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almotriptan

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Description

almotriptan : An indole compound having a 2-(dimethylamino)ethyl group at the 3-position and a (pyrrolidin-1-ylsulfonyl)methyl group at the 5-position. [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 CID123606
CHEMBL ID1505
CHEBI ID520985
SCHEMBL ID1957
MeSH IDM0363903

Synonyms (88)

Synonym
BIDD:GT0048
BRD-K67601717-001-02-0
las-31416
pnu-180638
almogran
las 31416
154323-57-6
almotriptan (usan)
D02824
SPECTRUM_001884
SPECTRUM5_001554
BSPBIO_002731
almotriptan
DB00918
1-(((3-(2-(dimethylamino)ethyl)indol-5-yl)methyl)sulfonyl)pyrrolidine
NCGC00095135-02
NCGC00095135-01
almotriptan [usan:inn:ban]
pyrrolidine, 1-(((3-(2-(dimethylamino)ethyl)-1h-indol-5-yl)methyl)sulfonyl)-
KBIO2_002408
KBIO2_007544
KBIOSS_002414
KBIO2_004976
KBIOGR_001647
KBIO3_001951
SPECTRUM2_000498
SPBIO_000395
SPECTRUM3_001006
SPECTRUM4_001134
SPECTRUM1505204
NCGC00095135-03
nsc-760092
CHEMBL1505
L000846
n,n-dimethyl-2-[5-(pyrrolidin-1-ylsulfonylmethyl)-1h-indol-3-yl]ethanamine
FT-0651595
HMS1922L13
chebi:520985 ,
n,n-dimethyl-2-{5-[(pyrrolidin-1-ylsulfonyl)methyl]-1h-indol-3-yl}ethanamine
A809522
pharmakon1600-01505204
nsc760092
cas-154323-57-6
dtxcid3024289
dtxsid5044289 ,
tox21_111444
n,n-dimethyl-2-(5-((pyrrolidin-1-ylsulfonyl)methyl)-1h-indol-3-yl)ethanamine
CCG-39569
unii-1o4xl5sn61
1o4xl5sn61 ,
nsc 760092
almotriptan-d6
NCGC00095135-04
AM84500
AKOS015895080
gtpl7110
dimethyl(2-{5-[(pyrrolidine-1-sulfonyl)methyl]-1h-indol-3-yl}ethyl)amine
1-[[3-(2-dimethylaminoethyl)-5-indolyl]methanesulphonyl]pyrrolidine
almotriptan [mi]
1-[[[3-[2-(dimethylamino)ethyl]indol-5-yl]methyl]sulfonyl]pyrrolidine
almotriptan [vandf]
almotriptan [inn]
almotriptan [usan]
almotriptan [who-dd]
SCHEMBL1957
NCGC00095135-05
tox21_111444_1
tox21 111444
CS-4530
almotrintan
HY-B0383A
AB01563047_01
AB01563047_02
pyrrolidine, 1-[[[3-[2-(dimethylamino)ethyl]-1h-indol-5-yl]methyl]sulfonyl]-
AC-8799
sr-05000001986
SR-05000001986-1
BCP06539
Q409729
SB19515
n,n-dimethyl-2-[5-(pyrrolidin-1-ylsulfonylmethyl)-1h- indol-3-yl]-ethanamine
n,n-dimethyl-2-(5-((pyrrolidin-1-ylsulfonyl)-methyl)-1h-indol-3-yl)ethanamine
D86136
WS-02332
las 31416almotriptan
EN300-18565831
n02cc05
almotriptanum

Research Excerpts

Overview

Almotriptan is a serotonin (5-hydroxytryptamine)(1B/1D) receptor agonist (triptan) that has shown consistent efficacy in the acute treatment of migraine with excellent tolerability. Almotriptan (LAS 31416) is a new, oral, speciallized, anti-migraine agent.

ExcerptReferenceRelevance
"Almotriptan is a 5HT1B/1D receptor agonist used for the treatment of migraine pain."( LC-MS/MS method for the quantification of almotriptan in dialysates: application to rat brain and blood microdialysis study.
Ajjala, DR; Aleti, R; Benade, V; Bhyrapuneni, G; Kandikere, V; Nirogi, R; Pantangi, HR; Srikakolapu, SR; Vurimindi, H,
)
1.12
"Almotriptan is a serotonin (5-hydroxytryptamine)(1B/1D) receptor agonist (triptan) that has shown consistent efficacy in the acute treatment of migraine with excellent tolerability. "( Almotriptan for the treatment of acute migraine: a review of early intervention trials.
Allena, M; Antonaci, F; Cuzzoni, MG; De Cillis, I, 2010
)
3.25
"Almotriptan is a safe, effective, and approved agent for the acute treatment of migraine headache in adolescents."( Almotriptan for the acute treatment of adolescent migraine.
Lewis, DW, 2010
)
3.25
"Almotriptan is a novel and specific serotonin 5-HT1B/1D agonist for the acute treatment of migraine. "( Almotriptan is an effective and well-tolerated treatment for migraine pain: results of a randomized, double-blind, placebo-controlled clinical trial.
Cabarrocas, X; Dowson, AJ; Laínez, JM; Massiou, H, 2002
)
3.2
"Almotriptan is a new anti-migraine agent with nanomolar affinity for human 5-HT(1B), 5-HT(1D), and 5-HT(1F) receptors, weak affinity for 5-HT(1A) and 5-HT(7) receptors and no significant affinity for more than 20 other pharmacological receptors. "( Almotriptan, a new anti-migraine agent: a review.
Cabarrocas, X; Gras, J; Jansat, JM; Jáuregui, J; Llenas, J; Palacios, JM, 2002
)
3.2
"Almotriptan is a novel highly selective 5-hydroxytryptamine(1B/1D) agonist developed for the acute oral treatment of migraine. "( Identification of the human liver enzymes involved in the metabolism of the antimigraine agent almotriptan.
Jansat, JM; Martinez-Tobed, A; Palacios, JM; Salva, M, 2003
)
1.98
"Almotriptan is a serotonin (5-hydroxytryptamine, 5HT)(1B/1D)-receptor agonist approved for the acute treatment of migraine. "( A review of the clinical efficacy and tolerability of almotriptan in acute migraine.
Dodick, DW, 2003
)
2.01
"Almotriptan (LAS 31416) is a new, oral, specific 5-hydroxytryptamine(1B/1D) receptor agonist for the treatment of migraine. "( Pharmacokinetics and safety of oral almotriptan in healthy male volunteers.
Cabarrocas, X; Jansat, JM; McEwen, J; Salva, M, 2004
)
2.04
"Almotriptan 12.5 mg is an effective and well-tolerated alternative for patients who respond poorly to sumatriptan 50 mg. "( Almotriptan in migraine patients who respond poorly to oral sumatriptan: a double-blind, randomized trial.
Beneke, M; Diener, HC; Gebert, I; Gendolla, A, 2005
)
3.21
"Almotriptan 12.5 mg is an effective and well-tolerated alternative for patients who respond poorly to sumatriptan 50 mg. "( Almotriptan in migraine patients who respond poorly to oral sumatriptan: a double-blind, randomized trial.
Beneke, M; Diener, HC; Gebert, I; Gendolla, A,
)
3.02
"Almotriptan is a 5-HT(1B/1D) receptor agonist, or triptan, indicated for the acute treatment of migraine. "( Focus on trial endpoints of clinical relevance and the use of almotriptan for the acute treatment of migraine.
Dahlöf, CG; Mathew, N; Nappi, G; Sandrini, G, 2005
)
2.01
"Almotriptan is a second-generation triptan successfully used for the acute treatment of migraine."( Efficacy and tolerability of almotriptan versus zolmitriptan for the acute treatment of menstrual migraine.
Acuto, G; Allais, G; Benedetto, C; Bussone, G; Cabarrocas, X; Esbri, R, 2006
)
1.35
"Almotriptan is a new highly potent selective 5-HT1B/1D receptor agonist developed for the treatment of migraine, and the disposition of almotriptan in different animal species is now addressed in the current study. "( Disposition and metabolism of almotriptan in rats, dogs and monkeys.
Aubets, J; Cardenas, A; Jansat, JM; Martinez-Tobed, A; Palacios, JM; Salva, M, 2006
)
2.07
"Almotriptan is an oral selective sertonin(1B/1D) receptor agonist (triptan) with a high bioavailability and short half-life, developed for the treatment of migraine. "( Meta-analysis examining the efficacy and safety of almotriptan in the acute treatment of migraine.
Ashcroft, DM; Chen, LC, 2007
)
2.03
"Almotriptan 12.5 mg is an effective treatment for acute attacks of migraine, in particular, it has been found to be as effective as sumatriptan 100 mg and zolmitriptan 2.5 mg. "( Meta-analysis examining the efficacy and safety of almotriptan in the acute treatment of migraine.
Ashcroft, DM; Chen, LC, 2007
)
2.03
"Almotriptan is a new 5-HT(1B/1D) receptor agonist whose clinical efficacy for the treatment of migraine attacks has been demonstrated in Phase III clinical trials. "( Functional profile of almotriptan in animal models predictive of antimigraine activity.
Bou, J; Fernández, AG; Gras, J; Llenas, J; Palacios, JM, 2000
)
2.06
"Almotriptan is a new 5-HT(1B/1D) receptor agonist effective for treating acute migraine attacks with or without aura. "( Cardiovascular safety profile of almotriptan, a new indolic derivative for the treatment of migraine.
Cardelús, I; Gras, J; Llenas, J; Palacios, JM, 2000
)
2.03
"Almotriptan is a new selective serotonin 1B/1D agonist triptan migraine treatment."( Treatment satisfaction, functional status, and health-related quality of life of migraine patients treated with almotriptan or sumatriptan.
Brod, MI; Colman, SS; Gomez-Mancilla, B; Jirgens, KJ; Krishnamurthy, A; Rowland, CR, 2001
)
1.24
"Almotriptan is a new 5-HT1B/1D receptor agonist similar to sumatriptan in mode of action and therapeutic efficacy. "( Oral almotriptan in the treatment of migraine: safety and tolerability.
Dodick, DW, 2001
)
2.27
"Almotriptan is a highly specific 5-HT(1B/1D) receptor agonist, which acts selectively on blood vessels of the brain. "( Tolerability and efficacy of almotriptan in the long-term treatment of migraine.
Cabarrocas, X; Docekal, R; Falk, R; Ferrer, P; Jelencsik, J; Luria, X; Pascual, J; Prusinski, A; Segarra, X, 2001
)
2.04
"Almotriptan malate is a novel, selective serotonin(1B/D) agonist, or triptan, developed for the abortive treatment of migraine. "( Oral almotriptan vs. oral sumatriptan in the abortive treatment of migraine: a double-blind, randomized, parallel-group, optimum-dose comparison.
Gomez-Mancilla, B; Grosz, DE; Jirgens, KJ; Rowland, CR; Spierings, EL; Whaley, FS, 2001
)
2.27
"Almotriptan is a selective serotonin 5-HT(1B/1D) receptor agonist ('triptan'). "( Almotriptan: a review of its use in migraine.
Figgitt, DP; Goa, KL; Keam, SJ, 2002
)
3.2
"Almotriptan is an effective drug for the acute treatment of moderate or severe attacks of migraine in adults. "( Almotriptan: a review of its use in migraine.
Figgitt, DP; Goa, KL; Keam, SJ, 2002
)
3.2
"Almotriptan is a second-generation 5-HT(1B/1D) agonist that exhibits vascular selectivity for meningeal arteries and has demonstrated efficacy for the treatment of acute migraine in short-term controlled trials."( A long-term open-label study of oral almotriptan 12.5 mg for the treatment of acute migraine.
Mathew, NT, 2002
)
2.03
"Almotriptan malate is a recently marketed triptan for the treatment of acute migraine. "( Use of rescue medication in trials of almotriptan versus placebo in the treatment of acute migraine.
Mathew, NT, 2002
)
2.03
"Almotriptan is a selective serotonin 5-HT(1B/1D) receptor agonist ('triptan'). "( Spotlight on almotriptan in migraine.
Figgitt, DP; Goa, KL; Keam, SJ, 2002
)
2.13
"Almotriptan is an effective drug for the acute treatment of moderate or severe attacks of migraine in adults. "( Spotlight on almotriptan in migraine.
Figgitt, DP; Goa, KL; Keam, SJ, 2002
)
2.13

Effects

Almotriptan is associated with a significantly lower incidence of chest pain than sumatriptan. Almotriptan has a favourable pharmacokinetic profile that translates clinically to a rapid onset of action and consistent absorption.

Almotriptan has proven to be more efficacious and tolerable than ergotamine plus caffeine but is more expensive, thus raising the question about its cost-efficacy. The drug has a good adverse event profile and a generally similar overall tolerability profile to sumatriptan.

ExcerptReferenceRelevance
"Almotriptan has a lower acquisition cost than other triptans and possibly lower overall health care costs because of a lower frequency of cardiovascular adverse effects."( Efficacy and safety of almotriptan malate for migraine.
Balbisi, EA, 2002
)
1.35
"Almotriptan has a favourable pharmacokinetic profile that translates clinically to a rapid onset of action and consistent absorption regardless of age, sex, food intake and status of the acute migraine attack."( Clinical profile and practice experience of almotriptan.
Gendolla, A, 2004
)
1.31
"Almotriptan has a high oral bioavailability, is absorbed rapidly, has a relatively short plasma half-life and its route of elimination presents few potential problems."( Oral almotriptan: practical uses in the acute treatment of migraine.
Dowson, AJ, 2004
)
1.56
"Oral almotriptan has a rapid onset of action (significant headache relief is observed 0.5 hours after administration of a 12.5mg dose) and efficacy is sustained in most patients who respond by 2 hours."( Almotriptan: a review of its use in migraine.
Figgitt, DP; Goa, KL; Keam, SJ, 2002
)
2.21
"Almotriptan has a good adverse event profile and a generally similar overall tolerability profile to sumatriptan; of note, almotriptan is associated with a significantly lower incidence of chest pain than sumatriptan."( Almotriptan: a review of its use in migraine.
Figgitt, DP; Goa, KL; Keam, SJ, 2002
)
2.48
"Almotriptan also has an improved tolerability profile compared with sumatriptan, including a lower incidence of drug-related adverse events, a lower incidence of chest pain, and better patient satisfaction in terms of adverse events."( Health outcomes evaluations: estimating the impact of almotriptan in managed care settings.
Mayo, KW; Osterhaus, JT, 2002
)
1.28
"Oral almotriptan has a rapid onset of action (significant headache relief is observed 0.5 hours after administration of a 12.5mg dose) and efficacy is sustained in most patients who respond by 2 hours."( Spotlight on almotriptan in migraine.
Figgitt, DP; Goa, KL; Keam, SJ, 2002
)
1.14
"Almotriptan has a good adverse event profile and a generally similar overall tolerability profile to sumatriptan; of note, almotriptan is associated with a significantly lower incidence of chest pain than sumatriptan."( Spotlight on almotriptan in migraine.
Figgitt, DP; Goa, KL; Keam, SJ, 2002
)
1.41
"Almotriptan has proven to be more efficacious and tolerable than ergotamine plus caffeine but is more expensive, thus raising the question about its cost-efficacy."( [Almotriptan vs. ergotamine plus caffeine for acute migraine treatment. A cost-efficacy analysis].
Comas, A; Heras, J; Láinez, JM; Slof, J, 2009
)
2.71
"Almotriptan has a lower acquisition cost than other triptans and possibly lower overall health care costs because of a lower frequency of cardiovascular adverse effects."( Efficacy and safety of almotriptan malate for migraine.
Balbisi, EA, 2002
)
1.35
"Almotriptan has a favourable pharmacokinetic profile that translates clinically to a rapid onset of action and consistent absorption regardless of age, sex, food intake and status of the acute migraine attack."( Clinical profile and practice experience of almotriptan.
Gendolla, A, 2004
)
1.31
"Almotriptan has pharmacodynamic and pharmacokinetic profiles that make it suitable for use in this indication."( Oral almotriptan: practical uses in the acute treatment of migraine.
Dowson, AJ, 2004
)
1.56
"Almotriptan has been investigated in approximately 3,500 patients enrolled in short-term clinical trials and 1,500 patients enrolled in long-term open-label trials."( Efficacy and tolerability of almotriptan in controlled clinical trials.
Mathew, NT, 2005
)
1.34
"Almotriptan has many positive features, which include rigorously demonstrated efficacy in sumatriptan nonresponders, as early therapy and in menstrual migraine."( Almotriptan: meeting today's needs in acute migraine treatment.
Láinez, MJ, 2007
)
2.5
"Oral almotriptan has a rapid onset of action (significant headache relief is observed 0.5 hours after administration of a 12.5mg dose) and efficacy is sustained in most patients who respond by 2 hours."( Almotriptan: a review of its use in migraine.
Figgitt, DP; Goa, KL; Keam, SJ, 2002
)
2.21
"Almotriptan has a good adverse event profile and a generally similar overall tolerability profile to sumatriptan; of note, almotriptan is associated with a significantly lower incidence of chest pain than sumatriptan."( Almotriptan: a review of its use in migraine.
Figgitt, DP; Goa, KL; Keam, SJ, 2002
)
2.48
"Almotriptan has been evaluated in more than 3,500 acute migraine patients in phase 2 and 3 double-blind, randomized trials and in 1,500 patients in long-term open-label trials."( Almotriptan: a review of pharmacology, clinical efficacy, and tolerability.
Von, S, 2002
)
3.2
"Almotriptan also has an improved tolerability profile compared with sumatriptan, including a lower incidence of drug-related adverse events, a lower incidence of chest pain, and better patient satisfaction in terms of adverse events."( Health outcomes evaluations: estimating the impact of almotriptan in managed care settings.
Mayo, KW; Osterhaus, JT, 2002
)
1.28
"Almotriptan has effects on blood pressure in subjects with controlled hypertension that are consistent with those of other members of the pharmalogic class."( Cardiovascular effect of almotriptan in treated hypertensive patients.
Azie, NE; Carel, BJ; Fleishaker, JC; Francom, SF; McEnroe, JD, 2002
)
2.06
"Oral almotriptan has a rapid onset of action (significant headache relief is observed 0.5 hours after administration of a 12.5mg dose) and efficacy is sustained in most patients who respond by 2 hours."( Spotlight on almotriptan in migraine.
Figgitt, DP; Goa, KL; Keam, SJ, 2002
)
1.14
"Almotriptan has a good adverse event profile and a generally similar overall tolerability profile to sumatriptan; of note, almotriptan is associated with a significantly lower incidence of chest pain than sumatriptan."( Spotlight on almotriptan in migraine.
Figgitt, DP; Goa, KL; Keam, SJ, 2002
)
1.41

Actions

ExcerptReferenceRelevance
"Almotriptan has a lower acquisition cost than other triptans and possibly lower overall health care costs because of a lower frequency of cardiovascular adverse effects."( Efficacy and safety of almotriptan malate for migraine.
Balbisi, EA, 2002
)
1.35

Treatment

Treatment with almotriptan 12.5 mg when headache pain was mild was associated with higher rates of pain relief and pain-free at 2 and 24 hours, and sustained pain relief. Treatment within 1 hour of migraine onset resulted in significantly better clinical outcomes than placebo.

ExcerptReferenceRelevance
"Almotriptan treatment, compared to placebo, resulted in a significantly greater proportion of patients achieving 2-hour pain free (37.0% vs 23.9%, P= .010), 2-hour pain relief (72.3% vs 48.4%, P < .001) and sustained pain free (24.7% vs 16.1%, P= .040)."( Early intervention with almotriptan: results of the AEGIS trial (AXERT Early Migraine Intervention Study).
Adelman, J; Cady, RK; Finlayson, G; Greenberg, SJ; Mao, L; Mathew, NT; Smith, TR; Wright, P, 2007
)
1.37
"Almotriptan treatment efficacy outcomes for MRM vs nonMRM, respectively, were: 2-hour pain relief, 77.4% vs 68.3%; 2-hour pain free, 35.4% vs 35.9%; and sustained pain free, 22.9% vs 23.8%."( Characteristics of migraine attacks and responses to almotriptan treatment: a comparison of menstrually related and nonmenstrually related migraines.
Biondi, DM; Cady, RK; Diamond, ML; Finlayson, G; Greenberg, SJ; Mao, L; Wright, P, 2008
)
1.32
"Almotriptan treatment was well tolerated, with the most common adverse events (>2%) of nausea, dizziness, and somnolence."( Efficacy and tolerability of almotriptan in adolescents: a randomized, double-blind, placebo-controlled trial.
Cady, RK; Finlayson, G; Ishkanian, G; Lewis, DW; Linder, SL; Mathew, NT, 2008
)
1.36
"Almotriptan treatment was well tolerated in this adolescent population."( Efficacy and tolerability of almotriptan in adolescents: a randomized, double-blind, placebo-controlled trial.
Cady, RK; Finlayson, G; Ishkanian, G; Lewis, DW; Linder, SL; Mathew, NT, 2008
)
1.36
"Almotriptan, a new treatment for acute migraine attacks, may improve health outcomes while reducing expenditures on drug costs and the costs associated with unwanted adverse events. "( Health outcomes evaluations: estimating the impact of almotriptan in managed care settings.
Mayo, KW; Osterhaus, JT, 2002
)
2.01
"Treatment with almotriptan while migraine pain is still mild and within 1 h of onset provides statistically significant and clinically relevant enhancements in efficacy compared with waiting until pain has reached higher severity levels."( The 'Act when Mild' (AwM) study: a step forward in our understanding of early treatment in acute migraine.
Goadsby, PJ, 2008
)
0.69
"Treating with almotriptan 12.5 mg when headache pain was mild was associated with higher rates of pain relief and pain-free at 2 and 24 hours, and sustained pain relief and sustained pain-free, compared with treatment initiated when pain was severe."( Long-term, open-label safety study of oral almotriptan 12.5 mg for the acute treatment of migraine in adolescents.
Armstrong, RB; Berenson, F; Biondi, DM; Mao, L; Pakalnis, A; Vasconcellos, E, 2010
)
0.97
"Treatment with almotriptan 12.5 mg during migraine attacks of mild pain intensity improves 1- and 2-hour pain-free and sustained pain-free responses."( Early intervention with almotriptan improves sustained pain-free response in acute migraine.
Mathew, NT,
)
0.79
"Treatment with almotriptan within 1 hour of migraine onset resulted in significantly better clinical outcomes than placebo and tolerability similar to placebo. "( Early intervention with almotriptan: results of the AEGIS trial (AXERT Early Migraine Intervention Study).
Adelman, J; Cady, RK; Finlayson, G; Greenberg, SJ; Mao, L; Mathew, NT; Smith, TR; Wright, P, 2007
)
1
"Treatment with almotriptan was associated with a significantly greater proportion of patients achieving 2-h pain free (20.9% vs."( Crossover, double-blind clinical trial comparing almotriptan and ergotamine plus caffeine for acute migraine therapy.
Galván, J; Heras, J; Láinez, MJ; Vila, C, 2007
)
0.93
"Treatment with almotriptan while migraine pain is still mild provides statistically significant and clinically relevant enhancements in efficacy compared with treatment when pain has reached higher severity levels."( Early vs. non-early intervention in acute migraine-'Act when Mild (AwM)'. A double-blind, placebo-controlled trial of almotriptan.
Cunha, L; de Klippel, N; Diaz-Insa, S; Falques, M; Fortea, J; Geraud, G; Goadsby, PJ; Gobel, H; Ivanoff, N; Zanchin, G, 2008
)
0.89
"Treatment with almotriptan compared with placebo resulted in consistently better 24-hour MQoL scores with significant results for all 3 migraine headache attacks in the social function and feelings/concern domains."( Effect of early intervention with almotriptan vs placebo on migraine-associated functional disability: results from the AEGIS Trial.
Biondi, D; Finlayson, G; Freitag, F; Greenberg, S; Mao, L; Mathew, N; Rupnow, M; Smith, T; Wright, P, 2008
)
0.96

Toxicity

Almotriptan was safe and well tolerated in nearly all adult patients with migraine, with and without aura, enrolled in these studies. The risk of adverse events associated with al Motriptan 12.

ExcerptReferenceRelevance
" About half of all patients experienced at least one adverse event, with 87% of the events being mild or moderate in nature."( Long-term efficacy and safety of oral almotriptan: interim analysis of a 1-year open study.
Cabarrocas, X; Esbri, R; Ferrer, P; Peris, F, 2001
)
0.58
"5 mg is safe antimigraine treatment."( Long-term efficacy and safety of oral almotriptan: interim analysis of a 1-year open study.
Cabarrocas, X; Esbri, R; Ferrer, P; Peris, F, 2001
)
0.58
" Sumatriptan is generally safe and well tolerated; however, in controlled clinical trials, it has been associated with chest symptoms (pressure, warmth, and other unpleasant sensations) with an incidence of 3% to 5%."( Oral almotriptan in the treatment of migraine: safety and tolerability.
Dodick, DW, 2001
)
0.82
"In phase 2 and 3 trials comprising more than 2500 patients with migraine and 15 000 attacks, adverse events were infrequent and mild."( Oral almotriptan in the treatment of migraine: safety and tolerability.
Dodick, DW, 2001
)
0.82
"Almotriptan was safe and well tolerated in nearly all adult patients with migraine, with and without aura, enrolled in these studies."( Oral almotriptan in the treatment of migraine: safety and tolerability.
Dodick, DW, 2001
)
2.27
"The pharmacology, pharmacokinetics, clinical efficacy, adverse effects, and dosage and administration of almotriptan are reviewed."( Efficacy and safety of almotriptan malate for migraine.
Balbisi, EA, 2002
)
0.84
" Reduction in headache severity, disability and adverse effects were studied."( Almotriptan in the acute treatment of migraine in patients 11-17 years old: an open-label pilot study of efficacy and safety.
Charles, JA, 2006
)
1.78
"Systematic review and meta-analysis of randomized controlled trials (RCTs) using a random-effects model to estimate the pooled rate ratios (RRs) and 95% confidence intervals (95%CI) for the proportions of patients achieving headache relief and pain-free responses at 1 or 2 hours post-dose, sustained pain-free response at 2-24 hours post-dose, and safety outcomes (proportions of patients experiencing any adverse events, dizziness, somnolence, asthenia, and chest tightness) comparing almotriptan against placebo, other triptans, and different dosages of almotriptan."( Meta-analysis examining the efficacy and safety of almotriptan in the acute treatment of migraine.
Ashcroft, DM; Chen, LC, 2007
)
0.75
" The risk of adverse events associated with almotriptan 12."( Meta-analysis examining the efficacy and safety of almotriptan in the acute treatment of migraine.
Ashcroft, DM; Chen, LC, 2007
)
0.85
" Safety was assessed descriptively and assessments included adverse event (AE) recording, change in laboratory values, vital signs, and electrocardiogram parameters."( Long-term, open-label safety study of oral almotriptan 12.5 mg for the acute treatment of migraine in adolescents.
Armstrong, RB; Berenson, F; Biondi, DM; Mao, L; Pakalnis, A; Vasconcellos, E, 2010
)
0.62

Pharmacokinetics

The method was validated and successfully applied to a pharmacokinetic study of almotriptan in rat plasma using sumatriptan as an internal standard. Pharmacokinetic parameters of al Motriptan were determined by non-compartment analysis.

ExcerptReferenceRelevance
" Statistical comparisons of pharmacokinetic parameters and vital sign data were made by ANOVA."( Pharmacokinetic interaction between verapamil and almotriptan in healthy volunteers.
Azie, NE; Carel, BJ; Fleishaker, JC; Sisson, TA, 2000
)
0.56
"Mean almotriptan peak concentration and area under the plasma concentration-time curve were significantly higher and volume of distribution and oral clearance were significantly lower after coadministration of almotriptan and verapamil compared with administration of almotriptan alone."( Pharmacokinetic interaction between verapamil and almotriptan in healthy volunteers.
Azie, NE; Carel, BJ; Fleishaker, JC; Sisson, TA, 2000
)
1.07
" Treatment effects on pharmacokinetic parameters were assessed by analysis of variance."( Evaluation of the potential pharmacokinetic interaction between almotriptan and fluoxetine in healthy volunteers.
Azie, NE; Carel, BJ; Fleishaker, JC; Ryan, KK, 2001
)
0.55
" Treatment effects on pharmacokinetic parameters were assessed by analysis of variance (ANOVA)."( Lack of pharmacokinetic interaction between the antimigraine compound, almotriptan, and propranolol in healthy volunteers.
Azie, NE; Carel, BJ; Fleishaker, JC; Sisson, TA, 2001
)
0.54
" Mean half-life was longer (4."( Effect of MAO-A inhibition on the pharmacokinetics of almotriptan, an antimigraine agent in humans.
Azie, NE; Bell, DJ; Burke, MT; Carel, BJ; Fleishaker, JC; Jansat, JM; Ryan, KK, 2001
)
0.56
" Blood and urine samples for pharmacokinetic evaluations were taken for up to 24 hours after dosing."( Absolute bioavailability, pharmacokinetics, and urinary excretion of the novel antimigraine agent almotriptan in healthy male volunteers.
Costa, J; Fernandez, FJ; Jansat, JM; Martinez-Tobed, A; Salvà, P, 2002
)
0.53
" Pharmacokinetic parameters of almotriptan were determined by non-compartment analysis."( A comparison of the pharmacokinetics and tolerability of the anti-migraine compound almotriptan in healthy adolescents and adults.
Azie, NE; Baldwin, JR; Carel, BJ; Fleishaker, JC, 2004
)
0.83
" The elimination half-life was constant at approximately 3 h across all dose levels."( Pharmacokinetics and safety of oral almotriptan in healthy male volunteers.
Cabarrocas, X; Jansat, JM; McEwen, J; Salva, M, 2004
)
0.6
" The compound has a half-life of approximately 3 hours."( Clinical pharmacokinetics of almotriptan, a serotonin 5-HT(1B/1D) receptor agonist for the treatment of migraine.
Fleishaker, JC; McEnroe, JD, 2005
)
0.62
" 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
" The method was validated and successfully applied to a pharmacokinetic study of almotriptan in rat plasma using sumatriptan as an internal standard."( LC-ESI-MS/MS determination of in vivo metabolites of almotriptan in rat plasma, urine and feces: application to pharmacokinetics.
Gangu Naidu, Ch; Guruprasad, K; Nageswara Rao, R; Raju, B; Srinivas, R, 2012
)
0.85
"The authors take a systematic approach to discuss the pharmacodynamic and pharmacokinetic aspects of almotriptan ."( Pharmacokinetic evaluation of almotriptan for the treatment of migraines.
Casolla, B; D'Alonzo, L; Lionetto, L; Marsibilio, F; Martelletti, P; Negro, A; Simmaco, M; Vignaroli, G, 2013
)
0.89

Compound-Compound Interactions

ExcerptReferenceRelevance
"5 mg combined with either aceclofenac 100 mg or placebo."( Almotriptan and its combination with aceclofenac for migraine attacks: a study of efficacy and the influence of auto-evaluated brush allodynia.
De Klippel, N; Giurgea, S; Herroelen, L; Jacquy, J; Louis, P; Monseu, G; Schoenen, J; Vandenheede, M, 2008
)
1.79

Bioavailability

Almotriptan is an oral selective sertonin(1B/1D) receptor agonist (triptan) with a high bioavailability and short half-life, developed for the treatment of migraine. After oral administration, the bioavailability was about 70% with a tmax of 1.

ExcerptReferenceRelevance
"Almotriptan, the new selective 5-HT1B/1D agonist, has a higher oral bioavailability than any other triptan, with more than two thirds of the administered dose absorbed within the first hour both inside and outside of a migraine attack."( How does almotriptan compare with other triptans? A review of data from placebo-controlled clinical trials.
Dahlöf, CG; Dodick, D; Dowson, AJ; Pascual, J, 2002
)
2.17
" Almotriptan is well absorbed orally; its absolute bioavailability in humans is 70%."( Almotriptan, a new anti-migraine agent: a review.
Cabarrocas, X; Gras, J; Jansat, JM; Jáuregui, J; Llenas, J; Palacios, JM, 2002
)
2.67
" It has a rapid onset of action, an oral bioavailability of 70-80%, and a longer half-life than sumatriptan."( Efficacy and safety of almotriptan malate for migraine.
Balbisi, EA, 2002
)
0.63
" Almotriptan is well absorbed after oral administration and the mean absolute bioavailability is 69."( Clinical pharmacokinetics of almotriptan, a serotonin 5-HT(1B/1D) receptor agonist for the treatment of migraine.
Fleishaker, JC; McEnroe, JD, 2005
)
1.53
" Almotriptan was well absorbed in rats (69."( Disposition and metabolism of almotriptan in rats, dogs and monkeys.
Aubets, J; Cardenas, A; Jansat, JM; Martinez-Tobed, A; Palacios, JM; Salva, M, 2006
)
1.53
" In contrast, the main bioavailability criteria parameters, C(max) and AUC, which show the rate and extent of systemic absorption, were not affected by alcohol ingestion."( Ethanol does not significantly affect the bioavailability of almotriptan: an open, randomized, crossover, single-dose, phase I clinical trial in healthy volunteers.
Cabarrocas, X; Costa, J; Pavesi, M; Salva, M, 2006
)
0.58
" Human oral bioavailability is an important pharmacokinetic property, which is directly related to the amount of drug available in the systemic circulation to exert pharmacological and therapeutic effects."( Hologram QSAR model for the prediction of human oral bioavailability.
Andricopulo, AD; Moda, TL; Montanari, CA, 2007
)
0.34
"Almotriptan is an oral selective sertonin(1B/1D) receptor agonist (triptan) with a high bioavailability and short half-life, developed for the treatment of migraine."( Meta-analysis examining the efficacy and safety of almotriptan in the acute treatment of migraine.
Ashcroft, DM; Chen, LC, 2007
)
2.03
"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

Dosage Studied

Almotriptan can be coadministered with drugs that share a common hepatic metabolic path. Dose reduction is required only in the presence of severe renal or hepatic impairment. Significantly more patients taking rizatriptan achieved onset of PR within 2 hours after dosing.

ExcerptRelevanceReference
" Almotriptan can be coadministered with drugs that share a common hepatic metabolic path; in addition, dosage reduction is required only in the presence of severe renal or hepatic impairment."( Almotriptan: a review of its use in migraine.
Figgitt, DP; Goa, KL; Keam, SJ, 2002
)
2.67
" Almotriptan can be coadministered with drugs that share a common hepatic metabolic path; in addition, dosage reduction is required only in the presence of severe renal or hepatic impairment."( Spotlight on almotriptan in migraine.
Figgitt, DP; Goa, KL; Keam, SJ, 2002
)
1.59
"The pharmacology, pharmacokinetics, clinical efficacy, adverse effects, and dosage and administration of almotriptan are reviewed."( Efficacy and safety of almotriptan malate for migraine.
Balbisi, EA, 2002
)
0.84
" Similar dosage recommendations are valid for patients with hepatic impairment, based on the clearance mechanisms for almotriptan."( Clinical pharmacokinetics of almotriptan, a serotonin 5-HT(1B/1D) receptor agonist for the treatment of migraine.
Fleishaker, JC; McEnroe, JD, 2005
)
0.83
" Recurrence rates 2-24 h after dosing were 32."( Efficacy and tolerability of almotriptan versus zolmitriptan for the acute treatment of menstrual migraine.
Acuto, G; Allais, G; Benedetto, C; Bussone, G; Cabarrocas, X; Esbri, R, 2006
)
0.63
" The primary efficacy endpoint was headache pain relief 2 hours after dosing, adjusted for baseline severity, with absence of nausea, photophobia, and phonophobia 2 hours after dosing as coprimary endpoints."( Efficacy and tolerability of almotriptan in adolescents: a randomized, double-blind, placebo-controlled trial.
Cady, RK; Finlayson, G; Ishkanian, G; Lewis, DW; Linder, SL; Mathew, NT, 2008
)
0.64
" Significantly more patients taking rizatriptan achieved onset of PR within 2 hours after dosing than those taking almotriptan (88."( Migraine treatment with rizatriptan and almotriptan: a crossover study.
Bigal, M; Hu, XH; Ng-Mak, DS, 2009
)
0.83
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
non-steroidal anti-inflammatory drugAn anti-inflammatory drug that is not a steroid. In addition to anti-inflammatory actions, non-steroidal anti-inflammatory drugs have analgesic, antipyretic, and platelet-inhibitory actions. They act by blocking the synthesis of prostaglandins by inhibiting cyclooxygenase, which converts arachidonic acid to cyclic endoperoxides, precursors of prostaglandins.
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 (3)

ClassDescription
indolesAny compound containing an indole skeleton.
sulfonamideAn amide of a sulfonic acid RS(=O)2NR'2.
tertiary amineA compound formally derived from ammonia by replacing three hydrogen atoms by hydrocarbyl groups.
[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 (4)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
glp-1 receptor, partialHomo sapiens (human)Potency8.91250.01846.806014.1254AID624172
EWS/FLI fusion proteinHomo sapiens (human)Potency0.07430.001310.157742.8575AID1259253
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency14.12540.01789.637444.6684AID588834
lamin isoform A-delta10Homo sapiens (human)Potency4.46680.891312.067628.1838AID1487
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (65)

Assay IDTitleYearJournalArticle
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.
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
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).
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.
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).
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).
AID311524Oral bioavailability in human2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Hologram QSAR model for the prediction of human oral bioavailability.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
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).
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.
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).
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).
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).
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).
AID567091Drug absorption in human assessed as human intestinal absorption rate2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Prediction of drug intestinal absorption by new linear and non-linear QSPR.
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).
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.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
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.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
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).
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).
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).
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).
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.
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).
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.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS 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.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (181)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's128 (70.72)29.6817
2010's43 (23.76)24.3611
2020's10 (5.52)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 53.31

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 Index53.31 (24.57)
Research Supply Index5.51 (2.92)
Research Growth Index5.99 (4.65)
Search Engine Demand Index120.49 (26.88)
Search Engine Supply Index2.85 (0.95)

This Compound (53.31)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials59 (31.38%)5.53%
Reviews56 (29.79%)6.00%
Case Studies8 (4.26%)4.05%
Observational0 (0.00%)0.25%
Other65 (34.57%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (9)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Long-Term, Open-Label Safety Study of Oral Almotriptan Malate 12.5 mg in the Treatment of Migraine in Adolescents [NCT00257010]Phase 3447 participants (Actual)Interventional2005-12-31Completed
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
AXERT® Early miGraine Intervention Study (AEGIS): Efficacy and Safety of Almotriptan Malate (AXERT®) Versus Placebo for the Acute Treatment of Migraine Headache [NCT00210509]Phase 4378 participants (Actual)Interventional2004-11-30Completed
A Randomized, Double-blind, Placebo-controlled Study of Oral Almotriptan Malate (AXERT®) 6.25 mg, 12.5 mg, and 25 mg in the Acute Treatment of Migraine in Adolescents [NCT00210483]Phase 3866 participants (Actual)Interventional2003-07-31Completed
AXERT® 12.5mg Time vs Intensity Migraine Study (AIMS): An Open-label Multicenter Trial to Evaluate the Efficacy of Almotriptan Malate (AXERT®) 12.5 Milligram Intervention at Onset of Migraine Pain [NCT00212823]Phase 41,450 participants (Actual)Interventional2004-06-30Completed
"Evaluation of Histamine, CGRP and VIP as Biological Markers for Activation of Trigeminal and Parasympathetic Nerve Fibers in Response to Sinus Symptoms" [NCT00208065]Phase 450 participants Interventional2004-05-31Completed
Efficacy of AXERT (Almotriptan Malate) in the Acute Treatment of Migraine: A Pilot Study of the Potential Impact of Preventive Therapy With TOPAMAX (Topiramate) [NCT00210496]Phase 4406 participants (Actual)Interventional2005-06-30Completed
Evaluation of Almotriptan and Topiramate in the Detoxification and Treatment of Subjects With Medication Overuse Headache [NCT00432549]Phase 460 participants Interventional2007-01-31Recruiting
A Randomized, Parallel-Group, Single-Attack, Open-Label Study to Evaluate the Efficacy of Almotriptan and Ubrogepant for the Acute Treatment of Migraine (ATOM). [NCT05214001]Phase 4645 participants (Anticipated)Interventional2022-06-30Recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00257010 (6) [back to overview]Number of Headaches Achieving Pain Relief at 2 and 24 Hours Post-Dose
NCT00257010 (6) [back to overview]Number of Headaches With Nausea
NCT00257010 (6) [back to overview]Number of Headaches With Phonophobia
NCT00257010 (6) [back to overview]Number of Headaches With Photophobia
NCT00257010 (6) [back to overview]Number of Headaches With Vomiting
NCT00257010 (6) [back to overview]Number of Pain Free Headaches at 2 and 24 Hours Post-Dose
NCT01086358 (4) [back to overview]Favorable Response on Migraine-ACT
NCT01086358 (4) [back to overview]Lost Activity Time
NCT01086358 (4) [back to overview]Lost Workplace Productivity
NCT01086358 (4) [back to overview]Workplace Productivity and Activity Impairment Scale (WPAI).

Number of Headaches Achieving Pain Relief at 2 and 24 Hours Post-Dose

Headache pain relief is defined as a decrease in baseline pain intensity from either severe or moderate intensity to mild or no pain, without the use of supplemental pain medication and/or anti-emetic medication (including a second dose of study medication) within 2 (or 24) hours of first dose of study medication. Sustained pain relief is defined as pain relief at 2 and 24 hours without the use of supplemental pain medication and/or anti-emetic medication (including a second dose of study medication) within 24 hours. (NCT00257010)
Timeframe: 2 hours and 24 hours post-dose

InterventionNumber of headaches (Number)
Headaches Pain Relief at 2 hoursHeadaches Pain Relief at 24 hoursHeadaches Sustained Pain Relief at 24 hours
Almotriptan Malate376541823384

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Number of Headaches With Nausea

Occurrence and intensity of nausea post-dose of study medication. Nausea is a feeling of sickness characterized by gastrointestinal distress and an urge to vomit. (NCT00257010)
Timeframe: Baseline (after onset of migraine headache pain and before treatment), 2 hours and 24 hours post-dose

InterventionNumber of headaches with nausea (Number)
At baselineAt 2 hoursAt 24 hours
Almotriptan Malate32621785542

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Number of Headaches With Phonophobia

Occurrence and intensity of phonophobia post-dose of study medication. Phonophobia is an abnormal sensitivity to or intolerance of noise. (NCT00257010)
Timeframe: Baseline (after onset of migraine headache pain and before treatment), 2 hours and 24 hours post-dose

InterventionNumber of headaches with phonophobia (Number)
At baselineAt 2 hoursAt 24 hours
Almotriptan Malate57832847805

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Number of Headaches With Photophobia

Occurrence and intensity of photophobia post-dose of study medication. Photophobia is an abnormal sensitivity to or intolerance of light, especially by the eyes. (NCT00257010)
Timeframe: Baseline (after onset of migraine headache pain and before treatment), 2 hours and 24 hours post-dose

InterventionNumber of headaches with photophobia (Number)
At baselineAt 2 hoursAt 24 hours
Almotriptan Malate61643150936

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Number of Headaches With Vomiting

Occurrence and intensity of vomiting post-dose of study medication. Vomiting is an act or instance of disgorging the contents of the stomach through the mouth also called emesis. (NCT00257010)
Timeframe: Baseline (after onset of migraine headache pain and before treatment), 2 hours and 24 hours post-dose

InterventionNumber of headaches with vomiting (Number)
At baselineAt 2 hoursAt 24 hours
Almotriptan Malate357258107

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Number of Pain Free Headaches at 2 and 24 Hours Post-Dose

Headache pain free is defined as a decrease in baseline pain intensity from severe, moderate or mild to no pain, without the use of supplemental pain medication and/or anti-emetic medication (including a second dose of study medication) within 2 (or 24) hours of first dose of study medication. Sustained pain free is defined as pain free at 2 and 24 hours without the use of supplemental pain medication and/or anti-emetic medication (including a second dose of study medication) within 24 hours. (NCT00257010)
Timeframe: 2 hours and 24 hours post-dose

InterventionNumber of headaches (Number)
Headaches Pain Free at 2 hoursHeadaches Pain Free at 24 hoursHeadaches Sustained Pain Free at 24 hours
Almotriptan Malate321852363048

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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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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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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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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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