Details
Stereochemistry | ACHIRAL |
Molecular Formula | C19H18F3N3O2 |
Molecular Weight | 377.3603 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CN1CCC(CC1)C(=O)C2=CC=CC(NC(=O)C3=C(F)C=C(F)C=C3F)=N2
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)
Molecular Formula | C19H18F3N3O2 |
Molecular Weight | 377.3603 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
CNS Activity
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL1805 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20855361 |
2.1 nM [Ki] |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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 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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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 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
Dose | Population | Adverse 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 n = 1265 Health Status: unhealthy Condition: migraine Age Group: 18-81 years Sex: M+F Population Size: 1265 Sources: |
Other AEs: Dizziness, Fatigue... Other AEs: Dizziness (15%) Sources: Fatigue (5%) Paresthesia (7%) Sedation (6%) Nausea and vomiting (4%) Muscle weakness (1%) |
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 n = 1258 Health Status: unhealthy Condition: migraine Age Group: 18-81 years Sex: M+F Population Size: 1258 Sources: |
Other AEs: Dizziness, Fatigue... Other AEs: Dizziness (17%) Sources: Fatigue (6%) Paresthesia (9%) Sedation (7%) Nausea and vomiting (4%) Muscle weakness (2%) |
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 n = 654 Health Status: unhealthy Condition: migraine Age Group: 18-81 years Sex: M+F Population Size: 654 Sources: |
Other AEs: Dizziness, Fatigue... Other AEs: Dizziness (9%) Sources: Fatigue (4%) Paresthesia (3%) Sedation (6%) Nausea and vomiting (3%) Muscle weakness (1%) |
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 n = 1 Health Status: unhealthy Condition: migraine Age Group: adults Population Size: 1 Sources: |
|
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 n = 70 Health Status: unhealthy Condition: migraine Age Group: adults Sex: M+F Population Size: 70 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 n = 991 Health Status: unhealthy Condition: migraine Age Group: adults Sex: M+F Population Size: 991 Sources: |
Disc. AE: Dizziness, Light headedness... AEs leading to discontinuation/dose reduction: Dizziness (2.8%) Sources: 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%) |
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 n = 1039 Health Status: unhealthy Condition: migraine Age Group: adults Sex: M+F Population Size: 1039 Sources: |
Disc. AE: Dizziness, Light headedness... Other AEs: Confusion, Delirium... AEs leading to discontinuation/dose reduction: Dizziness (4.2%) Other AEs: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%) Confusion (1.4%) Sources: Delirium (1.4%) Mental status changes (1.4%) Disorientation (1.4%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
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 n = 1265 Health Status: unhealthy Condition: migraine Age Group: 18-81 years Sex: M+F Population Size: 1265 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 n = 1265 Health Status: unhealthy Condition: migraine Age Group: 18-81 years Sex: M+F Population Size: 1265 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 n = 1265 Health Status: unhealthy Condition: migraine Age Group: 18-81 years Sex: M+F Population Size: 1265 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 n = 1265 Health Status: unhealthy Condition: migraine Age Group: 18-81 years Sex: M+F Population Size: 1265 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 n = 1265 Health Status: unhealthy Condition: migraine Age Group: 18-81 years Sex: M+F Population Size: 1265 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 n = 1265 Health Status: unhealthy Condition: migraine Age Group: 18-81 years Sex: M+F Population Size: 1265 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 n = 1258 Health Status: unhealthy Condition: migraine Age Group: 18-81 years Sex: M+F Population Size: 1258 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 n = 1258 Health Status: unhealthy Condition: migraine Age Group: 18-81 years Sex: M+F Population Size: 1258 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 n = 1258 Health Status: unhealthy Condition: migraine Age Group: 18-81 years Sex: M+F Population Size: 1258 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 n = 1258 Health Status: unhealthy Condition: migraine Age Group: 18-81 years Sex: M+F Population Size: 1258 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 n = 1258 Health Status: unhealthy Condition: migraine Age Group: 18-81 years Sex: M+F Population Size: 1258 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 n = 1258 Health Status: unhealthy Condition: migraine Age Group: 18-81 years Sex: M+F Population Size: 1258 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 n = 654 Health Status: unhealthy Condition: migraine Age Group: 18-81 years Sex: M+F Population Size: 654 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 n = 654 Health Status: unhealthy Condition: migraine Age Group: 18-81 years Sex: M+F Population Size: 654 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 n = 654 Health Status: unhealthy Condition: migraine Age Group: 18-81 years Sex: M+F Population Size: 654 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 n = 654 Health Status: unhealthy Condition: migraine Age Group: 18-81 years Sex: M+F Population Size: 654 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 n = 654 Health Status: unhealthy Condition: migraine Age Group: 18-81 years Sex: M+F Population Size: 654 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 n = 654 Health Status: unhealthy Condition: migraine Age Group: 18-81 years Sex: M+F Population Size: 654 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 n = 991 Health Status: unhealthy Condition: migraine Age Group: adults Sex: M+F Population Size: 991 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 n = 991 Health Status: unhealthy Condition: migraine Age Group: adults Sex: M+F Population Size: 991 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 n = 991 Health Status: unhealthy Condition: migraine Age Group: adults Sex: M+F Population Size: 991 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 n = 991 Health Status: unhealthy Condition: migraine Age Group: adults Sex: M+F Population Size: 991 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 n = 991 Health Status: unhealthy Condition: migraine Age Group: adults Sex: M+F Population Size: 991 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 n = 991 Health Status: unhealthy Condition: migraine Age Group: adults Sex: M+F Population Size: 991 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 n = 991 Health Status: unhealthy Condition: migraine Age Group: adults Sex: M+F Population Size: 991 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 n = 991 Health Status: unhealthy Condition: migraine Age Group: adults Sex: M+F Population Size: 991 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 n = 991 Health Status: unhealthy Condition: migraine Age Group: adults Sex: M+F Population Size: 991 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 n = 991 Health Status: unhealthy Condition: migraine Age Group: adults Sex: M+F Population Size: 991 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 n = 991 Health Status: unhealthy Condition: migraine Age Group: adults Sex: M+F Population Size: 991 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 n = 991 Health Status: unhealthy Condition: migraine Age Group: adults Sex: M+F Population Size: 991 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 n = 991 Health Status: unhealthy Condition: migraine Age Group: adults Sex: M+F Population Size: 991 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 n = 991 Health Status: unhealthy Condition: migraine Age Group: adults Sex: M+F Population Size: 991 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 n = 991 Health Status: unhealthy Condition: migraine Age Group: adults Sex: M+F Population Size: 991 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 n = 991 Health Status: unhealthy Condition: migraine Age Group: adults Sex: M+F Population Size: 991 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 n = 1039 Health Status: unhealthy Condition: migraine Age Group: adults Sex: M+F Population Size: 1039 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 n = 1039 Health Status: unhealthy Condition: migraine Age Group: adults Sex: M+F Population Size: 1039 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 n = 1039 Health Status: unhealthy Condition: migraine Age Group: adults Sex: M+F Population Size: 1039 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 n = 1039 Health Status: unhealthy Condition: migraine Age Group: adults Sex: M+F Population Size: 1039 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 n = 1039 Health Status: unhealthy Condition: migraine Age Group: adults Sex: M+F Population Size: 1039 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 n = 1039 Health Status: unhealthy Condition: migraine Age Group: adults Sex: M+F Population Size: 1039 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 n = 1039 Health Status: unhealthy Condition: migraine Age Group: adults Sex: M+F Population Size: 1039 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 n = 1039 Health Status: unhealthy Condition: migraine Age Group: adults Sex: M+F Population Size: 1039 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 n = 1039 Health Status: unhealthy Condition: migraine Age Group: adults Sex: M+F Population Size: 1039 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 n = 1039 Health Status: unhealthy Condition: migraine Age Group: adults Sex: M+F Population Size: 1039 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 n = 1039 Health Status: unhealthy Condition: migraine Age Group: adults Sex: M+F Population Size: 1039 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 n = 1039 Health Status: unhealthy Condition: migraine Age Group: adults Sex: M+F Population Size: 1039 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 n = 1039 Health Status: unhealthy Condition: migraine Age Group: adults Sex: M+F Population Size: 1039 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 n = 1039 Health Status: unhealthy Condition: migraine Age Group: adults Sex: M+F Population Size: 1039 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 n = 1039 Health Status: unhealthy Condition: migraine Age Group: adults Sex: M+F Population Size: 1039 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 n = 1039 Health Status: unhealthy Condition: migraine Age Group: adults Sex: M+F Population Size: 1039 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 n = 1039 Health Status: unhealthy Condition: migraine Age Group: adults Sex: M+F Population Size: 1039 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 n = 1039 Health Status: unhealthy Condition: migraine Age Group: adults Sex: M+F Population Size: 1039 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 n = 1039 Health Status: unhealthy Condition: migraine Age Group: adults Sex: M+F Population Size: 1039 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 n = 1039 Health Status: unhealthy Condition: migraine Age Group: adults Sex: M+F Population Size: 1039 Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000ClinPharmR.pdf#page=18 Page: 18.0 |
low | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000ClinPharmR.pdf#page=18 Page: 18.0 |
low | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000ClinPharmR.pdf#page=18 Page: 18.0 |
low | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000ClinPharmR.pdf#page=18 Page: 18.0 |
low | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000ClinPharmR.pdf#page=18 Page: 18.0 |
low | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000ClinPharmR.pdf#page=18 Page: 18.0 |
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 |
|||
Page: 8.0 |
no | |||
Page: 8.0 |
no | |||
Page: 8.0 |
no | |||
Page: 8.0 |
no | |||
Page: 8.0 |
no | |||
Page: 8.0 |
no | no (co-administration study) Comment: administered with caffeine, daily dosing of lasmiditan did not alter PK of caffeine Page: 8.0 |
||
Page: 8.0 |
no | no (co-administration study) Comment: administered with caffeine, daily dosing of lasmiditan did not alter PK of caffeine Page: 8.0 |
||
Page: 8.0 |
no | no (co-administration study) Comment: administered with tolbutamide, daily dosing of lasmiditan did not alter the PK of tolbutamide. Page: 8.0 |
||
Page: 8.0 |
no | no (co-administration study) Comment: administered with tolbutamide, daily dosing of lasmiditan did not alter the PK of tolbutamide. Page: 8.0 |
||
Page: 8.0 |
no | no (co-administration study) Comment: administered with midazolam, daily dosing of lasmiditan did not alter PK of midazolam Page: 8.0 |
||
Page: 8.0 |
no | no (co-administration study) Comment: administered with midazolam, daily dosing of lasmiditan did not alter PK of midazolam Page: 8.0 |
||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000ClinPharmR.pdf#page=37 Page: 37.0 |
yes [IC50 85 uM] | |||
yes [Ki 20.7 uM] | ||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000ClinPharmR.pdf#page=16 Page: 16.0 |
yes | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000ClinPharmR.pdf#page=18 Page: 18.0 |
yes | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000ClinPharmR.pdf#page=18 Page: 18.0 |
yes |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: 8.0 |
no | |||
Page: 8.0 |
no | |||
Page: 8.0 |
no | |||
Page: 8.0 |
no | |||
Page: 8.0 |
no | |||
Page: 8.0 |
no | |||
Page: 8.0 |
no | |||
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Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
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Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211280Orig1s000ClinPharmR.pdf#page=18 Page: 18.0 |
PubMed
Title | Date | PubMed |
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Acute treatment of migraine with the selective 5-HT1F receptor agonist lasmiditan--a randomised proof-of-concept trial. | 2010 Oct |
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Preclinical pharmacological profile of the selective 5-HT1F receptor agonist lasmiditan. | 2010 Oct |
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Molecule of the month. Lasmiditan hydrochloride. | 2010 Sep |
Patents
Sample Use Guides
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/20855361
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
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Related Record | Type | Details | ||
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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.
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EXCRETED UNCHANGED |
AMOUNT EXCRETED
URINE
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TRANSPORTER -> INHIBITOR |
Lasmiditan is an in-vitro inhibitor of P-gp and BCRP.
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TRANSPORTER -> INHIBITOR |
Lasmiditan is an in-vitro inhibitor of P-gp and BCRP.
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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
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SALT/SOLVATE -> PARENT | |||
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SALT/SOLVATE -> PARENT |
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Volume of Distribution | PHARMACOKINETIC |
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Biological Half-life | PHARMACOKINETIC |
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Tmax | PHARMACOKINETIC |
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ORAL ADMINISTRATION |
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