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levamisole 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 1561 | 14769-73-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An antihelminthic drug that has been tried experimentally in rheumatic disorders where it apparently restores the immune response by increasing macrophage chemotaxis and T-lymphocyte function. Paradoxically, this immune enhancement appears to be beneficial in rheumatoid arthritis where dermatitis, leukopenia, and thrombocytopenia, and nausea and vomiting have been reported as side effects. (From Smith and Reynard, Textbook of Pharmacology, 1991, p435-6)
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.15 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 4.08 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 65 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 1.170 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 1.422 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 14.488 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 2.208 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 76.270 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 79.170 | % | High | 1 |
| herg | hERG pIC50 | 4.860 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.096 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.690 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 74.870 | % | High | 1 |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 3.177 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 3.540 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 63.470 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 7.063 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 88.330 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 4.842 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 86.620 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 66.820 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 907.821 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| June 18, 1990 | 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 |
|---|---|---|---|---|---|---|
| Substance use disorder | 181.77 | 93.21 | 26 | 382 | 1994 | 90626045 |
| Toxicity to various agents | 167.92 | 93.21 | 58 | 350 | 287788 | 90340251 |
| Drug use disorder | 144.92 | 93.21 | 26 | 382 | 8317 | 90619722 |
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 |
|---|---|---|---|---|---|---|
| Toxicity to various agents | 360.65 | 83.33 | 157 | 1042 | 228979 | 42391157 |
| Adulterated product | 216.88 | 83.33 | 34 | 1165 | 732 | 42619404 |
| Drug abuse | 210.02 | 83.33 | 86 | 1113 | 104685 | 42515451 |
| Substance use disorder | 184.16 | 83.33 | 40 | 1159 | 5305 | 42614831 |
| Drug use disorder | 157.93 | 83.33 | 40 | 1159 | 10293 | 42609843 |
| Accidental death | 145.85 | 83.33 | 30 | 1169 | 3053 | 42617083 |
| Asphyxia | 106.50 | 83.33 | 28 | 1171 | 8298 | 42611838 |
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 |
|---|---|---|---|---|---|---|
| Toxicity to various agents | 501.35 | 78.04 | 203 | 1398 | 480352 | 110107346 |
| Substance use disorder | 360.41 | 78.04 | 66 | 1535 | 7224 | 110580474 |
| Drug use disorder | 300.64 | 78.04 | 66 | 1535 | 18008 | 110569690 |
| Drug abuse | 290.55 | 78.04 | 105 | 1496 | 177306 | 110410392 |
| Adulterated product | 263.93 | 78.04 | 39 | 1562 | 1116 | 110586582 |
| Accidental death | 181.73 | 78.04 | 35 | 1566 | 4974 | 110582724 |
| Miosis | 111.56 | 78.04 | 31 | 1570 | 21952 | 110565746 |
| Asphyxia | 110.02 | 78.04 | 28 | 1573 | 14187 | 110573511 |
| Overdose | 83.31 | 78.04 | 48 | 1553 | 233746 | 110353952 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | P02CE01 | ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS ANTHELMINTICS ANTINEMATODAL AGENTS Imidazothiazole derivatives |
| MeSH PA | D000276 | Adjuvants, Immunologic |
| MeSH PA | D000871 | Anthelmintics |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D000969 | Antinematodal Agents |
| MeSH PA | D000977 | Antiparasitic Agents |
| MeSH PA | D007155 | Immunologic Factors |
| MeSH PA | D018501 | Antirheumatic Agents |
| CHEBI has role | CHEBI:35444 | antinematodal drug |
| CHEBI has role | CHEBI:35842 | antirheumatic drug |
| CHEBI has role | CHEBI:50846 | immunomodulator |
| CHEBI has role | CHEBI:50847 | immunological adjuvant |
| CHEBI has role | CHEBI:63332 | EC 3.1.3.1 (alkaline phosphatase) inhibitor |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Ascariasis | indication | 2435008 | DOID:456 |
| Ancylostomiasis | indication | 63479002 | DOID:12841 |
🐶 Veterinary Drug Use
| Species | Use | Relation |
|---|---|---|
| Cattle | Nematode infections, removal of stomach worms, Haemonchus | Indication |
| Cattle | Nematode infections, removal of intestinal worms, Trichostrongylus | Indication |
| Cattle | Nematode infections, removal of lungworms, Dictyocaulus | Indication |
| Cattle | Nematode infections, removal of intestinal worms, Cooperia | Indication |
| Cattle | Nematode infections, removal of intestinal worms, Nematodirus | Indication |
| Cattle | Nematode infections, removal of intestinal worms, Bunostomum | Indication |
| Cattle | Nematode infections, removal of intestinal worms, Oesophagostomum | Indication |
| Cattle | Nematode infections, removal of stomach worms, Trichostrongylus | Indication |
| Cattle | Nematode infections, removal of stomach worms, Ostertagia | Indication |
| Sheep | Nematode infections, removal of stomach worms, Haemonchus | Indication |
| Sheep | Nematode infections, removal of intestinal worms, Trichostrongylus | Indication |
| Sheep | Nematode infections, removal of lungworms, Dictyocaulus | Indication |
| Sheep | Nematode infections, removal of intestinal worms, Cooperia | Indication |
| Sheep | Nematode infections, removal of intestinal worms, Nematodirus | Indication |
| Sheep | Nematode infections, removal of intestinal worms, Bunostomum | Indication |
| Sheep | Nematode infections, removal of intestinal worms, Oesophagostomum | Indication |
| Sheep | Nematode infections, removal of stomach worms, Trichostrongylus | Indication |
| Sheep | Nematode infections, removal of stomach worms, Ostertagia | Indication |
| Swine | Nematode infections, removal of large roundworms, Ascaris suum | Indication |
| Swine | Nematode infections, removal of nodular worms, Oesophagostomum species | Indication |
| Swine | Nematode infections, removal of lungworms, Metastrongylus species | Indication |
| Swine | Nematode infections, removal of intestinal threadworms, Strongyloides ransomi | Indication |
| Swine | Nematode infections, removal of kidney worms, Stephanurus dentatus | Indication |
🐶 Veterinary products
| Product | Applicant | Ingredients |
|---|---|---|
| Ripercol L Bolus, Tramisol Cattle Wormer Bolus | Zoetis Inc. | 1 |
| Ripercol L Soluble Drench Powder | Zoetis Inc. | 1 |
| Ripercol L, Tramisol Soluble Drench Powder for Sheep | Zoetis Inc. | 1 |
| Ripercol L Wormer Oblets, Tramisol Sheep Wormer Oblets | Zoetis Inc. | 1 |
| Ripercol L | Zoetis Inc. | 1 |
| Ripercol L | Zoetis Inc. | 1 |
| Levasole Cattle Wormer Bolus | Intervet Inc. | 1 |
| Ripercol L-Piperazine Soluble | Zoetis Inc. | 2 |
| Ripercol L-Piperazine | Zoetis Inc. | 2 |
| Tramisol Injectable Solution | Zoetis Inc. | 1 |
| Tramisol | Zoetis Inc. | 1 |
| Levasole Soluble Pig Wormer | Intervet Inc. | 1 |
| Levasole | Intervet Inc. | 1 |
| Levamisole Soluble Drench Powder, Levasole, Levasole Soluble Drench Powder, Tramisol Soluble Drench Powder | Intervet Inc. | 1 |
| Levasole Sheep Wormer Bolus, Tramisole Sheep Wormer Oblets Tablets | Intervet Inc. | 1 |
| Tramisol Gel | Zoetis Inc. | 1 |
| Levasole Injectable Solution | Intervet Inc. | 1 |
| Tramisol-X-Tra Cattle Anthelmintic and Extoparasitic Paste | Intervet Inc. | 2 |
| Totalon Topical Cattle Anthelmintic | Intervet Inc. | 1 |
| Tramisol Pour-On | Zoetis Inc. | 1 |
| Prohibit Soluble Drench Powder | Huvepharma EOOD | 1 |
| Levamisole Phosphate | Huvepharma EOOD | 1 |
| LevaMed | Bimeda Animal Health Limited | 1 |
| LevaMed Soluble Drench Powder | Bimeda Animal Health Limited | 1 |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.2 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Alkaline phosphatase, tissue-nonspecific isozyme | Enzyme | Ki | 4.80 | CHEMBL | |||||
| Intestinal-type alkaline phosphatase | Enzyme | IC50 | 4.69 | CHEMBL | |||||
| Nicotinic acetylcholine receptor alpha subunit | Ion channel | AGONIST | CHEMBL | CHEMBL | |||||
| Acetylcholine receptor subunit alpha-type unc-63 | Ion channel | WOMBAT-PK | |||||||
| Membrane-associated progesterone receptor component 1 | Membrane receptor | Ki | 5.57 | DRUG MATRIX | |||||
| Alkaline phosphatase, tissue-nonspecific isozyme | Enzyme | IC50 | 4.72 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D00750 | KEGG_DRUG |
| 16595-80-5 | SECONDARY_CAS_RN |
| 5036-02-2 | SECONDARY_CAS_RN |
| 4019531 | VANDF |
| C0023556 | UMLSCUI |
| CHEBI:6432 | CHEBI |
| CHEMBL1454 | ChEMBL_ID |
| DB00848 | DRUGBANK_ID |
| CHEMBL1770 | ChEMBL_ID |
| CHEMBL277775 | ChEMBL_ID |
| D007978 | MESH_DESCRIPTOR_UI |
| 26879 | PUBCHEM_CID |
| 7210 | IUPHAR_LIGAND_ID |
| 2643 | INN_ID |
| 5086-74-8 | SECONDARY_CAS_RN |
| 2880D3468G | UNII |
| DB16561 | DRUGBANK_ID |
| 1535214 | RXNORM |
| 4967 | MMSL |
| d00276 | MMSL |
| 003546 | NDDF |
| 004809 | NDDF |
| 387296006 | SNOMEDCT_US |
| 54391004 | SNOMEDCT_US |
| 81365005 | SNOMEDCT_US |
| 96118005 | SNOMEDCT_US |
| D013773 | MESH_DESCRIPTOR_UI |
| CHEMBL554891 | ChEMBL_ID |
| 32093-35-9 | SECONDARY_CAS_RN |
| 1973 | INN_ID |
Pharmaceutical products:
None