Details of the Drug

General Information of Drug (ID: DMXLVDT)

Drug Name

Lasmiditan

Synonyms

COL-144; LY-573144; Migraine therapy, CoLucid

Indication

Disease Entry	ICD 11	Status	REF
Migraine	8A80	Approved	[1]

Drug Type

Small molecular drug

Structure

3D MOL

2D MOL

#Ro5 Violations (Lipinski): 0

Molecular Weight (mw)

377.4

Topological Polar Surface Area (xlogp)

2.8

Rotatable Bond Count (rotbonds)

4

Hydrogen Bond Donor Count (hbonddonor)

1

Hydrogen Bond Acceptor Count (hbondacc)

7

ADMET Property

Absorption AUC: The area under the plot of plasma concentration (AUC) of drug is 1892 +/- 746.0 mcgh/L [2]
Absorption Cmax: The maximum plasma concentration (Cmax) of drug is 322.8 +/- 122.0 mcg/L [2]
Absorption Tmax: The time to maximum plasma concentration (Tmax) is 1.8 h [2]
Bioavailability: The bioavailability of drug is 40% [2]
Elimination: Of the small amount of drug found in the urine post-dose, approximately 66% is comprised of lasmiditan's S-M8 metabolite [2]
Half-life: The concentration or amount of drug in body reduced by one-half in 5.7 hours [2]
Metabolism: The drug is metabolized via the hepatic [2]

Chemical Identifiers

Formula: C19H18F3N3O2
IUPAC Name: 2,4,6-trifluoro-N-[6-(1-methylpiperidine-4-carbonyl)pyridin-2-yl]benzamide
Canonical SMILES: CN1CCC(CC1)C(=O)C2=NC(=CC=C2)NC(=O)C3=C(C=C(C=C3F)F)F
InChI: 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)
InChIKey: XEDHVZKDSYZQBF-UHFFFAOYSA-N

Cross-matching ID

PubChem CID: 11610526
CAS Number: 439239-90-4
DrugBank ID: DB11732
TTD ID: D01NQM
ACDINA ID: D01198

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
5-HT 1F receptor (HTR1F)	TT0MI3F	5HT1F_HUMAN	Agonist	[1]

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Molecular Interaction Atlas (MIA)

MIA Detail

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Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Same Disease as Lasmiditan

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Disease	REF
Ubrogepant	DM749I3	Moderate	Decreased clearance of Lasmiditan due to the transporter inhibition by Ubrogepant.	Migraine [8A80]	[9]
Rimegepant	DMHOAUG	Moderate	Decreased clearance of Lasmiditan due to the transporter inhibition by Rimegepant.	Migraine [8A80]	[10]
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Coadministration of a Drug Treating the Disease Different from Lasmiditan (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Oliceridine	DM6MDCF	Moderate	Additive CNS depression effects by the combination of Lasmiditan and Oliceridine.	Acute pain [MG31]	[11]
ABT-492	DMJFD2I	Moderate	Decreased clearance of Lasmiditan due to the transporter inhibition by ABT-492.	Bacterial infection [1A00-1C4Z]	[11]
Esketamine	DMVU687	Moderate	Additive CNS depression effects by the combination of Lasmiditan and Esketamine.	Depression [6A70-6A7Z]	[11]
Deutetrabenazine	DMUPFLI	Moderate	Additive CNS depression effects by the combination of Lasmiditan and Deutetrabenazine.	Dystonic disorder [8A02]	[11]
Ingrezza	DMVPLNC	Moderate	Additive CNS depression effects by the combination of Lasmiditan and Ingrezza.	Dystonic disorder [8A02]	[11]
Eslicarbazepine	DMZREFQ	Moderate	Additive CNS depression effects by the combination of Lasmiditan and Eslicarbazepine.	Epilepsy/seizure [8A61-8A6Z]	[11]
Ripretinib	DM958QB	Moderate	Decreased clearance of Lasmiditan due to the transporter inhibition by Ripretinib.	Gastrointestinal stromal tumour [2B5B]	[12]
Belladonna	DM2RBWK	Moderate	Additive CNS depression effects by the combination of Lasmiditan and Belladonna.	Infectious gastroenteritis/colitis [1A40]	[11]
Berotralstat	DMWA2DZ	Major	Decreased clearance of Lasmiditan due to the transporter inhibition by Berotralstat.	Innate/adaptive immunodeficiency [4A00]	[13]
Remimazolam	DMLVSYX	Moderate	Additive CNS depression effects by the combination of Lasmiditan and Remimazolam.	Labour/delivery anaesthesia complication [JB0C]	[11]
Allopregnanolone	DMNLHAC	Moderate	Additive CNS depression effects by the combination of Lasmiditan and Allopregnanolone.	Mental/behavioural/neurodevelopmental disorder [6E20-6E8Z]	[11]
Siponimod	DM2R86O	Major	Increased risk of bradycardia by the combination of Lasmiditan and Siponimod.	Multiple sclerosis [8A40]	[12]
Rucaparib	DM9PVX8	Moderate	Decreased clearance of Lasmiditan due to the transporter inhibition by Rucaparib.	Ovarian cancer [2C73]	[11]
MK-4827	DMLYGH4	Moderate	Decreased clearance of Lasmiditan due to the transporter inhibition by MK-4827.	Ovarian cancer [2C73]	[11]
Relugolix	DMK7IWL	Major	Decreased clearance of Lasmiditan due to the transporter inhibition by Relugolix.	Prostate cancer [2C82]	[14]
Lusutrombopag	DMH6IKO	Moderate	Decreased clearance of Lasmiditan due to the transporter inhibition by Lusutrombopag.	Thrombocytopenia [3B64]	[11]
Betrixaban	DM2C4RF	Moderate	Decreased clearance of Lasmiditan due to the transporter inhibition by Betrixaban.	Venous thromboembolism [BD72]	[11]
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⏷ Show the Full List of 17 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
Sodium lauryl sulfate	E00464	3423265	Emulsifying agent; Modified-release agent; Penetration agent; Solubilizing agent; Surfactant; lubricant
Carmellose sodium	E00625	Not Available	Disintegrant
Ferric oxide black	E00522	16211978	Colorant
Magnesium stearate	E00208	11177	lubricant
Polyethylene glycol 4000	E00654	Not Available	Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Polyvinyl alcohol	E00666	Not Available	Coating agent; Emulsion stabilizing agent; Film/Membrane-forming agent
Talc	E00520	16211421	Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide	E00322	26042	Coating agent; Colorant; Opacifying agent
Haematite red	E00236	14833	Colorant
Cellulose microcrystalline	E00698	Not Available	Adsorbent; Suspending agent; Diluent
Pregelatinized starch	E00674	Not Available	Binding agent; Diluent; Disintegrant
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⏷ Show the Full List of 11 Pharmaceutical Excipients of This Drug

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Lasmiditan 100 mg tablet	100 mg	Tablet	Oral
Lasmiditan 50 mg tablet	50 mg	Tablet	Oral
Lasmiditan 200 mg tablet	200 mg	Tablet	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

References

1	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
2	FDA Approved Drugs: Reyvow
3	Cloning and characterization of the guinea pig 5-HT1F receptor subtype: a comparison of the pharmacological profile to the human species homolog. Neuropharmacology. 1997 Apr-May;36(4-5):569-76.
4	Selective seratonin 1F (5-HT(1F)) receptor agonist LY334370 for acute migraine: a randomised controlled trial. Lancet. 2001 Oct 13;358(9289):1230-4.
5	Cloning of another human serotonin receptor (5-HT1F): a fifth 5-HT1 receptor subtype coupled to the inhibition of adenylate cyclase. Proc Natl Acad Sci U S A. 1993 Jan 15;90(2):408-12.
6	SB-216641 and BRL-15572--compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors. Naunyn Schmiedebergs Arch Pharmacol. 1997 Sep;356(3):312-20.
7	Discovery of 5-arylsulfonamido-3-(pyrrolidin-2-ylmethyl)-1H-indole derivatives as potent, selective 5-HT6 receptor agonists and antagonists. J Med Chem. 2005 Jan 27;48(2):353-6.
8	Isolation of a mouse "5HT1E-like" serotonin receptor expressed predominantly in hippocampus. J Biol Chem. 1992 Oct 5;267(28):19761-4.
9	Product Information. Ubrelvy (ubrogepant). Allergan Inc, Irvine, CA.
10	Product Information. Nurtec ODT (rimegepant). Biohaven Pharmaceuticals, New Haven, CT.
11	Product Information. Reyvow (lasmiditan). Lilly, Eli and Company, Indianapolis, IN.
12	Cerner Multum, Inc. "Australian Product Information.".
13	Product Information. Orladeyo (berotralstat). BioCryst Pharmaceuticals Inc, Durham, NC.
14	Product Information. Orgovyx (relugolix). Myovant Sciences, Inc., Brisbane, CA.