cevimeline Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
cholinergic agents (muscarine receptor agonists/partial antagonists used in the treatment of Alzheimer's disease) 584 107233-08-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • cevimeline hydrochloride hydrate
  • cevimeline
  • cevimeline hydrochloride
  • evoxac
  • cevimeline HCl
  • cevimeline hydrochloride hemihydrate
Cevimeline 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.
  • Molecular weight: 199.31
  • Formula: C10H17NOS
  • CLOGP: 1.14
  • LIPINSKI: 0
  • HAC: 2
  • HDO: 0
  • TPSA: 12.47
  • ALOGS: -1.92
  • ROTB: 0

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
90 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 13.50 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 15.05 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Approvals:

DateAgencyCompanyOrphan
Jan. 11, 2000 FDA DAIICHI SANKYO

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Dry mouth 23 19.58 19 1994 54907 46629142

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event

Pharmacologic Action:

SourceCodeDescription
ATC N07AX03 NERVOUS SYSTEM
OTHER NERVOUS SYSTEM DRUGS
PARASYMPATHOMIMETICS
Other parasympathomimetics
FDA MoA N0000000104 Cholinergic Muscarinic Agonists
CHEBI has role CHEBI:38325 muscarinic agonists
MeSH PA D018678 Cholinergic Agents
MeSH PA D018679 Cholinergic Agonists
MeSH PA D018721 Muscarinic Agonists
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D010277 Parasympathomimetics
MeSH PA D018373 Peripheral Nervous System Agents
FDA EPC N0000175884 Cholinergic Receptor Agonist

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Xerostomia Secondary to Sjogren's Syndrome indication
Renal colic contraindication 7093002
Reduced visual acuity contraindication 13164000
Myocardial infarction contraindication 22298006 DOID:5844
Conduction disorder of the heart contraindication 44808001
Chronic bronchitis contraindication 63480004 DOID:6132
Iritis contraindication 65074000 DOID:1406
Night blindness contraindication 65194006 DOID:8499
Cholecystitis contraindication 76581006 DOID:1949
Cholangitis contraindication 82403002 DOID:9446
Kidney stone contraindication 95570007
Angina pectoris contraindication 194828000
Asthma contraindication 195967001 DOID:2841
Calculus in biliary tract contraindication 266474003
Exacerbation of asthma contraindication 281239006
Severe chronic obstructive pulmonary disease contraindication 313299006
Non-Q wave myocardial infarction contraindication 314207007
Angle-closure glaucoma contraindication 392291006 DOID:13550
Breastfeeding (mother) contraindication 413712001
Acute exacerbation of asthma contraindication 708038006
Ureteral Spasm contraindication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 6.73 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Muscarinic acetylcholine receptor M3 GPCR AGONIST EC50 7.32 WOMBAT-PK CHEMBL
Muscarinic acetylcholine receptor M1 GPCR AGONIST EC50 7.64 WOMBAT-PK CHEMBL
Muscarinic acetylcholine receptor M5 GPCR EC50 7.20 WOMBAT-PK
Muscarinic acetylcholine receptor M4 GPCR EC50 5.88 WOMBAT-PK
Muscarinic acetylcholine receptor M2 GPCR EC50 5.98 WOMBAT-PK

External reference:

IDSource
4021212 VUID
N0000148658 NUI
D00661 KEGG_DRUG
153504-70-2 SECONDARY_CAS_RN
4021212 VANDF
C0093437 UMLSCUI
CHEBI:3568 CHEBI
CHEMBL168815 ChEMBL_ID
CHEMBL2218917 ChEMBL_ID
DB00185 DRUGBANK_ID
C059240 MESH_SUPPLEMENTAL_RECORD_UI
2684 PUBCHEM_CID
9658 IUPHAR_LIGAND_ID
7540 INN_ID
K9V0CDQ56E UNII
260036 RXNORM
193848 MMSL
31752 MMSL
8641 MMSL
d04512 MMSL
008105 NDDF
008106 NDDF
116345005 SNOMEDCT_US
409284005 SNOMEDCT_US
409285006 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Cevimeline Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0054-0334 CAPSULE 30 mg ORAL ANDA 17 sections
Cevimeline Hydrochloride Human Prescription Drug Label 1 16571-657 CAPSULE 30 mg ORAL ANDA 23 sections
EVOXAC HUMAN PRESCRIPTION DRUG LABEL 1 16590-859 CAPSULE 30 mg ORAL NDA 11 sections
cevimeline hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 40032-999 CAPSULE 30 mg ORAL ANDA 20 sections
cevimeline hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 43386-999 CAPSULE 30 mg ORAL ANDA 20 sections
Cevimeline HUMAN PRESCRIPTION DRUG LABEL 1 63304-479 CAPSULE 30 mg ORAL NDA 12 sections
Evoxac HUMAN PRESCRIPTION DRUG LABEL 1 63395-201 CAPSULE 30 mg ORAL NDA 12 sections