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Identification
NameCevimeline
Accession NumberDB00185  (APRD00224)
TypeSmall Molecule
GroupsApproved
DescriptionCevimeline is a parasympathomimetic and muscarinic agonist, with particular effect on M3 receptors. It is indicated by the Food and Drug Administration for the treatment of dry mouth associated with Sjögren's syndrome. [Wikipedia]
Structure
Thumb
Synonyms
2-Methyspiro(1,3-oxathiolane-5,3)quinuclidine
Cevimelina
Cevimelinum
Sni 2011
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Cevimelinecapsule30 mg/1oralRanbaxy Pharmaceuticals Inc.2012-10-07Not applicableUs
Cevimeline Hydrochloridecapsule30 mg/1oralAmerican Health Packaging2015-03-31Not applicableUs
Evoxaccapsule30 mg/1oralSTAT Rx USA LLC2000-01-11Not applicableUs
Evoxaccapsule30 mg/1oralDaiichi Sankyo Pharma Development2000-01-12Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Cevimeline Hydrochloridecapsule30 mg/1oralRoxane Laboratories, Inc.2013-07-08Not applicableUs
Cevimeline Hydrochloridecapsule30 mg/1oralPACK Pharmaceuticals, LLC2014-06-17Not applicableUs
Cevimeline Hydrochloridecapsule30 mg/1oralApotex Corp.2012-10-08Not applicableUs
Cevimeline Hydrochloridecapsule30 mg/1oralAvera Mc Kennan Hospital2015-10-30Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
SaligrenNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Cevimeline hydrochloride
Thumb
  • InChI Key: WUTYZMFRCNBCHQ-PSASIEDQSA-N
  • Monoisotopic Mass: 199.103084861
  • Average Mass: 199.313
DBSALT000805
Categories
UNIIK9V0CDQ56E
CAS number107233-08-9
WeightAverage: 199.313
Monoisotopic: 199.103084861
Chemical FormulaC10H17NOS
InChI KeyInChIKey=WUTYZMFRCNBCHQ-LHIURRSHSA-N
InChI
InChI=1S/C10H17NOS/c1-8-12-10(7-13-8)6-11-4-2-9(10)3-5-11/h8-9H,2-7H2,1H3/t8?,10-/m1/s1
IUPAC Name
(2R)-5'-methyl-4-azaspiro[bicyclo[2.2.2]octane-2,2'-[1,4]oxathiolane]
SMILES
CC1O[C@@]2(CS1)CN1CCC2CC1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as azaspirodecane derivatives. These are organic compounds containing a spirodecane moiety with at least one nitrogen atom.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassAzaspirodecane derivatives
Sub ClassNot Available
Direct ParentAzaspirodecane derivatives
Alternative Parents
Substituents
  • Azaspirodecane
  • Quinuclidine
  • Piperidine
  • Oxathiolane
  • Monothioacetal
  • Tertiary aliphatic amine
  • Tertiary amine
  • Oxacycle
  • Azacycle
  • Thioether
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Amine
  • Aliphatic heteropolycyclic compound
Molecular FrameworkAliphatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor the treatment of symptoms of dry mouth in patients with Sjögren's Syndrome.
PharmacodynamicsCevimeline is a cholinergic agonist which binds to muscarinic receptors. Muscarinic agonists in sufficient dosage can increase secretion of exocrine glands, such as salivary and sweat glands and increase tone of the smooth muscle in the gastrointestinal and urinary tracts.
Mechanism of actionMuscarinic agonists such as cevimeline bind and activate the muscarinic M1 and M3 receptors. The M1 receptors are common in secretory glands (exocrine glands such as salivary and sweat glands), and their activation results in an increase in secretion from the secretory glands. The M3 receptors are found on smooth muscles and in many glands which help to stimulate secretion in salivary glands, and their activation generally results in smooth muscle contraction and increased glandular secretions. Therefore, as saliva excretion is increased, the symptoms of dry mouth are relieved.
Related Articles
AbsorptionRapidly absorbed with peak concentration after 1.5 to 2 hours
Volume of distribution
  • 6 L/kg
Protein binding< 20%
Metabolism

Primarily hepatic, isozymes CYP2D6 and CYP3A4 are responsible for the metabolism of cevimeline. Approximately 44.5% of the drug is converted to cis and trans-sulfoxide, 22.3% to glucuronic acid conjugate, and 4% to N-oxide of cevimeline. Approximately 8% of the trans-sulfoxide metabolite is then converted into the corresponding glucuronic acid conjugate.

SubstrateEnzymesProduct
Cevimeline
cevimeline trans-sulfoxideDetails
Cevimeline
cevimeline cis-sulfoxideDetails
Cevimeline
cevimeline cis-sulfoxidationDetails
Cevimeline
cevimeline N-oxideDetails
Cevimeline
Not Available
Glucuronic acidDetails
Route of eliminationAfter 24 hours, 84% of a 30 mg dose of cevimeline was excreted in urine.
Half life5 ± 1 hours
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9899
Blood Brain Barrier+0.9823
Caco-2 permeable+0.6465
P-glycoprotein substrateSubstrate0.7063
P-glycoprotein inhibitor INon-inhibitor0.6941
P-glycoprotein inhibitor IINon-inhibitor0.9434
Renal organic cation transporterInhibitor0.6934
CYP450 2C9 substrateNon-substrate0.8083
CYP450 2D6 substrateSubstrate0.8918
CYP450 3A4 substrateSubstrate0.5719
CYP450 1A2 substrateNon-inhibitor0.8634
CYP450 2C9 inhibitorNon-inhibitor0.9047
CYP450 2D6 inhibitorNon-inhibitor0.6012
CYP450 2C19 inhibitorNon-inhibitor0.7312
CYP450 3A4 inhibitorNon-inhibitor0.9154
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.7686
Ames testNon AMES toxic0.7969
CarcinogenicityNon-carcinogens0.9054
BiodegradationNot ready biodegradable0.9942
Rat acute toxicity2.7785 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.6383
hERG inhibition (predictor II)Non-inhibitor0.8469
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Daiichi sankyo co ltd
Packagers
Dosage forms
FormRouteStrength
Capsuleoral30 mg/1
Prices
Unit descriptionCostUnit
Evoxac 30 mg capsule2.69USD capsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US4855290 No1992-08-302009-08-30Us
US5340821 No1993-07-072013-07-07Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point201-203 °C (HCl salt)Not Available
water solubilityVery solubleNot Available
logP1.3Not Available
Predicted Properties
PropertyValueSource
Water Solubility2.41 mg/mLALOGPS
logP1.46ALOGPS
logP1ChemAxon
logS-1.9ALOGPS
pKa (Strongest Basic)8.59ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area12.47 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity55.92 m3·mol-1ChemAxon
Polarizability21.89 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesN07AX03
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (34.3 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
1,10-PhenanthrolineThe risk or severity of adverse effects can be increased when 1,10-Phenanthroline is combined with Cevimeline.
AbirateroneThe metabolism of Cevimeline can be decreased when combined with Abiraterone.
AcebutololThe risk or severity of adverse effects can be increased when Acebutolol is combined with Cevimeline.
AlprenololThe risk or severity of adverse effects can be increased when Alprenolol is combined with Cevimeline.
AmbenoniumThe risk or severity of adverse effects can be increased when Ambenonium is combined with Cevimeline.
AmiodaroneThe metabolism of Cevimeline can be decreased when combined with Amiodarone.
AprepitantThe serum concentration of Cevimeline can be increased when it is combined with Aprepitant.
ArotinololThe risk or severity of adverse effects can be increased when Arotinolol is combined with Cevimeline.
ArtemetherThe metabolism of Cevimeline can be decreased when combined with Artemether.
AtazanavirThe metabolism of Cevimeline can be decreased when combined with Atazanavir.
AtenololThe risk or severity of adverse effects can be increased when Atenolol is combined with Cevimeline.
AtomoxetineThe metabolism of Cevimeline can be decreased when combined with Atomoxetine.
BefunololThe risk or severity of adverse effects can be increased when Befunolol is combined with Cevimeline.
BetaxololThe risk or severity of adverse effects can be increased when Betaxolol is combined with Cevimeline.
BevantololThe risk or severity of adverse effects can be increased when Bevantolol is combined with Cevimeline.
BexaroteneThe serum concentration of Cevimeline can be decreased when it is combined with Bexarotene.
BisoprololThe risk or severity of adverse effects can be increased when Bisoprolol is combined with Cevimeline.
BoceprevirThe metabolism of Cevimeline can be decreased when combined with Boceprevir.
BopindololThe risk or severity of adverse effects can be increased when Bopindolol is combined with Cevimeline.
BortezomibThe metabolism of Cevimeline can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Cevimeline can be decreased when it is combined with Bosentan.
BufuralolThe risk or severity of adverse effects can be increased when Bufuralol is combined with Cevimeline.
BupranololThe risk or severity of adverse effects can be increased when Bupranolol is combined with Cevimeline.
BupropionThe metabolism of Cevimeline can be decreased when combined with Bupropion.
CarbamazepineThe metabolism of Cevimeline can be increased when combined with Carbamazepine.
CarteololThe risk or severity of adverse effects can be increased when Carteolol is combined with Cevimeline.
CarvedilolThe risk or severity of adverse effects can be increased when Carvedilol is combined with Cevimeline.
CelecoxibThe metabolism of Cevimeline can be decreased when combined with Celecoxib.
CeliprololThe risk or severity of adverse effects can be increased when Celiprolol is combined with Cevimeline.
CeritinibThe serum concentration of Cevimeline can be increased when it is combined with Ceritinib.
ChloroquineThe metabolism of Cevimeline can be decreased when combined with Chloroquine.
ChlorpromazineThe metabolism of Cevimeline can be decreased when combined with Chlorpromazine.
CholecalciferolThe metabolism of Cevimeline can be decreased when combined with Cholecalciferol.
CimetidineThe metabolism of Cevimeline can be decreased when combined with Cimetidine.
CimetropiumCevimeline may decrease the anticholinergic activities of Cimetropium.
CinacalcetThe metabolism of Cevimeline can be decreased when combined with Cinacalcet.
CitalopramThe metabolism of Cevimeline can be decreased when combined with Citalopram.
ClarithromycinThe metabolism of Cevimeline can be decreased when combined with Clarithromycin.
ClemastineThe metabolism of Cevimeline can be decreased when combined with Clemastine.
ClobazamThe metabolism of Cevimeline can be decreased when combined with Clobazam.
ClomipramineThe metabolism of Cevimeline can be decreased when combined with Clomipramine.
ClotrimazoleThe metabolism of Cevimeline can be decreased when combined with Clotrimazole.
ClozapineThe metabolism of Cevimeline can be decreased when combined with Clozapine.
CobicistatThe serum concentration of Cevimeline can be increased when it is combined with Cobicistat.
CocaineThe metabolism of Cevimeline can be decreased when combined with Cocaine.
ConivaptanThe serum concentration of Cevimeline can be increased when it is combined with Conivaptan.
CoumaphosThe risk or severity of adverse effects can be increased when Coumaphos is combined with Cevimeline.
CrizotinibThe metabolism of Cevimeline can be decreased when combined with Crizotinib.
CyclosporineThe metabolism of Cevimeline can be decreased when combined with Cyclosporine.
DabrafenibThe serum concentration of Cevimeline can be decreased when it is combined with Dabrafenib.
DarifenacinThe metabolism of Cevimeline can be decreased when combined with Darifenacin.
DarunavirThe serum concentration of Cevimeline can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Cevimeline can be increased when it is combined with Dasatinib.
DecamethoniumThe risk or severity of adverse effects can be increased when Decamethonium is combined with Cevimeline.
DeferasiroxThe serum concentration of Cevimeline can be decreased when it is combined with Deferasirox.
DelavirdineThe metabolism of Cevimeline can be decreased when combined with Delavirdine.
DemecariumThe risk or severity of adverse effects can be increased when Demecarium is combined with Cevimeline.
DesipramineThe metabolism of Cevimeline can be decreased when combined with Desipramine.
DexamethasoneThe serum concentration of Cevimeline can be decreased when it is combined with Dexamethasone.
DichlorvosThe risk or severity of adverse effects can be increased when Dichlorvos is combined with Cevimeline.
DihydroergotamineThe metabolism of Cevimeline can be decreased when combined with Dihydroergotamine.
DiltiazemThe metabolism of Cevimeline can be decreased when combined with Diltiazem.
DiphenhydramineThe metabolism of Cevimeline can be decreased when combined with Diphenhydramine.
DonepezilThe risk or severity of adverse effects can be increased when Donepezil is combined with Cevimeline.
DoxycyclineThe metabolism of Cevimeline can be decreased when combined with Doxycycline.
DronedaroneThe metabolism of Cevimeline can be decreased when combined with Dronedarone.
DuloxetineThe metabolism of Cevimeline can be decreased when combined with Duloxetine.
EchothiophateThe risk or severity of adverse effects can be increased when Echothiophate is combined with Cevimeline.
EdrophoniumThe risk or severity of adverse effects can be increased when Edrophonium is combined with Cevimeline.
EfavirenzThe serum concentration of Cevimeline can be decreased when it is combined with Efavirenz.
EliglustatThe metabolism of Cevimeline can be decreased when combined with Eliglustat.
EnzalutamideThe serum concentration of Cevimeline can be decreased when it is combined with Enzalutamide.
ErythromycinThe metabolism of Cevimeline can be decreased when combined with Erythromycin.
Eslicarbazepine acetateThe serum concentration of Cevimeline can be decreased when it is combined with Eslicarbazepine acetate.
EsmololThe risk or severity of adverse effects can be increased when Esmolol is combined with Cevimeline.
EtravirineThe serum concentration of Cevimeline can be decreased when it is combined with Etravirine.
FenthionThe risk or severity of adverse effects can be increased when Fenthion is combined with Cevimeline.
FluconazoleThe metabolism of Cevimeline can be decreased when combined with Fluconazole.
FluoxetineThe metabolism of Cevimeline can be decreased when combined with Fluoxetine.
FluvoxamineThe metabolism of Cevimeline can be decreased when combined with Fluvoxamine.
FosamprenavirThe metabolism of Cevimeline can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Cevimeline can be increased when it is combined with Fosaprepitant.
FosphenytoinThe metabolism of Cevimeline can be increased when combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Cevimeline can be increased when it is combined with Fusidic Acid.
GalantamineThe risk or severity of adverse effects can be increased when Galantamine is combined with Cevimeline.
Gallamine TriethiodideThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Cevimeline.
Ginkgo bilobaThe risk or severity of adverse effects can be increased when Ginkgo biloba is combined with Cevimeline.
HaloperidolThe metabolism of Cevimeline can be decreased when combined with Haloperidol.
Huperzine AThe risk or severity of adverse effects can be increased when Huperzine A is combined with Cevimeline.
IdelalisibThe serum concentration of Cevimeline can be increased when it is combined with Idelalisib.
ImatinibThe metabolism of Cevimeline can be decreased when combined with Imatinib.
ImipramineThe metabolism of Cevimeline can be decreased when combined with Imipramine.
IndenololThe risk or severity of adverse effects can be increased when Indenolol is combined with Cevimeline.
IndinavirThe metabolism of Cevimeline can be decreased when combined with Indinavir.
IsavuconazoniumThe metabolism of Cevimeline can be decreased when combined with Isavuconazonium.
IsoflurophateThe risk or severity of adverse effects can be increased when Isoflurophate is combined with Cevimeline.
IsoniazidThe metabolism of Cevimeline can be decreased when combined with Isoniazid.
IsradipineThe metabolism of Cevimeline can be decreased when combined with Isradipine.
ItraconazoleThe metabolism of Cevimeline can be decreased when combined with Itraconazole.
IvacaftorThe serum concentration of Cevimeline can be increased when it is combined with Ivacaftor.
KetoconazoleThe metabolism of Cevimeline can be decreased when combined with Ketoconazole.
LabetalolThe risk or severity of adverse effects can be increased when Labetalol is combined with Cevimeline.
LevobunololThe risk or severity of adverse effects can be increased when Levobunolol is combined with Cevimeline.
LopinavirThe metabolism of Cevimeline can be decreased when combined with Lopinavir.
LorcaserinThe metabolism of Cevimeline can be decreased when combined with Lorcaserin.
LovastatinThe metabolism of Cevimeline can be decreased when combined with Lovastatin.
LuliconazoleThe serum concentration of Cevimeline can be increased when it is combined with Luliconazole.
LumefantrineThe metabolism of Cevimeline can be decreased when combined with Lumefantrine.
MalathionThe risk or severity of adverse effects can be increased when Malathion is combined with Cevimeline.
MefloquineThe risk or severity of adverse effects can be increased when Mefloquine is combined with Cevimeline.
MemantineThe risk or severity of adverse effects can be increased when Memantine is combined with Cevimeline.
MethadoneThe metabolism of Cevimeline can be decreased when combined with Methadone.
MethotrimeprazineThe metabolism of Cevimeline can be decreased when combined with Methotrimeprazine.
MetipranololThe risk or severity of adverse effects can be increased when Metipranolol is combined with Cevimeline.
MetoprololThe risk or severity of adverse effects can be increased when Metoprolol is combined with Cevimeline.
MifepristoneThe metabolism of Cevimeline can be decreased when combined with Mifepristone.
MinaprineThe risk or severity of adverse effects can be increased when Minaprine is combined with Cevimeline.
MirabegronThe metabolism of Cevimeline can be decreased when combined with Mirabegron.
MitotaneThe serum concentration of Cevimeline can be decreased when it is combined with Mitotane.
ModafinilThe serum concentration of Cevimeline can be decreased when it is combined with Modafinil.
NadololThe risk or severity of adverse effects can be increased when Nadolol is combined with Cevimeline.
NafcillinThe serum concentration of Cevimeline can be decreased when it is combined with Nafcillin.
NefazodoneThe metabolism of Cevimeline can be decreased when combined with Nefazodone.
NelfinavirThe metabolism of Cevimeline can be decreased when combined with Nelfinavir.
NeostigmineThe risk or severity of adverse effects can be increased when Neostigmine is combined with Cevimeline.
NetupitantThe serum concentration of Cevimeline can be increased when it is combined with Netupitant.
NevirapineThe metabolism of Cevimeline can be decreased when combined with Nevirapine.
NicardipineThe metabolism of Cevimeline can be decreased when combined with Nicardipine.
NilotinibThe metabolism of Cevimeline can be decreased when combined with Nilotinib.
OlaparibThe metabolism of Cevimeline can be decreased when combined with Olaparib.
OsimertinibThe serum concentration of Cevimeline can be increased when it is combined with Osimertinib.
OxprenololThe risk or severity of adverse effects can be increased when Oxprenolol is combined with Cevimeline.
PalbociclibThe serum concentration of Cevimeline can be increased when it is combined with Palbociclib.
PanobinostatThe metabolism of Cevimeline can be decreased when combined with Panobinostat.
ParoxetineThe metabolism of Cevimeline can be decreased when combined with Paroxetine.
Peginterferon alfa-2bThe serum concentration of Cevimeline can be decreased when it is combined with Peginterferon alfa-2b.
PenbutololThe risk or severity of adverse effects can be increased when Penbutolol is combined with Cevimeline.
PentobarbitalThe metabolism of Cevimeline can be increased when combined with Pentobarbital.
PhenobarbitalThe metabolism of Cevimeline can be increased when combined with Phenobarbital.
PhenytoinThe metabolism of Cevimeline can be increased when combined with Phenytoin.
PhysostigmineThe risk or severity of adverse effects can be increased when Physostigmine is combined with Cevimeline.
PindololThe risk or severity of adverse effects can be increased when Pindolol is combined with Cevimeline.
PosaconazoleThe metabolism of Cevimeline can be decreased when combined with Posaconazole.
PractololThe risk or severity of adverse effects can be increased when Practolol is combined with Cevimeline.
PrimidoneThe metabolism of Cevimeline can be increased when combined with Primidone.
PromazineThe metabolism of Cevimeline can be decreased when combined with Promazine.
PropranololThe risk or severity of adverse effects can be increased when Propranolol is combined with Cevimeline.
PyridostigmineThe risk or severity of adverse effects can be increased when Pyridostigmine is combined with Cevimeline.
QuinidineThe metabolism of Cevimeline can be decreased when combined with Quinidine.
QuinineThe metabolism of Cevimeline can be decreased when combined with Quinine.
RanolazineThe metabolism of Cevimeline can be decreased when combined with Ranolazine.
RifabutinThe metabolism of Cevimeline can be increased when combined with Rifabutin.
RifampicinThe metabolism of Cevimeline can be increased when combined with Rifampicin.
RifapentineThe metabolism of Cevimeline can be increased when combined with Rifapentine.
RitonavirThe metabolism of Cevimeline can be decreased when combined with Ritonavir.
RivastigmineThe risk or severity of adverse effects can be increased when Rivastigmine is combined with Cevimeline.
RolapitantThe metabolism of Cevimeline can be decreased when combined with Rolapitant.
RopiniroleThe metabolism of Cevimeline can be decreased when combined with Ropinirole.
SaquinavirThe metabolism of Cevimeline can be decreased when combined with Saquinavir.
SertralineThe metabolism of Cevimeline can be decreased when combined with Sertraline.
SildenafilThe metabolism of Cevimeline can be decreased when combined with Sildenafil.
SiltuximabThe serum concentration of Cevimeline can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Cevimeline can be increased when it is combined with Simeprevir.
SotalolThe risk or severity of adverse effects can be increased when Sotalol is combined with Cevimeline.
St. John's WortThe serum concentration of Cevimeline can be decreased when it is combined with St. John&#39;s Wort.
StiripentolThe serum concentration of Cevimeline can be increased when it is combined with Stiripentol.
SulfisoxazoleThe metabolism of Cevimeline can be decreased when combined with Sulfisoxazole.
TacrineThe risk or severity of adverse effects can be increased when Tacrine is combined with Cevimeline.
TelaprevirThe metabolism of Cevimeline can be decreased when combined with Telaprevir.
TelithromycinThe metabolism of Cevimeline can be decreased when combined with Telithromycin.
TerbinafineThe metabolism of Cevimeline can be decreased when combined with Terbinafine.
ThioridazineThe metabolism of Cevimeline can be decreased when combined with Thioridazine.
TiclopidineThe metabolism of Cevimeline can be decreased when combined with Ticlopidine.
TimololThe risk or severity of adverse effects can be increased when Timolol is combined with Cevimeline.
TipranavirThe metabolism of Cevimeline can be decreased when combined with Tipranavir.
TocilizumabThe serum concentration of Cevimeline can be decreased when it is combined with Tocilizumab.
TranylcypromineThe metabolism of Cevimeline can be decreased when combined with Tranylcypromine.
TrichlorfonThe risk or severity of adverse effects can be increased when Trichlorfon is combined with Cevimeline.
TubocurarineThe risk or severity of adverse effects can be increased when Tubocurarine is combined with Cevimeline.
VenlafaxineThe metabolism of Cevimeline can be decreased when combined with Venlafaxine.
VerapamilThe metabolism of Cevimeline can be decreased when combined with Verapamil.
VoriconazoleThe metabolism of Cevimeline can be decreased when combined with Voriconazole.
ZiprasidoneThe metabolism of Cevimeline can be decreased when combined with Ziprasidone.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Receptor activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover.
Gene Name:
CHRM3
Uniprot ID:
P20309
Molecular Weight:
66127.445 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Li X, Azlina A, Karabasil MR, Purwanti N, Hasegawa T, Yao C, Akamatsu T, Hosoi K: Degradation of submandibular gland AQP5 by parasympathetic denervation of chorda tympani and its recovery by cevimeline, an M3 muscarinic receptor agonist. Am J Physiol Gastrointest Liver Physiol. 2008 Jul;295(1):G112-G123. doi: 10.1152/ajpgi.00359.2007. Epub 2008 May 1. [PubMed:18450949 ]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Phosphatidylinositol phospholipase c activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover.
Gene Name:
CHRM1
Uniprot ID:
P11229
Molecular Weight:
51420.375 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Fisher A, Heldman E, Gurwitz D, Haring R, Karton Y, Meshulam H, Pittel Z, Marciano D, Brandeis R, Sadot E, Barg Y, Pinkas-Kramarski R, Vogel Z, Ginzburg I, Treves TA, Verchovsky R, Klimowsky S, Korczyn AD: M1 agonists for the treatment of Alzheimer's disease. Novel properties and clinical update. Ann N Y Acad Sci. 1996 Jan 17;777:189-96. [PubMed:8624083 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Washio T, Arisawa H, Kohsaka K, Yasuda H: Identification of human drug-metabolizing enzymes involved in the metabolism of SNI-2011. Biol Pharm Bull. 2001 Nov;24(11):1263-6. [PubMed:11725960 ]
  2. Washio T, Kohsaka K, Arisawa H, Masunaga H: Pharmacokinetics and metabolism of the novel muscarinic receptor agonist SNI-2011 in rats and dogs. Arzneimittelforschung. 2003;53(1):26-33. [PubMed:12608011 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Washio T, Arisawa H, Kohsaka K, Yasuda H: Identification of human drug-metabolizing enzymes involved in the metabolism of SNI-2011. Biol Pharm Bull. 2001 Nov;24(11):1263-6. [PubMed:11725960 ]
  2. Washio T, Kohsaka K, Arisawa H, Masunaga H: Pharmacokinetics and metabolism of the novel muscarinic receptor agonist SNI-2011 in rats and dogs. Arzneimittelforschung. 2003;53(1):26-33. [PubMed:12608011 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Nadp binding
Specific Function:
This protein is involved in the oxidative metabolism of a variety of xenobiotics such as drugs and pesticides. Form I catalyzes the N-oxygenation of secondary and tertiary amines.
Gene Name:
FMO1
Uniprot ID:
Q01740
Molecular Weight:
60310.285 Da
References
  1. Washio T, Arisawa H, Kohsaka K, Yasuda H: Identification of human drug-metabolizing enzymes involved in the metabolism of SNI-2011. Biol Pharm Bull. 2001 Nov;24(11):1263-6. [PubMed:11725960 ]
  2. Washio T, Kohsaka K, Arisawa H, Masunaga H: Pharmacokinetics and metabolism of the novel muscarinic receptor agonist SNI-2011 in rats and dogs. Arzneimittelforschung. 2003;53(1):26-33. [PubMed:12608011 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23