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cevimeline 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| cholinergic agents (muscarine receptor agonists/partial antagonists used in the treatment of Alzheimer's disease) | 584 | 107233-08-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 90 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| 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 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | -0.520 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 1.683 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 1.849 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 1.439 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 92.870 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 85.140 | % | High | 1 |
| herg | hERG pIC50 | 4.168 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.538 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.767 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 94.690 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,MAP3K21,MAPK7,MET,NTRK2,PDK2,PDK4,PIM2,PRKDC,SIK2,TEK,TGFBR1 | 27 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.865 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 4.955 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 96.310 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 1.315 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 94.900 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 4.256 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 84.180 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 95.040 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 864.968 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 11, 2000 | FDA | DAIICHI SANKYO |
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 |
|---|---|---|---|---|---|---|
| Headache | 25.16 | 18.83 | 78 | 3189 | 862668 | 89762512 |
| Product dose omission issue | 21.45 | 18.83 | 38 | 3229 | 291649 | 90333531 |
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 |
|---|---|---|---|---|---|---|
| Headache | 22.46 | 20.49 | 56 | 2414 | 882321 | 109704508 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N07AX03 | NERVOUS SYSTEM OTHER NERVOUS SYSTEM DRUGS PARASYMPATHOMIMETICS Other parasympathomimetics |
| FDA MoA | N0000000104 | Cholinergic Muscarinic Agonists |
| CHEBI has role | CHEBI:38325 | muscarinic agonist |
| MeSH PA | D010277 | Parasympathomimetics |
| MeSH PA | D018373 | Peripheral Nervous System Agents |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018678 | Cholinergic Agents |
| MeSH PA | D018679 | Cholinergic Agonists |
| MeSH PA | D018721 | Muscarinic Agonists |
| FDA EPC | N0000175884 | Cholinergic Receptor Agonist |
Related Drugs by ATC class:
N07AX Other parasympathomimetics 2 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| 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 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 6.73 | Basic |
Orange Book patent data (new drug applications)
None
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 |
|---|---|---|---|---|---|---|---|---|---|
| Muscarinic acetylcholine receptor M1 | GPCR | AGONIST | EC50 | 7.64 | WOMBAT-PK | CHEMBL | |||
| Muscarinic acetylcholine receptor M3 | GPCR | AGONIST | EC50 | 7.32 | WOMBAT-PK | CHEMBL | |||
| Muscarinic acetylcholine receptor M2 | GPCR | EC50 | 5.98 | WOMBAT-PK | |||||
| Muscarinic acetylcholine receptor M4 | GPCR | EC50 | 5.88 | WOMBAT-PK | |||||
| Muscarinic acetylcholine receptor M5 | GPCR | EC50 | 7.20 | WOMBAT-PK |
External reference:
| ID | Source |
|---|---|
| 4021212 | VUID |
| N0000148658 | NUI |
| D00661 | KEGG_DRUG |
| 153504-70-2 | SECONDARY_CAS_RN |
| 260036 | RXNORM |
| C0093437 | UMLSCUI |
| CHEBI:3568 | CHEBI |
| CHEMBL168815 | ChEMBL_ID |
| DB00185 | DRUGBANK_ID |
| CHEMBL2218917 | ChEMBL_ID |
| 25137844 | PUBCHEM_CID |
| C059240 | MESH_SUPPLEMENTAL_RECORD_UI |
| 9658 | IUPHAR_LIGAND_ID |
| 7540 | INN_ID |
| K9V0CDQ56E | UNII |
| 193848 | MMSL |
| 31752 | MMSL |
| 8641 | MMSL |
| d04512 | MMSL |
| 008105 | NDDF |
| 008106 | NDDF |
| 116345005 | SNOMEDCT_US |
| 409284005 | SNOMEDCT_US |
| 409285006 | SNOMEDCT_US |
| 4021212 | VANDF |
| K9V0CDQ56E | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Cevimeline Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0054-0334 | CAPSULE | 30 mg | ORAL | ANDA | 17 sections |
| Evoxac | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0713-0883 | CAPSULE | 30 mg | ORAL | NDA | 11 sections |
| cevimeline hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0713-0937 | CAPSULE | 30 mg | ORAL | NDA | 11 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 | 33342-216 | CAPSULE | 30 mg | ORAL | ANDA | 19 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 Hydrochloride | Human Prescription Drug Label | 1 | 59651-422 | CAPSULE | 30 mg | ORAL | ANDA | 17 sections |
| Cevimeline | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63304-479 | CAPSULE | 30 mg | ORAL | NDA | 12 sections |
| Cevimeline Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63629-9863 | CAPSULE | 30 mg | ORAL | ANDA | 23 sections |
| CEVIMELINE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69452-316 | CAPSULE | 30 mg | ORAL | ANDA | 11 sections |
| Cevimeline Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70771-1982 | CAPSULE | 30 mg | ORAL | ANDA | 2 sections |
| Cevimeline Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71335-2264 | CAPSULE | 30 mg | ORAL | ANDA | 17 sections |
| CEVIMELINE HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71335-2326 | CAPSULE | 30 mg | ORAL | ANDA | 11 sections |
| Cevimeline Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72162-2563 | CAPSULE | 30 mg | ORAL | ANDA | 17 sections |
| Cevimeline Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72578-208 | CAPSULE | 30 mg | ORAL | ANDA | 17 sections |
| CEVIMELINE HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72789-457 | CAPSULE | 30 mg | ORAL | ANDA | 11 sections |
| CEVIMELINE HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72789-457 | CAPSULE | 30 mg | ORAL | ANDA | 11 sections |
| CEVIMELINE HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72888-118 | CAPSULE | 30 mg | ORAL | ANDA | 11 sections |
| Cevimeline Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 87063-180 | CAPSULE | 30 mg | ORAL | ANDA | 23 sections |