U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ACHIRAL
Molecular Formula C19H18F3N3O2
Molecular Weight 377.361
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of LASMIDITAN

SMILES

CN1CCC(CC1)C(=O)c2cccc(n2)N=C(c3c(cc(cc3F)F)F)O

InChI

InChIKey=XEDHVZKDSYZQBF-UHFFFAOYSA-N
InChI=1S/C19H18F3N3O2/c1-25-7-5-11(6-8-25)18(26)15-3-2-4-16(23-15)24-19(27)17-13(21)9-12(20)10-14(17)22/h2-4,9-11H,5-8H2,1H3,(H,23,24,27)

HIDE SMILES / InChI

Molecular Formula C19H18F3N3O2
Molecular Weight 377.361
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

LASMIDITAN is a serotonin (5-HT) receptor agonist without vasoconstrictor activity, which selectively binds to the 5-HT(1F) receptor subtype. It is under development for the treatment of migraine.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
2.10000000000000009 nM [Ki]
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
322.8 ng/mL
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LASMIDITAN serum
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
394.7 ng/mL
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LASMIDITAN serum
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
526.15 ng/mL
400 mg single, oral
dose: 400 mg
route of administration: oral
experiment type: single
co-administered:
LASMIDITAN unknown
Homo sapiens
population: healthy
age:
sex:
food status:
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
1892 ng × h/mL
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LASMIDITAN serum
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
2244 ng × h/mL
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LASMIDITAN serum
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
3189.08 ng*h/mL
400 mg single, oral
dose: 400 mg
route of administration: oral
experiment type: single
co-administered:
LASMIDITAN unknown
Homo sapiens
population: healthy
age:
sex:
food status:
Doses

Doses

DosePopulationAdverse events​
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 18-81 years
Health Status: unhealthy
Age Group: 18-81 years
Sex: M+F
Sources:
Other AEs: Dizziness, Fatigue...
Other AEs:
Dizziness (15%)
Fatigue (5%)
Paresthesia (7%)
Sedation (6%)
Nausea and vomiting (4%)
Muscle weakness (1%)
Sources:
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy, 18-81 years
Health Status: unhealthy
Age Group: 18-81 years
Sex: M+F
Sources:
Other AEs: Dizziness, Fatigue...
Other AEs:
Dizziness (17%)
Fatigue (6%)
Paresthesia (9%)
Sedation (7%)
Nausea and vomiting (4%)
Muscle weakness (2%)
Sources:
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Sources:
unhealthy, 18-81 years
Health Status: unhealthy
Age Group: 18-81 years
Sex: M+F
Sources:
Other AEs: Dizziness, Fatigue...
Other AEs:
Dizziness (9%)
Fatigue (4%)
Paresthesia (3%)
Sedation (6%)
Nausea and vomiting (3%)
Muscle weakness (1%)
Sources:
120 mg 5 times / day single, oral
Highest studied dose
Dose: 120 mg, 5 times / day
Route: oral
Route: single
Dose: 120 mg, 5 times / day
Sources:
unhealthy, adults
400 mg 1 times / day single, oral
Highest studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: single
Dose: 400 mg, 1 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Disc. AE: Dizziness, Light headedness...
AEs leading to
discontinuation/dose reduction:
Dizziness (2.8%)
Light headedness (2.8%)
Somnolence (1.6%)
Sedation (1.6%)
Asthenia (0.7%)
Fatigue (0.7%)
Malaise (0.7%)
Weakness (0.7%)
Paresthesia (0.8%)
Hypoaesthesia (0.8%)
Nausea (0.7%)
Vomiting (0.7%)
Confusion (2.1%)
Delirium (2.1%)
Mental status changes (2.1%)
Disorientation (2.1%)
Sources:
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Disc. AE: Dizziness, Light headedness...
Other AEs: Confusion, Delirium...
AEs leading to
discontinuation/dose reduction:
Dizziness (4.2%)
Light headedness (4.2%)
Somnolence (1.2%)
Sedation (1.2%)
Asthenia (2.5%)
Fatigue (2.5%)
Malaise (2.5%)
Weakness (2.5%)
Paresthesia (1.8%)
Hypoaesthesia (1.8%)
Nausea (1.5%)
Vomiting (1.5%)
Confusion (1.4%)
Delirium (1.4%)
Mental status changes (1.4%)
Disorientation (1.4%)
Other AEs:
Confusion (1.4%)
Delirium (1.4%)
Mental status changes (1.4%)
Disorientation (1.4%)
Sources:
AEs

AEs

AESignificanceDosePopulation
Muscle weakness 1%
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 18-81 years
Health Status: unhealthy
Age Group: 18-81 years
Sex: M+F
Sources:
Dizziness 15%
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 18-81 years
Health Status: unhealthy
Age Group: 18-81 years
Sex: M+F
Sources:
Nausea and vomiting 4%
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 18-81 years
Health Status: unhealthy
Age Group: 18-81 years
Sex: M+F
Sources:
Fatigue 5%
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 18-81 years
Health Status: unhealthy
Age Group: 18-81 years
Sex: M+F
Sources:
Sedation 6%
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 18-81 years
Health Status: unhealthy
Age Group: 18-81 years
Sex: M+F
Sources:
Paresthesia 7%
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, 18-81 years
Health Status: unhealthy
Age Group: 18-81 years
Sex: M+F
Sources:
Dizziness 17%
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy, 18-81 years
Health Status: unhealthy
Age Group: 18-81 years
Sex: M+F
Sources:
Muscle weakness 2%
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy, 18-81 years
Health Status: unhealthy
Age Group: 18-81 years
Sex: M+F
Sources:
Nausea and vomiting 4%
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy, 18-81 years
Health Status: unhealthy
Age Group: 18-81 years
Sex: M+F
Sources:
Fatigue 6%
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy, 18-81 years
Health Status: unhealthy
Age Group: 18-81 years
Sex: M+F
Sources:
Sedation 7%
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy, 18-81 years
Health Status: unhealthy
Age Group: 18-81 years
Sex: M+F
Sources:
Paresthesia 9%
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy, 18-81 years
Health Status: unhealthy
Age Group: 18-81 years
Sex: M+F
Sources:
Muscle weakness 1%
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Sources:
unhealthy, 18-81 years
Health Status: unhealthy
Age Group: 18-81 years
Sex: M+F
Sources:
Nausea and vomiting 3%
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Sources:
unhealthy, 18-81 years
Health Status: unhealthy
Age Group: 18-81 years
Sex: M+F
Sources:
Paresthesia 3%
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Sources:
unhealthy, 18-81 years
Health Status: unhealthy
Age Group: 18-81 years
Sex: M+F
Sources:
Fatigue 4%
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Sources:
unhealthy, 18-81 years
Health Status: unhealthy
Age Group: 18-81 years
Sex: M+F
Sources:
Sedation 6%
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Sources:
unhealthy, 18-81 years
Health Status: unhealthy
Age Group: 18-81 years
Sex: M+F
Sources:
Dizziness 9%
50 mg 1 times / day steady, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Sources:
unhealthy, 18-81 years
Health Status: unhealthy
Age Group: 18-81 years
Sex: M+F
Sources:
Asthenia 0.7%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Fatigue 0.7%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Malaise 0.7%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Nausea 0.7%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Vomiting 0.7%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Weakness 0.7%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Hypoaesthesia 0.8%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Paresthesia 0.8%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Sedation 1.6%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Somnolence 1.6%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Confusion 2.1%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Delirium 2.1%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Disorientation 2.1%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Mental status changes 2.1%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Dizziness 2.8%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Light headedness 2.8%
Disc. AE
100 mg 1 times / day steady, oral
Recommended
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Sedation 1.2%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Somnolence 1.2%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Confusion 1.4%
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Delirium 1.4%
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Disorientation 1.4%
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Mental status changes 1.4%
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Confusion 1.4%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Delirium 1.4%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Disorientation 1.4%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Mental status changes 1.4%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Nausea 1.5%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Vomiting 1.5%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Hypoaesthesia 1.8%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Paresthesia 1.8%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Asthenia 2.5%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Fatigue 2.5%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Malaise 2.5%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Weakness 2.5%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Dizziness 4.2%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
Light headedness 4.2%
Disc. AE
200 mg 1 times / day steady, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
low
low
low
low
low
low
low
no (co-administration study)
Comment: "when administered with sumatriptan, no change in sumatriptan PK was observed; '""low potential of interactions"""
Page: 8, 18
no
no
no
no
no
no
no (co-administration study)
Comment: administered with caffeine, daily dosing of lasmiditan did not alter PK of caffeine
Page: 8
no
no (co-administration study)
Comment: administered with caffeine, daily dosing of lasmiditan did not alter PK of caffeine
Page: 8
no
no (co-administration study)
Comment: administered with tolbutamide, daily dosing of lasmiditan did not alter the PK of tolbutamide.
Page: 8
no
no (co-administration study)
Comment: administered with tolbutamide, daily dosing of lasmiditan did not alter the PK of tolbutamide.
Page: 8
no
no (co-administration study)
Comment: administered with midazolam, daily dosing of lasmiditan did not alter PK of midazolam
Page: 8
no
no (co-administration study)
Comment: administered with midazolam, daily dosing of lasmiditan did not alter PK of midazolam
Page: 8
yes [IC50 85 uM]
yes [Ki 20.7 uM]
yes
yes
yes
Drug as victimTox targets

Tox targets

PubMed

PubMed

TitleDatePubMed
Acute treatment of migraine with the selective 5-HT1F receptor agonist lasmiditan--a randomised proof-of-concept trial.
2010 Oct
Preclinical pharmacological profile of the selective 5-HT1F receptor agonist lasmiditan.
2010 Oct
Patents

Sample Use Guides

Lasmiditan in vitro binding studies show a Ki value of 2.21 nM at the 5-HT(1F) serotonin receptor, compared with Ki values of 1043 nM and 1357 nM at the 5-HT(1B) and 5-HT(1D) receptors, respectively. Lasmiditan did not contract rabbit saphenous vein rings, a surrogate assay for human coronary artery constriction, at concentrations up to 100 uM.
Substance Class Chemical
Created
by admin
on Fri Jun 25 20:35:04 UTC 2021
Edited
by admin
on Fri Jun 25 20:35:04 UTC 2021
Record UNII
760I9WM792
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
LASMIDITAN
INN   USAN   WHO-DD  
INN   USAN  
Official Name English
LASMIDITAN [WHO-DD]
Common Name English
2,4,6-TRIFLUORO-N-(6-((1-METHYLPIPERIDINE-4-YL)CARBONYL)PYRIDIN-2-YL)BENZAMIDE
Systematic Name English
COL-144
Code English
LASMIDITAN [INN]
Common Name English
LASMIDITAN [USAN]
Common Name English
Classification Tree Code System Code
DEA NO. 2790
Created by admin on Fri Jun 25 20:35:04 UTC 2021 , Edited by admin on Fri Jun 25 20:35:04 UTC 2021
Code System Code Type Description
FDA UNII
760I9WM792
Created by admin on Fri Jun 25 20:35:04 UTC 2021 , Edited by admin on Fri Jun 25 20:35:04 UTC 2021
PRIMARY
INN
9176
Created by admin on Fri Jun 25 20:35:04 UTC 2021 , Edited by admin on Fri Jun 25 20:35:04 UTC 2021
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WIKIPEDIA
LASMIDITAN
Created by admin on Fri Jun 25 20:35:04 UTC 2021 , Edited by admin on Fri Jun 25 20:35:04 UTC 2021
PRIMARY
PUBCHEM
11610526
Created by admin on Fri Jun 25 20:35:04 UTC 2021 , Edited by admin on Fri Jun 25 20:35:04 UTC 2021
PRIMARY
ChEMBL
CHEMBL3039520
Created by admin on Fri Jun 25 20:35:04 UTC 2021 , Edited by admin on Fri Jun 25 20:35:04 UTC 2021
PRIMARY
EPA CompTox
439239-90-4
Created by admin on Fri Jun 25 20:35:04 UTC 2021 , Edited by admin on Fri Jun 25 20:35:04 UTC 2021
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DRUG BANK
DB11732
Created by admin on Fri Jun 25 20:35:04 UTC 2021 , Edited by admin on Fri Jun 25 20:35:04 UTC 2021
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DRUG CENTRAL
5351
Created by admin on Fri Jun 25 20:35:04 UTC 2021 , Edited by admin on Fri Jun 25 20:35:04 UTC 2021
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NCI_THESAURUS
C166996
Created by admin on Fri Jun 25 20:35:04 UTC 2021 , Edited by admin on Fri Jun 25 20:35:04 UTC 2021
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LACTMED
Lasmiditan
Created by admin on Fri Jun 25 20:35:04 UTC 2021 , Edited by admin on Fri Jun 25 20:35:04 UTC 2021
PRIMARY
RXCUI
2256930
Created by admin on Fri Jun 25 20:35:04 UTC 2021 , Edited by admin on Fri Jun 25 20:35:04 UTC 2021
PRIMARY
CAS
439239-90-4
Created by admin on Fri Jun 25 20:35:04 UTC 2021 , Edited by admin on Fri Jun 25 20:35:04 UTC 2021
PRIMARY
Related Record Type Details
TRANSPORTER -> SUBSTRATE
In vitro studies showed that lasmiditan is a substrate of P-gp. However, lasmiditan is a BCS Class I drug and is unlikely to be affected by P-gp inhibitors.
EXCRETED UNCHANGED
AMOUNT EXCRETED
URINE
TRANSPORTER -> INHIBITOR
Lasmiditan is an in-vitro inhibitor of P-gp and BCRP.
TRANSPORTER -> INHIBITOR
Lasmiditan is an in-vitro inhibitor of P-gp and BCRP.
BINDER->LIGAND
The human plasma protein binding of lasmiditan is approximately 55% to 60% and independent of concentration between 15 and 500 ng/mL.
BINDING
SALT/SOLVATE -> PARENT
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Volume of Distribution PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC
Tmax PHARMACOKINETIC ORAL ADMINISTRATION