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

Description

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.

CNS Activity

Originator

Approval Year

2019
98
Targets

Targets

Primary TargetPharmacologyConditionPotency
Agonist
2456
 2.10000000000000009 nM [Ki]
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
322.8 ng/mL
REVIEW
https://pubmed.ncbi.nlm.nih.gov/29563831/
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
REVIEW
https://pubmed.ncbi.nlm.nih.gov/29563831/
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
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT03465436
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
REVIEW
https://pubmed.ncbi.nlm.nih.gov/29563831/
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
REVIEW
https://pubmed.ncbi.nlm.nih.gov/29563831/
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
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT03465436
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
unhealthy, 18-81 years
Health Status: unhealthy
Age Group: 18-81 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
Other AEs: Dizziness, Fatigue...
Other AEs:
Dizziness (15%)
Fatigue (5%)
Paresthesia (7%)
Sedation (6%)
Nausea and vomiting (4%)
Muscle weakness (1%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
unhealthy, 18-81 years
Health Status: unhealthy
Age Group: 18-81 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
Other AEs: Dizziness, Fatigue...
Other AEs:
Dizziness (17%)
Fatigue (6%)
Paresthesia (9%)
Sedation (7%)
Nausea and vomiting (4%)
Muscle weakness (2%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
unhealthy, 18-81 years
Health Status: unhealthy
Age Group: 18-81 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
Other AEs: Dizziness, Fatigue...
Other AEs:
Dizziness (9%)
Fatigue (4%)
Paresthesia (3%)
Sedation (6%)
Nausea and vomiting (3%)
Muscle weakness (1%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
unhealthy, 18-81 years
Health Status: unhealthy
Age Group: 18-81 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
unhealthy, 18-81 years
Health Status: unhealthy
Age Group: 18-81 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
unhealthy, 18-81 years
Health Status: unhealthy
Age Group: 18-81 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
unhealthy, 18-81 years
Health Status: unhealthy
Age Group: 18-81 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
unhealthy, 18-81 years
Health Status: unhealthy
Age Group: 18-81 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
unhealthy, 18-81 years
Health Status: unhealthy
Age Group: 18-81 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
unhealthy, 18-81 years
Health Status: unhealthy
Age Group: 18-81 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
unhealthy, 18-81 years
Health Status: unhealthy
Age Group: 18-81 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
unhealthy, 18-81 years
Health Status: unhealthy
Age Group: 18-81 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
unhealthy, 18-81 years
Health Status: unhealthy
Age Group: 18-81 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
unhealthy, 18-81 years
Health Status: unhealthy
Age Group: 18-81 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
unhealthy, 18-81 years
Health Status: unhealthy
Age Group: 18-81 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
unhealthy, 18-81 years
Health Status: unhealthy
Age Group: 18-81 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
unhealthy, 18-81 years
Health Status: unhealthy
Age Group: 18-81 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
unhealthy, 18-81 years
Health Status: unhealthy
Age Group: 18-81 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
unhealthy, 18-81 years
Health Status: unhealthy
Age Group: 18-81 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
unhealthy, 18-81 years
Health Status: unhealthy
Age Group: 18-81 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
unhealthy, 18-81 years
Health Status: unhealthy
Age Group: 18-81 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211280s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
unhealthy, adults
Health Status: unhealthy
Age Group: adults
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000MedR.pdf
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1470
inhibitor
1318

substrate
865

inducer
343
inhibitor
1421

substrate
1038
inhibitor
1360

OverviewOther

Other InhibitorOther SubstrateOther Inducer
P-gp
1089

BCRP
574

OCT1
473

CYP1A2
1268

CYP2A6
594

CYP2B6
679

CYP2C8
761

CYP2C19
1215

CYP2E1
761

CYP3A
175

FMO3
2

MATE1
290

MATE2
258

OCT2
582

OAT1
547

OAT3
570

OATP1B1
698

OATP1B3
613
P-gp
1223

CYP1A2
892

CYP2A6
452

CYP2B6
575

CYP2C8
586

CYP2C19
830

CYP2E1
567
CYP3A
102

CYP1A2
618
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
FMO3
2
 low
OAT1
551
 low
OAT3
572
 low
OATP1B1
713
 low
OATP1B3
622
 low
OCT2
583
 low
OCT1
488
 low
no (co-administration study)
Comment: "when administered with sumatriptan, no change in sumatriptan PK was observed; '""low potential of interactions"""
Page: 8, 18
CYP2A6
625
 no
CYP2B6
845
 no
CYP2C19
1277
 no
CYP2C8
810
 no
CYP2E1
841
 no
CYP1A2
1406
 no
no (co-administration study)
Comment: administered with caffeine, daily dosing of lasmiditan did not alter PK of caffeine
Page: 8
CYP1A2
1406
 no
no (co-administration study)
Comment: administered with caffeine, daily dosing of lasmiditan did not alter PK of caffeine
Page: 8
CYP2C9
1362
 no
no (co-administration study)
Comment: administered with tolbutamide, daily dosing of lasmiditan did not alter the PK of tolbutamide.
Page: 8
CYP2C9
1362
 no
no (co-administration study)
Comment: administered with tolbutamide, daily dosing of lasmiditan did not alter the PK of tolbutamide.
Page: 8
CYP3A
244
 no
no (co-administration study)
Comment: administered with midazolam, daily dosing of lasmiditan did not alter PK of midazolam
Page: 8
CYP3A
244
 no
no (co-administration study)
Comment: administered with midazolam, daily dosing of lasmiditan did not alter PK of midazolam
Page: 8
P-gp
1255
 yes [IC50 85 uM]
CYP2D6
1455
 yes [Ki 20.7 uM]
BCRP
639
 yes
MATE1
291
 yes
MATE2
258
 yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
CYP1A2
892
 no
CYP2A6
452
 no
CYP2B6
575
 no
CYP2C19
830
 no
CYP2C8
586
 no
CYP2C9
865
 no
CYP2D6
1038
 no
CYP2E1
567
 no
CYP3A4
1470
 no
P-gp
1223
 yes
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
1392
Sourcing

Sourcing

Vendor/AggregatorIDURL
001 Chemical
DY113432
1PlusChem LLC
1P00DBN7
1PlusChem LLC
1P00ECWX
A2B Chem
AG20819
AChemBlock
L22337
AK Scientific
6063AB
APExBIO
B1058
AbovChem LLC
HY-14861
AbovChem LLC
HY-14861A
Angene
AGN-PC-00CM98
AstaTech
42565
BLDpharm
BD00800999
BLDpharm
BD244364
BOC Sciences
439239-90-4
BlocksMatrix Scientific
90054
ChemShuttle
100654
Compound Cloud
11610526
Compound Cloud
46927777
Excenen
EX-A1300
Excenen
EX-A1654
Hairui
LAXF015
Hangzhou APIChem Technology
AC-30917
KeyOrganics
AS-35247
Lab Network
LN00188248
Lan Pharmatech
LQT-B13347
MolPort
MolPort-023-219-124
MolPort
MolPort-046-417-014
Molcore
MC113432
Molnova
M18554
MuseChem
I007621
Selleck Chemicals
S6489
ShangHai Biochempartner
BCP000574
ShangHai Biochempartner
BCP04734
ShangHai Biochempartner
BCP17274
TargetMol
T3704
ZINC
ZINC000003818355
http://zinc15.docking.org/substances/ZINC000003818355
eMolecules
43639862
eMolecules
89941840
mcule
MCULE-5457095827
mcule
MCULE-5623674277
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

Patents

07423050
2
08044207
2
08697876
2
08748459
2
20050222206
2

Sample Use Guides

In Vitro Use Guide
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
PRIMARY
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
PRIMARY
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
PRIMARY
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
PRIMARY
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
PRIMARY
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
MULTIDRUG RESISTANCE PROTEIN 1
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.
Structure of LASMIDITAN
EXCRETED UNCHANGED
AMOUNT EXCRETED
URINE
ATP-BINDING CASSETTE SUB-FAMILY G MEMBER 2
TRANSPORTER -> INHIBITOR
Lasmiditan is an in-vitro inhibitor of P-gp and BCRP.
MULTIDRUG RESISTANCE PROTEIN 1
TRANSPORTER -> INHIBITOR
Lasmiditan is an in-vitro inhibitor of P-gp and BCRP.
PLASMA PROTEIN FRACTION (HUMAN)
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
Structure of LASMIDITAN SUCCINATE
SALT/SOLVATE -> PARENT
Related Record Type Details
Structure of LASMIDITAN
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Volume of Distribution PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC
Tmax PHARMACOKINETIC ORAL ADMINISTRATION

NIH
NCATS
PRIVACY ACT
ACCESSIBILITY
DISCLAIMER
For language access assistance, contact the NCATS Public Information Officer
National Center for Advancing Translational Sciences (NCATS),
6701 Democracy Boulevard, Bethesda MD 20892-4874 • 301-594-8966