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

Stem definition	Drug id	CAS RN
antiparasitics, ivermectin derivatives	3972	70288-86-7

Description:

Molecule

Description

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:

Dose	Unit	Route
12	mg	O

ADMET properties:

Property	Value	Reference
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 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Approvals:

Date	Agency	Company	Orphan
Nov. 22, 1996	FDA	MERCK SHARP DOHME

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

Pharmacologic Action:

Source	Code	Description
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)

Disease	Relation	SNOMED_ID	DOID
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 strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent 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 strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
1%	IVERMECTIN	TEVA PHARMS USA	A210019	Sept. 13, 2019	RX	CREAM	TOPICAL	April 11, 2020	PATENT CHALLENGE

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	5.66		DRUG MATRIX
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN		Ki	5.41		DRUG MATRIX
D(3) dopamine receptor	GPCR	P35462	DRD3_HUMAN		Ki	6.12		DRUG MATRIX
Muscarinic acetylcholine receptor M1	GPCR	P11229	ACM1_HUMAN		Ki	5.92		DRUG MATRIX
Muscarinic acetylcholine receptor M3	GPCR	P20309	ACM3_HUMAN		Ki	5.89		DRUG MATRIX
Muscarinic acetylcholine receptor M5	GPCR	P08912	ACM5_HUMAN		Ki	5.59		DRUG MATRIX
Alpha-2C adrenergic receptor	GPCR	P18825	ADA2C_HUMAN		Ki	6.24		DRUG MATRIX
Sodium-dependent dopamine transporter	Transporter	Q01959	SC6A3_HUMAN		Ki	5.45		DRUG MATRIX
Adenosine receptor A3	GPCR	P0DMS8	AA3R_HUMAN		Ki	6.54		DRUG MATRIX
Multidrug resistance protein 1	Transporter	P08183	MDR1_HUMAN		IC50	7		WOMBAT-PK
Neuronal acetylcholine receptor subunit alpha-7	Ion channel	P36544	ACHA7_HUMAN	ALLOSTERIC MODULATOR	EC50	5.10		IUPHAR
Glycine Receptor	Ion channel	O75311 P23415 P23416 P48167	GLRA1_HUMAN GLRA2_HUMAN GLRA3_HUMAN GLRB_HUMAN	AGONIST	EC50	6.40		IUPHAR
Bile acid receptor	Nuclear hormone receptor	Q96RI1	NR1H4_HUMAN		IC50	6.59		CHEMBL
D(1A) dopamine receptor	GPCR	P21728	DRD1_HUMAN		Ki	5.65		DRUG MATRIX
Glutamate-gated chloride channel	Ion channel		GLUCB_HAECO	MODULATOR				CHEMBL	CHEMBL
Glutamate-gated chloride channel	Ion channel		Q25634_ONCVO	MODULATOR				CHEMBL	CHEMBL
Sodium/potassium-transporting ATPase subunit alpha-1	Unclassified		AT1A1_RAT		IC50	5.08		CHEMBL
Sarcoplasmic/endoplasmic reticulum calcium ATPase 2	Unclassified		AT2A2_RAT		IC50	5.17		CHEMBL
Sarcoplasmic/endoplasmic reticulum calcium ATPase 1	Unclassified		AT2A1_RAT		IC50	4.77		CHEMBL
SARS-CoV-2	Virus			INHIBITOR	IC50	5.69		SCIENTIFIC LITERATURE
P2X purinoceptor 4	Unclassified		P2RX4_RAT	ALLOSTERIC MODULATOR	EC50	6.60		IUPHAR

External reference:

ID	Source
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:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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