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mefloquine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| quinoline derivatives | 1665 | 53230-10-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A phospholipid-interacting antimalarial drug (ANTIMALARIALS). It is very effective against PLASMODIUM FALCIPARUM with very few side effects.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 1 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 9 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 47.20 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 80 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| fu (Fraction unbound in plasma) | 0 % | Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 2.433 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 3.606 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 20.045 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 3.006 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 8.380 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 18.990 | % | High | 1 |
| herg | hERG pIC50 | 5.233 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.122 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 6.039 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 10.470 | % | High | 1 |
| kinase-safety-class | ACVR2B,AXL,BRAF,CAMK2D,CDK5,EIF2AK3,ERBB2,GRK2,ITK,JAK3,MET,NTRK2,PDK2,PDK4,PIK3CG,PRKDC,TEK | 17 | |||
| kinase-selectivity-class | AXL,EIF2AK3 | 2 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 7.379 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 10.864 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 6.760 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 19.770 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 1 | |||
| pld-class | Phospholipidosis risk class (1 = positive, 0 = negative) | 1 | High | 1 | |
| pppb | Pig plasma protein binding (% unbound) | 13.600 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 21.878 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 25.350 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 7.630 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 736.207 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| May 2, 1989 | FDA |
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 |
|---|---|---|---|---|---|---|
| Progressive multifocal leukoencephalopathy | 125.85 | 45.35 | 26 | 426 | 15629 | 90612366 |
| Immune reconstitution inflammatory syndrome | 120.33 | 45.35 | 22 | 430 | 6997 | 90620998 |
| JC virus infection | 76.45 | 45.35 | 13 | 439 | 2706 | 90625289 |
| Product use in unapproved indication | 56.18 | 45.35 | 29 | 423 | 336207 | 90291788 |
FDA Adverse Event Reporting System (Male)
| 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 |
|---|---|---|---|---|---|---|
| Progressive multifocal leukoencephalopathy | 122.91 | 58.01 | 27 | 375 | 11509 | 42609424 |
| JC virus infection | 66.91 | 58.01 | 13 | 389 | 2991 | 42617942 |
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 |
|---|---|---|---|---|---|---|
| Progressive multifocal leukoencephalopathy | 232.45 | 46.35 | 50 | 758 | 24906 | 110563585 |
| JC virus infection | 143.75 | 46.35 | 26 | 782 | 5264 | 110583227 |
| Immune reconstitution inflammatory syndrome | 131.13 | 46.35 | 29 | 779 | 16197 | 110572294 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | P01BC02 | ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS ANTIPROTOZOALS ANTIMALARIALS Methanolquinolines |
| ATC | P01BF02 | ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS ANTIPROTOZOALS ANTIMALARIALS Artemisinin and derivatives, combinations |
| FDA EPC | N0000175482 | Antimalarial |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D000962 | Antimalarials |
| MeSH PA | D000977 | Antiparasitic Agents |
| MeSH PA | D000981 | Antiprotozoal Agents |
| CHEBI has role | CHEBI:38068 | antimalarial |
| CHEBI has role | CHEBI:22587 | antiviral agent |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
| CHEBI has role | CHEBI:149553 | anticoronaviral agent |
Related Drugs by ATC class:
P01BF Artemisinin and derivatives, combinations 11 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Vivax malaria | indication | 27052006 | DOID:12978 |
| Chloroquine-Resistant Plasmodium Falciparum Malaria Prevention | indication | ||
| Chloroquine Resistant Plasmodium Falciparum Malaria | indication | ||
| Ataxia | contraindication | 20262006 | |
| Generalized anxiety disorder | contraindication | 21897009 | DOID:14320 |
| Depressive disorder | contraindication | 35489007 | |
| Sinus bradycardia | contraindication | 49710005 | |
| Schizophrenia | contraindication | 58214004 | DOID:5419 |
| Sinus node dysfunction | contraindication | 60423000 | |
| Psychotic disorder | contraindication | 69322001 | |
| Prolonged QT interval | contraindication | 111975006 | |
| Seizure disorder | contraindication | 128613002 | |
| Atrioventricular block | contraindication | 233917008 | DOID:0050820 |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Psychiatric Disturbance | 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 | 13.95 | acidic |
| pKa2 | 8.56 | Basic |
| pKa3 | 4.89 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Adenosine receptor A2a | GPCR | Ki | 6.91 | CHEMBL | |||||
| Potassium voltage-gated channel subfamily H member 2 | Ion channel | IC50 | 5.25 | WOMBAT-PK | |||||
| Multidrug resistance protein 1 | Transporter | WOMBAT-PK | |||||||
| Adenosine receptor A1 | GPCR | Ki | 5.91 | CHEMBL | |||||
| Hemoglobin subunit alpha | Secreted | WOMBAT-PK | |||||||
| Glycine receptor subunit alpha-1 | Ion channel | EC50 | 5.60 | CHEMBL | |||||
| Protein kinase Pfmrk | Kinase | IC50 | 4.92 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019811 | VUID |
| N0000147900 | NUI |
| D00831 | KEGG_DRUG |
| 51773-92-3 | SECONDARY_CAS_RN |
| 4019498 | VANDF |
| 4019811 | VANDF |
| C0025153 | UMLSCUI |
| CHEBI:63609 | CHEBI |
| CHEMBL416956 | ChEMBL_ID |
| CHEMBL535650 | ChEMBL_ID |
| DB00358 | DRUGBANK_ID |
| D015767 | MESH_DESCRIPTOR_UI |
| 4046 | PUBCHEM_CID |
| 4252 | IUPHAR_LIGAND_ID |
| 3777 | INN_ID |
| TML814419R | UNII |
| 202989 | RXNORM |
| 1710 | MMSL |
| 43453 | MMSL |
| 5035 | MMSL |
| d00286 | MMSL |
| 003537 | NDDF |
| 004873 | NDDF |
| 387505001 | SNOMEDCT_US |
| 412243001 | SNOMEDCT_US |
| 87567009 | SNOMEDCT_US |
| A1A1V | PDB_CHEM_ID |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Mefloquine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0555-0171 | TABLET | 250 mg | ORAL | ANDA | 23 sections |
| Mefloquine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 21695-449 | TABLET | 250 mg | ORAL | ANDA | 23 sections |
| Mefloquine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 21695-561 | TABLET | 250 mg | ORAL | ANDA | 26 sections |
| Mefloquine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50090-2396 | TABLET | 250 mg | ORAL | ANDA | 23 sections |
| Mefloquine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 52959-803 | TABLET | 250 mg | ORAL | ANDA | 26 sections |
| Mefloquine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-5434 | TABLET | 250 mg | ORAL | ANDA | 13 sections |
| Mefloquine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 62135-973 | TABLET | 250 mg | ORAL | ANDA | 16 sections |