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

Stem definitionDrug idCAS RN
antiparasitics, ivermectin derivatives 3972 70288-86-7

Description:

MoleculeDescription

Synonyms:

  • ivermectin
  • noramectin
  • noromectin
  • zimecterin
A mixture of mostly avermectin H2B1a (RN 71827-03-7) with some avermectin H2B1b (RN 70209-81-3), which are macrolides from STREPTOMYCES avermitilis. It binds glutamate-gated chloride channel to cause increased permeability and hyperpolarization of nerve and muscle cells. It also interacts with other CHLORIDE CHANNELS. It is a broad spectrum antiparasitic that is active against microfilariae of ONCHOCERCA VOLVULUS but not the adult form.
  • Molecular weight: 1736.19
  • Formula: C95H146O28
  • CLOGP:
  • LIPINSKI: None
  • HAC: None
  • HDO: None
  • TPSA:
  • ALOGS:
  • ROTB: None

Drug dosage:

DoseUnitRoute
12 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 4 mg/mL Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.17 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Approvals:

DateAgencyCompanyOrphan
Nov. 22, 1996 FDA MERCK SHARP DOHME

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
Erythema 175.39 71.20 44 184 25115 2332742
Skin irritation 127.78 71.20 21 207 1364 2356493
Skin burning sensation 100.42 71.20 18 210 1938 2355919
Drug ineffective 76.04 71.20 33 195 101591 2256266
Dermatitis contact 71.90 71.20 13 215 1453 2356404

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
Asthenia 67.22 61.86 23 127 34647 1711984
Coma 65.35 61.86 16 134 7246 1739385

Pharmacologic Action:

SourceCodeDescription
ATC D11AX22 DERMATOLOGICALS
OTHER DERMATOLOGICAL PREPARATIONS
OTHER DERMATOLOGICAL PREPARATIONS
Other dermatologicals
ATC P02CF01 ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS
ANTHELMINTICS
ANTINEMATODAL AGENTS
Avermectines
FDA EPC N0000175484 Antiparasitic
FDA EPC N0000181811 Pediculicide
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000977 Antiparasitic Agents
MeSH PA D007306 Insecticides
MeSH PA D010575 Pesticides
CHEBI has role CHEBI:73333 scabicide
CHEBI has role CHEBI:35443 anthelminthic drug
CHEBI has role CHEBI:35820 antiprotozoal drug
CHEBI has role CHEBI:35444 antinematodal drug
CHEBI has role CHEBI:24852 insecticide

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Infection by Strongyloides indication 1214006 DOID:10955
Infection by Onchocerca volvulus indication 38539003 DOID:11678
Infection by Loa loa contraindication 44250009 DOID:13523
Liver function tests abnormal contraindication 166603001

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
1% SOOLANTRA GALDERMA LABS LP N206255 Dec. 19, 2014 RX CREAM TOPICAL 7550440 April 22, 2024 TREATMENT OF INFLAMMATORY LESIONS OF ROSACEA.
1% SOOLANTRA GALDERMA LABS LP N206255 Dec. 19, 2014 RX CREAM TOPICAL 8080530 April 22, 2024 TREATMENT OF INFLAMMATORY LESIONS OF ROSACEA.
1% SOOLANTRA GALDERMA LABS LP N206255 Dec. 19, 2014 RX CREAM TOPICAL 8093219 April 22, 2024 TREATMENT OF INFLAMMATORY LESIONS OF ROSACEA.
1% SOOLANTRA GALDERMA LABS LP N206255 Dec. 19, 2014 RX CREAM TOPICAL 8415311 April 22, 2024 TREATMENT OF INFLAMMATORY LESIONS OF ROSACEA.
1% SOOLANTRA GALDERMA LABS LP N206255 Dec. 19, 2014 RX CREAM TOPICAL 8470788 April 22, 2024 TREATMENT OF INFLAMMATORY LESIONS OF ROSACEA.
1% SOOLANTRA GALDERMA LABS LP N206255 Dec. 19, 2014 RX CREAM TOPICAL 8815816 April 22, 2024 TREATMENT OF INFLAMMATORY LESIONS OF ROSACEA.
0.5% SKLICE ARBOR PHARMS LLC N202736 Feb. 7, 2012 RX LOTION TOPICAL 8927595 Oct. 12, 2027 FOR HEAD LICE INFESTATIONS
1% SOOLANTRA GALDERMA LABS LP N206255 Dec. 19, 2014 RX CREAM TOPICAL 10206939 March 13, 2034 TREATMENT OF INFLAMMATORY LESIONS OF ROSACEA.
1% SOOLANTRA GALDERMA LABS LP N206255 Dec. 19, 2014 RX CREAM TOPICAL 9089587 March 13, 2034 TREATMENT OF INFLAMMATORY LESIONS OF ROSACEA.
1% SOOLANTRA GALDERMA LABS LP N206255 Dec. 19, 2014 RX CREAM TOPICAL 9233117 March 13, 2034 TREATMENT OF INFLAMMATORY LESIONS OF ROSACEA.
1% SOOLANTRA GALDERMA LABS LP N206255 Dec. 19, 2014 RX CREAM TOPICAL 9233118 March 13, 2034 TREATMENT OF INFLAMMATORY LESIONS OF ROSACEA.
1% SOOLANTRA GALDERMA LABS LP N206255 Dec. 19, 2014 RX CREAM TOPICAL 9782425 March 13, 2034 TREATMENT OF INFLAMMATORY LESIONS OF ROSACEA.

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
1% IVERMECTIN TEVA PHARMS USA A210019 Sept. 13, 2019 RX CREAM TOPICAL April 11, 2020 PATENT CHALLENGE

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Alpha-2A adrenergic receptor GPCR Ki 5.66 DRUG MATRIX
Sodium-dependent noradrenaline transporter Transporter Ki 5.41 DRUG MATRIX
D(3) dopamine receptor GPCR Ki 6.12 DRUG MATRIX
Muscarinic acetylcholine receptor M1 GPCR Ki 5.92 DRUG MATRIX
Muscarinic acetylcholine receptor M3 GPCR Ki 5.89 DRUG MATRIX
Muscarinic acetylcholine receptor M5 GPCR Ki 5.59 DRUG MATRIX
Alpha-2C adrenergic receptor GPCR Ki 6.24 DRUG MATRIX
Sodium-dependent dopamine transporter Transporter Ki 5.45 DRUG MATRIX
Adenosine receptor A3 GPCR Ki 6.54 DRUG MATRIX
Multidrug resistance protein 1 Transporter IC50 7 WOMBAT-PK
Neuronal acetylcholine receptor subunit alpha-7 Ion channel ALLOSTERIC MODULATOR EC50 5.10 IUPHAR
Glycine Receptor Ion channel AGONIST EC50 6.40 IUPHAR
Bile acid receptor Nuclear hormone receptor IC50 6.59 CHEMBL
D(1A) dopamine receptor GPCR Ki 5.65 DRUG MATRIX
Glutamate-gated chloride channel Ion channel MODULATOR CHEMBL CHEMBL
Glutamate-gated chloride channel Ion channel MODULATOR CHEMBL CHEMBL
Sodium/potassium-transporting ATPase subunit alpha-1 Unclassified IC50 5.08 CHEMBL
Sarcoplasmic/endoplasmic reticulum calcium ATPase 2 Unclassified IC50 5.17 CHEMBL
Sarcoplasmic/endoplasmic reticulum calcium ATPase 1 Unclassified IC50 4.77 CHEMBL
SARS-CoV-2 Virus INHIBITOR IC50 5.69 SCIENTIFIC LITERATURE
P2X purinoceptor 4 Unclassified ALLOSTERIC MODULATOR EC50 6.60 IUPHAR

External reference:

IDSource
D007559 MESH_DESCRIPTOR_UI
4021046 VUID
N0000148510 NUI
C0022322 UMLSCUI
D00804 KEGG_DRUG
96138006 SNOMEDCT_US
6069 RXNORM
387559003 SNOMEDCT_US
4941 MMSL
d04101 MMSL
4021046 VANDF
71965 MMSL
005266 NDDF
8883YP2R6D UNII
4828 INN_ID
DB00602 DRUGBANK_ID
CHEMBL1200633 ChEMBL_ID
IVM PDB_CHEM_ID
CHEBI:6078 CHEBI
6321424 PUBCHEM_CID
2373 IUPHAR_LIGAND_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
STROMECTOL HUMAN PRESCRIPTION DRUG LABEL 1 0006-0032 TABLET 3 mg ORAL NDA 12 sections
SOOLANTRA HUMAN PRESCRIPTION DRUG LABEL 1 0299-3823 CREAM 10 mg TOPICAL NDA 16 sections
Ivermectin HUMAN PRESCRIPTION DRUG LABEL 1 0591-4052 CREAM 10 mg TOPICAL ANDA 16 sections
Sklice HUMAN PRESCRIPTION DRUG LABEL 1 24338-183 LOTION 5 mg TOPICAL NDA 17 sections
Ivermectin HUMAN PRESCRIPTION DRUG LABEL 1 42799-806 TABLET 3 mg ORAL ANDA 12 sections
STROMECTOL HUMAN PRESCRIPTION DRUG LABEL 1 55695-019 TABLET 3 mg ORAL NDA 11 sections
Ivermectin HUMAN PRESCRIPTION DRUG LABEL 1 63629-7275 TABLET 3 mg ORAL ANDA 12 sections
Ivermectin HUMAN PRESCRIPTION DRUG LABEL 1 66993-948 CREAM 10 mg TOPICAL NDA authorized generic 16 sections
BRIMONIDINE TARTRATE 0.25% / IVERMECTIN 1% / METRONIDAZOLE 1% / NIACINAMIDE 4% HUMAN PRESCRIPTION DRUG LABEL 4 72934-1028 GEL 1 g TOPICAL unapproved drug other 4 sections
IVERMECTIN 1% / METRONIDAZOLE 1% HUMAN PRESCRIPTION DRUG LABEL 2 72934-1130 GEL 1 g TOPICAL unapproved drug other 4 sections
IVERMECTIN 1% / METRONIDAZOLE 1% / NIACINAMIDE 4% HUMAN PRESCRIPTION DRUG LABEL 3 72934-1131 GEL 1 g TOPICAL unapproved drug other 4 sections
Ivermectin HUMAN PRESCRIPTION DRUG LABEL 1 76413-155 TABLET 3 mg ORAL ANDA 12 sections