre-dose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 16, 24 and 30 hours following the dose at time 0 in each dosing period

Interventionnanogram per milliliter (ng/mL) (Geometric Mean)
Lasmiditan Alone268
Combination of Lasmiditan and Sumatriptan238

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Pharmacokinetics - Tmax

Time to maximum plasma concentration of lasmiditan alone compared to lasmiditan in combination with sumatriptan. (NCT03076970)
Timeframe: Pre-dose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 16, 24 and 30 hours following the dose at time 0 in each dosing period

Interventionhour (Mean)
Lasmiditan Alone2.00
Combination of Lasmiditan and Sumatriptan3.00

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Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)

Safety assessed from time of consent through end of study. A summary of all reported serious adverse events (SAE) and other adverse events regardless of causality are provided in the adverse events module of this record. (NCT03076970)
Timeframe: Up to 6 weeks

,,
InterventionParticipants (Count of Participants)
Adverse Events (AEs)Serious Adverse Events (SAEs)
Combination of Lasmiditan and Sumatriptan280
Lasmiditan 200 mg240
Sumatriptan 100 mg160

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Pharmacodynamics- Change From Pre-dose to 24 Hours in Vital Signs: Temperature

Vital signs were measured in semi-supine position after 5 minutes rest. Serial vital signs assessed when lasmiditan is administered alone and when sumatriptan is administered alone compared to when lasmiditan and sumatriptan are administered together. (NCT03076970)
Timeframe: Pre-dose, 24 hours post-dose

InterventionCelsius (C) (Mean)
Lasmiditan 200 mg0.0
Sumatriptan 100 mg-0.0
Combination of Lasmiditan and Sumatriptan-0.1

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Pharmacodynamics- Change From Pre-dose to 24 Hours in ECGs: Heart Rate

A standard, digital 12-lead ECG with a 10-second rhythm strip was used to assess cardiac function after participants have been at least 5 minutes supine. Serial ECGs collected when lasmiditan administered alone and when sumatriptan is administered alone compared to when lasmiditan and sumatriptan are administered together. (NCT03076970)
Timeframe: Pre-dose, 24 hours post-dose

Interventionbeats/min (Mean)
Lasmiditan 200 mg-0.8
Sumatriptan 100 mg-1.3
Combination of Lasmiditan and Sumatriptan0.4

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Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0 ∞]) of Lasmiditan and Sumatriptan

PK: AUC(0 ∞) of Lasmiditan and Sumatriptan was evaluated. (NCT03310411)
Timeframe: Lasmiditan: Predose, 0.5, 1, 1.5,2, 2.5, 3, 4, 6, 8, 12, 24 ,36 and 48 h postdose; Sumatriptan: Predose, 0.5, 1, 1.5,2, 2.5, 3, 4, 6, 8, 12 and 24 h postdose

Interventionnanogram*hour per milliliter (ng*hr/mL) (Geometric Mean)
200mg Lasmiditan + 100mg Sumatriptan (A): Analyte: Lasmiditan2110
200 mg Lasmiditan + Placebo (B): Analyte: Lasmiditan2170
200 mg Lasmiditan +100 mg Sumatriptan (A):Analyte: Sumatriptan253
100 mg Sumatriptan + Placebo (C): Analyte: Sumatriptan240

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Pharmacodynamics (PD): Change From Baseline in Mean 24-hour Systolic Blood Pressure (SBP)

Systolic Blood Pressure (SBP) was measured by using a 24-hour Ambulatory Blood Pressure Monitoring (ABPM) device attached to the participant's nondominant arm. Ambulatory blood pressure measurements were recorded every 20 minutes during the daytime (0700 to 2200 hours) and every 30 minutes during the nighttime hours (2200 to 0700), as preprogrammed into the device. For statistical analyses, diurnal hours were defined as 0800 to 2100 and nocturnal hours were defined as 0000 to 0600. Least squares (LS) mean peak changes from baseline were calculated using a linear mixed-effects model with baseline, treatment, period, and sequence as fixed effects and participant as a random effect. (NCT03310411)
Timeframe: Baseline (Day 1), Day 2

InterventionMillimeters of mercury (mmHg) (Least Squares Mean)
200 mg Lasmiditan + 100 mg Sumatriptan (A):13.81
200 mg Lasmiditan + Placebo (B)12.17
100 mg Sumatriptan + Placebo (C)13.63
Placebo + Placebo (D)11.42

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Pharmacokinetics (PK): Maximum Observed Concentration (Cmax) of Lasmiditan and Sumatriptan

PK: Cmax of Lasmiditan and Sumatriptan was evaluated. (NCT03310411)
Timeframe: Lasmiditan: Predose, 0.5, 1, 1.5,2, 2.5, 3, 4, 6, 8, 12 , 24 ,36 and 48 hours(h) postdose; Sumatriptan: Predose, 0.5, 1, 1.5,2, 2.5, 3, 4, 6, 8, 12 and 24 h postdose

Interventionnanogram per milliliter (ng/mL) (Geometric Mean)
200 mg Lasmiditan + 100 mg Sumatriptan (A):Analyte: Lasmiditan304
200 mg Lasmiditan + Placebo (B): Analyte: Lasmiditan328
200 mg Lasmiditan +100 mg Sumatriptan (A):Analyte: Sumatriptan56.8
100 mg Sumatriptan + Placebo (C): Analyte: Sumatriptan50.7

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Number of Participants Who Were Headache Pain Free at 120 Minutes After Treatment

Participants will self-report the severity of their headache. (NCT03338920)
Timeframe: 120 minutes

InterventionParticipants (Count of Participants)
Sumatriptan Nasal Powder8
Placebo9

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