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lasmiditan 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antimigraine (5-HT1 receptor agonists) | 5351 | 439239-90-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Reyvow (lasmiditan) is a serotonin (5-HT) 1F receptor agonist for oral administration, bindinding with high affinity to the 5-HT1F receptor. Lasmiditan presumably exerts its therapeutic effects in the treatment of migraine through agonist effects at the 5-HT1F receptor; however, the precise mechanism is unknown.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.10 | g | O |
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2B,ALK,AXL,BRAF,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK1,KIT,MAP3K21,MAP3K7,MAPK7,MARK4,MET,NTRK2,PDK2,PDK4,PIK3CB,PRKCD,PRKDC,SIK2,SIK3,STK33,TEK,TTK | 34 | |||
| kinase-selectivity-class | CAMK2D,CDK1,CDK9,DYRK1B,MAPK7,MARK4,PDK4,SIK2,SIK3 | 9 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Nov. 10, 2019 | FDA | ELI LILLY AND CO | |
| Jan. 20, 2022 | PMDA | ELI LILLY JAPAN K.K. | |
| Aug. 17, 2022 | EMA | Eli Lilly Nederland B.V. |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Dizziness | 220.05 | 63.36 | 102 | 645 | 589182 | 90038518 |
| Feeling abnormal | 162.48 | 63.36 | 58 | 689 | 167177 | 90460523 |
| Sedation | 150.65 | 63.36 | 41 | 706 | 48130 | 90579570 |
| Somnolence | 104.81 | 63.36 | 45 | 702 | 209039 | 90418661 |
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Dizziness | 135.64 | 63.81 | 56 | 271 | 698137 | 109890835 |
| Sedation | 72.33 | 63.81 | 20 | 307 | 69663 | 110519309 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N02CC08 | NERVOUS SYSTEM ANALGESICS ANTIMIGRAINE PREPARATIONS Selective serotonin (5HT1) agonists |
| MeSH PA | D017366 | Serotonin Receptor Agonists |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018490 | Serotonin Agents |
Related Drugs by ATC class:
N02CC Selective serotonin (5HT1) agonists 8 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Migraine | indication | 37796009 | DOID:6364 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 11.03 | acidic |
| pKa2 | 9.43 | Basic |
| pKa3 | 0.49 | Basic |
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| EQ 100MG BASE | REYVOW | ELI LILLY AND CO | N211280 | Jan. 31, 2020 | DISCN | TABLET | ORAL | 7423050 | Feb. 17, 2028 | ACUTE TREATMENT OF MIGRAINE |
| EQ 200MG BASE | REYVOW | ELI LILLY AND CO | N211280 | Dec. 18, 2020 | DISCN | TABLET | ORAL | 7423050 | Feb. 17, 2028 | ACUTE TREATMENT OF MIGRAINE |
| EQ 50MG BASE | REYVOW | ELI LILLY AND CO | N211280 | Jan. 31, 2020 | DISCN | TABLET | ORAL | 7423050 | Feb. 17, 2028 | ACUTE TREATMENT OF MIGRAINE |
| EQ 100MG BASE | REYVOW | ELI LILLY AND CO | N211280 | Jan. 31, 2020 | DISCN | TABLET | ORAL | 12257246 | July 7, 2030 | ACUTE TREATMENT OF MIGRAINE WITH OR WITHOUT AURA IN ADULTS |
| EQ 200MG BASE | REYVOW | ELI LILLY AND CO | N211280 | Dec. 18, 2020 | DISCN | TABLET | ORAL | 12257246 | July 7, 2030 | ACUTE TREATMENT OF MIGRAINE WITH OR WITHOUT AURA IN ADULTS |
| EQ 50MG BASE | REYVOW | ELI LILLY AND CO | N211280 | Jan. 31, 2020 | DISCN | TABLET | ORAL | 12257246 | July 7, 2030 | ACUTE TREATMENT OF MIGRAINE WITH OR WITHOUT AURA IN ADULTS |
| EQ 100MG BASE | REYVOW | ELI LILLY AND CO | N211280 | Jan. 31, 2020 | DISCN | TABLET | ORAL | 11053214 | Dec. 5, 2037 | ACUTE TREATMENT OF MIGRAINE |
| EQ 200MG BASE | REYVOW | ELI LILLY AND CO | N211280 | Dec. 18, 2020 | DISCN | TABLET | ORAL | 11053214 | Dec. 5, 2037 | ACUTE TREATMENT OF MIGRAINE |
| EQ 50MG BASE | REYVOW | ELI LILLY AND CO | N211280 | Jan. 31, 2020 | DISCN | TABLET | ORAL | 11053214 | Dec. 5, 2037 | ACUTE TREATMENT OF MIGRAINE |
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 1F | GPCR | AGONIST | Ki | 8.65 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| 5-hydroxytryptamine receptor 7 | GPCR | Ki | 5.27 | CHEMBL | |||||
| D(1B) dopamine receptor | GPCR | Ki | 6.60 | CHEMBL | |||||
| Muscarinic acetylcholine receptor M5 | GPCR | Ki | 6.20 | CHEMBL | |||||
| Sigma non-opioid intracellular receptor 1 | Membrane receptor | Ki | 5.50 | CHEMBL | |||||
| Kappa-type opioid receptor | GPCR | Ki | 6.45 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 1E | GPCR | Ki | 6.90 | CHEMBL | |||||
| Transmembrane protein 97 | Enzyme | Ki | 6.74 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 1D | GPCR | Ki | 6.06 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 760I9WM792 | UNII |
| 439239-92-6 | SECONDARY_CAS_RN |
| 4039151 | VANDF |
| C4519199 | UMLSCUI |
| CHEBI:755069 | CHEBI |
| CHEMBL3039520 | ChEMBL_ID |
| 11610526 | PUBCHEM_CID |
| DB11732 | DRUGBANK_ID |
| CHEMBL3039526 | ChEMBL_ID |
| D10338 | KEGG_DRUG |
| 9176 | INN_ID |
| C554777 | MESH_SUPPLEMENTAL_RECORD_UI |
| 3928 | IUPHAR_LIGAND_ID |
| 823027003 | SNOMEDCT_US |
| 823028008 | SNOMEDCT_US |
| 05X | PDB_CHEM_ID |
| 325205 | MMSL |
| d09395 | MMSL |
| 018168 | NDDF |
| 018169 | NDDF |
| 2256930 | RXNORM |
| 760I9WM792 | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Reyvow | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0002-4312 | TABLET | 50 mg | ORAL | NDA | 32 sections |
| Reyvow | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0002-4491 | TABLET | 100 mg | ORAL | NDA | 32 sections |